Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020473 (hyperlipidemia)
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The present status of oral contraceptive steroids and the IUD, the 2 most effective and increasingly popular contraceptive methods (used by 41.6% of all U.S. married couples practicing contraception in 1970), is presented. Oral steroid contraceptives with varying quantity and activity of estrogen (ethinyl estradiol or mestranol) and progestogen (norethindrone, norethynodrel, ethynodiol diacetate, or norgestrel), are of 3 types: combination, sequential, and minidose progestogen alone. The most effective contraceptive available is the combined oral pill with a pregnancy rate of less than .2 % per 100 women after 1 year. Contraceptive action is exerted primarily through inhibition of ovulation and secondarily by alterations in cervical mucus, endometrial glands, the ovary, and in the oviduct and uterine muscle. In comparison, sequential oral contraceptives are less effective with greater side effects, and should only be used in women with amenorrhea. Effects of oral contraceptives other than contraception include those on the (1) the primary targets of the female reproductive system, (2) on other endocrine oragans and (3) on the remainder of the body. In the first group, changes may include transitory stromal fibrosis in the ovary, enlarged fibromyomata, intermenstrual bleeding or amenorrhea, increased amount of cervical mucus, polypoid hyperplasia of the endocervical glands, breast tenderness, and changes in lactation. Changes in the second category which may occur affect the adrenal glands, hypothalamus, the thyroid (increased thyroid-binding globulin), and pancreas (alterations in glucose metabolism). Effects on the rest of the body may include increase in serum lipids and changed atherogenic index, abnormalities in liver function, thromboembolism (incidence in oral contraceptive users 4.4 times that in non-users), melasma, alterations in the central nervous system with increased incidence of cerebral vascular accidents, hypertension, and increased body weight. Absolute contraindications to oral contraceptive therapy include cancer of the breast and uterus, pregnancy, active liver disease, hyperlipidemia, and history of gestational diabetes, thromboembolic phenomena or coronary artery disease. Relative contraindications include depression, migraine, myomata of the uterus, hypertension, epilipsy, oligomenorrhea and amenorrhea. Reliable epidemiologic data on IUDs from the Cooperative Statistical Program indicated first year pregnancy rate of 2.5%. Problems with the IUD include: 1) pregnancy with device in situ, which is associated with a higher incidence of spontaneous abortion; 2) ectopic pregnancy, which is prevented at a rate of only 90% compared with intrauterine pregnancies prevented in 97-98%; and 3) expulsions (20% of which are unnoticed), the expulsion rate being higher with decreasing age and parity, higher in the first than second year of use, and higher with smaller than larger devices. A major problem is discontinuation for medical reasons (15% rate in the first year), mainly bleeding and pain. Perforation, another serious complication, occurs initially at time of insertion with an incidence of 1 per 2500 insertions for the loop. IUDs were found to produce a sterile inflammatory tissue reaction, which is postulated as the primary causative factor for their contraceptive effect in humans.
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PMID:Current status of contraceptive steroids and the intrauterine device. 459 80

Low dose estrogen tablets, containing less than 50 mcg of ethinyl estradiol, were formulated because of the recognized dose response relationship with the steroid content of the tablet and side effects. These new oral contraceptives (OCs) are as effective as the older high-dose OCs, and available evidence reports fewer side effects. This discussion reviews pharmacology of these new OCs, the mechanism of action, contraindications, side effects, and problems with the low-dose estrogen OC. Ethinyl estradiol is the only estrogen used in the low-dose combination OC. There are several synthetic progestins: norethindrone, norethindrone acetate, norgestrel, levonorgestrel, and ethynodiol diacetate. These progestins have different potencies so the pharmacologic activity cannot be accurately predicted based on the amount present in the tablet. The synthetic steroids in OCs are absorbed in the small intestine, metabolized in the liver, excreted in the bile and feces with a half-life of 24 hours. The low-dose estrogen combination preparation is taken 3 out of every 4 weeks. Its contraceptive effect is primarily a result of hypothalamic mediated gonadotropin suppression with subsequent inhibition of ovulation. Contraindications to taking the low-dose OC are the same as for the higher dose OC: thromboembolic or cardiovascular disease, estrogen dependent neoplasia, markedly impaired liver function, undiagnosed genital bleeding, congenital hyperlipidemia, pregnancy, and women over age 30 who smoke. Relative contraindications include hypertension, diabetes mellitus, migraine headaches, uterine myomas, and epilepsy. The often quoted 2-5-fold increased incidence of thromboembolic disease, myocardial infarction, and stroke is based on large epidemiologic studies involving patients taking the older higher dose OCs. Current data from patients taking the newer low-dose medication demonstrate minimal if any increased incidence of these problems in young women who do not smoke. The low-dose estrogen OCs have minimal effect on lipid levels. Early reports of patients using the low-dose OC have shown little if any increased incidence of hypertension. The low-dose contraceptives have little effect on glucose tolerance, and there is no evidence to show an increased incidence of overt diabetes in OC users. There is no evidence that use of the combination OC causes an increase in cancer of the cervix, uterus, or ovaries. Clinical complaints of nausea, breast discomfort, chloasma, weight changes, and depression are reduced with the low-dose estrogen preparation. Hypomenorrhea while taking the OC occasionally occurs because the lower dose of estrogen is insufficient to stimulate the endometrial growth in face of the predominant progestin-atrophy effect.
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PMID:Oral contraceptives in 1984. 649 Mar 38