Effects of Grapefruit Juice Consumption on Pharmacokinetics of Low Dose Simvastatin: Cross-over Study with a Review of the LiteratureAkira Kurata1*, Hiroyuki Hagiwara1, Taketomo Ohmomo1, Sachio Suzuki1, Kuniaki Nakahara1, Shingo Konno1, Chihiro Kijima1, Madoka Inukai1, Hitoshi Ozawa1, Kiyotaka Fujii1and Masataka Majima2
- *Corresponding Author:
- Dr. Akira Kurata
Department of Neurosurgery
Kitasato University School of Medicine, Kanagawa, Japan
E-mail: [email protected]
Received date: March 14, 2012; Accepted date: March 30, 2012; Published date: March 31, 2012
Citation: KKurata A, Hagiwara H, Ohmomo T, Suzuki S, Nakahara K, et al. (2012) Effects of Grapefruit Juice Consumption on Pharmacokinetics of Low Dose Simvastatin: Cross-over Study with a Review of the Literature. Med chem 2:048- 050. doi:10.4172/2161-0444.1000113
Copyright: © 2012 Kurata A, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
The effects of consumption of grapefruit juice on the pharmacokinetics of conventional low-dose simvastatin in Japan were investigated. In a randomized cross-over study with two phases, 10 healthy volunteers ingested grapefruit juice 400ml or water for 2 days. On day 3, a single 5mg dose of simvastatin was administered with grapefruit juice 200ml or water. Plasma concentrations of HMG-CoA reductase inhibitor were determined up to 8 h thereafter. Grapefruit juice increased the area under the plasma concentration-time curves from 0 to 8 h of total HMG-CoA reductase inhibitor 1.7- fold (p=0.002) and that of active HMG-CoA reductase inhibitor 1.7-fold (p=0.024). However, the peak concentrations (Cmax) and Tmax of total and active HMG-CoA reductase inhibitors were not significant influenced.Consumption of grapefruit juice with low-dose simvastatin thus resulted in mild increase of the plasma HMG-CoA reductase inhibitor, so that the pharmacokinetic interaction can be labeled as of weak CYP3A type.