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Our study was carried out to investigate the insecticide, imidacloprid toxicokinetics and its biochemical alterations in Male Albino rat post-treatment with a single oral dose (20 mg/kg b.w). Imidacloprid residue in samples were quantified using HPLC and compound kinetics as distribution and elimination were subjected to a non- compartmental model in blood and other tissues. Results revealed that the trend of maximal imidacloprid concentration 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.Dose regime, time sampling and predicting accurate area under the curve from zero time to 24 hours (AUC24h) were calculated and validated using toxicokinetic (TK) modeler Version 1.0; the results reflected the importance and utilizing possibility of TK modeler in toxicokinetics field. Alteration in biochemical parameters associated with imidacloprid kinetics showed significant gradual increase in liver and kidney functions parameters coincided with imidacloprid accumulation with varying quantities according to each organ then gradually decreased to the end of study.