Zanaflex: Targeted Muscle Spasm Relief with Tizanidine HCl
| Product dosage: 2mg | |||
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Zanaflex (tizanidine hydrochloride) is a centrally acting alpha-2 adrenergic agonist prescription medication specifically formulated for the management of acute muscle spasticity. Clinically proven to reduce the frequency and intensity of muscle spasms, it provides targeted relief for patients experiencing discomfort and functional impairment due to neurological conditions. By acting on the central nervous system, Zanaflex helps improve range of motion and daily functioning while addressing the underlying hypertonicity associated with spasticity. Its rapid onset of action makes it a valuable therapeutic option for both intermittent and chronic management needs under proper medical supervision.
Features
- Active ingredient: Tizanidine hydrochloride
- Available in 2 mg and 4 mg tablet strengths
- Also available as capsule formulation for modified absorption profile
- Centrally acting alpha-2 adrenergic agonist mechanism
- Rapid onset of action (within 1-2 hours post-administration)
- Short elimination half-life (approximately 2.5 hours)
- Hepatic metabolism primarily via cytochrome P450 1A2
- Renal excretion of metabolites
Benefits
- Effectively reduces painful muscle spasms and clonus
- Improves range of motion and functional mobility
- Decreases muscle tone and resistance to passive movement
- Enhances ability to perform activities of daily living
- Provides flexible dosing for individualized treatment regimens
- May facilitate physical therapy and rehabilitation efforts
Common use
Zanaflex is primarily indicated for the management of spasticity resulting from multiple sclerosis, spinal cord injury, and other neurological conditions characterized by increased muscle tone. Healthcare providers may prescribe it for patients experiencing muscle spasms that interfere with daily activities, sleep, or rehabilitation progress. The medication is particularly valuable when spasticity causes pain, positioning difficulties, or functional limitations. Some clinicians may also utilize Zanaflex off-label for certain types of chronic headaches or musculoskeletal pain conditions, though these uses require careful risk-benefit assessment.
Dosage and direction
The recommended initial dose of Zanaflex is 2 mg administered orally every 6-8 hours as needed for spasticity relief. Dosage may be gradually increased in 2-4 mg increments at intervals of approximately 1-4 days based on therapeutic response and tolerability. The total daily dose typically should not exceed 36 mg, divided into three or four administrations. Dosing should be individualized according to patient needs, with consideration given to the short duration of effect (3-6 hours). The capsules and tablets are not bioequivalent; patients should not switch formulations without medical supervision and appropriate dose adjustment. Administration with food may affect absorption characteristics differently between formulations.
Precautions
Patients taking Zanaflex should exercise caution when engaging in activities requiring mental alertness, such as operating machinery or driving, due to potential sedative effects. Regular monitoring of liver function tests is recommended during treatment, particularly during dose escalation. Blood pressure should be monitored regularly, especially during initial treatment and dose increases. Elderly patients may be more sensitive to the effects of Zanaflex and typically require lower doses. Abrupt discontinuation should be avoided due to potential rebound hypertension and tachycardia. Patients with renal impairment (creatinine clearance < 25 mL/min) require careful dose titration and monitoring.
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. The medication is not recommended for patients with significant hepatic impairment, as clearance may be substantially reduced. Use is also contraindicated in combination with other alpha-2 adrenergic agonists due to potential additive effects.
Possible side effects
The most frequently reported adverse reactions include somnolence (48%), dry mouth (49%), asthenia (41%), dizziness (16%), and urinary frequency (10%). Other common side effects may include hypotension, bradycardia, hallucinations, elevated liver enzymes, and visual disturbances. Less frequently, patients may experience nervousness, dyskinesia, constipation, vomiting, and speech disorders. The sedative effects are often dose-dependent and may diminish with continued therapy. Serious side effects requiring immediate medical attention include hepatotoxicity, severe hypotension, syncope, and hallucinations.
Drug interaction
Zanaflex exhibits significant interactions with several medication classes. Concurrent use with CYP1A2 inhibitors (fluvoxamine, ciprofloxacin, zileuton) may increase tizanidine concentrations up to 33-fold. Combination with other central nervous system depressants (alcohol, benzodiazepines, opioids) may potentiate sedative effects. Antihypertensive agents may have additive effects on blood pressure reduction. Oral contraceptives may decrease tizanidine clearance by approximately 50%. Acetaminophen may delay tizanidine absorption. Physicians should carefully review all concomitant medications before initiating therapy.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should never double the dose to make up for a missed administration. Due to the short half-life of tizanidine, occasional missed doses are unlikely to cause significant withdrawal effects, but may result in return of spasticity symptoms.
Overdose
Symptoms of Zanaflex overdose may include severe dizziness, somnolence, vomiting, hypotension, bradycardia, respiratory depression, and coma. Management involves supportive care with particular attention to maintaining adequate ventilation, cardiovascular support, and symptomatic treatment. Activated charcoal may be beneficial if administered soon after ingestion. Hypertension and tachycardia may occur following recovery from overdose due to rebound effects. Patients should seek immediate medical attention if overdose is suspected.
Storage
Zanaflex should be stored 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). The medication should be kept in its original container, tightly closed, and protected from light and moisture. Keep out of reach of children and pets. Properly discard any unused medication after the expiration date or when no longer needed, following appropriate medication disposal guidelines.
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 professional. Individual response to medication may vary, and only your healthcare provider can determine if this treatment is appropriate for your specific medical condition. Always follow your prescriber’s instructions regarding dosage, administration, and monitoring.
Reviews
Clinical studies demonstrate that Zanaflex provides significant improvement in muscle tone and spasm frequency compared to placebo. In controlled trials, 60-70% of patients experienced meaningful reduction in spasticity symptoms. Many patients report improved sleep quality and decreased pain associated with muscle spasms. Some users note the sedative effects can be bothersome initially but often diminish with continued use. Healthcare providers appreciate the flexibility of dosing options but emphasize the importance of careful patient selection and monitoring due to the potential for hypotension and hepatotoxicity. Overall satisfaction is highest when patients receive appropriate education about timing of administration and management of expected side effects.