Literature DB >> 6149911

Ketoconazole: a potent inhibitor of cytochrome P-450-dependent drug metabolism in rat liver.

J J Sheets, J I Mason.   

Abstract

Ketoconazole, an orally active imidazole antimycotic agent, is shown to be a potent inhibitor of drug N-demethylase activities of liver microsomes from rats pretreated with phenobarbital or pregnenolone-16 alpha-carbonitrile, and an inhibitor of 7-ethoxyresorufin O-deethylase activity of liver microsomes from rats pretreated with 5,6-benzoflavone. Spectrophotometric studies reveal that the imidazole compound binds to the cytochrome P-450 component of the monooxygenase complex, and has little effect on NADPH-cytochrome c (P-450) reductase activity. These results are strongly suggestive that cytochrome P-450 is the site of action of this potent inhibitor of drug metabolism in liver microsomes.

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Year:  1984        PMID： 6149911

Source DB:  PubMed          Journal:  Drug Metab Dispos        ISSN： 0090-9556            Impact factor:   3.922


  26 in total

Review 1.  In vitro models for studying toxicity of antifungal agents.

Authors:  V Joly; J Bolard; P Yeni
Journal:  Antimicrob Agents Chemother       Date:  1992-09       Impact factor: 5.191

2.  Pharmacokinetics of the cyclosporine-ketoconazole interaction in dogs.

Authors:  A D'mello; R Venkataramanan; M Satake; S Todo; S Takaya; R J Ptachcinski; G J Burckart; T E Starzl
Journal:  Res Commun Chem Pathol Pharmacol       Date:  1989-06

3.  Direct and metabolism-dependent toxicity of sulphasalazine and its principal metabolites towards human erythrocytes and leucocytes.

Authors:  M Pirmohamed; M D Coleman; F Hussain; A M Breckenridge; B K Park
Journal:  Br J Clin Pharmacol       Date:  1991-09       Impact factor: 4.335

4.  Deuteration of the farnesyl terminal methyl groups of δ-tocotrienol and its effects on the metabolic stability and ability of inducing G-CSF production.

Authors:  Xingui Liu; Zhengya Gao; Qiang Fu; Lin Song; Peiyi Zhang; Xuan Zhang; Howard Hendrickson; Peter A Crooks; Daohong Zhou; Guangrong Zheng
Journal:  Bioorg Med Chem       Date:  2020-04-08       Impact factor: 3.641

5.  Ketoconazole blocks bile acid synthesis in hepatocyte monolayer cultures and in vivo in rat by inhibiting cholesterol 7 alpha-hydroxylase.

Authors:  H M Princen; C M Huijsmans; F Kuipers; R J Vonk; H J Kempen
Journal:  J Clin Invest       Date:  1986-10       Impact factor: 14.808

6.  Integral membrane proteins Brr6 and Apq12 link assembly of the nuclear pore complex to lipid homeostasis in the endoplasmic reticulum.

Authors:  Christine A Hodge; Vineet Choudhary; Michael J Wolyniak; John J Scarcelli; Roger Schneiter; Charles N Cole
Journal:  J Cell Sci       Date:  2010-01-01       Impact factor: 5.285

7.  Cytotoxicity of ketoconazole in malignant cell lines.

Authors:  C F Rochlitz; L E Damon; M B Russi; A Geddes; E C Cadman
Journal:  Cancer Chemother Pharmacol       Date:  1988       Impact factor: 3.333

8.  Generation of oxygen free radicals during the metabolism of cyclosporine A: a cause-effect relationship with metabolism inhibition.

Authors:  F Serino; J Grevel; K L Napoli; B D Kahan; H W Strobel
Journal:  Mol Cell Biochem       Date:  1993-05-26       Impact factor: 3.396

9.  An investigation of the role of metabolism in dapsone-induced methaemoglobinaemia using a two compartment in vitro test system.

Authors:  M D Tingle; M D Coleman; B K Park
Journal:  Br J Clin Pharmacol       Date:  1990-12       Impact factor: 4.335

10.  Metabolism of retinoic acid and retinol during differentiation of F9 embryonal carcinoma cells.

Authors:  J B Williams; J L Napoli
Journal:  Proc Natl Acad Sci U S A       Date:  1985-07       Impact factor: 11.205
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