Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

At this time 3 triphasics are widely used in the US: Ortho-Novum 7/7/7, Tri-Norinyl, and Triphasil. Ethinyl estradiol is the preferred estrogenic agent for the triphasic products. Torethindrone and levonorgestrel were chosen as the progestins for the triphasic products. It is the combined effects of estrogen and progestin in the triphasics that provide their contraceptive action. Triphasil increases both the estrogen and the progestin at midcycle; Tri-Norinyl and Ortho-Novum 7/7/7 elevate the progestin only. The midcycle surges of estrogen and luteinizing hormone are dampened, and ovulation is inhibited. The triphasics represent a 98.7% reduction in total steroid content since oral contraceptives (OCs) were introduced. An estrogen dose of 30-50 mcg will inhibit ovulation, and side effects with such a dose are considered tolerable. The triphasic OCs are in this range. An estrogen dose of 20 mcg has been tested but is slightly less effective and is not recommended. Contraceptive failures have occurred with the triphasic products. In 1486 women studied, 6 pregnancies have occurred. Of these failures, one may have been because of a drug interaction with a barbituate. 1 pregnancy was due to patient failure; 3 consecutive pills were missed. Only 2 pregnancies were certain drug failures. Because of the gentle suppression of ovarian function, it has been observed that the menstrual flow is less affected than by standard OCs. Due to the fact that less total steroid is delivered and more endometrial shedding occurs, it is hoped that the triphasic preparations will have less of a "lingering" effect on the return to functional fertility. Most of the published data on side effects is available from the UK, North America, and Europe on the formulation known in the US as Triphasil. Nausea, vomiting, breakthrough bleeding, weight gain, and breast tenderness appear to be the most common side effects. The major medical reasons for triphasic discontinuation include breast tenderness, weight gain, breakthrough bleeding, nausea and vomiting, headache, and increased bleeding during the 1 week of withdrawal. Rifampin and phenobarbital are examples of drugs found to decrease pill efficiency, including triphasics. Also, a triphasic may interfere with the action of another drug. The new triphasics are appropriate when starting new patients on OCs. Patient counseling is essential. Due to the low margin of error as a consequence of lesser suppression of ovarian function, the patient needs to be well instructed in how to take the pill and advised of the consequences of missed tables.
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PMID:The triphasics: insights for effective clinical use. 382 67

40 women aged 18-36 used the Postinor brand, levonorgestrel-containing, pill from the Gedeon-Richter firm for 240 menstrual cycles. They did not have regular sexual intercourse: 26 were students, 2 were widows, 9 were women whose husbands commuted weekly to a workplace away from their home, and 3 were divorced. All of them had normal biphasic cycles validated both by basal temperature and hormonal cytology through 3 subsequent cycles. Average coital frequency during a menstrual cycle was 2.2. Every woman was instructed about the method of use: to take 1 pill, at the latest, 1 hour after coitus, and, if possible, maximum use should be once a week. In the event of repeated coitus, another tablet had to be taken 3 hours after coitus, and another the next day in case of another coitus. None of the women suffered form liver or gallbladder diseases. Before administering Postinor and 2 weeks after its use, hepatic tests and were done in all patients. The selected sample was nonsmoking, psychologically stable, and without bleeding disorders, and with normal colposcopic findings. The majority of women (25) experienced no side effects. 15 women (37.5%) had side effects: 6 (15%) had slight nausea, tachycardia, and a light headache. The spotting observed in 4 (10%) was controlled by Celaskon + 10% calcium gluconate iv 2-3 times. Omission of menstruation occurred in 4 cases, if the pill was taken several times in the second half of the cycle. There was 1 cases (2.5%) of failure because of belated use of the pill (2.5% hours after coitus). If properly used, Postinor proved to be an effective postcoital agent, without major side effects which could be recommended for occasional use.
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PMID:[Postcoital contraception]. 395 85

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

The efficacy, side effects, and biologic actions of the progestogen-only minipills marketed since February 1973 are reviewed. The preparations are: 350 mcg norethisterone (Micronor Ortho), 30 mcg d-norgestrel (Microlut Schering and Microval Wyeth), and 500 mcg lynestrenol (Exluton Organon). The efficacy of these drugs depends on motivation: Pearl indexes vary from 1.17-3.72 for norethisterone, .9-4.4 for d-norgestrel, and .8- 2.2 for lynestrenol. Some physiologic effects of minipills possibly related to their mode of action are impermeable cervical mucus and low levels of progesterone, pregnanediol, estrogen, and LH. The side effects influencing dropout most are spotting (40-55% in the first cycle), polymenorrhea (about 10%), and amenorrhea (about 5-10%). Some transient estrogenic side effects such as nausea, headaches, and breast pain may be due to estrogenic metabolites from lynestrenol and norethisterone. None of the severe estrogenic side effects, such as thrombophlebitis and impaired glucose tolerance and liver function, are characteristic of progestogen pills.
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PMID:[Minipill as the new contraceptive method]. 481 42

203 women 19-40 years of age were administered the gestagen preparations Volidan, Cyclofarlutal, Ovulen, Ciba AC-101, and Stediril as a contraceptive. 49 other women were administered these preparations as therapeutic and/or diagnostic measures in different gynecological complications. Side effects such as spotting, acylic bleeding, nausea, headaches and breast swelling were more frequent with the high-dose preparations such as Volidan and Cyclofarlutal. Intolerance to the preparation and subsequent discontinuation occurred only in a small percentage of the users. All of the preparations achieved 100% effectiveness as contraceptives. It is noted that these preparations were used with some success in treating dysmenorrhea, menometrorrhagia because of hyperplasia of the endometrium, and in severe climacteric syndromes. It has also been used as a pregnancy test. Constant medical control of the administration of these preparations is necessary both when they are used as contraceptives and as therapeutic measures, particularly in the case of young women.
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PMID:[Clinical aspects of the administration of gestagen preparations (Volidan, Cyclofarlutal, Ovulen, Ciba AC-101 and Steridil)]. 545 44

To study the safety and efficacy of a norgestrel-ethinyl estradol oral contraceptive compound, 300 Mexican women, 16-42 years of age were orally administered .5 mg norgestrel and .05 mg ethinyl estradiol (Ovral) daily over a total of 3175 study cycles. Most of the women were poor., uneducated and of high parity. None of the patients in the study became pregnant, even in the cycles where 1 or more doses were omitted. The menstrual cycle remained basically unaltered with breakthrough bleeding or spotting sometimes reported, usually when doses were missed. Unexplained amenorrhea occurred in 1.2% of the cycles. Though 5% of the women were ovulatory at one time of another as determined by pregnandiol levels, no pregnancy resulted, which is probably explained by changes in the cervical mucus caused by the pills making an inhospitable environment for sperm migration. Psychosomatic-related side-effects included nausea, headache and decreased libido in less than 1% of the cycles. Chloasma aggravated by poor dietary intake occurred in .5% of the cycles. No malignant, peripheral vascular or other serious disease occurred during the treatment and no significant endometrial alterations were seen.
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PMID:Norgestrel and ethynyl estradiol: a new low-dosage oral agent for fertility control. 563 91

264 women (about 50% private patients), all less than 40 years old and none with history contraindicating oral contraception, were started on a regimen with Ovral (.5 mg norgestrel and .05 mg ethinyl estradiol). Medication started on Day 5 of a menstrual cycle. Then therapy followed a 3 weeks on, 7 days off schedule. Patients continued for 1-22 cycles (mean 7 cycles) for a total of 1918 cycles. Despite the omission of 42 doses by 32 patients, no pregnancies occurred. The percentages of cycles with average flow, spotting, breakthrough bleeding, and dysmenorrhea were 74.4, 2.5, .4, and .6, respectively. The incidence of amenorrhea, .2%, was spectacularly low in comparison with findings in other studies. Papanicolaou smears (483) were all normal (Class I or II). Morphologic changes seen at endometrial biopsy (61) were similar to those produced by other available progestogen-estrogen compounds. No significant variation from control findings (1878) were found in 1463 laboratory studies. The studies included leukocyte and differential counts (724), and determinations of hemoglobin and hematocrit (388), fasting blood sugar and blood urea nitrogen (114), bilirubin and liver function (61), and renal function (176). Minor symptoms (nausea, vomiting, headache, etc.) were few and disappeared after the first few cycles. The preparation suppresses ovulation (probably through action of the estrogen), probably alters the cervical mucus to inhibit sperm penetration, possibly interferes with nidation, and may interfere with follicular development.
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PMID:Norgestrel, a low dose, oral progestogen for fertility contro. Supplementary report. 564 94

A total of 835 women in a Swedish multicenter study completed a total of 6472 oral contraceptive (OC) treatment cycles; half of the women were allotted at random to use the monophasic OC Neovletta, also known as Microgynon 30 (30 mcg ethinyl estradiol + 150 mcg levonorgestrel in each tablet) and the 2nd half was allotted to Trionetta, also known as Triquilar, Trigynon, and Logynon (6 tablets with 30 mcg ethinyl estradiol + 50 mcg levonorgestrel, 5 tablets with 40 mcg ethinyl estradiol + 75 mcg levonorgestrel and 10 tablets with 30 mcg ethinyl estradiol + 125 mcg levonorgestrel). The latter version was also present in a 28-day version containing in addition 7 placebo tablets to be used in the otherwise tablet-free interval. There was a comparatively high number of missed tablets. Tablets were omitted in 8.1% of the total number of cycles in the triphasic group and the corresponding figure for the monophasic group was 9.4%. Despite this fact, only 1 pregnancy occurred during the observation period and during treatment with Trionetta 21. This pregnancy was classified by the attending physician as clearly due to patient failure (3 consecutively missed tablets). Both formulations exerted a normalizing effect on cycle length, being more pronounced with the triphasic formulation. The 2 combinations reduced to the same extent previously prolonged bleeding periods, i.e., greater than 7 days. The percentage of women with bleeding periods longer than 7 days in the 6th and 12th treatment cycle was 1.4% and 0.6%, respectively, for Neovletta and 0.9% and 0.6%, respectively for Trionetta. The 2 combinations reduced to the same extent previously profuse bleedings. In the last untreated cycle, the percentage of women with profuse bleeding was 6.7% in the Neovletta group and 9.1% in the Trionetta group. Failure of getting withdrawal bleeding was rare in both treatment groups, but the triphasic formulation was found to be superior to the fixed dose combination. In the Neovletta group 85.9% completed the 1st trial period of 6 cycles. The corresponding figure for Trionetta was 83.9%. Acne and headache were, for both formulations, reported less frequently during treatment than in the last untreated cycle. 1 case of thrombophlebitis was reported during treatment with Neovletta. There was no statistically significant increase of the mean blood pressure or the mean body weight during treatment.
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PMID:Comparison of contraceptive acceptability of levonorgestrel and ethinyl oestradiol administered in one three-phasic (Trionetta) and one monophasic (Neovletta) version. 634 25

Contraceptive vaginal rings (CVRs), with approximate daily release rates of 250-290 mcg of levonorgestrel and 150-180 mcg of estradiol and manufactured in a shell design, were studied for effectiveness and acceptability in multicentered trials involving 1103 ring users in Brazil, Chile, Dominican Republic, Sweden, U.S., Denmark/Finland, and Nigeria. A comparison group of 533 women used the oral contraceptive Nordette. Both 1st and all segment 1 year gross pregnancy rates among CVR users were less than 3/100, rates similar to Nordette users. Continuation at 1 year was 50/100 users of the ring (all segments) and 38/100 among Nordette users, more of whom were lost to follow-up. Gross 1 year rates of termination for medical reasons ranged from 25-29/100. Ring users were more likely to terminate for vaginal problems and pill users for headache, nausea, and associated reasons. These trials indicate that CVRs of this design are as effective and have continuation rates equal to and possibly superior to Nordette under the same study conditions.
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PMID:A multicenter study of levonorgestrel-estradiol contraceptive vaginal rings. I-Use effectiveness. An international comparative trial. 645 8

Although no postcoital method has been developed for safe and effective regular use, postcoital contraception is being offered in Canada and Western Europe on an emergency basis to people who experience such problems as a burst condom. It is little known in the US, however. The 1st commercial version of a postcoital method recently became available to women in England. A former postcoital contraceptive was diethylstilbestrol (DES) which has been linked to cancer in the daughters of women who had taken the drug to prevent miscarriage. A new postcoital contraceptive regime was developed by Albert Yuzpe and consists of 4 ordinary contraceptive pills combining estrogen and progestin to be taken over a 12-hour period. In the US, this is the formulaion of birth control pill marketed under the trade name Ovral by Wyeth Laboratories. England and Germany are the only countries in which the Yuzpe method is officially approved for use as an emergency postocital contraceptive, but the method is used to some degree in most European countries, being well-known in France and Denmark. The most frequent side-effect reported by Yuzpe is vomiting experienced by 29% of women; another 22% felt nauseated. Other side effects, e.g. headache, were infrequent. The findings of the Pregnancy Advisory Service and the Brook Advisory Centre in Britain are reported. Overall very few side effects were found. Postcoital contraceptive treatment may cause the length of the cycle in which it occurs to be irregular. Treatment before day 15 has been found to shorten the cycle, whereas treatment after day 15 lengthens it. The majority of women who become pregnant due to treatment failure tend to seek an abortion. Ectopic pregnancy incidence may also be a result of treatment failure. In 1981, the International Planned Parenthood Federation (IPPF) issued a statement endorsing the use of postcoital contraceptives. Reasons for using them include rape, problems with barrier methods, ineffective use of the pill and IUD expulsion. No drug company in the US has expressed interest in getting FDA approval to market a postcoital contraceptive, partly because its usage might not be widespread. Opposition to approval from groups who believe life begins at conception and consequently that postcoital contraceptives are an abortifacient is expected.
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PMID:Contraception--the morning after. 651 38


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