Molecular and pharmacokinetic evaluation of rat hepatic and gastrointestinal cytochrome P450 induction by tamoxifen

Pharmacology

Volumn 63, Issue 4, 2001, Pages 210-219

  Cotreau, Monette M ^a   Von Moltke, Lisa L ^a   Harmatz, Jerold S ^a   Greenblatt, David J ^a  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Gastrointestinal cytochrome P450 3A; Induction; Midazolam hydroxylation; Quantitative Western blotting; RT PCR; Tamoxifen

Indexed keywords

4 HYDROXYTAMOXIFEN; CYTOCHROME P450 3A; DEXAMETHASONE; ISOPROTEIN; MESSENGER RNA; MIDAZOLAM; NORTAMOXIFEN; PHENOBARBITAL; TAMOXIFEN;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CATALYSIS; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; DRUG CLEARANCE; DRUG METABOLISM; ENZYME INDUCTION; FEMALE; INTESTINE; LIVER; NONHUMAN; PRIORITY JOURNAL; RAT;

ANALYSIS OF VARIANCE; ANIMALS; ANTI-ANXIETY AGENTS; ANTINEOPLASTIC AGENTS, HORMONAL; ARYL HYDROCARBON HYDROXYLASES; CATALYSIS; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; DIGESTIVE SYSTEM; FEMALE; LIVER; MIDAZOLAM; OXIDOREDUCTASES, N-DEMETHYLATING; RATS; RATS, SPRAGUE-DAWLEY; RNA, MESSENGER; TAMOXIFEN;

EID: 0035208511     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000056136     Document Type: Article

References (47)

1. Tamoxifen, raloxifene, and the prevention of breast cancer
2. Tamoxifen for prevention of breast cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study
3. Variable contribution of cytochromes P450 2D6, 2C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes
4. Identification of the cytochrome P450 IIIA family as the enzymes involved in the N-demethylation of tamoxifen in human liver microsomes
5. Tamoxifen metabolism by microsomal cytochrome P450 and flavin-containing monooxygenase
6. Metabolism of the antimammary cancer antiestrogen agent tamoxifen. I. Cytochrome P-450-catalyzed N-demethylation and 4-hydroxylation
7. Metabolism of the antimammary cancer antiestrogen agent tamoxifen. II. Flavin-containing monooxygenase-mediated N-oxidation
8. Alterations of drug metabolizing and antioxidant enzyme activities during tamoxifen-induced hepatocarcinogenesis in the rat
9. Regulation of gene expression of various phase I and phase II drug metabolizing enzymes by tamoxifen in rat liver
10. Effects of tamoxifen administration on the expression of xenobiotic metabolizing enzymes in rat liver
11. Structure-activity relationships for triphenylethylene antiestrogens on hepatic phase-I and phase-II enzyme expression
12. Induction of CYP2B1 and 3A1, and associated monooxygenase activities by tamoxifen and certain analogues in the livers of female rats and mice
13. Metabolites, pharmacodynamics, and pharmacokinetics of tamoxifen in rats and mice compared to the breast cancer patient
14. A comparative study of tamoxifen metabolism in female rat, mouse and human microsomes
15. Distribution of tamoxifen and its metabolites in rat and human tissue during steady-state treatment
16. Tamoxifen-associated reduction in tricyclic antidepressant levels in blood
17. Metabolism of tricyclic antidepressants
18. N-demethylation of amitriptyline in vitro: Role of cytochrome P-450 3A (CYP3A) isoforms, and effect of metabolic inhibitors
19. Major pathway of imipramine metabolism is catalyzed by cytochromes P-450 1A2 and P-450 3A4 in human liver
20. Molecular and physical mechanisms of first-pass extraction
21. Effect of dexamethasone on the intestinal first-pass metabolism of indinavir in rats: Evidence of cytochrome P-4503A and p-glycoprotein induction
22. Differences between small and large intestine and liver in the inducibility of microsomal enzymes in response to stimulation by phenobarbitone and beta-naphthoflavone in the diet
23. Intestinal epithelial cell surface membrane glycoprotein synthesis. I. An indicator of cellular differentiation
24. Methodologies to study the induction of rat hepatic and intestinal cytochrome P450 3A at the mRNA, protein, and catalytic activity level
25. Preparation of microsomes with calcium
26. 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
27. A major glucocorticoid-inducible P450 in rat liver is not P450 3A1
28. Cleavage of structural proteins during the assembly of the head of bacteriophage T4
29. Midazolam hydroxylation by human liver microsomes in vitro: Inhibition by fluoxetine, norfluoxetine, and by azole antifungal agents
30. Quantitation by gas chromatography of the 1-and 4-hydroxy metabolites of midazolam in human plasma
31. Electron-capture gas chromatographic analysis of the triazolobenzodiazepines alprazolam and triazolam
32. Pharmacokinetics of tamoxifen in premenopausal and postmenopausal women with breast cancer
33. Distribution of 4-hydroxy-n-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment
34. A cytochrome P-450 multigene family: Characterization of a gene activated by phenobarbital administration
35. Phenobarbital induction of cytochrome P-450 gene expression
36. Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cDNA-expressed human cytochrome P450
37. Influence of tamoxifen and its N-desmethyl and 4-hydroxy metabolites on rat liver microsomal enzymes
38. The influence of polyethylene glycol and acetone on the in vitro biotransformation of tamoxifen and alprazolam by human liver microsomes
39. Induction of cytochrome P-450 by glucocorticoids in rat liver. I. Evidence that glucocorticoids and pregnenolone 16 alpha-carbonitrile regulate de novo synthesis of a common form of cytochrome P-450 in cultures of adult rat hepatocytes and in the liver in vivo
40. Comparative fates of clomiphene and tamoxifen in the immature female rat
41. Metabolism of tamoxifen and its uterotrophic activity
42. Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism
43. Pharmacokinetics and bioavailability of midazolam after intravenous, subcutaneous, intraperitoneal and oral administration under a chronic food-limiting regimen: Relating DRL performance to pharmacokinetics
44. A novel mechanism for the enhancement of acetaminophen hepatotoxicity by phenobarbital
45. Effect of phenobarbital and p-hydroxyphenobarbital glucuronide on acetaminophen metabolites in isolated rat hepatocytes: Use of a kinetic model to examine the rates of formation and egress
46. Impaired biliary excretion of acetaminophen glucuronide in the isolated perfused rat liver after acute phenobarbital treatment and in vivo phenobarbital treatment
47. Acute phenobarbital administration alters the disposition of acetaminophen metabolites in the rat