Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
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Pregnon is a new low-dosage ovulation-inhibiting agent containing 1 mg of lynestrenol and .05 mg of ethinyl estradiol in each tablet. It is also marketed under the name of Pregnon 28 or Ovostat 28 in which each package contains 22 active plus 6 placebo tablets. Data were collected from Belgian clinics and evaluated by the Medical Unit of Organon in Belgium and the Netherlands. During this study, 639 women of fertile age were monitored through 9159 cycles. The maximum period of treatment was 36 cycles. Clinical and gynecological examinations were made before treatment and then every 2 or 3 months. Treatment was begun by taking the 1st tablet on the 1st day of menstruation. After taking 22 tablets there was a 6-day tablet-free interval during which withdrawal bleeding usually occurred. The intensity of the withdrawal bleeding was normal in 57.3%, slight in 41.7%, and heavy in 1%. Spotting was noted in 3.1% of the cycles and breakthrough bleeding occurred in 2.9%. Usually they occurred in the first 3 cycles. Amenorrhea was observed in 2.9% of the cycles. Body weights were relatively unchanged. Blood pressures remained the same. Side effects were headache, nausea, vomiting, breast tenderness, heavy legs, leucorrhea, nervousness, depression, and decreased libido. Only 46 patients discontinued treatment because of these drug effects yielding an acceptability level of about 93%. Since no pregnancies occurred during this study, the Pearl index was 0.
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PMID:Clinical evaluation of a new oral contraceptive, 'Pregnon'. 114 83

Research in the area of oral contraception currently focuses on the development of selective progestogens that combine targeted progestational and antiovulatory activity with a minimal potential for androgenicity. The present dual-center study was conducted to investigate the efficacy, tolerability, and safety of a new monophasic oral contraceptive (OC) containing 250 micrograms norgestimate in combination with 35 micrograms ethinyl estradiol (Ortho-Cyclen or Cilest). Ninety-seven healthy women of childbearing age participated in the study: 37 received the new norgestimate/ethinyl estradiol combination OC as primary therapy and 31 were switched over from other OCs. The norgestimate/ethinyl estradiol formulation was well tolerated and was associated with excellent cycle control. After six cycles of use, there were no statistically significant differences in the incidence of spotting or breakthrough bleeding compared with baseline, nor were there any significant changes in the incidence of headache, nausea, or mastalgia. Body weights remained constant for the duration of the study, as did systolic and diastolic blood pressures. Of particular note was the absence of any statistically significant alterations in metabolic parameters, including blood glucose or lipoprotein levels. These findings are consistent with the results of several other European studies and indicate that the norgestimate/ethinyl estradiol combination OC combines superior cycle control with minimal risk of androgenic side effects.
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PMID:Clinical experience with a new norgestimate-containing oral contraceptive. 134 20

In addition to oral contraceptives (OCs), the morning-after pill, the minipill, and depot preparations also belong to hormonal contraceptives. The latter two contraceptives have not become established among young women because of inadequate cycle control. For postcoital contraception in Austria, Neogynon and Stediril-D, consisting of 0.05 mg of ethinyl estradiol (EE) + 0.25 mg of levonorgestrel, are used within 48 hours of unprotected intercourse. Lower dose OCs have considerably reduced the risks of side effects. Micropills are the optimal OCs with EE under 50 mcg combined with the new generation of gestagens. The beneficial effects include menstrual regularity and the prevention of anemia, ovarian cysts, and fibrocystic mastopathy. Nausea, headache, spotting, and weight gain do occur in individual cases, even among young people. The potential risk of thromboembolism is the most important, although arterial cardiovascular risk is minimal in young age. The probability of postpill amenorrhea is less than 1%. Micropills can be used by young diabetics provided the disease is not beyond 10 years' duration and there is no angiopathy. Acne, seborrhea, and hirsutism are beneficially influenced by a combination of 0.035 mg of EE with 2 mg of cyproterone acetate. The relative risk of endometrial and ovarian cancer are only about half as high among OC users as among nonusers. The risk of breast cancer in young OC users has not been conclusively explained. Regular colposcopy and cytology is recommended for young OC users to preclude the risk of malignancies of the genital tract. Sex education and the use of OCs that are the most suitable and effective for young people can reduce the number of unwanted pregnancies and abortion. The comparison of two 5-year periods in the 1970s and 1980s at the University Obstetrical-Gynecological Clinic in Graz showed that the incidence of births among women under 18 years of age decreased from 3.6% (778) to 1.6% (353).
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PMID:[Benefits and risks of hormonal contraception]. 146 64

Estrogens, gestagens, or estrogen-gestagen combinations can be employed as postcoital oral contraceptives. High dose estrogens, such as 5 mg of ethinyl estradiol (EE) daily for 5 days started at the latest 72 hours after unprotected coitus have been proved quite effective with a failure rate of about 1%. However, in about half of the women nausea and in one=third vomiting occurred. Among gestagens the highly effective 19=testosterone preparations are notable. Most experiences pertain to norgestrel (Razemat) as well as to the twice as effective levonorgestrel (D-(-)-norgestrel) LNG. After unprotected coitus, 0.6 mg of LNG taken within 12 hours but possibly even after 1-3 hours is effective. It is common to use a combination of 0.25 mg of LNG and 0/05 mg of EE (Tetragynon). 2 tablets are taken within 48 hours after unprotected intercourse and 2 more 24 hours later. In 4 large studies in Canada and the US with a total of 1540 women who were given instead of LNG the double dose of the half so effective Razemat, the pregnancy rate was 0.9% (14 pregnancies) and the corrected failure rate was 0.65% after excluding women with several unprotected exposures. Assuming a probability of pregnancy of up to 30% after unprotected intercourse depending on the day of the menstrual cycle, the action of the gestagen=estrogen preparation can be regarded as reliable. The side effects are less frequent compared with the high-dose EE therapy. In an Austrian study of 50 women taking Tetragynon, 11 women had nausea, 2 had breast tension, and 4 had vomiting. The duration of bleeding lasted an average of 2 days longer after the taking the pill. 2 women who vomited 2 hours after taking the 1st Tetragynon dose became pregnant. Therefore, in case of nausea it is recommended that an antiemetic be given, and in case of vomiting, the 1st dose of Tetragynon has to be repeated to assure an effective action.
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PMID:[The postcoital pill]. 150 66

Mifepristone (RU 486) is a synthetic steroid with potent antiprogestational and antiglucocorticoid properties that offers an effective medical means of inducing abortion in early pregnancy. Since progesterone is essential for implantation, the authors tested the use of mifepristone for emergency postcoital contraception. 800 women and adolescents were studied who requested emergency postcoital contraception and who had had unprotected intercourse within the preceding 72 hours. A total of 398 women and adolescents were randomly assigned to treatment with 100 mcg of ethinyl estradiol and 1 mg of norgestrel, each given twice 12 hours apart (standard therapy) and 402 women and adolescents who were randomly assigned to receive 600 mg of mifepristone. None of the women or adolescents who received mifepristone became pregnant, as compared with 4 of those who received standard therapy; the difference in failure rates between the 2 regimens was not statistically significant. The number of pregnancies in each group was significantly lower than the number expected according to calculations based on the day of the cycle during which intercourse had taken place (p0.001). In many subjects, the stage of the cycle as calculated by menstrual history was inconsistent with measurements of plasma progesterone or urinary pregnanediol excretion. The subjects treated with mifepristone reported less nausea (40% vs. 60%) and vomiting (3% vs. 17%) on the day of treatment, as well as lower rates of other side effects, than those subjects treated with the standard regimen. However, they were more likely to have a delay in the onset of the next menstrual period (42% vs. 13%). Mifepristone is a highly effective postcoital contraceptive agent which, if more widely used, could help reduce the number of unplanned and unwanted pregnancies.
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PMID:Mifepristone (RU 486) compared with high-dose estrogen and progestogen for emergency postcoital contraception. 848 75

55 women took the combined oral contraceptive Minulet (30 mcg ethinyl estradiol and 75 mcg gestodene) for 42 consecutive days, using 2 active pill strips, to lengthen the interval between withdrawal bleeding and assess acceptability. The study was an open multi-center trial in which 38 general practitioners each supervised 1 or 2 women. The women averaged 27 years old (range 18-40), and had used Minulet without problems for the previous 6 months. 10 women noted spotting, and 2 had breakthrough bleeding, both after Day 21 of pill intake. There was 1 dropout for unrelated medical reasons. Other minor side effects were breast tenderness (7%), nausea (4%), abdominal bloating (4%), headache (2%), and dysmenorrhea (2%). 92% of the women reported extreme to moderate satisfaction, but 4% were not satisfied because of breakthrough bleeding. Nevertheless, these data on breakthrough bleeding were much lower than published data from trials with other combined pills, especially those containing levonorgestrel.
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PMID:The acceptance of a 7-week cycle with a modern low-dose oral contraceptive (Minulet). 155 35

The forms of administration, mechanisms of action, side effects and complications, and other aspects of female hormonal contraception are set forth in this "lesson" for medical students. Female hormonal contraception has been in use for over 30 years and is used by more than 150 million women worldwide. Oral contraceptives suppress the preovulatory peak of follicle stimulating hormone and luteinizing hormone, preventing ovulation and follicular maturation. Progestins render the cervical mucus impermeable to sperm and modify the endometrium so that it will no longer support implantation. The synthetic estrogen ethinyl estradiol is used in most combined oral contraceptives (OCs). Among the numerous progestins in use are the newer desogestrel, gestodene, and norgestimate, which have fewer androgenic and metabolic effects than did the 1st generation. the different forms of administration of hormonal methods include combined OCs, oral preparations containing low doses of progestin continuously administered or high doses continuously or discontinuously administered. Intramuscular injection of progestins and the so-called "morning after" postcoital pills are less often prescribed. The combined preparations may be monophasic, biphasic, triphasic, or sequential. Sequential preparations should be avoided because of the hyperestrogenic climate they induce. The low-dose progestin preparations are indicated for women with contraindications to synthetic estrogen. They must be taken at the same time each day and have a relatively high rate of side effects, especially ovarian and breast cysts and irregular bleeding. High-dose progestin preparations have significant metabolic effects and are indicated primarily for patients with gynecological problems such as fibromas and endometriosis. Intramuscular injection of medroxyprogesterone acetate every 3 months is effective but has the same side effects as high-dose progestins. It is indicated primarily for patients unable to control their own behavior. The hormonal methods are all highly effective in preventing pregnancy when correctly administered. Side effects may be minor problems, such as nervousness and nausea, that are usually of short duration. the more serious side effects, including modifications of lipid or carbohydrate metabolism, hemostasis, blood pressure, or hepatic functioning and cardiovascular effects, have been reduced with the new lower dosed formulations. Absolute contraindications to hormonal contraception include undiagnosed vaginal bleeding or amenorrhea, history of thromboembolic or cerebral vascular accidents, severe cardiopathy or hypertension, hyperlipidemia, hepatopathy, hormonodependent cancer, pituitary tumors, porphyria, and severe mental problems. Relative contraindications impose the need for careful monitoring and follow-up. The practitioner should be aware of the possibility of interactions between OCs and certain other drugs.
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PMID:[Hormonal contraception]. 160 74

The efficacy and tolerability of a new oral contraceptive, norgestimate/ethinyl estradiol (250 micrograms of norgestimate/35 micrograms of ethinyl estradiol; Cilag GmbH Research, Sulzbach, Germany) were examined in an open-label study of 59,701 women who were evaluated during 342,348 menstrual cycles; 42,022 women completed the planned treatment regimen of six cycles. A use-efficacy (overall) Pearl index of 0.25 pregnancies per 100 woman-years was calculated based on 342,348 cycles. Tolerability was assessed for all women who completed six treatment cycles. Reductions in mean cycle length and duration of bleeding were noted; 32% of the women experienced reductions in the intensity of bleeding by the end of cycle 6. After six cycles of use, amenorrhea occurred in 1%, spotting in 4%, and breakthrough bleeding in 3% of the participating women. Treatment with norgestimate/ethinyl estradiol had minimal effects on weight, blood pressure, pulse, lipid metabolism, and blood glucose. Adverse effects (acne, nausea, or headaches) occurred at low frequencies and in many cases, were reduced compared with pretreatment levels. The results of this large-scale open trial were comparable with results from two other multicenter trials of the same formulation.
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PMID:The efficacy and tolerability of norgestimate/ethinyl estradiol (250 micrograms of norgestimate/35 micrograms of ethinyl estradiol): results of an open, multicenter study of 59,701 women. 160 86

Research in the area of oral contraception currently focuses on the development of selective progestogens that combine targeted progestational and antiovulatory activity with a minimal potential for androgenicity. The present dual-center study was conducted to investigate the efficacy, tolerability, and safety of a new monophasic oral contraceptive (OC) which contains 250 mcg norgestimate in combination with 35 mcg ethinyl estradiol (EE; Ortho-Cyclen or Cilest). 97 healthy women of childbearing age were part of this study; 37 received the new norgestimate/EE combination OC as primary therapy and 31 were switched over from the other OCs. The formulation was well-tolerated and was associated with excellent cycle control. After 6 cycles of use, there was no statistically significant difference in the incidence of spotting or breakthrough bleeding as compared with the baseline. Nor were there any significant changes in the incidence of headache, nausea, or mastalgia. Body weights remained constant for the duration of the study as did systolic and diastolic blood pressures. Of particular interest was the absence of any statistically significant alterations in metabolic parameters, including blood glucose or lipoprotein levels. These findings are consistent with the results of several other European studies and indicate that the norgestimate/EE combination OC combines superior cycle with minimal risk of androgenic side effects.
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PMID:Clinical experience with a new norgestimate-containing oral contraceptive. 167 78

Health workers took blood samples from 41 black women living in the greater Harare area of Zimbabwe before they began taking a combines oral contraceptive (OC) with 30 mcg ethinyl estradiol and 150 mg desogestrel (Marvelon formulation) and 3, 6, 9, and 12 months after taking it to conduct metabolic tests. They also recruited 190 other black women from Harare and rural Chiweshe, Mazowe, and Domboshawa populations taking the same new generation progestogen-containing OC to determine the efficacy, acceptability, and safety of the OC. Only high density lipid (HDL) cholesterol levels rose considerably between pretreatment and 12 months (0.94-1.3 mmol/ml; p.05). Low density lipid (LDL) cholesterol levels remained basically the same. This accounted for the significant rise of the HDL cholesterol/LDL cholesterol ratio over 12 months from 0.41 to 0.61. Triglyceride levels did not rise significantly and always stayed within the normal range. No woman became pregnant during the clinical trial. 2% experienced minor side effects including backache, spotting, headache, and nausea. Body weight and blood pressure did not change significantly. Sociodemographic reasons accounted for the high dropout rate (60%). The leading reason was change of address since many women were migrant farm workers. Since HDL levels rose and LDL levels were the same, this OC appears to have a reduced risk of atherosclerosis and cardiovascular disease. The findings indicated that the Marvelon formulation OC did not adversely affect lipid metabolism and therefore did not increase the risk of atherosclerosis or cardiovascular disease among these women. It also effectively protected them from pregnancy and induced minimal side effects.
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PMID:Evaluation of a combined oral contraceptive pill in black Zimbabwean women. 180 54


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