How effective is tizanidine for treating neuropathic pain. What dosage of tizanidine is used for pain relief. What are the side effects of tizanidine for neuropathic pain. How does tizanidine compare to other medications for nerve pain.

Overview of Tizanidine for Neuropathic Pain

Tizanidine is a medication that has shown promise in treating neuropathic pain, a complex and often debilitating condition. This open-label study aimed to evaluate the effectiveness and tolerability of tizanidine in patients suffering from neuropathic pain.

The study enrolled 23 patients who were administered tizanidine over an 8-week period. Starting with a low dose of 1-4 mg once daily for the first week, the dosage was then escalated weekly by 2-8 mg until reaching the effective or maximum tolerated dose, up to a maximum of 36 mg per day.

Dosage and Administration of Tizanidine

How was tizanidine administered in the study? The initial dosage was 1-4 mg once daily for the first week. This was followed by weekly dose escalations of 2-8 mg. The goal was to reach each patient’s effective or maximum tolerated dose, with an upper limit of 36 mg per day over the 8-week study period.

What was the average effective dose? The mean effective or maximum tolerated dose was 23 mg/day, with a range from 6 to 36 mg/day. This indicates that there is significant variability in the optimal dosage among patients, highlighting the importance of individualized treatment approaches.

Titration Schedule

• Week 1: 1-4 mg once daily
• Weeks 2-8: Weekly increases of 2-8 mg
• Maximum dose: 36 mg/day

Effectiveness of Tizanidine for Pain Relief

The study found promising results regarding the effectiveness of tizanidine for neuropathic pain relief. Patients experienced a significant reduction in pain intensity over the course of the treatment period.

How much did pain scores decrease? The mean average weekly pain score at baseline was 6.9 on a numeric rating scale. By the end of week 8, this had decreased by 1.7 points to 5.2, which was statistically significant (p ≤ 0.01). This represents a meaningful reduction in pain intensity for many patients.

What percentage of patients reported improvement? A total of 15 patients (68%) reported that their pain relief was improved or much improved with tizanidine therapy. Notably, 2 of these patients became completely pain-free during the study period.

Improvements in Specific Pain Qualities

The study also assessed changes in various qualities of neuropathic pain. The following pain characteristics were significantly lower at week 8 compared to baseline:

• Intense pain
• Sharp pain
• Hot pain
• Dull pain
• Cold pain
• Sensitive pain
• Unpleasant pain
• Deep pain

This comprehensive improvement across multiple pain qualities suggests that tizanidine may be effective in addressing various aspects of neuropathic pain.

Impact on Quality of Life

Beyond pain relief, the study also examined how tizanidine affected patients’ overall quality of life. There was a significant decline in pain quantity and interference of pain on quality of life from baseline to week 8.

How does pain impact daily functioning? Neuropathic pain can severely limit a person’s ability to perform everyday activities, work, and enjoy life. The reduction in pain interference observed in this study suggests that tizanidine may help patients regain some of their lost functionality and improve their overall well-being.

Areas of Improvement

1. Sleep quality
2. Physical activity
3. Mood and emotional well-being
4. Social interactions
5. Work performance

Side Effects and Tolerability of Tizanidine

While tizanidine showed promising results for pain relief, it’s important to consider the potential side effects and overall tolerability of the medication. The study reported several common side effects experienced by patients.

What are the most common side effects of tizanidine? The study found the following side effects:

• Dizziness/lightheadedness (52% of patients)
• Drowsiness (48%)
• Fatigue/weakness (43%)
• Dry mouth (39%)
• Gastrointestinal upset (30%)
• Sleep difficulty (22%)

These side effects are generally consistent with the known safety profile of tizanidine. However, it’s important to note that individual experiences may vary, and some patients may find these side effects more bothersome than others.

Liver Function Concerns

One patient in the study developed a significant elevation in liver function tests (LFTs) with symptoms at week 4, leading to discontinuation of tizanidine therapy. The LFTs returned to normal within 3 weeks after stopping the medication.

Is liver monitoring necessary during tizanidine treatment? This case highlights the importance of monitoring liver function in patients taking tizanidine, especially during the initial weeks of treatment. Regular blood tests to check LFTs may be advisable for patients on long-term tizanidine therapy.

Comparison to Other Neuropathic Pain Treatments

While this study focused specifically on tizanidine, it’s important to consider how it compares to other treatments for neuropathic pain. The authors suggest that tizanidine might offer an alternative for patients who have responded poorly to other medications.

What are some other common treatments for neuropathic pain?

• Anticonvulsants (e.g., gabapentin, pregabalin)
• Antidepressants (e.g., duloxetine, amitriptyline)
• Topical treatments (e.g., lidocaine patches, capsaicin cream)
• Opioids (used cautiously due to risk of dependence)
• Non-pharmacological approaches (e.g., physical therapy, cognitive behavioral therapy)

How does tizanidine’s mechanism of action differ from these treatments? Tizanidine is a central alpha-2 adrenergic agonist, which is distinct from the mechanisms of action of anticonvulsants or antidepressants commonly used for neuropathic pain. This unique mechanism may explain why some patients who don’t respond well to other medications might benefit from tizanidine.

Limitations and Future Research Directions

While the results of this open-label study are promising, there are several limitations to consider when interpreting the findings.

What are the main limitations of this study?

• Small sample size (23 patients)
• Lack of a control group
• Open-label design (potential for placebo effect)
• Relatively short duration (8 weeks)

These limitations highlight the need for further research to confirm the effectiveness of tizanidine for neuropathic pain.

Recommendations for Future Studies

The authors of the study make several recommendations for future research:

1. Conduct a larger, randomized placebo-controlled trial to more definitively establish the efficacy of tizanidine for neuropathic pain.
2. Perform comparative studies with alternative agents to determine how tizanidine stacks up against other established treatments.
3. Investigate the long-term efficacy and safety of tizanidine for neuropathic pain management.
4. Explore potential combinations of tizanidine with other pain medications to optimize treatment outcomes.

Clinical Implications and Patient Selection

The findings of this study have several potential implications for clinical practice and patient care.

Which patients might be good candidates for tizanidine therapy? Based on the study results, tizanidine may be particularly beneficial for:

• Patients who have not responded well to first-line treatments for neuropathic pain
• Those who experience multiple qualities of neuropathic pain (e.g., burning, shooting, sensitivity)
• Individuals who can tolerate the potential side effects, particularly drowsiness and dizziness
• Patients without pre-existing liver conditions, given the potential for liver enzyme elevation

How should clinicians approach tizanidine therapy for neuropathic pain? The study suggests a gradual titration approach, starting with low doses and slowly increasing to find the optimal balance between pain relief and side effects. Close monitoring, especially during the initial weeks of treatment, is essential to ensure patient safety and optimize outcomes.

Potential Advantages of Tizanidine

1. Novel mechanism of action, potentially effective for treatment-resistant cases
2. Improvement across multiple pain qualities
3. Positive impact on quality of life and daily functioning
4. Non-opioid option for pain management

In conclusion, while more research is needed, tizanidine shows promise as a potential treatment option for neuropathic pain. Its unique mechanism of action and ability to address multiple pain qualities make it an intriguing candidate for further study and clinical consideration.

Effectiveness of tizanidine in neuropathic pain: an open-label study

. 2000 Winter;1(4):285-92.

doi: 10.1054/jpai.2000.9435.

M R Semenchuk 
¹
, S Sherman

Affiliations

Affiliation

• ¹ University of Arizona Neurology Clinic, Tucson, 85743, USA. [email protected]

• PMID:

  14622612

• DOI:

  10.1054/jpai.2000.9435

M R Semenchuk et al.

J Pain.

2000 Winter.

. 2000 Winter;1(4):285-92.

doi: 10.1054/jpai. 2000.9435.

Authors

M R Semenchuk 
¹
, S Sherman

Affiliation

• ¹ University of Arizona Neurology Clinic, Tucson, 85743, USA. [email protected]

• PMID:

  14622612

• DOI:

  10.1054/jpai.2000.9435

Abstract

The purpose of this research trial is to assess the effectiveness and tolerability of tizanidine in neuropathic pain. In an open-label study, patients with neuropathic pain received 1 to 4 mg of tizanidine once daily for 7 days, followed by weekly dose escalation of 2 to 8 mg to his/her effective or maximum tolerated dose or a maximum of 36 mg over an 8-week period. Treatment effects were assessed, using average weekly pain scores as well as biweekly scores for patient global assessment of pain relief, the neuropathic pain scale, and wisconsin brief pain inventory. Frequency and severity of adverse events were examined also. Twenty-three patients were enrolled. The mean average weekly pain score at baseline was 6.9, which decreased by 1.7 points at the end of week 8 to 5.2 (p < or =.01). A total of 15 patients (68%) reported that their pain relief was improved or much improved with tizanidine therapy, and 2 of these patients became completely pain-free. The following neuropathic pain qualities were significantly lower at week 8 compared with baseline: intense, sharp, hot, dull, cold, sensitive, unpleasant, and deep pain. There was a significant decline in pain quantity and interference of pain on quality of life from baseline to week 8. The mean effective or maximum tolerated dose was 23 mg/day (range 6 to 36 mg/day). Side effects consisted primarily of dizziness/lightheadedness (52%), drowsiness (48%), fatigue/weakness (43%), dry mouth (39%), gastrointestinal upset (30%), and sleep difficulty (22%). One patient developed significant elevation in liver function tests (LFTS) With symptoms at week 4. Tizanidine therapy was discontinued. LFTS returned to normal in 3 weeks. Tizanidine might be an effective treatment for neuropathic pain, offering an alternative for patients poorly responsive to other medications. A larger, randomized placebo-controlled trial is recommended. In addition, comparative studies with alternative agents should be sought.

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Tizanidine Uses, Dosage, Side Effects

Generic name: tizanidine [ tye-ZAN-i-deen ]
Brand name: Zanaflex
Drug class: Skeletal muscle relaxants

Medically reviewed by Sanjai Sinha, MD. Last updated on Jan 10, 2022.

What is tizanidine?

Tizanidine is a short-acting muscle relaxer. It works by blocking nerve impulses (pain sensations) that are sent to your brain.

Tizanidine is used to treat spasticity by temporarily relaxing muscle tone.

Tizanidine may also be used for purposes not listed in this medication guide.

Warnings

Tizanidine is a short-acting medication that should be taken only for daily activities that require relief from muscle spasticity.

You should not take tizanidine if you are also taking fluvoxamine (Luvox) or ciprofloxacin (Cipro).

Do not use tizanidine at a time when you need muscle tone for safe balance and movement during certain activities. In some situations, it may endanger your physical safety to be in a state of reduced muscle tone.

Switching between tablets and capsules, or changing the way you take it with regard to eating, can cause an increase in side effects or a decrease in therapeutic effect. Follow your doctor’s instructions carefully. After making any changes in how you take tizanidine, contact your doctor if you notice any change in how well the medicine works or if it causes increased side effects.

The recommended starting dose of tizanidine is 2 mg every 6 to 8 hours, up to a maximum of 3 doses in 24 hours. Do not take more than 36 mg of tizanidine in a 24-hour period. Too much of this medicine can damage your liver. Cold or allergy medicine, narcotic pain medicine, sleeping pills, other muscle relaxers, and medicine for seizures, depression or anxiety can add to sleepiness caused by tizanidine.

Avoid drinking alcohol. It can increase some of the side effects of this medicine.

Before taking this medicine

You should not use tizanidine if you are allergic to it, or if:

To make sure tizanidine is safe for you, tell your doctor if you have ever had:

• liver disease;

• kidney disease; or

• low blood pressure.

It is not known whether tizanidine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It may not be safe to breastfeed while using this medicine. Ask your doctor about any risk.

How should I take tizanidine?

Take tizanidine exactly as it was prescribed for you. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Tizanidine is usually taken up to 3 times in one day, starting at 2mg per dose. Allow 6 to 8 hours to pass between doses. Do not take more than 36 mg in a 24-hour period. Too much of this medicine can damage your liver.

You may take tizanidine with or without food, but take it the same way each time. Switching between taking with food and taking it without food can make the medicine less effective or cause increased side effects.

Switching between tablets and capsules may cause changes in side effects or how well the medicine works.

If you make any changes in how you take tizanidine, tell your doctor if you notice any change in side effects or in how well the medicine works.

Tizanidine is a short-acting medication, and its effects will be most noticeable between 1 and 3 hours after you take it. You should take this medicine only for daily activities that require relief from muscle spasms.

You will need frequent blood tests to check your liver function.

If you stop using this medicine suddenly after long-term use, you may have withdrawal symptoms such as dizziness, fast heartbeats, tremors, and anxiety. Ask your doctor how to safely stop using this medicine.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include weakness, drowsiness, confusion, slow heart rate, shallow breathing, feeling light-headed, or fainting.

What to avoid

Do not use tizanidine at a time when you need muscle tone for safe balance and movement during certain activities. In some situations, it may be dangerous for you to have reduced muscle tone.

Drinking alcohol with this medicine can cause side effects.

Avoid driving or hazardous activity until you know how this medicine will affect you. Your reactions could be impaired. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

Tizanidine side effects

Get emergency medical help if you have signs of an allergic reaction to tizanidine: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• a light-headed feeling, like you might pass out;

• weak or shallow breathing;

• confusion, hallucinations; or

• pain or burning when you urinate.

Common tizanidine side effects may include:

• drowsiness, dizziness, weakness;

• feeling nervous;

• blurred vision;

• flu-like symptoms;

• dry mouth, trouble speaking;

• abnormal liver function tests;

• runny nose, sore throat;

• urination problems, painful urination;

• vomiting, constipation; or

• uncontrolled muscle movements.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect tizanidine?

Taking tizanidine with other drugs that make you sleepy or slow your breathing can cause dangerous side effects or death. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Tell your doctor about all your other medicines, especially:

• acyclovir;

• ticlopidine;

• zileuton;

• birth control pills;

• an antibiotic – ciprofloxacin, levofloxacin, moxifloxacin, or ofloxacin;

• blood pressure medicine – clonidine, guanfacine, methyldopa;

• heart rhythm medicine – amiodarone, mexiletine, propafenone, verapamil; or

• stomach acid medicine – cimetidine, famotidine.

This list is not complete. Other drugs may interact with tizanidine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Popular FAQ

The maximum effect of tizanidine occurs about 1 hour to 2 hours after taking a dose. It wears off in about 3 to 6 hours after taking it. Tizanidine is typically given no more than 3 times a day.

Tizanidine is not listed as a controlled substance by the U.S. Drug Enforcement Administration (DEA). Abuse potential has not been evaluated in human studies.

Tizanidine can cause sleepiness, but it has not been approved by the U.S. Food and Drug Administration (FDA) to treat sleep disorders. Tizanidine is a skeletal muscle relaxant. It is approved by the FDA to help relieve muscle spasms.

Tizanidine is known to cause low blood pressure. In some cases, it may cause low blood pressure that is so low that you could faint or pass out. The chances of fainting can be lowered if your doctor raises the dose of tizanidine very slowly. You may also have to be careful when you move from a sitting position to a standing position. In clinical trials, the most common side effects of tizanidine were dry mouth, sleepiness, dizziness and asthenia (defined as weakness, fatigue and/or tiredness).

Tizanidine normally starts working 1 to 2 hours after taking it. It wears off about 3 hours to 6 hours after taking it. Tizanidine can be taken up to 3 times a day to help relieve muscle spasms.

Tizanidine may be addictive, but it has not been evaluated in human studies. Withdrawal symptoms have been reported after abruptly stopping tizanidine, but abuse of other medications concomitantly was suspected in these cases. Dosing should be tapered off to avoid possible withdrawal symptoms.

Tizanidine is not known to cause weight gain. In clinical trials, the most common side effects of tizanidine were dry mouth, sleepiness, dizziness and asthenia (defined as weakness, fatigue and/or tiredness).

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The use of tizanidine (Sirdalud) in the treatment of pain and spasm | Danilov A.B.

The drug tizanidin (Sirdalud) belongs to the centrally acting muscle relaxants (α2-adrenergic agonists) and implements its effect at the spinal and supraspinal levels [4]. By stimulating presynaptic α2 receptors, it inhibits the release of excitatory amino acids that stimulate NMDA receptors. This leads to the suppression of the transmission of excitation through the polysynaptic reflexes of the spinal cord. The drug mainly inhibits the polysynaptic reflexes of the spinal cord responsible for muscle hypertonicity, which causes a decrease in the increased tone of the flexor and extensor muscles and a decrease in painful muscle spasms. In addition to muscle relaxant properties, tizanidine also has a central, moderately pronounced analgesic effect (by reducing the release of excitatory neurotransmitters in the brain at the level of the locus coeruleus). In animal studies, it has been shown that tizanidine (Sirdalud) can realize its effect through a decrease in central sensitization [11]. These properties of tizanidine allow it to be used both as a means to reduce muscle spasm, and for the treatment of a number of pain syndromes (associated with muscle spasm).

Tizanidin (Sirdalud)
for pain syndromes
Monotherapy with tizanidine (Sirdalud) for pain syndromes. Muscular tonic and myofascial pain syndromes are very often the main reason for patients to seek medical attention. In the treatment of muscular-tonic pain, the central place belongs to local influences aimed at relaxing the muscle (massage, applications of warming ointments, gels, wet compresses, etc.), and in the case of myofascial pain syndrome, on the destruction of trigger points using post-isometric relaxation, the introduction of dry needles or anesthetic into the trigger zone. The terms of therapy are significantly reduced with effective anesthesia of the patient. A common method of pain relief for myofascial pain is also the use of non-steroidal anti-inflammatory drugs (NSAIDs).
Muscle relaxants can be of great help in the treatment of muscular-tonic and myofascial pain syndromes by reducing the intensity of pain, reducing painful muscle tension, and improving motor activity. The use of muscle relaxants is justified by the recognition of the important role of muscle spasm in the pathogenesis of pain in the lower back. Pain of various origins (due to damage to the intervertebral discs, facet joints of the spine, the muscles themselves and other causes) increases the activity of the motor neurons of the spinal cord, which leads to muscle spasm, which in turn plays a significant role in maintaining the pain itself. Pathologically increased muscle tone has various mechanisms for increasing pain: direct irritation of muscle pain receptors, deterioration of blood supply to the muscles, which leads to the formation of a vicious circle leading to increased muscle spasm and accompanying pain. Muscle relaxants break the vicious circle of “pain – muscle spasm – pain” and, as a result, can accelerate the recovery period [6]. In European guidelines for the treatment of acute pain in the lower back, tizanidine, dantrolene, diazepam, baclofen are noted as effective muscle relaxants [19]. In our country, of these drugs, tizanidine (Sirdalud) is most commonly used [6].
The effective daily dose range of tizanidine (Sirdalud) for pain syndromes is 2–12 mg (the optimal dose is 6–8 mg/day). For mild pain syndromes, the appointment of tizanidine (Sirdalud) can be limited to taking the drug at night at a dose of 2-4 mg until the pain stops (usually 5-7 days). With a moderately severe pain syndrome, it is also better to prescribe the first dose at night at a dose of 2–4 mg (the patient will “oversleep” the side effects), then gradually increase the dose to 6–8 mg / day. In severe cases, an additional 2–4 mg of tizanidine (Sirdalud) at night can be added. A positive effect, as a rule, is already noted on the 3rd day of taking the drug. In chronic pain syndromes, a course of therapy is usually carried out lasting 2-4 weeks, adjusting the duration of treatment and the dose of the drug depending on the efficacy / tolerability.
It should be noted that for mild to moderate pain associated with muscle spasm (eg, acute pain in the neck or lower back), it may be sufficient to prescribe tizanidine (Sirdalud) as monotherapy.
The effectiveness of tizanidine monotherapy (Sirdalud) has been confirmed in many studies, incl. and in a multicenter study that included 2251 patients with acute pain caused by muscle spasm in the lower back, neck, or shoulder. 89% of patients rated the treatment outcome as “good” or “very good”. The study also noted a very good tolerability of the drug (90% of patients reported tolerability as “good” or “very good”). These results allowed the authors to recommend tizanidine as the drug of choice among muscle relaxants for the treatment of pain associated with muscle spasm [13].
Combination of tizanidine (Sirdalud) with NSAIDs. With more severe pain, or when it is based on inflammatory changes, it is advisable to use tizanidine and NSAIDs together. Studies show that the use of tizanidine potentiates the effect of NSAIDs [9,16]. In addition, taking tizanidine (Sirdalud) has a gastroprotective effect, which is associated with its adrenergic activity and antispasmodic effect. Tizanidin (Sirdalud) reduces basal and induced acid secretion in the stomach, eliminates the imbalance of glycoproteins in the gastric mucosa and gastric secretions [11,16].
In experimental studies, the use of tizanidine demonstrated a significant decrease in the ulcerogenic effect of acetylsalicylic acid, indomethacin, meloxicam, nimesulide and naproxen. The gastroprotective activity of tizanidine has also been proven in clinical studies. In patients receiving the combination of ibuprofen and tizanidine, the incidence of gastrointestinal side effects, including bleeding, was significantly (p=0.002) lower than in patients receiving the combination of ibuprofen and placebo [9]. Similar results were obtained when comparing the combination of diclofenac and tizanidine with the combination of diclofenac and placebo in a multicenter (12 centers), prospective, double-blind, placebo-controlled, randomized clinical trial conducted in 6 countries of the Asia-Pacific region and including 405 participants [16]. Gastropathy was reported in 12% of patients treated with a combination of diclofenac and tizanidine versus 32% of patients treated with diclofenac in combination with placebo (p<0.001). The frequency of positive fecal occult blood test results was 5% in the main group compared to 11% in the control group.
The gastroprotective effect of Sirdalud is especially important for the management of patients with chronic pain syndromes who take NSAIDs for a long period of time (for rheumatological diseases), which often leads to the development of erosive gastritis and gastric and duodenal ulcers [1].
Combination of tizanidine (Sirdalud) with antidepressants and anticonvulsants. The management of chronic pain is more complex than the management of acute pain and requires an integrated approach. The use of muscle relaxants here is only a component of treatment and should be justified by the presence of a therapeutic target – muscle spasm. In this regard, the patient’s expectations regarding the effect of a muscle relaxant should be correctly formed: the use of tizanidine (Sirdalud) can reduce pain, facilitate the patient’s movements, but will not stop the pain completely, because. in chronic pain, the muscle component is not the leading one.
In the treatment of chronic pain syndromes, anticonvulsants, antidepressants are used, so it is important to consider how tizanidine (Sirdalud) interacts with these drugs. There are works that show that tizanidine (Sirdalud) potentiates the action of tricyclic antidepressants (amitriptyline) [10]. At the same time, it must be remembered that tizanidine (Sirdalud) cannot be combined with fluvoxamine, an antidepressant from the SSRI group. Simultaneous administration of tizanidine (Sirdalud) and fluvoxamine can lead to a significant decrease in blood pressure and cause complications from the central nervous system.
Thus, due to high efficiency and minor side effects, a number of domestic and foreign experts consider tizanidine (Sirdalud) as the drug of choice for the treatment of acute and subacute myofascial pain in monotherapy and as the drug of first choice for the treatment of chronic myofascial syndrome in combination with other drugs [2 ,13].
Tizanidin (Sirdalud)
in neurological practice
Disturbances in muscle tone, associated pain syndromes, restrictions on motor functions, secondary changes in joints and muscles are part of the clinical manifestations of many diseases of the nervous system. As a rule, the problem of increasing muscle tone – hypertonicity or spasticity – acquires clinical significance [8]. However, the causes of hypertonicity and the mechanisms underlying it may be different, and therefore the treatment of spasticity requires differentiated approaches to treatment.
The use of tizanidine (Sirdalud) is most widely used in the treatment of spasticity in traumatic injuries of the brain and spinal cord, multiple sclerosis, and stroke. With spasticity associated with dystonic disorders, parkinsonism, it is more appropriate to use other drugs (for example, clonazepam, diazepam).
Spasticity leads to significant functional disorders and impaired quality of life of the patient. However, it should be remembered that spasticity itself does not always require treatment. For example, in some patients with severe paresis, the presence of spasticity in the muscles that anatomically oppose gravity (anti-gravity muscles) can make standing and walking easier. In addition, the presence of increased muscle tone can prevent the development of muscle atrophy, soft tissue edema and osteoporosis, as well as reduce the risk of thrombosis of the lower extremities. Indications for the treatment of spasticity are only those cases when, due to increased tone, the “functioning, positioning or comfort” of the patient is disturbed.
The use of tizanidine (Sirdalud) in stroke. In stroke, the main objectives of treatment are not only to reduce the severity of spasticity, but also to improve the functionality of paretic limbs, reduce pain and discomfort associated with high muscle tone, and facilitate care for a paralyzed patient.
The most effective means in the fight against spasticity are exercise therapy and physiotherapy, especially at an early stage. In cases where patients with post-stroke limb paresis have local spasticity, local administration of botulinum toxin preparations can be used. A significant contribution to the treatment of spasticity can be made by the use of anti-spastic drugs (muscle relaxants) for oral administration. The use of muscle relaxants can reduce muscle tone, improve motor functions, facilitate the care of an immobilized patient, relieve painful muscle spasms, enhance the effect of physical therapy and, as a result, prevent the development of contractures. In our country, tizanidine, baclofen, tolperisone, diazepam are used to treat post-stroke spasticity.
An analysis of 20 studies comparing the use of various antispastic agents in a variety of neurological diseases accompanied by spasticity showed that tizanidine, baclofen and diazepam are approximately equally able to reduce spasticity, but tizanidine (Sirdalud) is more effective than other antispastic agents in reducing clonus [14] . Unlike baclofen, tizanidin (Sirdalud) does not cause a decrease in muscle strength with a decrease in spasticity (which is very important for improving the functionality of the limb), it is better tolerated by patients than baclofen and diazepam (when using it, patients are less likely to stop treatment due to side effects) [14,15,20]. Among the side effects identified during the study of tizanidine in patients with post-stroke spasticity, conducted by Gelber (2001), the most common side effects were drowsiness, weakness, dizziness, dry mouth, orthostatic hypotension. These phenomena took place with the abolition or reduction of the dose of the drug. At the same time, no serious side effects were noted during treatment with tizanidine [Gelber, 2001], which allowed the authors to conclude that it is highly safe.
Authors who have conducted studies on the clinical effects of tizanidine (Sirdalud) and many clinicians agree that among muscle relaxants, tizanidine (Sirdalud) is the drug of first choice for the treatment of post-stroke spasticity [7,12,14,15,20].
For the treatment of spasticity due to neurological diseases, higher doses of tizanidine (Sirdalud) are usually used than for the treatment of pain syndromes. Usually the optimal therapeutic effect is achieved with a daily dose of 12 to 24 mg (effective dose range is 2-36 mg). However, given the dose-dependent increase in the risk of side effects with increasing doses of the drug, treatment should be started with small (2-6 mg / day) doses, then gradually increase the dose until a therapeutic effect is achieved, observing individual tolerability (usually 2-6 mg / day). 4 mg every 3 to 7 days divided into 3 daily doses). If side effects occur, you can temporarily stop increasing the dose (if you do not increase the dose, in many cases the side effects disappear after a few days) and continue increasing the dose after the patient gets used to the drug. This allows, firstly, to select the most effective minimum dose of the drug for a particular patient (in some patients (due to individual variability), a sufficient therapeutic effect may occur when taking smaller doses than recommended standards), as well as to relieve unnecessary suffering of patients with individual poor tolerance to tizanidine (in patients with poor tolerance to tizanidine, side effects appear already at a dose of 2-4 mg / day). Dose titration usually takes 2-4 weeks. The duration of treatment is set individually (from several weeks to several months) [8].
The use of prolonged forms of tizanidine (Sirdalud MR). For long-term use, a dosage form of tizanidine in the form of modified-release capsules (Sirdalud MR), which is available in a dose of 6 mg, is convenient. Clinical experience shows that for most patients the optimal dose is 12 mg / day. (2 capsules), in rare cases, it may be necessary to increase the daily dose to 24 mg. Treatment also begins with a minimum dose of 6 mg (1 capsule), if necessary, gradually increasing the dose by 6 mg (1 capsule) at intervals of 3-7 days.
The use of tizanidine (Sirdalud) in traumatic brain injury. Among muscle relaxants, tizanidine (Sirdalud) is the most commonly used drug for the treatment of spasticity associated with traumatic brain injury [5]. The reasons for prescribing, dose selection tactics and warnings are the same as in the treatment of post-stroke spasticity.
The use of tizanidine (Sirdalud) in multiple sclerosis and spinal injury. Restriction of mobility in patients with multiple sclerosis is associated with a significant increase in spastic muscle tone, mainly in the lower extremities. The basis of the treatment of muscle tone disorders are special exercises that should be performed under the supervision of a specialist in physical therapy. Drug therapy plays a complementary role. Among the drugs used to treat spasticity are tolperisone, baclofen, tizanidine, diazepam. Drug treatment of spastic tone should be individual, controlled by the doctor and the patient himself. This is because most anti-tonus drugs increase the weakness of the paralyzed limbs and may worsen the patient’s condition. In this regard, the dose of the antispastic drug should be gradually increased from the minimum to the optimum, when spasticity decreases, but there is no increase in weakness. Sirdalud in this regard is more preferable than baclofen and diazepam (when using tizanidine (Sirdalud), muscle weakness develops less often; due to excessive relaxation of the sphincters of the bladder when using baclofen, patients often complain of an increase in pelvic disorders; the use of diazepam is associated with a greater frequency development of side effects, drug dependence) [3,17]. Sirdalud is more effective than other muscle relaxants against clonuses [14].
The optimal daily dose of Sirdalud for the treatment of spasticity in multiple sclerosis is 6–8 mg (maximum daily dose is 36 mg). It is also necessary to start treatment with the minimum dose, the step of increasing the dose is 2 mg [3].
In patients with spasticity due to spinal injury, tizanidine (Sirdalud) and baclofen are most commonly used, and diazepam is used to relieve painful muscle spasms. Treatment begins with a minimum dose (4-6 mg Sirdalud), which is gradually brought to a therapeutic dose over several days or weeks, trying to avoid unwanted side effects (muscle weakness and sedation). Baclofen is effective mainly when administered intrathecally; when administered orally, tizanidine (Sirdalud) gives a more pronounced positive effect and is better tolerated by patients than baclofen [18].
For other types of spasticity encountered in neurological practice (with parkinsonism, torsion dystonia, torticollis, ALS), the use of tizanidine (Sirdalud) is not justified. In these cases, the use of clonazepam and diazepam is more appropriate. These drugs have a higher likelihood of side effects, but their antispasmodic effect is more pronounced in these disorders.
Treatment Optimization
when using tizanidine
(Sirdaluda)
A sufficiently wide range of effective doses of tizanidine (Sirdalud) (from 2 to 36 mg / day) allows the use of the drug for short and long courses of treatment of pain syndromes and spasticity as monotherapy or in combination with other drugs. To improve clinical performance, the following recommendations for the practical use of tizanidine (Sirdalud) may be helpful.
Start treatment with small doses of the drug. The development of side effects with the use of tizanidine (Sirdalud) is dose-dependent (for example, the likelihood of side effects with a dose of 12-24 mg is 2 times higher than with a dose of 6-12 mg). At the same time, a sufficient therapeutic effect can sometimes be achieved at lower doses than recommended in the treatment standards. In this regard, it is recommended to start treatment with a minimum dose (2-4 mg), then gradually increase it, observing individual tolerance.
Gradual withdrawal of the drug. After prolonged use of tizanidine (Sirdalud), especially in large doses, it is necessary to gradually discontinue the drug, because. abrupt withdrawal can cause the development of muscle weakness (this is also characteristic of other muscle relaxants).
The use of tizanidin (Sirdalud) to normalize sleep
Side effects of tizanidine (Sirdalud) include increased drowsiness. Therefore, patients who experience drowsiness while taking tizanidine (Sirdalud) should avoid all activities that require increased concentration and responsiveness. At the same time, many patients, especially those with chronic pain syndromes, have disturbed sleep. This side effect of tizanidine (Sirdalud) can be used therapeutically by prescribing the drug at night to improve the patient’s sleep. Given that the effect of tizanidine (Sirdalud) is short-lived, some doctors, in order to maintain the patient’s social activity, prescribe the drug only at night or distribute the main daily dose of the drug in the afternoon and at night. This allows the patient to maintain social activity in the morning (work, drive a car), and in the evening helps to fall asleep, as well as “sleep” other side effects.
Use of tizanidine (Sirdalud) as an antihypertensive
funds
One of the side effects when using tizanidine (Sirdalud) is a moderate decrease in blood pressure. Simultaneous use with antihypertensive agents may enhance the antihypertensive effect. If long-term use of tizanidine (Sirdalud) is necessary (for example, in the treatment of post-stroke spasticity), the hypotensive effect of tizanidine (Sirdalud) can be used to reduce the dose or stop taking blood pressure-lowering drugs if the patient is receiving antihypertensive therapy.
Conclusion
Tizanidine is an effective drug both in the treatment of spasticity in a number of neurological disorders, and for the treatment of a wide range of pain syndromes associated with increased muscle tone. However, the success of the treatment in each particular case depends not only on the correct choice of a particular drug in terms of the symptoms described in the instructions for use and evidence-based studies on the effectiveness of the drug, but also on how the attending physician manages to correlate the features of pharmacokinetic properties of the drug with individual clinical manifestations of the disease in this (specific) patient.

Literature
1. Badokin V.V. The use of Sirdalud in rheumatological practice // Rus. honey. magazine. – 2005. – T. 13, No. 24. – S. 1588-1589.
2. Vorobieva O.V. Possibilities of alpha2-adrenergic agonists in the treatment of myofascial pain // Rus. honey. magazine – 2007. – No. 5. – C. 445–448.
3. Gusev E.I., Boyko A.N. Multiple sclerosis: from new knowledge to new methods of treatment // Ros. honey. magazine. – 2001. – No. 1. – P. 4–10.
4. Danilov A.B. Possibilities of using tizanidine (Sirdalud) in clinical practice. Literature review // RMJ. – 2010. – No. 1. – P. 4–10.
5. Parfenov V.A. Management of patients with spasticity // Rus. honey. magazine. – 2004. – T. 12, No. 10.
6. Parfenov V.A. Diagnosis and treatment of acute pain in the lower back // Rus. honey. magazine – 2007. – T 15 No. 6.
7. Parfenov V.A. Post-stroke spasticity and its treatment // Rus. honey. magazine – 2006. – T. 14, No. 9.
8. Shirokov, E.A. Sirdalud: areas of clinical application // Rus. honey. magazine – 2004. – No. 14. – C. 874–875.
9. Berry H., Hutchinson D.R. Tizanidine and ibuprofen in acute low-back pain: Results of a double-blind multicentre study in general practice // J. Intern. Med. Res. 1988.Vol.16. R. 83–91.
10. Bettucci D., Testa L., Calzoni S. et al. Combination of tizanidine and amitriptyline in the prophylaxis of chronic tension — type headache: evaluation of efficacy and impact on quality of life // J Headache Pain. 2006 Vol. 7(1). P. 34–36.
11. Coward D.M. Tizanidine: Neuropharmacology and mechanism of action // Neurol. 1994 Vol. 44 (Suppl. 9). P. 6–11.
12. Gelber D.A., Good D.C., Dromerick A. et al. Open–Label Dose–Titration Safety and Efficacy Study of Tizanidine Hydrochloride in the Treatment of Spasticity Associated With Chronic Stroke // Stroke. 2001. Vol.32. P. 1841–1846.
13. Hutchinson D.R., Daniels F. A multinational study in general practice to evaluate the effectiveness and tolerability of tizanidine in the treatment of painful muscle spasms // Br. J.Clin. Res. 1990 Vol. 1. P. 39–48.
14. Lataste X., Emre M., Davis C., Groves L. Comparative profile of tizanidine in the management of spasticity // Neurol. 1994 Vol. 44 (suppl 9). P.53–59.
15. Leiphart J.W., Dills C.V., Levy R.M. Alpha2 – adrenergic receptor subtype specificity of intrathecally administered tizanidine used for analgesia for neuropathic pain // J. Neurosurg. 2004 Vol. 101(24). P. 641–647.
16. Sirdalud Ternilin Asia–Pacific Study group. Efficacy and gastroprotective effects of tizanidine plus diclofenac versus placebo plus diclofenac in patients with painful muscle spasm // Curr. Ther. Res. 1998 Vol. 59. P. 13–22.
17. Smolenski C., Muff S., Smolenski–Kautz S. A double–blind comparative trial of new muscle relaxant, tizanidine (DS 103–282), and baclofen in the treatment of chronic spasticity in multiple sclerosis // Curr. Med. Res. Opin. 1981 Vol. 7(6). P. 374–383.
18. Tarrico M., Adone R., Pagliacci C., Telaro E. Pharmacological interventions for spasticity following spinal cord injury. Cochrane Database Systematic Review // The Cochrane Library, 2000. Issue 4.
19. van Tulder M., Becker A., ​​Bekkering T. Et al. European guidelines for the management of acute nonspecific low back pain in primary care // Eur. Spine J. 2006. Vol. 15. (Suppl. 2). S.169–S.191.
20. Wallace J.D. Summary of combined clinical analysis of controlled clinical trials with tizanidine // Neurol. 1994 Vol. 44 (suppl 9). P60-P69.

Tizanidine customer reviews and experiences

Tizanidine reviews

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from 119  ₽

Advantages: No

Disadvantages: No sense

Comment: I took 2 mg 3r / day result zero.

Thinks the product is excellent

from 153  ₽

Drawing pains in the arms, legs, headaches – symptoms that followed me for almost a month, which I took, and like all ordinary people – painkillers, I wanted to make myself feel better. But if at first they helped a little, at least I could sleep a little at night, then later they stopped working. I am not a supporter of going to hospitals, I do not recognize white coats, for me this is a wild horror. Therefore, I decided to get on the Internet and see how people are saved from a similar situation like mine and stumbled (not immediately) on “Tizanidin”, read reviews about it. I understood – I need to try. I don’t call anyone for self-treatment, but I can say with confidence that it’s worth buying these pills, they did their job perfectly. Moreover, the price for them is affordable for every person.

Thinks the product is good

from 153  ₽

I have more than ten years of work experience and sedentary work, in the evening you come and start doing household chores, there is no time to do exercise therapy or go for a walk to stretch your back, as doctors recommend. I took Tizanidin 2 times a day after meals, for its intended purpose, he did an excellent job, but caused terrible drowsiness, it was impossible to work. A colleague advised me to buy it, the price did not push me away, so I decided not to hesitate.

Thinks the product is excellent

from 153  ₽

The drug Tizanidin was prescribed to me in the complex therapy of osteochondrosis. Osteochorosis is an evil sore that can threaten absolutely anyone. With osteochondrosis, pain occurs, muscle spasm occurs from pain, and as a result, the pain intensifies. And Tizanidin removes this spasm. And accordingly, the pain decreases and you can calmly feel like a person. The price for it is much lower than the original drug, I don’t see the point in overpaying because it helps a lot. I recommend buying, but first go to the doctor, suddenly you have a completely different diagnosis.

Thinks the product is excellent

from 153  ₽

After undergoing spinal surgery, my doctor told me to buy Tizanidin. Nothing bothered me, but the drug should be at home in reserve, at any moment there may be pain that needs to be eliminated. Fortunately, I decided to buy and put the pills at home immediately after discharge, they came in handy literally on the third day, when something shot in my back and excruciating pain. The very next day I felt much better, the pain receded. There was some discomfort, but this is a trifle. Yes, and the price of the pills is adequate.

Thinks the product is good

from 153  ₽

In the side effects of the drug Tizanidin, drowsiness is indicated, when I took the first pill, I decided to play it safe and took it at night. In the morning I got up to work quite calmly, my head was not like a box. After a couple of days, I added a dose – I drank a pill both in the morning and in the evening. A similar situation, I didn’t want to sleep, I was alert + unpleasant discomfort left. Only after a certain time I decided to go to the doctor and ask if I was doing the right thing and whether this drug suits me or not (in general, it was worth buying at all or wasting money).