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)

A placebo-controlled, double-blind study of triphasic oral contraceptives for prospectively confirmed premenstrual syndrome (PMS) was conducted with 82 subjects, 59 of whom completed the study and who were later confirmed to have moderate to severe premenstrual symptoms. 212 subjects were recruited between April 1987 - June 1988, and completed a menstrual history form and a 95-item retrospective questionnaire on premenstrual symptoms. Subjects took Synphasic (Syntex, Mississauga, Canada) containing 35 mcg ethinyl estradiol and 0.5 mg, 1.0 mg, and 0.5 mg norethindrone. Subjects were monitored for 1 menstrual cycle for baseline, then took triphasic or placebo for 3 cycles. 23 oral contraceptive taking and 36 placebo subjects completed the trial: completers had higher status occupations and lower symptom severity scores than dropouts. Both pill and placebo groups showed significant clinical improvement on every symptom except headache. Symptom scores decreased significantly between baseline and 3rd treatment cycle, and between menstrual phase scores and the variables "mood swings," "more sleep," "unhappy," and "tense" in the 2nd treatment cycle compared with the 1st treatment cycle in both groups. In the pill group ratings of premenstrual breast pain were significantly lower in the 3rd treatment cycle compared with baseline (p0.05), and to the 1st treatment cycle (p0.01). No significant changes in breast pain were found in the placebo group. Some pill cycles showed significant reduction in edema. Those in the pill group who were initially rated as "depressed" showed greater improvement in work impairment, sleep requirements, and energy level premenstrually. The pill group, however, reported significantly lower sexual interest during treatment. This is the 1st reported double-blind, placebo-controlled, prospectively confirmed study of oral contraceptives for PMS.
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PMID:A prospective treatment study of premenstrual symptoms using a triphasic oral contraceptive. 156 78

A 31-year old mother of a 3-year old child visited a rheumatologist complaining of pain in both wrists, nose bleeding, and headaches. Since her delivery her weight dropped 12 kg and she has taken Synthroid daily. Before her pregnancy, she took the combined oral contraceptive (OC) Norinyl for 7 years. After childbirth, she took the OC Ortho Novum 1/80. She did not smoke or abuse drugs or alcohol. She did not have a history of hepatic or gastrointestinal diseases. Her alkaline phosphatase and glutamyl transferase levels were higher than normal (632 IU/L and 142 IU/L vs. =or 110 IU/L and =or 55 IU/L, respectively). Other liver function tests, her electrolytes, and her complete blood cell count were not unusual. She underwent an abdominal computed tomography scan and ultrasonography which indicated a single right hepatic lobe lesion (9 cm in diameter). It was well vascularized and circumscribed (12 x 10.5 cm) with big arteries leading to the immediate subcapsular region. The veins and arteries of the other lobe and the spleen appeared normal. Based on these tests, surgeons removed a segment of the right liver. She recovered well. 18 months after surgery, she was in good health. Pathologic examination of the 748 gm segment revealed that endothelial cells lined the sinusoidal spaces indicating true sinusoidal ectasia. The segment also exhibited individual hepatocyte atrophy and necrosis and inflammatory reaction and early fibrosis. Bile ducts had proliferated many portal spaces. Hepatic sinusoidal ectasia may be a forerunner of focal nodular hyperplasia.
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PMID:Hepatic sinusoidal ectasia. 164 40

During testing new sequential preparations such as Trinordiol the weak suppression of gonadotropin and the partly increased endogenous estradiol (E2) and also partly increased progesterone were noted in the course of 30,000 checkups by contraceptive users when clinical symptoms were confirmed by ultrasound and biochemical analysis. In micropill users these were acute abdominal and breast pain, often follicular ripening in the ovaries, and cysts in the ovaries and in the breast with increased E2 values up to ovulatory values in some. The strong pain in the lower abdomen required intervention. It has been known that ethinyl estradiol (EE) and gestagens inhibit ovulation. In a study of 7 patients taking 40 mcg of gestoden there were 6 cases of ovulation inhibition (4 times along with follicular ripening) and 1 case of corpus luteum insufficiency. There were 2 instances of follicular ripening in 32 patients using Femovan containing 30 mcg of EE with 75 mcg of gestoden. With a 20 mcg preparation these signs occurred repeatedly when young girls complained of strong breast pain and breast enlargement. Shifting to a preparation containing 30 mcg of EE with the same dose of gestagen eliminated the complaints. This contradicts the hypothesis that all receptors are occupied by Ee and that endogenous E2 production cannot exercise its effect. Therefore, development of micropills with a somewhat higher gestagen dose has been suggested. There are patients whose cycle regulation is aided only by sequential preparations with 50 mcg of EE. It is concluded that ovulation inhibition is dependent on the dose and structure of gestagens, with the resorption and current metabolism of steroids in agreement with individually differing suppression of the ovaries.
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PMID:[Response to the letter by Prof. Kuhl: "Does a rise in endogenous estradiol during treatment with low-dose ovulation inhibitor signify increased risk"?]. 179 81

Health practitioners use many methods and agents to bring on cervical ripening in early pregnancy, such as intracervical tents and pharmacological techniques, to induce a therapeutic abortion. Prostaglandins alter myometrial and cervical tissue and are the most often used pharmacological technique. Reduced collagen concentration, an increase in water volume, an increase in prostaglandins (PGE2, PGI2, and PGF2 alpha), and a change in the glycosaminoglycan (GAG) content coincide with cervical ripening, yet the mechanism responsible for these changes is obscure. Prostaglandins appear to cause the breakdown of collagen or change the GAG/proteoglycan content. Research shows that prostaglandins can initiate cervical ripening at any stage of pregnancy. Estradiol stimulates prostaglandin production thereby al so inducing cervical dilation. Relaxin also demonstrates an ability to ripen the cervix. In addition, mifepristone (RU-486) is gaining acceptance as a cervical ripening agent. In fact, RU-486 and gemeprost have at least 95% success rate compared to 92% for gemeprost alone or 85% with RU-486 alone. The only effective and acceptable prostaglandins to use at gestation of 0-8 weeks are sulprostone, gemeprost, and 9-methylene-PGE2. At t his gestational age, pharmacological modulation is all that is needed. Even though they are effective (abortion rate 90%), side effects are expected to occur (pain, nausea, and vomiting). Similarly, prostaglandin analogues are preferable for cervical ripening in women at 8-12 weeks gestation. Suction curettage or other surgical techniques then are used to remove the conceptus. At 12-16 weeks gestation, many physicians prefer the same protocol as that of 8-12 weeks gestation. Other choose to infuse PGE2 and saline into the amniotic fluid to stimulate uterine contractions. Another procedure at 12-16 weeks involves 1mg vaginal pessaries of gemeprost every 3 hours to ripen the cervix and stimulate contractions. After 16 weeks, the methods for 12-16 weeks still apply.
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PMID:Pharmacological modulation of cervical compliance in the first and second trimesters of pregnancy. 187 72

Although there is a critical need for effective contraception in the immediate postpartum period for women who are not breastfeeding, this need must be balanced against the inherent risks. The most effective form of contraceptive protection--oral contraceptives (OCs)--can present an increased risk of thromboembolism in the period after delivery. The thrombotic changes associated with pregnancy, and the statistics and vascular damage following a delivery, can combine to create greater potential for thromboembolism after delivery than during pregnancy. Reported here is the case of a 21-year-old woman who, 4 weeks postpartum, developed pain and swelling in the right lower calf and mottled discoloration extending from the proximal thigh to the toes. A diagnosis of deep venous thrombosis was made and heparin was administered. In the hospital, the patient experienced pleuritic chest pain and diaphoresis. A ventilation-perfusion scan indicated a pulmonary embolism. 1 week after delivery, the patient had initiated use of Triphasil. Although this woman had other risk factors (obesity, light cigarette smoking, and a sedentary life-style), OC use in the immediate postpartum period may have been the final factor precipitating the thromboembolic event. It is recommended that OC use should be delayed until at least 2 weeks postpartum in women without other risk factors for thromboembolism and until 4-6 weeks postpartum in those with such factors.
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PMID:Oral contraceptives in the immediate postpartum period. 201 Jul 44

From August 1988-June 1989, 983 physicians participated in a phase IV trial by following 7759 women using the monophasic oral contraceptive (OC), Demulen 1/35 (1 mg ethynodiol diacetate and 35 ug ethinyl estradiol) to evaluate its efficacy and safety. The total number of cycles for the study stood at 21,440. In addition, the total woman-years stood at 1787. Only 6382 patients could be evaluated for safety. 4.4% of the patients had adverse reactions to the OC, but only 1.7% of all patients stopped taking it. The leading side effects included nausea (67 cases), headache (45), amenorrhea (42), emotional changes (30), breast pain (19), dysmenorrhea (12), and 11 cases of weight gain, abdominal/pelvic pain, and bloating. Of the 280 reported adverse reactions, only 87 (31%) were considered severe. The leading serious adverse reactions were depression (10) and hypertension (6). Only 5412 patients could be used to determine efficacy. The physicians initially reported 121 (2.2%) pregnancies during the study. The researchers learned that 33 of the 84 returned 2nd questionnaires (response rate, 70%) reported that the women conceived after enrollment but before taking the OC. 36 conceived while taking it, but 8 did not take it daily. Noncompliance may have contributed to pregnancy for the remaining 28 cases. Therefore the 36 confirmed pregnancies made for a failure rate of .7%. 85.7% of the pregnancies happened in the 1st 3 months of taking the OC. Either patient noncompliance or true medication failure accounted for treatment failure. Therefore it is important for physicians to instruct patients on how to take OCs correctly.
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PMID:Efficacy and safety of ethynodiol diacetate, 1 mg, with ethinyl estradiol, 35 micrograms, with an emphasis on contraceptive efficacy. A phase IV trial. 204 81

A case is presented of a 37-year-old Japanese woman who presented to the hospital with arthralgia of the extremities and erythema of the hypothenar and thenar extremities. Also present were pain, swelling of the extremities, general malaise, and erythematous lesions. Abnormal laboratory findings included an elevated erythrocyte sedimentation rate, proteinuria, and weakly positive antinuclear antibodies. A biopsy from the erythematous lesion of the palm revealed mild inflammation of the lymphocytes around dermal small vessels. In addition, the lupus band test was positive in uninvolved skin sites. A month prior to the onset of symptoms, the patient had begun taking an oral contraceptive (OC) that contained 0.5 mg of etynodil acetate and 0.1 mg of mestranol. All symptoms disappeared within 2 weeks of discontinuation of OC use and the laboratory findings returned to normal. This is assumed to be a case of drug-induced lupus erythematosus. Estradiol has been demonstrated to play a significant role in the development of skin lesions in lupus erythematosus, and the estrogen in OCs may trigger a lupus episode. However, this is only the 4th case of OC-induced lupus reported from Japan.
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PMID:Oral contraceptive-induced lupus erythematosus in a Japanese woman. 205 Sep 10

The safety and efficacy of leuprolide acetate (LA) for depot suspension (Lupron depot; TAP Pharmaceuticals, North Chicago, IL), 3.75 mg versus placebo, in the treatment of pain associated with endometriosis was assessed in a randomized, double-blind, multicenter study involving 52 patients. Dysmenorrhea, pelvic pain, and pelvic tenderness all responded significantly to LA treatment in comparison with placebo. Menses were suppressed in all of the LA patients. Estradiol decreased significantly to menopausal levels in the LA group. There were small to moderate changes in a variety of laboratory parameters, but these were not clinically significant. The most common adverse event was vasodilatation, occurring significantly more frequently in the LA group. Lupron depot was shown to be safe and effective in inducing a hormonal and menstrual suppression in patients with endometriosis, resulting in alleviation of pain symptoms.
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PMID:Lupron depot (leuprolide acetate for depot suspension) in the treatment of endometriosis: a randomized, placebo-controlled, double-blind study. Lupron Study Group. 211 58

Unlike the proven causal association between oral contraceptive (OC) use and hepatic cell adenoma, the link between OCs and hepatocellular carcinoma remains speculative. The case history of a 53-year-old US woman suggests, however, that hepatic cell adenomas may transform into hepatocellular carcinoma. The patient, who had used Ovral continuously since 1966, presented in 1985 with vague abdominal pain and a palpable right upper quadrant mass. Computed tomography revealed a 12 x 8 cm mass in the right hepatic lobe and 2 small lesions in the left lobe. Serum alpha-fetoprotein and ferritin levels were normal and tests for hepatitis B were negative. A needle biopsy of the right lobe mass indicated benign hepatic adenoma. OC use was discontinued and the patient was examined at bimonthly intervals. Although she continued to report vague pain, there were no significant changes in radiologic findings or levels of alpha-fetoprotein over the next 18 months. At the 18-month follow-up visit, the alpha-fetoprotein level showed an increase to 227 mcg/L and had risen to 2300 mcg/L by the 30-month follow-up visit. At this time, computed tomography showed slight enlargement of the right lobe mass and inhomogeneity, while biopsy revealed sclerosing hepatocellular carcinoma. This is the 3rd case reported in the literature in which there is evidence of a transformation of hepatic cell adenomas into hepatocellular carcinoma in longterm OC users. Thus, the premalignant potential of hepatic cell carcinomas in OC users should be considered by physicians who follow such cases.
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PMID:Transformation of hepatic cell adenoma to hepatocellular carcinoma due to oral contraceptive use. 253 93

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


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