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Chỉ định và Liều dùng
Oral
Spasticity Adult: In patient with multiple sclerosis or spinal cord injury or disease: Initially, 2 mg as a single dose, increase according to patient’s requirement and response in increments of 2-4 mg daily at 3-4 days interval. Dose should be taken in 3-4 divided doses. Usual dose: 24 mg daily. Max: 36 mg daily.
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Suy thận
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Suy gan
Contraindicated.
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Chống chỉ định
Concomitant use with potent CYP1A2 inhibitors (e.g. fluvoxamine, ciprofloxacin). Hepatic impairment.
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Thận trọng
Patient with psychiatric disorder, CV disorder, coronary artery disease. Renal impairment. Elderly. Pregnancy and lactation. Avoid abrupt dose reduction and withdrawal.
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Tác dụng không mong muốn
Significant: Hepatotoxicity, hypersensitivity reactions, hypotension, sedation, hallucinations.
Gastrointestinal disorders: Xerostomia. General disorders and administration site conditions: Weakness, fatigue, withdrawal hypertension. Infections and infestations: Infection. Investigations: Increased liver enzymes. Nervous system disorders: Dizziness, drowsiness. Cardiac disorders: Bradycardia, tachycardia. |
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Thông tin tư vấn bệnh nhân
This drug may cause drowsiness, dizziness, and hypotension, if affected, do not drive or operate machinery.
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Chỉ số theo dõi
Monitor LFT at baseline and monthly for the first 4 months of therapy; blood pressure, renal function, and ECG periodically.
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Quá liều
Symptoms: Nausea, vomiting, hypotension, bradycardia, QT prolongation, dizziness, miosis, respiratory distress, coma, restlessness, somnolence. Management: Symptomatic and supportive treatment. Employ gastric lavage or administer high doses of activated charcoal. Maintain adequate hydration.
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Tương tác
Enhanced CNS effects with sedatives and other CNS depressants (e.g. benzodiazepines, opioids, TCA). Increased hypotensive effects, rebound hypertension and tachycardia with β-adrenoceptor blockers, digoxin. Increased plasma concentration with oral contraceptives.
Potentially Fatal: Increased serum concentration with potent CYP1A2 inhibitors (e.g. fluvoxamine, ciprofloxacin). |
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Tương tác với thức ăn
Enhanced CNS effects with alcohol.
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Tác dụng
Description:
Mechanism of Action: Tizanidine is an α2-adrenergic agonist that acts on the spinal and supraspinal levels to block excitatory interneurons. It reduces spasticity by increasing presynaptic inhibition and has great effects in the polysynaptic pathways. It also possesses a moderate central analgesic effect. Onset: 1-2 hours. Duration: 3-6 hours. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Food alters absorption and bioequivalence. Bioavailability: Approx 40% (oral). Time to peak plasma concentration: Approx 1 hour. Distribution: Volume of distribution: 2.4 L/kg. Plasma protein binding: Approx 30%. Metabolism: Undergoes extensive first-pass hepatic metabolism by CYP1A2 to inactive metabolites. Excretion: Mainly via urine (60%); faeces (20%). Elimination half-life: Approx 2.5 hours. |
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Đặc tính
 Source: National Center for Biotechnology Information. PubChem Database. Tizanidine, CID=5487, https://pubchem.ncbi.nlm.nih.gov/compound/Tizanidine (accessed on Jan. 23, 2020) |
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Bảo quản
Store at 25°C.
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Phân loại MIMS
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Phân loại ATC
M03BX02 - tizanidine ; Belongs to the class of other centrally-acting muscle relaxants.
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Tài liệu tham khảo
Anon. Tizanidine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/11/2017. Buckingham R (ed). Tizanidine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/11/2017. Joint Formulary Committee. Tizanidine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/11/2017. McEvoy GK, Snow EK, Miller J et al (eds). Tizanidine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 18/01/2018. Tizanidine Hydrochloride (Par Pharmaceutical, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/11/2017.
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