Pharmacokinetics of ethinyl estradiol and mestranol

Goldzieher, Joseph W.; Brody, Steven A.

doi:10.1016/0002-9378(90)90550-q

Cited by 63 publications

(28 citation statements)

References 16 publications

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“…For statistical testing among different treatment groups, one-way analysis of variance test was performed for multiple comparisons followed by posthoc Dunnett's test. (Goldzieher and Brody, 1990;Kuhl, 1990). In studying the effects of estradiol and progesterone on the expression of major P450s using human hepatocytes, we first determined elimination rates of estradiol and progesterone in the hepatocyte cultures.…”

Section: Methodsmentioning

confidence: 99%

Isoform-Specific Regulation of Cytochromes P450 Expression by Estradiol and Progesterone

2012

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Section: Methodsmentioning

confidence: 99%

Isoform-Specific Regulation of Cytochromes P450 Expression by Estradiol and Progesterone

2012

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“…However, poor compliance with this treatment is a common problem and can result in greatly impaired efficacy. 5 There are additional problems with COCs, such as the low bioavailability of EE (38%-48%) after oral administration, 6 rapid and large fluctuations in serum hormone concentrations, 7 and large intra-and interindividual pharmacokinetic variations. 8 Transdermal delivery of contraceptive hormones, in contrast, offers several advantages over oral administration, including effective absorption and the provision of relatively constant serum concentrations.…”

Section: Introductionmentioning

confidence: 99%

Effect of a Low-Dose Contraceptive Patch on Efficacy, Bleeding Pattern, and Safety: A 1-Year, Multicenter, Open-Label, Uncontrolled Study

et al. 2014

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This Phase III, uncontrolled, open-label, multicenter study was conducted to investigate the contraceptive efficacy, bleeding pattern, and cycle control of a novel once-a-week contraceptive patch, delivering low-dose ethinyl estradiol (EE) and gestodene (GSD) at the same systemic exposure seen after oral administration of a combined oral contraceptive containing 0.02 mg EE/0.06 mg GSD. Participants were women aged 18 to 35 years, all of whom received the EE/GSD patch for 13 cycles each of 21 treatment days (one patch per week for 3 weeks) followed by a 7-day, patch-free interval. The primary efficacy variable was the occurrence of unintended pregnancies during the study period as assessed by life table analysis and the Pearl Index. Secondary efficacy variables were days with bleeding during four 90-day reference periods and during 1 treatment year, bleeding pattern, and cycle control. The Kaplan-Meier probability of contraceptive protection after 364 treatment days was 98.8% and the adjusted Pearl Index was 0.81. The percentage of participants with intracyclic bleeding/spotting decreased over time, from 11.4% to 6.8% in cycles 1 and 12, respectively. Almost all participants (range: 90.8%-97.6%) experienced withdrawal bleeding across the study period. Compliance was very high (mean: 97.9%; median: 100%). The most frequent adverse events were headache (9.5%) and application site reaction (8.5%); no clinically significant safety concerns were observed. Results suggest the EE/GSD patch is highly effective in preventing pregnancy. Menstrual bleeding pattern was favorable and within the ranges expected of a healthy female population. The patch was well tolerated and treatment compliance was high.

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“…Two studies have provided conflicting evidence on the bioequivalence of 50 µg EE and mestranol. 109,110 The CEU suggests an alternative regimen using two low-dose COCs providing a total daily dose of 50-60 µg EE (e.g. Loestrin 20 ® plus Loestrin 30 ® , or Marvelon ® plus Mercilon ® , or two Microgynon 30 ® ).…”

Section: Women Using Even Short Courses Of Rifampicin (For Prophylaximentioning

confidence: 99%

FFPRHC Guidance (April 2005) Drug interactions with hormonal contraception

2005

j fam plann reprod health care

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This Guidance provides information for clinicians and women using hormonal contraception applicable when concurrent medications are prescribed. A key to the grades of recommendations, based on levels of evidence, is given at the end of this document. Details of the methods used by the Clinical Effectiveness Unit (CEU) in developing this Guidance and evidence tables summarising the research basis of the recommendations are available on the Faculty website (www.ffprhc.org.uk). Abbreviations (in alphabetical order) used include:

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Pharmacokinetics of ethinyl estradiol and mestranol

Cited by 63 publications

References 16 publications

Isoform-Specific Regulation of Cytochromes P450 Expression by Estradiol and Progesterone

Isoform-Specific Regulation of Cytochromes P450 Expression by Estradiol and Progesterone

Effect of a Low-Dose Contraceptive Patch on Efficacy, Bleeding Pattern, and Safety: A 1-Year, Multicenter, Open-Label, Uncontrolled Study

FFPRHC Guidance (April 2005) Drug interactions with hormonal contraception

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