title: Blood concentration curve of cyclosporine: impact of itraconazole in lung transplant recipients.
abstract: Although the influence of cytochrome P450 inhibitory drugs on the area under the curve (AUC) of cyclosporine (CsA) has been described, data concerning the impact of these substances on the shape of the blood concentration curve are scarce. By assessment of CsA blood levels before and 1, 2, and 4 hr after oral intake (C0, C1, C2, and C4, respectively) CsA profiling examinations were performed in 20 lung transplant recipients taking 400 mg, 200 mg, and no itraconazole, respectively. The three groups showed comparable results for C0, C2, and AUC(0-12). Greater values were found for Cmax, Cmax-C0, peak-trough fluctuation and rise to Cmax in favor of the non-itraconazole group. Additionally, tmax was shorter in the non-itraconazole group. Comedication with the metabolic inhibitor itraconazole is associated with a flattening of the CsA blood concentration profile in lung transplant recipients. These changes cannot be assessed by isolated C0, C2, or AUC(0-12) values alone.
authors: Clinic of Pulmonary Medicine, University Hospital Zurich, Zurich, Switzerland.
authors: Sarosh
authors: S
authors: Irani
authors: Karin
authors: K
authors: Fattinger
authors: Cornelia
authors: C
authors: Schmid-Mahler
authors: Eva
authors: E
authors: Achermann
authors: Rudolf
authors: R
authors: Speich
authors: Annette
authors: A
authors: Boehler
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D016572:Cyclosporine / Q000097:blood* / Q000493:pharmacokinetics / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D017964:Itraconazole / Q000494:pharmacology*; D016040:Lung Transplantation; D008297:Male; D008875:Middle Aged
chemical_list: D017964:Itraconazole; D016572:Cyclosporine