Journal ArticleDOI
Perazine, chlorpromazine and imipramine as inducers of microsomal drug metabolism.
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The tricyclic drugs investigated are potent inducers of the drug-metabolizing enzyme system, the induction pattern differing in some respects from that seen after phenobarbital.Abstract:
Male rats were treated orally for 7 days with perazine, chlorpromazine, imipramine or phenobarbital. Isolated liver microsomes were tested for their metabolic activities towards perazine, ethylmorphine and aniline. N-Demethylation of perazine and ethylmorphine was increased 2–3.5 fold by all pretreatments. Aromatic hydroxylation of perazine was decreased in microsomes from pretreated animals, whereas aniline hydroxylation was enhanced even more by perazine and imipramine than by phenobarbital. The yield of perazine sulfoxide was increased by phenobarbital treatment only. Perazine N-oxide formation was reduced by treatment with psychoactive drugs to 75–90% of control values and by phenobarbital to less than 50%. The microsomal cytochrome P-450 concentration was slightly elevated by perazine and substantially by chlorpromazine and imipramine treatment. The tricyclic drugs investigated are potent inducers of the drug-metabolizing enzyme system, the induction pattern differing in some respects from that seen after phenobarbital.read more
Citations
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Journal ArticleDOI
Induction of drug metabolizing enzyme system in the liver
TL;DR: Accelerated drug metabolism in liver cells was discovered during studies of the cause of barbiturate tolerance and of the way in which polycyclic hydrocarbons protect against the actions of several carcinogenic compounds as discussed by the authors.
Journal ArticleDOI
Classes of hepatic microsomal mixed function oxidase inducers.
Robert Snyder,Herbert Remmer +1 more
Journal ArticleDOI
Cerebral pharmacokinetics of imipramine in rats after single and multiple dosages
TL;DR: The elimination curves of IMI and DMI from the blood and brain show that both the whole body and the brain behave as multi-compartment systems and desipramine in the brain is present for the whole period between injections at concentrations sufficient to inhibit the noradrenaline uptake.
Book ChapterDOI
Induction of the drug-metabolizing enzymes.
TL;DR: The deactivation of drugs and detoxication of environmental chemicals is brought about by the metabolism of these xenobiotics by enzymes, found primarily in the liver, which decrease the lipid-solubility of these compounds and facilitate their excretion.
References
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Journal ArticleDOI
The Carbon Monoxide-binding Pigment of Liver Microsomes I. EVIDENCE FOR ITS HEMOPROTEIN NATURE
Tsuneo Omura,Ryo Sato +1 more
TL;DR: The present paper gives a detailed account of the investigations on rabbit liver microsomes and crude microsomal digests, which have led to postulate the hemoprotein nature of the pigment.
Journal ArticleDOI
The colorimetric estimation of formaldehyde by means of the Hantzsch reaction
TL;DR: A chronology of key events leading up to and including the birth of Bonnichsen, R. K. & Bonner, J. (1952).
Journal Article
Spectral studies of drug interaction with hepatic microsomal cytochrome.
TL;DR: Two types of spectral changes are described as resulting from substrate interaction with a hepatic microsomal cytochrome; the magnitude of these spectral changes is dependent on protein concentration and substrate concentration as well as the substrate employed.
Journal ArticleDOI
Drug interactions in man. i. lowering effect of phenobarbital on plasma levels of bishydroxycoumarin (dicumarol) and diphenylhydantoin (dilantin)
TL;DR: The ability of a drug to stimulate its own metabolism or the metabolism of another drug appears to have important implications in clinical pharmacologic studies, as weU as to the problem of drug therapy in man.
Journal ArticleDOI
Further studies on the inhibition and stimulation of microsomal drug-metabolizing enzymes of rat liver by various compounds
TL;DR: The results of the present studies are of practical importance in the evaluation of the action of two compounds administered simultaneously or after short time intervals.
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