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Troglitazone



Troglitazone
Systematic (IUPAC) name
5-(4-((6-hydroxy-2,5,7,8-
tetramethylchroman-2-yl-methoxy)
benzyl)-2,4-thiazolidinedione)
Identifiers
CAS number 97322-87-7
ATC code A10BG01
PubChem 5591
DrugBank APRD00488
Chemical data
Formula C24H27NO5S 
Mol. mass 441.541 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 16-34 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Troglitazone (Rezulin, Resulin or Romozin) is an anti-diabetic and antiinflammatory drug, and a member of the drug class of the thiazolidinediones. It was introduced in the late 1990s but turned out to be associated with an idiosyncratic reaction leading to drug-induced hepatitis. It was withdrawn from the USA market on 21 March 2000, and from other markets soon afterwards.

Additional recommended knowledge

Mode of action

Troglitazone, like the other thiazolidinediones (pioglitazone and rosiglitazone), works by activating PPARs (peroxisome proliferator-activated receptors). Troglitazone is a ligand to both PPARα and - more strongly - PPARγ. Troglitazone also contains an α-tocopheroyl moiety, potentially giving it vitamin E-like activity in addition to its PPAR activation. It has been shown (Aljada et al) to reduce inflammation: troglitazone use was associated with a decrease of nuclear factor kappa-B (NFκB) and a concomitant increase in its inhibitor (IκB). NFκB is an important cellular transcription regulator for the immune response.

References

  • Aljada A, Garg R, Ghanim H, et al (2001). "Nuclear factor-kappaB suppressive and inhibitor-kappaB stimulatory effects of troglitazone in obese patients with type 2 diabetes: evidence of an antiinflammatory action?". J. Clin. Endocrinol. Metab. 86 (7): 3250–6. doi:10.1210/jc.86.7.3250. PMID 11443197.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Troglitazone". A list of authors is available in Wikipedia.
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