Tizanidine: Effective Muscle Spasm Relief for Enhanced Mobility
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Tizanidine hydrochloride is a centrally acting alpha-2 adrenergic agonist indicated for the management of spasticity. It is primarily prescribed to alleviate the increased muscle tone associated with conditions such as multiple sclerosis, spinal cord injury, and certain neurological disorders. By reducing the frequency and amplitude of muscle spasms, tizanidine helps improve patient mobility, decrease discomfort, and facilitate daily activities and rehabilitation efforts. Its therapeutic action is mediated through presynaptic inhibition of motor neurons, offering a targeted approach to spasticity management.
Features
- Active Ingredient: Tizanidine hydrochloride
- Available Formulations: Oral tablets (scored and unscored) and capsules
- Standard Strengths: 2 mg, 4 mg, and 6 mg tablets; 2 mg, 4 mg, and 6 mg capsules
- Pharmacologic Class: Centrally acting alpha-2 adrenergic agonist
- Mechanism of Action: Presynaptic inhibition of spinal motor neurons
- Onset of Action: Approximately 1-2 hours post-administration
- Duration of Effect: 3-6 hours
- Half-life: 2.5 hours on average (range: 1.5-4.5 hours)
- Metabolism: Primarily hepatic via cytochrome P450 1A2 (CYP1A2)
- Excretion: Mainly renal (approximately 60%) and fecal (20%)
Benefits
- Provides rapid relief from painful muscle spasms and spasticity
- Enhances range of motion and functional capacity for daily activities
- Reduces muscle tone without diminishing muscle strength
- Facilitates participation in physical therapy and rehabilitation programs
- Improves sleep quality by minimizing nocturnal spasms
- Offers flexible dosing options to accommodate individual patient needs
Common use
Tizanidine is predominantly prescribed for the management of spasticity resulting from multiple sclerosis, spinal cord injuries, and other neurological conditions characterized by upper motor neuron lesions. It is particularly effective in addressing the muscular hypertonicity that interferes with voluntary movement, causes discomfort, and contributes to functional impairment. Clinicians may also utilize tizanidine off-label for certain types of chronic pain syndromes, tension headaches, and as an adjunct in managing muscle spasm-related conditions. The medication is typically employed as part of a comprehensive treatment plan that may include physical therapy, occupational therapy, and other pharmacological interventions.
Dosage and direction
The initial dosage of tizanidine is typically 2 mg administered orally every 6-8 hours as needed for relief of spasticity. Dosage may be gradually increased in 2-4 mg increments, with intervals of approximately 1/4 to 1 week between increases, based on efficacy and tolerability. The total daily dose should not exceed 36 mg, though most patients achieve optimal effects at doses between 12-24 mg per day, divided into three or four doses.
For patients with renal impairment (creatinine clearance < 25 mL/min), the initial dose should be reduced to 2 mg once daily, with careful titration and monitoring. Hepatically impaired patients require particular caution due to significantly reduced clearance; starting dose should be 2 mg once daily with slow titration.
Administration with food may increase bioavailability but also prolongs the time to peak concentration. Consistency in administration relative to meals is recommended to maintain stable plasma levels.
Precautions
Tizanidine therapy requires careful monitoring due to its potential to cause hypotension, sedation, and hepatotoxicity. Blood pressure should be monitored regularly, especially during dose titration. Patients should be cautioned about activities requiring mental alertness, such as driving or operating machinery, particularly during the initial treatment period.
Liver function tests (ALT, AST) should be performed at baseline and periodically during treatment, as approximately 5% of patients develop elevated transaminases. The medication should be discontinued if ALT or AST levels exceed five times the upper limit of normal.
Elderly patients may be more susceptible to the hypotensive and sedative effects of tizanidine and typically require lower doses. The medication should be used with caution in patients with renal impairment (creatinine clearance < 25 mL/min) due to reduced clearance.
Abrupt discontinuation of tizanidine should be avoided due to the potential for rebound hypertension, tachycardia, and hypertonia. Tapering over 2-4 days is recommended.
Contraindications
Tizanidine is contraindicated in patients with known hypersensitivity to the drug or any component of the formulation. Concurrent use with potent CYP1A2 inhibitors such as fluvoxamine or ciprofloxacin is contraindicated due to the risk of significantly increased tizanidine exposure and enhanced adverse effects.
The medication is contraindicated in patients with severe hepatic impairment (Child-Pugh Class C) due to substantially reduced clearance and increased risk of adverse events. It should not be used concomitantly with other alpha-2 adrenergic agonists due to potential additive effects.
Possible side effect
The most frequently reported adverse reactions include dry mouth (49%), somnolence (48%), asthenia (41%), dizziness (16%), and urinary tract infection (10%). Other common side effects comprise constipation (4%), vomiting (4%), speech disorder (3%), blurred vision (3%), and hypotension (2%).
Less frequent but potentially serious adverse effects include hepatotoxicity (elevated transaminases in 5% of patients), hallucinations (3%), and syncope (2%). Some patients may experience nervousness (1%), anxiety (1%), or rash (1%).
The sedative effects are typically dose-dependent and may diminish with continued therapy. Most side effects are mild to moderate in severity and often transient, though some may necessitate dose adjustment or discontinuation.
Drug interaction
Tizanidine has several clinically significant drug interactions, primarily mediated through CYP1A2 inhibition. Concomitant use with fluvoxamine increases tizanidine AUC by 33-fold and is absolutely contraindicated. Ciprofloxacin increases tizanidine AUC by 10-fold and is also contraindicated.
Other CYP1A2 inhibitors (amiodarone, mexiletine, propafenone, verapamil, oral contraceptives) may increase tizanidine concentrations and require dose adjustment. Concurrent use with other central nervous system depressants (alcohol, benzodiazepines, opioids, barbiturates) may potentiate sedation and cognitive impairment.
Tizanidine may enhance the hypotensive effects of antihypertensive medications and diuretics. Acetaminophen may delay tizanidine absorption when administered concomitantly. The medication may potentiate the QTc-prolonging effects of other drugs that prolong the QT interval.
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.
Due to the short half-life of tizanidine, missing a dose may result in the return of spasticity symptoms. Patients should be educated about maintaining a consistent dosing schedule and may benefit from setting reminders or using pill organizers to improve adherence.
Overdose
Tizanidine overdose may manifest as pronounced hypotension, bradycardia, sedation, respiratory depression, and coma. Other symptoms may include vomiting, weakness, dizziness, and miosis. Management of overdose should include supportive care with close monitoring of vital signs and cardiac function.
Gastric lavage or administration of activated charcoal may be considered if presentation is early. There is no specific antidote for tizanidine overdose. Hypotension may require intravenous fluids and vasopressors, while bradycardia may respond to atropine. Respiratory depression may necessitate ventilatory support.
Patients should be monitored for at least 24 hours due to the potential for delayed effects, particularly with extended-release formulations. Dialysis is not expected to be effective due to tizanidine’s extensive protein binding.
Storage
Tizanidine should be stored at controlled room temperature (20-25°C or 68-77°F), with excursions permitted between 15-30°C (59-86°F). The medication should be kept in its original container, tightly closed, and protected from light and moisture.
Tablets and capsules should be kept out of reach of children and pets. Unused medication should be properly disposed of according to local regulations or through drug take-back programs. Patients should be advised not to store tizanidine in bathrooms or other areas with high humidity.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Tizanidine is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Dosage and treatment decisions must be made by a physician based on individual patient assessment.
The information presented here may not include all possible uses, directions, precautions, or interactions. Patients should consult their healthcare provider for complete information about their specific medical condition and treatment options. Never disregard professional medical advice or delay seeking it because of something you have read in this document.
Reviews
Clinical studies demonstrate that tizanidine provides significant improvement in muscle tone and spasticity compared to placebo. In randomized controlled trials, approximately 60-70% of patients experienced meaningful reduction in muscle tone as measured by the Ashworth Scale.
Patient-reported outcomes indicate improved quality of life measures, particularly regarding sleep quality, pain reduction, and ease of performing daily activities. Many patients report the rapid onset of action as particularly beneficial for managing breakthrough spasticity.
Some reviews note the sedative effects as a limiting factor for some patients, though this often diminishes with continued use. The short duration of action requires multiple daily dosing, which some patients find inconvenient compared to longer-acting alternatives.
Overall, tizanidine is considered an effective first-line option for managing spasticity, with a favorable risk-benefit profile when used appropriately under medical supervision.