Contraceptive agents hormonal

Whole microbial cells as well as microbially derived enzymes have played a significant role in the production of novel antibiotics. The potential of microorganisms as chemical catalysts, however, was first fully realized in the synthesis of industrially important steroids. These reactions have assumed increasing importance following the discovery that certain steroids such as hydrocortisone have anti-inflammatory activity, whilst derivatives of the steroidal sex hormones are nsefiil as oral contraceptive agents. More recently, chiral inversion of non-steroidal anti-inflammatory dmgs (NS AIDs) has been demonstrated. 

A wealth of epidemiological, clinical, and experimental studies link estrogens with cardiovascular disease (CVD). This evidence has promoted CVD as a key area within the extragenital effects of estrogens. The question is of interest because it directly affects the wide clinical use of estrogens as contraceptive agents or as principal constituents of hormonal therapy (HT) formulations in postmenopausal women. The significance of the subject is further reinforced by the relevance of CVD as a cause of mortality and morbidity in both women and men. 

The chief therapeutic uses of estrogens and progestins are as oral contraceptives and hormone replacement therapy. Progestins and SERMs are also important agents in the treatment of osteoporosis, breast cancer, endometrial cancer, and infertility. 

Drugs That Interfere with Hormonal Contraceptives Concomitant use of HIV-protease inhibitors, griseofulvin, modafinil, penicillins, rifampin, rifabutin, phenytoin, carbamazepine, or certain herbal supplements such as St. John s wort with hormonal contraceptive agents may reduce the effectiveness of the contraception and up to one month after discontinuation of these concomitant therapies. Therefore, women requiring treatment with one or more of these drugs must use two other effective or highly effective methods of contraception or abstain from heterosexual sexual contact while taking thalidomide... 

Fasting growth hormone concentrations are higher in women using a contraceptive agent than in controls (162). 

The second discovery, by Pincus et al. at the Worcester Foundation, was the demonstration that the female hormone progesterone acts as contraceptive agent in animals [3]. 

Hormonal Control of Copper Metabolism Recent evidence suggests that metabolism of copper as well as zinc is controlled by the pituitary-adrenal axis (97,98,99). For example, administration of large doses of corticosteroids in humans leads to rapid and sustained drop in serum copper and zinc. Pregnant women and women on oral contraceptive agents show a significant increase in serum copper levels (iOO, 101,102),... 

Since 19-hydroxycholesterol 3-acetate is readily available from cholesterol by the illustrated synthesis, it is possible to predict that this method or one closely allied to it will supplant presently used technology for estrone manufacture to some degree. Estrone, in addition to its uses as a female hormone is a key intermediate for the commercial synthesis of many widely used contraceptive agents. It has been selling for a price in the range of 0.50- 1.00/gram (1965). 

Injected formulation of leuptoleine and triptoreline [57773-63 ] ate used to treat metastasized cancer of the prostrate, whereas an encapsulated formulation of bromocryptin [25614-03-3] is used to inhibit milk production in women after pregnancy. The performance of encapsulated hormonal polypeptides is weU documented (47). Injectable biodegradable mictocapsules loaded with fertUity control agents have been under development for a number of years and have been carried to various stages of clinical development (48) (see Contraceptives). 

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