Uses for baclofen. Baclofen: Uses, Dosage, Side Effects, and Addiction Treatment Potential

24.08.202327.06.2023 by alexxlab

What is baclofen used for. How does baclofen work for muscle spasms and addiction. What are the side effects and proper dosage of baclofen. How effective is baclofen for alcohol and drug addiction treatment.

Содержание

What Is Baclofen and How Does It Work?

Baclofen is a prescription muscle relaxant medication that goes by brand names like Kemstro and Lioresal. It was originally synthesized in 1962 as a potential treatment for epilepsy. While it proved only minimally effective for seizures, baclofen found widespread use in treating muscle spasticity caused by multiple sclerosis, spinal cord injuries, and other neurological conditions.

The primary mechanism of action for baclofen is as an agonist of GABA-B receptors in the central nervous system. By activating these receptors, baclofen produces muscle relaxation, pain relief, and improved muscle movement in patients with spasticity disorders. Its ability to modulate GABA neurotransmission also underlies its potential applications in addiction treatment.

FDA-Approved Uses of Baclofen

The U.S. Food and Drug Administration (FDA) has approved baclofen for the following medical uses:

Treating muscle spasms caused by multiple sclerosis
Relieving muscle spasticity due to spinal cord injuries or diseases
Improving muscle movement in patients with neurological disorders

For these approved indications, baclofen helps relax tense and rigid muscles, alleviate pain associated with muscle spasms, and enhance mobility and range of motion for patients. It is considered an effective first-line treatment option for spasticity in many cases.

How quickly does baclofen take effect?

Baclofen is absorbed rapidly from the gastrointestinal tract after oral administration. Peak concentrations in the bloodstream typically occur within 1-3 hours of taking the medication. However, the full therapeutic effects may take several days to manifest as the body adjusts to the medication. Doctors often start patients on a low dose and gradually increase it over time to minimize side effects.

Baclofen Dosage and Administration

Proper dosing of baclofen is crucial for maximizing its benefits while minimizing potential side effects. Here are some key points regarding baclofen dosage:

Initial doses are typically low, starting at 5 mg taken 3 times per day
The dose is gradually increased over several weeks as tolerated
Most patients require 40-80 mg per day divided into 3-4 doses
The maximum recommended daily dose is 100 mg unless under close medical supervision
Dosage adjustments may be needed for elderly patients or those with impaired kidney function
Abrupt discontinuation should be avoided – doses are tapered down slowly over 1-2 weeks

It’s important to follow the prescribed dosing regimen carefully and not adjust doses without consulting a healthcare provider. Taking more than the recommended amount of baclofen can increase the risk of adverse effects.

How long does baclofen stay in your system?

Baclofen has a relatively short half-life of 3-4 hours in plasma. This means that about half of the drug is eliminated from the bloodstream within that timeframe. However, the duration of effects may last longer. Most of the drug is excreted unchanged in the urine within 24 hours of the last dose. Factors like kidney function, age, and dosage can influence how long baclofen remains detectable in the body.

Common Side Effects of Baclofen

While generally well-tolerated, baclofen can cause some side effects, especially when first starting treatment or adjusting doses. Common side effects may include:

Drowsiness and sedation
Dizziness
Weakness
Fatigue
Nausea
Headache
Confusion
Insomnia

These effects are usually mild and transient, often improving as the body adjusts to the medication. However, if side effects persist or worsen, it’s important to consult a healthcare provider.

Are there any serious side effects of baclofen?

While rare, baclofen can potentially cause more severe adverse reactions in some individuals. Serious side effects that require immediate medical attention include:

Seizures
Difficulty breathing
Severe allergic reactions (anaphylaxis)
Severe mood changes or hallucinations
Suicidal thoughts

Patients should be monitored closely when starting baclofen therapy and report any concerning symptoms to their doctor promptly. Certain individuals, such as those with a history of seizures or psychiatric disorders, may be at higher risk for serious side effects.

Baclofen Interactions and Precautions

Baclofen can interact with various medications and substances, potentially altering its effectiveness or increasing the risk of side effects. Some notable interactions include:

Alcohol – can enhance CNS depression
Opioids – may increase respiratory depression
Tricyclic antidepressants – can potentiate muscle relaxation
Antihypertensive drugs – may enhance blood pressure-lowering effects
NSAIDs – can increase the risk of kidney problems
Lithium – may alter lithium levels

Additionally, certain populations should use baclofen with caution or avoid it altogether:

Pregnant women, especially during the first trimester
Breastfeeding mothers
Individuals with severe psychiatric disorders
Patients with active peptic ulcers
Those with severe liver disease
People with porphyria

Always inform your healthcare provider about all medications, supplements, and medical conditions before starting baclofen therapy.

Can baclofen be taken during pregnancy?

Baclofen use during pregnancy is generally not recommended, especially during the first trimester. Animal studies have shown potential risks to fetal development, and the drug can cross the placental barrier. While human data is limited, the potential risks to the fetus outweigh the benefits in most cases. Women who are pregnant or planning to become pregnant should discuss alternative treatment options with their healthcare provider.

Baclofen Withdrawal and Dependence

Although baclofen is not considered addictive in the traditional sense, abrupt discontinuation can lead to withdrawal symptoms. This is particularly true for patients who have been taking high doses or using the medication long-term. Baclofen withdrawal symptoms may include:

Anxiety and agitation
Confusion
Hallucinations
Seizures
Increased muscle spasticity
Fever
Tachycardia (rapid heart rate)

To prevent these potentially dangerous withdrawal effects, baclofen should always be tapered off gradually under medical supervision. The typical tapering period is 1-2 weeks, but may be longer for patients on high doses or with a history of withdrawal symptoms.

How to safely discontinue baclofen?

The safest way to stop taking baclofen is under the guidance of a healthcare provider. A typical tapering schedule might involve reducing the daily dose by 10-20% every 2-3 days. The exact timeline and reduction amounts will depend on the individual’s current dose, duration of use, and overall health status. It’s crucial to follow the prescribed tapering plan and report any withdrawal symptoms that occur during the process.

Baclofen in Addiction Treatment: An Emerging Application

In recent years, baclofen has gained attention as a potential treatment for alcohol and drug addiction. This off-label use was sparked by French cardiologist Olivier Ameisen’s 2009 memoir detailing his personal recovery from alcoholism using high-dose baclofen. Since then, numerous studies have explored the efficacy of baclofen in addiction treatment.

The proposed mechanism for baclofen’s anti-addictive properties involves its action on GABA-B receptors, which may help reduce cravings and anxiety associated with substance withdrawal. Some potential benefits of baclofen in addiction treatment include:

Reducing alcohol cravings and consumption
Easing withdrawal symptoms from various substances
Potentially decreasing anxiety and depression in recovering addicts
Helping to maintain abstinence in some patients

While promising, it’s important to note that baclofen’s use in addiction treatment is still considered experimental. More large-scale clinical trials are needed to establish its efficacy and safety for this purpose.

How effective is baclofen for alcohol addiction?

The effectiveness of baclofen for alcohol addiction remains a topic of ongoing research and debate. Some studies have shown promising results, with baclofen helping to reduce alcohol cravings and consumption in certain patients. A 2018 meta-analysis published in the journal Addiction found that baclofen may be effective in promoting abstinence and reducing heavy drinking days in patients with alcohol use disorder. However, results have been mixed, and not all studies have shown significant benefits. The optimal dosing regimen and patient selection criteria for baclofen in alcohol addiction treatment are still being investigated.

Future Directions and Research

As interest in baclofen’s potential for addiction treatment grows, several areas of research are being pursued:

Optimizing dosing protocols for addiction treatment
Identifying genetic or physiological markers that may predict response to baclofen therapy
Exploring combinations of baclofen with other medications or psychosocial interventions
Investigating baclofen’s potential in treating other forms of addiction beyond alcohol
Developing new formulations of baclofen with improved pharmacokinetics or reduced side effects

These ongoing studies aim to clarify baclofen’s role in addiction medicine and potentially expand its therapeutic applications.

What are the latest developments in baclofen research?

Recent research has focused on several aspects of baclofen use:

High-dose baclofen protocols for alcohol use disorder
Baclofen’s potential in treating cocaine and methamphetamine addiction
The role of baclofen in reducing anxiety and depression in recovering addicts
Development of extended-release formulations to improve patient adherence
Investigating genetic factors that may influence response to baclofen treatment

As these studies progress, they may provide new insights into optimizing baclofen therapy and expanding its use in addiction medicine.

Baclofen Side Effects & Uses in Addiction Treatment

Baclofen, also known by the brand names Kemstro and Lioresal, is a prescription muscle relaxant drug used to relieve muscle spasms, primarily in the treatment of multiple sclerosis or spinal cord diseases.

According to the U.S. National Library of Medicine, this medication relieves spasms of the musculoskeletal system, relieves pain, and improves muscle movement.

Baclofen was originally designed as a drug for the treatment of epilepsy. GABAb Receptor Pharmacology reports that after first being synthesized in 1962, the drug was only minimally successful in the treatment of seizures, but it was widely used to decrease spasticity caused by a variety of diseases. In 2009, a cardiologist named Olivier Ameisen published a memoir detailing his own recovery from alcoholism using baclofen, and this led to subsequent investigations into the efficacy of the drug as a treatment for addiction. While use of baclofen in addiction treatment is still considered experimental, it is gaining prominence in the field, and clinical trials continue to explore the possibilities of its use.

In the past decade, baclofen has been used with increasing frequency in the treatment of drug and alcohol addiction. In this usage, baclofen functions to lessen the symptoms of withdrawal. Prescribing baclofen to treat addiction is still considered an “off-label” use of the medication, or a use outside of what is approved by the FDA, but this use has shown some success in clinical trials, according to a study published by Cochrane Database of Systematic Review.

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Baclofen Side Effects, Dosage & Interactions

According to the U.S. National Library of Medicine, side effects of baclofen may include the following:

Drowsiness
Dizziness
Muscle weakness
Confusion
Upset stomach

More severe side effects of this drug include difficulty breathing and seizures; medical help should be sought immediately if either of these side effects is experienced. Side effects are generally minimal and occur primarily when first starting treatment with this medication.

Some individuals may be more susceptible to side effects, including the elderly, and those with impaired renal function. Individuals with galactose intolerance, active peptic ulceration, and porphyria should not take this medication. Additionally, baclofen should be prescribed with caution to the following individuals:

Those with severe psychiatric disorders
Individuals with seizure disorders
Those already receiving antihypertensive therapy
Anyone suffering from sphincter hypertonia
Individuals with liver disease or diabetes mellitus

According to the Electronic Medicines Compendium, dosage of baclofen is increased and decreased gradually over time; initial high doses of baclofen, without tapering up to that amount, can cause side effects to be more severe. The maximum recommended daily dose of this medication is 100 mg unless careful medical supervision is provided. Small, frequent doses are generally prescribed rather than larger doses. It may take several days for baclofen to first take effect.

Baclofen may interact with other medications and substances, including alcohol, anesthetics, tricyclic antidepressants, antihypertensives, dopaminergics, lithium, memantine, and NSAIDS. Baclofen should be avoided during pregnancy, especially during the first three months of gestation, as the drug crosses the placental barrier. Very small quantities of baclofen can be passed to babies through breast milk, but amounts are minimal – low enough that no undesirable effects are typically expected.

Baclofen Withdrawal Symptoms

Sudden withdrawal from baclofen can lead to the following symptoms:

Anxiety and confusion
Psychosis
Convulsions
Tachycardia

To prevent these withdrawal symptoms, the dosage of baclofen should be decreased incrementally over a period of 1-2 weeks.

Baclofen Half-Life & Timeline

Baclofen is absorbed quickly from the gastrointestinal tract, and peak concentration in the bloodstream occurs about 1-3 hours after oral administration of the medication. Baclofen’s half-life is 3-4 hours in plasma, and its shelf life is three years from the date of manufacture. Oral tablets of the medication also contain lactose, pregelatinised maize starch, maize starch, magnesium stearate, and water.

Baclofen Use in Addiction Treatment

Addiction is a problem that affects people from all demographics. The National Institute on Drug Abuse (NIDA) reports a 2.5-fold increase in total overdose deaths from the years 2001-2013, and overdose deaths relating to opioid pain relievers saw an even larger increase.

The Substance Abuse and Mental Health Services Administration (SAMHSA) reported in 2009 that 23.5 million people needed treatment for alcohol or drug addiction. In the face of this ever-growing prevalence of addiction, the medical field has increasingly begun to explore the possibilities of addiction recovery that is assisted by medication. According to SAMHSA, various medications are currently used for this purpose, including buprenorphine, methadone, and naltrexone. In addition to these medications, other medications like baclofen are often use in an off-label manner to assist in addiction treatment.

Baclofen may treat alcohol and drug addiction by altering the chemical processes responsible for substance addiction.

According to an a research article in Frontiers in Psychiatry, the chemical makeup of this medication may mimic gamma-aminobutyric acid (GABA), which has a calming effect on mood. This calming effect leads to an increase in dopamine levels, thereby lessening cravings for the addictive substance.

Baclofen is well tolerated by most people. Since the drug has shown promise in the treatment of alcohol and opioid addiction when assessed through clinical trials, off-label use of baclofen in addiction recovery continues to gain prominence. Additional clinical trials are needed to assess the efficacy of the medication for this purpose before it can be approved by the FDA for the treatment of substance addiction, although prescription of the drug for off-label use is allowed.

The Substance Abuse and Mental Health Services Administration (SAMHSA) states that they do not currently recommend the use of baclofen in clinical patient settings due to a lack of sufficient data demonstrating the medication’s effectiveness for the purpose of addiction treatment. While some success has been shown in this area, use of the drug is still considered experimental by SAMHSA.

An analysis of recent studies exploring the efficacy of baclofen for the treatment of addiction, published by Cochrane Database of Systematic Reviews, found that baclofen showed limited success in treating alcohol withdrawal syndrome, equal to the success shown by other drugs, such as diazepam. Slightly more success was shown in the treatment of opioid dependence. Clinical trials published in BMC Psychiatry have shown promising results in the use of baclofen for maintenance treatment of opioid dependence.

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Last Updated on Sep 13, 2022

Side Effects, Dosage, Uses & More

Highlights for baclofen

Baclofen oral tablet is only available as a generic drug.
Baclofen only comes as a tablet you take by mouth.
Baclofen is used to treat muscle spasms.

Stopping baclofen

Don’t stop taking this drug without talking to your doctor. Stopping it suddenly can cause seizures and hallucinations (seeing or hearing something that’s not real). If you need to stop taking this drug, your doctor will slowly lower your dosage over time.

Drowsiness warning

This drug can cause drowsiness. Don’t drive, use machinery, or do other dangerous activities until you know how it affects you. Also, don’t drink alcohol or take other medications that may make you feel drowsy while using baclofen. It may make your drowsiness worse.

Baclofen oral tablet is a prescription drug that’s only available in a generic form. There is no brand-name version available.

Baclofen also comes as a spinal injection, which is only given by a healthcare provider.

Why it’s used

Baclofen is used to treat muscle spasms. It may be used as part of a combination therapy. This means you may need to take it with other medications.

How it works

Baclofen belongs to a class of drugs called muscle relaxers. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

It isn’t known exactly how baclofen works to treat painful muscle spasms. It’s thought that baclofen blocks the signals from your nervous system that tell your muscles to spasm.

Baclofen oral tablet drug may cause drowsiness. It may also cause other side effects.

More common side effects

The more common side effects of baclofen oral tablet can include:

headaches
dizziness
drowsiness
nausea
low blood pressure
constipation

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious side effects

Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

withdrawal symptoms, such as hallucinations and seizures
feeling very drowsy
agitation
trouble urinating

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.

Baclofen oral tablet can interact with other medications, vitamins, or herbs you may be taking. An interaction is when a substance changes the way a drug works. This can be harmful or prevent the drug from working well.

To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Examples of drugs that can cause interactions with baclofen are listed below.

Central nervous system depressants

If you take these drugs with baclofen, you may have increased drowsiness. Examples of these drugs include:

benzodiazepines, such as triazolam and midazolam
narcotics, such as oxycodone and codeine

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions. This information is not a substitute for medical advice. Always speak with your healthcare provider about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.

This drug comes with several warnings.

Allergies

Baclofen can cause a severe allergic reaction. Symptoms can include trouble breathing and swelling of your throat or tongue.

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call 911 or go to the nearest emergency room.

Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

Alcohol interaction

The use of drinks that contain alcohol can increase your risk of nervous system side effects such as drowsiness, dizziness, and difficulty concentrating on tasks from baclofen. If you drink alcohol, talk to your doctor before mixing with baclofen.

Warnings for people with certain health conditions

For people with epilepsy: Talk to your doctor about whether this drug is safe for you. Baclofen may make your seizure control worse.

For people with kidney problems: If you have kidney problems or a history of kidney disease, you may not be able to clear this drug from your body well. This may increase the levels of baclofen in your body and cause more side effects. If you have kidney disease, your doctor may start you at a lower dose.

For people with a history of stroke: If you’ve had stroke, you may have more side effects with baclofen. This drug may also not work for your muscle spasms.

Warnings for other groups

For pregnant women: It isn’t known if baclofen is safe and effective for use in pregnant women. Tell your doctor if you’re pregnant or plan to become pregnant. Baclofen should be used during pregnancy only if the potential benefit justifies the potential risk.

Call your doctor right away if you become pregnant while taking this drug.

For women who are breastfeeding: It isn’t known if baclofen passes into breast milk. If it does, it may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

For children: This medication hasn’t been studied and shouldn’t be used in children younger than 12 years of age.

This dosage information is for baclofen oral tablet. All possible dosages and drug forms may not be included here. Your dosage, drug form, and how often you take the drug will depend on:

your age
the condition being treated
how severe your condition is
other medical conditions you have
how you react to the first dose

Forms and strengths

Generic: Baclofen

Form: oral tablet
Strengths: 10 milligrams (mg), 20 mg

Dosage for muscle spasms

Adult dosage (ages 18 years and older)

Typical starting dosage. You should start taking this drug on the following schedule:
- Days 1 through 3: Take 5 mg three times per day.
- Days 4 through 6: Take 10 mg three times per day.
- Days 7 through9: Take 15 mg three times per day.
- Days 10 through 12: Take 20 mg three times per day.
Dosage increases. Your doctor will slowly increase your dosage every three days. Your doctor may further increase your dosage if needed.
Maximum dosage. A total of 80 mg per day taken in four divided doses of 20 mg each.

Child dosage (ages 12 to 17 years)

Typical starting dosage. You should start taking this drug on the following schedule:
- Days 1 through 3: Take 5 mg three times per day.
- Days 4 through 6: Take 10 mg three times per day.
- Days 7 through 9: Take 15 mg three times per day.
- Days 10 through 12: Take 20 mg three times per day.
Dosage increases. Your doctor will slowly increase your dosage every three days. Your doctor may further increase your dosage if needed.
Maximum dosage. A total of 80 mg per day taken in four divided doses of 20 mg each.

Child dosage (ages 0 to 11 years)

This medication hasn’t been studied in children. It shouldn’t be used in people younger than 12 years.

Dosage warnings

The manufacturer of this drug recommends that you don’t take more than 80 mg per day.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always speak with your doctor or pharmacist about dosages that are right for you.

Baclofen oral tablet is used for either short-term or long-term treatment. It comes with serious risks if you don’t take it as prescribed.

If you stop taking the drug suddenly or don’t take it at all: Your muscle spasms won’t get better and may get worse.

If you miss doses or don’t take the drug on schedule: Your medication may not work as well or may stop working completely. For this drug to work well, a certain amount needs to be in your body at all times.

If you take too much: You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug include:

vomiting
muscle weakness
coma (being unconscious for a long time)
stopped breathing
seizure

If you think you’ve taken too much of this drug, call your doctor or local poison control center. If your symptoms are severe, call 911 or go to the nearest emergency room right away.

What to do if you miss a dose: Take your dose as soon as you remember. But if you remember just a few hours before your next scheduled dose, take only one dose. Never try to catch up by taking two doses at once. This could result in dangerous side effects.

How to tell if the drug is working: You should have less pain and stiffness.

Keep these considerations in mind if your doctor prescribes baclofen oral tablet for you.

General

You can take baclofen with or without food.
If the drug upsets your stomach, try taking it with food or milk.
You can split or crush the tablet.

Storage

Store baclofen at room temperature. Keep it between 68°F and 77°F (20°C and 25°C).
Don’t store this medication in moist or damp areas, such as bathrooms.

Refills

A prescription for this medication is refillable. You shouldn’t need a new prescription for this medication to be refilled. Your doctor will write the number of refills authorized on your prescription.

Travel

When traveling with your medication:

Always carry your medication with you. When flying, never put it into a checked bag. Keep it in your carry-on bag.
Don’t worry about airport X-ray machines. They can’t hurt your medication.
You may need to show airport staff the pharmacy label for your medication. Always carry the original prescription-labeled box with you.
Don’t put this medication in your car’s glove compartment or leave it in the car. Be sure to avoid doing this when the weather is very hot or very cold.

Clinical monitoring

Your doctor will likely monitor certain health issues. This can help make sure you stay safe while you take this drug.

Your doctor may do blood tests to check how well your kidneys are working. If your kidneys aren’t working well, your doctor may lower your dosage of this drug.

There are other drugs available to treat your condition. Some may be better suited for you than others. Talk to your doctor about other drug options that may work for you.

Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Baclofen – description of the substance, pharmacology, use, contraindications, formula

Structural formula
Russian name
English title
Latin name
chemical name
Gross formula
Pharmacological group of the substance Baclofen
Nosological classification
CAS code
pharmachologic effect
Characteristic
Pharmacology
Application of the substance Baclofen
Contraindications
Application restrictions
Use during pregnancy and lactation
side effects of baclofen
Interaction
Overdose
Dosage and administration
Precautionary measures
Trade names with the active ingredient Baclofen

Structural formula

Russian name

Baclofen

English name

Baclofen

Latin name

Baclophenum ( born Baclopheni)

Chemical name

beta-(Aminomethyl)-4-chlorobenzenepropanoic acid

General formula

C ₁₀ H ₁₂ ClNO 90 073 2

Pharmacological group of the substance Baclofen

Drugs affecting neuromuscular transmission

Nosological classification

ICD-10 code list

C72. 0 Spinal cord
D43.4 Spinal cord
F10.2 Alcohol dependence syndrome
G03.9 Meningitis, unspecified
G12. 2 Motor neuron disease
G35 Multiple sclerosis
G80 Infantile cerebral palsy
G95.0 Syringomyelia and syringobulbia
G95. 9 Disease of spinal cord, unspecified
I64 Stroke, not specified as haemorrhage or infarction
R25.2 Convulsions and spasm
S06 Intracranial injury
T09. 3 Injury of spinal cord, level unspecified

CAS code

1134-47-0

Pharmacological action

Pharmacological action –

antispastic , muscle relaxant .

Characteristics

Muscle relaxant of central action.

White or almost white crystalline powder, almost odorless. Slightly soluble in water, very little in methanol and insoluble in chloroform.

Pharmacology

Stimulates GABA _B receptors, reduces the excitability of the terminal sections of afferent sensory fibers, inhibits mono- and polysynaptic spinal reflexes, which leads to a decrease in muscle tension and an analgesic effect.

When taken orally, it is rapidly and almost completely absorbed from the gastrointestinal tract. max “> C _max is achieved in 2-3 hours. Protein binding – 30%. Passes through the placental barrier, penetrates into breast milk. Approximately 15% is biotransformed in the liver by deamination. T _1/2 – 2.5-4 hours Excreted mainly by the kidneys (70-80%) unchanged and as metabolites.

Application of the substance Baclofen

Inside: muscle spasticity in multiple sclerosis, tumors and diseases of the spinal cord of infectious, degenerative and traumatic origin (including syringomyelia, motor neuron disease, trauma), stroke, cerebral palsy, meningitis , TBI, alcoholism.

Intrathecal: Severe chronic spasticity in the spinal cord (eg, due to trauma, multiple sclerosis) or brain in case of failure or intolerance of oral muscle relaxant therapy.

Contraindications

Hypersensitivity, epilepsy, seizures (history), Parkinson’s disease, psychosis, chronic renal failure, pregnancy, lactation.

Restrictions for use

Cerebrovascular insufficiency, atherosclerosis of cerebral vessels, peptic ulcer of the stomach and duodenum, old age, children’s age (up to 12 years).

Use in pregnancy and lactation

Contraindicated in pregnancy.

FDA fetal category has not been determined.

Breast-feeding should be discontinued during treatment.

Side effects of the substance Baclofen

From the side of the nervous system and sensory organs: drowsiness, insomnia, dizziness, headache, weakness, fatigue, confusion, imbalance, decreased reaction rate, mental agitation, euphoria, hallucinations, depression, nightmares, seizures, decreased seizure threshold.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): decrease in blood pressure, palpitations, chest pain, collapse.

From the digestive tract: aversion to food, taste perversion, nausea, vomiting, constipation/diarrhea, dyspepsia, abdominal pain.

From the genitourinary system: dysuria, enuresis, urinary retention; with prolonged use – impaired renal function.

Respiratory side: feeling of nasal congestion and suffocation, respiratory depression.

Other: muscle pain, skin rash, itching, swelling of the feet, sweating, weight gain, paradoxical reaction.

Interaction

When used simultaneously, baclofen enhances the effect of antihypertensive drugs, ethanol.

Tricyclic antidepressants increase the decrease in muscle tone. Levodopa and carbidopa increase the risk of hallucinations, confusion, agitation.

Overdose

Symptoms: vomiting, muscle hypotension, respiratory depression, convulsions, coma (after the return of consciousness, muscle hypotension may persist for 72 hours).

Treatment: induction of vomiting or gastric lavage, activated charcoal, symptomatic and supportive therapy (ventilation, maintenance of cardiovascular activity). There is no specific antidote.

Dosage and administration

Inside, intrathecally. The dosing regimen is set individually. Inside, the initial dose is 5 mg 3 times a day, then the dose is increased every 3 days until the optimal therapeutic effect is achieved (usually up to 30-75 mg / day). In patients over 65 years of age, the dose should be increased with caution due to an increased risk of side effects. The maximum daily dose is 100 mg. The dose for children is established depending on age and body weight.

Precautions

In patients with liver disease and diabetes, it is necessary to periodically monitor the activity of hepatic transaminases, alkaline phosphatase, blood glucose levels.

Baclofen should be discontinued gradually (may cause hallucinations and exacerbation of spastic conditions). In the event of symptoms such as chest pain, suffocation, collapse, hematuria, depression, confusion, hallucinations, skin rash, convulsions, blurred vision, a significant decrease in muscle strength, vomiting, you should immediately consult a doctor.

Should not be used during work by drivers of vehicles and people whose profession is associated with increased concentration of attention.

Trade names with active substance Baclofen

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Lek. form
All lek. Forms solution for intrathecal administration substance-powder tablets

Dosage
All dosages 0.05 mg/ml 0.5 mg/ml 10 mg 2 mg/ml 25 mg No dosage

Manufacturer
All manufacturers Delpharm Dijon Medana Pharma AO Novartis Pharma Stein AG Polpharma S.A., Poland Pharmaceutical plant Usolye-Sibirskiy KhPZ AO

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