Tizanidine

Muscle Relaxant · Alpha-adrenergic agonist (skeletal muscle relaxant)

Indications

Painful muscle spasm. Spasticity due to neurological disorders.

Dosage

Adults: Painful muscle spasm: 2 to 4 tab daily in divided doses. Spasticity due to neurological disorders: Max initial dose 6 mg/day in 3 divided doses, the increase stepwise to 12-36 mg/day. Children: Not recommended.

Adverse Effects

Fatigue, dizziness, dry mouth, nausea, reduction in blood pressure, muscle weakness, insomnia, bradycardia, somnolence, GI upset, hypotension, tachycardia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Caution advised or effect undetermined. Contraindications: Severe hepatic impairment. Precautions: Impaired liver or kidney function. Perform LFTs monthly for 1st four months; discontinue if enzymes persistently >3 × ULN. Cardiovascular disorders, coronary artery disease. Elderly.

Interactions

Antihypertensives, diuretics, alcohol, sedatives, fluvoxamine, ciprofloxacin, other CYP1A2 inhibitors, digoxin, drugs that prolong QT interval, oral contraceptives, CNS depressants.

Advice to Patient

Take on an empty stomach. If you miss a dose, take it within an hour of the scheduled time otherwise skip the dose and wait for the next dose. Do not take double dose. Contact prescriber if there is constant dizziness, skin rash, difficulty in breathing, chest pain, palpitations, confusion, delusions, muscle weakness, tremors, dry mouth that lasts longer than 2 weeks. Avoid alcohol during therapy.

Pharmacokinetics

Onset: Single dose (8mg): Peak effect: 1-2 hours. Duration: Single dose (8mg): 3-6 hours. Absorption: Tablets and capsules are bioequivalent under fasting conditions, but not under non-fasting conditions. Tablets administered with food: Peak plasma concentration is increased by approx. 30%; time to peak increased by 25 minutes; extent of absorption increased by approx. 30%. Capsules administered with food: Peak plasma concentration decreased by 20%; time to peak increase by 2-3 hours; extent of absorption increased by approx.10%. Capsules opened and sprinkled on applesauce are not bioequivalent to administration of intact capsules under fasting conditions. Peak plasma concentration and AUC are increased by 15% to 20%; time to peak decreased by 15 minutes. Metabolism: Extensively hepatic. Bioavailability: Approx. 40% (extensive first-pass metabolism). Half-life elimination: Approx. 2.5…

Brands with this active ingredient

Compiled by Healify Pharmacy from published drug references. How we compile it →

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