Authors : P.B. Dandge and S.P. Govindwar
Abstract: Sulfamerazine (SMR) administration (i.p., 3 days) of different doses to adult male rats showed significant decrease in electron transport components and drug metabolizing enzymes. In longer duration study, 100 mg SMR kg-1 caused significant decreases in cytochrome P-450 and activities of aminopyrine N-demethylase and aniline hydroxylase. In inhibitory dose of 100 mg SMR kg-1 was selected for dosing young male, old male and adult female rats. Sulfamerazine administration to young, old male and female rats resulted in a significant decrease in electron transport component and drug metabolizing activities at 100 mg SMR kg-1 dose level. All other parameters were unchanged. Sulfamerazine resulted in uncompetitive type of inhibition (Ki = 3.0 mM) of aminopyrine N-demethylase in vitro. Sulfamerazine destructed the spectral and catalytic activity of cytochrome P-450. The studies suggest that SMR is a substrate of the mixed function oxidase system and inhibition is dependent on dosage, age and sex of the animals.
P.B. Dandge and S.P. Govindwar, 2011. In vivo and In vitro Effect of Sulfamerazine on Hepatic Mixed Function Oxidase in Rats. Research Journal of Pharmacology, 5: 53-58.