2010•Chinese Journal of New Drugs and Clinical RemediesRequires access

Interaction between grapefruit juice and calcium channel blockers

HU Fana

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Abstract

The grapefruit juice(Citrus paradisi)is a major component of fruit juice drinks.Calcium channel blockers(CCB)are widely used in clinical treatment of hypertension and cardio-cerebrovascular diseases.Therefore,when both of them are in taken at the same time,grapefruit juice can effect absorption and metabolism of CCB,change the pharmacokinetic parameters of CCB,and result in adverse reactions.The grapefruit juice can inhibit the metabolic enzyme cytochrome P450(CYP3A4)and the transportation of P-glycoprotein(P-gp).However,most CCB are substrates of CYP3A4 and P-gp,which may be the mechanisms of the grapefruit juice and CCB relations.Studies on the food-drug interaction between grapefruit juice and CCB in recent years are reviewed in this paper.

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What this paper is about

The grapefruit juice(Citrus paradisi)is a major component of fruit juice drinks.Calcium channel blockers(CCB)are widely used in clinical treatment of hypertension and cardio-cerebrovascular diseases.Therefore,when both of them are in taken at the same time,grapefruit juice can effect absorption and metabolism of CCB,change the pharmacokinetic parameters of CCB,and result in adverse reactions.The grapefruit juice can inhibit the metabolic enzyme cytochrome P450(CYP3A4)and the transportation of P-glycoprotein(P-gp).However,most CCB are substrates of CYP3A4 and P-gp,which may be the mechanisms of the grapefruit juice and CCB relations.Studies on the food-drug interaction between grapefruit juice and CCB in recent years are reviewed in this paper.

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Available abstract

The grapefruit juice(Citrus paradisi)is a major component of fruit juice drinks.Calcium channel blockers(CCB)are widely used in clinical treatment of hypertension and cardio-cerebrovascular diseases.Therefore,when both of them are in taken at the same time,grapefruit juice can effect absorption and metabolism of CCB,change the pharmacokinetic parameters of CCB,and result in adverse reactions.The grapefruit juice can inhibit the metabolic enzyme cytochrome P450(CYP3A4)and the transportation of P-glycoprotein(P-gp).However,most CCB are substrates of CYP3A4 and P-gp,which may be the mechanisms of the grapefruit juice and CCB relations.Studies on the food-drug interaction between grapefruit juice and CCB in recent years are reviewed in this paper.

Key concepts: Grapefruit juice, Citrus paradisi, CYP3A4, Chemistry, Pharmacology, Pharmacokinetics, Calcium channel, Pharmacokinetic interaction

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