Zanaflex: Targeted Muscle Spasm Relief with Tizanidine
Zanaflex
| Product dosage: 2mg | |||
|---|---|---|---|
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| 360 | $0.79
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Synonyms | |||
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Zanaflex (tizanidine hydrochloride) is a short-acting muscle relaxant indicated for the management of increased muscle tone associated with spasticity. It functions as a central alpha-2-adrenergic agonist, effectively reducing the frequency and amplitude of muscle spasms to improve functional capacity and comfort. This prescription medication is commonly utilized in conditions such as multiple sclerosis, spinal cord injury, and certain neurological disorders where spasticity impairs daily activities or causes discomfort. Proper dosing and medical supervision are essential to maximize therapeutic outcomes while minimizing potential adverse effects.
Features
- Active ingredient: Tizanidine hydrochloride
- Available in 2 mg and 4 mg tablet formulations
- Short half-life of approximately 2.5 hours
- Metabolized primarily by cytochrome P450 1A2
- Central alpha-2-adrenergic agonist mechanism
- FDA-approved for the management of spasticity
Benefits
- Reduces muscle spasticity and clonus, improving range of motion
- Alleviates pain and discomfort associated with muscle spasms
- May enhance ability to perform activities of daily living
- Short-acting profile allows for flexible dosing around functional needs
- Can be used as part of a comprehensive spasticity management program
- Available in generic formulations for cost-effective treatment
Common use
Zanaflex is primarily prescribed for the management of spasticity resulting from multiple sclerosis, spinal cord injuries, and other neurological conditions characterized by increased muscle tone. It is particularly useful when spasticity interferes with function, causes discomfort, or complicates nursing care. Clinicians may also prescribe it off-label for certain types of musculoskeletal pain, tension headaches, or as an adjunct in managing trigeminal neuralgia, though these uses lack formal FDA approval and require careful risk-benefit assessment.
Dosage and direction
The recommended initial dose is 2 mg, taken orally every 6-8 hours as needed for spasticity relief. Dosage may be gradually increased in 2-4 mg increments, with typical maintenance doses ranging from 6-24 mg daily divided into three or four doses. The maximum recommended daily dose is 36 mg. Dosing should be individualized based on efficacy and tolerability, with particular attention to hypotensive effects. Tablets should be taken with water and may be administered with or without food, though consistency in administration relative to meals is advised to minimize pharmacokinetic variability.
Precautions
Zanaflex may cause hypotension, with syncope reported in approximately 3% of patients. Blood pressure monitoring is recommended, especially during dose titration. Sedation occurs frequently, affecting up to 48% of users; patients should avoid driving or operating machinery until they understand how the medication affects them. Hepatotoxicity has been observed, with ALT elevations occurring in approximately 5% of patients; baseline and periodic liver function tests are advised. Abrupt discontinuation after prolonged use may cause rebound hypertension, tachycardia, and hypertonia. Use with caution in elderly patients and those with renal impairment (creatinine clearance < 25 mL/min).
Contraindications
Zanaflex is contraindicated in patients with known hypersensitivity to tizanidine or any component of the formulation. Concurrent use with potent CYP1A2 inhibitors such as fluvoxamine or ciprofloxacin is contraindicated due to significantly increased tizanidine exposure and risk of adverse effects. Severe hepatic impairment represents an absolute contraindication due to impaired metabolism and elimination. The medication should not be administered concomitantly with other alpha-2-adrenergic agonists due to additive pharmacodynamic effects.
Possible side effects
Common adverse reactions (occurring in >5% of patients) include dry mouth (49%), somnolence (48%), asthenia (41%), dizziness (16%), urinary frequency (10%), constipation (9%), and elevated liver enzymes (5%). Less frequent but clinically significant effects include hypotension (4%), bradycardia (2%), hallucinations (3%), and visual disturbances (2%). Rare but serious adverse events include hepatotoxicity, syncope, and anaphylaxis. Most side effects are dose-dependent and may diminish with continued therapy or dose adjustment.
Drug interaction
Tizanidine undergoes extensive metabolism by cytochrome P450 1A2, creating numerous clinically significant interactions. Potent CYP1A2 inhibitors including fluvoxamine, ciprofloxacin, and oral contraceptives may increase tizanidine AUC by up to 33-fold. Concomitant use with antihypertensives may potentiate hypotensive effects. Additive CNS depression occurs with alcohol, benzodiazepines, opioids, and other sedating medications. The combination with other alpha-2-adrenergic agonists may produce excessive cardiovascular effects. Acetaminophen may modestly increase tizanidine concentrations. Physicians should review all medications, including over-the-counter products and supplements, before initiating therapy.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Given the short half-life of tizanidine, a single missed dose is unlikely to cause significant withdrawal effects, though some return of spasticity symptoms may occur. Consistent dosing is important for maintaining therapeutic effects, particularly in patients with severe spasticity.
Overdose
Tizanidine overdose may manifest as pronounced CNS depression, respiratory depression, bradycardia, hypotension, and coma. Management involves supportive care with particular attention to maintaining airway patency and adequate ventilation. Gastric lavage or activated charcoal may be considered if presentation occurs shortly after ingestion. Hypotension typically responds to intravenous fluids and Trendelenburg positioning; vasopressors may be required in severe cases. Bradycardia may necessitate atropine administration. There is no specific antidote for tizanidine overdose. Dialysis is unlikely to be beneficial due to extensive protein binding and volume of distribution.
Storage
Store Zanaflex tablets at controlled room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). Protect from light and moisture. Keep in the original container with the lid tightly closed. Do not store in bathroom cabinets where humidity may compromise stability. Keep all medications out of reach of children and pets. Properly dispose of expired or unused medication through drug take-back programs or according to FDA guidelines to prevent accidental ingestion or environmental contamination.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Zanaflex is a prescription medication that should be used only under the supervision of a qualified healthcare provider. Individual response to therapy may vary, and only a healthcare professional can determine the appropriate treatment based on a patient’s specific medical condition, concomitant medications, and overall health status. Patients should not alter their dosage or discontinue medication without consulting their physician.
Reviews
Clinical studies demonstrate that approximately 60-70% of patients with spasticity experience meaningful improvement in muscle tone with Zanaflex therapy. Many patients report significant reduction in painful spasms and improved ability to perform daily activities. The sedative effects are frequently cited as a limiting factor, particularly during the dose titration phase. Patients appreciate the short duration of action, which allows for dosing around specific activities requiring reduced spasticity. Long-term users note the importance of consistent dosing timing to maintain stable therapeutic effects while minimizing side effects.