Tizanidine: Effective Muscle Spasticity Relief
Tizanidine
| Product dosage: 2mg | |||
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| 60 | $2.52 | $176.00 $151.00 (14%) | 🛒 Add to cart |
| 90 | $2.38
Best per pill | $264.00 $214.00 (19%) | 🛒 Add to cart |
Synonyms | |||
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 muscle spasticity, tizanidine helps improve patient mobility, decrease painful spasms, and enhance overall functional capacity. Its short half-life allows for flexible dosing, though it requires careful titration to balance efficacy with its sedative properties.
Features
- Centrally acting alpha-2 adrenergic receptor agonist
- Available in 2 mg and 4 mg oral tablets, and capsule formulations
- Rapid onset of action, typically within one hour
- Short elimination half-life of approximately 2.5 hours
- Metabolized primarily by cytochrome P450 1A2 (CYP1A2)
- Excreted mainly via the kidneys
Benefits
- Provides significant reduction in muscle tone and frequency of spasms
- Enhances range of motion and voluntary motor function
- Can alleviate associated pain and discomfort from spasticity
- Improves ability to perform activities of daily living
- Offers flexible dosing due to short duration of effect
- May be used as needed or on a scheduled basis per physician guidance
Common use
Tizanidine is indicated for the management of spasticity. It is most commonly prescribed for patients with neurological conditions such as multiple sclerosis and chronic spinal cord injury, where upper motor neuron lesions lead to clinically significant spasticity that interferes with daily function or rehabilitation. It is used to manage both chronic spasticity and acute painful muscle spasms. Its use is typically part of a comprehensive treatment plan that includes physical therapy and other modalities.
Dosage and direction
The initial dose is 2 mg, administered orally every 6 to 8 hours as needed. Dosage can be gradually titrated upward in 2–4 mg increments, with a typical dosing interval of every 6 to 8 hours. The maximum recommended total daily dose is 36 mg, though most patients do not require more than 24 mg per day. Doses should be spaced a minimum of 6 hours apart. Administration with food can significantly affect absorption; consistency in relation to meals is advised to maintain predictable plasma levels. The dose must be individualized based on efficacy and tolerability, particularly regarding sedation and hypotension.
Precautions
Tizanidine can cause significant hypotension. Monitor blood pressure, especially with initial dose titration and when adding other antihypertensive agents. It exerts sedative effects; patients should be cautioned about operating machinery or driving until they know how the medication affects them. Use with caution in patients with renal impairment (creatinine clearance < 25 mL/min), as clearance is reduced. Hepatic impairment significantly increases drug exposure; use is contraindicated in patients with significant liver disease. Abrupt discontinuation should be avoided due to the potential for rebound hypertension, tachycardia, and hypertonia.
Contraindications
Concomitant use with potent CYP1A2 inhibitors, such as fluvoxamine or ciprofloxacin, is contraindicated. Tizanidine is contraindicated in patients with known hypersensitivity to the drug or any of its components. Its use is also contraindicated in patients with significant hepatic impairment.
Possible side effect
The most common side effects are dose-related and include:
- Sedation, somnolence, and drowsiness (up to 48% of patients)
- Dry mouth (up to 49% of patients)
- Asthenia (weakness) and fatigue
- Dizziness
- Hypotension
- Elevated liver enzymes (ALT) Other reported side effects include hallucinations, visual disturbances, bradycardia, nausea, and gastrointestinal discomfort.
Drug interaction
Tizanidine has numerous clinically significant interactions. Concomitant use with other CNS depressants (alcohol, benzodiazepines, opioids) can potentiate sedation and cognitive impairment. It interacts strongly with CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin, zileuton, oral contraceptives), which can dramatically increase tizanidine plasma levels and the risk of adverse effects. Use with other antihypertensive agents or alpha-adrenergic agonists can potentiate hypotension and bradycardia. Acetaminophen may delay the absorption of tizanidine.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. Do not double the dose to make up for a missed one.
Overdose
Symptoms of overdose are an extension of its pharmacological effects and may include severe dizziness, profound sedation, somnolence, coma, respiratory depression, bradycardia, and hypotension. Ventricular tachycardia and QT prolongation have been reported. Management is supportive and includes gastric lavage (if presented early) and activated charcoal. Vital signs should be monitored closely, with attention to airway protection and cardiovascular support. There is no specific antidote.
Storage
Store at room temperature, 20°C to 25°C (68°F to 77°F), in a tight, light-resistant container. Excursions are permitted between 15°C and 30°C (59°F and 86°F). Keep out of reach of children and pets. Do not use after the expiration date printed on the bottle.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
“Tizanidine has been a cornerstone in my spasticity management protocol for appropriate patients. Its rapid onset is highly effective for breaking severe spasms. The primary challenge remains balancing its undeniable efficacy with the nearly universal side effect of sedation, which requires careful, slow titration and patient education.” – Neurologist, 15 years of experience.
“In my rehabilitation practice, tizanidine is invaluable for improving range of motion prior to physical therapy sessions. The flexibility of as-needed dosing allows patients to use it strategically. We consistently observe that its benefits for functional improvement often outweigh the sedative effects, which tend to diminish over time for many patients.” – Physiatrist, 10 years of experience.
“While effective, tizanidine requires meticulous management of drug interactions in a primary care setting. Its interaction profile, particularly with common antibiotics and antidepressants, demands constant vigilance. For a well-selected patient without contraindications, it is a powerful tool, but it is not a first-line agent to be initiated without thorough review of the patient’s complete medication list.” – General Practitioner, 12 years of experience.