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)

Serial plasma unconjugated estradiol-17 beta was measured by a radioimmunoassay method in 26 cases of hypertensive disorder of pregnancy, 13 cases of poor obstetric history and 4 cases of intra-uterine growth retardation. There was considerable overlap of hormonal values between pregnancies, resulting in delivery of normal fetuses and those with dysmature fetuses. Serial estimation of estradiol-17 beta were not found to be useful in the prediction of intra-uterine death, although low values were obtained after fetal death has occurred. Estradiol-17 beta estimation appeared to be an unreliable index of fetoplacental function.
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PMID:Plasma estradiol-17 beta as an index of fetoplacental function. 1 13

These studies were designed to investigate the differences in blood plasma levels of ethynylestradiol (EE2) in women who developed hypertension while taking combined estrogen and progesterone oral contraceptives (OCs) and in normotensive OC users. Blood samples were collected in heparinized tubes 10 hours after OC ingestion, the plasma was separated, and EE2 was measured by radioimmunoassay. The results showed significantly higher plasma levels of EE2 in the hypertensive OC users as compared with the levels in normotensive OC users (P less than 0.01). In another study, blood samples from hypertensive and normotensive OC users were obtained for 3 consecutive days at fixed intervals following OC ingestion, and plasma levels of EE2 were measured. The results showed consistently higher EE2 blood levels during this 3-day period in the hypertensive subjects (P less than 0.01). It is postulated that the higher blood levels of EE2 in hypertensive OC users result from either decreased metabolism or excretion of synthetic estrogens.
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PMID:Evidence of higher ethynylestradiol blood levels in human hypertensive oral contraceptive users. 86 74

Estradiol 17-sulphate is readily converted to 2-OH or 4-OH estradiol 17-sulphate. The latter two strongly antagonize lipid peroxidation, which may play certain roles during pregnancy, such as pregnancy-induced hypertension. Serum estradiol 17-sulphate during mid and late pregnancy was measured using a direct radioimmunoassay without hydrolysis, and the level increased as pregnancy progressed. The levels in the sixth (20-23 weeks) and tenth months (36-39 weeks) of gestation were 1.42 +/- 0.04 nmol/l (mean +/- SD) and 3.42 +/- 1.09 nmol/l, respectively. The maternal venous levels before and at delivery and in the umbilical veins and artery were 3.38 +/- 0.83, 3.48 +/- 1.53, 4.11 +/- 1.40 and 4.30 +/- 1.81 nmol/l, respectively. The latter two values were slightly higher than the former two. Estradiol 17-sulphate in maternal venous blood began to decrease around delivery. Serum lipid peroxides were measured using the method of Yagi. Estradiol 17-sulphate and lipid peroxides showed a simple regression slope (r = -0.548, p less than 0.05) during late pregnancy. These results suggest that estradiol 17-sulphate may be converted to 2-OH or 4-OH estradiol 17-sulphate, which act as lipid peroxide scavengers during pregnancy.
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PMID:Serum estradiol 17-sulphate and lipid peroxides in late pregnancy. 131 29

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

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

1. Systolic blood pressure (SBP), bodyweight, organ weight, renal beta-adrenoceptor and myocardial beta- and myocardial alpha 1-adrenoceptor characteristics were investigated in female Sprague-Dawley rats after chronic subcutaneous (s.c.) administration of ethynyloestradiol (EE2, 0.2 microgram/day), levonorgestrel (NG, 2.0 micrograms/day) separately and in combination (EE2/NG). 2. EE2 caused a sustained increase in SBP from 6 weeks (maximum at 14 weeks, +22 mmHg compared to control) which was accompanied by increased kidney and ventricle weight after 12 weeks. EE2/NG-treated rats also demonstrated a gradual rise in SBP (maximum at 9 weeks, +18 mmHg compared with control) with renal and ventricular hypertrophy, but were normotensive by week 17 of treatment. In contrast, NG induced only transient SBP increases (maxima at 5 and 10 weeks, +14 mmHg compared with control), unaccompanied by organ hypertrophy. Norethisterone (2 micrograms/day) also produced transient increases (weeks 6-8, +13 mmHg) in SBP. 3. alpha 1- and beta-adrenoceptors were investigated using [3H]-prazosin and (-)-[125I]-iodocyanopindolol (ICYP), respectively. Myocardial alpha 1- and beta-adrenoceptors were unaffected by steroid contraceptive administration for up to 12 weeks. Renal beta-adrenoceptor affinity was markedly reduced in 12 week EE2-treated rats (equilibrium dissociation constant, KD, 53 +/- 7 pmol/L) compared with controls (KD, 31 +/- 4 pmol/L), an effect which was prevented by co-administration of NG (KD, 34 +/- 8 pmol/L). Renal beta-adrenoceptor number was not altered by any treatment. 4. The relatively late onset of organ hypertrophy and beta-adrenoceptor changes appear to result from, rather than cause, EE2-induced hypertension.
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PMID:Renal and myocardial adrenoceptors in steroid contraceptive-induced hypertension in rats. 217 69

This guide to choice of oral contraceptives, for U.S. clinicians, includes a review of the available types of pills, the pharmacology of the steroids in pills, safety issues regarding thrombosis, arterial disease and hypertension related to estrogens and progestins in pills, common side effects, and therapeutic uses of orals. Choice of an oral contraceptive narrows down to which of the 5 available progestins and their formulation, since all contain ethinyl estradiol as the estrogen. While Briggs' theory espoused picking a pill with the minimal metabolic effect, recent evidence suggests that some estrogenic activity may be preferable to the unopposed progestagen, actually an anti-estrogenic receptor effect, to prevent adverse lipid and blood pressure effects in users. Current pills with low doses of estrogens probably are not significant risks for women as regards thrombosis, particularly if predisposed women and smokers are excluded. Pills containing 0.35 mg ethinyl estradiol and 0.5 mg norethindrone, based on large population trials, are probably the minimal effective dose yet even these are more effective than most other contraceptive methods. Breakthrough bleeding and spotting have been further minimized, however, with multiphasic pills. It is best to start with a 0.30-0.35 mg estrogen oral contraceptive, such as Loestrin, Demulin, Orthonovum 1.35, Orthonovum 7/7/7 or Nordette, encouraging the patient to accept early side effects for 3 months before switching to others. Disorders that can be managed with oral contraceptives include recurring and pre-existing ovarian cysts, endometriosis, dysfunctional uterine bleeding and dysmenorrhea. Brief guidelines for handling normal side effects and treatment of the above disorders are included.
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PMID:Choosing the best oral contraceptive. 274 45

Female Sprague-Dawley rats were injected s.c. with 0.2 micrograms day-1 ethinyloestradiol (EE2) or 2.0 micrograms day-1 levonorgestrel (NG), procedures previously shown to increase systolic blood pressure. Increases in perfusion pressure to clonidine, phenylephrine, noradrenaline (NA) and angiotensin II (AII) were observed in rat isolated tail arteries, and to NA in the isolated mesenteric vasculature from steroid and vehicle-treated rats. NG treatment for four weeks produced increases in sensitivity to phenylephrine and NA in rat tail arteries; at 6 weeks the increases in sensitivity had largely disappeared but the maximum responses to clonidine and phenylephrine were increased. No change in sensitivity to AII was observed with NG. In contrast, EE2 treatment for six weeks produced increases in sensitivity to AII, and a decrease in sensitivity and maximum response to clonidine but not to phenylephrine or NA, in tail arteries. Responses to NA in the mesenteric vasculature were increased after 6 weeks NG treatment but unaffected after 12 weeks EE2 treatment. It is concluded that NG treatment stimulates alpha-adrenoceptor number, affinity or receptor-linked Ca2+ events which may contribute to its previously demonstrated hypertensive effect. The increased responsiveness to AII but not the decrease in alpha 2-adrenoceptor responsiveness may be associated with the chronic hypertension induced by EE2.
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PMID:Effect of levonorgestrel and ethinyloestradiol on vasoconstriction in rat isolated vasculature. 290 11

Oral contraceptives (OCs) containing 0.150 mg desogestrel plus 0.020 or 0.030 mg ethinylestradiol (Marvelon) were studied with respect to their effect on blood pressure. Data on 3,421 women were obtained covering 41,132 treatment cycles. The drop-out rate due to hypertension was 2.92 per thousand women-years (TWY). Mean changes in blood pressure were small, indicating that low doses of ethinylestradiol when combined with desogestrel do not adversely affect blood pressure.
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PMID:Desogestrel-containing oral contraceptives and blood pressure. 294 57

Female Sprague-Dawley rats were injected s.c. with ethynyloestradiol (EE2, 0.2 microgram/day) and levonorgestrel (NG, 2.0 micrograms/day) separately and in combination (EE2/NG). Binding of [3H]rauwolscine (alpha 2-adrenoceptor specific) and [3H]prazosin (alpha 1-adrenoceptor specific) was examined in crude membrane suspensions prepared from whole rat kidney after 3, 6 and 12 weeks of steroid administration. Receptor affinity was high for both ligands (KD, equilibrium dissociation constant [3H]rauwolscine, congruent to 2.0 nM; [3H]prazosin, congruent to 0.2 nM) and was not altered in rats chronically treated with steroid contraceptives. The Bmax (maximum density of binding sites) for [3H]prazosin binding was not altered, indicating no change in the number of renal alpha 1-adrenoceptors. NG administered alone did not affect the numbers of alpha 1- or alpha 2-adrenoceptors. Catechol metabolites of endogenous oestrogens did not displace the binding of either radioligand, suggesting that these metabolites do not directly interact with renal alpha-adrenoceptors. However, after 12 weeks treatment, the number of [3H]rauwolscine binding sites was reduced in both EE2 (Bmax, 133 +/- 7 fmol/mg protein)- and combined EE2/NG (135 +/- 11 fmol/mg protein)-treated rats, compared to controls (162 +/- 9 fmol/mg protein). Since renal alpha 2-adrenoceptors inhibit renin release, this reduction in alpha 2-adrenoceptor number may contribute to increased renin levels associated with oestrogen-induced hypertension.
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PMID:Chronic steroid contraceptive treatment decreases renal alpha-adrenoceptor levels in the rat. 302 4


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