Oral contraceptives formulations

Cyproterone acetate (CPA) is a progestational antiandrogen that blocks the androgen receptors. It is combined with ethinyl estradiol in an oral contraceptive formulation, which is indicated in female acne patients with a high level of seborrhea, therapy resistant papulo-pustular acne or acne conglobata not responding to other treatments. 

Progestin-only oral contraceptive formulations consist of a low dose of either norethindrone or norgestrel... 

C. Although progestin-only oral contraceptive formulations are available, the combination of estrogen and progestin is considered the safest and most desirable type. 

Diffuse prickly erythema has been attributed to ethinylestradiol in various oral contraceptive formulations. 

G. Carignan, B. A., B. A. Lodge, and W. Skakum, General re-versed-phase high-performance liquid chromatography procedure for the analysis of oral contraceptive formulations, J. Chromatogr., 375 470(1984). 

One is an anabolic steroid called oxymetho-lone and the other, called norgestrel, is used in oral contraceptive formulations. Identify these compounds based on their stmctural features. 

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

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. 

Future efforts should be directed at optimizing current formulations to finally come up with an ideal oral contraceptive which would reduce the risk of breast, ovarian and endometrial cancer without any cardiovascular complications. 

The oral contraceptives have changed a great deal since their introduction in the 1960s. Today the levels of hormones provide lower dosages of hormones compared with the older formulations, while retaining the same degree of effectiveness (>99% when used as prescribed). 

Finally, another unique formulation is a chewable tablet available to women who have difficulty swallowing medications. Ovcon 35 (norethindrone/ethinyl estradiol) has all 28 tablets in chewable form and has added spearmint flavoring.30 Along with each of these unique oral contraceptives, there are preparations currently being studied that contain 24 active pills and 4 placebo pills per pack, shortening the hormone-free period.1... 

As an alternative to oral contraceptive pills, which must be taken daily in order to reliably prevent pregnancy, non-oral contraceptives in the form of transdermal, transvaginal, and injectable preparations are available and offer patients safe and effective alternatives to the pills for prevention of pregnancy. These formulations also do not require daily administration, making them more convenient than the pill formulations. 

Adverse effects include nausea, weight gain, breast tenderness, and breakthrough bleeding. Oral contraceptives have also been associated with an increased incidence of thromboembolic disease, particularly in women who use tobacco products or have other risk factors for thromboembolism. The development of these complications is significantly reduced when low-dose estrogen formulations of oral contraceptives are used.3... 

Sustained-release formulations can produce stable serum concentrations with once or twice daily dosage. Therapeutic effects occur at blood levels > 5 mg/1, and side effects increase considerably at levels > 15 mg/1. Smoking, alcohol, anticonvulsants, and rifampicin induce the drug-metabolizing enzyme system in liver and reduce the half-life of theophylline. On the other hand, heart and liver failure, sustained fever, old age and drugs such as cimeti-dine, ciprofloxacin, and oral contraceptives reduce theophylline clearance and thereby increase serum concentrations. 

The incidence of serious known toxicities associated with the use of these drugs is low—far lower than the risks associated with pregnancy. There are a number of reversible changes in intermediary metabolism. Minor adverse effects are frequent, but most are mild and many are transient. Continuing problems may respond to simple changes in pill formulation. Although it is not often necessary to discontinue medication for these reasons, as many as one third of all patients started on oral contraception discontinue use for reasons other than a desire to become pregnant. 

For the sake of simplicity the carcinogenic effects of estrogens in all formulations, including the combined oral contraceptives, are included here. 

A meta-analysis of epidemiological studies of ovarian cancer showed a summary estimated relative risk of 0.64 for ever-use of combined oral contraceptives, implying a 36% reduction in ovarian cancer risk (130). This protective effect increased with increasing duration of oral contraceptive use and continued for at least 10 years after discontinuation. Although most of the oral contraceptives reported in these studies were older, higher-dose formulations, the Cancer and Steroid Hormone (CASH) study included users of tablets containing ethinylestradiol 35 pg or less, and this subgroup of women had a reduced risk of ovarian cancer (115). 

There are some circumstances in which it is prudent to avoid using oral contraceptives, or in which frequent control of the state of the breasts is essential. These include (a) very long-term use before the first full pregnancy (b) prolonged use of high-dose formulations (c) uninterrupted use in women with a family history of breast cancer or with a personal history of fibroadenoma. 

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