Abstract

A REVIEW ON CLINICAL PHARMACOKINETIC AND PHARMACODYNAMIC PROFILE OF METFORMIN

A. Bharath Kumar*, S. Mohan, R. Siva Sakthi and S. Ramkanth

Abstract

Metformin is classified as a biguanide oral hypoglycemic agent used in first line treatment of type 2 diabetes mellitus. Metformin hydrochloride is a white crystalline compound having molecular formula of C4H11N5.HCl and a molecular weight of 165.63. It is freely soluble in water and is practically insoluble organic compounds like acetone, ether, and chloroform. Metformin has an oral bioavailability of 50-60% and exhibits slow absorption, bound to plasma proteins, approximately 90% of the absorbed drug is eliminated through renal route and half life is 6.2 hours. Metformin diminishes hepatic glucose production, and decrease intestinal absorption of glucose, and improve insulin sensitivity. It is available in the market under various trade names such as Glucophage, glumetza, formet, glucophage XR, obimet, gluformin, formin. Metformin can be prescribed with other anti diabetic drug medications such as glipizide, glimepiride, rosiglitazone, pioglitazone, to improve patient compliance and achieve the glycemic control. Metformin used to treat type 2 diabetes mellitus, prediabetes, polycystic ovarian syndrome, female infertility, gestational diabetes. Metformin drug interacts with furosemide, nifedipine, cationic drugs and less interact with highly plasma protein bound drugs. The most common adverse effect of Metformin includes diarrhea, cramps, nausea, vomiting, and increased flatulence, lactic acidosis, vitamin B12 deficiency. It is contraindicated in people with risk of lactic acidosis, kidney disorders and liver disease. It is prescribed with other oral hypoglycemic drugs thereby improve patient compliance and maintaining the controlled levels of blood glucose levels to prevent the development of diabetic complications.

Keywords: Metformin hydrochloride, bioavailability, insulin sensitivity, type 2 diabetes mellitus, lactic acidosis.