Guidelines Basic Science
Copyright ©2011 Baishideng Publishing Group Co., Limited. All rights reserved.
World J Cardiol. May 26, 2011; 3(5): 144-152
Published online May 26, 2011. doi: 10.4330/wjc.v3.i5.144
PPARγ activator, rosiglitazone: Is it beneficial or harmful to the cardiovascular system?
Siripong Palee, Siriporn Chattipakorn, Arintaya Phrommintikul, Nipon Chattipakorn
Siripong Palee, Nipon Chattipakorn, Cardiac Electrophysiology Unit, Department of Physiology, Faculty of Medicine, Chiang Mai University, Chiang Mai, 50200, Thailand
Siripong Palee, Siriporn Chattipakorn, Arintaya Phrommintikul, Nipon Chattipakorn, Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai, 50200, Thailand
Siriporn Chattipakorn, Faculty of Dentistry, Chiang Mai University, Chiang Mai, 50200, Thailand
Arintaya Phrommintikul, Department of Medicine, Faculty of Medicine, Chiang Mai University, Chiang Mai, 50200, Thailand
Author contributions: All authors contributed equally to this review.
Supported by Grants from the Thailand Research Fund RTA 5280006 (NC), BRG (SC), MRG5280169 (AP) and the Commission of Higher Education Thailand (SP, NC)
Correspondence to: Nipon Chattipakorn, MD, PhD, Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai, 50200, Thailand. nchattip@gmail.com
Telephone: +66-53-945329 Fax: +66-53-945368
Received: March 17, 2011
Revised: April 4, 2011
Accepted: April 11, 2011
Published online: May 26, 2011
Abstract

Rosiglitazone is a synthetic agonist of peroxisome proliferator-activated receptor γ which is used to improve insulin resistance in patients with type II diabetes. Rosiglitazone exerts its glucose-lowering effects by improving insulin sensitivity. Data from various studies in the past decade suggest that the therapeutic effects of rosiglitazone reach far beyond its use as an insulin sensitizer since it also has other benefits on the cardiovascular system such as improvement of contractile dysfunction, inhibition of the inflammatory response by reducing neutrophil and macrophage accumulation, and the protection of myocardial injury during ischemic/reperfusion in different animal models. Previous clinical studies in type II diabetes patients demonstrated that rosiglitazone played an important role in protecting against arteriosclerosis by normalizing the metabolic disorders and reducing chronic inflammation of the vascular system. Despite these benefits, inconsistent findings have been reported, and growing evidence has demonstrated adverse effects of rosiglitazone on the cardiovascular system, including increased risk of acute myocardial infarction, heart failure and chronic heart failure. As a result, rosiglitazone has been recently withdrawn from EU countries. Nevertheless, the effect of rosiglitazone on ischemic heart disease has not yet been firmly established. Future prospective clinical trials designed for the specific purpose of establishing the cardiovascular benefit or risk of rosiglitazone would be the best way to resolve the uncertainties regarding the safety of rosiglitazone in patients with heart disease.

Keywords: Rosiglitazone, Ischemic reperfusion injury, Heart disease, Type II diabetic, Thiazolidinediones