ArticleAntimicrobial agents and chemotherapy2009
Model-based approach to characterize efavirenz autoinduction and concurrent enzyme induction with carbamazepine.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 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
27 citing papers in PubMed, 58 citations in OpenAlex.
- A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe.CPT: pharmacometrics & systems pharmacology · 2025Trial
- Population Pharmacokinetics, Safety and Tolerability of Extended-Release Bupropion and Its Three Metabolites in Chinese Healthy Volunteers.European journal of drug metabolism and pharmacokinetics · 2019Trial
- Vatalanib population pharmacokinetics in patients with myelodysplastic syndrome: CALGB 10105 (Alliance).British journal of clinical pharmacology · 2014Trial
- Population pharmacogenetic-based pharmacokinetic modeling of efavirenz, 7-hydroxy- and 8-hydroxyefavirenz.Journal of clinical pharmacology · 2014Trial
- CYP2B6 pharmacogenetics-based in vitro-in vivo extrapolation of efavirenz clearance by physiologically based pharmacokinetic modeling.Drug metabolism and disposition: the biological fate of chemicals · 2013Trial
- Pharmacokinetic modelling of efavirenz, atazanavir, lamivudine and tenofovir in the female genital tract of HIV-infected pre-menopausal women.Clinical pharmacokinetics · 2012Trial
- Induction of CYP2C19 and CYP3A activity following repeated administration of efavirenz in healthy volunteers.Clinical pharmacology and therapeutics · 2012Trial
- No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.Antimicrobial agents and chemotherapy · 2010Trial
- Effects of four different meal types on the population pharmacokinetics of single-dose rifapentine in healthy male volunteers.Antimicrobial agents and chemotherapy · 2010Trial
- Pharmacokinetics of darunavir at 900 milligrams and ritonavir at 100 milligrams once daily when coadministered with efavirenz at 600 milligrams once daily in healthy volunteers.Antimicrobial agents and chemotherapy · 2010Trial
- Article
- Population pharmacokinetics of efavirenz in HIV and TB/HIV coinfected children: the significance of genotype-guided dosing.The Journal of antimicrobial chemotherapy · 2019Article
- The Utility of Efavirenz-based Prophylaxis Against HIV Infection. A Systems Pharmacological Analysis.Frontiers in pharmacology · 2019Article
- Article
- Prediction of plasma efavirenz concentrations among HIV-positive patients taking efavirenz-containing combination antiretroviral therapy.Scientific reports · 2017Article
- MicroRNA hsa-miR-25-3p suppresses the expression and drug induction of CYP2B6 in human hepatocytes.Biochemical pharmacology · 2016Article
- Towards a Best Practice Approach in PBPK Modeling: Case Example of Developing a Unified Efavirenz Model Accounting for Induction of CYPs 3A4 and 2B6.CPT: pharmacometrics & systems pharmacology · 2016Article
- Once-Daily, Single-Tablet Regimens For the Treatment of HIV-1 Infection.P & T : a peer-reviewed journal for formulary management · 2015Article
- Impact of CYP polymorphisms, ethnicity and sex differences in metabolism on dosing strategies: the case of efavirenz.European journal of clinical pharmacology · 2014Review
- Efavirenz-mediated induction of omeprazole metabolism is CYP2C19 genotype dependent.The pharmacogenomics journal · 2014Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Characterization of the time course and magnitude of enzyme induction due to multiple inducers is important for interpretation of clinical data from drug-drug interaction studies. A population interaction model was developed to quantify efavirenz autoinduction and further induction with concurrent carbamazepine coadministration. Efavirenz concentration data in the absence and presence of carbamazepine following single- and multiple-dose oral administrations in healthy subjects were used for model development. The proposed model was able to describe the time-dependent efavirenz autoinduction and the further induction with carbamazepine when the agents were combined. The estimated population averages of efavirenz oral clearance were 5.5, 9.4, 14.4, and 16.7 liters/h on days 1, 14, and 35 and at steady state for the interaction, respectively, for efavirenz monotherapy for 2 weeks followed by the coadministration of carbamazepine for 3 weeks. The estimated times to 50% of the steady state for efavirenz autoinduction and for the induction resulting from the concurrent administration of efavirenz and carbamazepine were similar (around 10 to 12 days). With this model-based analysis, efavirenz exposures can be projected prior to and at the steady state of induction, allowing a better understanding of the time course and magnitude of enzyme induction.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.