What is tizanidine used for. How does tizanidine work. What are the common side effects of tizanidine. What are the serious side effects of tizanidine. How does tizanidine interact with other medications. What precautions should be taken when using tizanidine. How is tizanidine dosage determined.

Understanding Tizanidine: A Powerful Muscle Relaxant

Tizanidine, available under the brand name Zanaflex, is a prescription medication primarily used to manage muscle spasms. This alpha-2-adrenergic agonist works by reducing nerve activity in the spinal cord, effectively decreasing muscle tightness, pain, and stiffness. It’s particularly beneficial for individuals with multiple sclerosis, spinal cord injuries, or muscle spasticity.

Tizanidine is available in two forms: oral tablets and oral capsules. While the brand-name version Zanaflex is well-known, generic alternatives are also available, often at a lower cost. The availability of generic options may vary in terms of strength and form compared to the brand-name drug.

The Mechanism of Action: How Tizanidine Works

How does tizanidine actually work to alleviate muscle spasms? Tizanidine belongs to a class of drugs called alpha-2-adrenergic agonists. These medications function by targeting specific receptors in the central nervous system. When tizanidine binds to these receptors, it reduces the activity of nerves in the spinal cord that control muscle function. This decreased nerve activity leads to a reduction in muscle spasms and associated symptoms.

Key Benefits of Tizanidine’s Mechanism

• Reduces muscle tightness
• Alleviates pain associated with muscle spasms
• Decreases muscle stiffness
• Improves mobility and function for patients with certain neurological conditions

Common Side Effects: What to Expect When Taking Tizanidine

What are the most common side effects of tizanidine? Like all medications, tizanidine can cause various side effects, although not everyone experiences them. Some of the more frequently reported side effects include:

• Dry mouth
• Tiredness and weakness
• Dizziness
• Urinary tract infection
• Constipation
• Vomiting
• Speech difficulties
• Runny nose and sore throat
• Vision problems

These side effects are typically mild and may subside within a few days or weeks as your body adjusts to the medication. However, if these effects persist or worsen, it’s important to consult your healthcare provider.

Serious Side Effects: When to Seek Medical Attention

While less common, tizanidine can potentially cause serious side effects that require immediate medical attention. What are the serious side effects of tizanidine that warrant urgent care?

1. Hallucinations: Seeing things that aren’t real
2. Delusions: Believing things that aren’t real
3. Extremely low blood pressure: Causing dizziness or lightheadedness, especially when changing positions
4. Liver damage: Symptoms may include increased bleeding, bruising, or yellowing of the skin or eyes
5. Severe sedation: Extreme dizziness, weakness, fatigue, or sleepiness

If you experience any of these serious side effects, it’s crucial to stop taking tizanidine and seek immediate medical attention. In case of life-threatening symptoms, call emergency services right away.

Tizanidine Interactions: Medications to Avoid

Tizanidine can interact with various medications, potentially altering its effectiveness or increasing the risk of side effects. How does tizanidine interact with other medications, and which drugs should be avoided?

Some medications that should not be used concurrently with tizanidine include:

• Fluvoxamine: An antidepressant that can significantly increase tizanidine levels in the body
• Ciprofloxacin (Cipro): An antibiotic that can also increase tizanidine concentrations
• Other alpha-2 adrenergic agonists: Combining these medications can lead to additive effects and increased risk of side effects

Using these medications with tizanidine can result in dangerously low blood pressure, increased drowsiness, or decreased muscle control. It’s essential to inform your healthcare provider about all medications, vitamins, and herbal supplements you’re taking to avoid potential interactions.

Precautions and Warnings: Ensuring Safe Use of Tizanidine

What precautions should be taken when using tizanidine? Several important warnings and precautions should be considered when taking this medication:

Low Blood Pressure Risk

Tizanidine can cause very low blood pressure, leading to dizziness or fainting. To mitigate this risk, doctors typically prescribe the lowest effective dose. If you’re already taking blood pressure-lowering medications, more frequent monitoring may be necessary.

Liver Function Concerns

There’s a risk of liver damage associated with tizanidine use. Patients with pre-existing liver disease should discuss the safety of this medication with their healthcare provider. Regular monitoring of liver function may be required during treatment.

Sedation and Drug Interactions

Tizanidine can cause significant drowsiness. This effect can be intensified when combined with alcohol, benzodiazepines, opioids, or tricyclic antidepressants. It’s crucial to avoid these combinations and inform your doctor about all substances you’re using.

Dosage Guidelines: Finding the Right Balance

How is tizanidine dosage determined? The appropriate dosage of tizanidine varies depending on several factors, including the individual’s medical condition, response to treatment, and other medications they may be taking.

Starting Dose

Typically, the initial dose is 2 mg taken orally every 6 to 8 hours, as needed. The dosage may be gradually increased by 2 to 4 mg at each dose, with 1 to 4 days between dosage increases. The maximum recommended dose is 36 mg per day.

Dosage Adjustments

Dosage adjustments may be necessary for patients with renal impairment or those taking certain interacting medications. It’s crucial to follow your healthcare provider’s instructions carefully and not adjust the dose without consultation.

Long-Term Use and Monitoring: Ensuring Continued Safety and Efficacy

For patients using tizanidine over extended periods, regular monitoring is essential to ensure ongoing safety and effectiveness. What aspects of long-term tizanidine use require careful attention?

Liver Function Tests

Due to the potential for liver damage, periodic liver function tests may be recommended, especially during the first few months of treatment or when dosage is increased.

Blood Pressure Monitoring

Regular blood pressure checks are important, particularly for patients with a history of cardiovascular issues or those taking other medications that affect blood pressure.

Efficacy Assessment

Healthcare providers will periodically assess the continued effectiveness of tizanidine in managing muscle spasms and may adjust the treatment plan as needed.

Addiction Potential

While tizanidine is not considered highly addictive, long-term use can lead to physical dependence. Any plans to discontinue the medication should be discussed with a healthcare provider to develop an appropriate tapering schedule.

By maintaining open communication with your healthcare provider and adhering to recommended monitoring protocols, the long-term use of tizanidine can be managed safely and effectively.

Alternative Treatments: Exploring Options Beyond Tizanidine

While tizanidine is an effective treatment for muscle spasms, it may not be suitable for everyone. What alternative treatments are available for managing muscle spasticity?

Other Medications

• Baclofen: Another muscle relaxant that works differently from tizanidine
• Dantrolene: Acts directly on skeletal muscles to reduce spasticity
• Benzodiazepines: Can help relax muscles but carry a risk of dependence
• Botulinum toxin injections: Useful for localized muscle spasticity

Non-Pharmacological Approaches

1. Physical therapy: Stretching exercises and range-of-motion techniques
2. Occupational therapy: Adaptive equipment and strategies for daily activities
3. Heat therapy: Can help relax tight muscles
4. Massage: May provide temporary relief from muscle tension
5. Acupuncture: Some patients find relief through this traditional Chinese medicine practice

The choice of treatment depends on individual factors such as the underlying condition, severity of symptoms, and potential side effects. A comprehensive treatment plan often involves a combination of approaches tailored to the patient’s specific needs.

Patient Experiences: Real-World Insights on Tizanidine Use

Understanding the experiences of patients who have used tizanidine can provide valuable insights for those considering or starting this medication. What do patients typically report about their experiences with tizanidine?

Positive Experiences

• Significant reduction in muscle spasms and associated pain
• Improved sleep quality due to reduced nighttime muscle tension
• Enhanced ability to perform daily activities and exercises
• Rapid onset of action, with some patients reporting relief within an hour of taking the medication

Challenges and Side Effects

Some patients report challenges such as:

• Initial drowsiness that may improve over time
• Dry mouth, which can be managed with proper hydration and oral hygiene
• Dizziness, particularly when changing positions quickly
• The need for careful timing of doses to balance symptom relief with daily activities

It’s important to note that individual experiences can vary significantly. Open communication with healthcare providers about both benefits and side effects is crucial for optimizing treatment outcomes.

Future Developments: Advancing Muscle Spasticity Treatment

As medical research continues to advance, what future developments might we see in the treatment of muscle spasticity? Several promising areas of research are underway:

Targeted Drug Delivery Systems

Researchers are exploring ways to deliver muscle relaxants more directly to affected areas, potentially reducing systemic side effects. This could include advanced transdermal patches or localized injection techniques.

Combination Therapies

Studies are investigating the potential benefits of combining tizanidine with other medications or therapies to enhance efficacy while minimizing side effects.

Genetic Factors in Treatment Response

Ongoing research aims to identify genetic markers that may predict an individual’s response to tizanidine and other muscle relaxants, paving the way for more personalized treatment approaches.

Novel Drug Development

Pharmaceutical companies continue to research new compounds that may offer improved efficacy or safety profiles compared to existing muscle relaxants.

These advancements hold promise for improving the management of muscle spasticity and enhancing the quality of life for individuals affected by conditions such as multiple sclerosis and spinal cord injuries.

Side Effects, Dosage, Uses, and More

Highlights for tizanidine

1. Tizanidine oral tablet is available as both a generic and brand-name drug. Brand name: Zanaflex.
2. Tizanidine also comes as an oral capsule.
3. Tizanidine oral tablet is used to manage muscle spasms. It’s often used for people with multiple sclerosis, spinal cord injury, or muscle spasticity.

• Low blood pressure warning. Tizanidine can cause very low blood pressure that leads to dizziness or fainting. To help reduce this risk, your doctor may prescribe the lowest dose of this drug that works for you. If you already take medications that lower blood pressure, your doctor may check your blood pressure more often.
• Liver damage warning. Tizanidine can cause liver damage. If you have liver disease, talk with your doctor about whether this drug is safe for you. If you take this drug, your doctor may monitor you for changes in how well your liver works.
• Hallucinations or delusions warning. Tizanidine can cause visual hallucinations (seeing things that aren’t real). It can also cause delusions (believing things that aren’t real). If have either of these side effects, stop taking this drug and call your doctor right away.
• Sedation (drowsiness) warning. Tizanidine can cause sedation. Taking tizanidine with alcohol or certain drugs (benzodiazepines, opioids, or tricyclic antidepressants) can increase sedation. Tell your doctor or pharmacist about all medications, vitamins, or herbs you’re taking.

Tizanidine is a prescription drug that comes as an oral tablet and an oral capsule.

Tizanidine oral tablet is available as a brand-name drug Zanaflex. It’s also available as a generic drug. Generic drugs usually cost less than the brand-name version. In some cases, they may not be available in all strengths or forms as the brand-name drug.

Why it’s used

Tizanidine oral tablet is used to manage muscle spasms. Symptoms can include muscle tightness, pain, or stiffness. This drug is often used for people with multiple sclerosis, spinal cord injury, or muscle spasticity.

How it works

Tizanidine belongs to a class of drugs called alpha-2-adrenergic agonists. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

Tizanidine reduces the activity of nerves in the spinal cord that control muscles. This helps to reduce muscle spasms.

Tizanidine oral tablet may cause drowsiness. It may also cause other side effects.

More common side effects

The more common side effects of tizanidine can include:

• dry mouth
• tiredness
• weakness
• dizziness
• urinary tract infection
• constipation
• vomiting
• trouble speaking
• runny nose
• sore throat
• vision problems

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 with 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:

• Hallucinations. Symptoms can include:
  • seeing things that aren’t real
• Delusions. Symptoms can include:
  • believing things that aren’t real
• Extremely low blood pressure. Symptoms can include:
  • dizziness or lightheadedness, especially when standing after sitting or lying down
• Liver damage. Symptoms can include:
  • increased bleeding or bruising
  • yellowing of your skin or the whites of your eyes
• Sedation. Symptoms can include:
  • dizziness
  • weakness
  • fatigue and sleepiness

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 professional who knows your medical history.

Tizanidine 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 with your doctor or pharmacist.

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

Drugs that should not be used with tizanidine

Do not take these drugs with tizanidine. When used with tizanidine, these drugs can cause dangerous effects in the body. Examples of these drugs include:

• Fluvoxamine and ciprofloxacin (Cipro). Using these drugs with tizanidine may cause very low blood pressure. It may also cause increased drowsiness or decreased muscle control.
• Other alpha-2 agonist medications such as clonidine, methyldopa, or guanfacine. Using these drugs with tizanidine can cause very low blood pressure.

Drugs that increase the risk of side effects from tizanidine

Taking tizanidine with certain medications raises your risk for side effects from tizanidine. This is because the amount of tizanidine in your body is increased. Avoid using these drugs with tizanidine if possible. Examples of these drugs include:

• Zileuton. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.
• Certain antibiotics called fluoroquinolones (other than ciprofloxacin), such as levofloxacin, moxifloxacin, or gemifloxacin. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.
• Certain heart rhythm drugs such as amiodarone, mexiletine, propafenone, or verapamil. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.
• Antacids such as cimetidine or famotidine. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.
• Oral contraceptives. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.
• Acyclovir. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.
• Ticlopidine. Increased side effects can include decreased blood pressure, decreased heart rate, or extreme drowsiness.

Using tizanidine with the following drugs can cause excessive sedation (drowsiness):

• benzodiazepines such as alprazolam, lorazepam, or diazepam.
• opioids such as morphine, methadone, or oxycodone.
• certain antidepressants such as amitriptyline, nortriptyline, or protriptyline.

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 professional about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.

Tizanidine oral tablet comes with several warnings.

Allergy warning

Tizanidine can cause a severe allergic reaction. Symptoms can include:

• trouble breathing
• itching
• 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 warning

The use of drinks that contain alcohol increases the amount of tizanidine in your body. This can cause increased side effects from tizanidine.

Warnings for people with certain health conditions

For people with decreased liver function. Talk with your doctor about whether tizanidine is safe for you. If you take this drug, your doctor may give you a lower dose. Also, your doctor should check your liver function at the start of treatment. They may check it again 1 month after your maximum dose has been prescribed.

For people with decreased kidney function. Talk with your doctor about whether tizanidine is safe for you. If you take this drug, your doctor may give you a lower dose. Also, your doctor will watch for buildup of too much tizanidine in your body. Symptoms can include dry mouth, dizziness, or drowsiness.

Warnings for other groups

For pregnant women. Tizanidine is a category C pregnancy drug. That means two things:

1. Research in animals has shown adverse effects to the fetus when the mother takes the drug.
2. There haven’t been enough studies done in humans to be certain how the drug might affect the fetus.

Talk with your doctor if you’re pregnant or planning to become pregnant. This drug should only be used if the potential benefit justifies the potential risk to the fetus. Call your doctor if you become pregnant while taking this drug.

For women who are breastfeeding. It’s not known if tizanidine passes into breast milk and causes side effects in a child who is breastfed. Talk with your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

For seniors. The kidneys of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stays in your body for a longer time. This raises your risk for side effects.

For children. This medication has not been studied in children. It should not be used in people younger than 18 years.

This dosage information is for tizanidine 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: Tizanidine

• Form: oral tablet
• Strengths: 2 mg, 4 mg

Brand: Zanaflex

• Form: oral tablet
• Strengths: 4 mg

Dosage for muscle spasms

Adult dosage (ages 18 years and older)

• Typical starting dosage: 2 mg every 6–8 hours as needed.
• Dosage increases: Your doctor may increase your dosage by 2–4 mg until your symptoms are controlled. They will wait 1–4 days between any increases.
• Maximum dosage: 3 doses in 24 hours.

Child dosage (ages 0–17 years)

This medication has not been studied in children. It should not be used in people younger than 18 years.

Senior dosage (ages 65 years and older)

The kidneys of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stays in your body for a longer time. This raises your risk for side effects. Your doctor may start you on a lowered dose or a different dosing schedule. This can help keep levels of this drug from building up too much in your body.

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.

Tizanidine oral tablet is used for long-term or short-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: If you stop taking tizanidine suddenly, you are at risk for withdrawal symptoms. This risk is higher if you’ve been taking high doses of the drug or taking it for a long period of time.

Withdrawal symptoms can include high blood pressure, a fast heart rate, or worsened muscle spasms. If you decide to stop this drug, your doctor should slowly decrease your dosage by 2–4 mg per day.

If you don’t take this drug at all, your muscle spasms may not improve.

If you miss doses or don’t take the drug on schedule: Your medication may not work as well or may stop working completely. If you miss too many doses, you may have withdrawal symptoms.

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

• extreme tiredness
• confusion
• coma
• decreased heart rate
• severe decrease in blood pressure
• slowed breathing

If you think you’ve taken too much of this drug, call your doctor or seek guidance from the American Association of Poison Control Centers at 800-222-1222 or through their online tool. But 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 fewer symptoms of muscle spasms. These symptoms can include muscle tightness, pain, or stiffness.

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

General

• You can take tizanidine with or without food. But you should be consistent. Take it the same way each time.
• You can cut or crush the tablet.

Storage

• Store tizanidine tablets at 77°F (25°C). You can store them for a short time at temperatures between 59°F and 86°F (15°C and 30°C).
• Don’t store this medication in moist or damp areas, such as bathrooms.

Refills

A prescription for this medication is refillable. You should not 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 container 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

You and your doctor should monitor certain health issues. This can help make sure you stay safe while you take tizanidine. These issues include:

• Kidney function. Blood tests can check how well your kidneys are working. If your kidneys aren’t working well, your doctor may lower your dosage of this drug.
• Liver function. Blood tests can check how well your liver is working. If your liver isn’t working well, your doctor may lower your dosage of this drug.
• Blood pressure. Your doctor may check your blood pressure to make sure that it does not get too low while you’re taking this drug.

Availability

Not every pharmacy stocks this drug. When filling your prescription, be sure to call ahead to make sure your pharmacy carries it.

Insurance

Many insurance companies require a prior authorization for this drug. This means your doctor may need to get approval from your insurance company before your insurance company will pay for the prescription.

There are other drugs available to treat your condition. Some may be better suited for you than others. Talk with 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.

Generic Zanaflex Availability – Drugs.com

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Last updated on Jul 12, 2023.

Zanaflex is a brand name of tizanidine, approved by the FDA in the following formulation(s):

ZANAFLEX (tizanidine hydrochloride – capsule;oral)

• Manufacturer: LEGACY PHARMA
  Approval date: August 29, 2002
  Strength(s): EQ 2MG BASE ^[RLD][AB], EQ 4MG BASE ^[RLD][AB], EQ 6MG BASE ^[RLD][AB]

ZANAFLEX (tizanidine hydrochloride – tablet;oral)

• Manufacturer: LEGACY PHARMA
  Approval date: November 27, 1996
  Strength(s): EQ 4MG BASE ^[RLD][AB]
• Manufacturer: LEGACY PHARMA
  Approval date: February 4, 2000
  Strength(s): EQ 2MG BASE (discontinued) ^[RLD]

Has a generic version of Zanaflex been approved?

Yes. The following products are equivalent to Zanaflex:

tizanidine hydrochloride capsule;oral

• Manufacturer: ALEMBIC
  Approval date: January 13, 2020
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: ALKEM LABS LTD
  Approval date: March 27, 2019
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: APOTEX INC
  Approval date: February 3, 2012
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: AUROBINDO PHARMA LTD
  Approval date: March 24, 2020
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: CADILA PHARMS LTD
  Approval date: March 26, 2019
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: JUBILANT GENERICS
  Approval date: August 4, 2017
  Strength(s): EQ 6MG BASE ^[AB], EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB]
• Manufacturer: NOVAST LABS
  Approval date: March 12, 2019
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: RUBICON
  Approval date: May 27, 2020
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]
• Manufacturer: ZYDUS PHARMS
  Approval date: March 3, 2017
  Strength(s): EQ 2MG BASE ^[AB], EQ 4MG BASE ^[AB], EQ 6MG BASE ^[AB]

tizanidine hydrochloride tablet;oral

• Manufacturer: ALKEM LABS LTD
  Approval date: January 25, 2019
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: APOTEX
  Approval date: January 16, 2004
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: CADILA
  Approval date: March 9, 2018
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: CASI PHARMS INC
  Approval date: June 27, 2002
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: DR REDDYS LABS INC
  Approval date: July 3, 2002
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: EPIC PHARMA LLC
  Approval date: October 11, 2002
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: OXFORD PHARMS
  Approval date: October 20, 2003
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: SUN PHARM INDS INC
  Approval date: September 29, 2003
  Strength(s): EQ 4MG BASE ^[AB]
• Manufacturer: UNICHEM LABS LTD
  Approval date: November 28, 2012
  Strength(s): EQ 4MG BASE ^[AB]

Note: Fraudulent online pharmacies may attempt to sell an illegal generic version of Zanaflex. These medications may be counterfeit and potentially unsafe. If you purchase medications online, be sure you are buying from a reputable and valid online pharmacy. Ask your health care provider for advice if you are unsure about the online purchase of any medication.

See also: Generic Drug FAQ.

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Glossary

Term	Definition
Drug Patent	A drug patent is assigned by the U. S. Patent and Trademark Office and assigns exclusive legal right to the patent holder to protect the proprietary chemical formulation. The patent assigns exclusive legal right to the inventor or patent holder, and may include entities such as the drug brand name, trademark, product dosage form, ingredient formulation, or manufacturing process A patent usually expires 20 years from the date of filing, but can be variable based on many factors, including development of new formulations of the original chemical, and patent infringement litigation.
Drug Exclusivity	Exclusivity is the sole marketing rights granted by the FDA to a manufacturer upon the approval of a drug and may run simultaneously with a patent. Exclusivity periods can run from 180 days to seven years depending upon the circumstance of the exclusivity grant.
RLD	A Reference Listed Drug (RLD) is an approved drug product to which new generic versions are compared to show that they are bioequivalent. A drug company seeking approval to market a generic equivalent must refer to the Reference Listed Drug in its Abbreviated New Drug Application (ANDA). By designating a single reference listed drug as the standard to which all generic versions must be shown to be bioequivalent, FDA hopes to avoid possible significant variations among generic drugs and their brand name counterpart.
AB	Products meeting necessary bioequivalence requirements. Multisource drug products listed under the same heading (e.g. identical active ingredients, dosage form, and routes of administration) and having the same strength (see Therapeutic Equivalence-Related Terms, Pharmaceutical Equivalents) generally will be coded AB if a study is submitted demonstrating bioequivalence. In certain instances, a number is added to the end of the AB code to make a three character code (e.g. AB1, AB2, AB7). Three-character codes are assigned only in situations when more than one reference listed drug of the same strength has been designated under the same heading. Two or more reference listed drugs are generally selected only when there are at least two potential reference drug products which are not bioequivalent to each other. If a study is submitted that demonstrates bioequivalence to a specific listed drug product, the generic product will be given the same three-character code as the reference listed drug it was compared against.

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Pharmacological properties

Pharmacodynamics

Tizanidin is a centrally acting skeletal muscle relaxant. The main site of action of the drug is the spinal cord: available evidence shows that by stimulating presynaptic alpha ₂ receptors, the drug inhibits the release of excitatory amino acids that stimulate N-methyl-D-aspartate (NMDA) receptors. At the same time, polysynaptic signaling at the level of spinal interneurons, which is responsible for excessively high muscle tone, is suppressed, and muscle tone decreases. Tizanidine has no direct effect on skeletal muscle, the neuromuscular junction, or monosynaptic spinal reflexes. In addition to muscle relaxant properties, tizanidine also has a moderately pronounced central analgesic response.

In humans, tizanidine reduces pathologically increased muscle tone, including resistance to passive movement, and relieves painful spasms and muscle contractions.

Pharmacokinetics

Absorption

Tizanidine is rapidly absorbed, reaching peak plasma concentrations approximately 1 hour after dosing.

Distribution

Tizanidine is only 30% bound to plasma proteins and in animal studies it rapidly crosses the blood-brain barrier. The mean volume of distribution at steady state (V _SS ) after intravenous administration is 2. 6 l/kg.

Biotransformation

Despite the good absorption of tizanidine, first pass metabolism limits the availability of the substance from blood plasma to 34% of the intravenous dose. Tizanidine undergoes rapid and extensive metabolism in the liver. Tizanidine is predominantly metabolized by cytochrome P450 isoenzyme 1A2 in vitro .

Excretion

Metabolites are predominantly excreted via the kidneys (about 70% of the dose) and are inactive. Renal excretion of the parent substance is about 53% after a single dose of 5 mg and 66% after doses of 4 mg 3 times a day. The plasma half-life of tizanidine is 2-4 hours.

Linearity

Tizanidine exhibits linear pharmacokinetics over a dose range of 4 mg to 20 mg. The low interindividual variability in pharmacokinetic parameters (C _max and AUC) makes it possible to reliably predict plasma levels after oral administration.

Characteristics in special groups of patients

Pharmacokinetic parameters of tizanidine do not depend on the patient’s gender.

In patients with renal insufficiency (creatinine clearance < 25 ml/min), maximum mean plasma levels of the substance were twice as high as in healthy volunteers, and the terminal half-life increased to approximately 14 hours, resulting in higher (mean 6 times) AUC values.

Effect of food

Simultaneous ingestion of food does not have a clinically significant effect on the pharmacokinetic profile of tizanidine tablets.

Indications for use

• painful muscle spasms;
• spasticity due to multiple sclerosis;
• spasticity due to spinal cord injury;
• spasticity due to brain damage.

Dosage and administration

Rotalud is taken orally. The effect of tizanidine on spasticity is maximal within 2-3 hours after administration with a relative short duration of action. The drug has a high concentration variability in different patients. For this reason, the dose, time and frequency of taking the drug is selected individually depending on the needs of the patient. As a rule, treatment is started with a single dose of 2 mg to minimize adverse reactions. If necessary, the dose is gradually increased.

Painful muscle spasm: adults are prescribed 2-4 mg 3 times a day. In severe cases, an additional dose of 2-4 mg is possible, preferably at bedtime.

Spasticity due to neurological diseases: the dose is selected individually. The initial daily dose should not exceed 6 mg divided into 3 doses. The dose is increased gradually by 2 mg no more than 2 times a week. The optimal therapeutic response is usually achieved with a daily dose of 12 mg to 24 mg administered in 3 or 4 divided doses at regular intervals. A single dose should not exceed 12 mg, the total daily dose is 36 mg.

Slow titration minimizes the risk of adverse reactions.

Use in patients over 65 years of age

Limited experience with elderly patients. Application is recommended only in cases where the benefits clearly outweigh the risks. The results of pharmacokinetic studies indicate that renal excretion in elderly patients in some cases may be significantly reduced. It is recommended to be careful when using: treatment begins with a minimum dose, titration is carried out taking into account efficacy and tolerability.

Use in children

Limited experience with tizanidine in patients under 18 years of age. Tizanidine is not recommended for use in this group of patients.

Use in patients with impaired renal function

In patients with impaired renal function (creatinine clearance < 25 ml/min), treatment should be started at a dose of 2 mg once a day with slow titration until an effective dose is reached. The dose should be increased by no more than 2 mg at a time, guided by tolerability and efficacy: if necessary, it is recommended to slowly increase a single dose, and only then increase the frequency of use. Regular monitoring of kidney function is recommended.

Use in patients with hepatic impairment

Tizanidine is metabolized by the liver. Tizanidine is contraindicated in patients with severe hepatic impairment. It is used with caution in patients with impaired liver function. Treatment begins with a minimum dose, increasing the dose – taking into account tolerability.

Stopping treatment

The duration of treatment is determined by the doctor. If it is necessary to stop treatment, especially in patients who have taken high doses for a long time, it is necessary to reduce the dose slowly to minimize the risk of hypertension and tachycardia.

Adverse effects

The adverse reaction rates used below are defined as follows: common (≥1/100 but <1/10), rare (≥1/10000 but <1/1000), very rare (<1/1000) 10000), the frequency is unknown (according to the available data, it was not possible to establish the frequency of occurrence).

Immune system disorders: frequency unknown – hypersensitivity reactions.

Mental disorders: rarely – hallucinations, insomnia, sleep disturbances; frequency unknown – anxiety disorders, confusion.

Nervous system disorders: often – drowsiness, dizziness; frequency unknown – headache, ataxia, dysarthria.

Violations of the organ of vision: frequency unknown – disturbances of accommodation.

Cardiac disorders: often – bradycardia, tachycardia; the frequency is unknown – in the post-registration period, an increase in the QT interval was observed.

Vascular disorders: often – hypotension, rebound hypertension.

Gastrointestinal disorders: often – dry mouth; rarely – nausea, a violation of the gastrointestinal tract; frequency unknown – abdominal pain, vomiting.

Liver and biliary tract disorders: rarely – increased levels of hepatic transaminases in the blood serum; very rarely – hepatitis, liver failure.

Skin and subcutaneous tissue disorders: frequency unknown – itching, rash.

Musculoskeletal and connective tissue disorders: rarely – muscle weakness.

General disorders: often – fatigue; frequency unknown – lack of appetite.

Laboratory and instrumental studies: often – lowering blood pressure; rarely – increased levels of transaminases.

Hallucinations show no signs of psychosis; hallucinations occurred exclusively in patients who simultaneously took potentially hallucinogenic substances, such as antidepressants.

At low doses, such as those recommended for the relief of painful muscle spasms, drowsiness, fatigue, dizziness, dry mouth, decreased blood pressure, nausea, gastrointestinal disturbances, and increased transaminase levels have been observed; these adverse reactions were usually mild and transient.

At the higher doses recommended for the treatment of spasticity, the adverse reactions observed at lower doses were observed; these reactions were more frequent and more severe, but rarely severe enough to warrant discontinuation of treatment.

In addition, the following adverse reactions may occur: confusion, hypotension, bradycardia, muscle weakness, insomnia, sleep disturbances, hallucinations, hepatitis.

Withdrawal syndrome

Rebound hypertension and tachycardia have been observed after abrupt withdrawal of tizanidine when used for a long time and / or in high daily doses, and / or simultaneously with antihypertensive agents. In extreme cases, rebound hypertension can lead to stroke.

Reporting suspected adverse reactions

Reporting suspected adverse reactions after drug registration is important. If a patient has a serious adverse drug reaction or a new adverse reaction that is not described in the package leaflet for the use of the medicinal product, please inform in accordance with the National Pharmacovigilance System.

Contraindications

• hypersensitivity to tizanidine or to any of the excipients that make up the preparation;
• severe liver dysfunction;
• concomitant use of tizanidine with potent inhibitors of CYP1A2 such as fluvoxamine or ciprofloxacin.

Drug interactions

CYP inhibitors

Contraindicated combinations

Concomitant use of drugs that inhibit CYP1A2 activity may increase plasma levels of tizanidine. The simultaneous use of tizanidine with fluvoxamine or ciprofloxacin is contraindicated. Clinically significant and prolonged hypotension may occur, as well as drowsiness, dizziness, and reduced psychomotor activity.

Combinations not recommended

Co-administration of tizanidine with other CYP1A2 inhibitors such as certain antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, certain fluoroquinolones (enoxacin, pefloxacin, norfloxacin), rofecoxib , oral contraceptives and ticlopidine, not recommended .

Elevated plasma levels of tizanidine may lead to overdose symptoms such as prolongation of the QT(c) interval. The simultaneous use of tizanidine (in high doses) with other drugs that can increase the QT interval (c) is not recommended. ECG monitoring is recommended.

Antihypertensives

Since tizanidine can cause hypotension, it may enhance the effect of antihypertensives, including diuretics, so caution should be exercised in patients receiving antihypertensive therapy. Caution should also be exercised when tizanidine is co-administered with antihypertensive agents, beta-adrenergic receptor blockers, or digoxin, as such combinations may exacerbate hypotension or bradycardia. Some patients have experienced rebound hypertension and tachycardia after abrupt discontinuation of tizanidine taken concomitantly with antihypertensive agents. Rebound hypertension can lead to stroke.

Oral contraceptives

Pharmacokinetic data on single and multiple doses of tizanidine show that the excretion of the substance is reduced by approximately 50% in women taking oral contraceptives at the same time. Specific pharmacokinetic studies of the potential interaction of tizanidine with oral contraceptives have not been conducted, however, one should be aware of the possible clinical response and / or the occurrence of adverse events at lower doses of tizanidine when prescribing the drug to patients taking contraceptives. No clinically significant interactions were observed in clinical studies.

Other interactions

Alcohol and sedatives may increase the sedative effect of tizanidine.

Warnings

CYP inhibitors

Concomitant use of tizanidine with CYP1A2 inhibitors is not recommended.

Hypotension

Hypotension may develop during treatment with tizanidine and as a result of drug interactions with CYP1A2 inhibitors and/or antihypertensive agents. Severe manifestations of hypotension, such as loss of consciousness and circulatory collapse, have been noted.

Withdrawal syndrome

Rebound hypertension and tachycardia have been observed after abrupt withdrawal of tizanidine when used for a long time and / or in high daily doses, and / or simultaneously with antihypertensive agents. Rebound hypertension can lead to stroke. Tizanidine is canceled gradually.

Renal insufficiency

In patients with renal insufficiency (creatinine clearance < 25 ml/min), it is recommended to start treatment with a dose of 2 mg 1 time per day. Dose escalation should be slow, taking into account tolerability and efficacy. If it is necessary to increase the effectiveness, it is recommended to slowly increase a single dose, and only then increase the frequency of use.

Cardiovascular, hepatic, or renal impairment

Caution is required in patients with cardiovascular, coronary artery disease, or impaired renal or hepatic function. Regular monitoring of liver function, kidney function, ECG is recommended.

Impaired liver function

Cases of tizanidine-related liver dysfunction have been reported, but these cases have been rare with daily doses up to 12 mg. It is recommended to monitor liver function tests monthly during the first 4 months of treatment in patients taking doses of 12 mg and above, as well as in patients with suspected liver dysfunction (unexplained nausea, anorexia or fatigue). Treatment with tizanidine should be discontinued if serum levels of AST and ALT persistently exceed the upper limit of normal by 3 times or more. Tizanidine should be discontinued in patients with symptoms of hepatitis or jaundice.

Rotalud tablets contain lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.

Use in pregnancy and lactation

Pregnancy

In animal studies, pre- and postnatal mortality was observed at doses that are toxic to the mother’s body.

Since no controlled studies have been conducted in pregnant women, the drug should be used during pregnancy only if the benefit clearly outweighs the risk.

Lactation

Although only small amounts of tizanidine are excreted in breast milk, women who are breastfeeding should not take tizanidine.

Pediatric use

Due to lack of data, the use of the drug in children and adolescents under 18 years of age is not recommended.

Influence on the ability to drive vehicles and control mechanisms

Patients experiencing drowsiness, dizziness or other signs or symptoms of hypotension should refrain from activities that require a high degree of concentration.

The drug should be kept out of the reach of children and not used after the expiration date.

Overdose

Clinical experience is limited. A case of oral administration of 400 mg of tizanidine has been described in an adult patient. The patient received mannitol and furosemide, recovery was uneventful.

Possible symptoms

Nausea, vomiting, hypotension, bradycardia, QT prolongation, dizziness, miosis, respiratory depression, coma, restlessness, drowsiness.

Treatment

If less than an hour has passed after taking the drug, it is necessary to induce vomiting, gastric lavage, give high doses of activated charcoal, ensure sufficient hydration of the patient, since forced diuresis is expected to accelerate the elimination of tizanidine. Further treatment should be symptomatic.

Presentation

Tablets. 10 tablets in a blister. 1, 2 or 3 blisters with instructions for use in a cardboard box.

Storage conditions

Store below 25°C.

Shelf life

3 years.

Terms of dispensing from pharmacies

Available by prescription.

Manufacturer

The trademark and registration certificate are owned by

Rotapharm Ilaçlari Limited Shirketi, Turkey

(“Rotapharm Ilaçlari Limited Şirketi”, Turkey).

Manufactured by

World Medical Ilach San. ve Tij. A.Sh., Türkiye

(Bagcilar Ilchesi, Guneshli, Evren Mahallesi,

Jami Yolu Jad. No. 50 K. 1B Zemin 4-5-6, Istanbul)

“World Medicine İlaç San. ve Tic. A.Ş.”, Turkey

Name and address of the organization accepting claims (proposals) on the quality of medicines in the Republic of Uzbekistan

Tar Pharm Alliance LLC,

Republic of Uzbekistan, Tashkent, Mirabad district, Sayhun street, house 166

Phone: 277-76-78, 277-76-48

INN:
Rec.INN

Single component preparations

trade names of preparations containing only the active substance
TIZANIDINE

Descriptions of drugs with inactive reg. beats or not supplied to the Russian market