In vitro, pharmacokinetic, and pharmacodynamic interactions of ketoconazole and midazolam in the rat

Journal of Pharmacology and Experimental Therapeutics

Volumn 302, Issue 3, 2002, Pages 1228-1237

  Kotegawa, Tsutomu ^a   Laurijssens, Bart E ^b   Von Moltke, Lisa L ^a   Cotreau, Monette M ^a   Perloff, Michael D ^b   Venkatakrishnan, Karthik ^a   Warrington, Jill S ^b   Granda, Brian W ^b   Harmatz, Jerold S ^a   Greenblatt, David J ^a,b  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b TUFTS MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 HYDROXYMIDAZOLAM; ALPHA HYDROXYMIDAZOLAM; BENZODIAZEPINE RECEPTOR; DRUG METABOLITE; KETOCONAZOLE; MIDAZOLAM; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG INHIBITION; ELECTROENCEPHALOGRAPHY; GASTROINTESTINAL MUCOSA; HYDROXYLATION; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; RAT;

ALGORITHMS; ANIMALS; ANTI-ANXIETY AGENTS; ANTIFUNGAL AGENTS; BIOTRANSFORMATION; BODY WEIGHT; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; INJECTIONS, INTRAVENOUS; INTESTINES; INTUBATION, GASTROINTESTINAL; KETOCONAZOLE; LIVER CIRCULATION; MALE; MICROSOMES, LIVER; MIDAZOLAM; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY;

EID: 0036720879     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.035972     Document Type: Article

References (41)

1. Quantitation by gas chromatography of the 1- and 4-hydroxy metabolites of midazolam in human plasma
2. Methodologies to study the induction of rat hepatic and intestinal cytochrome P450 3A at the mRNA, protein and catalytic activity level
3. Differential selectivity of cytochrome P450 inhibitors against probe substrates in human and rat liver microsomes
4. Effect of ketoconazole on triazolam pharmacokinetics, pharmacodynamics and benzodiazepine receptor binding in mice
5. Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human and cDNA-expressed human cytochrome P450
6. Regioselective biotransformation of midazolam of members of the human cytochrome P450 3A (CYP3A) subfamily
7. The contribution of intestinal and hepatic CYP3A to the interaction between midazolam and clarithromycin
8. Effect of age, gender and obesity on midazolam kinetics
9. Kinetics and dynamics of lorazepam during and after continuous intravenous infusion
10. Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole and fluconazole
11. Ketoconazole inhibition of triazolam and alprazolam clearance: Differential kinetic and dynamic consequences
12. A novel cytochrome P450 3A isoenzyme in rat intestinal microsomes
13. Dose-dependent intestinal and hepatic first-pass metabolism of midazolam, a cytochrome P4503A substrate with differently modulated enzyme activity in rats
14. In vivo and in vitro metabolic clearance of midazolam, a cytochrome P4503A substrate, by the liver under normal and increased enzyme activity in rats
15. Hepatic metabolic clearance of midazolam, a Cytochrome P450 3A substrate, in the presence of ketoconazole in rats
16. Substrate specificity for rat cytochrome P450 (CYP) isoforms: Screening with cDNA-expressed systems of the rat
17. Pharmacokinetics and electroencephalographic effects of ketoconazole in the rat
18. Use of one cannula for both blood sampling and drug administration: A potential cause of overestimation of drug concentration
19. Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4
20. Pharmacokinetics and bioavailability of midazolam after intravenous, subcutaneous, intraperitoneal and oral administration under a chronic food-limited regimen: Relating DRL performance to pharmacokinetics
21. Pharmacokinetic-pharmacodynamic relationships for benzodiazepines
22. Effect of 7-day exposure to midazolam on electroencephalogram pharmacodynamics in rats: A model to study multiple pharmacokinetic-pharmacodynamic relationships in individual animals
23. Electroencephalogram effect measures and relationships between pharmacokinetics and pharmacodynamics of centrally acting drugs
24. Disposition of azole antifungal agents. 1. Nonlinearities in ketoconazole clearance and binding in rat liver
25. Concentration-independent plasma protein binding of benzodiazepines
26. Midazolam and triazolam biotransformation in mouse and human liver microsomes: Relative contribution of CYP3A and CYP2C isoforms
27. Simultaneous assessment of CYP3A4 and CYP1A2 activity in vivo with alprazolam and caffeine
28. In vitro and in vivo drug interactions involving human CYP3A
29. Differentiation of intestinal and hepatic cytochrome P450 3A activity with use of midazolam as an in vivo probe: Effect of ketoconazole
30. Effects of the antifungal agents on oxidative drug metabolism in humans: Clinical relevance
31. Human drug metabolism and the cytochromes P450: Application and relevance of in vitro models
32. Inhibitors of alprazolam metabolism in vitro: Effect of serotonin-reuptake-inhibitor antidepressants, ketoconazole and quinidine
33. Zolpidem metabolism in vitro: Responsible cytochromes, chemical inhibitors and in vivo correlations
34. Triazolam biotransformation by human liver microsomes in vitro: Effects of metabolic inhibitors and clinical confirmation of a predicted interaction with ketoconazole
35. Midazolam hydroxylation by human liver microsomes in vitro: Inhibition by fluoxetine, norfluoxetine and by azole antifungal agents
36. Metabolism of drugs by Cytochrome P450 3A isoforms: Implications for drug interactions in psychopharmacology
37. In vitro approaches to predicting drug interactions in vivo
38. The effects of age on in vitro midazolam biotransformation in male CD-1 mouse liver microsomes
39. Quantitative prediction of metabolic inhibition of midazolam by itraconazole and ketoconazole in rats: Implication of concentrative uptake of inhibitors into liver
40. Correlation between in vivo and in vitro hepatic uptake of metabolic inhibitors of cytochrome P-450 in rats
41. Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam and triazolam