Contraceptive, oral

Unwanted effects An increased incidence of thrombosis and embolism is attributed to the estrogen component in particular. Hypertension, fluid reten-Liillmann, Color Atlas of Pharmacology 

Minipill. Continuous low-dose administration of progestin alone can prevent conception. Ovulations are not suppressed regularly the effect is then due to progestin-induced alterations in cervical and endometrial function. Because of the need for constant intake at the same time of day, a lower success rate, and relatively frequent bleeding anomalies, these preparations are now rarely employed. 

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Insulin is used in the replacement therapy of diabetes mellitus to supplement a deficient secretion of endogenous hormone. 

It is useful to compare the activity profile of a SERM with that of estradiol, particularly in relation to effects seen postmenopausally. During chronic administration of estradiol, the risk of endometrial cancer rises co-ad-ministration of a progestin prevents this effect. Breast cancers occur more frequently, likewise thromboembolic diseases. Estradiol effectively alleviates climacteric hot flashes and sweating. After chronic treatment it reduces the incidence of osteoporotic bone fractures by preventing the loss of an estrogen-dependent portion of bone mass. Nonetheless, estrogens can no longer be recommended for this purpose because of the unfavorable benefit-risk constellation (p.330). 

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Mestranol an estrogenic component of oral contraceptive drugs... 

Optoelectronics Optosil Oraflex Oragrafin Oral care products Oral contraceptives Oral formulations Oral polio virus vaccine Oral toxicity Oramec Orange... 

Desogestrel. Desogestrel is used ia oral contraceptives. It is a white powder and can be recrystallized from pentane (71). It is practically insoluble in water and its crystal stmcture has been reported (72). 

EthynodlolDia.ceta.te, Ethynodiol diacetate has been used alone, and in combination with an strogen, as an oral contraceptive and to treat disorders associated with progesterone deficiency (76). It may be crystallised from aqueous methanol (77) and is soluble in chloroform, ether, and ethanol sparingly soluble in fixed oils and insoluble in water (76). Extensive spectral and chromatographic data have been compiled (78). 

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). 

LynestrenoL Lynestrenol (73) has been used in oral contraceptives and to treat menstrual disorders. It is converted in vivo to its active metabohte norethindrone (102,103). It can be recrystallized from methanol, and is soluble in ethanol, ether, chloroform, and acetone, and insoluble in water (102). The crystal stmcture (104) and other spectral and analytical data have been reported for lynestrenol (62). 

Meg estrolAceta.te. This compound is used outside the United States as an oral contraceptive. In the United States, it is used for the paUiative treatment of breast cancer and endometrial cancer, or as an adjunct to other therapies. Its use has been associated with an increased appetite and food intake and has been evaluated in the treatment of anorexia and cachexia (107). 

Norethindrone andISlorethindrone Acetate. Norethindrone (28) and its acetate or enanthate are used in oral contraceptives. 

Norgestimate. Norgestimate (82) is used in oral contraceptives. It can be recrystakhed from methylene chloride (117) and is the... 

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. 

U. Lachnit-Eixson, Tbe Development of aMew Triphasic Oral Contraceptive, MTP Press, Lancaster, U.K., 1980, p. 23. 

The two synthetic steroidal estrogens which have attained the greatest degree of therapeutic use are ethinyl estradiol [57-63-6] (EE) (5) and its 3-methyl ether, mestranol [72-33-3]((5). In contrast to the naturally occurring estrone derivatives, these acetylenic analogues are orally active and are the main estrogenic components of combination oral contraceptives (see Contraceptives) and certain estrogen replacement products. 

Oral Contraceptives, Population Reports, Series A, No. 6, Population Information Program, The Johns Hopkins University, Baltimore, Md. 1982, p. A190. 

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. 

L-Fohc acid is available as a crystalline dihydrate containing 8% water. Approximately 80% of the commercial production is consumed for feed enrichment in animal nutrition. FoHc acid is being offered by the pharmaceutical industry for therapeutic and prophylactic use (see Pharmaceuticals). Pharmacological doses of fohc acid are commonly used as a rescue dose during cancer chemotherapy, in women using oral contraceptives, and alcohoHcs. Several studies have provided evidence that multivitamins or foHc acid (0.8—4 mg/day) supplementation prevent the majority of neural tube defects (101). 

The typical U.S. daily diet contains 1.1—3.6 mg of vitamin B, most coming from meats and vegetables. Poor diets may provide less than half of these amounts and less than the RDA. Some populations require higher amounts persons with high protein intakes, pregnant and lactating women, users of oral contraceptives, alcohoHcs, users of dmgs which interfere with vitamin B function, and those afflicted with some diseases. Several reviews have examined the relationship of vitamin B and specific diseases in more detail (4,23). 

Oral contraceptives are among the most popular form of reversible contraception in most countries. As of the early 1990s, over 60 million women around the world use the pill and almost 150 million women have used oral contraceptives sometime during their reproductive fives (7). The commercial market for oral contraceptives is large and expanding. U.S. dmg store purchases alone will exceed 1 biUion in 1992. 

History. Detailed reviews of biological, chemical, and clinical research that led to the introduction of oral contraceptives are available in the scientific and medical literature (8,9). 

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

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