Attempts have been made over the years to replace ethinyl estradiol (EE) in combined oral contraceptives (COCs) with the less potent natural estrogen estradiol (E), or its prodrug, E valerate (EV), to improve their safety and tolerability. Recently, a COC incorporating a novel weak natural estrogen, estetrol (E), combined with drospirenone, has become available. We present a comparative analysis of the three prevailing estrogens used in COCs, focusing on their structure-function relationships, receptor-binding affinity, potency, metabolism, pharmacokinetic parameters, and pharmacodynamics.
View Article and Find Full Text PDFObjective: To investigate the efficacy of elagolix when administered at different time points in a menstrual cycle.
Design: Clinical case series.
Setting: Academic reproductive endocrinology center.
Septate uteri have been associated with adverse pregnancy outcomes including spontaneous abortion, preterm delivery, and malpresentation. It is unclear if uterine septa are associated with infertility. Although some studies have shown improved pregnancy outcomes after septum resection, indications for resection are not well established.
View Article and Find Full Text PDFExpert Rev Pharmacoecon Outcomes Res
April 2009
Premenstrual symptoms are distressing for up to 20% of reproductive-aged women and are associated with impairment in interpersonal or workplace functioning for at least 3-8%. Typical symptoms of premenstrual syndrome and the severe form, premenstrual dysphoric disorder, include irritability, anger, mood swings, depression, tension/anxiety, abdominal bloating, breast pain and fatigue. The symptoms recur monthly and last for an average of 6 days per month for the majority of the reproductive years.
View Article and Find Full Text PDFDrospirenone 3 mg/ethinyl estradiol 20 microg (24/4) is a new unique oral contraceptive formulation that combines in a novel dosing regimen the lowest dosage of ethinyl estradiol commonly used today with drospirenone, an innovative progestin. Drospirenone is a compound closely resembling progesterone, but with the antimineralocorticoid and antiandrogenic properties of a related therapeutic agent, the diuretic, antihypertensive and androgen receptor antagonist, 17alpha-spironolactone. The prolongation of hormonally active pills in the monthly drospirenone/ethinyl estradiol cycle from 21 days to 24 days, followed by 4 days of inactive pills, is an interesting variant of the recently developed extended pill regimens (1).
View Article and Find Full Text PDFExpert Opin Pharmacother
February 2008
Premenstrual dysphoric disorder (PMDD) is characterized by physical, affective and behavioral symptoms that are linked to the luteal phase of the menstrual cycle and relieved soon after the onset of menses. The disorder is chronic and exerts a major impact on personal relationships and occupational productivity for the estimated 6% of reproductive-aged women who fulfill strict PMDD criteria and the almost 20% of women who nearly meet these criteria. There are now various pharmacologic options that have demonstrated efficacy for PMDD and two of these approaches have an approved indication for treatment from the US FDA: three selective serotonin re-uptake inhibitors; and for women who also desire hormonal contraception, a low dose oral contraceptive pill containing the progestin drospirenone, in a new dosing regimen.
View Article and Find Full Text PDFA combined oral contraceptive pill containing 20 microg of ethinyl estradiol and 3 mg of the progestin drospirenone in a novel dose regimen (24 active pills followed by 4 placebo pills), has demonstrated efficacy for the symptoms of premenstrual dysphoric disorder, a severe form of premenstrual syndrome, with an emphasis on the affective symptoms. Drospirenone has progestagenic, anti-androgenic and anti-aldosterone properties, which differ from earlier generations of progestins, and reducing the hormone pill-free interval allows for better suppression of ovarian steroid production.
View Article and Find Full Text PDFDrospirenone is a novel progestin available in combined oral contraceptives and menopausal hormonal therapy. Similar to its parent compound spirolactone, an analog of spironolactone, drospirenone has antimineralocorticoid and antiandrogenic activity. Combined with ethinyl estradiol in oral contraceptive formulations, drospirenone-containing contraceptives have similar efficacy and safety profiles to other low-dose oral contraceptives, but seem to offer improved tolerability with regard to weight gain, mood changes, acne and treatment of a severe form of premenstrual syndrome called premenstrual dysphoric disorder.
View Article and Find Full Text PDFMillions of reproductive-age U.S. women experience premenstrual symptoms with varying degrees of severity.
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