Fluconazole but not itraconazole decreases the metabolism of losartan to E-3174

European Journal of Clinical Pharmacology

Volumn 53, Issue 6, 1998, Pages 445-449

  Kaukonen, K M ^a   Olkkola, K T ^a   Neuvonen, P J ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

Author keywords

Fluconazole; Losartan

Indexed keywords

FLUCONAZOLE; ITRACONAZOLE; LOSARTAN; LOSARTAN POTASSIUM;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD PRESSURE MONITORING; CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG METABOLISM; FEMALE; HEART RATE; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ADULT; ANTIFUNGAL AGENTS; ANTIHYPERTENSIVE AGENTS; ARYL HYDROCARBON HYDROXYLASES; CROSS-OVER STUDIES; CYTOCHROME P-450 ENZYME SYSTEM; DOUBLE-BLIND METHOD; DRUG INTERACTIONS; FEMALE; FLUCONAZOLE; HUMANS; IMIDAZOLES; ITRACONAZOLE; LOSARTAN; MALE; MIXED FUNCTION OXYGENASES; REFERENCE VALUES; STEROID 16-ALPHA-HYDROXYLASE; STEROID HYDROXYLASES; TETRAZOLES;

EID: 0031957174     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002280050405     Document Type: Article

References (16)

1. Munafo A, Christen Y, Nussberger J, Shum LY, Borland RM, Lee RJ, Waeber B, Biollaz J. Brunner HR (1992) Drug concentration response relationships in normal volunteers after oral administration of losartan, an angiotensin II receptor antagonist. Clin Pharmacol Ther 51: 513-521
2. Stearns RA, Chakravarty PK, Chen R. Chiu S-HL (1995) Biotransformation of losartan to its active carboxylic acid metabolite in human liver microsomes. Role of cytochrome P4502C and 3A subfamily members. Drug Metab Dispos 23: 207-215
3. Yun C-H, Lee HS, Lee H, Rho JK, Jeong HG, Guengerich FP (1995) Oxidation of the angiotensin II receptor antagonist losartan (DuP 753) in human liver microsomes. Role of cytochrome P4503A(4) in formation of the active metabolite FXP3174. Drug Metab Dispos 23: 285-289
4. Olkkola KT, Ahonen J, Neuvonen PJ (1996) The effect of the systemic antimycotics, itraconazole and fluconazole, on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Anesth Analg 82: 511-516
5. Varhe A, Olkkola KT, Neuvonen PJ (1996) Effect of fluconazole dose on the extent of fluconazole-triazolam interaction. Br J Clin Pharmacol 42: 465-470
6. Blum RA, Wilton JH, Hilligoss DM, Gardner MJ, Henry EB, Harrison NJ, Schentag JJ (1991) Effect of fluconazole on the disposition of phenytoin. Clin Pharmacol Ther 49:420-425
7. Jalava K-M. Olkkola KT. Neuvonen PJ (1997) Itraconazole greatly increases plasma concentrations and effects of felodipine. Clin Pharmacol Ther 61: 410-415
8. Olkkola KT, Backman JT, Neuvonen PJ (1994) Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole. Clin Pharmacol Ther 55: 481-485
9. Varhe A, Olkkola KT, Neuvonen PJ (1994) Oral triazolam is potentially hazardous to patients receiving systemic antimycotics ketoconazole or itraconazole. Clin Pharmacol Ther 56: 601-607
10. Hargreaves JA, Jezequel S. Houston JB (1994) Effect of azole antifungals on human microsomal metabolism of diclofenac and midazolam [abstract]. Br J Clin Pharmacol 38: 175P
11. Furtek CI, Lo M-W (1992) Simultaneous determination of a novel angiotensin II receptor blocking agent, losartan and its metabolite in human plasma and urine by high-performance liquid chromatography. J Chromatogr 573: 295-301
12. Allenmark S, Edebo A, Lindgren K (1990) Determination of itraconazole in serum with high-performance liquid chromatography and fluorescence detection. J Chromatogr 532: 203-206
13. Remmel RP, Dombrowskis D, Canafax DM (1988) Assay of itraconazole in leucemic patients by reverse-phase small-bore liquid chromatography. J Chromatogr 432: 388-394
14. Harris SC, Wallace JE, Foulds GF, Rinaldi MG (1989) Assay of fluconazole by megabore capillary gas-liquid chromatography with nitrogen-selective detection. Antimicrob Agents Chemother 33: 714-716
15. Lo M-W, Goldberg MR, McCrea JB, Lu H, Furtek CI, Bjornsson TD (1995) Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans. Clin Pharmacol Ther 58: 641-649
16. Wong PC, Price WA, Chiu AT, Duncia JV, Cavini DJ, Wexler RR, Johnson AL, Timmermans PBMWM (1991) Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent. J Pharmacol Exp Ther 255: 211-217