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Tizanidine

Muscle Relaxant

Muscle RelaxantATC M03BX10
CDSCO approvedSchedule HATC M03BX10
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AcebutololSevereDatabaseDDInter
  • AcyclovirSevereDatabaseDDInter
  • AldesleukinSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter

Mechanism

Tizanidine is a centrally acting alpha-2 adrenergic agonist structurally related to clonidine that reduces spasticity by enhancing presynaptic inhibition of spinal motor neurons. It acts primarily in the spinal cord, increasing inhibitory neurotransmission at alpha-2 receptors on spinal interneurons, which reduces the release of excitatory amino acids (aspartate, glutamate) and suppresses polysynaptic reflexes. Unlike dantrolene (which acts peripherally on muscle), tizanidine's central mechanism does not cause generalized muscle weakness.

Indications

Muscle cramps (off-label)Muscle stiffness (off-label)Spasticity (off-label)Increased muscle tone (off-label)Spasticity in multiple sclerosis (off-label)Spasticity due to multiple sclerosisSpasticity due to spinal cord injuryspasticity associated with cerebral and spinal disordersSpasticity in multiple sclerosisSpasticity after strokeMay be effective in patients with ALSspasticity due to neurological disorderspainful muscle spasms of spinal origin

Dosing

Adult
16 Guidance on intravenous infusions

Pharmacokinetics

Half-life
Short
Metabolism
undergoes first pass metabolism
Excretion
excreted by the kidney

Contraindications

  • patients receiving antihypertensives, especially clonidine

Side effects

Common
XerostomiaDizzinessSedationDry mouthdrowsinessastheniadry-mouthnight-time insomniahallucinationsdose-dependent elevation of liver enzymes
Serious
  • Rebound spasms
  • Tachycardia
  • Hypertension (if withdrawn rapidly)

Drug interactions

Acebutolol
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Acyclovir
Severe
Database

Drug interaction classified as: metabolism.

Source: DDInter

Aldesleukin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Aliskiren
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Ambrisentan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiloride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amrinone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amyl Nitrite
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Muscle Relaxant drugs

Ask House about Tizanidine

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-10 · House clinical team