Alfentanil Disposition in Vivo Is Mediated by Cyp3a4 in Humans

Krivoruk, Y.; Kinirons, Mark; Wood, A J; Wood, M.

doi:10.1097/00000542-199409001-00380

Cited by 9 publications

(1 citation statement)

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“…Therefore it is plausible that the administration of voriconazole resulted in a major 77% to 90% reduction in alfentanil CL. The effect of voriconazole was stronger than that of erythromycin (25%) or fluconazole (55%) and similar to that of troleandomycin (79%) or ketoconazole (88%) 2 , 21 , 22 , 28 . In our study voriconazole also reduced the mean V ss of alfentanil by 25%.…”

Section: Discussionsupporting

confidence: 76%

Voriconazole, but not terbinafine, markedly reduces alfentanil clearance and prolongs its half-life

Saari

Laine

Leino

et al. 2006

Clinical Pharmacology & Therapeutics

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Section: Discussionsupporting

confidence: 76%

Voriconazole, but not terbinafine, markedly reduces alfentanil clearance and prolongs its half-life

Saari

Laine

Leino

et al. 2006

Clinical Pharmacology & Therapeutics

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Alfentanil und Remifentanil in der Kinderanästhesie

Reinhold¹,

Schneider²

1998

Neue Pharmaka Und Techniken in Der Kinderanästhesie

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The Effect of the Systemic Antimycotics, Itraconazole and Fluconazole, on the Pharmacokinetics and Pharmacodynamics of Intravenous and Oral Midazolam

Olkkola¹,

Ahonen²,

Neuvonen³

1996

Anesthesia & Analgesia

134

117

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We studied the interaction of azole antimycotics with intravenous (IV) and oral midazolam using a cross-over design in 12 volunteers, who ingested placebo, itraconazole, or fluconazole for 6 days. A 7.5-mg dose of midazolam was ingested on the first day, 0.05 mg/kg was administered IV on the fourth day, and 7.5 mg orally on the sixth day. Itraconazole reduced the clearance of IV midazolam by 69% and fluconazole reduced the clearance of IV midazolam by 51% (P < 0.001). A single dose of itraconazole and fluconazole increased the area under the oral midazolam concentration-time curve [AUC(0-infinity)] 3.5-fold (P < 0.001) and the peak concentration two-fold (P < 0.05) compared to placebo. On the sixth day the AUC(0-infinity) of oral midazolam was almost seven times greater with itraconazole (P < 0.001) and 3.6 times greater with fluconazole (P < 0.001) than without the antimycotics. The psychomotor effects of midazolam were also profoundly increased (P < 0.001). The psychomotor tests demonstrated only a weak interaction between the antimycotics and IV midazolam. When bolus doses of midazolam are given for short- time sedation, the effect of midazolam is not increased to a clinically significant degree by itraconazole and fluconazole, and it can be used in normal doses. However, the use of large doses of IV midazolam increases the risk of clinically significant interactions also after IV midazolam. Use of oral midazolam with itraconazole and fluconazole should be avoided.

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Alfentanil Disposition in Vivo Is Mediated by Cyp3a4 in Humans

Cited by 9 publications

References 0 publications

Voriconazole, but not terbinafine, markedly reduces alfentanil clearance and prolongs its half-life

Voriconazole, but not terbinafine, markedly reduces alfentanil clearance and prolongs its half-life

Alfentanil und Remifentanil in der Kinderanästhesie

The Effect of the Systemic Antimycotics, Itraconazole and Fluconazole, on the Pharmacokinetics and Pharmacodynamics of Intravenous and Oral Midazolam

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