The purpose of this study was to investigate the time course of changes in enzymes activity during distribution of imidaclopride (IMI) in Male Albino rat (Rattus norvegicus)  after 1, 3, 6, 12, 24 and 48 hr., treatment with a single oral dose (20 mg/kg body weight). The results showed significant gradual increase in liver and kidney function parameters coincided with accumulation of imidacloprid with varying quantities according to each organ, then gradually decreased to the end of study. The highest activity in liver enzymes, ALT (97.33 U/L), AST (78 U/L) ALP (169.66 IU/L) and LDH (5190.67 U/L) was recorded six hours post treatment, as well as increasing in total protein (8.94 g/dl). Kidney function parameters, i.e. urea, creatinine and uric acid levels (75.67, 2.283, 19.15 mg/dl, respectively) were also revealed the highest increase comparing with control. Liver and brain acetylcholinesterase (AChE) activity was reached the lowest level with the inhibition percent 82.9, 81.4%, respectively at the same time agreed with the concentration peak of IMI in blood (8.04 µg/ml) liver (2.42 µg/g) and brain (4.06 µg/g).The trend of maximal concentration of IMI in different organs and body fluids at six hours post dosing was in the following order: urine > blood > lungs > brain > testes > spleen > kidney > liver > muscles.