Estrogenic effect of gestodene- or desogestrel-containing oral contraceptives on lipoprotein metabolism

Article Abstract:

Altered fat and cholesterol metabolism has been linked with cardiovascular disease. Studies have shown that women who take oral contraceptives are at risk for cardiovascular disease. Women naturally produce estrogen until menopause, which tends to protect against cardiovascular disease by affecting lipoprotein metabolism. After menopause, the incidence of heart disease increases. Women who take estrogen replacement therapy during menopause reduce their risk of cardiovascular disease by decreasing the levels of low-density lipoproteins (LDL) and increasing the more ''beneficial'' high-density lipoproteins (HDL). In men, androgens (male hormones) have a tendency to lower HDL, contributing to the higher incidence of heart disease among men. The level of HDL is related to the balance of estrogen and androgens. It is suggested that the other female hormone, progesterone, acts like an androgen and diminishes the action of estrogen. This would explain why progesterone modifies the estrogen (ethinyl estradiol) found in the oral contraceptive formulas. Lipoprotein metabolism was measured after administration of one of two progesterone compounds contained in the low-dose estrogen oral contraceptive pills, to determine their effect on the estrogen/androgen balance. Sixty-eight nonpregnant women were given either 75 micrograms of gestodene plus 30 micrograms of ethinyl estradiol (GTD-EE) or 150 micrograms of desogestrel plus 30 micrograms of ethinyl estradiol (DSG-EE) for 12 months. Lipid profiles were performed before and after every three cycles of the pill. After three months, there was an increase in triglycerides and HDL. There was also an increase in apolipoprotein A and B, other types of lipoprotein. This persisted after cycles three and six. The changes in lipids were virtually the same in both progesterone groups which remained within the normal range. Estrogen-dominance affected lipoprotein metabolism. It is not likely, however, that these changes could induce atherosclerosis. (Consumer Summary produced by Reliance Medical Information, Inc.)

Lipoproteins, Progestational hormones, Blood lipoproteins

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Clinical acceptability of monophasic gestodene

Article Abstract:

Gestodene is a new progesterone-like hormone. It is being marketed as an oral contraceptive in a low-dose formulation in combination with an estrogen-like hormone. Gestodene is expected to provide certain advantages over other progesterones due to its endocrine activities. These include a reliable contraceptive effect even at low doses and the ability to block undesirable estrogenic side effects. In addition, gestodene has no androgenic (male sex hormone) effects, so side effects such as acne, weight increase, and unfavorable effects on fat levels are not expected. In addition, gestodene can slightly block the effects of another steroid, and advantageous effects on blood pressure may result. The contraceptive reliability and prevalence of symptoms in users of the gestodene-containing oral contraceptives were evaluated in studies of over 10,000 women, some of whom were studied for over three years. Contraceptive reliability was very high, with most of the few pregnancies attributable to user errors in taking the pills. A tablet-free interval, when menstruation occurs, is part of the monthly dosage protocol. Amenorrhea (absence of bleeding) occurred in less than one percent of all the women's cycles, while breakthrough bleeding occurred at other times in the cycle in up to 2.8 percent of cycles. Breakthrough spotting occurred in up to 8.2 percent of cycles, mostly during the first cycles after OC use was begun. Nausea and vomiting occurred somewhat frequently during initial use but then decreased. The prevalence of breast tension and headaches was similar before and after treatment, as was that of migraines. The prevalence of acne and fluid retention declined as the studies progressed. Body weights and blood pressure, on average, remained stable. Dropouts occurred primarily due to breakthrough bleeding, weight gain, and headaches. The study indicates that gestodene is effective and well-tolerated. (Consumer Summary produced by Reliance Medical Information, Inc.)

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Inhibition of ovulation by low-dose monophasic contraceptive containing gestodene

Article Abstract:

Gestodene is a new progesterone-like hormone, which is an effective oral contraceptive at low doses and is used in combination with an estrogen-like hormone. It is important to document the effects of gestodene and similar hormones on the pituitary-ovarian systems, the major endocrine tissues which regulate estrogen production. The effects of low-dose gestodene- and estrogen-containing oral contraceptives on pituitary hormones and ovarian function were studied in 25 healthy women. Luteinizing hormone (LH) and follicle-stimulating hormone (FSH) are the two pituitary hormones that regulate ovarian function. Typical cyclical peaks of each were suppressed by gestodene therapy. The cycle after treatment resumed the normal pattern of hormone secretion. Similar effects on ovarian secretion of estrogen and progesterone occurred. However, intensive analysis of data showed that there was a slight increase in estrogen in the initial days of all but the first treatment cycle, suggesting that in some subjects, egg-containing ovarian follicles could mature during the pill-free seven-day interval in the monthly dosage schedule. These effects were confirmed by ultrasound studies of ovarian follicular structure. The subjects who had elevated estrogen at cycle beginnings also had maturing follicles. However, estrogen was suppressed thereafter, ensuring a contraceptive effect. The study indicates that the gestodene-containing oral contraceptive effectively inhibits secretion of pituitary hormones and ovarian estrogen and progesterone, thereby blocking steroid-dependent functions such as egg maturation. (Consumer Summary produced by Reliance Medical Information, Inc.)

Ovulation

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