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Inhibition and Induction of Cytochrome P450 and the Clinical Implications

Data up to Jan 2025

Published1998
Citations821
References179

Total Citations Per Year

Abstract

References (179)

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Omeprazole is an aryl hydrocarbon-like inducer of human hepatic cytochrome P450

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Induction of Rat Hepatic N-Nitrosodimethylamine Demethylase by Acetone Is Due to Protein Stabilization

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Metabolism of the immunosuppressant tacrolimus in the small intestine: cytochrome P450, drug interactions, and interindividual variability.

1995 • 270 citations

Inhibition of Cytochrome P450 Enzymes

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Oxidation of 17 alpha-ethynylestradiol by human liver cytochrome P-450.

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Oxidation of the antihistaminic drug terfenadine in human liver microsomes. Role of cytochrome P-450 3A(4) in N-dealkylation and C-hydroxylation.

1993 • 225 citations

Metoprolol and mephenytoin oxidation polymorphisms in Far Eastern Oriental subjects: Japanese versus mainland Chinese

1989 • 221 citations

Immunochemical evidence for induction of the alcohol-oxidizing cytochrome P-450 of rabbit liver microsomes by diverse agents: ethanol, imidazole, trichloroethylene, acetone, pyrazole, and isoniazid.

1985 • 215 citations

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Pharmacokinetic Interactions of Cimetidine 1987

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1975 • 183 citations

Macrolide antibiotics inhibit the degradation of the glucocorticoid-responsive cytochrome P-450p in rat hepatocytes in vivo and in primary monolayer culture.

1986 • 177 citations

Structure-activity relationships in the effects of 1-alkylimidazoles on microsomal oxidation in vitro and in vivo

1974 • 169 citations

Thiophene derivatives as new mechanism-based inhibitors of cytochromes P-450: Inactivation of yeast-expressed human liver cytochrome P-450 2C9 by tienilic acid

1994 • 168 citations

An Overview of Current Cytochrome P450 Technology for Assessing the Safety and Efficacy of New Materials

1996 • 167 citations

Ketoconazole to Reduce the Need for Cyclosporine after Cardiac Transplantation

1995 • 164 citations

Effect of omeprazole treatment on diazepam plasma levels in slow versus normal rapid metabolizers of omeprazole

1990 • 163 citations

The activation of the biguanide antimalarial proguanil co‐segregates with the mephenytoin oxidation polymorphism‐a panel study.

1991 • 162 citations

Pharmacokinetic Interactions Between Antiepileptic Drugs

1996 • 160 citations

Catalytic selectivity of human cytochrome P450 enzymes: relevance to drug metabolism and toxicity

1994 • 160 citations

Identification of the rabbit and human cytochromes P-450IIIA as the major enzymes involved in the N-demethylation of diltiazem.

1990 • 158 citations

Warfarin-fluconazole. I. Inhibition of the human cytochrome P450-dependent metabolism of warfarin by fluconazole: in vitro studies.

1996 • 157 citations

The mechanism of the interaction between amiodarone and warfarin in humans

1992 • 155 citations

Pharmacokinetic Drug Interactions with Cyclosporin (Part I)1

1990 • 154 citations

Inhibition of desipramine hydroxylation in vitro by serotonin-reuptake-inhibitor antidepressants, and by quinidine and ketoconazole: a model system to predict drug interactions in vivo.

1994 • 151 citations

The effect of cimetidine on in vitro and in vivo microsomal drug metabolism in the rat

1980 • 147 citations

Species differences in the pharmacokinetics and metabolism of indinavir, a potent human immunodeficiency virus protease inhibitor.

1996 • 143 citations

Influence of Extracellular Matrix Overlay on Phenobarbital-Mediated Induction of CYP2B1, 2B2, and 3A1 Genes in Primary Adult Rat Hepatocyte Culture

1993 • 140 citations

Mechanism of induction of cytochrome P-450ac (P-450j) in chemically induced and spontaneously diabetic rats

1988 • 140 citations

Role of cytochrome P450 3A4 in human metabolism of MK-639, a potent human immunodeficiency virus protease inhibitor.

1996 • 139 citations

Inhibition of human CYP3A catalyzed 1'-hydroxy midazolam formation by ketoconazole, nifedipine, erythromycin, cimetidine, and nizatidine.

1994 • 139 citations

Effect of rifampicin.treatment on the metabolism of oestradiol and 17?-ethinyloestradiol by human liver microsomes

1975 • 138 citations

Increase of cytochrome P450IA2 activity by omeprazole: Evidence by the 13C-[N-3-methyl]-caffeine breath test in poor and extensive metabolizers of S-mephenytoin

1992 • 138 citations

Induction of Cytochrome P4501 as an Indicator of Potential Chemical Carcinogenesis

1993 • 135 citations

The genetic polymorphism of debrisoquine/sparteine metabolism—molecular mechanisms

1990 • 129 citations

Enoxacin-warfarin interaction: Pharmacokinetic and stereochemical aspects

1987 • 127 citations

Cyclosporin A metabolism in human liver, kidney, and intestine slices. Comparison to rat and dog slices and human cell lines.

1992 • 126 citations

Differential inhibition of individual human liver cytochromes P-450 by cimetidine

1991 • 118 citations

Metabolism of the Chemoprotective Agent Diallyl Sulfide to Glutathione Conjugates in Rats

1997 • 118 citations

In Vitro Prediction of the Terfenadine‐Ketoconazole Pharmacokinetic Interaction

1994 • 117 citations

Dual effects of macrolide antibiotics on rat liver cytochrome P-450

1983 • 116 citations

Interaction of Sodium Warfarin and Rifampin

1974 • 114 citations

Structural Basis of Selective Cytochrome P450 Inhibition

1995 • 111 citations

Induction of cytochrome P450IA genes (CYP1A) by omeprazole in the human alimentary tract

1992 • 110 citations

Particular ability of cytochromes P450 3A to form inhibitory P450-iron-metabolite complexes upon metabolic oxidation of aminodrugs

1995 • 110 citations

SKF 525-A inhibition, induction, and 452-nm complex formation.

1976 • 110 citations

Cytochrome P450 mediated metabolism of diazepam in human and rat: involvement of human CYP2C in N-demethylation in the substrate concentration-dependent manner

1993 • 109 citations

REDUCED INDUCTION OF DRUG METABOLISM IN THE ELDERLY

1978 • 109 citations

Species variation in the response of the cytochrome P-450-dependent monooxygenase system to inducers and inhibitors

1990 • 109 citations

The mechanism of the warfarin-rifampin drug interaction in humans

1987 • 109 citations

Steric factors in the inhibitory interaction of imidazoles with microsomal enzymes

1977 • 108 citations

Characterization of cDNAs, mRNAs, and proteins related to human liver microsomal cytochrome P-450 S-mephenytoin 4-hydroxylase

1988 • 106 citations

Inhibition of mixed-function oxidations by substrates forming reduced cytochrome P-450 metabolic-intermediate complexes

1977 • 105 citations

Inhibitors of Adrenal Steroid Biosynthesis

1970 • 105 citations

Effects of erythromycin on hepatic drug-metabolizing enzymes in humans

1983 • 104 citations

Influence of stiripentol on cytochrome P450-mediated metabolic pathways in humans: In vitro and in vivo comparison and calculation of in vivo inhibition constants*

1997 • 102 citations

Development of a simple incubation system for metabolism studies with precision-cut liver slices.

1993 • 101 citations

Pharmacokinetic and Pharmacodynamic Properties of Histamine H2-Receptor Antagonists

1991 • 101 citations

Mechanism of Inhibition of Adrenal Steroid 11β-Hydroxylase by Methopyrapone (Metopirone)

1963 • 101 citations

Induction of polymorphic 4′‐hydroxylation of S‐mephenytoin by rifampicin.

1990 • 99 citations

The complex interaction between ethanol and acetaminophen*

1996 • 96 citations

Physiological pharmacokinetics of ethoxybenzamide based on biochemical data obtainedin vitro as well as on physiological data

1982 • 93 citations

The potentiation of warfarin anticoagulation by amiodarone.

1982 • 93 citations

In Vitro Toxicology

2000 • 91 citations

Self-induction by erythromycin of its own transformation into a metabolite forming an inactive complex with reduced cytochrome P-450.

1981 • 91 citations

CLINICAL IMPLICATIONS OF ENZYME INDUCTION

1971 • 90 citations

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

1994 • 89 citations

Formation of an inactive cytochrome P-450 Fe(II)-metabolite complex after administration of troleandomycin in humans

1982 • 88 citations

Inhibition of the Carcinogenic Action of 7,12-Dimethylbenz(a)anthracene by Beta-Naphthoflavone

1968 • 86 citations

Specific and dose-dependent enzyme induction by omeprazole in human beings

1994 • 86 citations

Inhibition of Terfenadine Metabolism In Vitro by Azole Antifungal Agents and by Selective Serotonin Reuptake Inhibitor Antidepressants

1996 • 83 citations

Human Drug Metabolism: From Molecular Biology to Man

1992 • 83 citations

Studies on the interaction of safrole with rat hepatic microsomes

1975 • 82 citations

Induction of drug-metabolizing enzymes by xenobiotics

1990 • 82 citations

The effect of rifampicin on norethisterone pharmacokinetics

1979 • 82 citations

Antidepressant Drug Interactions and the Cytochrome P450 System: A Critical Appraisal

1995 • 81 citations

ACUTE REJECTION AND MASSIVE CYCLOSPORINE REQUIREMENTS IN HEART TRANSPLANT RECIPIENTS TREATED WITH RIFAMPIN

1985 • 81 citations

Diltiazem enhances the effects of triazolam by inhibiting its metabolism*

1996 • 78 citations

Syncope and cardiac arrhythmia due to an interaction between intraconazole and terfenadine

1993 • 76 citations

Formation and binding of carbanions by cytochrome P-450 of liver microsomes.

1973 • 75 citations

Covalent modification of lysine during the suicide inactivation of rat liver cytochrome P-450 by chloramphenicol

1981 • 75 citations

A class of strong inhibitors of microsomal monooxygenases: The elupticines

1979 • 73 citations

Diphenylhydantoin intoxication. A complication of isoniazid therapy.

1970 • 72 citations

Die Beschleunigung des Evipanabbaues unter der Wirkung von Barbituraten

1958 • 69 citations

Interethnic difference in omeprazole's inhibition of diazepam metabolism*

1995 • 66 citations

Rifampicin induction of lidocaine metabolism in cultured human hepatocytes.

1995 • 65 citations

Iron porphyrin-nitrene complexes: preparation from 1,1-dialkylhydrazines. Electronic structure from NMR, Moessbauer, and magnetic susceptibility studies and crystal structure of the [tetrakis(p-chlorophenyl)porphyrinato][(2,2,6,6-tetramethyl-1-piperidyl)nitrene]iron complex

1984 • 64 citations

On the mechanism of the inactivation of the major phenobarbital-inducible isozyme of rat liver cytochrome P-450 by chloramphenicol.

1985 • 64 citations

Induction of Cytochrome P450 Enzymes That Metabolize Xenobiotics

1995 • 64 citations

Inhibition of oxidative drug metabolism by orphenadrine: in vitro and in vivo evidence for isozyme-specific complexation of cytochrome P-450 and inhibition kinetics.

1989 • 63 citations

Further studies on the dissociation of the isosafrole metabolite-cytochrome p-450 complex

1979 • 62 citations

Prediction of in vivo disposition from in vitro systems: clearance of phenytoin and tolbutamide using rat hepatic microsomal and hepatocyte data.

1995 • 62 citations

The Use of Other Drugs to Allow a Lower Dosage of Cyclosporin to Be Used

1997 • 61 citations

Stereo- and regioselective N- and S-oxidation of tertiary amines and sulfides in the presence of adult human liver microsomes.

1993 • 61 citations

CYP1A1: Friend or Foe?

1993 • 58 citations

Selective inhibition of rat hepatic microsomal cytochrome P-450. I. Effect of the in vivo administration of cimetidine.

1992 • 58 citations

Effect of albumin on the estimation, in vitro, of phenytoin Vmax and Km values: implications for clinical correlation.

1997 • 56 citations

The molecular basis of genetic polymorphisms of drug metabolism.

1994 • 55 citations

Cyclosporine pharmacokinetic drug interactions

1989 • 55 citations

Differences between white subjects and Chinese subjects in the in vivo inhibition of cytochrome P450s 2C19, 2D6, and 3A by omeprazole*

1996 • 54 citations

Kinetics of drug metabolism in rat liver slices. II. Comparison of clearance by liver slices and freshly isolated hepatocytes.

1996 • 54 citations

Correlation betweenin vitro andin vivo drug metabolism rate: Oxidation of ethoxybenzamide in rat

1978 • 53 citations

Mechanism-based inactivation of cytochrome P450 2B1 by 2-ethynylnaphthalene: Identification of an active-site peptide

1993 • 52 citations

In vitro effects of quinoline derivatives on cytochrome p-450 and aminopyrine n-demethylase activity in rat hepatic microsomes

1984 • 51 citations

Influence of pyridine and some pyridine derivatives on spectral properties of reduced microsomes and on microsomal drug metabolizing activity

1974 • 50 citations

Generation of carbon monoxide during the microsomal metabolism of methylenedioxyphenyl compounds

1980 • 48 citations

Cytochrome P450 Monooxygenases and Interactions of Psychotropic Drugs: A Five-Year Update

1995 • 46 citations

Mechanism of the inhibitory action of isoniazid on microsomal drug metabolism

1981 • 44 citations

Inactivation of multiple hepatic cytochrome P-450 isozymes in rats by allylisopropylacetamide: mechanistic implications.

1987 • 43 citations

Interaction of Isoniazid and Warfarin

1977 • 39 citations

Isozyme selectivity of the inhibition of rat liver cytochromes P-450 by chloramphenicol in vivo.

1985 • 38 citations

Antipyrine metabolite kinetics in healthy human volunteers during multiple dosing of phenytoin and carbamazepine.

1985 • 38 citations

Inactivation of cytochrome P‐450 and production of N‐alkylated porphyrins caused in isolated hepatocytes by substituted dihydropyridines

1982 • 37 citations

Selective inhibitory interactions of alkoxymethylenedioxybenzenes towards mono-oxygenase activity in rat-hepatic microsomes

1985 • 37 citations

Metabolism of diazepam in vitro by human liver. Independent variability of N-demethylation and C3-hydroxylation.

1988 • 36 citations

Age‐dependent stereoselective increase in the oral clearance of hexobarbitone isomers caused by rifampicin.

1991 • 35 citations

Complexation of cytochrome P-450 isozymes in hepatic microsomes from SKF 525-A-induced rats

1988 • 35 citations

Human immunodeficiency virus protease inhibitors From drug design to clinical studies

1997 • 34 citations

2,3,7,8-Tetrachlorodibenzo-p-dioxin: Potent anticarcinogenic activity in CD-1 mice

1979 • 31 citations

The biotransformation of the ergot derivative CQA 206-291 in human, dog, and rat liver slice cultures and prediction of in vivo plasma clearance.

1993 • 30 citations

Self-induction by oleandomycin of its own transformation into a metabolite forming an inactive complex with reduced cytochrome P-450. Comparison with troleandomycin.

1982 • 29 citations

Oxidative metabolism of spironolactone: evidence for the involvement of electrophilic thiosteroid species in drug-mediated destruction of rat hepatic cytochrome P 450

1989 • 26 citations

Further insight into the stereoselective interaction between warfarin and cimetidine in man.

1991 • 25 citations

Cumene Hydroperoxide-Mediated Formation of Inhibited Complexes of Methylenedioxyphenyl Compounds with Cytochrome P-450

1975 • 25 citations

Effect of mefloquine on hepatic drug metabolism in the rat: Comparative study with primaquine

1985 • 24 citations

Time- and dose-dependent pharmacokinetics of L-754,394, an HIV protease inhibitor, in rats, dogs and monkeys.

1995 • 24 citations

Time-Dependent Kinetics IV: Pharmacokinetic Theory of Enzyme Induction

1979 • 23 citations

Differential haemin-mediated restoration of cytochrome P-450 N-demethylases after inactivation by allylisopropylacetamide

1985 • 22 citations

Effect of product inhibition on elimination kinetics of ethoxybenzamide in rabbits. Analysis by physiological pharmacokinetic model.

1984 • 20 citations

The discovery of fluconazole

1996 • 20 citations

Genetically determined steady-state interaction between encainide and quinidine in patients with arrhythmias.

1990 • 19 citations

Enzyme induction and beta‐adrenergic receptor blocking drugs.

1984 • 19 citations

Influence of pentobarbital on effect and plasma levels of alprenolol and 4‐hydroxy‐alprenolol

1979 • 17 citations

Time-dependent kinetics. V: Time course of drug levels during enzyme induction (one-compartment model)

1979 • 15 citations

Principles, mechanisms and biological consequences of induction

1992 • 13 citations

Phenobarbital and related compounds: approaches to interspecies extrapolation.

1992 • 11 citations

Mechanistic aspects of the inhibition of microsomal drug oxidation by primaquine

1986 • 9 citations

Time-Dependent Kinetics VI: Direct Relationship Between Equations for Drug Levels During Induction and Those Involving Constant Clearance

1979 • 6 citations

Deleted Work

1955 • 0 citations

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