Contraceptive steroids, synthetic

Since the development of the oral contraceptive steroids in the 1960s, various steroids and procedures have been used. Synthetic steroids are now used since their half-hves in the body are longer than the natural steroids. Combined oestrogen-progesterone contraception involves taking one piU each day which contains a synthetic progestogen plus an oestrogen. The pill is taken for 21 dyas, with a break for... 

Other new but conventional radioimmunoassays have involved oestra-l,3,5(10)-triene-3,15a,16a,17/S-tetrol ( oestetrol ), as its 6-(0-carboxy-methyloximino)-derivative, the 16-carboxymethyloximino-derivative of androst-5-ene-3/S,17 8-diol, the 15-hemisuccinate of 15a-hydroxy-testosterone, some oestriol monoglucoside derivatives, the 6-carboxy-methyloximino- and 3-hemisuccinate derivatives of the synthetic oestrogen 17a-ethynyloestradiol, the 3-carboxymethyloximes of the contraceptive steroids norethindrone and norgestrel , and the pituitary gonadotropin inhibitor, the isoxazole derivative Danazol (25), which was effectively bound by an antiserum for the corresponding 17-carboxymethyloxime (26)7°... 

Zl. Zanartu, J., Dabancens, A., Rodriguez-Bravo, R., and Schally, A. V., Induction of ovulation with synthetic gonadotrophin-releasing hormone in women with constant anovulation induced by contraceptive steroids. Brit. Med. J. 1, 805-608... 

Figure 22.16 Steroids. In mammals, male and female sex hormones are steroids. Oral contraceptives are synthetic steroids. AnaboUc steroids increase muscle mass. Adrenocorticoid hormones such as cortisone have amazing anti-inflammatory properties. Hundreds of steroid-based drugs are available by prescription in the United States. 

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. 

Combined oral contraceptives contain a combination of a synthetic estrogen and one of several steroids with progestational activity. Most oral contraceptives contain one of two types of estrogen ethinyl estradiol, which is pharmacologically... 

Elaboration of a commercially viable route for total synthesis of 19-nor steroids led to the introduction of the totally synthetic product norgestrel (71) as the progestational component of an oral contraceptive. As was observed in the "natural" 19-nor-compounds, reduction of the 17-ethynyl group to 17-ethyl affords compounds with androgenic/anabolic... 

Synthetic steroids, especially estrogenic drugs, are used extensively in estrogen-replacement therapy and oral contraceptives, in veterinary medicine for growth enhancement, and in athletic performance enhancement. In general, large portions... 

Synthetic steroid hormones retain the common steroid nucleus, but they may contain novel substituents that affect their pharmacological activity. The two most widely used synthetic steroid estrogens are ethinyl estradiol (Estinyl) and mestranol, found in oral contraceptives. Synthetic steroids containing an ethinyl substitution are metabolized more slowly. Thus, these synthetic steroid hormones have better oral absorption properties and extended biological half-lives than the natural estrogens. 

Several synthetic steroids have been synthesized in an effort to investigate their physiological effects. Prednisone is an example of a synthetic drug. The oral contraceptives and anabolic steroids are the best known of all steroids. 

Another example of concern is the effect of antibiotic therapy on the efficiency of the synthetic and semisynthetic steroids used by more than 50 million women as contraceptive agents. Since 1973, many antibiotics such as ampicillin, amoxycillin, chloramphenicol, and sulfonamides have been shown to cause failures of oral contraceptives due to perturbation of intestinal microflora (56, 57). 

---