Effect of roxithromycin on the pharmacokinetics of lovastatin in volunteers

Bucher, M. and Mair, G. and Kees, Frieder (2002) Effect of roxithromycin on the pharmacokinetics of lovastatin in volunteers. EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 57 (11). pp. 787-791. ISSN 0031-6970

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Abstract

Objective: To investigate the influence of concomitant administration of roxithromycin on the plasma pharmacokinctics of lovastatin. Methods: In an open, randomized, crossover study, 12 healthy volunteers received 80 mg lovastatin orally either alone or concomitantly with 300 mg roxithromycin after 5-day pretreatment with roxithromycin 30 mg daily. Plasma concentrations of lovastatin (lactone and acid) were determined using high-performance liquid chromatography, and the pharmacokinetic parameters were estimated. Results: The mean (+/-SD) pharmacokinetic parameters of lovastatin lactone with and without roxithromycin were maximum concentration (C-max) 8.49 +/- 6.80/16.3 +/- 9.4ng ml(-1), time to Cmax (t(max)) 1.8 +/- 04/1.7 +/- 0.6h, terminal plasma half-life (t(1/2)) 4.3 +/- 2.0/3.7 +/- 2.5 h, area under the plasma concentration-time curve from zero to infinity (AUC(0) (infinity)) 53 +/- 60/85 +/- 67 ng ml(-1) h. The respective parameters of lovastatin acid were C-max 24.6 +/- 13.4/17.8 +/- 11.0 ng ml(-1), t(max) 3.7 +/- 1.1/4.1 +/- 0.7 h, t(1/2) 3.2 +/- 2.5/4.3 +/- 2.8 h, AUC(0) (infinity) 149 +/- 123/105 +/- 58 ng ml(-1) h. Mean bioavailability of lovastatin lactone was lower and that of lovastatin acid was higher with concomitant treatment. However, the differences were significant only with respect to lovastatin lactone (AUC and C-max) and C-max of lovastatin acid. Conclusion: Roxithromycin does not influence the pharmacokinetics of lovastatin in such a way that dosage adjustment of lovastatin seems to be necessary during co-administration.

Item Type: Article
Uncontrolled Keywords: PERFORMANCE LIQUID-CHROMATOGRAPHY; REDUCTASE INHIBITORS; GRAPEFRUIT JUICE; ERYTHROMYCIN; SIMVASTATIN; THERAPY; ACID; ATHEROSCLEROSIS; RHABDOMYOLYSIS; ANTIBACTERIALS; lovastatin; roxithromycin; pharmacokinetics
Subjects: 600 Technology > 610 Medical sciences Medicine
600 Technology > 615 Pharmacy
Divisions: Medicine > Lehrstuhl für Anästhesiologie
Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Frieder Kees
Depositing User: Dr. Gernot Deinzer
Date Deposited: 16 Nov 2021 05:48
Last Modified: 16 Nov 2021 05:48
URI: https://pred.uni-regensburg.de/id/eprint/40734

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