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troglitazone

 
Dictionary: tro·gli·ta·zone   (trō'glĭ-tə-zōn') pronunciation

n.
An oral antidiabetic agent that lowers blood glucose by improving the response of target cells to insulin without increasing insulin secretion.

[tro-, of unknown meaning + gli- (ultimately shortening and alteration of HYPOGLYCEMIA) + t(hi)az(olidinedi)one, one of its constituents.]


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Drug Info: Troglitazone
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Chemical formula:



Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Veterinary Dictionary: troglitazone
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A thiazolidinedione compound that enhances peripheral insulin resistance in the management of diabetes mellitus.

Wikipedia: Troglitazone
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Troglitazone
Systematic (IUPAC) name
5-(4-[(6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)methoxy]benzyl)thiazolidine-2,4-dione
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 developed by Daiichi Sankyo Co.(Japan). It was introduced and manufactured by Parke-Davis in the late 1990s but turned out to be associated with an idiosyncratic reaction leading to drug-induced hepatitis. Evaluating FDA medical officer Dr. John Gueriguian had disapproved it due to high liver toxicity. But the FDA stripped Gueriguian of his post and discarded his report under successful corporate pressure to approve the drug. [1]
It was withdrawn from the United Kingdom market (sailing by Glaxo) on December 1997.after,from the USA market on 21 March 2000, and from the Japan markets(introduced and manufactured by Sankyo.Co.) soon afterwards.

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. 

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Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Troglitazone" Read more