Trial reportBritish journal of clinical pharmacology2015
Pharmacokinetic interaction between the CYP3A4 inhibitor ketoconazole and the hormone drospirenone in combination with ethinylestradiol or estradiol.
Trial report in British journal of clinical pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
16 citing papers in PubMed, 33 citations in OpenAlex.
- Bioequivalence study of low dose drospirenone/ethinyl estradiol 3 mg/0.03 mg film tablets under fasting conditions in Turkish healthy female subjects.Pharmacology research & perspectives · 2024Trial
- Evaluation of the food effect on a drospirenone only contraceptive containing 4 mg administered with and without high-fat breakfast in a randomised trial.BMC women's health · 2022Trial
- Factors Associated With Serum Estradiol Levels Among Postmenopausal Women Using Hormone Therapy.Obstetrics and gynecology · 2020Trial
- Multicenter, phase III trials on the contraceptive efficacy, tolerability and safety of a new drospirenone-only pill.Acta obstetricia et gynecologica Scandinavica · 2019Trial
- Pharmacokinetic interaction between the CYP3A4 inhibitor ketoconazole and the hormone drospirenone in combination with ethinylestradiol or estradiol.British journal of clinical pharmacology · 2015Trial
- Effects of Ensitrelvir on the Pharmacokinetics of Combined Oral Contraceptives (Ethinyl Estradiol/Drospirenone) in Healthy Adult Women: A Phase 1 Fixed-Sequence, Multiple-Dose, Drug-Drug Interaction Study.Clinical drug investigation · 2026Article
- A detailed review of pharmacokinetics/pharmacodynamics of progestogens in oral contraception.Frontiers in endocrinology · 2026Review
- Investigating Sulfotransferase Mediated Drug Interactions of Ethinylestradiol using a Physiologically Based Pharmacokinetic Model.The AAPS journal · 2025Article
- Physiologically-based pharmacokinetic modeling of prominent oral contraceptive agents and applications in drug-drug interactions.CPT: pharmacometrics & systems pharmacology · 2024Article
- Combined Oral Contraceptives As Victims of Drug Interactions.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception.Pharmacology & therapeutics · 2021Review
- Structural Perspectives of the CYP3A Family and Their Small Molecule Modulators in Drug Metabolism.Liver research (Beijing, China) · 2019Article
- Risk-Benefit Assessment of Ethinylestradiol Using a Physiologically Based Pharmacokinetic Modeling Approach.Clinical pharmacology and therapeutics · 2018Article
- Role of CYP3A in Oral Contraceptives Clearance.Clinical and translational science · 2018Review
- Pharmacokinetics of antifungal drugs: practical implications for optimized treatment of patients.Infection · 2017Review
- Pharmacological and metabolic effects of drospirenone as a progestin-only pill compared to combined formulations with estrogen.Women's health (London, England)Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsThe present study was conducted to investigate the influence of the strong CYP3A4 inhibitor ketoconazole (KTZ) on the pharmacokinetics of drospirenone (DRSP) administered in combination with ethinylestradiol (EE) or estradiol (E2).
methodsThis was a randomized, multicentre, open label, one way crossover, fixed sequence study with two parallel treatment arms. A group sequential design allowed terminating the study for futility after first study cohort. About 50 healthy young women were randomized 1 : 1 to 'DRSP/EE' or 'DRSP/E2'. Subjects in the 'DRSP/EE' group received DRSP 3 mg/EE 0.02 mg (YAZ®, Bayer) once daily for 21 to 28 days followed by DRSP 3 mg/EE 0.02 mg once daily plus KTZ 200 mg twice daily for 10 days. Subjects in the 'DRSP/E2' group received DRSP 3 mg/E2 1.5 mg (research combination) once daily for 21 to 28 days followed by DRSP 3 mg/E2 1.5 mg once daily plus KTZ 200 mg twice daily for 10 days.
resultsOral co-administration of DRSP/EE or DRSP/E2 and KTZ resulted in an increase in DRSP exposure (AUC(0,24 h)) in both treatment groups: DRSP/EE group: 2.68-fold DRSP increase (90% CI 2.44, 2.95); DRSP/E2 group: 2.30-fold DRSP increase (90% CI 2.08, 2.54). EE and estrone (metabolite of E2) exposures were increased ~1.4-fold whereas E2 exposure was largely unaffected by KTZ co-administration.
conclusionsA moderate pharmacokinetic drug-drug interaction between DRSP and KTZ was demonstrated in this study. No relevant changes of medical concern were detected in the safety data collected in this study.
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