PMID: 12883234

Issn Print: 0163-4356

Publication Date: 2003/08/01


Print

Itraconazole-Tacrolimus Drug Interaction

Matthew J. Cervelli; Graeme R. Russ

+ Author Information

Author Information: Pharmacy Department, Renal Unit The Queen Elizabeth Hospital Adelaide, South Australia 5011, Australia

    loading  Checking for direct PDF access through Ovid

Excerpt

To the Editor: The immunosuppressant drug tacrolimus (Tac) is primarily metabolized by cytochrome P450 3A4 (CYP 3A4) and is a P-glycoprotein (P-gp) drug efflux pump substrate. Tac is therefore prone to several theoretical and confirmed interactions with drugs that interfere with CYP 3A4 and P-gp function. Such drugs include diltiazem, erythromycin, verapamil, and the azole antifungals such as itraconazole.
In fact, several interactions between itraconazole and tacrolimus have been reported. These cases describe a need to reduce the Tac dosage to between 20 and 50% of the original dose to achieve target trough blood concentrations.1–5 This case describes a more powerful interaction than previously reported, whereby a 17.5-fold reduction in Tac dose (6% of original) was needed to maintain a target trough (whole blood) Tac concentration.
    loading  Loading Related Articles