What is baclofen and how does it work. What are the primary uses of baclofen. How is baclofen administered and what are the dosage guidelines. What are the potential risks and precautions associated with baclofen use. How should baclofen therapy be monitored and adjusted over time.

Understanding Baclofen: Classification and Chemical Properties

Baclofen is a GABA-derivative skeletal muscle relaxant and antispastic agent. Its chemical name is 4-Amino-3-(4-chlorophenyl)-butanoic acid, with the molecular formula C10H12ClNO2. Baclofen is known by various brand names, including Gablofen and Lioresal.

To better understand the nature of this medication:

• Chemical class: GABA-derivative
• Therapeutic class: Skeletal Muscle Relaxants
• CAS Number: 1134-47-0

Baclofen’s unique chemical structure allows it to interact with GABA receptors in the central nervous system, which contributes to its muscle-relaxing and antispastic effects.

Primary Therapeutic Applications of Baclofen

Baclofen is primarily used to manage spasticity associated with various neurological conditions. Its applications include:

Oral Baclofen for Spasticity Management

Oral baclofen is indicated for the management of spasticity and its sequelae secondary to severe chronic disorders such as multiple sclerosis and other types of spinal cord lesions. It’s important to note that oral baclofen is not recommended for patients with rheumatic disorders, stroke, cerebral palsy, or Parkinson’s disease due to limited efficacy data in these populations.

Intrathecal Baclofen Therapy

Intrathecal baclofen administration is used in cases where oral therapy is ineffective or poorly tolerated. It’s particularly useful for:

• Severe spasticity of spinal cord origin
• Intractable spasticity secondary to multiple sclerosis, spinal ischemia, spinal tumors, transverse myelitis, cervical spondylosis, and degenerative myelopathy
• Severe spasticity of cerebral origin, including cerebral palsy and acquired brain injury

Intrathecal baclofen is often considered an alternative to destructive neurosurgical procedures, providing a reversible method of managing severe spasticity.

Baclofen Administration: Routes and Guidelines

The administration of baclofen requires careful consideration of the route, dosage, and individual patient factors. Here are the key points regarding baclofen administration:

Routes of Administration

Baclofen can be administered through two primary routes:

1. Oral administration: Tablets or liquid formulation
2. Intrathecal administration: Direct delivery into the spinal fluid via an implanted pump

It’s crucial to note that baclofen injection for intrathecal use should never be administered intravenously, intramuscularly, subcutaneously, or epidurally due to the risk of severe adverse effects.

Dosage Guidelines

The dosage of baclofen must be carefully individualized based on the patient’s specific requirements and response. The general principle is to use the lowest effective dose that produces an optimal response while minimizing side effects.

For oral administration:

• Start with a low dose and gradually increase
• Some patients may require 1-2 months of treatment to see full benefits
• If no benefits are observed after a reasonable trial period, discontinue therapy by slowly reducing the daily dosage

For intrathecal administration:

• Patients must undergo a screening phase with a test dose to ensure a positive response before pump implantation
• Close monitoring in a fully equipped environment is necessary during the initial titration period
• Dosage adjustments may be needed over time due to potential tolerance development

Crucial Precautions: Intrathecal Baclofen Withdrawal

One of the most critical aspects of baclofen therapy, particularly with intrathecal administration, is the risk of withdrawal. Abrupt discontinuation of intrathecal baclofen can lead to severe and potentially life-threatening complications.

Symptoms of Intrathecal Baclofen Withdrawal

Patients experiencing baclofen withdrawal may exhibit:

• High fever
• Altered mental status
• Exaggerated rebound spasticity
• Muscle rigidity

In rare cases, these symptoms can progress to rhabdomyolysis, multisystem organ failure, and even death.

Preventing Baclofen Withdrawal

To mitigate the risk of withdrawal, healthcare providers should:

1. Carefully program and monitor the infusion system
2. Adhere to refill scheduling and procedures
3. Pay close attention to pump alarms
4. Educate patients and caregivers about the importance of scheduled refill visits
5. Inform patients about early signs and symptoms of baclofen withdrawal

Special attention should be given to patients at higher risk for withdrawal, such as those with spinal cord injuries at T6 level or above, communication difficulties, or a history of withdrawal symptoms from oral or intrathecal baclofen.

Monitoring and Adjusting Baclofen Therapy

Effective management of baclofen therapy requires ongoing monitoring and adjustment to ensure optimal therapeutic outcomes while minimizing risks.

Clinical Goals of Baclofen Therapy

The primary objectives of baclofen treatment are:

• Maintaining muscle tone as close to normal as possible
• Minimizing the frequency and severity of spasms
• Avoiding intolerable adverse effects

It’s important to note that maintaining some degree of muscle tone and allowing occasional spasms may be beneficial for supporting circulatory function, minimizing the risk of deep vein thrombosis, and optimizing activities of daily living.

Adjusting Baclofen Dosage

Dosage adjustments should be made based on the patient’s response and tolerance. Key considerations include:

• Starting with the lowest effective dose
• Gradually increasing the dose as needed
• Monitoring for signs of tolerance development
• Adjusting the dose to maintain efficacy while minimizing side effects

In cases of tolerance to intrathecal baclofen, some patients may require a temporary reduction in dosage or alternation with other spasticity management methods to regain sensitivity to the medication.

Potential Risks and Side Effects of Baclofen Therapy

While baclofen is an effective treatment for spasticity, it’s associated with various potential risks and side effects that require careful consideration and management.

Common Side Effects

Patients using baclofen may experience:

• Drowsiness
• Dizziness
• Weakness
• Fatigue
• Nausea
• Headache

These side effects are often dose-dependent and may improve as the body adjusts to the medication.

Serious Risks

More serious risks associated with baclofen therapy include:

• Respiratory depression
• Seizures (particularly in epileptic patients)
• Psychiatric symptoms (e.g., hallucinations, depression)
• Increased risk of falls due to muscle weakness

For intrathecal baclofen, additional risks include pump malfunction, catheter-related complications, and the severe withdrawal syndrome discussed earlier.

Special Considerations for Long-Term Baclofen Use

Long-term use of baclofen requires ongoing vigilance and management to ensure continued efficacy and safety.

Tolerance Management

Tolerance to baclofen’s effects may develop over time, necessitating dose adjustments. Strategies to manage tolerance include:

• Gradual dose increases
• Temporary dose reductions
• Drug holidays (under close medical supervision)
• Combination with other spasticity management techniques

Monitoring for Long-Term Effects

Patients on long-term baclofen therapy should be regularly monitored for:

• Changes in spasticity control
• Development of new side effects
• Impact on quality of life and functional status
• Potential drug interactions with other medications

Regular follow-up appointments and assessments are crucial to ensure the ongoing appropriateness and effectiveness of baclofen therapy.

In conclusion, baclofen is a valuable tool in the management of spasticity associated with various neurological conditions. Its use, whether oral or intrathecal, requires careful consideration of individual patient factors, close monitoring, and ongoing adjustment to achieve optimal therapeutic outcomes while minimizing risks. Healthcare providers must remain vigilant about the potential for withdrawal and other complications, particularly with intrathecal administration. By following best practices in baclofen therapy management, clinicians can help patients achieve improved quality of life and functional status despite challenging neurological conditions.

Baclofen Monograph for Professionals – Drugs.com

Class: GABA-derivative Skeletal Muscle Relaxants
VA Class: MS200
Chemical Name: 4-Amino-3-(4-chlorophenyl)-butanoic acid
Molecular Formula: C₁₀H₁₂ClNO₂
CAS Number: 1134-47-0
Brands: Gablofen, Lioresal

Medically reviewed by Drugs.com on Oct 5, 2020. Written by ASHP.

Warning

Intrathecal Baclofen Withdrawal

• Abrupt discontinuance of intrathecal baclofen has resulted in high fever, altered mental status, exaggerated rebound spasticity, and muscle rigidity; in rare cases, progression to rhabdomyolysis, multisystem organ failure, and death has occurred.

• Give careful attention to programming and monitoring of infusion system, refill scheduling and procedures, and pump alarms to prevent abrupt discontinuance. (See Warnings under Cautions.)

• Advise patients and caregivers of the importance of keeping scheduled refill visits and of the early signs and symptoms of baclofen withdrawal.

• Give special attention to patients at apparent risk for withdrawal (e.g., spinal cord injury at T6 level or above, communication difficulties, history of withdrawal symptoms from oral or intrathecal baclofen).

• Consult technical manual of implantable infusion system for additional postimplant clinician and patient information.

Introduction

Skeletal muscle relaxant and antispastic agent; a GABA derivative.

Uses for Baclofen

Spasticity

Oral management of spasticity and its sequelae secondary to severe chronic disorders such as multiple sclerosis and other types of spinal cord lesions. Not indicated for use in patients with rheumatic disorders. Efficacy not established in patients with stroke, cerebral palsy, or Parkinson’s disease; use not recommended in these patients.

Intrathecal management of severe spasticity of spinal cord origin in patients who do not tolerate or respond adequately to oral baclofen; considered an alternative to destructive neurosurgical procedures. Also, intrathecal management of intractable spasticity secondary to severe chronic disorders such as multiple sclerosis and other types of spinal diseases such as spinal ischemia, spinal tumor, transverse myelitis, cervical spondylosis, and degenerative myelopathy; designated an orphan drug by FDA for use in these conditions.

Intrathecal management of severe spasticity of cerebral origin, including cerebral palsy and acquired brain injury; considered an alternative to destructive neurosurgical procedures. Designated an orphan drug by FDA for management of spasticity in patients with cerebral palsy. Patients with spasticity secondary to traumatic brain injury should wait ≥1 year after the injury before considering long-term intrathecal baclofen therapy.

Baclofen Dosage and Administration

General

• Clinical goal is to maintain muscle tone as close to normal as possible and to minimize frequency and severity of spasms without inducing intolerable adverse effects. May be important to maintain some degree of muscle tone and allow occasional spasms to help support circulatory function, minimize risk of DVT occurrence, and optimize activities of daily living and ease of care.

• Individualize dosage according to patient’s requirements and response; use lowest dosage that produces optimum response.

• Some patients require 1–2 months of oral treatment for full benefit. If benefits are not evident after a reasonable trial period, discontinue therapy by slowly reducing daily dosage.

• Prior to implantation of pump for chronic intrathecal baclofen therapy, patient must exhibit positive response (clinically important decrease in muscle tone and/or frequency and/or severity of spasms over 4- to 8-hour observation period) to initial intrathecal test dose(s) (screening phase).

• In patients receiving intrathecal baclofen therapy, closely monitor patients in a fully equipped and staffed environment during initial test for responsiveness and dosage-titration period immediately following implantation of pump. Resuscitative equipment should be immediately available for use in case of life-threatening or intolerable adverse effects.

• Tolerance may develop during chronic intrathecal baclofen therapy. No firm recommendations regarding amelioration of tolerance; patients occasionally have been hospitalized and intrathecal baclofen dosage decreased gradually over 2- to 4-week period, during which baclofen was alternated with other methods of spasticity management. Sensitivity to baclofen may return after a few days, and continuous intrathecal baclofen therapy may be resumed at the previously effective initial dosage.

Administration

Administer orally or intrathecally.

Baclofen injection for intrathecal administration is not recommended or intended for IV, IM, sub-Q, or epidural administration.

Avoid abrupt discontinuance (because of risk of precipitating withdrawal). Reduce dosage slowly when discontinuing drug, except for serious adverse reactions. (See Warnings under Cautions.)

Oral Administration

Administer orally 3 times daily.

Intrathecal Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer test dose(s) during screening phase by direct intrathecal injection (via lumbar puncture or catheter) over ≥1 minute employing barbotage.

Administer maintenance regimen by continuous intrathecal infusion into a lumbar intrathecal space via an implantable controlled-infusion device (e.g., Medtronic SynchroMed ^pump).

Consult manufacturer’s labeling for specialized administration techniques.

Consult manual provided by manufacturer of implantable infusion device for specific instructions and precautions for programming pump and/or refilling reservoir. Various pumps (with different reservoir volumes) and refill kits are available; clinicians must be familiar with these products in order to select the appropriate refill kit for the particular pump in use.

Dilution

To prepare test doses for screening phase, use 1-mL ampuls containing 50 mcg of baclofen without further dilution. Ampuls are for single use only; discard any unused portion.

For maintenance therapy in patients receiving concentrations other than the commercially available strengths (i.e., 0.5 or 2 mg/mL), injection concentrate must be diluted with sterile, preservative-free 0.9% sodium chloride for injection.

Rate of Administration

Test dose(s): Direct intrathecal injection by barbotage over ≥1 minute.

Maintenance regimen: Continuous intrathecal infusion.

Dosage

Pediatric Patients

Spasticity

Oral

Children ≥12 Years of Age: Initially, 5 mg 3 times daily. Increase daily dosage by 15 mg (in 3 divided doses) at 3-day intervals (i.e., 5 mg 3 times daily for 3 days, then 10 mg 3 times daily for 3 days, then 15 mg 3 times daily for 3 days, then 20 mg 3 times daily for 3 days) until optimum effect is achieved.

Usual dosage in children ≥12 years of age is 40–80 mg daily.

Screening for Response to Intrathecal Baclofen in Severe Spasticity

Intrathecal

Administer test dose of 50 mcg (1 mL of 50-mcg/mL solution) into intrathecal space by barbotage over ≥1 minute; may consider an initial dose of 25 mcg in very small children.

If response observed at 4–8 hours after initial test dose is less than desired, administer a second test dose of 75 mcg (1.5 mL of a 50-mcg/mL solution) 24 hours after first test dose.

If response observed at 4–8 hours after the second test dose remains inadequate, administer a final test dose of 100 mcg (2 mL of a 50-mcg/mL solution) 24 hours after second test dose.

Patients not responding to 100-mcg test dose are not candidates for chronic intrathecal therapy.

Maintenance Therapy for Severe Spasticity

Intrathecal

Following establishment of responsiveness to intrathecal baclofen, administer initial daily dose over 24 hours.

Initial daily dose is twice the test dose that produced a positive response with a duration not >8 hours. If positive response to test dose persisted >8 hours, initial dose is the same as the test dose that produced a positive response.

Following the initial infusion dose in children with spasticity of spinal cord or cerebral origin, increase daily dosage slowly (by 5–15% increments at 24-hour intervals) until desired clinical response is achieved.

May need to adjust maintenance dosage often during initial months of therapy. During periodic pump refills, increase the 24-hour dose by up to 10–40% in patients with spasticity of spinal cord origin or up to 5–20% in those with spasticity of cerebral origin as necessary to maintain adequate control of symptoms. In patients who develop intolerable adverse effects, reduce the 24-hour dose by 10–20%.

Patients achieving relatively satisfactory relief may derive further benefit from more complex dosing schedules. For example, patients who commonly experience an exacerbation of spasticity that disrupts sleep may require a 20% increase in the hourly infusion rate (programmed to begin approximately 2 hours before the time of desired clinical benefit).

Maintenance dosage in most children >12 years of age: 300–800 mcg daily (range: 12–2003 mcg daily) in those with spasticity of spinal cord origin; 90–703 mcg daily (range: 22–1400 mcg daily) in those with spasticity of cerebral origin.

Average maintenance dosage in children <12 years of age: 274 mcg daily (range: 24–1199 mcg daily).

Adults

Spasticity

Oral

Initially, 5 mg 3 times daily. Increase daily dosage by 15 mg (in 3 divided doses) at 3-day intervals (i.e., 5 mg 3 times daily for 3 days, then 10 mg 3 times daily for 3 days, then 15 mg 3 times daily for 3 days, then 20 mg 3 times daily for 3 days) until optimum effect is achieved.

Usual dosage is 40–80 mg daily.

Screening for Response to Intrathecal Baclofen in Severe Spasticity

Intrathecal

Administer test dose of 50 mcg (1 mL of 50-mcg/mL solution) into intrathecal space by barbotage over ≥1 minute.

If response observed at 4–8 hours after initial test dose is less than desired, administer a second test dose of 75 mcg (1.5 mL of a 50-mcg/mL solution) 24 hours after first test dose.

If response observed at 4–8 hours after the second test dose remains inadequate, administer a final test dose of 100 mcg (2 mL of a 50-mcg/mL solution) 24 hours after second test dose.

Patients not responding to 100-mcg test dose are not candidates for chronic intrathecal therapy.

Maintenance Therapy for Severe Spasticity

Intrathecal

Following establishment of responsiveness to intrathecal baclofen, administer initial daily dose over 24 hours.

Initial daily dose is twice the test dose that produced a positive response with a duration not >8 hours. If positive response to test dose persisted >8 hours, initial dose is the same as the test dose that produced a positive response.

Following the initial infusion dose, increase daily dosage slowly until the desired clinical response is achieved: increase dosage by 10–30% increments at 24-hour intervals in adults with spasticity of spinal cord origin and by 5–15% increments at 24-hour intervals in adults with spasticity of cerebral origin.

May need to adjust maintenance dosage often during initial months of therapy. During periodic pump refills, increase the 24-hour dose by up to 10–40% in patients with spasticity of spinal cord origin or up to 5–20% in those with spasticity of cerebral origin as necessary to maintain adequate control of symptoms. In patients who develop intolerable adverse effects, reduce the 24-hour dose by 10–20%.

Patients achieving relatively satisfactory relief may derive further benefit from more complex dosing schedules. For example, patients who commonly experience an exacerbation of spasticity that disrupts sleep may require a 20% increase in the hourly infusion rate (programmed to begin approximately 2 hours before the time of desired clinical benefit).

Maintenance dosage in most patients: 300–800 mcg daily (range: 12–2003 mcg daily) in those with spasticity of spinal cord origin; 90–703 mcg daily (range: 22–1400 mcg daily) in those with spasticity of cerebral origin.

Prescribing Limits

Pediatric Patients

Spasticity

Oral

Some clinicians suggest that daily dosages up to 150 mg are well tolerated and provide additional therapeutic benefit in some patients; however, one manufacturer states that dosage should not exceed 80 mg daily (20 mg 4 times daily).

Intrathecal

Limited experience with maintenance dosages >1000 mcg daily.

Adults

Spasticity

Oral

Some clinicians suggest that daily dosages up to 150 mg are well tolerated and provide additional therapeutic benefit in some patients; however, one manufacturer states that dosage should not exceed 80 mg daily (20 mg 4 times daily).

Intrathecal

Limited experience with maintenance dosages >1000 mcg daily.

Special Populations

Renal Impairment

Reduction of oral or intrathecal dosage may be necessary.

Geriatric Patients

Increase oral dosage more gradually.

Patients with Psychiatric or Brain Disorders

Increase oral dosage more gradually.

Cautions for Baclofen

Contraindications

Warnings/Precautions

Warnings

Abrupt Withdrawal of Oral Therapy

Abrupt discontinuance of oral baclofen may result in hallucinations and seizures.

Abrupt Withdrawal of Intrathecal Therapy

Abrupt discontinuance of intrathecal baclofen has resulted in high fever, altered mental status, exaggerated rebound spasticity, and muscle rigidity; in rare cases, progression to rhabdomyolysis, multisystem organ failure, and death have occurred.

Symptoms usually appear within hours to days following interruption of therapy. Early symptoms may include return of baseline spasticity, pruritus, hypotension, and paresthesias. Advanced withdrawal syndrome may resemble autonomic dysreflexia, sepsis, malignant hyperthermia, neuroleptic malignant syndrome, or other conditions associated with a hypermetabolic state or widespread rhabdomyolysis.

Rapid, accurate diagnosis and treatment in emergency room or intensive care setting are needed to prevent potentially life-threatening CNS and systemic effects.

Restore intrathecal baclofen therapy at or near the dosage used prior to interruption.

If reinstitution of intrathecal delivery is delayed, drugs that enhance GABA effects (e.g., oral or enteral baclofen; oral, enteral, or IV benzodiazepines) may prevent potentially fatal sequelae. However, do not rely on oral or enteral baclofen alone to halt progression of intrathecal baclofen withdrawal.

Experience in Intrathecal Administration

Should be administered intrathecally only by qualified individuals familiar with the administration techniques and patient management problems.

Initial test for responsiveness to intrathecal baclofen, implantation of pump, and subsequent periods of dosage titration must be performed in a medically supervised setting that is adequately equipped for the management of potential complications; resuscitative equipment should be readily available.

Risks of Intrathecal Administration

Potentially life-threatening CNS depression, cardiovascular collapse, and respiratory failure reported following intrathecal administration. Fatalities (including one case of unexpected death after administration of 3 test doses and 2 cases of sudden and unexpected death occurring within 2 weeks of pump implantation) reported rarely during intrathecal therapy; however, manufacturer states that causal relationship not established.

Patients, caregivers, and health-care providers should receive adequate information regarding the risks of intrathecal baclofen therapy, including information on recognition and management of potential overdosage and proper care of the pump and catheter insertion site.

Management of Controlled Infusion Device

Delay implantation of controlled-infusion device until response to test dose(s) is adequately evaluated.

Familiarization with the implantable infusion device (e.g., instructions and precautions for pump programming and refilling) is essential.

Fill drug reservoir under aseptic conditions (to avoid bacterial contamination and serious infection), following the directions provided by the device’s manufacturer; only fully trained and qualified personnel should fill reservoir. Follow proper refill frequency to avoid depletion of drug reservoir during use.

Monitor patient carefully, particularly during the initial phase of pump use, dosage titration, and reservoir refilling to ensure an acceptable, reasonably stable response.

Any sudden increase in dosage requirement should suggest the possibility of pump and/or catheter malfunction (i.e., catheter kink or dislodgement). If no increase in response is observed with upward titration of dosage, check pump function and catheter patency.

Intrathecal Baclofen Overdose

Signs of intrathecal baclofen overdose may appear suddenly or over a period of time.

Acute, massive overdose may present as coma.

Less sudden and/or less severe forms of overdose may present with drowsiness, lightheadedness, dizziness, somnolence, respiratory depression, seizures, rostral progression of hypotonia, and loss of consciousness progressing to coma.

Overdose generally related to pump malfunction or dosing error.

If overdose appears likely, immediately take patient to hospital for assessment and emptying of pump reservoir.

Fill pump with extreme caution; refill only through the pump reservoir refill septum. If reservoir refill septum is not properly accessed, inadvertent injection into sub-Q tissue can occur, possibly resulting in life-threatening overdosage or early depletion of reservoir. Some pumps are equipped with a catheter access port that allows direct access to the intrathecal catheter; direct injection into this catheter may cause life-threatening overdosage.

General Precautions

Autonomic Dysreflexia

Use intrathecal baclofen with caution in patients with a history of autonomic dysreflexia; the presence of nociceptive stimuli or abrupt withdrawal of therapy may precipitate episode of dysreflexia.

CNS Depression

Risk of sedation and/or drowsiness. Performance of activities requiring mental alertness may be impaired.

Concurrent use of other CNS depressants may potentiate CNS depression. (See Specific Drugs under Interactions.)

Maintenance of Muscle Tone

Use with caution and titrate dosage carefully when spasticity is necessary to sustain upright posture and balance in locomotion or whenever spasticity is used to obtain increased or optimal body function.

Neurological Disorders

Possible exacerbation of psychotic disorders, schizophrenia, or confusional states; use with caution and monitor such patients carefully.

Possible deterioration in seizure control and EEG in epileptic patients; monitor patient’s clinical state and EEG at regular intervals.

Concomitant Antispasmodic Therapies

If intrathecal therapy is to be employed, attempt to discontinue concomitant oral antispasmodic drugs to avoid possible overdose and drug interactions, either prior to screening phase or following implantation of infusion device. Monitor patient carefully; avoid abrupt dosage reduction or discontinuance of concomitant antispasmodics.

Presence of Infection

Presence of infection may interfere with assessment of the patient’s response to baclofen test dose(s), increase surgical complications after pump implantation, and complicate attempts to adjust dosage.

Patients being considered for intrathecal baclofen therapy should be without concurrent infection.

Intrathecal Mass

Development of intrathecal mass at the tip of implanted catheter reported following long-term intrathecal baclofen therapy. Most common sequelae or manifestations include decreased therapeutic response (i.e., worsening spasticity, return of spasticity despite previous response, withdrawal symptoms, poor response to escalating doses, frequent or large dosage increases), pain, and neurologic deficit or dysfunction.

Monitor patients carefully for any new neurologic manifestations. If new neurologic manifestations suggestive of an intrathecal mass occur, consider neurosurgical consultation, since many symptoms of inflammatory mass are similar to those associated with severe spasticity. In some cases, an imaging procedure may be appropriate to confirm or rule out diagnosis of an intrathecal mass.

Ovarian Cysts

Ovarian cysts found in about 4% of multiple sclerosis patients receiving oral baclofen for up to 1 year; cysts disappeared spontaneously despite continued baclofen use in most patients. Estimated rate of occurrence in healthy females is approximately 1–5%.

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk following oral administration; not known whether baclofen distributes into milk following intrathecal administration.

Nursing not recommended in women receiving oral baclofen. Women receiving intrathecal baclofen should nurse infant only if potential benefit justifies potential risks to infant.

Pediatric Use

Safety and efficacy of oral baclofen not established in children <12 years of age.

Safety and efficacy of intrathecal baclofen not established in children <4 years of age.

Children being considered for intrathecal therapy should have sufficient body mass to accommodate the pump. Consult directions provided by the device’s manufacturer.

Renal Impairment

Excreted principally in urine as unchanged drug; use with caution in patients with impaired renal function. (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

For oral baclofen, drowsiness, dizziness, weakness, fatigue.

For intrathecal baclofen in patients with spasticity of spinal cord origin, somnolence, dizziness, nausea, hypotension, headache, seizures, hypotonia.

For intrathecal baclofen in patients with spasticity of cerebral origin, agitation, constipation, somnolence, leukocytosis, chills, urinary retention, hypotonia.

Interactions for Baclofen

Specific Drugs

Insufficient experience with concomitant use of intrathecal baclofen and other drugs to predict specific drug-drug interactions.

Baclofen Pharmacokinetics

Absorption

Bioavailability

Rapidly and almost completely absorbed following oral administration, with peak blood concentrations attained within 2–3 hours. GI absorption is reduced as dosage is increased.

Following intrathecal administration, plasma concentrations are 100 times less than those achieved following oral administration.

Onset

Oral administration: Onset in hours to weeks.

Intrathecal injection: Onset in 0.5–1 hour in adults; peak effect in about 4 hours.

Continuous intrathecal infusion: Onset at 6–8 hours in adults; peak effect at 24–48 hours.

Onset and peak response may vary depending on dose and severity of symptoms.

Duration

Following intrathecal injection, effects may last 4–8 hours. Duration may vary depending on dose and severity of symptoms.

Distribution

Extent

Widely distributed following oral administration, but only small amounts cross the blood-brain barrier.

Crosses the placenta and distributes into milk following oral administration.

Plasma Protein Binding

30%.

Elimination

Metabolism

About 15% of a dose is metabolized in the liver, mostly by deamination.

Elimination Route

Excreted mainly (70–80%) in urine as unchanged drug or metabolites; remainder is excreted in feces.

Half-life

Serum half-life: 2.5–4 hours.

CSF elimination half-life: 1.51 hours for the first 4 hours following intrathecal injection. Following intrathecal administration, CSF clearance of baclofen approximates CSF turnover.

Stability

Storage

Oral

Tablets

Well-closed containers at 20–25°C.

Parenteral

Injection

≤30°C. Refrigeration not required. Do not freeze or autoclave.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility113

Drug Compatibility

Actions

• Decreases frequency and amplitude of muscle spasms (tonic reflexes) that arise in response to muscle stretching in patients with various spinal cord lesions.

• Simultaneously and equally suppresses cutaneous reflexes and muscle tone but only slightly depresses amplitude of tendon jerks (phasic reflexes).

• Inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by decreasing excitatory neurotransmitter release from primary afferent terminals; actions at supraspinal sites also may occur and contribute to drug’s clinical effect.

• Intrathecal administration in animals increases antinociception and decreases muscle rigidity and spasticity.

Advice to Patients

• Importance of not abruptly discontinuing therapy. For patients receiving intrathecal baclofen, importance of keeping scheduled refill visits and of recognizing early signs and symptoms of withdrawal.

• If baclofen is to be administered intrathecally, risks associated with intrathecal baclofen therapy, recognition and management of overdosage, and proper care of pump and catheter insertion site.

• Risk of drowsiness; exercise caution when driving or operating machinery.

• Potential for additive CNS depression if other CNS depressants (e.g., alcohol) are used concomitantly.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of women informing their clinician if they are or plan to become pregnant or to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

AHFS ^{DI Essentials™. © Copyright 2021, Selected Revisions October 15, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.}

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Medical Disclaimer

Baclofen for muscle spasm | Medicines for Children

Baclofen for muscle spasm

This leaflet is about the use of baclofen for severe muscle spasm (spasticity). This may be due to cerebral palsy or other conditions that affect the brain or spinal cord.

This leaflet has been written specifically for parents and carers about the use of this medicine in children. Our information sometimes differs from that provided by the manufacturers, because their information is usually aimed at adult patients. Please read this leaflet carefully. Keep it somewhere safe so that you can read it again.

Do not stop giving baclofen suddenly, as this will cause serious side-effects.

Name of drug

Baclofen
Common brands: Baclospas®, Lioresal®, Lyflex®

Why is it important for my child to take this medicine?

Baclofen will help your child’s muscles to relax. This will help your child to move, and make it easier and less painful for you to move them. Baclofen may also help to reduce muscle pain.

What is baclofen available as?

• Tablets: 10 mg
• Liquid medicine: 1 mg in 1 mL

Different tablets or medicines may contain different ingredients in addition to baclofen. Read the packet or leaflet that comes with it to find out if the medicine contains anything that your child should not have.

All the above products have to be ordered specially by your pharmacist.

When should I give baclofen?

You and your doctor will work out when and how often to give baclofen to suit your child.

How much should I give?

Your doctor will work out the amount of baclofen (the dose) that is right for your child. The dose will be shown on the medicine label.

You will start by giving your child a small amount and then increase the dose bit by bit. Your doctor will ask you how well the medicine is working, and may suggest that you change the amount you give, or when you give it, to get the best effect. If you think the dose is not right, talk to your doctor.

It is important that you follow your doctor’s instructions about how much to give.

How should I give it?

Baclofen should be taken with or just after food.

Tablets should be swallowed with a glass of water, juice or similar. Your child should not chew the tablets. Your doctor may have told you to give half or quarter of a tablet.

Liquid medicine: Measure out the right amount using an oral syringe or medicine spoon. You can get these from your pharmacist. Do not use a kitchen teaspoon as it will not give the right amount.

When should the medicine start working?

Your child’s muscles should begin to feel less stiff after taking baclofen regularly for 3–4 days. It may take up to 10 days for the maximum effect.

What if my child is sick (vomits)?

• If your child is sick less than 30 minutes after having a dose of baclofen, give them the same dose again.
• If your child is sick more than 30 minutes after having a dose of baclofen, you do not need to give them another dose. Wait until the next normal dose.

What if I forget to give it?

If you forget to give a dose, your child’s muscles may become a little stiffer. Give the dose as soon as you remember. Wait at least 4 hours before giving the next dose.

What if I give too much?

It can be dangerous to give your child too much baclofen.

If you think your child may have had too much baclofen, contact your doctor or take your child to hospital straight away. Tell the doctor that they may have had too much baclofen. Take the medicine or packaging with you, so that the doctor can see what has been taken. Have the packaging with you if you telephone for advice.

Are there any possible side-effects?

We use medicines to make our children better, but sometimes they have other effects that we don’t want (side-effects).

Side-effects you must do something about

If your child has a seizure (also called a fit or convulsion) or is very sleepy or difficult to wake up, they may have had too much baclofen. Take them to hospital straight away.

If your child has difficulty breathing, take them to hospital straight away.

Tell the doctor that your child is taking baclofen. Take the medicine or packet with you.

Other side-effects you need to know about

• If your child is confused, can’t sleep or has nightmares, or seems anxious or shaky, contact your doctor.
• Your child may be more sleepy than usual, they may feel sick, and they may find it hard to pass urine (have a wee).
• Your child may feel light-headed when moving from lying down to sitting up. Tell your doctor if this happens, as your child’s blood pressure may be a bit low.
• If your child’s muscles become floppy (hypotonic), contact your doctor, as you may need to give less baclofen.

There may, sometimes, be other side-effects that are not listed above. If you notice anything unusual and are concerned, contact your doctor. You can report any suspected side-effects to a UK safety scheme at www.mhra.gov.uk/yellowcard.

Can other medicines be given at the same time as baclofen?

• You can give your child medicines that contain paracetamol or ibuprofen, unless your doctor has told you not to.
• Check with your doctor or pharmacist before giving any other medicines to your child. This includes herbal or complementary medicines.

Is there anything else I need to know about this medicine?

• If your doctor decides that baclofen is not right for your child, you will need to reduce the dose bit by bit over a few weeks so that your child doesn’t get side-effects. Do not reduce the dose without talking to your doctor first.
• If your child is already taking other medicines, tell your doctor before starting baclofen.
• If your child has kidney problems, tell your doctor before starting baclofen.
• Baclofen may not be suitable for children with stomach ulcers, mental health problems or who have difficulty passing urine (having a wee). If your child has any of these conditions, tell your doctor.

General advice about medicines

• If baclofen does not seem to be controlling your child’s spasms, contact your doctor for advice.
• Try to give medicines at about the same times each day, to help you remember.
• Only give this medicine to your child. Never give it to anyone else, even if their condition appears to be the same, as this could do harm. 

If you think someone else may have taken the medicine by accident, contact your doctor straight away.

• Make sure that you always have enough medicine. Order a new prescription at least 2 weeks before you will run out.
• Make sure that the medicine you have at home has not reached the ‘best before’ or ‘use by’ date on the packaging. Give old medicines to your pharmacist to dispose of.

Where should I keep this medicine?

• Keep all medicines where children cannot see or reach them.
• Keep this medicine somewhere cool and dry, away from direct heat and light. It does not need to be kept in the fridge.
• Keep the medicine in the container it came in.

Who to contact for more information

Your doctor or pharmacist will be able to give you more information about baclofen, and about pain relief for muscle spasticity

APO-Baclofen Tablets – NPS MedicineWise

What is in this leaflet

This leaflet answers some common questions about this medicine. It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking this medicine against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine.
You may need to read it again.

What this medicine is used for

The name of your medicine is APO-Baclofen Tablets. It contains the active ingredient baclofen.

It is used to treat:

• multiple sclerosis
• spinal cord damage resulting from disease or physical injury

Baclofen belongs to a group of medicines called muscle relaxants. It is used to reduce excess tension in your muscles which causes spasms.

Because this medicine reduces spasms and the pain that goes with them, it helps to make you more mobile. This helps you to manage your daily activities more easily.

Ask your doctor if you have any questions about why this medicine has been prescribed for you.
Your doctor may have prescribed it for another reason.

There is no evidence that this medicine is addictive.

This medicine is available only with a doctor’s prescription.

Use in children

Baclofen should be used with extreme caution in children under 16 years of age as only limited information is available. Baclofen should not be used in children who weigh less than 33 kg.

Before you take this medicine

When you must not take it

Do not take this medicine if you have an allergy to:

• baclofen
• any of the ingredients listed at the end of this leaflet

Symptoms of an allergic reaction may include:

• cough, shortness of breath, wheezing or difficulty breathing
• swelling of the face, lips, tongue, throat or other parts of the body
• rash, itching or hives on the skin
• fainting; or hay fever-like symptoms.

Do not take this medicine if you are currently pregnant or you plan to become pregnant.
Do not take this medicine until you and your doctor have discussed the risks and benefits involved.

If you must take baclofen during pregnancy, your baby may have convulsions and other symptoms related to sudden discontinuation of the medicine just after delivery.

Do not take this medicine if you are currently breastfeeding or you plan to breastfeed.
Baclofen may pass into breast milk and there is a possibility that your baby may be affected.

Do not take this medicine until you and your doctor have discussed the risks and benefits involved.

Do not take this medicine after the expiry date printed on the pack or if the packaging is torn or shows signs of tampering.
If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking this medicine, talk to your doctor.

Before you start to take it

Tell your doctor if you have allergies to any other medicines, foods, preservatives or dyes.

Tell your doctor if you have or have had any of the following medical conditions:

• lactose intolerance – this medicine contains a small amount of lactose
• any mental/psychiatric illness
• Parkinson’s disease
• seizures (fits) from any cause
• stiffness and restriction of movement in a group of muscles
• stomach or duodenal ulcers
• stroke or other blood vessel diseases
• heart problems
• kidney problems
• liver problems
• lung problems which make breathing difficult
• diabetes
• high blood pressure
• porphyria, a disorder which can affect liver function and blood formation
• history of alcoholism, drink alcohol to excess or you have a history of drug abuse or dependence. Some people being treated with baclofen have had thoughts of harming themselves or have tried to kill themselves. Most of these people also had depression, had been using alcohol excessively or were prone to having thoughts of killing themselves. If you have thoughts of harming or killing yourself at any time, speak to your doctor straightaway or go to a hospital. Also, ask a relative or close friend to tell you if they are worried about any changes in your behaviour and ask them to read this leaflet.

Tell your doctor if you are pregnant or plan to become pregnant or are breastfeeding.
Your doctor can discuss with you the risks and benefits involved.

If you have not told your doctor about any of the above, tell them before you start taking this medicine.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you get without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may interact with baclofen. These include:

• any medicine that tends to make you sleepy, such as medicines used to help you sleep or calm you down (e.g. diazepam), relax muscles (e.g. tizanidine), pain relievers (e.g. morphine), travel sickness medicines and medicines for colds or allergies – these may add to the sedative effect of baclofen
• medicines used to treat mood disorders such as tricyclic antidepressants, lithium and monoamine oxidase inhibitors (MAOIs)
• medicines for high blood pressure
• medicines used to treat Parkinson’s disease, including levodopa and carbidopa
• medicines used to treat diabetes
• medicines which may affect the way your kidney works

These medicines may be affected by baclofen or may affect how well it works. You may need different amounts of your medicines, or you may need to take different medicines.

Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

How to take this medicine

Follow all directions given to you by your doctor or pharmacist carefully.
They may differ from the information contained in this leaflet.

If you do not understand the instructions on the label, ask your doctor or pharmacist for help.

How much to take

This will depend on your condition and whether you are taking any other medicines.

Treatment is normally started in hospital with small doses of baclofen.

The dose is then gradually increased to an amount that works best for you.

For example, baclofen may be started at a dose of 15 mg a day, then increased slowly to anywhere from 30 to 75 mg a day. Sometimes, doses up to 100 mg a day may be needed.

If you are under the age of 16 or over 65, or you have kidney disease, your doctor may start you on a lower doseand increase it more gradually to prevent side effects.

How to take it

Swallow the tablets during meals with some water.
This will lessen the chance of a stomach upset.

Baclofen is usually taken in at least three divided doses throughout the day. But your doctor may tell you to take it more or less often, depending on your situation.

How long to take it for

Continue taking your medicine for as long as your doctor tells you.

Your doctor will check your progress to make sure the medicine is working and will discuss with you how long your treatment should continue.

If you forget to take it

If it is almost time to take your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for missed doses.
This may increase the chance of you experiencing side effects.

If you are not sure what to do, ask your doctor or pharmacist.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints to help you remember.

If you take too much (overdose)

Immediately telephone your doctor or the Poisons Information Centre (telephone 13 11 26) for advice or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have taken too much of this medicine. Do this even if there are no signs of discomfort or poisoning.
You may need urgent medical attention.

Symptoms of an overdose include feeling drowsy, having problems breathing or losing consciousness.

You may also feel confused, hallucinate (imagine things that are not there), have unusual muscle weakness, blurred vision, feel sick (nausea), be sick (vomit), faint, have diarrhoea, increased saliva, slow or irregular heartbeat, or fits (seizures).

If you have kidney disease and have accidentally taken more tablets than your doctor has prescribed, you may experience neurological symptoms of overdose (e.g. drowsiness, feeling confused, hallucinations)

While you are taking this medicine

Things you must do

If you are about to be started on any new medicine, remind your doctor and pharmacist that you are taking this medicine.

Tell any other doctors, dentists, and pharmacists who treat you that you are taking this medicine.

If you are going to have surgery, tell the surgeon or anaesthetist that you are taking this medicine.
It may affect other medicines used during surgery.

If you become pregnant or start to breastfeed while taking this medicine, tell your doctor immediately.

If you are about to have any blood tests, tell your doctor that you are taking this medicine.
It may interfere with the results of some tests.

Keep all your doctor’s appointments so that your progress can be checked.
Your doctor may occasionally do tests to make sure the medicine is working and to prevent side effects.

Go to your doctor regularly for a check-up.

Things you must not do

Do not take this medicine to treat any other complaints unless your doctor tells you to.

Do not give your medicine to anyone else, even if they have the same condition as you.

Do not stop taking your medicine or lower the dosage without checking with your doctor.

This medicine is not habit-forming but stopping it suddenly may bring on severe spasms and other unwanted symptoms, such as nervousness, feeling confused, hallucinations, abnormal thinking or behaviour, convulsions, uncontrollable twitching, jerking or writhing movements, fast heartbeat, high body temperature, pain in muscles, fever and dark urine. The excessive stiffness (spasms) in your muscles may also get worse.

If baclofen must be stopped, your doctor will reduce the dose gradually over a period of 1 to 2 weeks so that these unwanted effects are avoided.

Things to be careful of

Be careful when driving, operating machinery or doing jobs that require you to be alert until you know how this medicine affects you.
Baclofen may cause sleepiness, dizziness, light-headedness and decreased alertness in some people, especially at the start of treatment.

Be careful when drinking alcohol while you are taking baclofen.
The combination may make you feel more sleepy, dizzy or lightheaded and less alert than usual.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking this medicine.

All medicines can have side effects. Sometimes they are serious but most of the time they are not.

Do not be alarmed by the following lists of side effects. You may not experience any of them.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor if you notice any of the following and they worry you:

• daytime sleepiness or drowsiness
• lack of energy or feeling exhausted
• dizziness or light-headedness
• spinning sensation (vertigo)
• mental confusion
• headache
• difficulty sleeping or nightmares
• nausea (feeling sick), retching or vomiting
• constipation, stomach cramps or diarrhoea
• loss of appetite
• stuffy or blocked nose
• dry mouth
• change in sense of taste
• misuse, abuse and dependence
• suicide or suicide attempts
• problems with co-ordination and balance
• difficulty in speaking
• swelling of the ankles due to fluid build-up
• blurred or double vision
• mild rash or mildly itchy skin
• ringing in the ears
• frequent urination or bed wetting
• excessive sweating
• erection problems or inability to ejaculate
• weight gain
• increased blood sugar
• low body temperature

Tell your doctor as soon as possible if you notice any of the following:

• mental confusion
• numbness or tingling in hands and feet
• muscle weakness, spasms or pain
• swelling of ankles due to fluid build-up
• blurred or double vision
• problems with coordination, balance and movement
• difficulty in speaking
• increased blood sugar
• low body temperature.

These may be serious side effects and you may need medical attention.

If any of the following happen, tell your doctor immediately or go to Accident and Emergency at your nearest hospital:

• slow or difficult breathing
• fast or irregular heart beat
• fainting or loss of consciousness
• seizures (fits)
• chest pain
• uncontrollable muscle spasms affecting the eyes, head, neck or body
• depression or other severe mood or mental changes
• hallucinations (feeling, hearing or seeing things that are not there)
• being unable to urinate or pain when urinating; blood in the urine
• symptoms following sudden discontinuation of the medicine (such as spasms).

The above list includes very serious side effects. You may need urgent medical attention or hospitalisation.

Other side effects not listed above may occur in some patients.

Storage and disposal

Storage

Keep your medicine in its original packaging until it is time to take it.
If you take your medicine out of its original packaging it may not keep well.

Keep your medicine in a cool dry place where the temperature stays below 25°C.

Do not store this medicine or any other medicine in the bathroom or near a sink. Do not leave it on a window sill or in the car.
Heat and dampness can destroy some medicines.

Keep this medicine where children cannot reach it.
A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking this medicine or the expiry date has passed, ask your pharmacist what to do with any medicine that is left over.

Product description

What APO-Baclofen looks like

Baclofen 10 mg tablets:

White, oval, flat-faced, bevel-edged tablets scored and engraved “APOB10” on one side. AUST R 77577.

Baclofen 25 mg tablets:

White, round, flat-faced, bevel-edged tablets, scored on one side. AUST R 77576.

Bottle packs of 100 tablets.

* Not all strengths, pack types and/or pack sizes may be available.

Ingredients

Each tablet contains 10 mg or 25 mg of baclofen as the active ingredient.

It also contains the following inactive ingredients:

• lactose monohydrate
• maize starch
• microcrystalline cellulose
• magnesium stearate.

This medicine is gluten-free, sucrose-free, tartrazine-free and free of other azo dyes.

Sponsor

Apotex Pty Ltd
16 Giffnock Avenue
Macquarie Park NSW 2113

APO and APOTEX are registered trade marks of Apotex Inc.

This leaflet was last updated in February 2020.

Published by MIMS April 2020

Single-dose baclofen-induced neurotoxicity in a patient with end stage renal disease: case report | BMC Nephrology

Baclofen is a natural derivative agonist of GABA_B receptors at the level of the spinal cord thus producing its attenuating effect on the muscle tone if used within the therapeutic range [1]. The daily therapeutic dose ranges between 5 and 60 mg [7, 8]. Adverse effects with baclofen overdose have been noticed among people with normal kidney function such as sedation, confusion, muscle weakness and impaired consciousness [1] and these effects are attributed to its inhibitory effect on the central nervous system [6]. The reported doses of intoxication were between 80 mg and 2500 mg with the more severe among those who have ingested more than 200 mg requiring more intensive care unit admissions and for longer durations [9].

The situation becomes more complicated in those with impaired renal function as baclofen is mainly excreted by the renal system (85–90%) and the rest, 10–15%, becomes metabolized by the liver [6]. Based on this data, and knowing that the liver function is intact, or, at least, not impaired, as the liver enzymes and other related laboratory variables were within the normal range, the impaired kidney functioning capacity is the only one to be blamed as the cause of baclofen toxicity. The reported doses of baclofen toxicity among patients with chronic kidney disease ranges between 5 mg and 60 mg per day, and most of the patients were known to have advanced kidney disease [10]. The onset of symptoms usually started 2–3 days after the ingestion of baclofen [4, 10] but as early as 24 h have also been documented among those with end-stage renal disease [6]. However, our case developed a state of sleepiness and unconsciousness as soon as 12 h post ingestion of a single dose of 25 mg. The impaired excretion is responsible for the toxic effects of baclofen even with normal therapeutic doses as it accumulates and induces neurotoxicity [4].

Among the presumed differentials is PRES, posterior reversible encephalopathy syndrome. PRES is a group of neurological signs and symptoms and characteristic radiologic findings that are usually reversible [11]. Clinically, PRES is diagnosed by acute onset of headache, seizures, visual problems and encephalopathy^, in addition to the radiologic findings of vasogenic edema, either by CT or MRI (Preferred), mainly affecting the parieto-occipital lobes [12]. Referring to our patient, PRES could easily be excluded as, by definition, PRES should have radiologic findings as part of the diagnostic criteria and both CT and MRI were done for the patient and no one could identify any consistent findings for PRES or any other intracranial lesion that might explain the clinical picture of the patient.

The manifestations of baclofen toxicity are dizziness, nausea, vomiting, respiratory depression, altered mental status, ataxia, dystonia and coma [3, 6, 8, 13]. Reversible akinetic mutism [14] and severe comatose state with absent brain stem reflexes have been documented with severe baclofen intoxication [15]. The degree of chronic renal failure varied among patients from acute kidney injury to stage 5 chronic renal failure and eventually end stage renal disease [6, 15].

The mainstay of treatment is supportive and close monitoring for possible respiratory compromise [6]. Hemodialysis is also a very reliable method of treatment as it decreases baclofen half-life in ESRD patients from 15 to 2 h [16]. Some reported cases improved dramatically after only one session as it is thought to eliminate baclofen from the body as do normal kidneys [16–18] but other patients needed up to five sessions for complete recovery [6]. Our patient started to show improvement after two hemodialysis sessions and the complete recovery was gained after a total of five. Continuous Renal Replacement Therapy seems to be a good substitution for those patients who are not a candidate for hemodialysis [6].

In the published literature, there is still a much debate of what dose of baclofen to use in patients with impaired kidney function and when to start decreasing or discontinuing the dose [4, 7, 15]. Roberts et al. [6] provided a clear suggestion of totally avoiding baclofen use among ESRD and acute renal failure patients and those with a glomerular filtration rate less than 60 ml/minute. They also suggested to use the lowest possible dose for those with mild chronic kidney disease, GFR more than 60 ml/minute [6].

Another presumed hypothesis to explain what happened to the patient is the finding of significantly elevated blood pressure at the time of diagnosis and whether or not it might have contributed to the increased risk of baclofen toxicity, even with a single dose as noticed in our case. Up to the authors’ knowledge, not one study was reported to prove or disprove this hypothesis as most of the reported cases had normal or slightly elevated blood pressures [1, 3, 4, 8, 15].

Baclofen – MotherToBaby

This sheet is about exposure to baclofen in pregnancy and while breastfeeding. This information should not take

the place of medical care and advice from your healthcare provider.

What is baclofen?

Baclofen is a muscle relaxant and antispasmodic medication. It helps muscles connected to the skeleton relax.  Baclofen is used to treat spastic movement disorders or rigid muscles caused by conditions like multiple sclerosis, cerebral palsy, and spinal cord or brain injuries. Baclofen can also be used to treat certain cases of hiccups, autism, and alcohol use disorder. It can be taken by mouth or given directly to the spinal cord through a pump (intrathecal pump).  Also, as cream, baclofen can be applied directly to the skin (topically). Sometimes it is combined with other prescription medications (amitriptyline, ketamine, ketoptofen) that are applied to skin and other tissues to treat pain. Some brand names for baclofen are Lioresal®, Kemstro®, and Gablofen®. Topically applied baclofen is sold by the name EnorvaRX-Baclofen®.

I take baclofen. Can it make it harder for me to get pregnant?

Studies have not yet been done to see if baclofen could make it harder to get pregnant.

I just found out I am pregnant. Should I stop taking baclofen?

Talk with your healthcare providers before making any changes to how you take your medication. The benefits of taking your medication may outweigh the risks of untreated illness. Suddenly stopping baclofen can cause serious withdrawal symptoms including seizures, hallucinations, confusion, delusions, disorientation, general agitation, insomnia, dizziness, nausea, and personality changes. It is not known if or how withdrawal symptoms may affect a pregnancy.

Does taking baclofen during my pregnancy increase the chance of miscarriage? 

Miscarriage can occur in any pregnancy. Studies have not yet been done to see if baclofen can increase the chance of miscarriage.

Does taking baclofen increase the chance of having a baby with a birth defect?

Every pregnancy starts out with a 3-5% chance of having a birth defect. This is called the background risk. Experimental studies in animals raised concern that baclofen could increase the chance for birth defects.  But, the animals were given doses of baclofen that were much higher than what a person would take. There is no evidence that taking baclofen during pregnancy increases the chance of having a baby with birth defects above the background risk. There are also several case reports of children that were exposed to baclofen during pregnancy and did not have birth defects. More information is needed in order to know if baclofen can increase the chance for birth defects.

Could taking baclofen cause other pregnancy complications?

It is not known if taking baclofen can cause other pregnancy complications.

I need to take baclofen throughout my entire pregnancy. Will it cause withdrawal symptoms in my baby after birth?

Withdrawal symptoms have been reported in babies whose mothers had taken baclofen by mouth (orally) throughout pregnancy. The withdrawal symptoms may include seizures, tremors, rigidity, drowsiness, dilated pupils, dry mouth, and problems feeding. Short-term treatment with baclofen in newborns who were exposed to baclofen up to delivery has been used to manage or prevent withdrawal symptoms.

No withdrawal symptoms have been reported in babies whose mothers were treated with baclofen by intrathecal pump.

Does taking baclofen in pregnancy cause long-term problems in behavior or learning for the baby? 

Studies on long-term development of children exposed to baclofen during pregnancy have not yet been done.

Can I breastfeed while taking baclofen? 

There is limited information about the use of baclofen during breastfeeding. One study found that very low amounts of baclofen enter the breastmilk when baclofen is taken by mouth. When baclofen is taken via intrathecal pump, another study found even less enters the breastmilk.  No harmful effects in nursing infants have been reported.

If you suspect that the baby has any symptoms that could be related to your baclofen use, such as drowsiness, dry mouth, tremor, rigidity and dilated pupils, contact the child’s healthcare provider. Be sure to talk to your healthcare provider about all of your breastfeeding questions.

I take baclofen. Can it make it harder for me to get my partner pregnant or increase the chance of birth defects? 

There are no studies looking male fertility and the use of baclofen. In general, exposures that fathers and sperm donor have are unlikely to increase risks to a pregnancy. For more information, please see the MotherToBaby fact sheet Paternal Exposures at https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/.    

Please click here for references.

OTIS/MotherToBaby recognizes that not all people identify as “men” or “women.” When using the term “mother,” we mean the source of the egg and/or uterus and by “father,” we mean the source of the sperm, regardless of the person’s gender identity.

View PDF Fact Sheet

Prevalence and risk factors of baclofen neurotoxicity in patients with severely impaired renal function

Introduction

Baclofen is a derivative of γ-aminobutyric acid (GABA), which acts mainly on the vertebral GABA-B receptors to inhibit synaptic motor neurons, thereby resulting in a central anticonvulsant response.1,2 The GABA-B receptor, which is associated with the G protein, opens the nearby potassium channel, hence increasing the potassium membrane conductivity, promoting cell membrane polarization, and preventing action potentials from occurring.3 Baclofen is used for treating spastic movement disorders, such as spinal cord injury, cerebral palsy, and multiple sclerosis. It is also used for managing uncontrolled hiccups (>48h) in patients with cancer or patients undergoing alcohol and drug withdrawal symptoms.1,3–11

The therapeutic dose of baclofen is 15–80mg/day, and the plasma concentration is 80–400ng/mL.6,12,13 The half-life of baclofen is 2–6h, the molecular weight is 213Da, and the volume of distribution is 0.8L/kg in adults and 2.6L/kg in children.1,3,7,12,14–16 Also, it is moderately lipophilic and approximately 30% binds to serum protein.12 It is well distributed in the vascular space and blood-rich organs (liver and kidney), but it is distributed at a low plasma concentration of 12% in the central nervous system (CNS), as it passes through the blood–brain barrier.4,5,12,13 Orally administered baclofen is rapidly absorbed in the digestive tract. Liver metabolism plays a small role. Approximately, 85% of this agent is excreted in the kidneys; so, if the patient’s renal function is poor, the half-life of the agent will be long.1,3,6,7,14,15,17

Baclofen slowly passes through the blood-brain barrier and exhibits neurotoxicity.5,12 In the CNS, the removal of baclofen is also slow. Therefore, the CNS symptoms may persist even though the plasma baclofen concentration is decreased.3,13,15,18 The most common symptom is alteration in consciousness. Abdominal pain often occurs due to a cholinergic reaction mediated by GABA.4,18 At low doses of baclofen, patients might experience such symptoms as temporary drowsiness and nausea. A high-dose baclofen administration can cause CNS depression, such as sedation, drowsiness, and respiratory depression. Patients with a history of seizures may have more pronounced seizures.3 If baclofen-induced acute encephalopathy occurs, an electroencephalogram is requested, in which case, the results may reveal various patterns, such as periodic 3 phase complex; however, no special treatment is required.19–22

There is no specific antidote to baclofen toxicity, and hemodialysis is most commonly used for treating neurotoxicity because of its low-molecular-weight, lipophilic nature, and low binding to proteins.1,4,7,15,23 Dialysis can remove the drug from the body at the same rate as in people with normal renal function, and when dialyzed for 4h, about 79% can be eliminated, and the half-life can be reduced from 15h to 2h.15,24 Even in patients with normal renal function, baclofen overuse may cause neurotoxicity, and dialysis is also useful in this case.23

Baclofen is, for the most part, excreted in the kidneys; so, patients with acute kidney injury or chronic kidney disease (CKD) who do not reduce the dose will have symptoms, such as encephalopathy, respiratory failure, and unconsciousness.3,6 In many cases, the symptom appears as iatrogenic, and there is room for prevention. However, there is still no standard for drug dosage reduction according to renal function, which makes it difficult to control the drug.3,5,25 Previous studies have shown that even a small amount of baclofen (5mg) may cause neurotoxicity, but the greater the dose, the older the age, and the more extensive the brain lesion, the greater the chance of neurotoxicity.1,7,12,18,26 It is also reported that neurotoxicity is more pronounced in men (56.3%), patients with end-stage renal disease who receive dialysis (62.9%), or people with concomitant use of CNS depressants.1,16,27 There were no data on the prevalence of neurotoxicity.

In this study, we analyzed the prevalence and the risk factors of neurotoxicity in patients with severe CKD who were treated with baclofen at XXXX Medical Center for the last 11 years.

MethodsPatients

We retrospectively studied CKD stage 4, non-dialysis stage 5, and on-dialysis patients, who were treated with baclofen at XXXX Medical Center from January 1, 2006, to December 31, 2016. A search using the XXXX Biomedical Research Environment revealed that 17,041 patients were treated with baclofen during this period. Of the total patients, 523 patients had a Modification of Diet in Renal Disease estimated Glomerular Filtration Rate (MDRD-eGFR) of

mL/min/1.73m2 and were assigned the disease code N18* ICD-9-CM (except N181, N182, and N183, which correspond to CKD stages 1, 2, and 3, respectively). We extracted the data on these patients with MDRD-eGFR of mL/min/1.73m2 measured at the closest date to the last baclofen prescription. Consequently, we extracted the data on 401 of 523 individuals, and we analyzed and compared their information. This study is a retrospective analysis of the medical records. Because there is little likelihood of any type of infringement on the patients’ human rights, we did not obtain the patients’ informed consent.Data collection

The following data were collected:

• 1.

  Baseline characteristics of patients: sex, age, height, weight, and body mass index (BMI)

• 2.

  Underlying diseases: diabetic nephropathy, hypertension, congestive heart failure, cancer, and CNS disease

• 3.

  Baclofen medication information

• (1)

  Reason for medication: hiccups, muscle cramps, others

• (2)

  Prescribed place: inpatient, outpatient

• (3)

  Total dose

• (4)

  Medication period

• (5)

  Daily dose (total dose/medication period)

• 4.

  Clinical features of patients with neurotoxicity

  • (1)

    Neurotoxic symptoms

  • (1)

    Mental change

  • (2)

    Seizure

  • (3)

    Time to symptom onset

  • (4)

    Duration of symptoms

  • (2)

    Neurotoxicity treatment

• (1)

  Intensive care unit (ICU): Yes/No

• (2)

  ICU duration

• (3)

  Use of ventilator: Yes/No

• (4)

  Ventilator duration

• (5)

  Therapeutic hemodialysis, number of times

• (6)

  Therapeutic peritoneal dialysis, days

• 5.

  Taking other drugs acting on the CNS: Yes/No

• 6.

  Laboratory results

• (1)

  Serum creatinine

• (2)

  Serum MDRD-eGFR

• (3)

  Serum albumin

• (4)

  Serum cholesterol

• (5)

  Serum C-reactive protein (CRP)

• (6)

  Serum total CO2

• (7)

  Plasma pCO2

• (8)

  Plasma bicarbonate

Baclofen neurotoxicity was defined as a state in which neurological symptoms, such as mental alterations, seizures, encephalopathy, and respiratory depression, which occurred after baclofen administration could not be explained by causes other than baclofen. The laboratory results at the time of neurotoxicity diagnosis were documented for patients with neurotoxicity, and for patients without neurotoxicity, the laboratory results from the last day of baclofen administration were recorded. When baclofen was prescribed several times during the study period, the total dose was defined as the total dose at the time of the first prescription period. Severe CKD was defined as a state in which the renal function was stage 4 or lower.

Ethics statements

The study was conducted in accordance with the ethical standards of the Declaration of Helsinki (as revised in Brazil, 2013). The protocol was approved by an Institutional Review Board of XXXXX XXXX Medical Center (No. 2017-0429).

Statistical analysis

The numerical data were expressed as the mean±standard deviation values when the normality was satisfied, and as the median, minimum, and maximum values when the normality was not satisfied. The frequency of occurrence was expressed as a percentage (%). The normality test was performed using the Kolmogorov–Smirnov test. Student’s t-test was used for comparison between two independent groups that met the normality. The difference between the three groups was analyzed using one-way analysis of variance. The Mann–Whitney U test was used for comparison between two independent groups that did not satisfy the normality, and the Kruskal–Wallis test was used for comparison between the three groups. The categorical data were analyzed using the chi-squared test. A multiple logistic regression analysis was used to evaluate the independent association of neurotoxicity with significant factors. All of the analyses were performed using SPSS version 20.0 (IBM Co., Armonk, NY, USA), and p

0.05 was considered to be statistically significant.ResultsComparison of neurotoxicity with the severity of CKD

Of the 401 patients, 355 (88.5%) patients were male and 46 (11.5%) patients were female. CKD stage 4, non-dialysis stage 5, and on-dialysis patients did not differ in age, sex, medication period, reason for medication, and neurotoxicity. There was a difference in diabetic nephropathy (p=0.029), daily dose (p=0.002), and total dose (p=0.005) (Table 1).

Factors associated with the development of baclofen neurotoxicity

We investigated whether the incidence of neurotoxicity was related to the patient’s baseline characteristics, underlying disease, laboratory data, baclofen dose and duration, and dialysis. Diabetic nephropathy (p=0.045), serum albumin (p=0.003), and baclofen total dose (p=0.041) were associated with neurotoxicity. Other factors were not associated with neurotoxicity (Table 2).

Baclofen dose and neurotoxicity by age

The patients were divided into two groups: those younger than 60 years of age and those older than 60 years. Baclofen doses did not differ between the daily doses, the dosing duration, and the total dose. There was no significant difference in the incidence of neurotoxicity (Table 3).

Factors independently associated with baclofen neurotoxicity

Diabetic nephropathy and serum albumin, which were associated with neurotoxicity, were analyzed using a multiple logistic regression analysis. As a result, serum albumin was independently associated with baclofen neurotoxicity (p=0.007), and diabetic nephropathy was not independently associated (Table 4).

Clinical characteristics of patients with neurotoxicity

Twenty-six (92.9%) patients received baclofen to treat hiccups, and two (7.1%) patients were treated for muscle spasms. Regarding the prescribed place, the inpatient prescription was the most common (92.9%). Mental alteration was present in 26 (92.9%) patients, and seizure occurred in five (17.9%) patients. The time to symptom onset was 39.5 (9.0, 240.0) h, and the duration of symptom was 2.0 (1.0, 16.0) days. Four (14.3%) patients received treatment in the ICU for 17.5 (5.0, 35.0) days. One patient (Table 5, #7) had community-acquired pneumonia and received ventilatory treatment in the ICU. He started taking baclofen to control hiccups. After 41h, complete sedation and loss of spontaneous breathing were observed, and there was no change in the sedation drug dose. There was no specific finding on brain imaging, and he recovered after 12 days of ceasing baclofen treatment. Three (10.7%) patients had used the ventilator for baclofen neurotoxicity for 12.0 (8.0, 27.0) days. A total of 15 (53.6%) patients underwent hemodialysis (number of dialysis, 2.0 [1.0, 7.0] times) for the treatment of baclofen neurotoxicity. One patient applied continuous renal replacement therapy in the ICU (Table 5, #12). Two (7.1%) patients underwent therapeutic peritoneal dialysis for 3.0 (2.0, 4.0) days (Table 27, #28). Patients who had been on dialysis continued to receive dialysis for 3.0 (1.0–7.0) years. Among them, 10 patients (35.7%) had hemodialysis, and two patients (7.1%) had peritoneal dialysis (Table 6).

Of the patients with baclofen neurotoxicity, the lowest total dose was 5mg in patients who received peritoneal dialysis (Table 5, #28) and the highest total dose was 150mg in CKD stage 4 patients (Table 5, #6). The minimum daily dose for baclofen neurotoxicity was 10mg, 10mg, and 5mg, respectively, in patients with CKD stage 4, non-dialysis stage 5, and on-dialysis patients (Tables 6 and 7).

Baclofen dose according to the CKD stages in patients with neurotoxicity

Patients with baclofen neurotoxicity were divided into CKD stage 4, non-dialysis stage 5, and on-dialysis patients, and there was no significant difference between the three groups. The daily dosage was 10.0mg (10.0, 20.0), 12.5mg (10.0, 20.0), and 10.0mg (5.0, 20.0), and the total dosage was 20.0mg (10.0, 150.0), 30.0mg (10.0, 50.0), and 17.5mg (5.0, 100.0), respectively (Table 7).

Discussion

To our knowledge, this is the first study regarding the prevalence of baclofen neurotoxicity in patients with severe CKD. In this study, among 401 patients with severe CKD, 28 (7.0%) patients had baclofen neurotoxicity. However, there are, in fact, a number of other cases that have not been reported in the medical records because they are not as severe as compared with these patients. The baclofen neurotoxicity is not well known; there is no clearly defined dose reduction criterion, and there is a high likelihood of iatrogenic neurotoxicity. According to the results of this study, baclofen should be used with caution when the serum albumin level is low.

This is also the first study showing that hypoalbuminemia is the independent risk factor for baclofen neurotoxicity. About 30–35% of baclofen binds to protein, and what is actually working is free baclofen that does not bind to protein.17 For this reason, the lower the serum albumin, the higher the concentration of baclofen and the greater the likelihood of neurotoxicity. However, the study by Benet and Hoener28 showed that the level of protein-binding in plasma does not, in fact, affect patients; so, there is no need to adjust the concentration. Therefore, pharmacokinetic studies on baclofen, plasma protein, and albumin are necessary to define the exact mechanism. The concentration of baclofen can be measured using a gas chromatography/mass spectrometry or high-performance liquid chromatography on a blood sample, but the results are delayed and unusable as a toxicological screening test.1,14 In the future, good tests for monitoring baclofen dosage should be developed.

Because many other risk factors cause baclofen neurotoxicity besides renal function, it is difficult to precisely define the degree of renal dysfunction that might lead to contraindicate the use of baclofen medication.18 Su et al.4 and El-Husseini et al.1 recommended not using baclofen when the eGFR was

mL/min/1.73m2 and recommended lower doses and longer intervals when the eGFR was between 30mL/min/1.73m2 and 60mL/min/1.73m2. Roberts et al.3 recommended that baclofen be administered at the lowest dose, according to the manufacturer’s guidelines, in patients with mild CKD (eGFR >60mL/min/1.73m2). For patients with moderate or severe CKD (eGFR mL/min/1.73m2), baclofen is avoided. Vlovonou et al.5 suggested that baclofen daily doses should be reduced by 1/3, 1/2, and 2/3, respectively, because in mild, moderate, and severe CKD, baclofen removal rates are reduced by 34%, 49%, and 64%. Hadjiyannacos et al.25 recommended that patients on dialysis should not be given >5mg baclofen per day. According to Wolf et al.,29 when baclofen is difficult to use due to decreased kidney function, it may be replaced by cyclobenzaprine, tizanidine, and dantrolene for muscle spasm.

When patients with baclofen neurotoxicity were divided into CKD stage 4, non-dialysis stage 5, and on-dialysis patients, the median values of daily doses were 10.0mg, 12.5mg, and 10.0mg, respectively, and the minimum daily dosage was 10.0mg, 10.0mg, and 5.0mg, respectively. The median doses of medication up to symptom onset were 20.0mg, 30.0mg, and 17.5mg, respectively (Table 7). Vlovonou et al.5 recommended a baclofen dose of 2.5mg q 12h for severe CKD mL/min/1.73m2eGFR. However, according to the results of this study, it may be possible to use up to 7.5mg in patients with CKD stages 4 and 5 (non-dialysis), and 2.5mg in dialysis patients.

In the case of diabetic nephropathy, which showed significant results when analyzed using a chi-squared test for neurotoxicity according to the underlying disease of the patient, a multiple logistic regression analysis showed no significant results (Tables 2 and 4). According to the American Diabetes Association, diabetic nephropathy is a clinical diagnosis made based on the presence of albuminuria and/or reduced eGFR in the absence of signs or symptoms of other primary causes of kidney damage.30 The stage of albuminuria is divided by measuring the albumin-creatinine ratio, which is defined as normal =30–299, and overt proteinuria ≥300 (mg/g creatinine). Moreover, >0.5g of proteinuria in 24h occurs in 15–40% of people with type 1 diabetes and 5–20% of people with type 2 diabetes.31 Although the amount of total proteinuria in patients with diabetic nephropathy is typically subnephrotic (g/24h), in some earlier studies of patients with type 1 and type 2 diabetes and nephropathy, as many as 70–80% patients had nephrotic range proteinuria.32 In patients with diabetic nephropathy, severe proteinuria leads to hypoalbuminemia, and hypoalbuminemia is a risk factor for baclofen neurotoxicity. For this reason, a multiple logistic regression analysis that controlled the influence of serum albumin could be interpreted as showing no significant results in diabetic nephropathy.

The male population was overwhelmingly large in the entire population receiving baclofen, but the interpretation is not clear. There are reports that cisplatin-induced hiccups are common in men (97.4%).33 In Cymet’s study of hiccups,34 91% of the population was male, but the reason was unclear. In many other studies, the majority of people with hiccups were males.35,36 There is a reason why hiccups are more likely to occur in men, but it is not yet clear. In this study, 93.0% (373) of the patients received baclofen because of hiccups, which seems to account for the male majority (Table 1).

The total dose was significantly lower in the neurotoxic group (p=0.041) (Table 2), which was perceived to be due to the early drug withdrawal in patients with neurotoxicity. In the neurotoxic group, the median dose of daily baclofen was 10.6mg (Table 2). In the study by El-Husseini et al.,1 the mean value of the daily dose was 20mg, which was different from that in this study. The median time to symptom onset after baclofen treatment was 39.5h, which was shorter than the outcome found by El-Husseini et al.1 (Table 6).

This study has potential limitations. First, the major limitation of this study is its unicentric, retrospective, and observational nature, which may have inherent selection bias including controlling the dosage of baclofen or the characteristics of the patient. However, because of ethical issues, prospective research including dose control may be difficult in the future. Second, it is impossible to completely exclude the history of CNS diseases and the effects of other drugs that affect the CNS. Although CNS disease and CNS drugs were found to be unrelated to neurotoxicity (Table 2), 26 out of 28 baclofen neurotoxic patients took drugs that affect the CNS (Table 5). CNS drugs can be a confusing variable, so this requires careful attention to interpretation.

Conclusions

The prevalence of baclofen-induced neurotoxicity in patients with severe CKD was 7.0% (28 of 401 patients). Serum albumin is an independent risk factor for neurotoxicity, and baclofen should be used cautiously in patients with hypoalbuminemia. In the studied population, it was found that a lower baclofen dose such as 7.5mg in patients with CKD stages 4 and 5 (non-dialysis) and 2.5mg in patients who receive dialysis was associated with the presence of fewer adverse effects.

Conflicts of interest

The authors have no conflicts of interest to declare.

Efficacy and Tolerability of Baclofen in Substance Use Disorders on JSTOR

Background: It has been reported that baclofen, a drug used in the treatment of spasticity, reduces the severity of withdrawal symptoms and substance use disorders (SUDs) for some psychoactive drugs. Aims and Methods: To evaluate the effectiveness and safety of baclofen in the treatment of withdrawal syndrome and/or SUDs, providing (1) an outline of its pharmacological features; (2) a summary of studies that have suggested its possible effectiveness in the treatment of SUDs, and (3) a review of randomized, controlled trials (RCTs) on baclofen and SUDs. Results: Baclofen tolerability is generally considered to be good. Eleven RCTs investigated its effectiveness in the treatment of SUDs. Of these, 5 RCTs found that baclofen is effective, 5 RCTs found that it is ineffective and the results of 1 RCT were not appreciable because it did not achieve the preplanned level of participation. Conclusion: The number of RCTs on baclofen and SUDs is still low, and their results are divergent. Further RCTs should be undertaken, particularly with higher doses of baclofen. Its administration may be suggested in patients who fail to respond to other approved drugs or who are affected by liver disease that prevents their administration, or in patients affected by SUDs for which no approved drugs are available. Treatment should be conducted under strict medical supervision.

Journal Information

European Addiction Research is a unique international scientific journal for the rapid publication of innovative research covering all aspects of addiction and related disorders. Representing an interdisciplinary forum for the exchange of recent data and expert opinion, it reflects the importance of a comprehensive approach to resolve the problems of substance abuse and addiction in Europe. Coverage ranges from clinical and research advances in the fields of psychiatry, biology, pharmacology and epidemiology to social, and legal implications of policy decisions. The goal is to facilitate open discussion among those interested in the scientific and clinical aspects of prevention, diagnosis and therapy as well as dealing with legal issues. An excellent range of original papers makes European Addiction Research the forum of choice for all.

90,000 Baclofen for alcohol abuse disorder

Review question

We reviewed the evidence for the efficacy and safety of baclofen for the treatment of people with alcohol abuse disorder (ADD) who continue to drink (use alcohol), to achieve and maintain sobriety (to stop drinking), or to reduce alcohol consumption.

RIA and other alcohol-related disorders are among the most common mental disorders resulting in specific physical and emotional problems, learning and memory problems, and consequences for general well-being and health.Alcohol abuse is one of the greatest health risks worldwide, causing 20% ​​to 30% of esophageal cancer, liver disease, epilepsy, road traffic accidents, homicide and other intentional injuries.

Psychosocial strategies have been the main treatment for RLA for many years, but the use of psychosocial therapies alone has had limited success. Most people with RAD do not respond at all to treatment, and those who do do not stay alcohol free in the long term.Medicines such as baclofen can play an important role in the treatment of people with RUA.

Search date
Evidence is current to January 2018.

Research characteristics

In this review, we reviewed 12 randomized clinical trials (studies in which participants were randomly assigned to one of two or more treatment groups and a control group) with 1128 participants.On average, the interventions lasted about 5 months, while the researchers followed the participants for 4 to 52 months. Five studies were conducted in the United States and one each in Australia, France, Germany, India, Israel, Italy, and the Netherlands.

Studies have looked at different doses of baclofen (from 10 mg per day to 150 mg per day), and in some cases the doses have been increased during treatment. None of the studies added other medications or other treatments to the baclofen treatment.All studies compared baclofen to placebo, with the exception of one study that compared baclofen to acamprosate 666.66 mg three times daily for three months.

Main Findings
Compared to placebo, baclofen has little or no effect on participants who drop out (drop out), refuse treatment because of adverse events (side effects), or the number of participants with at least one adverse event.Baclofen likely has little effect on the number of participants who start drinking again, as well as how much and how often they drink. Baclofen may have little or no effect on the percentage of days people stay free from alcohol.

Baclofen appears to increase alcohol consumption, as measured by the number of “drinks” (drinks) per day.

We found that baclofen increased the incidence of adverse events such as depression, dizziness, drowsiness, numbness, and muscle stiffness, but we found no significant differences between baclofen and placebo for other adverse events.

Certainty of the evidence
Certainty of the evidence (how confident we can be that the evidence is reliable) was high in terms of the number of participants with at least one adverse event, and that people dropped out of research for any reason or because of adverse events. The certainty of the evidence was moderate for results that people returned to drinking and how many days of alcohol abuse they had.It was low in terms of results on the number of “drinks” (drinking) on ​​the day of alcohol abuse and on the percentage of days of sobriety (no alcohol).

Baclofen (baclosan) – one of the most affordable drugs

Description

Description of properties of Baclofen: the drug reduces the excitability of the terminal sections of muscle fibers, suppresses intermediate neurons, inhibits nerve impulses, reduces muscle tension. However, it does not affect neuromuscular transmission.

The drug weakens skin and tendon reflexes, spasms and convulsions, increases the range of motion of the joints, facilitates the ongoing kinesitherapy (massage, exercise, manual therapy). It also has a mild pain relieving effect.

Registration number:

Trade name of the preparation: BAKLOSAN®
International non-proprietary name: baclofen | baclofen
Chemical name: 4-amino-3- (4-chlorophenyl) -butyric acid

Dosage form:

Tablets

Baclofen and its chemical formula

Baclofen is a muscle relaxant that consists of potent components.Each tablet contains:

• Magnesium stearate.
• Lactose.
• Gelatin.
• Potato starch.
• Baclofen (10 or 25 mg.).
• Ethyl cellulose.

Chemical formula of the substance C10h22ClNO2. It can only be reproduced under laboratory conditions.

Release form

White tablets, round, biconvex with a dividing line.

Composition

Baclofen contains an active ingredient with the international name Baclofen, its dosage in a tablet can be 10 or 25 mg.

Pharmacology

The drug is capable of providing muscle relaxant, analgesic and antispastic action.

Pharmacological action

The active ingredient of the drug reduces the excitability of nerve fibers and suppresses polysynaptic and monosynaptic impulse transmission, as well as inhibits intermediate neurons. Due to this, the drug reduces the tension of the muscle spindles, and at the same time does not affect the neuromuscular transmission.

Pharmacokinetics

Baclofen is rapidly absorbed and widely distributed throughout the body.Biotransformation is very limited, and most (85%) of the active ingredient is excreted unchanged, mainly in the urine. More lipophilic than GABA due to its halogenated aromatic groups, baclofen has a weak ability to cross the blood-brain barrier.

The molecule tends to pass into breast milk. The half-life is 3 to 4 hours. Peak serum levels are reached after 30 minutes to 1 hour 30 minutes. About 30% binds to plasma proteins.85% of the dose is excreted intact and 15% is metabolized primarily through deamination. With an oral dose of 40 mg, 80% of the dose is excreted within 24 hours, primarily through renal excretion in an unmetabolized form. A small part is excreted in the faeces.

The history of the drug

Originally Baclofen was created as a drug for the treatment of epileptic diseases. The substance was first synthesized by the large Swiss company Ciba-Geigy in 1962 by the famous pharmaceutical chemist Heinrich Keberle.Despite the fact that the drug did not succeed in the treatment of epilepsy, it had a positive effect on the condition of patients who previously had:

• Stroke.
• Muscle spasms.
• Traumatic brain injury.

The synthesized drug was originally intended to be used only by the oral route, but the intrathecal method made it possible to achieve more effective treatment, without the side effects that could occur with the usual swallowing of tablets.Currently, Baclofen is used to treat a variety of diseases.

Mechanism of Action

Baclofen is a muscle relaxant due to its beneficial effects on neuromuscular function. The drug also has antispastic, antidepressant and analgesic effects. Removal of spasticity in the presence of neurological disorders is a necessary measure. Drug treatment carried out by means of Baclofen is accompanied by massage, kinesitherapy, therapeutic exercises, diet, psychotherapy sessions.

The muscle relaxant effect is manifested by stress relief, anesthesia, elimination of convulsive syndrome. The tablet is absorbed in the gastrointestinal tract. Withdrawal of Baclofen from the body occurs 70-73 hours after ingestion. The drug easily penetrates the blood-brain barrier. The active ingredient binds to blood proteins. Baclofen works for 6-8 hours. It should not be taken by pregnant women or nursing mothers.

Baclofen activates GABA B receptors, making the patient indifferent to alcohol.Today, scientists are conducting fundamental research, as a result of which they hope to determine the presence of neural correlates. According to neurologists, it is they who contribute to the elimination of the irrepressible desire to abuse alcohol uncontrollably.

In case of an overdose of Baclofen, the central nervous system is suppressed, which is especially dangerous for persons suffering from chronic neurological pathologies. Therefore, it is strictly forbidden to change the prescribed dosage and course of administration. If you feel unwell, you should immediately contact your doctor.

Effects on the body

Once inside the body, the drug Baclofen has a strong effect on the central nervous system and the work of internal organs in general. An hour later, a person who has taken 6 to 14 tablets has an unnatural activity and a feeling of joy. The patient has a burst of energy, increased efficiency and no need for rest. This effect lasts about 1.5–2 hours after which drowsiness, dizziness and headaches appear, as well as hand tremors.

Principle of action of Baklosan

The drug has an inhibitory effect on GABA-B receptors, in other words, inhibitory mediators. Scientists have shown that these receptors regulate the sensation of euphoria during alcohol intoxication. Muscle tone is reduced by impulses passing from effector cells to neurons. The nervous system under the influence of Baklosan is depressed, the muscles relax and the pain or cramps associated with the tone stop.

Baklosan – an effective antispasmodic

Indications for the use of the medicine can be:

• infectious diseases;
• sciatica;
• osteochondrosis;
• degenerative changes;
• benign and malignant formations;
• injuries to the limbs, back;
• Pain syndrome caused by spasms.

The drug is often prescribed for strokes, meningitis, cerebral palsy. Baklosan is produced in the form of tablets of 10 and 25 mg, respectively. It is necessary to take the medicine strictly according to the prescription of a specialist, who calculates the maximum daily dose based on the patient’s disease, his condition and the characteristics of the body.

As a rule, the maximum therapeutic dose is 15 mg, divided into three daily doses. People with renal failure and diabetes mellitus should not exceed a dose of 5 mg, otherwise intoxication cannot be avoided, and the body’s reaction can lead to irreparable consequences.

Before using Baklosan, do not forget to read the instructions.

If no undesirable effects are found within three days of taking Baklosan, and the patient normally tolerates treatment, feels the effect, then the daily dose is gradually increased by 5 mg, not exceeding the maximum allowable dose of 100 mg per day. For children aged three to ten years, the maximum therapeutic dose is no more than 25 mg, and for older children, the dose is calculated according to the formula 2.5 mg per 1 kg of body weight (no more than 75 mg per day).

Expected results

Baclofen cannot be attributed to psychotropic and narcotic drugs, therefore, dependence arising from prolonged use of the medication is considered a manifestation of substance abuse. The onset of her symptoms is a good reason to visit a specialist. In this case, a specific treatment will be prescribed, including detoxification of the body.

When used correctly, the psychoactive drug helps to relieve alcohol cravings and improve the patient’s well-being.It stabilizes the state of the central nervous system, relieves pain, accelerates the regeneration of damaged tissues. Since 2014, Baclofen has been used as a medication that can eliminate alcohol dependence. It is most commonly used to treat alcohol withdrawal symptoms.

The question of the benefits of this drug is still being considered. French physician O. Amesen proved from his own experience that Baclofen works. Through this drug, he managed to suppress alcohol dependence, which arose against the background of a psychological disorder.Some neurologists believe that a synthetic drug is not able to get rid of addiction for a long time, without reducing the functionality of vital organs.

Indications for the use of Baclofen

Indications for the use of Baclofen are neurological diseases caused mainly by spinal cord injuries. The drug is used for diseases accompanied by skeletal muscle spasms. These may be:

• traumatic brain injury,
• multiple sclerosis,
• strokes,
• meningitis,
• cerebral palsy,
• affective disorders of alcoholism.

Baclofen is also prescribed for spinal diseases of various origins – degenerative, infectious, tumor, traumatic. In order to prevent the above diseases, Baclofen is not used.

Baclofen as a muscle relaxant

Since 1975 Baclofen has been approved for the treatment of spastic contractures (involuntary muscle contraction) of cerebral origin or neurological disorders such as multiple sclerosis or after spinal cord injury with severe chronic spasticity (infectious, degenerative, traumatic, neoplastic) , or secondary contractures associated with cerebral palsy.
Baclofen has some efficacy in refractory hiccups.

Other indications of Baclofen

Baclofen is used to treat skeletal muscle spasticity in multiple sclerosis, in spastic conditions in diseases of the spinal cord of infectious, degenerative, traumatic genesis, as well as in infantile cerebral palsy.

Baclofen is also used to treat alcohol and drug addiction.

The drug is dispensed by prescription.

Instructions for the use of Baclofen

Method of administration of Baclofen: tablets are taken orally during meals. The initial dose is 5 mg three times a day, then it increases every three days by 5 mg. But at the same time it is necessary to ensure that the dose does not exceed 20-25 mg at a time. The maximum dose of the drug is 100 mg per day, but you need to take Baclofen only for a short time and in a hospital setting.

How much baclofen to take for patients with hypersensitivity, the doctor prescribes, usually in a lower dosage – about 5-10 mg per day and increase it more slowly.For children, Baclofen should be drunk at the rate of 0.75-2 mg per kilogram of weight. For adult men and women, the course of treatment with Baclofen is prescribed by a prescription specialist. Long-term use of Baclofen can be addictive. The drug is withdrawn slowly and gradually over a period of 1-2 weeks.

Dosages

Oral: To reduce muscle tone after injuries and in diseases of the spinal cord (such as spinal cord tumors, syringomyelia, motor neuron disease, transverse myelitis), in multiple sclerosis, cerebrovascular accident, cerebral palsy, meningitis and after traumatic brain injury.

The drug in the form of a solution for administration into the subarachnoid space is used in adults for the treatment of patients with severe chronic spasticity against the background of multiple sclerosis, with spinal cord injuries or traumatic brain injuries that cannot be effectively treated with oral baclofen, as well as in children at the age of 4-18 years with severe chronic spasticity of cerebral or spinal origin (against the background of trauma, multiple sclerosis or other diseases of the spinal cord) who do not respond to treatment with oral antispastic drugs (including oral baclofen) and / or who develop unacceptable side effects after the administration of effective doses of oral medications.

The dose depends on the patient’s illness, body weight, any other medical conditions and other medications taken. Taking into account the effect of the drug and the need to control its side effects, a slow increase in the dose is required. In neurology, baclofen is used in doses of 30-75 mg / day, and in hospitalized patients, the dose can reach 100-120 mg / day. The starting dose is usually 3 x 5 mg for the first 3 days. The dose is then increased to 3 x 10 mg for the next three days.And so on, in 10 mg increments up to the effective dose.

Baclofen can be taken up to 80 mg per day. However, very often doctors prescribe higher doses of the drug. Neurologists from Albert Einstein Universities and Columbia University have conducted studies of high doses of Baclofen (up to 300 mg per day) for several years in patients with muscle spasticity. Once the dose that produces the desired effect is reached, the body does not need to increase the dose to achieve the same effect, even after many years of use.

In case of alcohol withdrawal, Baclofen should be taken with a daily dose of 15 mg per day, then the dose is gradually increased by 5-10 mg every 2 or 3 days until the expected effect (reduction or cessation of alcohol consumption) appears. For a total dose of more than 120 mg per day, consult a physician experienced in the treatment of alcohol dependence.

For taking more than 180 mg per day, you should contact a center for supportive therapy and drug prevention or a specialized health care center.The maximum dose of Baclofen is 300 mg per day. When the goal is achieved while taking Baclofen, the dosage should be gradually reduced to the optimal level of efficacy (reduced alcohol consumption or abstinence at the lowest dosage). In the absence of a clinical response in the patient, treatment should be gradually discontinued.

Intrathecal injections: directly into the cerebrospinal fluid, using a subcutaneous implant, to increase the effectiveness of the active ingredient, reaching the sites of drug exposure, which are at the level of the spinal horn of the spinal cord.With this application, the first dose of the drug is administered epidurally to assess the effect.

Long-term administration of the drug is provided using a pump and a subcutaneous catheter, the dose is adjusted by the programmer and the doctor in accordance with the patient’s needs. This mode of administration is more effective if there is no therapeutic alternative in the treatment of severe spasticity, after failed oral administration of baclofen, or if effective doses cause central nervous system side effects.

This method is especially useful for patients with spinal cord injury or multiple sclerosis with painful spasms who cannot take Baclofen tablets or for patients with spastic diplegia (a form of cerebral palsy where the spasms can be controlled by regularly administering the drug through the implantable system). pump). When injected subcutaneously, baclofen pumps can cause infections. Because of the risks associated with withdrawal symptoms, with intrathecal administration, increased patient monitoring should be ensured.

Side effects

Baclofen is strictly forbidden to be taken by people with a history of:

Baclofen is contraindicated in case of gastric ulcer

• individual intolerance to the active and auxiliary substances;
• peptic ulcer of the stomach, esophagus or duodenum;
• psychotic disorders;
• pathologies, in the clinical picture of which there is a convulsive syndrome;
• Parkinson’s disease.

It is recommended to refuse taking the drug Baclofen for people over 65 years old. Ignoring these recommendations is fraught with more intense manifestation of adverse reactions.

They can also be caused by a sharp decrease in the dosage of Baclofen, its independent use (without the appointment of the attending physician), violations of the dosage regimen. On the part of the nervous system, symptoms such as:

• problems with sleep may occur;
• nightmares;
• loss of orientation in space;
• depressive disorder;
• hallucinations;
• chronic fatigue;
• euphoria;
• weakness throughout the body;
• mental overexcitement;
• confusion of consciousness;
• impaired coordination of movements.

Baclofen can have a negative effect on the cardiovascular system. The consequence of this is arterial hypertension, cardiac collapse, heart rhythm disturbances, painful sensations in the chest area. Side effects of Baclofen on the part of the digestive system include:

The drug may cause excessive sweating

• Loss of appetite;
• abdominal pain;
• taste change;
• dyspeptic disorder.

The negative effect of Baclofen on the genitourinary system is expressed by urinary incontinence (enuresis), impotence, lack of control over the emptying of the intestines and bladder, erectile dysfunction, premature ejaculation.

Baclofen can also provoke the appearance of:

• painful sensations in the muscles;
• excessive sweating;
• skin rashes;
• swelling of the limbs; 90 064 90 063 itching;
• the appearance of overweight;
• nasal congestion
• respiratory failure.

Baclofen impairs the ability to concentrate. Therefore, during the treatment period, it is necessary to limit the time spent driving and at the workplace. Otherwise, the likelihood of unpleasant consequences is high.

Taking the drug Baclofen is allowed only after consulting a doctor. Only he will be able to assess the advisability of prescribing a medication, which is characterized by an impressive list of side effects, to a person suffering from addiction.Treatment of alcoholism with Baclofen should take place in a stationary setting under the supervision of a physician. Subject to all prescriptions, addiction will not occur.

Signs of using baclofen

Signs of using baclosan for a long time:

• muscle spasticity;
• nausea and vomiting;
• asthenic condition;
• drowsiness and apathy;
• the appearance of dizziness and headaches;
• dry mouth;
• appearance of constipation up to one week;
• tremor of the limbs;
• illusions and hallucinations;
• depressed state.

How drug use affects the psyche

By using the drug in large quantities or in combination with other drugs or alcohol, a person falls into a psychedelic state. In simple terms, it is called a “trip”. This concept includes strange experiences, nervousness, persecution mania.

Baclofen toxicity

Most of the side effects are observed at the beginning of treatment. They usually disappear within a few days when the dosage stabilizes.

General: sedation, drowsiness, weakness and / or muscle pain, nausea. Sometimes: dry mouth, decreased blood pressure, dizziness, breathing problems, diarrhea, headache, insomnia, confusion, hyperventilation.

Rare: a feeling of well-being or, conversely, depression, imbalance, tremors, blurred vision, hallucinations and nightmares. Problems with attention are more prominent and often present in patients with renal insufficiency, including those after coma (five cases of intrathecal use described) and dialysis.

A clinical case of severe hypertriglyceridemia was reported in a patient taking Baclofen in conjunction with Risperidone, published in 2013. The first case of intoxication and coma, requiring at least three days of intensive care, was described in the United States in 1976. The patient took 900 to 970 mg of Lioresal to relieve the symptoms of Huntington’s disease.

Overdose

Side effects of the drug Baclofen were usually observed with its overdose.Manifest mainly in the form of vomiting and nausea, dizziness and gait disturbances, asthenia and confusion, dry mouth and gait disturbances, urinary retention, constipation or diarrhea, and decreased blood pressure.

In addition, apathy or euphoria, depression, hallucinations, paresthesias, maisthenia or myalgia, ataxia, nystagmus, tremors, enuresis, dysuria may occur. Convulsions may appear, or, conversely, a decrease in the convulsive threshold, muscle hypotension, and even coma.

With prolonged use of the drug, liver dysfunction may occur. Treatment used in case of an overdose of Baclofen is drinking plenty of fluids and taking diuretics, in case of respiratory depression, a ventilator is used.

Signs of poisoning

In most cases, the drug is well tolerated, however, sometimes Baklosan poisoning occurs, which manifests itself as:

• unstable mental;
• Disorders of the gastrointestinal tract – nausea, heartburn, upset stools or, conversely, constipation;
• disorder of the urinary-reproductive system;
• muscle weakness, tremor, impaired coordination of movement;
• impaired renal and liver function;
• convulsions.

An overdose of Baklosan can occur if the patient has sharply increased the dose of the drug on his own or, having missed one day of taking it, has taken a double dose. Most often, the consequences of an overdose are felt by children and elderly patients.

Disruption of the gastrointestinal tract – the first signs of poisoning with Baklosan

An overdose manifests itself in the form of hypotension for 72 hours or more, hypotension, depression, fainting, delusional states, hallucinations, in rare cases – a state of immobility and coma, pathological conditions in the form of a syndrome Cheyne-Stokes.Dangerous in case of an overdose is the suppression of the respiratory part of the brain. If oxygen stops flowing to the brain, then this will lead to the death of the organ and the death of a person.

Help in case of poisoning

There is no specific antidote for Baklosan overdose. If one or more symptoms of poisoning appear, the first step is to stop taking the medicine and get rid of the drug remaining in the body. Baclofen affects the spastic contractions of the stomach muscles and slows down the elimination of the drug from the body.However, gastric lavage should be continued.

You can give the patient 2 liters of salted water to drink and continue to induce the gag reflex by pressing the root of the tongue with your finger, after which you need to replenish the loss of fluid by the body. Enterosorbents are used to remove toxic substances. In the hospital, the hospital uses hydration therapy (Ringer’s solution and sodium chloride) with diuretics to reduce the dose of the drug in the body.

To stabilize the dropped blood pressure and the activity of the heart muscles, adrenaline or glucocorticoid hormones are administered to the patient and the respiratory activity is monitored.In some cases, artificial lung ventilation is used. Hospital treatment can last a week, or even longer, depending on the severity of the patient’s condition.

As a rule, Baklosan is well tolerated. To exclude an overdose and drug poisoning, you must adhere to the doctor’s recommendations and not self-medicate.

Fatal consequences of use and assistance in case of an overdose of Baclofen

The use of Baclofen as a drug is characterized by a strong overdose in order to achieve maximum pleasure and obtain hallucinations.Often, in pursuit of such sensations, patients receive oppression of the respiratory center and simply die.

People lose touch with the real world, their heart muscle and the vast majority of internal organs are disrupted. Also developing:

• Manic-depressive syndrome.
• Complete lack of connection with reality.
• Sociopathy.

According to experts, regular use of the drug in excessive doses for several weeks can lead to death.

In case of an overdose of Baclofen, act immediately. The optimal sequence of actions will be as follows:

• Call an ambulance.
• Provide fresh air supply.
• Rinse the diseased stomach.
• Give plenty of fluids.
• If ​​there is no pulse or breathing, take resuscitation measures.

There are no specific antidotes for this substance, therefore, the removal of intoxication consists in the elimination of its most dangerous manifestations.

Baclofen is a cheap, youth drug that leads to fatal consequences literally from the first use. Such a drug is easy to get and this makes it one of the most dangerous, which is why if your loved ones are addicted to the drug without the necessary evidence, then seek help.

Special instructions

It is necessary to clearly distinguish between the symptoms of the disease, which is treated with Baclofen, and the side effects of its administration, since they are similar. With concomitant epilepsy, treatment is carried out without discontinuing antiepileptic drugs.

In diabetes mellitus and liver diseases, the activity of liver transaminases, the level of glucose and alkaline phosphatase in the blood should be monitored regularly. During treatment, one should refrain from activities associated with the need for increased attention, quick reactions.

Baclofen for children

Baclofen is prohibited for children under 12 years of age.

Pregnancy and lactation

Category C. In pregnant women, use only if urgently needed.Excreted in breast milk; breastfeeding is not recommended during baclofen therapy.

Withdrawal symptoms

Abrupt discontinuation of baclofen can be dangerous. The most severe cases are associated with delirium. Withdrawal symptoms include: auditory, tactile or visual hallucinations, confusion, agitation, disorientation, fluctuations in levels of consciousness, insomnia, memory problems, anxiety, hypertension, hyperthermia, mood disorders, tachycardia, epileptic seizures, tremors.

No deaths have been reported with oral administration of Baclofen. A gradual dose reduction should be carried out exclusively under the supervision of a physician. Likewise, the dosage should not be changed during treatment without medical advice. The risks associated with discontinuation are increased with intrathecal administration.

Driving a car

Reduces the ability to drive vehicles and maintain mechanical equipment.

Drug interactions

Enhances the effect of antihypertensive drugs, and therefore may need to adjust their doses.Tricyclic antidepressants can potentiate the effects of baclofen and significantly reduce muscle tone. Strengthens the effect of ethanol and drugs that depress the central nervous system. Concomitant use with lithium salts can increase the patient’s motor hyperactivity.

Drugs that can impair renal function increase the T1 / 2 of baclofen, which is the cause of toxic effects. Patients with Parkinson’s disease, while using baclofen with levodopa and [carbidopa | carbidopa], may experience hallucinations, confusion, agitation.Baclofen prolongs fentanyl-induced analgesia.

The use of the drug in the form of a solution for injection into the subarachnoid space in combination with morphine can lead to a decrease in blood pressure. In such cases, the risk of respiratory disorders and disorders of the central nervous system cannot be ruled out. Concomitant use of intrathecal baclofen and general anesthetics (eg, fentanyl, propofol) may increase the risk of cardiac dysfunction and seizures.

Contraindications to use

The drug is contraindicated for use in Parkinson’s disease, psychosis, chronic renal failure, epilepsy, hypersensitivity, history of seizures. Baclofen can be used with caution in cerebrovascular insufficiency, cerebral atherosclerosis, gastric ulcer and duodenal ulcer.

During pregnancy and lactation, that is, during lactation, Baclofen should be taken under constant medical supervision.Particular care should be taken when using Baclofen in the elderly and in children under 12 years of age.

Baclofen – development of addiction

This drug is often used by patients to enhance other drugs, so it is often combined with alcohol. The development of addiction is due to the fact that the drug opens up potentially hidden opportunities in a person. Fears, complexes, depression, nervousness – all this disappears.

The addict is filled with energy and wants to do something exactly as long as the effect of the next dose lasts.Chemical dependence is not typical for this drug, the main threat is the development of psychological attraction.

The mechanism of development of addiction can be represented as follows:

• Drug use.
• Effects of the substance on the body.
• Feeling of euphoria.
• End of the pleasure effect.
• Repeated dose to restore the effect.

After the development of persistent mental dependence, a person feels bad without taking another dose.

Is Baklosan a drug?

You cannot take the drug for a long time, otherwise the drug is addictive, therefore many people recognize it as a narcotic drug. Those who stop using the drug abruptly do experience the so-called “withdrawal syndrome” familiar to drug addicts. The patient feels depressed, depressed, apathetic to everything, does not want to live, suicidal moods, anxiety, up to attacks of uncontrollable fear may appear.

It is necessary to stop taking the drug as gradually as to start. Abrupt withdrawal of the drug worsens the patient’s quality of life. Soreness returns, the mobility of the spine and limbs decreases. It seems to the patient that the pain has intensified, although in fact it has remained at the same level.

People with an unstable mental state need to be especially careful, and if the symptoms worsen, the help of a narcologist and sometimes even a psychiatrist is needed. You should not close your eyes to the patient’s depression, because it will not go away by itself and will only get worse.The sooner the patient seeks a specialist, the better.

How to treat addiction

Not every drug addict is able to fully realize his problem. The question of how to get off Baklosan is asked by a few. Addiction of this kind is very difficult to treat, accompanied by a variety of problems.

An attempt to independently refuse the drug leads to the development of the strongest withdrawal syndrome. The main symptoms are:

1. Severe atony;
2. Body aches;
3. Hallucinations;
4. Depression
5. Cephalalgia;
6. Pain in the lower and upper extremities;
7. Convulsions accompanied by loss of consciousness.

Only a competent doctor can help to get rid of addiction. In order for the patient to really feel better, special conditions will be required, created only in the relevant institutions.

Key aspects of Baklosan addiction

The drug is not physically addictive. Chemically, the product is completely safe, but baclofen, as an active ingredient, can cause a psychological need for the constant use of tablets.

It is known that Baklosan is able to multiply the euphoric effect of other drugs, so drug addicts “with experience” use it to enhance their feelings.Sometimes they try to combine a muscle relaxant with alcoholic beverages.

The use of a pharmacological product ultimately strongly affects the psyche. Psychedelic states, into which a person falls, are dangerous for himself and for people who are nearby. The effect that Baklosan produces is a “trip”, followed by a feeling of fear, nervousness, and persecution mania.

Physical dependence

Physical dependence manifests itself in muscle hypotonia, that is, the addict gains energy and strength, his consciousness becomes clear and precise.Then respiratory depression sets in, accommodation is disturbed, the pupillary reflex disappears, a feeling of anxiety and danger appears, so the addict begins to behave inadequately.

Deterioration of brain activity, digestion, respiratory system.

Consequences of taking Baclofen

Baclofen addiction is growing rapidly. Getting rid of it is not easy. The psyche disintegrates (is disturbed) due to persistent hallucinations, manic-depressive syndrome, obsessive states and a desire to commit suicide.The possibility of perceiving reality is lost, sociopathy is actively developing.

Overdose is common in people taking Baclofen tablets. This is with the desire to increase the dose. In case of an overdose, lethargy and drowsiness appear, loss of consciousness, respiratory depression, persistent hallucinations. All this speaks of the need for medical intervention, because such a condition can be fatal.

Tablets are harmful to the body – problems arise with the cardiovascular system, respiratory organs, and musculoskeletal functions.The physical disorders caused by the drug are often chronic. Mental abnormalities become incurable.

Treatment of dependence on baclofen

Baclofen has the effect of enhancing and prolonging the action of other drugs and alcohol, therefore it is most often used together with other types of drugs, or alcohol, this drug contributes to the development of polydrug addiction – a subtype of drug addiction, which is much harder to treat than others types of addiction.

Can I quit on my own?

Baclofen addiction is very difficult and problematic to treat. It is possible to save a drug addict only with the participation of competent specialists. Self-rejection of the drug entails atony, aches throughout the body, hallucinations, depression, headaches, pain in the extremities, loss of consciousness, convulsions.

Baclofen and alcohol

When Baclofen interacts with alcohol or drugs that affect the central nervous system, the sedative effect is enhanced.Hallucinations, confusion, increased agitation, and decreased muscle tone may appear. The interaction of Baclofen with antibiotics has not been identified.

Baclofen for alcohol dependence

The use of Baclofen in the treatment of certain addictions (including alcoholism) is currently being investigated. Since 2014, the drug has been temporarily approved for use in alcohol withdrawal. The use of baclofen for this indication is a controversial issue and the cause of medical controversy, one of the main characters of which is the French physician Olivier Amesen, who, being himself susceptible to alcohol dependence, took high doses of baclofen and achieved a general suppression of psychological alcohol dependence (drug addiction).

He first published his discovery in a medical journal, for which he had to carry out a certain public work to mobilize public opinion against the medical community. In fact, the Amesen Protocol, as opposed to the usual practice of using lower doses of Baclofen (to reduce addiction, not get rid of it), is being investigated in clinical trials, with many positive reviews from practitioners. Some attribute this resistance from the health authorities to the economic interests of certain companies, which may be at risk.

Action from Baclofen with alcohol

Strong dependence on Baclofen occurs at the time of its use with alcohol or withdrawal from drugs. Doses of the drug are increasing at a rapid rate. Most often, the drug is used by adolescents, because they are most susceptible to influence from their peers, and have many psychological problems that, they believe, can be solved with the help of drugs.

The mood changes dramatically – at first a person is in a peaceful and cheerful state, and then these states are replaced by aggression and irritability.Depression comes, and the feeling of happiness goes away. When taking Baclofen in a drug addict, there is a brightness of physical sensations, hallucinations, they sharply perceive the world around them.

Therapeutic effect and clinical studies

Baclofen for the treatment of alcoholism is presented in tablet form under the trade names Baklosan and Lioresal. The original pharmaceutical formulation was developed as a treatment for epilepsy. A positive effect was noted with high spasticity.Since 1990, clinical studies have begun on the use of the drug for alcoholism.

Promising results lacked laboratory confirmation and evidence. Doctor-cardiologist Olivier Amesen in 1992 applied the effect of high doses of the drug on himself to eliminate alcohol dependence. The addiction to alcoholic beverages was completely eliminated. Subsequently, a model of a therapeutic course was developed.

The French alcoholic society has requested more extensive research statistics.Amesen’s book, who described his personal experience of treatment, contains individual reviews of patients who follow the old course of the drug regimen. Most people who leave reviews on Internet forums report a persistent indifference to alcohol. It should be noted that there is also an opposite opinion of experts.

Chronic use of large doses of centrally acting drugs can cause a lot of side effects and provoke persistent dependence on drugs based on benzodiazepines.

The severity of the effect depends on the individual characteristics of the human body and the level of alcohol consumption during therapy. The latest clinical trials in 2014 were presented in France at a Paris conference. The developers of the drug announced the data on the study among 320 people. 57% of patients receiving the drug reduced the dose of alcohol consumption or completely stopped taking alcoholic beverages.

Efficacy of Baclofen for alcoholism

Drugs for alcoholism prevent the processing of alcohol.As a result, instead of the pleasure caused by intoxication, unpleasant sensations arise. The treatment regimen often includes substitution therapy drugs, opium receptor blockers, and antidepressants.

Properly conducted coding will avoid unnecessary irritation and despotism. Comprehensive treatment of alcoholism is prescribed for those who need psychotherapeutic and rehabilitation assistance. It takes a lot of effort to get rid of an addiction.

The treatment regimen with Baclofen is determined by a narcologist and psychiatrist.Baclofen helps relieve muscle cramps and reduce cravings for drinks containing ethanol.

The effectiveness of the drug has been proven experimentally. Clinical studies were carried out by French physicians. As a result, the participants began to adhere to a sober lifestyle. Baclofen is allowed to be taken even during a binge. The only condition is the timely adjustment of the single dose. Lack of constant monitoring during treatment is fraught with complications. Unfortunately, not everyone is allowed to use Baclofen.People at risk should not drink Baclofen.

Analogs of Baclofen

Substitutes for Baclofen with a similar effect can be found in pharmacies. These include:

Storage conditions

Baclofen should be stored out of reach of children at room temperature.

Shelf life

Shelf life of such preparations is 5 years from the date of manufacture.

Approximate price of the drug

Reviews of the drug Baclofen

Margarita, 38 years old: Once had meningitis.I remember that Baklosan was prescribed, but I heard that it was a drug, so I gave it up.

Rostislav, 56 years old: I have a complex form of prostatitis – with sclerosis. The pain was such that I wanted to commit suicide. No pain relievers helped. Only Baklosan solved my problems.

Baklosan is an effective antispasmodic based on the active ingredient baclofen. It is used to relieve cramps and spastic pain in muscles caused by diseases of the nervous system or the musculoskeletal system.It is necessary to take the drug strictly under the supervision of a doctor, not exceeding the dosage and adhering to the established instructions. If you take Baklosan uncontrollably, an overdose and its dangerous symptoms will not be long in coming.

Baclofen for prostatitis

Has anti-spasm and analgesic effect. Medication, it is good to combine it in folk methods, for more details on the page treatment of prostatitis with beesworm.

Sources

• https: // prostatit-faq.ru / lechenie / lekarstva / baklofen /
• https://lekotzyvy.com/preparat/b/baklosan/
• https://NetNarkotiki.ru/entsiklopediya-narkotikov/antidepressanty/baklofen-deshevyy-variantya.rasslabits
• http://vlagi.net/baklofen-ochen-effektiven-pri-lechenii-alkogolizma-podtverzhdeno
• http://lifebio.wiki/%D0%B1%D0%B0%D0%BA%D0%BB%D0 % BE% D1% 84% D0% B5% D0% BD
• http://alkogolu.net/lechenie/baklofen-dlya-lecheniya-alkogolizma.html
• http: // help-prostata.ru / kak-slezt-s-baklosana-instrukciya-po-primeneniyu /
• https://clinic-top.ru/entsiklopediya/%D0%91%D0%B0%D0%BA%D0%BB%D0%BE % D1% 84% D0% B5% D0% BD.html
• https://narko-info.ru/baklofen/
• https://MedExpert.guru/alco-lechit/baklofen-ot-alkogolizma.html

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Baclofen the drug and how it came about

Baclofen is a drug with analgesic and sedative effect, which is indicated for strokes, traumatic brain injuries, spasms, atherosclerosis and meningitis.However, due to its potent effect and euphoria, the remedy has become very popular in drug addiction circles.

Baclofen and its chemical formula

Baclofen is a muscle relaxant with potent ingredients. Each tablet contains:

• Magnesium stearate.
• Lactose.
• Gelatin.
• Potato starch.
• Baclofen (10 or 25 mg.).
• Ethyl cellulose.

Chemical formula of the substance C10h22ClNO2. It can only be reproduced under laboratory conditions.

The history of the drug

Initially, Baclofen was created as a treatment for epileptic diseases. The substance was first synthesized by the large Swiss company Ciba-Geigy in 1962 by the famous pharmaceutical chemist Heinrich Keberle. Despite the fact that the drug did not succeed in the treatment of epilepsy, it had a positive effect on the condition of patients who previously had:

• Stroke.
• Muscle spasms.
• Traumatic brain injury.

The synthesized drug was originally intended to be used only by the oral route, but the intrathecal method made it possible to achieve more effective treatment, without the side effects that could occur with the usual swallowing of tablets. Currently, Baclofen is used to treat a variety of diseases.

Medical Applications

Depending on the purpose, the medicinal product is used by several methods, namely:

Oral route:

• State of increased muscle tone.
• For tumors.
• Cerebral Palsy.
• Stroke.
• Meningitis.
• With alcohol withdrawal syndrome.

Intrathecal route (injection into the spinal cord):

• Pronounced static.
• Multiple sclerosis.
• Damage to the brain or spinal cord.

The intrathecal method can also be used if the patient has an intolerance to certain components when taken orally.

Signs of Baclofen Use

Due to the potent component, the drug is actively used by drug addicts of predominantly young age. The fact is that in case of an overdose, Baclofen has a strong, intoxicating effect.

To “get high” drug addicts take from 6 to 14 tablets at the same time and wash down with low alcohol drinks. After 30-40, narcotic intoxication occurs, which is accompanied by the following symptoms:

• Nausea and vomiting.
• Severe dry mouth.
• The appearance of visual and auditory hallucinations.
• Severe trembling of hands.
• Sleepiness.
• A state of complete apathy.
• Dilated pupils.
• Slurred speech.
• Dizziness.
• Impaired coordination of movements.

Baclofen is also frequently used by amphetamine addicts. The drug can easily dilute a synthetic analogue of cocaine, thus converting one dose into two.Addicts who take such a “mix” give off a strong feeling of euphoria, a surge of energy and auditory hallucinations.

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Effect on the body

Once inside the body, the drug Baclofen has a strong effect on the central nervous system and the work of internal organs in general.An hour later, a person who has taken 6 to 14 tablets has an unnatural activity and a feeling of joy. The patient has a burst of energy, increased efficiency and no need for rest. This effect lasts about 1.5–2 hours after which drowsiness, dizziness and headaches appear, as well as hand tremors.

Baclofen – development of addiction

This drug is often used by patients to enhance other drugs, so it is often combined with alcohol.The development of addiction is due to the fact that the drug opens up potentially hidden opportunities in a person. Fears, complexes, depression, nervousness – all this disappears.

The addict is filled with energy and wants to do something exactly as long as the effect of the next dose lasts. Chemical dependence is not typical for this drug, the main threat is the development of psychological attraction.

The mechanism of development of addiction can be represented as follows:

• Drug use.
• Effects of the substance on the body.
• Feeling of euphoria.
• End of the pleasure effect.
• Repeated dose to restore the effect.

After the development of persistent mental dependence, a person feels bad without taking another dose.

Fatal consequences of use and assistance in case of an overdose of Baclofen

The use of Baclofen as a drug is characterized by a strong overdose in order to achieve maximum pleasure and obtain hallucinations.Often, in pursuit of such sensations, patients receive oppression of the respiratory center and simply die.

People lose touch with the real world, they disrupt the activity of the heart muscle and the vast majority of internal organs. Also evolving:

• Manic-depressive syndrome.
• Complete lack of connection with reality.
• Sociopathy.

According to experts, regular use of the drug in excessive doses for several weeks can lead to death.

In case of an overdose of Baclofen, act immediately. The optimal algorithm of actions will be as follows:

• Call an ambulance.
• Provide fresh air supply.
• Rinse out a sick stomach.
• Give plenty of fluids.
• If ​​there is no pulse or breathing, take resuscitation measures.

There are no specific antidotes for this substance, therefore, the removal of intoxication consists in the elimination of its most dangerous manifestations.

Baclofen is a cheap, youth drug that leads to fatal consequences literally from the first use. Such a drug is easy to get and this makes it one of the most dangerous, which is why if your loved ones are addicted to the drug without the necessary evidence, then seek drug treatment.

Video What a drug addict looks like under baclofen

Baklosan: side effects, overdose, consequences

Baclosan is an effective antispasmodic based on the active ingredient baclofen.It is used to relieve cramps and spastic pain in muscles caused by diseases of the nervous system or the musculoskeletal system. It is necessary to take the drug strictly under the supervision of a doctor, not exceeding the dosage and adhering to the established instructions. If you take Baklosan uncontrollably, an overdose and its dangerous symptoms will not be long in coming.

Operating principle of Baklosan

The drug has a depressing effect on GABA-B receptors, in other words, inhibitory mediators.Scientists have shown that these receptors regulate the sensation of euphoria during alcohol intoxication. Muscle tone is reduced by impulses passing from effector cells to neurons. The nervous system under the influence of Baklosan is depressed, the muscles relax and the pain or cramps associated with the tone stop.

Baklosan – effective antispasmodic

Indications for the use of the medicine can be:

• infectious diseases;
• sciatica;
• osteochondrosis;
• degenerative changes;
• benign and malignant formations;

90,063 injuries to the limbs, back;

• pain syndrome caused by spasms.

The drug is often prescribed for strokes, meningitis, cerebral palsy. Baklosan is produced in the form of tablets of 10 and 25 mg, respectively. It is necessary to take the medicine strictly according to the prescription of a specialist, who calculates the maximum daily dose based on the patient’s disease, his condition and the characteristics of the body.

As a rule, the maximum therapeutic dose is 15 mg, divided into three daily doses. People with renal failure and diabetes mellitus should not exceed a dose of 5 mg, otherwise intoxication cannot be avoided, and the body’s reaction can lead to irreparable consequences.

Before using Baklosan, do not forget to read the instructions

If, within three days of taking Baklosan, no undesirable effects were found, and the patient normally tolerates the treatment, feels the effect, then the daily dose is gradually increased by 5 mg, not exceeding the maximum allowable dose of 100 mg per day. For children aged three to ten years, the maximum therapeutic dose is no more than 25 mg, and for older children, the dose is calculated according to the formula 2.5 mg per 1 kg of body weight (no more than 75 mg per day).

Is Baklosan a drug?

It is impossible to take the drug for a long time, otherwise the drug is addictive, therefore many recognize it as a narcotic drug. Those who stop using the drug abruptly do experience the so-called “withdrawal syndrome” familiar to drug addicts. The patient feels depressed, depressed, apathetic to everything, does not want to live, suicidal moods, anxiety, up to attacks of uncontrollable fear may appear.

It is necessary to stop taking the drug as gradually as to start. Abrupt withdrawal of the drug worsens the patient’s quality of life. Soreness returns, the mobility of the spine and limbs decreases. It seems to the patient that the pain has intensified, although in fact it has remained at the same level.

People with an unstable mental state need to be especially careful, and if the symptoms worsen, the help of a narcologist and sometimes even a psychiatrist is needed. You should not close your eyes to the patient’s depression, because it will not go away by itself and will only get worse.The sooner the patient seeks a specialist, the better.

Mechanism of action of Baklosan

Contraindications Baklosan

The drug is usually not prescribed for people suffering from psychosis and epileptic seizures. Baklosan is contraindicated in Parkinson’s disease, atherosclerosis, stomach ulcer, individual intolerance to the components of the drug, as well as during pregnancy and during breastfeeding.

The effect of baclofen on fetal development has not yet been studied, so it is not recommended to take it during pregnancy.For the same reason, during the period of taking the medicine, it is worth refusing to breastfeed. The drug is quickly absorbed into the bloodstream and enters the baby’s body, which can lead to unknown consequences.

It is forbidden to take alcohol during treatment with Baklosan. Alcoholic beverages can cause toxicity and aggravate side effects. Baclofen with ethanol has a hypotensive effect, in other words, it causes drowsiness, muscle weakness, hypotension, and hallucinations.

It is undesirable for people suffering from alcoholism to take Baklosan.A person who drinks cannot adequately assess his condition, and outsiders can take poisoning for the result of alcohol intoxication. In addition, in alcohol addicts, in most cases, liver and kidney dysfunctions are observed, and baclofen can only aggravate their condition. Outwardly, intoxication can manifest itself in yellowing of the sclera, jaundice and itching of the skin.

Indications for Baklosan’s use

Signs of poisoning

In most cases, the drug is well tolerated, however, sometimes Baklosan poisoning occurs, manifested in the form:

• unstable mental;
• disorders of the gastrointestinal tract – nausea, heartburn, upset stools, or, conversely, constipation;
• disorder of the urinary system;
• muscle weakness, tremor, impaired coordination of movement;
• impaired activity of the kidneys and liver;
• convulsions.

An overdose of Baklosan can occur if the patient has sharply increased the dose of the drug on his own or, having missed one day of taking, took a double dose. Most often, the consequences of an overdose are felt by children and elderly patients.

Disruption of the gastrointestinal tract – the first signs of poisoning with Baklosan

An overdose manifests itself in the form of hypotension for 72 hours or more, hypotension, depression, fainting, delusional states, hallucinations, in rare cases – a state of immobility and coma, pathological conditions in the form of Chain-Stokes syndrome.Dangerous in case of an overdose is the suppression of the respiratory part of the brain. If oxygen stops flowing to the brain, then this will lead to the death of the organ and the death of a person.

Help with poisoning

There is no specific antidote for Baklosan overdose. If one or more symptoms of poisoning appear, the first step is to stop taking the medicine and get rid of the remaining drug in the body. Baclofen affects the spastic contractions of the stomach muscles and slows down the elimination of the drug from the body.However, gastric lavage should be continued.

You can give the patient 2 liters of salted water to drink and continue to induce the gag reflex by pressing the root of the tongue with your finger, after which the body needs to replenish the loss of fluid. Enterosorbents are used to remove toxic substances. In the hospital, the hospital uses hydration therapy (Ringer’s solution and sodium chloride) with diuretics to reduce the dose of the drug in the body.

To stabilize the fallen blood pressure and the activity of the heart muscles, the patient is injected with adrenaline or glucocorticoid hormones and monitored for respiratory activity.In some cases, artificial lung ventilation is used. Hospital treatment can last a week, or even longer, depending on the severity of the patient’s condition.

As a rule, Baklosan is well tolerated.