Thiazolidinedione

Jump to: navigation, search

WikiDoc Resources for Thiazolidinedione

Articles

Most recent articles on Thiazolidinedione

Most cited articles on Thiazolidinedione

Review articles on Thiazolidinedione

Articles on Thiazolidinedione in N Eng J Med, Lancet, BMJ

Media

Powerpoint slides on Thiazolidinedione

Images of Thiazolidinedione

Photos of Thiazolidinedione

Podcasts & MP3s on Thiazolidinedione

Videos on Thiazolidinedione

Evidence Based Medicine

Cochrane Collaboration on Thiazolidinedione

Bandolier on Thiazolidinedione

TRIP on Thiazolidinedione

Clinical Trials

Ongoing Trials on Thiazolidinedione at Clinical Trials.gov

Trial results on Thiazolidinedione

Clinical Trials on Thiazolidinedione at Google

Guidelines / Policies / Govt

US National Guidelines Clearinghouse on Thiazolidinedione

NICE Guidance on Thiazolidinedione

NHS PRODIGY Guidance

FDA on Thiazolidinedione

CDC on Thiazolidinedione

Books

Books on Thiazolidinedione

News

Thiazolidinedione in the news

Be alerted to news on Thiazolidinedione

News trends on Thiazolidinedione

Commentary

Blogs on Thiazolidinedione

Definitions

Definitions of Thiazolidinedione

Patient Resources / Community

Patient resources on Thiazolidinedione

Discussion groups on Thiazolidinedione

Patient Handouts on Thiazolidinedione

Directions to Hospitals Treating Thiazolidinedione

Risk calculators and risk factors for Thiazolidinedione

Healthcare Provider Resources

Symptoms of Thiazolidinedione

Causes & Risk Factors for Thiazolidinedione

Diagnostic studies for Thiazolidinedione

Treatment of Thiazolidinedione

Continuing Medical Education (CME)

CME Programs on Thiazolidinedione

International

Thiazolidinedione en Espanol

Thiazolidinedione en Francais

Business

Thiazolidinedione in the Marketplace

Patents on Thiazolidinedione

Experimental / Informatics

List of terms related to Thiazolidinedione

Overview

The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type 2) and related diseases.

Mode of action

Thiazolidinediones or TZDs act by binding to PPARs (peroxisome proliferator-activated receptors), a group of receptor molecules inside the cell nucleus, specifically PPARγ (gamma). The normal ligands for these receptors are free fatty acids (FFAs) and eicosanoids. When activated, the receptor migrates to the DNA, activating transcription of a number of specific genes.

Genes upregulated by PPARγ can be found in the main article on peroxisome proliferator-activated receptors.

By activating PPARγ:

Members of the class

The chemical structure of thiazolidinedione

Chemically, the members of this class are derivatives of the parent compound thiazolidinedione, and include:

Experimental agents include MCC-555, a powerful antidiabetic agent and the early non-marketed thiazolidinedione ciglitazone.

Uses

The only approved use of the thiazolidinediones is in diabetes mellitus type 2.

It is being investigated experimentally in polycystic ovary syndrome (PCOS), non-alcoholic steatohepatitis (NASH),[2] psoriasis,[3] and other conditions.[4]

Several forms of lipodystrophy cause insulin resistance, which has responded favorably to thiazolidinediones. There are some indications that thiazolidinediones provide some degree of the protection against initial stages of the breast carcinoma development.

Side effects and contraindications

The withdrawal of troglitazone has led to concerns of other thiazolidinediones increasing the risk of hepatitis. Guidelines now mention that for the first year of thiazolidinedione therapy, a two- or three-monthly check of liver enzymes is conducted to ascertain that no liver damage is occurring.

The main side effect of all thiazolidinediones is fluid retention, leading to edema, weight gain, and potentially aggravating heart failure. Therefore, thiazolidinediones should not be prescribed in patients with decreased ventricular function (NYHA grade III or IV heart failure).

Recent studies have shown there may be an increase risk of CHD with Rosiglitazone.[5] However, the PROactive study has shown that pioglitazone dose not have this same risk.

Footnotes

  1. Panigrahy D, Singer S, Shen LQ; et al. (2002). "PPARgamma ligands inhibit primary tumor growth and metastasis by inhibiting angiogenesis". J. Clin. Invest. 110 (7): 923–32. PMID 12370270.
  2. Belfort R et. al. A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis. N Engl J Med 2006; 355(22): 2297-307. PMID 17135584 Clinical trial info
  3. Krentz AJ, Friedmann PS. Type 2 diabetes, psoriasis and thiazolidinediones. Int J Clin Pract 2006;60:362-3. PMID 16494655.
  4. Clinical Trials for Rosiglitazone - from ClinicalTrials.gov, a service of the U.S. National Institutes of Health
  5. "Avandia to Carry Stronger Heart Failure Warning - Forbes.com". Retrieved 2007-08-15.

de:Insulin-Sensitizer



Linked-in.jpg