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Tizanidine (trade names Zanaflex ( Acorda Therapeutics ), Sirdalud ( Novartis ), Relentus ( Beximco Pharma ) Is a centrally acting α 2 adrenergic agonist used as a muscle relaxant. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, ALS, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label for migraine headaches, as a sleep aid, and as an anticonvulsant. It is also prescribed for some symptoms of fibromyalgia.
Tizanidine has been found to be 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, so caution is advised when it is used in patients who have a history of orthostatic hypotension, or when switching from gel cap to tablet form and vice versa.
Tizanidine can occasionally cause acute liver failure. Clinical trials show that up to 5% of patients treated with tizanidine had elevated liver function test values, though symptoms disappeared upon withdrawal of the drug. Care should be used when first beginning treatment with tizanidine with regular liver tests for the first six months of treatment. As of 2015 the cost for a typical month of medication in the United States is US$100–200.
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Concomitant use of tizanidine and moderate or potent CYP1A2 inhibitors (such as zileuton, certain antiarrhythmics ( amiodarone, mexiletine, propafenone, verapamil ), cimetidine, famotidine, aciclovir, ticlopidine and oral contraceptives ) is contraindicated. Concomitant use of tizanidine with fluvoxamine, a potent CYP1A2 inhibitor in humans, resulted in a 33-fold increase in the tizanidine AUC (plasma drug concentration-time curve). :
antibiotics such as enoxacin, gatifloxacin, levofloxacin, lomefloxacin, moxifloxacin, ofloxacin, sparfloxacin, trovafloxacin, or norfloxacin ;
blood pressure medications such as clonidine, guanabenz, guanfacine (Tenex), or methyldopa ;
heart rhythm medications such as amiodarone (Cordarone, Pacerone), mexiletine (Mexitil), propafenone (Rhythmol), and verapamil (Calan, Covera, Isoptin).
It has a volume of distribution of 2.4 L/kg following intravenous administration.
Side effects include dizziness, drowsiness, weakness, nervousness, hallucinations, depression, vomiting, dry mouth, constipation, diarrhea, stomach pain, heartburn, increased muscle spasms, back pain, rash, sweating, and a tingling sensation in the arms, legs, hands, and feet.
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