2000
DOI: 10.4065/75.9.933
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Abstract: Grapefruit juice, a beverage consumed in large quantities by the general population, is an inhibitor of the intestinal cytochrome P-450 3A4 system, which is responsible for the first-pass metabolism of many medications. Through the inhibition of this enzyme system, grapefruit juice interacts with a variety of medications, leading to elevation of their serum concentrations. Most notable are its effects on cyclosporine, some 1,4-dihydropyridine calcium antagonists, and some 3-hydroxy-3-methylglutaryl coenzyme A … Show more

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Cited by 236 publications
(142 citation statements)
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“…Another difference in the method of the various studies is the ingestion of a single glass vs repeated ingestions. Despite results that demonstrated higher intensity after repeated ingestions (Lilja et al, 2000a), it appears that in most cases, ingestion of a single glass (250 ml) of regular strength grapefruit juice is enough to produce the maximum effect (Rau et al, 1997;Kane & Lipsky, 2000). In this fashion, no further changes in the pharmacokinetics of felodipine have been detected following 14 days of daily intake of grapefruit juice, compared to the effects after the first glass (Lundahl et al, 1998).…”
Section: Amounts and Timingmentioning
confidence: 90%
“…Another difference in the method of the various studies is the ingestion of a single glass vs repeated ingestions. Despite results that demonstrated higher intensity after repeated ingestions (Lilja et al, 2000a), it appears that in most cases, ingestion of a single glass (250 ml) of regular strength grapefruit juice is enough to produce the maximum effect (Rau et al, 1997;Kane & Lipsky, 2000). In this fashion, no further changes in the pharmacokinetics of felodipine have been detected following 14 days of daily intake of grapefruit juice, compared to the effects after the first glass (Lundahl et al, 1998).…”
Section: Amounts and Timingmentioning
confidence: 90%
“…Many popular herbal medicines have been routinely used or marketed as dietary supplements, such as St. John's wort and Ginkgo biloba (1). Flavonoids and their derivatives can be metabolized by CYP450 isozymes and/or directly inhibit CYP450 activities (2,3).…”
Section: Introductionmentioning
confidence: 99%
“…Both P450s 2B6 and 3A5 exhibit genetic polymorphisms and wide tissue distribution and play an important role in the metabolism of endobiotics and xenobiotics including clinical drugs routinely used in cancer chemotherapy, hormone therapy, inhibition of HIV protease, depression, immunosuppression, and calcium channel blockers (Kane and Lipsky, 2000;Ingelman-Sundberg, 2004). Knowledge concerning the effect of BG and related compounds on the function of P450s 2B6 and 3A5 is important for effective drug therapy and drug development.…”
mentioning
confidence: 99%