IJPCBS 2014, 4(1), 53-63 Divya et al. ISSN: 2249-9504 53 I NTERNATI ONAL JOURNAL OF PHARMACEUTI CAL, CHEMI CAL AND BI OLOGI CAL SCI ENCES Available online at www.ijpcbs.com ADDITI ONAL PHARMACOLOGI CAL ACTI VI TI ES OF PI OGLI TAZONE: A RETROSPECTIVE REVI EW S. Divya 1 * , S. Sudha Rani 2 , S. Kavimani 1 and R. Murali 1 1 Department of Pharmacology, Mother Theresa Post graduate and Research Institute of Health Sciences, Puducherry-605 006, Tamil Nadu, India. 2 Department of Biochemistry and Molecular Biology, Pondicherry University, Puducherry-605 014, Tamil Nadu, India. I NTRODUCTI ON Glitazones ar e a new er class of antihyperglycemic agent s which include rosiglitazone and pioglitazone that are currently in use in the treatment of Type II Diabetes. Pioglitazone has been shown to act as potent and selective agonist for the nuclear receptor Peroxisome Proliferator Activated Receptor- gamma (PPAR-γ) and activation of PPAR-γ promotes transcription of insulin responsive genes and thereby regulate glucose and lipid metabolism. Pioglitazone action leads to improvement in insulin sensitivity in target tissues through increased membrane expression of GLUT-4 glucose transporters in skeletal muscle and adipose tissue, and by decreased hepatic glucose output through inhibition of gluconeogenesis. Pioglitazone also enhance HDL cholesterol and lower triglyceride levels (Sharma HL and Sharma KK). Pioglitazone, apart from its well-known antihyperglycaemic and hypolipidemic effects, has been reported to exert its positive effects in several debilitating diseases and hold promise in the treatment of many such di seases. In this r evi ew , we summarize the additional pharmacological activities of Pioglitazone more than its effects on lipid and carbohydrate metabolism. PI OGLITAZONE-DRUG HISTORY Troglitazone the first glitazone was launched in USA by march 1997 but was withdrawn on grounds of liver toxicity in march 2000 (Rishi Shukla and Sanjay Karla, 2011). Rosiglitazone and Pioglitazone reached the US market in 1999 as first line agents to be used alone or in combination with metformin or sulfonyureas in the treatment of for diabetes mellitus (Gale, 2001). PI OGLITAZONE-CURRENT STATUS Pioglitazone in addition to its glucose lowering effect also benefits cardiovascular parameters such as lipids, blood pressure, endothelial function, inflammatory biomarkers and fibrinolytic status. Other activities like anti- parkinsonism (Quinn et al., 2008), anti-bacterial (Masadeh et al., 2011), hypolipidemic also have been studied (Francis et al., 2003; de Souza et al., 2001; Bhosale et al., 2012). Additionally Review Article ABSTRACT Glitazones are the antihyperglycemic agents used in the treatment of Type-II diabetes mellitus (T2DM) as monotherapy or in combination with metformin, insulin and sulfonylureas. The drugs - Rosiglitazone and Pioglitazone under this class exert their pharmacological action by directly stimulating the nuclear Peroxisome Proliferator Activated Receptor (PPAR-γ) and thereby regulating peripheral insulin resistance. Pioglitazone, the PPAR- γ agonist apart from exerting its hypolipidemic effects and anti-hyperglycaemic effect also has positive pleiotropic effects such as anti-Parkinson’s, anti-bacterial, anti-hypertensive, antiinflammatory actions etc. Renal and hepatic cyst growth inhibition, learning and memory enhancement, blockade of L-type calcium channels in vascular smooth muscles are other effects influenced by pioglitazones. The present review throws light on the additional pharmacological effects of pioglitazone other than its positive effect on glucose metabolism. Keywords: Pioglitazone, Thiazolidinediones(TZDs), Troglitazone, Type-II Diabetes mellitus.