Effects of 3-trifluoromethyl-alpha-ethylbenzhydrol (RGH-3332), a new enzyme inducer, on the microsomal drug metabolism. Part I.
Intensity and duration of action of several compounds which are metabolized in the liver, are reduced in rats following pretreatment with 3-trifluoromethyl-alpha-ethylbenzhydrol (RGH-3332, Zixoryn), e.g., hexobarbital, methohexitone, glutethimide, hydroxymephenesine, chlorzoxazone, zoxazolamine, ketamine, chlordiazepoxide, diphenylhydantoin, ethylmorphine and pentylenetetrazol, hydroquinone, acenocumarol, respectively. Hypnotic effect of barbital is not altered by RGH-3332. Hexobarbital, meprobamate, mephenesine, nikethamide, canrenone, metyrapone, antipyrine, bromsulphophthalein, inocyanin green, bilirubin disappearance are enhanced, excretion of ascorbic acid is increased after RGH-3332 treatment. The effect of RGH=3332 is inhibited by D,L-ethionine. Hepatic cytochrome P450 concentration is increased following treatment with RGH-3332. Results of in vivo studies proved that 3-trifluoromethyl-alpha-ethylbenzhydrol has enzyme inducing activity.
D000818:Animals; D001205:Ascorbic Acid / Q000652:urine; D001559:Benzhydryl Compounds / Q000494:pharmacology*; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004790:Enzyme Induction / Q000187:drug effects*; D005036:Ethylmorphine / Q000378:metabolism; D005260:Female; D006873:Hydroquinones / Q000378:metabolism; D006993:Hypnotics and Sedatives / Q000378:metabolism; D008862:Microsomes, Liver / Q000187:drug effects*; D009125:Muscle Relaxants, Central / Q000378:metabolism; D010433:Pentylenetetrazole / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010672:Phenytoin / Q000378:metabolism; D051381:Rats
D001559:Benzhydryl Compounds; D006873:Hydroquinones; D006993:Hypnotics and Sedatives; D009125:Muscle Relaxants, Central; D004364:Pharmaceutical Preparations; D010672:Phenytoin; D003577:Cytochrome P-450 Enzyme System; D001205:Ascorbic Acid; D005036:Ethylmorphine; D010433:Pentylenetetrazole