U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1 - 10 of 11 results

Dienogest (Natazia) is a hybrid progestogen that combines properties of both the 19-nortestosterone derivatives and the progesterone derivatives. It is indicated for use by women to prevent pregnancy and for the treatment of heavy menstrual bleeding in women without organic pathology. Dienogest is also approved in Europe, Australia, Malaysia, Singapore and Japan for the treatment of endometriosis. It is lowers the risk of becoming pregnant primarily by suppressing ovulation. Other possible mechanisms may include cervical mucus changes that inhibit sperm penetration and endometrial changes that reduce the likelihood of implantation. Dienogest exhibits highly selective binding to the progesterone receptor. It has high progestational and significant antiandrogenic activity, but only moderate antigonadotrophic activity. The most common adverse reactions in clinical trials for Natazia are headache (including migraines), breast pain, menstrual disorders, nausea or vomiting, acne, mood changes and increased weight.
Drospirenone (INN, USAN), also known as 1,2-dihydrospirorenone, is a steroidal progestin of the spirolactone group. Drospirenone binds strongly to the progesterone receptor (PR) and mineralocorticoid receptor (MR), with lower affinity, to the androgen receptor (AR), and very low affinity for the glucocorticoid receptor (GR). Drospirenone is an ingredient in some birth control pills and hormone replacement therapy. In combination with ethinylestradiol it is used as contraception, and for women who want contraception it is also approved by the U.S. Food and Drug Administration (FDA) to treat vasomotor symptoms due to menopause.It is sold as a combined oral contraceptive under the brand names Yasmin (US, EU, Latin America), Jasmine (France), Yarina (Russia) in a dosage containing drospirenone 3 mg/ethinylestradiol 30 µg. In the United States, Bayer Schering released a pill based on Yasmin with the B vitamin folate (B9), which is marketed under the names Safyral and Beyaz.
Status:
First approved in 1992

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Desogestrel is a prodrug of etonogestrel (3-keto-desogestrel) which was approved as oral contraceptove medicine. Desogestrel acts selectively binding to progesterone receptor and enchancing its activity.
Medroxyprogesterone acetate (INN, USAN, BAN), also known as 17α-hydroxy-6α-methylprogesterone acetate, and commonly abbreviated as MPA, is a steroidal progestin, a synthetic variant of the human hormone progesterone. Medroxyprogesterone acetate (MPA) administered orally or parenterally in the recommended doses to women with adequate endogenous estrogen, transforms proliferative into secretory endometrium. Androgenic and anabolic effects have been noted, but the drug is apparently devoid of significant estrogenic activity. While parenterally administered MPA inhibits gonadotropin production, which in turn prevents follicular maturation and ovulation, available data indicate that this does not occur when the usually recommended oral dosage is given as single daily doses. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate, what is normally being administered is MPA and not MP. Used as a contraceptive and to treat secondary amenorrhea, abnormal uterine bleeding, pain associated with endometriosis, endometrial and renal cell carcinomas, paraphilia in males, GnRH-dependent forms of precocious puberty, as well as to prevent endometrial changes associated with estrogens. Progestins diffuse freely into target cells in the female reproductive tract, mammary gland, hypothalamus, and the pituitary and bind to the progesterone receptor. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.
Status:
Possibly Marketed Outside US
Source:
Myvlar by OASIS TRADING
Source URL:
First approved in 2018

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gestodene (17alpa-ethynyl-13beta-ethyl-17beta-hydroxy-4,15-gonadien-3-one) is the most potent synthetic progestin currently available and it is widely used as a fertility regulating agent in a number of contraceptive formulations because of its high effectiveness, safety and acceptability. Products containing gestoden include Meliane, which contains 20 ug of ethinylestradiol and 75 ug of gestodene; and Gynera, which contains 30 ug of ethinylestradiol and 75 ug of gestodene. Gestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills. Gestodene displays a high binding affinity to the progesterone receptor, also binds to adrogen and glucocorticoid receptors but no measurable affinity for the estrogen receptor.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quingestanol is a metabolite of the quingestanol acetate, oral contraceptive, which was studied for therapy of menopausal diabetic women. Quingestanol is also a prodrug of norethisterone, which is used in birth control.
mixture
Status:
First approved in 2001

Class:
MIXTURE



Norelgestromin, the progestin, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor. Johnson & Johnson developed an adhesive female contraceptive patch that contains ethinylestradiol (0.75mg) and the progestogen norelgestromin (6mg). his product is a combination contraceptive acting via the inhibition gonadotropins. Its primary mechanism of action involves the suppression of ovulation, including changes in the cervical mucus and endometrium. The patch delivers a continuous flow of hormones through the skin and into the bloodstream. The contraceptive patch is available in countries worldwide.
mixture
Status:
First approved in 1989

Class:
MIXTURE



Norgestimate is a steroidal progestin of the 19-nortestosterone group that is used in combination with ethinylestradiol as an oral contraceptive and for treatment of acne. and in combination with estradiol in menopausal hormone replacement therapy. Norgestimate shows high selectivity for the progesterone receptor and low androgenic activity.

Showing 1 - 10 of 11 results