Metabolic and analytical interactions of grapefruit juice and 1,2-benzopyrone (coumarin) in man

Runkel, M.; Tegtmeier, M.; Legrum, Wolfgang

doi:10.1007/s002280050097

Cited by 20 publications

(5 citation statements)

References 13 publications

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“…Inconsistent data were derived from studies performed with coumarins. The percentage of 7‐hydroxycoumarin excreted in urine was found to be decreased, 115 but in a second study, the appearance of the metabolite was delayed, whereas the recovery in urine was unchanged 116 . The delay in appearance of the metabolite was confirmed in a third study 117 .…”

Section: Classes Of Drugs Interacting With Grapefruit Juicementioning

confidence: 78%

Grapefruit‐Drug Interactions: Can Interactions With Drugs Be Avoided?

Mertens‐Talcott

Zadezensky

Castro

et al. 2006

The Journal of Clinical Pharma

106

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Grapefruit is rich in flavonoids, which have been demonstrated to have a preventive influence on many chronic diseases, such as cancer and cardiovascular disease. However, since the early 1990s, the potential health benefits of grapefruit have been overshadowed by the possible risk of interactions between drugs and grapefruit and grapefruit juice. Several drugs interacting with grapefruit are known in different drug classes, such as HMG-CoA reductase inhibitors, calcium antagonists, and immunosuppressives. Currently known mechanisms of interaction include the inhibition of cytochrome P450 as a major mechanism, but potential interactions with P-glycoprotein and organic anion transporters have also been reported. This review is designed to provide a comprehensive summary of underlying mechanisms of interaction and human clinical trials performed in the area of grapefruit drug interactions and to point out possible replacements for drugs with a high potential for interactions.

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Section: Classes Of Drugs Interacting With Grapefruit Juicementioning

confidence: 78%

Grapefruit‐Drug Interactions: Can Interactions With Drugs Be Avoided?

Mertens‐Talcott

Zadezensky

Castro

et al. 2006

The Journal of Clinical Pharma

106

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“…These molecules exhibit various biological activities such as antibacterial (Schinkovitz et al, 2003; Stavri et al, 2003; Céspedes et al, 2006), antioxidant (Bajerova et al, 2014), anti-inflammatory (Witaicenis et al, 2013), rodenticidal (Lotfi et al, 1996), termiticidal (Adfa et al, 2010, 2011), and other activities (Stahmann et al, 1941; Murray, 1989; Runkel et al, 1996; Song et al, 2014). In addition, the role(s) of coumarins in plants have also been reported.…”

Section: Introductionmentioning

confidence: 99%

2-Oxoglutarate-dependent dioxygenases in the biosynthesis of simple coumarins

Shimizu

2014

Front. Plant Sci.

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Coumarins are natural plant products that have been the subject of extensive phytochemical and pharmacological research studies in the past few decades. The core structure of coumarins is derived from the respective cinnamates via ortho-hydroxylation of the aromatic ring, trans/cis isomerization, and lactonization. Various substitution patterns of coumarins have been reported, whereas the biosynthesis of coumarins remains elusive. Ortho-hydroxylation is a key step in simple coumarin biosynthesis as a branch point from the lignin biosynthetic pathway. 2-Oxoglutarate-dependent dioxygenases (2OGDs) from plants convert cinnamate derivatives into simple coumarins through the process of ortho-hydroxylation. This review describes the 2OGDs involved in coumarin biosynthesis and their substrate specificities.

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“…Употребление грейпфрутового сока за 2 ч до приема фексофенадина снижало среднюю AUC на 38%, а за 4 ч -не влияло на абсорб- цию препарата [13,16]. Грейпфрут взаимодействует с варфарином, ингибируя активность ферментов цитохрома Р450, участвующих в его метаболизме [17]. Варфарин представляет собой рацемическую смесь двух активных энантиомеров R-и S-форм [18].…”

Section: грейпфрутовый сокunclassified

Potential clinically significant drug interactions of drugs with fruit and berry juices

Переверзев¹,

Остроумова²

2021

CPT

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Any drug can potentially cause adverse drug reactions (ADRs), including serious and fatal. Some of them are caused by interactions with food, in particular, fruit and berry juices. Juices have a complex chemical composition and each of the chemicals can interact with drugs. Grapefruit juice is one of the most popular and well-studed in terms of potential drug interactions juices. Grapefruit juice is an inhibitor of CYP3A enzymes in the intestine involved in the presystemic metabolism of drug substrates. Therefore, it can increase their absorption. Apple juice at a concentration of 5% significantly reduces the activity of OATP, but not the activity of P-glycoprotein, which, for example, leads to a decrease in AUC and Cmax of fexofenadine to 30- 40% relative to the concentration of fexofenadine in patients drinking only water. Taking 200 ml of grape juice can reduce the concentration of phenacetin in blood plasma and increase the ratio of AUC of paracetamol to phenacetin due to the induction of CYP1A2 activity by grape juice flavonoids or by reducing the rate of absorption of phenacetin. To prevent ADRs, it is recommended to take drugs with water and and not consume simultaneously juices that are known to interact with drugs.

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Metabolic and analytical interactions of grapefruit juice and 1,2-benzopyrone (coumarin) in man

Abstract: Only grapefruit juice given at high doses (1 L) retards the appearance of the main metabolite of coumarin administered orally but increases its recovery. Due to scopoletin formed from the grapefruit juice, experiments especially with coumarin are strongly affected.

Cited by 20 publications

References 13 publications

Grapefruit‐Drug Interactions: Can Interactions With Drugs Be Avoided?

Grapefruit‐Drug Interactions: Can Interactions With Drugs Be Avoided?

2-Oxoglutarate-dependent dioxygenases in the biosynthesis of simple coumarins

Potential clinically significant drug interactions of drugs with fruit and berry juices

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