Drug information of Tizanidine

Tizanidine

Drug group:

Tizanidine is a short-acting muscle relaxer. It works by blocking nerve impulses (pain sensations) that are sent to your brain. Tizanidine is used to treat spasticity by temporarily relaxing muscle tone.

Mechanism of effect

nidine reduces spasticity by increasing presynaptic inhibition of motor neurons through agonist action at a2-adrenergic receptor sites.

Pharmacokinetics

Absorption : Not Available

Volume of distribution : 2.4 L/kg

Protein binding : 30%

Metabolism : Liver

Route of elimination : Approximately 95% of an administered dose is metabolized.

Half life:  2.5 hours

Dosage

Usual Adult Dose:

Muscle Spasm: Initial dose: 2 mg orally every 6 to 8 hours as needed
-Peak effects occur in approximately 1 to 2 hours and last for 3 to 6 hours; treatment can be repeated as needed to a maximum of 3 doses in 24 hours; gradually increase dose by 2 to 4 mg at intervals of 1 to 4 days until satisfactory reduction of muscle tone is achieved.
Maximum single dose: 16 mg
Maximum daily dose: 36 mg in 24 hours

Renal Dose Adjustments: Severe renal impairment (CrCl less than 25 mL/min): Individualize therapy with lower doses during dose titration; if higher doses are required, individual doses should be increased rather increasing the dosing frequency; closely monitor for toxicity. 

Dose Adjustments:

Use with caution in elderly patients, especially those with renal impairment.
Drug withdrawal:
-Decrease by 2 to 4 mg per day, especially in patients who have been receiving doses of 20 to 36 mg per day for periods of 9 weeks or more.

Safety and efficacy have not been established in patients younger than 18 years.
Consult WARNINGS section for additional precautions.

Alerts

you should know that tizanidine may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking tizanidine .

 To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up. tizanidine can decrease muscle tone, so be careful when walking or doing other activities where you rely on your muscle tone to help with your posture or balance.

- remember that alcohol can add to the drowsiness caused by this medication.

- you should know that this medication may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you. (dose related)

-Caution in renal/hepatic impairment

Hepatotoxicity may occur; monitor aminotransferases prior to and during use

- may potentiate effect of sedative drugs or ethanol

- Visual hallucinations may occur

- CYP1A2 inducers may decrease levels

- Rebound hypertension, tachycardia, and hypertonia reported upon abrupt discontinuation.

Points of recommendation

decrease doses slowly in patients taking concomitant narcotics or high doses (20-28 mg/day) for prolonged periods 

tell your doctor if you have or have ever had kidney or liver disease.

tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking tizanidine , call your doctor.

if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking tizanidine

tell your doctor and pharmacist if you are allergic to tizanidine or any other medications.

tell your doctor if you are taking ciprofloxacin (Cipro) or fluvoxamine. Your doctor will probably tell you not to take tizanidine if you are taking either of these medications

Pregnancy level

C


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