Grapefruit juice–nifedipine interaction: possible involvement of several mechanisms

  title={Grapefruit juice–nifedipine interaction: possible involvement of several mechanisms},
  author={Pascal Odou and Nicolas Ferrari and Christine Barth{\'e}l{\'e}my and Serge Brique and Michel Lhermitte and A Vincent and Christian Libersa and Hugues Robert},
  journal={Journal of Clinical Pharmacy and Therapeutics},
Objective:  To develop a model based on mean residence time for better understanding the effect of grapefruit juice on the metabolism of nifedipine (NIF). 

Grapefruit-Drug Interactions

The aim of this review is to outline the mechanisms of grapefruit-drug interactions and present a comprehensive summary of those agents affected and whether they are likely to be of clinical relevance.

The effect of grapefruit juice on drug disposition

In vitro effects of GFJ and its constituents on the activity of CYP enzymes, organic anion-transporting polypeptides, P-glycoprotein, esterases and sulfotransferases are reviewed.

The grapefruit: an old wine in a new glass? Metabolic and cardiovascular perspectives

It has recently emerged that grapefruit, by virtue of its rich flavonoid content, is beneficial in the management of degenerative diseases such as diabetes and cardiovascular disorders.

The grapefruit: an old wine in a new glass? Metabolic and cardiovascular perspectives

  • P. Owira
  • Medicine
    Cardiovascular Journal of Africa
  • 2012
It has recently emerged that grapefruit, by virtue of its rich flavonoid content, is beneficial in the management of degenerative diseases such as diabetes and cardiovascular disorders.

In vitro dissolution of sustained-release Nifedipine brands marketed in the Kumasi Metropolis

A thesis submitted to the School of Graduate Studies in partial fulfilment of the requirement for the Master of Philosophy, 2013

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

To determine how closely physiologically based pharmacokinetic models can predict oral bioavailability using a priori knowledge of drug‐specific properties, and to examine the influence of the biopharmaceutics classification system class on the simulation success.

Utilizing in vitro and PBPK tools to link ADME characteristics to plasma profiles: case example nifedipine immediate release formulation.

Physiologically based pharmacokinetic (PBPK) modeling was used to simulate pharmacokinetics of a nifedipine immediate release formulation following concomitant grapefruit juice ingestion, and a link between the dissolution characteristics of the formulation and its in vivo performance could be established.

Assessment of a Candidate Marker Constituent Predictive of a Dietary Substance–Drug Interaction: Case Study with Grapefruit Juice and CYP3A4 Drug Substrates

Results suggest that DHB could be used to predict the CYP3A4-mediated effect of GFJ, and this time- and cost-effective IVIVE approach could be applied to other dietary substance–drug interactions to help prioritize new and existing drugs for more advanced (dynamic) modeling and simulation and clinical assessment.

Grapefruit juice and licorice increase cortisol availability in patients with Addison's disease.

Licorice and in particular GFJ increased cortisol available to tissues in the hours following oral CA administration, and both patients and physicians should be aware of these interactions.

Spectroscopic investigation on the food components-drug interaction: the influence of flavonoids on the affinity of nifedipine to human serum albumin.

  • Xin WangYang Liu Xin Wang
  • Chemistry, Biology
    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association
  • 2015



Quercetin, an in vitro inhibitor of CYP3A, does not contribute to the interaction between nifedipine and grapefruit juice.

Oral doses of quercetin, similar to those possible from the ingestion of other fruits such as strawberries, do not produce in vivo inhibition of CYP3A mediated metabolism of nifedipine.

Influence of grapefruit juice on the pharmacokinetics of a slow release nifedipine formulation.

The data contradict the assumption of a selective inhibition of only one cytochrome P450 subfamily and the observed effect could be clinically significant, especially if other factors affecting the elimination of 1 occur.

Grapefruit juice-drug interactions.

In vitro findings support the flavonoid, naringin, or the furanocoumarin, 6',7'-dihydroxybergamottin, as being active ingredients, but a recent investigation indicated that neither of these substances made a major contribution to grapefruit juice-drug interactions in humans.

Factors affecting the absolute bioavailability of nifedipine.

The AUC of nifedipine after intravenous administration was significantly higher in South Asian subjects than in Caucasians and this was due to a lower systemic clearance in the South Asians which was 50% of that in the Caucasians.

The Nifedipine Gastrointestinal Therapeutic System (GITS)

The majority of clinical trials with the nifedipine GITS have assessed its efficacy in patients with mild-to-moderate essential hypertension, and have found it to be at least equivalent to other dosage forms of the drug.


Results indicate that, in addition to hepatic extraction, substantial first‐pass elimination of nifedipine occurs within the wall of the small intestine but not the colon of the rat.