ArticleEuropean journal of clinical pharmacology2010
Proposal of a new limited sampling strategy to predict CYP3A activity using a partial AUC of midazolam.
Article in European journal of clinical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed.
- Effect of Clarithromycin, a Strong CYP3A and P-glycoprotein Inhibitor, on the Pharmacokinetics of Edoxaban in Healthy Volunteers and the Evaluation of the Drug Interaction with Other Oral Factor Xa Inhibitors by a Microdose Cocktail Approach.Cardiovascular drugs and therapy · 2024Trial
- Time Course of the Interaction Between Oral Short-Term Ritonavir Therapy with Three Factor Xa Inhibitors and the Activity of CYP2D6, CYP2C19, and CYP3A4 in Healthy Volunteers.Clinical pharmacokinetics · 2024Trial
- Evaluation of Hydroxychloroquine as a Perpetrator on Cytochrome P450 (CYP) 3A and CYP2D6 Activity with Microdosed Probe Drugs in Healthy Volunteers.European journal of drug metabolism and pharmacokinetics · 2024Trial
- Perpetrator Characteristics of Azole Antifungal Drugs on Three Oral Factor Xa Inhibitors Administered as a Microdosed Cocktail.Clinical pharmacokinetics · 2022Trial
- Minor contribution of cytochrome P450 3A activity on fentanyl exposure in palliative care cancer patients.Scientific reports · 2019Trial
- Systemic exposure of topical erythromycin in comparison to oral administration and the effect on cytochrome P450 3A4 activity.British journal of clinical pharmacology · 2014Trial
- Concentration effect relationship of CYP3A inhibition by ritonavir in humans.European journal of clinical pharmacology · 2013Trial
- Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity.European journal of clinical pharmacology · 2013Trial
- Influence of a Short Course of Ritonavir Used as Booster in Antiviral Therapies Against SARS-CoV-2 on the Exposure of Atorvastatin and Rosuvastatin.Cardiovascular drugs and therapy · 2025Article
- Effect of the frequently used antiepileptic drugs carbamazepine, gabapentin, and pregabalin on the pharmacokinetics of edoxaban and other oral factor xa inhibitors in healthy volunteers.Frontiers in pharmacology · 2025Article
- Article
- Limitations of fexofenadine limited sampling strategy using plasma concentrations and partial area under the concentration-time curve to estimate transporter activity in healthy adults.International journal of clinical pharmacology and therapeutics · 2023Article
- Evaluation of the drug-drug interaction potential of the novel hepatitis B and D virus entry inhibitor bulevirtide at OATP1B in healthy volunteers.Frontiers in pharmacology · 2023Article
- Physiologically-based pharmacokinetic modeling to predict CYP3A4-mediated drug-drug interactions of finerenone.CPT: pharmacometrics & systems pharmacology · 2022Article
- Validation of a 3-h Sampling Interval to Assess Variability in Cytochrome P450 3A Phenotype and the Impact of Induction and Mechanism-Based Inhibition Using Midazolam as a Probe Substrate.Frontiers in pharmacology · 2019Article
- Rivaroxaban and macitentan can be coadministered without dose adjustment but the combination of rivaroxaban and St John's wort should be avoided.British journal of clinical pharmacology · 2018Article
- Towards better dose individualisation: metabolic phenotyping to predict cabazitaxel pharmacokinetics in men with prostate cancer.British journal of cancer · 2017Article
- Physiologically Based Modelling of Darunavir/Ritonavir Pharmacokinetics During Pregnancy.Clinical pharmacokinetics · 2016Article
- Limited sampling strategy of partial area under the concentration-time curves to estimate midazolam systemic clearance for cytochrome P450 3A phenotyping.Therapeutic drug monitoring · 2015Article
- Evaluation of limited sampling models for prediction of oral midazolam AUC for CYP3A phenotyping and drug interaction studies.European journal of clinical pharmacology · 2013Article
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeMidazolam metabolic clearance to 1'-hydroxymidazolam is an accurate measure of CYP3A activity which requires extensive plasma and urine sampling. The objective of this study was to find a new limited sampling strategy (LSS) to predict midazolam metabolic clearance to 1'-hydroxymidazolam and subsequently CYP3A activity in an easy and reliable way, reducing costs and labour.
methodsThe development of this LSS is based on data from an in vivo drug-drug interaction study carried out in our clinical research unit. Various partial AUCs of midazolam were calculated and correlated with metabolic clearance of midazolam to 1'-hydroxymidazolam by non-linear regression. The correlation with highest r (2) values was chosen to predict the midazolam metabolic clearance. Statistical significance of this method was verified by calculating the 95% confidence interval of the differences (%) between predicted and measured metabolic clearance of midazolam to 1'-hydroxymidazolam.
resultsThe midazolam partial AUC from 2 to 4 h after oral administration correlated best with metabolic clearance of midazolam to 1'-hydroxymidazolam with r (2) = 0.9816. This partial AUC comprised four midazolam concentrations at 2, 2.5, 3 and 4 h after oral administration of a midazolam solution. The 95% confidence interval of the differences between predicted metabolic clearance and measured metabolic clearance of midazolam to 1'-hydroxymidazolam was -0.97 to +13.2.
conclusionThe determination of the partial AUC using four plasma samples from 2 to 4 h after oral administration of a midazolam solution is proposed to be an easy and reliable CYP3A phenotyping measure which of course needs to be validated in prospective clinical trials.
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