Thiazolidinedione
In medicine, thiazolidinediones are "thiazoles with two keto oxygens. Members are insulin-sensitizing agents which overcome insulin resistance by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma)."[1] Thiazolidinediones are used for the treatment of diabetes mellitus type 2
Examples
Examples in include rosiglitazone and pioglitazone.
Avandia brand of rosiglitazone was approved by the Food and Drug Administration in the United States with a New Drug Application (NDA) in 1999.[2] A generic version was approved with a Abbreviated New Drug Application (ANDA) in 2004.[3]
Actos brand of pioglitazone was approved by the Food and Drug Administration in the United States with a New Drug Application (NDA) in 1999.[4] A generic version was approved with a Abbreviated New Drug Application (ANDA) in 2005.[5]
Effectiveness
The initial choice of anti-diabetic drug has been compared in a randomized controlled trial which found "cumulative incidence of monotherapy failure at 5 years of 15% with rosiglitazone, 21% with metformin, and 34% with glyburide."[6]
Pioglitazone, an insulin sensitizer, may reduce atherosclerosis compared to sulfonylureas which are insulin secretagogues.[7]
Adverse effects
Cardiac
Thiazolidinediones as a class may increase the risk of heart failure according to a meta-analysis of 20,191 patients in 7 trials.[8]
In addition, rosiglitazone[9], but not pioglitazone[10], may increase risk of death from cardiovascular causes according to larger meta-analyses that included unpublished trials.
Rosiglitazone is safer than pioglitazone according to a systematic review published in 2011.[11]
Fractures
Long term use of thiazolidinediones may double the risk of fractures in women.[12]
References
- ↑ Anonymous (2024), Thiazolidinedione (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Kahn SE, Haffner SM, Heise MA, et al (2006). "Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy". N. Engl. J. Med. 355 (23): 2427-43. DOI:10.1056/NEJMoa066224. PMID 17145742. Research Blogging.
- ↑ Nissen, S. E., Nicholls, S. J., Wolski, K., Nesto, R., Kupfer, S., Perez, A., et al. (2008). Comparison of Pioglitazone vs Glimepiride on Progression of Coronary Atherosclerosis in Patients With Type 2 Diabetes: The PERISCOPE Randomized Controlled Trial. JAMA, 299(13), 1561-1573. doi: 10.1001/jama.299.13.1561.
- ↑ Lago RM, Singh PP, Nesto RW (September 2007). "Congestive heart failure and cardiovascular death in patients with prediabetes and type 2 diabetes given thiazolidinediones: a meta-analysis of randomised clinical trials". Lancet 370 (9593): 1129–36. DOI:10.1016/S0140-6736(07)61514-1. PMID 17905165. Research Blogging.
- ↑ Nissen SE, Wolski K (2007). "Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes.". N Engl J Med 356 (24): 2457-71. DOI:10.1056/NEJMoa072761. PMID 17517853. Research Blogging. Review in: ACP J Club. 2007 Nov-Dec;147(3):66 Review in: Evid Based Med. 2007 Dec;12(6):169-70
- ↑ Lincoff AM, Wolski K, Nicholls SJ, Nissen SE (2007). "Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials.". JAMA 298 (10): 1180-8. DOI:10.1001/jama.298.10.1180. PMID 17848652. Research Blogging.
- ↑ Loke, Y. K.; C. S. Kwok, S. Singh (2011). "Comparative cardiovascular effects of thiazolidinediones: systematic review and meta-analysis of observational studies". BMJ 342 (mar17 1): d1309-d1309. DOI:10.1136/bmj.d1309. ISSN 0959-8138. Retrieved on 2011-03-24. Research Blogging.
- ↑ Loke YK, Singh S, Furberg CD (January 2009). "Long-term use of thiazolidinediones and fractures in type 2 diabetes: a meta-analysis". CMAJ 180 (1): 32–9. DOI:10.1503/cmaj.080486. PMID 19073651. PMC 2612065. Research Blogging.