P.B.  Dandge, S.P.  Govindwar, 
    <I>In vivo</I> and <I>In vitro</I> Effect of Sulfamerazine on Hepatic Mixed Function Oxidase in Rats,
    Research Journal of Pharmacology,
    Volume 5,Issue 5,
    2011,
    Pages 53-58,
    ISSN 1815-9362,
    rjpharm.2011.53.58,
    (https://makhillpublications.co/view-article.php?doi=rjpharm.2011.53.58)
    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<SUP>-1</SUP> caused significant decreases in cytochrome P-450 and activities of aminopyrine N-demethylase and aniline hydroxylase. In inhibitory dose of 100 mg SMR kg<SUP>-1</SUP> 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<SUP>-1</SUP> dose level. All other parameters were unchanged. Sulfamerazine resulted in uncompetitive type of inhibition (Ki = 3.0 mM) of aminopyrine N-demethylase <I>in vitro</I>. 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.
    Keywords: Aminopyrine N-demethylase;aniline hydroxylase;cytochrome P-450;mixed function oxidase;sodium;sulfamerazine