Fluconazole, but not terbinafine, enhances the effects of triazolam by inhibiting its metabolism

British Journal of Clinical Pharmacology

Volumn 41, Issue 4, 1996, Pages 319-323

  Varhe, Anu ^a   Olkkola, Klaus T ^a   Neuvonen, Pertti J ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

Author keywords

Fluconazole; Interaction; Pharmacodynamics; Pharmacokinetics; Terbinafine; Triazolam

Indexed keywords

FLUCONAZOLE; PLACEBO; TERBINAFINE; TRIAZOLAM;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENTIATION; FEMALE; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACODYNAMICS; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; VOLUNTEER;

EID: 0029981350     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.1996.03189.x     Document Type: Article

References (23)

1. Dollery C, ed. Therapeutic drugs, vol 2. Edinburgh, Great-Britain: Churchill Livingstone, 1991: T133-136.
2. Kronbach T, Mathys D, Umeno M, Gonzales FJ, Meyer UA. Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4. Mol Pharmacol 1989; 36: 89-96.
3. Varhe A, Olkkola KT, Neuvonen PJ. Oral triazolam is potentially hazardous to patients receiving systemic antimycotics ketoconazole or itraconazole. Clin Pharmacol Ther 1994; 56: 601-607.
4. Back DJ, Tjia JF, Abel SM. Azoles, allylamines and drug metabolism. Br J Dermatol 1992; 126: 14-18.
5. Honig PK, Wortham DC, Zamani K, et al. Terfenadine-ketoconazole interaction: pharmacokinetic and electrocardiographic consequences. JAMA 1993; 269: 1513-1518.
6. Pohjola-Sintonen S, Viitasalo M, Toivonen L, Neuvonen PJ. Itraconazole prevents terfenadine metabolism and increases risk of torsades de pointes ventricular tachycardia. Eur J Clin Pharmacol 1993; 45: 191-193.
7. Honig PK, Wortham DC, Zamani K, et al. The effect of fluconazole on the steady-state pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine in humans. Clin Pharmacol Ther 1993; 53: 630-636.
8. Olkkola KT, Ahonen J, Neuvonen PJ. Effect of the systemic antimycotics itraconazole and fluconazole on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Acta Anaesthesiol Scand 1995; 105: 158. [Abstract]
9. Canafax DM, Graves NM, Hilligoss DM, Carleton BC, Gardner MJ, Matas AJ. Interaction between cyclosporine and fluconazole in renal allograft recipients. Transplantation 1991; 51: 1014-1018.
10. Mattila MJ, Vainio P, Vanakoski J. Fluconazole moderately increases midazolam effects on performance. Br J Clin Pharmacol 1995; 39: 567P. [Abstract]
11. Grant SM, Clissold SP. Fluconazole: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial and systemic mycoses. Drugs 1990; 39: 877-916.
12. Balfour JA, Faulds D. Terbinafine: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial mycoses. Drugs 1992; 43: 259-284.
13. Back DJ, Tjia JF. Comparative effects of two antimycotic agents, ketoconazole and terbinafine on the metabolism of tolbutamide, ethinyloestradiol, cyclosporin and ethoxycoumarin by human liver microsomes in vitro. Br J Clin Pharmacol 1989; 28: 166-170.
14. DeKroon IFI, Langendijk PNJ, De Goede PNFC. Simultaneous determination of midazolam and its three hydroxy metabolites in human plasma by electron-capture gas chromatography without derivatization. J Chromatogr 1989; 491: 107-116.
15. Gaillard Y, Gay-Montchamp J-P, Ollagnier M. Simultaneous screening and quantitation of alpidem, zolpidem, buspirone and benzodiazepines by dual-channel gas chromatography using electron-capture and nitrogen-phosphorpus detection after solid-phase extraction. J Chromatogr 1993; 622: 197-208.
16. Kovarik JM, Kirkesseli S, Humbert H, Grass P, Kutz K. Dose-proportional pharmacokinetics of terbinafine and its N-demethylated metabolite in healthy volunteers. Br J Dermatol 1992; 126: 8-23.
17. Inagaki K, Takagi J, Lor E, Okamoto MP, Gill MA. Determination of fluconazole in human serum by solid-phase extraction and reversed-phase HPLC. Ther Drug Monitor 1992; 14: 306-311.
18. Gibaldi M, Perrier D. Pharmacokinetics. 2nd ed. New York: Marcel Dekker, 1982.
19. Gorski JC, Hall SD, Jones DR, VandenBranden M, Wrighton SA. Regioselective biotransformation of midazolam by members of the human cytochrome P450 3A (CYP3A) subfamily. Biochem Pharmacol 1994; 47: 1643-1653.
20. Pelkonen O, Breimer DD. Role of environmental factors in the pharmacokinetics of drugs: Considerations with respect to animal models, P-450 enzymes, and probe drugs. In Handbook of Experimental Pharmacology, Vol 110. Berlin: Springer-Verlag, 1994.
21. Robin DW, Lee M, Hasan SS, Wood AJJ. Triazolam in cirrhosis: pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther 1993; 54: 630-637.
22. Hargreaves JA, Jezequel S, Houston JB. Effect of azole antifungals on human microsomal metabolism of diclofenac and midazolam. Br J Clin Pharmacol 1994; 38: 175P. [Abstract]
23. Grant SM, Clissold SP. Itraconazole: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in superficial and systemic mycoses. Drugs 1989; 37: 310-344.