Oral Pharmacokinetics of Felodipine in Mexican Healthy Volunteers: Evidence for Interethnic Differences

Inter‐ethnic variability in pharmacokinetics (PK) has been attributed to several factors ranging from genetic to environmental. It is not clear how current teaching in higher education (HE) reflects what published literature suggests on this subject. This study aims to gain insights into current knowledge about inter‐ethnic differences in PK based on reports from published literature and current teaching practices in HE. A systematic literature search was conducted on PubMed and Scopus to identify suitable literature to be reviewed. Insights into inter‐ethnic differences in PK teaching among educators in HE and industry were determined using a questionnaire. Thirty‐one percent of the studies reviewed reported inter‐ethnic differences in PK, of these, 37% of authors suggested genetic polymorphism as possible explanation for the inter‐ethnic differences observed. Other factors authors proposed included diet and weight differences between ethnicities. Most respondents (80%) who taught inter‐ethnic difference in PK attributed inter‐ethnic differences to genetic polymorphism. While genetic polymorphism is one source of variability in PK, the teaching of genetic polymorphism is better associated with interindividual variabilities rather than inter‐ethnic differences in PK as there are no genes with PK implications specific to any one ethnic group. Nongenetic factors such as diet, weight, and environmental factors, should be highlighted as potential sources of interindividual variation in the PK of drugs.

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Inter‐ethnic differences in pharmacokinetics—is there more that unites than divides?

Olafuyi

Parekh

Wright

et al. 2021

Pharmacology Res & Perspec

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Oral Ciprofloxacin Pharmacokinetics in Healthy Mexican Volunteers and Other Populations: Is There Interethnic Variability?

Tolentino-Hernández

Cruz-Antonio

Pèrez‐Urizar

et al. 2020

Archives of Medical Research

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A Physiologically Based Pharmacokinetic and Pharmacodynamic Model of the CYP3A4 Substrate Felodipine for Drug–Drug Interaction Modeling

et al. 2022

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The antihypertensive felodipine is a calcium channel blocker of the dihydropyridine type, and its pharmacodynamic effect directly correlates with its plasma concentration. As a sensitive substrate of cytochrome P450 (CYP) 3A4 with high first-pass metabolism, felodipine shows low oral bioavailability and is susceptible to drug–drug interactions (DDIs) with CYP3A4 perpetrators. This study aimed to develop a physiologically based pharmacokinetic/pharmacodynamic (PBPK/PD) parent–metabolite model of felodipine and its metabolite dehydrofelodipine for DDI predictions. The model was developed in PK-Sim® and MoBi® using 49 clinical studies (94 plasma concentration–time profiles in total) that investigated different doses (1–40 mg) of the intravenous and oral administration of felodipine. The final model describes the metabolism of felodipine to dehydrofelodipine by CYP3A4, sufficiently capturing the first-pass metabolism and the subsequent metabolism of dehydrofelodipine by CYP3A4. Diastolic blood pressure and heart rate PD models were included, using an Emax function to describe the felodipine concentration–effect relationship. The model was tested in DDI predictions with itraconazole, erythromycin, carbamazepine, and phenytoin as CYP3A4 perpetrators, with all predicted DDI AUClast and Cmax ratios within two-fold of the observed values. The model will be freely available in the Open Systems Pharmacology model repository and can be applied in DDI predictions as a CYP3A4 victim drug.

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Oral Pharmacokinetics of Felodipine in Mexican Healthy Volunteers: Evidence for Interethnic Differences

Cited by 4 publications

References 20 publications

Inter‐ethnic differences in pharmacokinetics—is there more that unites than divides?

Inter‐ethnic differences in pharmacokinetics—is there more that unites than divides?

Oral Ciprofloxacin Pharmacokinetics in Healthy Mexican Volunteers and Other Populations: Is There Interethnic Variability?

A Physiologically Based Pharmacokinetic and Pharmacodynamic Model of the CYP3A4 Substrate Felodipine for Drug–Drug Interaction Modeling

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