Contraceptives, production

The currendy (ca 1992) marketed injectable and implantable contraceptives are designed to be effective for maximum periods of three months and five years, respectively. There is Htde evidence from programmatic or health reasons that an injectable formulation with a longer effective life span, eg, six months, would not be equally effective. The acceptabiUty and effectiveness of long-acting contraceptives may be determined by the means by which a community deUvers contraceptive products to the pubHc the active life of a product may be determined by economic rather than programmatic or health related factors. 

Berliner, VR. (1974). U.S. Food and Drug Administration requirements for toxicity testing of contraceptive products. In Briggs, M.H. and Diczbalusy, E., eds. Pharmacological models in contraceptive development. Acta Endocrinol (Copenhagen) supp. 185 240-253. 

It is obvious that these commonalties can be tailored to achieve successful contraceptive formulations with varying degrees of efficacy, user friendliness, and aesthetics. U.S. marketed contraceptive products all contain N9 as the spermicide at various concentrations. These products rely only on the mechanism of sperm destruction by the nondiscriminating surfactant effects of the spermicide, as effects of the carrier system on sperm motility are generally minimal. No claim of activity against STDs and HIV are made by current contraceptive products, with the exception of full barrier methods such as condoms. 

Some limitations are that the amount of drug that can be injected in this fashion is fairly small and that the injected drug must not irritate or inflame the subcutaneous tissues. The subcutaneous route can also be used when certain types of drug preparations are implanted surgically beneath the skin, so that the drug is slowly dispersed from the implanted preparation and then absorbed into the bloodstream for prolonged periods of time.62,86 A common example of this form of subcutaneous administration is the use of implanted hormonal contraceptive products (e.g., Norplant).9,53 The use of these implantable contraceptives is discussed in more detail in Chapter 30. 

Prominent among toxicants that adversely affect both male and female reproductive systems are endocrine disruptors (see Section 9.7). Toxicants that mimic the actions of sex hormones are agonists, and those that prevent hormonal action or bind competitively to hormone receptor sites are antagonists,12 Male patients treated with cimetidine for peptic ulcers have exhibited low sperm counts and abnormal breast enlargement, a condition called gynecomastia. Gynecomastia has also been caused in men working in oral contraceptive production. Ketoconozole inhibits the enzymes required to produce hormones involved in sperm production and can immobilize sperm in seminal fluid. 

The progesiins are primarily used in oral contraceptive products and in hormone replaceinenl regimens for women. They are also used to treat several gynecological disorders dys-... 

Scheme 3.33). Addition of acetylene is notable for the mild reaction conditions. A good yield of 33-1 is obtained on simply bubbling acetylene into a solution of the steroid and potassium hydroxide. This product, dubbed mestranol, is a potent estrogen present in very small quantities in the great majority of oral contraceptive products. 

RATIO OF OBSERVED/EXPECTED NUMBERS OF REPORTS OF THROMBOSES WITH COMBINED TYPE ORAL CONTRACEPTION PRODUCTS... 

The first generation of the oral contraceptive products, introduced in around 1960,... 

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