Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Sirdalud, Tizanidin; Belgium: Sirdalud; Bulgaria: Tizanidine; Cyprus: Sirdalud; Czech Republic: Sirdalud; Denmark: Sirdalud, Tizanidin; Estonia: Sirdalud, Tizanidin; Finland: Sirdalud, Tizanidin; Germany: Sirdalud, Tizanidin; Greece: Sirdalud; Hungary: Sirdalud; Ireland: Tizaflex, Tizanidine, Zanaflex; Italy: Sirdalud, Tizanidina; Latvia: Sirdalud, Tizanidine; Lithuania: Sirdalud, Tizanidine; Netherlands: Sirdalud, Tizanidine; Poland: Sirdalud, TizaniTeva; Portugal: Sirdalud, Tizanidina; Romania: Sizolan, Tizanidina; Slovakia: Sirdalud; Slovenia: Sirdalud, Tizanidin; Spain: Sirdalud; UK: Tizanidine, Zanaflex.

North America

Canada: Tizanidine, Zanaflex; USA: Zanaflex.

Latin America

Argentina: Sirdalud; Brazil: Sirdalud; Mexico: Sirdalud.


Japan: Astonelin, Enchinin, Gibonz, Mekitack, Motonalin, Sevretin, Telzanine, Ternelin, Terrelark, Tetorinen, Tirolbit, Tizanelin, Tizanin, Zanpeak.

Drug combinations


Tizanidine Hydrochloride: C~9~H~8~ClN~5~S HCl. Mw: 290.17. (1) 2,1,3-Benzothiadiazol-4-amine, 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-, monohydrochloride; (2) 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole monohydrochloride. CAS-64461-82-1; CAS-51322-75-9 (tizanidine)(1993).

Pharmacologic Category

Centrally Acting Skeletal Muscle Relaxants; α~2~-Adrenergic Agonist. (ATC-Code: M03BX02).

Mechanism of action

An α~2~-adrenergic agonist agent which decreases excitatory input to α motor neurons. An imidazole derivative which acts as centrally acting muscle relaxant with α~2~-adrenergic agonist properties. Acts on level of spinal cord.

Therapeutic use

Skeletal muscle relaxant used for treatment of muscle spasticity.

Pregnancy and lactiation implications

Use with caution in pregnancy. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Tension headaches, low back pain, and trigeminal neuralgia.


Hypersensitivity to tizanidine or any component of the formulation. Concomitant therapy with ciprofloxacin or fluvoxamine (potent CYP1A2 inhibitors).

Warnings and precautions

Potential for hepatotoxicity. AST/ALT elevations and rarely hepatic failure occurred. Dose-related sedation common. Significant and severe sedation may also occur (use with caution in risk for sedative effects). Hypotensive effects may be potentiated when used with antihypertensives. Sedative effects may be potentiated when used with other CNS depressants. Avoid or use extreme caution in hepatic impairment (potential for effects probably due to extensive hepatic metabolism of tizanidine). In general, avoid use in patients taking other CYP1A2 inhibitors. Dose-related significant hypotension may occur (use with caution in patients with cardiac disease or those at risk for severe hypotensive effects). Withdrawal resulting in rebound hypertension, tachycardia, and hypertonia may occur upon discontinuation. Use with caution in renal impairment (clearance decreased significantly in severe impairment (CrCl <25 mL/minute)). Use associated with visual hallucinations or delusions, generally in first 6 weeks of therapy. Use caution in psychiatric disorders. Food alters absorption profile relative to administration under fasting conditions. In addition, bioequivalence between capsules and tablets altered by food. Capsules and tablets bioequivalent under fasting conditions, but not under nonfasting conditions.



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