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The effect of grapefruit juice on the pharmacokinetics of orally administered verapamil

  • PHARMACOKINETICS AND DISPOSITION
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Abstract

Objective: To investigate the effect of grapefruit juice (GJ) on the pharmacokinetics of orally administered verapamil in hypertensive patients.

Methods: Ten hypertensive patients on chronic verapamil treatment participated in a two-day study. On day 1 200 ml of water was given 1 hour before, and together with the morning verapamil dose; on the day 2, water was replaced by GJ in the same order. Serial blood samples were collected and the concentrations of verapamil and its main dealkylated metabolite (D-617) were determined by high-performance liquid chromatography (HPLC). The area under the concentration versus time curve of verapamil (AUCv) and its metabolite D-617 (AUCM) were calculated before and after GJ ingestion. The peak serum concentration (Cmax) and the time until its appearance (tmax) were also determined.

Results: GJ did not affect Cmax, tmax, AUCv or AUVm. The AUCv/AUCm ratio (AUCR) was slightly, but significantly, increased after GJ (1.67 vs 1.92).

Conclusions: A single administration of GJ with short-acting verapamil has no significant effect on the pharmacokinetics, of verapamil.

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Received: 2 October 1997 / Accepted in revised form: 2 March 1998

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Zaidenstein, R., Dishi, V., Gips, M. et al. The effect of grapefruit juice on the pharmacokinetics of orally administered verapamil. E J Clin Pharmacol 54, 337–340 (1998). https://doi.org/10.1007/s002280050470

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  • DOI: https://doi.org/10.1007/s002280050470

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