Comparative studies of the ethynyl estrogens used in oral contraceptives

Goldzieher, Joseph W.; Maqueo, M; Chenault, C. Brandon; Woutersz, Theodore B.

doi:10.1016/0002-9378(75)90060-5

Cited by 51 publications

(12 citation statements)

References 8 publications

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“…EE alone at 50 μg/day does not consistently inhibit ovulation but the combination of EE at doses of 20–40 μg/day and low doses of progestins does inhibit ovulation. 31 Given that doses of EE of 20 μg/day combined with progestins inhibit ovulation and are contraceptive, the levels of EE seen in this study using patch delivered 20 μg/day EE with LPV/r were adequate to inhibit ovulation. The substantial decrease in progesterone levels observed in all the subjects studied indicates suppression of ovulation occurred in all patients including the one patient who complained of breakthrough bleeding.…”

Section: Discussionmentioning

confidence: 73%

Contraceptive Efficacy of Oral and Transdermal Hormones When Co-Administered With Protease Inhibitors in HIV-1-Infected Women: Pharmacokinetic Results of ACTG Trial A5188

Vogler¹,

Patterson²,

Kamemoto³

et al. 2010

JAIDS Journal of Acquired Immune Deficiency Syndromes

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Background Pharmacokinetic (PK) interactions between lopinavir/ritonavir (LPV/r) and transdermally delivered ethinyl estradiol (EE) and norelgestromin (NGMN) are unknown. Methods Using a standard noncompartmental PK analysis, we compared EE area under the time–concentration curve (AUC) and NGMN AUC during transdermal contraceptive patch administration in HIV-1–infected women on stable LPV/r to a control group of women not on highly active antiretroviral therapy (HAART). In addition, EE AUC after a single dose of a combination oral contraceptive pill including EE and norethindrone was measured before patch placement and was compared with patch EE AUC in both groups. Contraceptive effects on LPV/r PKs were estimated by measuring LPV/r AUC at baseline and during week 3 of patch administration. Results Eight women on LPV/r, and 24 women in the control group were enrolled. Patch EE median AUC0–168 h was 45% lower at 6010.36 pg·h·mL−1 in those on LPV/r versus 10911.42 pg·h·mL−1 in those on no HAART (P = 0.064). Pill EE median AUC0–48 hours was similarly 55% lower at 344.67 pg·h·mL−1 in those on LPV/r versus 765.38 pg·h·mL−1 in those on no HAART (P = 0.003). Patch NGMN AUC0–168 h however, was 138.39 ng·h·mL−1, 83% higher in the LPV/r group compared with the control AUC of 75.63 ng·h·mL−1 (P = 0.036). After 3 weeks on the patch, LPVAUC0–8 h decreased by 19%, (P = 0.156). Conclusions Although PKs of contraceptive EE and NGMN are significantly altered with LPV/r, the contraceptive efficacy of the patch is likely to be maintained. Larger studies are indicated to fully assess contraceptive efficacy versus risks of the transdermal contraceptive patch when co-administered with protease inhibitors.

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Section: Discussionmentioning

confidence: 73%

Contraceptive Efficacy of Oral and Transdermal Hormones When Co-Administered With Protease Inhibitors in HIV-1-Infected Women: Pharmacokinetic Results of ACTG Trial A5188

Vogler¹,

Patterson²,

Kamemoto³

et al. 2010

JAIDS Journal of Acquired Immune Deficiency Syndromes

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“…Describing the principal contraceptive action as inhibition of ovulation, however, is somewhat over simplified. By inhibiting tonic gonadotropin secre tion from the beginning of the cycle, [15][16][17][18] contracep tive steroids prevent the selection and emergence of a dominant follicle, which is the principal source of the mid-cycle surge of circulating estradiol levels in untreated cycles. The mid-cycle surge of estradiol is an obligatory physiologic trigger for the mid-cycle surge of luteinizing hormone (LH) secretion, which in turn causes the rupture of the dominant follicle and the release of a mature oocyte, i.e., ovulation.…”

Section: Mode Of Actionmentioning

confidence: 99%

The Biochemistry of Oral Contraceptive Steroids

Goodman¹

1989

Semin Reprod Med

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“…Combination OCs work primarily by inhibiting the output of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). 28 Cytochrome P450 isozymes are known to mediate the oxidative metabolism of ethinyl estradiol (EE). 29 There is currently no evidence of any meaningful DDIs occurring among approved GLP-1 agonists or any of the aforementioned compounds.…”

Section: Introductionmentioning

confidence: 99%