Progestogens

Table 1. Low Dose Monophasic Estrogen—Progestogen Combination Oral Contraceptives Marketed in the United States...

Trade name Estrogen, Progestogen, mg Launch date Manufacturer... 

Trade name Ethinyl estradiol Regimen, days Dosage, Hg Progestogen Regimen, days a Dosage, mg Launch date Manufacturer... 

Trade name Regimen, total days breakdown Progestogen Estrogen Launch date Manuf... 

Chemical Analysis. Chemically, the various progestogens belong to one of three classes. Estranes are 19-nortestosterone derivatives (Fig. 1) gonanes are 19-nortestosterone derivatives with a C-13 ethyl group (Fig. 2) and pregnanes are 17-alpha-OH progesterone derivatives similar in stmcture to progesterone itself. 

Fig. 2. Selected gonane progestogens. (8) desogestrel [54024-22-5] C22H3QO (9) gestodene [60282-87-3] C2 H2g02 (10) norgestimate [35189-28-7] ...

Implanted Contraceptives. Controlled release of contraceptive progestins also can be accompHshed by incorporating the dmg into an implantable cylinder or rod. The best known implant is Norplant, developed by the Population Council. Norplant is composed of six matchlike silastic cylinders with the progestogen levonorgestrel (11) incorporated on the inside of each cylinder. After implantation under the skin, the product can provide effective contraception for a period of five years (43,44). Since silastic is not biodegradable, the implant can be removed from a patient at any time. 

Clinical studies with Norplant attest to its high contraceptive efficacy and safety. The main reason patients request the removal of Norplant is unpredictable vaginal bleeding episodes followed by amenorrhea. The bleeding problem is an unavoidable sequela of progestogen-only contraception. 

Progestogens Reproductive organs Improved reproductive capacity... 

Glucocorticoids have inhibitory (apoptotic) effects on lymphocyte proliferation and are used to treat leukemias and lymphomas. Estrogens (fosfestrol) are used to block the effect of androgens in prostate cancer. Progestogens (megestrol, medroxyprogesteroneacetate) have been useful for treating endometrial carcinoma, renal tumors, and breast cancer. 

---