Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00691 (EE2)
 7,802 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Medroxyprogesterone acetate (Provera) was administered orally during 2-4 days to women undergoing endometrial curettage during the follicular phase of the menstrual cycle. Estradiol (E2) receptor levels were estimated from the amounts of 2H-E2 tightly bound in nuclei after incubation of endometrial tissue with an excess of the labeled hormone. An average value (9 subjects) of 1.5 pmole E2/mg DNA +/- 0.7 (mean +1- SD) was found. This value is significantly lower than the average E2 receptor levels in proliferative endometrium of untreated subjects (3.2 +/- 1.3, n = 33) and equals the level observed in the early secretory phase (1.5 +/- 0.5, n = 5). These results indicate that one of the progestin effects on human endometrium is the reduction of E2 receptor levels.
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PMID:Effects of progestins on estradiol receptor levels in human endometrium. 16 81

Radioimmunoassay of serum medroxyprogesterone (MPA, Provera) in 7 wo men following oral and intravaginal administration is presented. The assay utilizes benzene: isooctane extraction, tritiated-MPA to assess procedural losses, goat-MPA-(O-carboxymethyl) oxime-bovine serum albumin serum, and dextran coated charcoal separation. Buffer and control serum blanks were indistinguishable from 0. 200 pg/ml of MPA was measurable with high reliability, and intra- and interassy coefficients of variation were 6 and 13%, respectively. Various amounts of MPA added to control serum were measured with accuracy. MPA levels in the 3 women who injested 10 mg of MPA rose to 3.4-4.4 ng/ml within 1-4 hours after oral intake and fell rapidly thereafter to .3-.6 ng/ml within 24 hours. MPA levels in the 4 women with Silastic intravaginal rings (IVRs) containing 100 or 200 mg of MPA rose rapidly after insertion, were rather stable (.9-1.6 ng/ml) while the IVRs were in place, and declined rapidly following IVR removal. Estradiol-17 beta and progesterone levels indicated that ovulation was consistently inhibited. The MPA levels in this study were approximately 5 times lower than those reported by others using a double-antibody radioimmunoassay of MPA in unextracted serum.
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PMID:Radioimmunoassay of serum medroxyprogesterone acetate (Provera) in women following oral and intravaginal administration. 119 24

The effects of hormonal contraceptive agents on the vascular system were studied in rats, dogs, and 34 women taking oral or injectable steroid contraceptive agents. Changes in the surface charge characteristics of the blood vessel wall and blood cells were observed. In dogs, the reduction in pore surface charge was greater in veins than in arteries. In rats, the induced mesenteric occlusion times were significantly reduced (p less than .001). However, Provera did not significantly reduce induced occlusion time in these animals (p greater than .01). Ov ral and Demulen lowered the mobilities of erythrocytes and platelets in women. Plasma coagulation times were not markedly altered in women receiving injectable progestin. Acitivated partial thromboplastin times were slightly decreased by Ovral and Demulen. The results suggest an increased tendency toward thrombosis in women taking steroid hormone contraceptive agents.
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PMID:Hormonal steroids: effects on the vascular system. 121

In 1989, researchers conducted a situation analysis of 100 service delivery points (SDPs) in Kenya. They wanted to evaluate the usefulness of collecting and analyzing data on factors that influence the impact of family planning (FP). FP workers took a gynecological history and blood pressure on 96% of new clients and did a pelvic exam on 73%. 80 SDPs had Depo-Provera and foam tablets on hand and 85 had condoms. Even though the Ministry of Health had 8 varieties of oral contraceptives (OCs), not all SDPs had all types. 97 SDPs had the OC Microgynon, yet 24 had 10 cycles. 53 SDPs had at least 1 FP poster on the wall. 38 had charts or other educational aids. None provided educational material for the clients to take home with them. 32 SDPs had health talks and only 16 addressed FP. 1 on 1 client counseling made up somewhat for this lack of information (31% of clients interviewed reported the clinic as their 1st source of FP information). Yet the SDP workers often did not tell clients about contraindications, complications, and how to manage complications. Supervision was minimal. 87 SDPs kept records on FP clients. 81 SDPs had referred some women for FP services. Only 54% of the nurses and midwives attended the core 7 week training course in FP designed to certify them to deliver FP services. A mean of 9443 clients attended these SDPs each month. 71% used OCs, 19% Depo-Provera, 5% condoms, and 5% IUDs and foam. 94% of clients learned of 2+ methods at the SDPs, especially OCs and Depo-Provera. FP workers provided little information about sterilization. The researchers observed the quality of care indicators on an 1 client/clinic basis which probably biased the results in a positive direction. Nevertheless, FP workers did know how to provide acceptable good care. These results showed that the quality of FP in Kenya should be upgraded from weak and poor to moderate to moderately high.
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PMID:The Situation Analysis Study of the family planning program in Kenya. 194 97

Researchers followed 68 women who attended the Family Welfare Clinic at the Kenyatta National Hospital in Nairobi, Kenya to determine if the low estrogen combined oral contraceptive (OC) Microgynon, a progestogen only OC, and Depo-Provera induce changes in the oral glucose test. These women did not take any steroidal contraceptives before entry into the study. Blood glucose levels were significantly higher after 60, 90 and 120 minutes than the control levels for women taking Microgynon. In addition, the mean areas under the glucose curves were substantially elevated after 1, 3, and 6 months above the control (p.002, .005, and .01 respectively). The only significant change in blood glucose levels in women taking the progestogen only OC occurred at 30 minutes after 6 months. Yet the mean areas under the curve were significantly higher than the control after ,1 2, and 3 months (p.005, .05 and .002 respectively). As for Depo-Provera, significantly lowered blood glucose levels only occurred after 1 month at 30, 50, and 90 minutes although no significant changes occurred after 1, 3, and 6 months in the mean areas under the glucose curves. Metabolic change occurred earlier and more often in Microgynon users than progestogen only OC users. This could be due to the progestogen levonorgestrel which has been shown to interrupt glucose metabolism. These changes could possible adversely effect women who are predisposed to developing diabetes, since 1 woman did develop a diabetic curve after 1 month of using Microgynon. Nevertheless no pattern towards abnormal glucose tolerance existed. Standard deviations of areas under the curves indicated that the number of women who develop glucose intolerance may increase with duration of use.
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PMID:The effect of low-oestrogen combined pill, progestogen-only pill and medroxyprogesterone acetate on oral glucose tolerance test. 214 46

Contraceptive development in the US has been halted by all but one company Ortho Pharmaceuticals. The reasons for this are complex and the problem is very serious. Legal and regulatory pressures have taken away the incentive to do research. There are 3 million unwanted pregnancies each year in this country. If contraceptive use were more widespread and the technology was constantly being improved by a highly competitive market, then this number would be much lower. There are several new forms of birth control being studies for use in the US, such as injectables using microspheres or microcapsules which can last for 1, 3, or 6 months, biodegradable pellets that are inserted under the skin of the hip or upper arm slowly release hormones, the vaginal ring which is saturated with time-released hormones and is worm around the opening of the uterus like a diaphragm, transdermal patches which are changed weekly for 3 weeks with a placebo patch to allow menstruation, osmotic pills which gradually release hormones on a lower and less frequent schedule, and vaccines which can immunize women against hormones in the placenta, egg or from sperm. This research is at an early stage. Luteinizing hormone-releasing hormone (LHRH) analogues suppress ovulation by affecting the pituitary gland. This method has the side effect of blocking ovarian production of estrogen and progesterone. Male methods like Inhibit inhibit the production of follicle-stimulating hormone (FSH). Gossypol has been used in China, but one side effect is that it is sometimes irreversible. Outside the US the injectables Depo-Provera and Noristerat are approved in 90 and 40 countries respectively. Norplant is a progesterone releasing implant, made in Finland, that lasts up to 5 years; it was recommended for approval in 1989 by the FDA's Fertility and Maternal Health Drug Advisory Committee RU-486 prevents the cells in the uterus from receiving progesterone, was developed in France. The Filshie clip is a titanium and silicone rubber barrier that blocks the fallopian tubes. Ovablock is a silicone plug that blocks the fallopian tubes and increase reversibility.
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PMID:Contraceptive development lags in U.S. 233 17

The androgen status of a hirsute woman can be diagnosed today by new techniques for measuring circulating androgens. Unfortunately, a battery of expensive tests is required to make this assessment. Two specific basic screening tests, DHEA-S and total free testosterone determinations, should be done. If the patient is interested in and can afford it, further testing can be done; it includes 17-hydroxyprogesterone, prolactin, compound S (serum 11-deoxycortisol) and cortisol measurements and a dexamethasone suppression test. Elevations of androgens, whereas elevations of testosterone can be due to ovarian or adrenal secretion. Establishing the site of androgen hypersecretion allows one to be more selective regarding the antiandrogen therapy. When excess androgen secretion is primarily adrenal in origin, adrenal suppression is effective with the use of such drugs as dexamethasone. If the excess androgen is primarily of ovarian origin, cyclic estrogens, for example, Demulen or Premarin with Provera, would be helpful. The evaluation of a hirsute patient takes time, interest, and knowledge of specific androgen-dependent cutaneous syndromes involving multiple possible enzymatic defects in the conversion of cholesterol to testosterone or intercellular pathways of androgen metabolism. If the dermatologist is not interested in or lacks the knowledge for such an evaluation, the patient is best referred to an interested endocrinologist.
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PMID:Hirsutism. 330 Nov 8

Serum lipid and apoprotein levels were determined in fasting women after longterm use (5-12 years) of Depo-Provera, Orgametril, Ortho Novum SQ, Binordiol, Microgynon-50, and Ministat. Compared with matched controls, pure progestogens (Depo-Provera and Orgametril) caused a moderate decrease of triglycerides (TG), HDL cholesterol, and Apo Al, whereas estrogen-dominant oral contraceptives (Ortho Novum SQ) increased the same parameters. The effects of longterm use of hormonal contraception on lipids did not differ from those predicted from short-term (6 months) studies.
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PMID:Effect of long-term hormonal contraception on plasma lipids. 404 61

Drug companies have been at work throughout the 1960s, 1970s, and 1980s trying to reduce the steroid content of their oral contraceptives (OCs). Researchers have been successful in reducing steroid content while maintaining effectiveness, thereby making OCs safer. In the 1st half of the natural menstrual cycle, a woman secretes estrogen as the dominant steroid product. In the 2nd half, estrogen is the principal reproductive hormone. Estrogens inhibit ovulation, possibly by inhibiting implantation, altering ovum transplant, or in some way preventing corpus luteum function, which is necessary to maintain early pregnancies and the endometrium. There are still only 2 estrogens and 6 progestins on the market today. They are probably the most thoroughly studied chemical ever seen in the history of pharmacy or medicine. 1 of the estrogens, mestranol, is really a drug of the past. In the body, mestranol is converted to ethinyl estradiol, the other estrogen on the market. Consequently, there is no reason to use mestranol itself. Within the dose range of 50-100 mcg, there's little difference in contraceptive effect. Progestins are the other active ingredient in the combination OC. Their principal action is the thickening of the cervical mucus, which prevents sperm penetration. Also, with sufficient progesterone, ovulation is inhibited, but this happens in only 40% of those patients taking, for instance, the "mini-pill" (which consists of progesterone only). The progestins and the estrogens work in concert to make OCs a highly effective contraceptive method. Recent surveys conducted by the Centers for Disease Control and National Cancer Institute looked into the relative effectiveness of OCs. Nordette had a use effectiveness failure rate of 3.5; Ovral, 3.6. Loestrin 1/20 -- norethindrone acetate, 1 mg, and estinyl estradiol, 20 mcg -- shows a failure rate of 4.5. This indicates that the threshold for an effective dose of estinyl estradiol in OCs is 30 mcg. For 1 mini-pill, Ovrette, the failure rate is 9.5 -- much higher. Depo-Provera has a failure rate of 0.7. The primary complaint from women taking OCs is spotting and breakthrough bleeding during the cycle. 30-50% of women given OCs stop taking them within a year. OC side effects include nausea, fluid retention, breast tenderness, leukorrhea, hypomenorrhea, headaches, spotting around the face, hypertension, and visual changes. 1 of the risks of birth control pills may be cervical dysplasia -- changes in the cells of the cervix. The relative risk of cervical cancer with OCs after 5-9 years is approximately 1.8. Clinical cases of deep vein thrombosis number 1/1000 per year among nonusers of OCs. Among users, the rate is 3 times as high: 3/1000. The most serious potential adverse effect is myocardial infarction. Of the excess deaths attributed to OCs (23.3 total per 100,000 users), 22.7 are due to myocardial infarctions and hemorrhage. The discussion also briefly reviews other methods of contraception -- Depo-Provera, male contraceptives, implants, the diapragm, and IUDs.
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PMID:Prescription contraceptives: countering the risks. 405 Jun 70

A 21-year-old unmarried female, with a history of periodic psychotic behavior, was admitted to the hospital after exhibiting overt psychotic symptoms. Several months of hospital observtion and a review of her earlier psychotic episodes suggested that the patient's psychotic behavior was associated with the onset of menses. The symptoms disappeared after oral contraceptives were administered on a regular basis. The patient experienced her 1st psychotic episode 1 year after menache. Several episodes during the intervening years required hospitalization. One of these episodes occurred during a period of prolonged menstrual flow. The patient's menstrual cycles were frequently irregular. During the present hospitalization the patient exhibited psychotic symptoms at the onset of 3 of her 4 menstrual cycles. She became agitated and delusional and exhibited dissociated thought patterns and autonomic symptoms. Despite the use of high doses of antipsychotic drugs, the symptoms persisted until the menstrual flow stopped 7 days later. After the 3rd episode the patient did not menstruate for 2 months. 69 days after the onset of her last menstrual flow the patient was given Provera to induce menstruation. 5 days later the menstrual flow began and Ortho-Novum 1/50 was administered. During the next 6 months she took the contraceptive regularly and remained free of any overt symptoms. The mechanism by which oral contraceptives prevent menstrual psychosis is unknown. Perhaps the estrogen decreases monoamine oxidase activity which in turn alters the level of norepinephine at the synapses.
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PMID:Prevention of recurrent menstrual psychosis by an oral contraceptive. 610 29


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