The evaluation and management of combination drug therapy assumes much importance especially where the drugs are used for prolonged time-period. Management of HIV/AIDS is gradually expanding to include the chronic and metabolic complications and the adverse effects associated with its treatments like Type II diabetes. Repaglinide is a novel oral hypoglycaemic agent chemically unrelated to sulphonylureas, metformin or acarbose used for the treatment of type II diabetes. Nevirapine is widely used NNRTIs for the treatment of HIV infection. The role of nevirapine on the pharmacodynamic and pharmacokinetic activity of repaglinide is not currently known. The objective of this study was to examine the effect of oral administration of nevirapine on blood glucose and investigate their effect on the activity of repaglinide in various animal models to evaluate the safety and effectiveness of the combination.