Trade name Zanaflex.
A centrally acting α2 adrenergic agonist used as a muscle relaxant.
It is used to treat the spasms, cramping, and tightness of muscles due to varying conditions including: multiple sclerosis, ALS, spastic diplegia, back pain, and injuries to the spine or central nervous system.
Additional uses include: migraine, sleep aid, anticonvulsant and for fibromyalgia.
Pregnancy category C.
Oral administration by tablets or capsules.
Bioavailability is about 40%.
Protein binding about 30%.
Metabolism-Liver (CYP1A2, 95%)
Elimination half-life 2.54 hours.
Excretion Urine (60%), feces (20%).
As effective as other antispasmodic drugs and is more tolerable than baclofen and diazepam.
Tizanidine can be very strong even at the 2 mg dose and
May cause hypotension.
Can occasionally cause acute liver failure.