The leaves of Bacopa monnieri are very effective in a wide range of health problems. The present study was performed to investigate the effect of Bacopa extract and acephate on Acetylcholinesterase activity, its kinetics and histological parameters in the kidney of male albino Wistar rats. Rats were divided into four groups of five animals each. Group, I served as control and given orally groundnut oil. Group II, III and IV have given acephate and leaf extract of Bacopa monnieri each alone and in their combinations respectively. Acetylcholinesterase (AChE) activity was measured by Ellman’s method and AChE kinetics was analyzed by Line Weaver Burk plots. The Kidney showed significant differences (P < 0.05) of 65-71% AChE inhibition in the test groups intoxicated with Bacopa monnieri and acephate when compared with the control. The kinetic study reveals the competitive nature of AChE inhibition of both Bacopa monnieri and acephate. On the other hand, acephate showed histopathological alterations in kidney like necrosis in renal tubules and space in Bowman’s capsule layer. However, Bacopa monnieri causes mild changes in the kidney structure.