Tizanidine: Effective Muscle Spasm Relief and Improved Mobility
| Product dosage: 2mg | |||
|---|---|---|---|
| Package (num) | Per pill | Price | Buy |
| 30 | $2.96 | $88.71 (0%) | 🛒 Add to cart |
| 60 | $2.54 | $177.43 $152.22 (14%) | 🛒 Add to cart |
| 90 | $2.40
Best per pill | $266.14 $215.73 (19%) | 🛒 Add to cart |
Synonyms | |||
Tizanidine hydrochloride is a short-acting central alpha-2-adrenergic receptor 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 spasms, cramping, and tightness, it helps improve range of motion, facilitate physical therapy, and enhance overall comfort and functional capacity. Its mechanism involves presynaptic inhibition of motor neurons, effectively modulating excitatory input and diminishing hypertonia without directly acting on the neuromuscular junction.
Features
- Active ingredient: Tizanidine hydrochloride
- Available in 2 mg and 4 mg oral tablets, and as a capsule in various strengths
- Short half-life of approximately 2.5 hours
- Peak plasma concentration reached within 1–2 hours post-administration
- Metabolized primarily by cytochrome P450 1A2 (CYP1A2)
- Excreted mainly via the kidneys (approximately 60%) and feces (20%)
Benefits
- Reduces the frequency and intensity of painful muscle spasms
- Improves passive and active range of motion
- Enhances ability to perform activities of daily living and participate in rehabilitation
- May decrease clonus and muscle rigidity
- Can aid in reducing caregiver burden in severe spasticity cases
- Provides relatively rapid onset of action for acute spasm management
Common use
Tizanidine is commonly prescribed for the management of spasticity resulting from multiple sclerosis, spinal cord injury, or other acquired neurological pathologies. It is used both as scheduled therapy for chronic spasticity and as needed for breakthrough spasms. Off-label uses may include tension headaches, certain types of chronic pain, and as an adjunct in musculoskeletal conditions where muscle relaxation is beneficial. It is not indicated for use in pediatric populations.
Dosage and direction
The initial dose is typically 2 mg to 4 mg orally, up to three times daily, with a minimum 6–8 hour interval between doses. Dosage may be titrated gradually in 2–4 mg increments based on tolerability and therapeutic response. The maximum recommended daily dose is 36 mg, though most patients do not exceed 24 mg daily. Administration with food may affect absorption; consistency in relation to meals is advised. Tablets should be swallowed whole with water. Dosing in patients with renal impairment (creatinine clearance < 25 mL/min) requires caution and often a reduced dosage.
Precautions
Use with caution in patients with hepatic impairment, as tizanidine is extensively metabolized in the liver. Orthostatic hypotension may occur; advise patients to rise slowly from sitting or lying positions. Sedation is common; avoid activities requiring mental alertness until response is known. Abrupt discontinuation after prolonged use may lead to rebound hypertension, tachycardia, and hypertonia; taper dose gradually. Not recommended during pregnancy unless potential benefit justifies potential risk. Use in elderly patients may require lower doses due to increased susceptibility to adverse effects.
Contraindications
Concomitant use with potent CYP1A2 inhibitors such as fluvoxamine or ciprofloxacin. Known hypersensitivity to tizanidine or any component of the formulation. Severe hepatic impairment. Use with other alpha-2-adrenergic agonists (e.g., clonidine). Not intended for use in children.
Possible side effect
- Dry mouth (≈49% of patients)
- Somnolence/sedation (≈48%)
- Asthenia (weakness) (≈41%)
- Dizziness (≈16%)
- Hypotension (≈5–10%)
- Elevated liver enzymes (dose-related; ≈5%)
- Hallucinations or confusion (rare; <1%)
- Bradycardia
- Gastrointestinal discomfort
Drug interaction
Potent CYP1A2 inhibitors (fluvoxamine, ciprofloxacin) significantly increase tizanidine plasma levels—contraindicated. Oral contraceptives may moderately increase tizanidine exposure. Alcohol, benzodiazepines, and other CNS depressants may enhance sedative effects. Antihypertensives may potentiate hypotension. Acetaminophen may delay tizanidine absorption. Use with caution with other alpha-2-adrenergic agents.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next dose. Do not double the dose to make up for a missed one. Resume the regular dosing schedule. Consult a healthcare provider if multiple doses are missed or if uncertainty exists regarding dosing.
Overdose
Symptoms may include severe dizziness, somnolence, hypotension, bradycardia, respiratory depression, and coma. Management is supportive and symptomatic; ensure airway patency, administer IV fluids for hypotension, and use vasopressors if needed. Activated charcoal may be considered if ingestion was recent. There is no specific antidote. Dialysis is not expected to be effective due to high protein binding. Contact a poison control center immediately.
Storage
Store at controlled room temperature (20–25°C or 68–77°F). Excursions permitted to 15–30°C (59–86°F). Keep in the original container, tightly closed, and protect from light and moisture. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.
Disclaimer
This information is for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting, changing, or stopping any medication. Individual response to therapy may vary. Do not disregard professional medical advice or delay seeking it based on information provided here.
Reviews
Clinical studies and patient reports generally indicate that tizanidine is effective in reducing muscle spasticity and associated pain. Many users report significant improvement in mobility and comfort, though sedation and dry mouth are frequently noted. Adherence to dosing instructions and close monitoring by a healthcare professional are emphasized for optimal outcomes.