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An Ethinyl Estradiol-Levonorgestrel Containing Oral Contraceptive Does Not Alter Cytochrome P4502C9 In Vivo Activity

Ganesh Cherala, Jacob Pearson, Cheryl Maslen and Alison Edelman
Drug Metabolism and Disposition March 2014, 42 (3) 323-325; DOI: https://doi.org/10.1124/dmd.113.054346
Ganesh Cherala
Department of Pharmacy Practice, College of Pharmacy, Oregon State University/Oregon Health & Science University, Portland, Oregon (G.C., J.P.); and Departments of Molecular and Medical Genetics (C.M.) and Obstetrics and Gynecology (G.C., A.E.), Oregon Health & Science University, Portland, Oregon
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Jacob Pearson
Department of Pharmacy Practice, College of Pharmacy, Oregon State University/Oregon Health & Science University, Portland, Oregon (G.C., J.P.); and Departments of Molecular and Medical Genetics (C.M.) and Obstetrics and Gynecology (G.C., A.E.), Oregon Health & Science University, Portland, Oregon
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Cheryl Maslen
Department of Pharmacy Practice, College of Pharmacy, Oregon State University/Oregon Health & Science University, Portland, Oregon (G.C., J.P.); and Departments of Molecular and Medical Genetics (C.M.) and Obstetrics and Gynecology (G.C., A.E.), Oregon Health & Science University, Portland, Oregon
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Alison Edelman
Department of Pharmacy Practice, College of Pharmacy, Oregon State University/Oregon Health & Science University, Portland, Oregon (G.C., J.P.); and Departments of Molecular and Medical Genetics (C.M.) and Obstetrics and Gynecology (G.C., A.E.), Oregon Health & Science University, Portland, Oregon
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Abstract

Oral contraceptives have been in wide use for more than 50 years. Levonorgestrel, a commonly employed progestin component of combined oral contraceptives, was implicated in drug–drug interactions mediated via CYP2C9. Although in vitro studies refuted this interaction, there are no confirmatory in vivo studies. In the current study, we examined the phenotypic status of CYP2C9 using low-dose (125 mg) tolbutamide before and after oral contraceptive use in reproductive age women. Blood was collected 24 hours after the tolbutamide oral dose was administered, plasma was isolated, and tolbutamide concentration (C24) was measured using liquid chromatography–mass spectrometry. The natural logarithm of tolbutamide C24, a metric for CYP2C9 phenotype, was found to be equivalent (within 80%–125% equivalency boundaries) before and after oral contraceptive use. In conclusion, levonorgestrel-containing oral contraceptives, the most commonly used form of oral contraception, do not affect the status of the CYP2C9 enzyme. This suggests that it is safe to coadminister levonorgestrel-containing oral contraceptives and CYP2C9 substrates, which include a wide array of drugs.

Footnotes

    • Received August 19, 2013.
    • Accepted December 24, 2013.
  • This research was supported by the National Institutes of Health Eunice Kennedy Shriver National Institute of Child Health and Human Development [Grants R01HD06158201 and 2K12HD043488]; the Oregon Health & Science University Oregon Clinical & Translational Research Institute and the National Institutes of Health National Center for Research Resources [Grant 1UL1RR024120]; and the Bioanalytical Shared Resource/Pharmacokinetics Core at Oregon Health & Science University.

  • dx.doi.org/10.1124/dmd.113.054346.

  • Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 42 (3)
Drug Metabolism and Disposition
Vol. 42, Issue 3
1 Mar 2014
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Rapid CommunicationShort Communication

Combined Oral Contraceptives—CYP2C9 Activity

Ganesh Cherala, Jacob Pearson, Cheryl Maslen and Alison Edelman
Drug Metabolism and Disposition March 1, 2014, 42 (3) 323-325; DOI: https://doi.org/10.1124/dmd.113.054346

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Rapid CommunicationShort Communication

Combined Oral Contraceptives—CYP2C9 Activity

Ganesh Cherala, Jacob Pearson, Cheryl Maslen and Alison Edelman
Drug Metabolism and Disposition March 1, 2014, 42 (3) 323-325; DOI: https://doi.org/10.1124/dmd.113.054346
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