Gene/Protein Disease Symptom Drug Enzyme Compound
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Prevalence rates of various side effects were studied comparatively among 3 oral contraceptive preparations containing 50 mcg of the estrogen component. Norinyl 1/50, Ovral, and Norlestrin 1 were each randomly assigned to groups of 160 healthy women who had consented to participate in the study designed to quantitate probabilities of experiencing specific side effects and of their continuing into the subsequent cycles. Acne, breast discomfort, nausea, abdominal bloating, headache, fatigue, depression, irritability, vaginal discharge, and breakthrough bleeding were the specific side effects studied; only breakthrough bleedings showed a statistical difference in prevalence. The rate of breakthrough bleeding associated with Ovral use in the 1st 3 cycles (16.6%) was significantly (P .05) lower than that associated with using either Norinyl or Norlestrin (46% and 51.7%, respectively). Norelestrin, aside from breakthrough bleeding, was reported as generally freer of side effects than the other 2 preparations. The probabilities of side effects being experienced in the 2nd or 3rd cycle after the effect(s) was experienced in the 1st cycle showed that overall, for all 3 combination pills, the probabilities significantly decreased from the 2nd to the 3rd cycle (P .05). Also examined was the probability that a side effect would occur in the 2nd or 3rd cycle if the user had not experienced such an effect in the 1st cycle. In each instance, the probabilities are significantly lower (P .05) than the corresponding probabilities where the symptom had been experienced in a previous cycle. These data support the contention that side effects experienced on inititation of oral contraceptives should not prohibit its continuation because the majority of symptoms will disappear as the patient becomes accustomed to the hormonal preparation.
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PMID:The probability of side effects with ovral, norinyl 1/50 and norlestrin. 16 Aug 60

A double-blind study of 2 well-known brands of contraceptives, Ovral and Norinyl, was performed in Trinidad and Costa Rica to determine if 1 brand of oral contraceptive were as acceptable as another. Differences in race and ethnic origin were large between the 2 study populations. There were no significant differences in reporting of gastrointestinal side effects for the 2 formulations. Women using Ovral in Costa Rica reported acne and chloasma in significantly greater (P .001) numbers than did women using Norinyl. Participants in Trinidad were virtually free of such complaints. Overall in both study populations, Ovral affected significantly more users (P .05) both with regard to chloasma and all skin conditions than did Norinyl. A moderate excess of cervicitis and cervical erosion among Ovral users in Trinidad was seen; in Costa Rica, cervical erosion occurred in 13% of users of either drug, whereas cervicitis was noted in 3% of each group. Both brands reduced the average number of days of menstrual bleeding in the 2 countries, and both formulations effected a reduction in the % of women reporting relatively heavy menstrual flow. Intermenstrual spotting or bleeding was strongly (P .001 overall) associated with the use of Norinyl; in both countries, the % of women using Norinyl reporting intermenstrual bleeding was at least 2 times that of Ovral users. In Costa Rica, continuation rates for Norinyl were badly affected by the frequency of intermenstrual bleeding (27.9 for Norinyl and 8.2 for Ovral). Otherwise, it is concluded that there were no important differences between the 2 formulations.
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PMID:A randomized double blind study of two oral contraceptives. 47 15

The Authors have been showed the utility of LHRH analogues in the treatment of PCO disease, through hormonal dosages and echographic examination made before, during and after the therapy both with Enantone depot, CPA and EE2, and with only CPA and EE2 of control cases. The association of analogue to traditional therapy has determined a more speedy reduction of haematic levels of LH, T free, DHEA-S, than the ones we have found in control case, an evident reduction (50%) of pilonidal growth and an important improvement of acne and seborrhea.
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PMID:LHRH analogues and PCO disease: validity of the use of enantone depot in the treatment of the disease. 134 54

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

The purpose of prescribing combined oral contraceptives (OCs) is achievement of good cycle control and effective contraception with the least side effects, using an OC with the lowest possible dose of estrogen. Triphasil, Triquilar, Nordette, Microgynon 30, and Brevinor are good 1st choices because of the low estrogen dose (30-35 mcg). Women who probably cannot tolerate breakthrough bleeding and who need simple packaging should use a monophasic, more progestogenic OC, e.g., Nordette or Microgynon 30. Physicians should suggest a low dose estrogen and low dose antiandrogenic progestogen (OC) (e.g., Diane-35 ED) for women who have acne. They should advise patients that when they take OCs, their menstrual periods usually become shorter, regular, and lighter. Women need not take a break from OC usage. Vitamin C, antibiotics, griseofulvin, rifampicin, and anticonvulsants (except sodium valproate) interact with OCs. Women using warfarin and oral hypoglycemics and wanting to start using OCs need to consult their physician about changing requirements for warfarin and oral hypoglycemics. The effectiveness of OCs can be diminished by diarrhea and vomiting. Absolute contraindications to OCs include pregnancy, use during the first 2 weeks postpartum, history of thromboembolism, undiagnosed abnormal vaginal bleeding, focal migraine, coronary heart disease, steroid-dependent tumors, recent impaired liver function, and cardiovascular accidents. Some relative contraindications are older than 35 years old and smoking, breast feeding, and hypertension. This article provides a section on how to manage common side effects. For example, if the side effect is acne, the physician should prescribe an OC with increased estrogen and reduced progestogen (e.g., Triphasil/Triquilar to Biphasil/Sequilar). This article lists trade names of various OCs and their estrogen and progestogen doses, e.g., Nordette has 30 mcg ethinyl estradiol and 150 mcg levonorgestrel.
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PMID:Combined oral contraception. 147 9

A comparison of the triphasic Triphasil and the combined oral contraceptive Diane 50 for treatment of acne for 6 cycles showed significant improvement in both groups. Triphasil (Wyeth-Ayerst) contains 50 mcg levonorgestrel and 30 mcg ethinyl estradiol, 75 mcg levonorgestrel and 40 mcg ethinyl estradiol for 5 days and 125 mcg levonorgestrel and 30 mcg ethinyl estradiol for 10 days. Diane 50 (Schering Ag) contains 2 mg cyproterone acetate and 50 mcg ethinyl estradiol for 21 days per cycle. 10 women in each group had physical, pelvic, ophthalmologic and neurologic exams, hematologic and biochemical screens, assays of free testosterone, sex hormone binding globulin (SHBG), androstenedione, dehydroepiandrosterone SO4 (DHEAS), progesterone, and computations of acne and hirsutism scores. Subjects had used tetracyclines, isotretinoin, erythromycin, topical clindamycin and benzoyl peroxide previously, but were withdrawn from medication in the cycle before the intervention. The mean acne scores, derived from grading and counting lesions and comedones, fell from 63.3 to 6 in the Diane 50 and from 64.2 to 4.5 in the Triphasil group. Subjective results were excellent for 6, good for 2 and unsatisfactory for 2 in the Diane 50 group, and excellent for 8 and good for 2 in the Triphasil group. In both groups mean free testosterone, androgen index, androstenedione and DHEAS, and an increase in SHBG were documented. 5 Triphasil and 5 Diane 50 subjects had increased cholesterol levels during the trial, the only abnormality detected. Side effects reported were recurrence of varicose veins and hemorrhoids in 1 women who withdrew, and complaints of mastalgia, nausea, dysmenorrhea, migraine, headache, backache and vaginal discharge.
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PMID:An open study of Triphasil and Diane 50 in the treatment of acne. 183 45

Desogestrel is the most selective progestogen used in oral contraceptives (OCs). The clinical characteristics of the monophasic combined OC containing 150 micrograms desogestrel and 30 micrograms EE per tablet (Marvelon) are in accordance with the strong progestogenic and minimal androgenic effects of desogestrel: a very high contraceptive efficacy is combined with minimal and, in the case of lipid metabolism, even potentially positive effects on metabolic parameters. Through increasing the plasma levels of sex hormone binding globulin, and thereby decreasing the plasma levels of free testosterone, the desogestrel-containing OC also has substantial beneficial effects on acne.
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PMID:Desogestrel: using a selective progestogen in a combined oral contraceptive. 183 55

The performance of a low-dose triphasic oral contraceptive (OC) in the first four cycles of use was evaluated by 1,326 primary-care physicians and specialists across Canada in a phase-IV postmarketing trial. Data were available from 5,460 women who completed 19,756 cycles of use with Synphasic. The incidence of intermenstrual bleeding characteristically decreased over the four cycles to 10% in women who were first-time users of OCs, to 14% in women who had previously used OCs but had discontinued use until this trial, and to 16% in women who had switched from another OC to Synphasic. The women reported a low incidence of headache, nausea, weight gain, breast complaints, and acne while receiving Synphasic. The results demonstrate good endometrial control with Synphasic and a high level of patient acceptance.
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PMID:Synphasic tablets in Canadian practice: a phase-IV multicenter study. 186 41

A combination oral contraceptive (OC) called Cileste, containing norgestimate and 35 mcg ethinyl estradiol, was assessed in a study involving 46 gynecologists and their patients by administering a questionnaire about acceptance before treatment (first evaluation) and during the 4th cycle of its use (second evaluation). 683 subjects were enrolled: 424 patients took part in a comprehensive evaluation. 379 cases were fully analyzed. The average age was 25.4 years. 14.2 had completed mandatory schooling, 39.6% had graduated from apprentice or trade school, and 42.2% had graduated from secondary school or college. 38.8% were smokers. 13.7% had spotting; amenorrhea was rare in 10.8% and frequent in 3.4%; 22.4% had light and 14% had strong dysmenorrhea. 63.3% of participants rated Cileste very good, 23% rated it good, and 3.4% rated it middling (a low figure compared to the 10.6% middling rating of Trinovum users). 15.6% of 379 patients had strong bleeding at first evaluation vs. 4.7% at the second evaluation. 10% and 2.6% had strong dysmenorrhea, respectively. 33.7% of 377 patients had signs of depression at the first evaluation vs. 22% of 369 patients at the second assessment. Skin impurities and fatty hair associated with acne were side effects in 22.5% of 378 patients during the first evaluation and in 10.8% of 369 patients at the second evaluation. 28.2% of 638 patients at the first evaluation as compared to 15.6% of 425 patients at the second evaluation agreed that medication should be avoided in conditions of environmental pollution. The decrease was probably attributable to lack of side effects after 4 months of OC use. Women complaining of skin problems often suffered from stronger dysmenorrhea during the first phase. Strong bleeding and depression were also interrelated. Cileste also improved skin blemishes and fatty hair, thus during the second evaluation, fewer patients complained of depressive symptoms.
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PMID:[Acceptance and subjective well-being with a norgestimate combination pill]. 191 21

An open, randomized, multicenter study was carried out to compare two oral contraceptives as regards their therapeutic efficacy in androgenization symptoms such as acne, seborrhea and hirsutism in women. The preparations used were the combination of 2 mg cyproterone acetate (CPA) with 0.035 mg ethinyl estradiol (EE) (Diane 35, Schering AG, Berlin-West) and 0.150 mg desogestrel (DG) with 0.03 mg ethinyl estradiol (Marvelon, Organon, Oss, The Netherlands). The duration of therapy was 9 months. The combination of CPA-EE was used by 83 patients for 658 cycles and the combination of DG-EE by 79 women for 618 cycles. No pregnancy occurred under either therapy. Both preparations are well tolerated. However, some side-effects, such as reduced libido, nervousness and breast tenderness, were observed more frequently (p less than 0.05) in the DG-EE group than among the users of the CPA-EE combination. The therapeutic outcome was better in the CPA-EE group, especially in cases of facial acne (p less than 0.05). Seborrheic symptoms also responded better to the CPA-EE therapy. The results show that the CPA-EE combination is superior to the DG-EE combination in the treatment of acne and seborrhoea.
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PMID:Ovulation inhibitors containing cyproterone acetate or desogestrel in the treatment of hyperandrogenic symptoms. 214 Jun 63


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