TY - JOUR
T1 - In vivo and In vitro Effect of Sulfamerazine on Hepatic Mixed Function Oxidase in Rats
AU - Dandge, P.B. AU - Govindwar, S.P.
JO - Research Journal of Pharmacology
VL - 5
IS - 5
SP - 53
EP - 58
PY - 2011
DA - 2001/08/19
SN - 1815-9362
DO - rjpharm.2011.53.58
UR - https://makhillpublications.co/view-article.php?doi=rjpharm.2011.53.58
KW - Aminopyrine N-demethylase
KW -aniline hydroxylase
KW -cytochrome P-450
KW -mixed function oxidase
KW -sodium
KW -sulfamerazine
AB - 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.
ER -