Contraceptives progestins

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. 

Progestins are nsed for varions menstmal cycle disorders, for functional uterine bleeding of various origins, and as a contraceptive. Progestin therapy is also used to treat endometriosis and endometrial carcinomas. Progesterone is not effective when taken orally due to intensive metabolism, and therefore it is used by either parenteral or transvaginal introduction. 

Estimated Relative Oral Contraceptive Progestin/Estrogen/Androgen Activi... 

Benagiano G, Primiero FM, Farris M. Clinical profile of contraceptive progestins. EurJ Contracept Reprod Health Care. 2004 9 182-193. 

Ovrette Norgestrel 0.075 mg Tablet Oral contraceptive progestin receptor Cellulose, lactose, magnesium stearate, polacrilin potassium Wyeth... 

All medical therapies (nonsteroidal anti-inflammatory drugs, oral contraceptives, progestins, danazol, or gonadotropinreleasing hormone agonists) are equally efficacious in treating endometriosis-related pain based on available evidence. Choice among agents is determined primarily by side-effect profile, cost, and individual patient response. 

Perlman JA, Russell-Briefel R, Ezzati T, Lieberknecht G. Oral glucose tolerance and the potency of contraceptive progestins. JC 2ronDi5(1985) 38, 857-64. 

Table 2. Progestins Marketed in the United States and Europe for Contraceptive and Noncontraceptive Uses...

Gestodene Gestodene (54), along with norgestimate and desogestrel, are the progestin components of the third-generation oral contraceptives (see Contraceptives). It may be crystallised from hexane/acetone (81) or ethyl acetate (82), and its crystal stmcture (83) and other spectral data have been reported (84). 

As of 1994, there were approximately 47 progestin-containing contraceptive dmg formulations sold in the United States for use as oral contraceptives (Table 3). In addition, there are three nonoral contraceptive formulations containing progestins ie, one injectable (Depo-Provera), one as an intrauterine device (lUD) (Progestasert), and one implantable (Norplant). Of the oral formulations, all but two also contain an estrogen component, ethynylestradiol. 

Noncontraceptive Uses of Progestins. Progestins have other therapeutic uses aside from contraception. Hormone-dependent tumors and cysts involving reproductive tissues respond to progestins. Megestrol acetate and MPA are the two most commonly used progestins to treat breast cancer... 

The 1950s and 1960s saw the development of orally active progestins based on the synthesis of steroids that lack the C19-angular methyl substituent (19-norsteroids). The commercial production of these compounds for the regulation of menstmal disorders began in 1957, and for oral contraception in 1960. 

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