Tizanidine - Wikipedia, the free encyclopedia

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Tizanidine
From Wikipedia, the free encyclopedia

Tizanidine (trade names Zanaflex, Sirdalud) is a drug that is used as a muscle relaxant. It is a centrally acting 2 adrenergic agonist. 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.[1] Tizanidine has been found to be as effective as other antispasmodic drugs and has superior tolerability to that of baclofen and diazepam.[2] Tizanidine may cause hypotension, so caution is advised when it is used in patients who have a history of orthostatic hypotension. Use caution with this drug as it can be very strong even at the 2 mg dose. Also use caution when switching from gel cap to tablet form and vice versa. Tizanidine can occasionally cause liver damage, generally the hepatocellular type. 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 6 months of treatment.

Tizanidine

Systematic (IUPAC) name

5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)benzo[c][1,2,5] thiadiazol-4-amine

Clinical data Trade names Zanaflex

AHFS/Drugs.com monograph MedlinePlus Pregnancy cat. Legal status Routes a601121 ?

-only (US)
Oral, Intranasal, Injection

Pharmacokinetic data Protein binding 30% Metabolism Half-life CYP 1A2 2.54 hours Identifiers CAS number 51322-75-9 M03BX02 CID 5487 DB00697 5287 6AI06C00GW D08611 CHEMBL1079

Contents
1 Availability 2 Interactions 3 Side effects 4 References

ATC code PubChem DrugBank ChemSpider UNII KEGG

Availability

ChEMBL Synonyms

http://en.wikipedia.org/wiki/Tizanidine

6/2/2013

Tizanidine - Wikipedia, the free encyclopedia

Page 2 of 2

Tizanidine is supplied as 2 and 4 mg tablets for oral administration, and in gel cap form in doses of 2 mg, 4 mg, and 6 mg. The tablets are composed of the active ingredient, tizanidine hydrochloride (2.288 mg equivalent to 2 mg tizanidine base and 4.576 mg equivalent to 4 mg tizanidine base), and the inactive ingredients, silicon dioxide colloidal, stearic acid, microcrystalline cellulose and anhydrous lactose.

4-chloro-N-(4,5-dihydro-1H-imidazol2-yl)-8-thia-7,9-diazabicyclo[4.3.0] nona-2,4,6,9-tetraen-5-amine

Chemical data Formula Mol. mass

SMILES InChI

C9H8ClN5S 253.712 g/mol

Interactions

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Concomitant use of tizanidine and moderate or potent CYP1A2 inhibitors is contraindicated. Concomitant use of tizanidine with fluvoxamine, a potent CYP1A2 inhibitor in man, resulted in a 33fold increase in the tizanidine AUC (plasma drug concentration-time curve).[citation needed] Tizanidine is a potent sedative.[citation needed] It therefore has the potential to interact with other CNS depressants. Alcohol should be avoided, particularly as it can cause stomach upset. It has a Volume of Distribution of 2.6L/Kg (Manufacturers notes).

Side effects
Side effects include dizziness, drowsiness, weakness, nervousness, depression, vomiting, tingling sensation in the arms, legs, hands, and feet, dry mouth, constipation, diarrhea, stomach pain, heartburn, increased muscle spasms, back pain, rash and sweating.[3]

References
1. ^ Zanaflex for Fibromyalgia (http://www.fibromyalgia-reviews.com/Drg_Zanaflex.cfm) 2. ^ Kamen, L.; Henney, HR.; Runyan, JD. (Feb 2008). "A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury.". Curr Med Res Opin 24 (2): 42539. doi:10.1185/030079908X261113 (http://dx.doi.org/10.1185%2F030079908X261113). PMID 18167175 (//www.ncbi.nlm.nih.gov/pubmed/18167175). 3. ^ Tizanidine - PubMed Health (http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000106/)

Retrieved from "http://en.wikipedia.org/w/index.php?title=Tizanidine&oldid=556683345" Categories: Muscle relaxants Alpha-adrenergic agonists Imidazolines Organochlorides Benzothiadiazoles This page was last modified on 25 May 2013 at 04:18. Text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization.

http://en.wikipedia.org/wiki/Tizanidine

6/2/2013