Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00627 (MAP)
 15,705 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A WHO sponsored comparative trail (9 centers) studied the bleeding patterns and side effects experienced by 1678 women using injectable (every 12 weeks) norethisterone enanthate (NOR) and depot-medroxyprogesterone (DMPA). 388.8 women-years of menstrual experience with NOR and 372.5 with DMPA were studied. The percentage of women with total amenorrhea with DMPA was significantly higher than with NOR for all injection intervals. The porportion of women with total amenorrhea increased significantly over time with both drugs (chi-square=33.9 for NOR and 73.4 for DMPA; P .001). After 1 year, 35% of DMPA and 8.6% of NOR users had total amenorrhea. With NOR, the cycle length distribution changed markedly over time, with the percentage of short cycles under 25 days diminishing as the percentage of long cycles in excess of 46 days increased. In contrast, DMPA held cycle length patterns more or less constant. Length of bleeding and spotting episodes were significantly greater with DMPA. The mean number of bleeding/spotting days decreased over time with both drugs; the difference from the 1st to 4th injection was statistically significant (P .001). Though the overwhelming majority of women experienced abnormal cycles with both drugs, the percentage of normal cycles remained fairly constant during consecutive intervals. Headache was the most frequently reported complaint: 10.7% of DMPA and 6.9% of NOR users. Other nonmenstrual side effects were reported with similar frequencies in both groups.
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PMID:Multinational comparative clinical evaluation of two long-acting injectable contraceptive steroids: noresthisterone oenanthate and medroxyprogesterone acetate. 2. Bleeding patterns and side effects. 65 7

Five hundred Black Rhodesian women given injections of 150 mg Depo-Provera every 3 months (group A) and 500 women given an injection of 450 mg Depo-Provera every 6 months (group B) were reviewed after 6 months. Group B had a significantly lower rate of defaulters. There was no significant difference between the groups with regard to weight gain, systolic and diastolic blood pressure increase, overall abnormal bleeding patterns and complaints of side-effects. Among those women who reported abnormal bleeding patterns, significantly more in group B had amenorrhoea. There was no significant increase of prolonged bleeding in group B. Among those women who complained of side-effects, significantly more in group B complained of headaches and a bloated abdomen. No pregnancies occurred in either group. The increased annual cost of the 450 mg injections, which was the main reason for women not accepting this regimen, is outweighed by convenience and reduced travel costs. Depo-Provera 450 mg given by 6-monthly injection is well tolerated and effective, and appears to be even more satisfactory as regards continued acceptance than 150 mg given every 3 months.
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PMID:Efficacy and acceptability of injectable medroxyprogesterone. A comparison of 3-monthly and 6-monthly regimens. 69 38

The US Food and Drug Administration (FDA) has not approved any injectable contraceptives, but, in December 1990, it approved Norplant, an implantable contraceptive. Family planning providers insert 6 capsules, each with 36 mg levonorgestrel, in a fan shape under the dermis of the upper arm. Norplant protects against pregnancy for at least 5 years . Fecundity returns within 2 weeks after capsules' removal. The steady low levels of levonorgestrel keep down both luteinizing hormone and follicle stimulating hormone levels. It suppresses ovulation and thickens the cervical mucus. Contraindications of Norplant are active thromboembolism, undiagnosed genital bleeding, acute liver disease, liver tumors, and breast cancer. Phenytoin and other drugs which speed up liver metabolism reduce Norplant's efficacy. The leading side effect of Norplant is irregular bleeding patterns. Some less common side effects include headaches, nervousness, dizziness, and acne. First year continuation rates range from 76 to 99% and 25 to 78% for 5 years of use. More than 85% of Norplant users are satisfied. Both continuation and satisfaction are associated with patient counseling. Research and development of biodegradable and other nonbiodegradable implants is ongoing. The most common injectable contraceptive in the world is Depo-Provera. 150 mg of Depo-Provera every 3 months suppresses ovulation, deteriorates the endometrium, thickens cervical mucus, and reduces motility of the tubes, thereby providing adequate protection against pregnancy. Some research shows Depo-Provera use significantly increases the low-density lipoprotein to high-density lipoprotein ratio, thereby increasing the risk for atherogenesis. Effectiveness rates match those of Norplant. Norethindrone enanthate was the first injectable contraceptive. Even though 40 countries approve it, the US does not. Animal studies of injectable microspheres or microcapsules with either progestogen or progestogen and estrogen are in progress.
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PMID:Injectable and implantable contraceptives. 138 11

To assess the contribution of gonadal steroids to sexual behavior in aging women, we conducted a 10-week, double-blind, hormone replacement study of 40 naturally menopausal women (mean age, 58.3 yr). Prospective measurements of basal and stimulated vaginal vasocongestion and daily self-reports of mood, physical symptoms, sexual behavior, and perceived sexual pleasure were collected. Daily treatments were either conjugated equine estrogen, i.e. Premarin (P; 0.625 mg), Premarin and medroxyprogesterone acetate, i.e. Provera (PP; 0.625 and 5 mg, respectively), Premarin and methyltestosterone (PT; 0.625 and 5 mg, respectively), or placebo (PL). Compared to placebo, hormone treatment had significantly reduced hot flashes in the P and PP groups by week 4 and in the PT group by week 5. Headaches were reduced in the P vs. PL group, only. Hormone treatment did not significantly alter mood ratings, sexual behaviors, or psychophysiologically measured sexual arousal. PT treatment significantly increased reports of pleasure from masturbation compared to the other three groups, underscoring the apparent contribution of androgens to self-stimulatory behavior. However, the data suggest that in these physically and sexually healthy women, gonadal steroids do not influence major components of sexual functioning, including arousal and a wide variety of sexual activity and experience.
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PMID:Effects of estrogen, androgen, and progestin on sexual psychophysiology and behavior in postmenopausal women. 169 Jul 46

Oral contraceptives (OCs, long-acting progestins (LAPs), and IUDS are reviewed in terms of new information on safety and efficacy. OC formulations are described and their mechanism of action and efficacy indicated. Reports are provided for thromboembolism, hemorrhagic and thrombotic stroke, ischemic heart diseases, alterations in lipid and hypoprotein and carbohydrate metabolism, hypertension, coagulation changes, breast and cervical cancers, and such minor side effects as menstrual irregularities, nausea, headaches, weight gain, premenstrual syndrome effects, and mood and libido changes. Noncontraceptive health benefits and clinical considerations are discussed. Norplant, as the only long acting progestin available in the US is described in terms of its formulations, mechanism of action, sequelae and metabolic effects, menstrual irregularities, metabolic effects, nuisance side effects, candidates for insertion, method of insertion and removal, and continuation rates. 2 IUD types are identified as the only ones available in the US, Progestasert T and T-Cu-380A (Paragard). Mechanism of action, efficacy, candidates, major sequelae such as salpingitis, infertility, and uterine perforation, minor sequelae such as metrorrhagia and dysmenorrhea, and other considerations are indicated. OCs in the US contain an average of 35 mg of ethinyl estradiol and assorted progestins e.g.s, ethynodiol diacetate, norethindrone acetate, nortestosterone derivatives with a complex mechanism of action. The failure rate for use effectiveness is 6 pregnancies/100 woman years. Modern formulations have combined rates of no more than 50 to 100 adverse events/100,000 users. Some of the effects are indicated as follows: Thromboembolism accounts for 60% of adverse effects and appears to be declining along with hemorrhagic and thrombotic stroke, however, modern use studies are only partially available. Myocardial infarction related to OC use may be embolic, and has a low risk at 7/100,000 users. Low-dose contraceptives substantially reduce the associated risks. Those with risk factors need close monitoring. Norplant is useful for those not wanting to take a daily regimen and is commonly accompanied by menstrual irregularity and sometimes headaches. Continuation is 80% after the 1st year and 40% after 5 years. Candidates for IUDs are parous women in monogamous relationships, who are not at risk for salpingitis, which is related to IUD use, or sexually transmitted diseases. Continuation is 70% after 1 year compared with 50% of OC users.
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PMID:Modern trends in contraception. 212 11

Medroxyprogesterone acetate injections (Depo-Provera) were given to 625 women at 3 monthly intervals involving 693 episodes. Ages at entry to the study ranged from 15-51 years with the majority in their 20s and a mean age of 30. Length of exposure ranged from 3-168 cycles. 4 women have received more than 160 continuous cycles of DMPA. Of the medication-induced reasons for discontinuing DMPA, bleeding was the most common with an incidence of 10.5% followed by depression (1.4%), weight gain (1.4%), and loss of libido (1.6%). No patient ceased treatment because of headaches, recurrent vaginal infections, mastalgia, nausea, chloasma, hypertension, or other vascular illnesses. The 59 women who move away or were lost to follow-up accounted for 405 cycles of treatment. The solitary unplanned pregnancy occurred in a 28-year-old obese woman who had previously had other method failures, once with an IUD and once with oral contraceptives (OCs). No association was found with carcinoma of the cervix. Of 80 women ceasing treatment to become pregnant, only 1 women has required the assistance of chlomiphene and conceived 2 years after ceasing DMPA. Amenorrhea was the side effect most appreciated by the women using DMPA. Due to the problem of irregular bleeding, it is wise to warn prospective patients about the lack of bleeding control that they have 1 chance in 10 of having relative menorrhagia. Women using OC subject to frequent vaginal moniliasis had a marked reduction in episodes after switching to DMPA. Chloasma, 1 of the minor stigmas of OC, was not induced in any of the patients. DMPA is a safe and efficient reversible method of contraception for women who have various gynecological conditions or problems associated with using OCs.
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PMID:Medroxyprogesterone acetate as an injectable contraceptive. 296 70

Synthetic progestins derived from nortestosterone provide a promising contraceptive alternative for women with contraindications for estrogens. Progesterone and synthetic progestins reduce vasodilatation and edema induced by estrogens and stop estrogen-dependent cellular multiplication in target tissue. Progestins have 2 kinds of contraceptive affect: antigonadotropic action at sufficient doses, and peripheral action at lower doses. The cervical mucus is modified in composition and volume, becoming hostile to sperm; the endometrial mucus atrophies; and tubal motility is slowed. High dose progestins are administered from the 5th or 10th to the 25th cycle day, with the earlier date preferred for women with shorter cycles. They are an ideal method for women with endometrial hyperplasia or benign breast disease or histories of breast or uterine cancer, as well as for women over 40 with dysovulatory cycles. Contraindications to high dose progestins include obesity, hypertension, lipid metabolic anomalies, and diabetes. Low dose progestin-only pills are administered at the exact same time each day including during menstruation. They are attractive for some women because they contain no estrogen, a reduced progestin dose causing fewer headaches and less somnolence, and fewer metabolic effects. Low dose progestins are indicated for lactating women, those with contraindications to estrogens such as obesity, hypertension, hyperlipidemia, and diabetes, and those with renal or cardiac insufficiency with valvulopathy. Low dose progestins are also indicated for nulliparas and other women for whom IUDS are contraindicated. Women using low dose progestins should never take drugs that act as enzymatic inductors, which speed hepatic degradation of steroids and reduce their efficiency. A resulting pregnancy is likely to be extrauterine because of slowed tubal transport. The failure rate of low dose progestins ranges from .9-3%, with higher failure rates among younger women. About 30% of users initially experience spotting, which despite its usual disappearance after 2-3 months of use is the most common reason for discontinuing the method. Low dose progestins have no metabolic or vascular effects, but they may cause a relative hyperestrogenism is some users. Other modes of administration of progestin contraception include continuous high doses, never justified solely for contraception. Trimonthly injections of medroxyprogesterone acetate of norethindrone enanthate provide contraception through a long lasting antigonadotropic effect. Metrorrhagia and amenorrhea are among possible side effects. The method is used primarily in developing countries where its ease of use is a major advantage. Subcutaneous implants releasing continuous doses of levonorgestrel provide contraceptive protection for over 5 years. The cumulative failure rate is 1.7 at 5 years. Metabolic tolerance is good. The major side effect is menstrual irregularity.
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PMID:[Progestational contraception]. 365 94

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 study involving an injectable contraceptive regimen utilizing 2 commercially available hormonal preparations, medroxyprogesterone acetate (Depo-Provera, The Upjohn Company) and estradiol-17 beta-cyclopentylpropionate (Depo-Estradiol Cypionate, The Upjohn Company), is described. 90 multigravidas received intramuscular injections of 50 mg of medroxyprogesterone acetate and 10 mg of estradiol-17 beta-cyclopentylpropionate as a contraceptive every 5 weeks, for a total of 1155 periods. The injections were found to be safe and completely effective. In 15% of the therapeutic cycles, bleeding did not appear for a period of 30 or more days. In 14%, bleeding and/or spotting lasted for longer than 9 days during a 30 day period. The incidence of aminorrhea increased somewhat after the first 10 months of treatment. Endometrial biopsies showed a "suppressed" endometrium. Adrenal pituitary responsiveness to metyrapone was found to be normal in 17 of 21 patients tested. Although almost half of the patients presented some complaints during the study, these were mostly transient and minor in nature. Headache was the complaint most frequently observed (14%), but it was generally limited to 1 cycle. The monthly injectable contraceptive regimen may be useful in a particular population of patients who, for various reasons, cannot tolerate or cannot be relied upon to take oral contraceptives. The authors believe that because of the high incidence of alterations in the bleeding pattern while on the therapeutic regimen, as well as the frequent occurrence of aminorrhea following discontinuation of therapy, the use of such a contraceptive regimen in the general population might not be desirable.
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PMID:Evaluation of an injectable progestin-estrogen as a contraceptive. 491 52

The article reports on 33 insertions of the progesterone-releasing IUD, Progestasert, in patients aged 17-45 with an average age of 31; most patients had 2 children. Insertion of the device was easy, and the device itself was extremely well tolerated; 12 of the original 33 patients carried the device for more than 24 months, and 5 carried it for more than 36 months. There were no pregnancies, 2 cases of spontaneous expulsion, 2 removals for pelvic pain, and 2 for desire of pregnancy. Not only were there no side effects, but a positive action of the device was noted against genital inflammation, together with marked improvement of mammary tension and intramenstrual occurrence of headache. Vaginal cytology remained normal or it improved.
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PMID:[A new intrauterine device with progesterone for control of reproduction]. 732 25


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