Evaluation of the effects of rifampicin, ketoconazole and erythromycin on the steady-state pharmacokinetics of the components of a novel oral contraceptive containing estradiol valerate and dienogest in healthy postmenopausal women

Blode, Hartmut; Zeun, Susan; Parke, Susanne; Zimmermann, Till; Rohde, Beate; Mellinger, Uwe; Kunz, Michael

doi:10.1016/j.contraception.2012.01.010

Cited by 27 publications

(24 citation statements)

References 17 publications

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“…Three studies addressed COC hormone PK with rifampin, and all demonstrated reductions in estrogen and/or progestin exposure . A single‐sequence crossover study of eight women on chronic rifampin therapy for tuberculosis reported ethinyl estradiol (EE) and NET PK after a single COC pill during and after rifampin therapy .…”

Section: Resultsmentioning

confidence: 99%

Drug interactions between rifamycin antibiotics and hormonal contraception: a systematic review

Simmons

Haddad

Nanda

et al. 2017

BJOG

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Section: Resultsmentioning

confidence: 99%

Drug interactions between rifamycin antibiotics and hormonal contraception: a systematic review

Simmons

Haddad

Nanda

et al. 2017

BJOG

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“…However, the optimal regimen of ET required to achieve the desired relief is controversial, and some studies reported that low-dose systemic regimens may be inadequate for relieving vaginal symptoms [4, 5]. Estradiol valerate, a natural estrogen 17 β -estradiol, is a synthetic 17-pentanoyl ester commonly used in clinical hormone treatment for menopausal symptoms, such as vaginal symptoms, hot flashes, and night sweats [6, 7]. …”

Section: Introductionmentioning

confidence: 99%

Differential Regulation of Morphology and Estrogen Receptor-Alpha Expression in the Vagina of Ovariectomized Adult Virgin Rats by Estrogen Replacement: A Histological Study

Zhang

et al. 2016

International Journal of Endocrinology

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Background. To determine the exact role of estrogen in vaginal tissue morphology and estrogen receptor-alpha (ERα) distribution in the vagina, which remains controversial. Methods. Sixty rats were randomly categorized: sham-operated (sham), ovariectomy (OVX), and four estradiol treatments (estradiol valerate at 0.4, 0.8, 1.6, and 3.2 mg/kg/day) for 2 weeks. Thereafter, vaginal samples were biopsied from the distal- and proximal-half portions. The percentage of ERα-immunoreactive cells and the ERα score were quantified using immunohistochemistry to assess changes in ERα expression and distribution. Results. OVX induced significant vaginal atrophy and organic index. Estrogen-replacement therapy (ERT) reversed vaginal atrophy. The vaginal distal-half areas showed lower ERα% than the proximal-half areas. The ERα% increased sharply 4 weeks after OVX, especially in the epithelial layer (P = 0.023). ERT elicited different degrees of reductions in tissues after the 2-week treatment, but the ERα% in only the epithelium recovered in parallel with that in the sham group (P = 0.001). The OVX group showed higher ERα histological scores than the sham group, and the distal-half area changed more evidently than the proximal-half area. ERα expression was nearly unchanged after ERT (P > 0.05). Conclusions. ERT is effective for treating obesity and vulvovaginal atrophy caused by hypoestrogenism and advancing age in menopausal women but cannot recover the distribution and expression of ERα.

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“…Of the other publications, one was a pooled study summarizing menstrual blood loss (MBL) data across two individual studies previously identified, and was included as appropriate 23. The other seven articles reported on outcomes that were not the focus of this review but were included, where appropriate, as supportive references 11,19–21,25–27. Ten other pertinent articles were identified from published manuscripts known to the authors or from unpublished manuscripts that were available to them and were included for discussion,14,29–37 but three others were not included as the outcomes reported were not the focus of this review 38–40.…”

Section: Methodsmentioning

confidence: 99%

Noncontraceptive benefits of the estradiol valerate/dienogest combined oral contraceptive: a review of the literature

Nappi¹,

Serrani²,

Jensen³

2014

IJWH

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Combined oral contraceptives formulated to include estradiol (E2) have recently become available for the indication of pregnancy prevention. A combined estradiol valerate and dienogest pill (E2V/DNG), designed to be administered using an estrogen step-down and a progestin step-up regimen over 26 days of active treatment followed by 2 days of placebo (26/2-day regimen), has also undergone research to assess the potential for additional noncontraceptive benefits. Randomized, placebo-controlled studies have demonstrated that E2V/DNG is an effective treatment for heavy menstrual bleeding – a reduction in median menstrual blood loss approaching 90% occurs after 6 months of treatment. To date, E2V/DNG is the only oral contraceptive approved for this indication. Comparator studies have also demonstrated a reduction in hormone withdrawal-associated symptoms in users of E2V/DNG compared with a conventional 21/7-day regimen of ethinylestradiol/levonorgestrel. Other potential noncontraceptive benefits associated with E2V/DNG, like improvement in dysmenorrhea, sexual function, and quality of life, are comparable with those associated with other combined oral contraceptives and are discussed further in this review.

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Evaluation of the effects of rifampicin, ketoconazole and erythromycin on the steady-state pharmacokinetics of the components of a novel oral contraceptive containing estradiol valerate and dienogest in healthy postmenopausal women

Cited by 27 publications

References 17 publications

Drug interactions between rifamycin antibiotics and hormonal contraception: a systematic review

Drug interactions between rifamycin antibiotics and hormonal contraception: a systematic review

Differential Regulation of Morphology and Estrogen Receptor-Alpha Expression in the Vagina of Ovariectomized Adult Virgin Rats by Estrogen Replacement: A Histological Study

Noncontraceptive benefits of the estradiol valerate/dienogest combined oral contraceptive: a review of the literature

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