Pharmacokinetics and electroencephalographic effects of ketoconazole in the rat

Biopharmaceutics and Drug Disposition

Volumn 20, Issue 1, 1999, Pages 49-52

  Kotegawa, Tsutomu ^a   Laurijssens, Bart E ^a   Durol, Anna Liza B ^a   Greenblatt, David J ^a  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Electroencephalogram; Ketoconazole; Pharmacokinetics

Indexed keywords

BENZODIAZEPINE DERIVATIVE; KETOCONAZOLE;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG HALF LIFE; DRUG METABOLISM; ELECTROENCEPHALOGRAM; INTRAPERITONEAL DRUG ADMINISTRATION; MALE; NONHUMAN; RAT;

ANIMALS; ANTI-ANXIETY AGENTS; ANTIFUNGAL AGENTS; BIOLOGICAL AVAILABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; ELECTROENCEPHALOGRAPHY; HALF-LIFE; INJECTIONS, INTRAPERITONEAL; KETOCONAZOLE; MALE; METABOLIC CLEARANCE RATE; MIDAZOLAM; RATS; RATS, SPRAGUE-DAWLEY;

EID: 0032929396     PISSN: 01422782     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1099-081X(199901)20:1<49::AID-BDD158>3.0.CO;2-5     Document Type: Article

References (17)

1. J.W. Mandema, E. Tukker and M. Danhof, Pharmacokinetic-pharmacodynamic modelling of the EEG effects of midazolam in individual rats: influence of rate and route of administration. Br. J. Pharmacol., 102, 663-668 (1991).
2. D.J. Greenblatt, B.L. Ehrenberg, J. Gunderman, A. Locniskar, J.M. Scavone, J.S. Harmatz and R.I. Shader, Pharmacokinetic and electroencephalographic study of intravenous diazepam, midazolam, and placebo. Clin. Pharmacol. Ther., 45, 356-366 (1989).
3. D.J. Greenblatt, B.L. Ehrenberg, J. Gunderman, J.M. Scavone, N.T. Tai, J.S. Harmatz and R.I. Shader, Kinetic and dynamic study of intravenous lorazepam: comparison with intravenous diazepam. J. Pharmacol. Exp. Ther., 250, 134-140 (1989).
4. J.W. Mandema, B. Tuk, A.L. van Steveninck, D.D. Breimer, A.F. Cohen and M. Danhof, Pharmacokinetic-pharmacodynamic modelling of the central nervous system effects of midazolam and its main metabolite a-hydroxymidazolam in healthy volunteers. Clin. Pharmacol. Ther., 51, 715-728 (1992).
5. D.J. Greenblatt, J.S. Harmatz, T.A. Gouthro, J. Locke and R.I. Shader, Distinguishing a benzodiazepine agonist (triazolam) from a nonagonist anxiolytic (buspirone) by electroencephalography: kinetic-dynamic studies. Clin. Pharmacol. Ther., 56, 100-111 (1994).
6. L.L. von Moltke, D.J. Greenblatt, J.S. Harmatz, S.X. Duan, L.M. Harrel, MM. Cotreau-Bibbo, G.A. Pritchard, C.E. Wright and R.I. Shader, Triazolam biotransformation by human liver microsomes in vitro: effects of metabolic inhibitors and clinical confirmation of a predicted interaction with ketoconazole. J. Pharmacol. Exp. Ther., 276, 370-379 (1996).
7. D.J. Greenblatt, C.E. Wright, L.L. von Moltke, J.S. Harmatz, B.L. Ehrenberg, J.M. Harrel, K. Corbett, M. Counihan, S. Tobias and R.I.Shader, Ketoconazole inhibition of triazolam and alprazolam clearance: differential kinetic and dynamic consequences. Clin. Pharmacol. Ther., 64, 237-247 (1998).
8. J.M. Fahey, G.A. Pritchard, L.L. von Moltke, J.S. Pratt, J.M. Grassi, R.I. Shader and D.J. Greenblatt, Effect of ketoconazole on triazolam pharmacokinetics, pharmacodynamics and benzodiazepine receptor binding in mice. J. Pharmacol. Exp. Ther., 285, 271-276 (1998).
9. L.L. von Moltke, D.J. Greenblatt, J. Schmider, Duan, C.E. Wright, J.S. Harmatz and R.I. Shader, Midazolam hydroxylation by human liver microsomes in vitro: inhibition by fluoxetine, norfluoxetine, and by azole antifungal agents. J. Clin. Pharmacol., 36, 783-791 (1996).
10. L.L. von Moltke, D.J. Greenblatt, S.X. Duan, J.S. Harmatz and R.I. Shader, In vitro prediction of the terfenadine-ketoconazole pharmacokinetic interaction. J. Clin. Pharmacol., 34, 1222-1227 (1994).
11. C.M. Riley, Determination of ketoconazole in the plasma, liver, lung and adrenal of the rat by high-performance liquid chromatography. J. Chromatogr., 337, 287-294 (1986).
12. P.C. Iwen and N.G. Miller, Enhancement of ketoconazole penetration across the blood-brain barrier of mice by dimethyl sulfoxide. Antimicrob. Agents Chemother., 30, 617-618 (1986).
13. D. Matthew, B. Brennan, K. Zomorodi and J.B. Houston, Disposition of azole antifungal agents. I. Nonlinearities in ketoconazole clearance and binding in rat liver. Pharm. Res., 10, 418-422 (1993).
14. T.K. Daneshmend and D.W. Warnock, Clinical Pharmacokinetics of ketoconazole. Clin. Pharmacokinet., 14, 13-34 (1988).
15. L.W. Whitehouse, A. Menzies, B. Dawson, J. Zamecnik and W.W. Sy, Deacetylated ketoconazole: a major ketoconazole metabolite isolated from mouse liver. J. Pharmaceut. Biomed. Anal., 8, 603-606 (1990).
16. R.J. Rodriguez, and D. Acosta, Metabolism of ketoconazole and deacetylated ketoconazole by rat hepatic microsomes and flavin-containing monooxygenase. Drug Metab. Dispos., 25, 772-777 (1997).
17. R.P. Remmel, K. Amoh and M.M. Abdel-Monem, The disposition and pharmacokinetics of ketoconazole in the rat. Drug Metab. Dispos., 15, 735-739 (1987).