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Endocrine Disorders, Contraception, and Hormone Therapy during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
This synthetic progestational agent is used with estrogen compounds in oral contraceptives and for menstrual disorders. There are no controlled studies of congenital anomalies among infants born to women who used norgestrel during pregnancy. Although no human reports have associated the use of norgestrel during pregnancy with masculinization of external female genitalia, large doses administered in the latter two-thirds of pregnancy would be expected to produce virilization based upon clinical experience with other closely related compounds. The frequency of congenital anomalies was not increased among mouse and rabbit litters born to females treated with very large doses of norgestrel during pregnancy (Heinecke and Kohler, 1983; Klaus, 1983).
Endocrine, paracrine and intracrine mechanisms of growth regulation in normal and malignant breast epithelium
Published in A. R. Genazzani, Hormone Replacement Therapy and Cancer, 2020
J. R. Pasqualini, G. S. Chetrite
It was observed that 19-nor-progestins (such as those derived from testosterone: norethindrone, norgestrel or norethynodrel) possess a weak estrogenic activity and can stimulate (at 10–6 mol/l) the proliferation of estrogen receptor-positive but not estrogen receptor-negative breast cancer cells32. Interesting data were obtained with nomegestrol acetate (Lutenyl®), a 19-nor-progestin derivative. This compound does not possess estrogenic activity and is exclusively antiproliferative in MCF-7 and T-47D cells. It was postulated that the estrogenic activity is determined mainly by the 17α-hydroxyl group associated with estrogenic progestins, rather than by the absence of a methyl group at the C19 position38.
Birth control
Published in Frank J. Dye, Human Life Before Birth, 2019
Emergency contragestion drugs (“morning after” pills) have been available in the United States since the late 1960s. Patients who face an unwanted pregnancy resulting from rape, failure of contraception, or unprotected sex may take a high dose of certain common birth control pills. These can reduce the risk of pregnancy by more than 75% when taken within 72 hours after sex. The most commonly used morning after pills are norgestrel and levonorgestrel. A deliberate overdose of these pills provides emergency contragestion. They prevent pregnancy by rapidly elevating a woman's hormone levels, which prevents the fertilized egg from implanting into the endometrium.
Pharmacodynamics of combined estrogen-progestin oral contraceptives 3. Inhibition of ovulation
Published in Expert Review of Clinical Pharmacology, 2018
Carlo Bastianelli, Manuela Farris, Elena Rosato, Ivo Brosens, Giuseppe Benagiano
The ovulation-inhibiting activity of a combination of EE 30 μg plus LNG (at the time called + d-Norgestrel) 150 μg was first tested almost 40 years ago [83]. Hormone production (LH, FSH, E2) and gonadotropin response to GnRH were significantly suppressed, while at the completion of the inactive tablet period, basal gonadotropin and E2 concentrations and gonadotropic response to GnRH were not significantly different to pretreatment levels. In a further investigation, this preparation was evaluated when the pill was started on day 1 or 5 [84]; it was found that mean E2 levels of day 5 ‘starters’ were significantly higher than those of day 1 ‘starters’ (p > 0.05). The consequences of omitting pills were investigated also with this combination; it was found that the deliberate omission on day 4 did not produce any marked hormonal effect, either early or late in the cycle [85]; in addition, omitting pills at the beginning of a cycle, as well as prolonging the IFP to 9 days, did not cause any major problem [86].
An update on the pathogenesis of hidradenitis suppurativa: implications for therapy
Published in Expert Review of Clinical Immunology, 2018
Deborah Negus, Christine Ahn, William Huang
HS patients often suffer from PCOS, and many females with HS have increased testosterone levels. Therefore, Mortimer et al. studied the effects of antiandrogens on HS. This study treated 24 patients with ethinyl estradiol 50 μg plus either cyproterone acetate 50 mg or norgestrel 500 μg. No significant difference was found between the two treatments, but both treatments significantly improved HS as measured by patient subjective assessment [59]. Furthermore, a later retrospective study comparing various antiandrogen therapies to antibiotics found that 55% of women treated with antiandrogens noted improvement in their disease compared to only 26% of women treated with antibiotics. This study recommends considering antiandrogen therapies in all women with HS [60].
Menopausal hormone therapy: a better and safer future
Published in Climacteric, 2018
Progestin-containing intrauterine devices (IUDs) offer an attractive way of delivering progestins to the endometrium and preventing endometrial hyperplasia and carcinoma in perimenopausal and postmenopausal women receiving estrogens. IUDs provide contraception and reduce the amount of blood loss in dysfunctional uterine bleeding, which is a common problem in perimenopausal women. An IUD containing levonorgestrel (l-norgestrel), marketed as Mirena, was introduced in 1990 and found to provide effective contraception for 5 years. The device contains 52 mg l-norgestrel and initially releases approximately 20 µg of l-norgestrel daily, declining to 14 µg daily after 5 years. In 2013, a smaller IUD, marketed as Skyla or Jaydess, containing 11 mg l-norgestrel and releasing approximately 10 µg l-norgestrel daily, declining to 5 µg daily, was introduced and found to provide effective contraception for 3 years. The use of both Mirena and Skyla in pre- and postmenopausal women has been extensively investigated in Finland. l-Norgestrel administered by an IUD acts directly on the endometrium and only a small amount enters the circulation. In a study of 110 premenopausal women using Mirena, the plasma levels of l-norgestrel, as measured by LC-MS, were 191 ± 71 pg/ml during the 1st year of use and 141 ± 59 pg/ml during the 5th year46. In a prospective, randomized, controlled study of 163 postmenopausal women using Mirena and receiving 2 mg estradiol valerate daily orally, the median plasma levels of l-norgestrel were 478 pg/ml at 12 months, as measured by radioimmunoassay (RIA) which measures metabolites as well as progesterone47. In the women using the Skyla IUD, the median l-norgestrel levels as measured by RIA were 185 pg/l at 12 months and were significantly lower than those in the women using Mirena. After 12 months of therapy, strong endometrial suppression was found in all 55 women using Mirena and in 46 out of 47 women who used Skyla. After 6 months of therapy, 54 out of the 55 women who used Mirena and 43 out of the 47 women who used Skyla had no bleeding.