Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:2.7.10.1 (ERK)
95,504 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Injectable progestogen, norethisterone enanthate (NET-EN, 200 mg/ml at 60 day intervals), was administered to 150 women for 2 years as their method of contraception. Blood levels of acid phosphatase, alkaline phosphatase, glutamate pyruvate transaminase, glutamate oxaloacetate transaminase, acetylcholinesterase (AChe), sialic acid were determined in all subjects to ascertain whether NET-EN therapy causes any adverse metabolic effect or damage to the functional status of the liver. NET-EN contraception did not alter the liver function enzymes but there is a significant increase (P0.001) in AChE activity after 2 years. Serum sialic acid level showed a transient increase up to 1 year, which however returned to control level later. The mechanism responsible for these changes and whether the rise in sialic acid and AChE activity are related to any pathological condition remain unclear at this stage.
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PMID:Studies on some enzymes and sialic acid during progestational contraceptive therapy. 646 44

Ovulation was confirmed by daily analyses of the peripheral plasma levels of estradiol (E2)4) and progesterone (P) in a pre-treatment cycle of 14 subjects. An endometrial biopsy was taken either in the proliferative or in the secretory phase of the cycle. On the 5th day of a subsequent cycle 200 mg norethisterone enanthate (NET-EN) was administered intramuscularly. The levels of E2, P and those of NET were analyzed during the next 19 days and again during 44-60 days following the injection. The endometrial biopsy was repeated on the 23rd and 59th day of the treated cycle. The levels of NET reached a peak of 34.3 nmol/1 on the sixth post-injection day and decreased to below detectable limits in 3 of 12 subjects by the end of the observation. Ovarian activity was completely suppressed in all women during the first period, but returned to different levels in 11 subjects during the second. Four of them exhibited ovulatory steroid pattern. The morphologic changes of the endometrium reflected the progestogen effect in the first post-injection period but were characteristic of the ovarian reaction in the second.
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PMID:Pharmacokinetics, pharmacodynamic and endometrial effects of a single dose of 200 mg norethisterone enanthate. 650 78

The time course of the concentration of the 14C- and 3H-labelled substances and of unchanged norethisterone was determined in maternal plasma and selected tissues of the feto-placental unit after intragastric administration of a combination of 14C-norethisterone acetate (NET-Ac) and 3H-ethinylestradiol (EE2), respective commercial formulation: Ostro - Primolut , to pregnant rats. When given intragastrically in doses of 1 mg NET-Ac/kg and 0.002 mg EE2/kg both synthetic steroids were rapidly and completely absorbed. Highest concentrations of 14C-labelled substances were measured 0.5 h p. admin . in maternal and fetal tissues. Only approximately 1% of total radioactivity in maternal plasma (= 30 ng NET/ml) corresponded to unchanged norethisterone. Less than 1% of the dose administered passed the placental barrier. The maximum NET-levels in the fetuses amounted to 4 ng NET/g tissue. The highest levels of EE2-metabolites in the fetuses were found 2-5 h after administration with 34 pg EE2-equiv./g corresponding to only 0.15% of the dose administered in total fetuses. 14C- and 3H-radioactivity was eliminated from the fetuses with a similar or only a slightly lower rate than from the maternal organism. When administered intragastrically the twofold dose (2 mg NET-Ac/kg plus 0.004 mg EE2/kg) to pregnant rhesus monkeys maximum NET plasma levels of 40 ng/ml were observed after 2 h. Thereafter the NET plasma levels decreased with a half-life of 1.4 hours. The time course of NET concentrations in ovary and pituitary mirrored plasma levels whereas that in placenta and amniotic fluid paralleled plasma levels at a 30-50% and 3-15% niveau , respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Distribution of norethisterone and ethinylestradiol in the gravid rat and in the feto-placental unit of rhesus monkeys following intragastric administration of norethisterone acetate in combination with ethinylestradiol. I. Direct determinations. 654 Jan 2

The tissue distribution of 14C- and 3H-radioactivity was studied in pregnant rats and in fetuses of rhesus monkeys after intragastric administration of a combination of 14C-norethisterone acetate (14C-NET-Ac; 1 mg/kg rat, 2 mg/kg rhesus monkey) and of 3H-ethinyl-estradiol (3H-EE2; 2 micrograms/kg rat, 10 micrograms/kg rhesus monkey), respective commercial formulation: Ostro-Primolut, by means of autoradiographic methodology. The results of these present investigations confirm quantitative studies of a low, transitory passage of 14C-NET-Ac and 3H-EE2 into the fetuses. Within the fetuses the highest concentrations of 14C-radioactivity were found in the liver, in the vertebra, in heart and brain. No 3H-radioactivity could be observed within the fetuses. The autoradiographic studies do not indicate any specific enrichment of NET-Ac or EE2 and their metabolites in fetal organs and tissues.
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PMID:Distribution of norethisterone and ethinylestradiol in the gravid rat and in the feto-placental unit of rhesus monkeys following intragastric administration of norethisterone acetate in combination with ethinylestradiol. II. Autoradiography. 654 May 77

The effects of 2 hormonal contraceptives upon the biliary lipid composition of Mexican women were evaluated in a prospective study. 21 healthy volunteers of reproductive age were assigned to 3 groups (7 subjects each). Group 1 served as the experimental control (all subjects wore a nonmedicated IUD), group 2 received 200 mg norethisterone enanthate (NET-e) intramuscularly every 2 months, and group 3 received an oral combination of 150 mcg l-norgestrel and 30 mcg ethinyl estradiol. The bile lithogenic index as assessed by the relative proportion of cholesterol to bile acids and lecithin was determined in duodenal bile samples obtained before (baseline), during (4 months), and after (12 months) contraceptive administration. Results indicated that NET-e administration resulted in a slight although significant increase of the lithogenic index while the oral formulation did not. The overall data were interpreted as demonstrating that administration of these steroid contraceptives does not constitute a risk factor in terms of gallstone formation in the population studied. The estrogen-like behavior exhibited by NET-e is discussed.
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PMID:Effects of synthetic steroid contraceptives on biliary lipid composition of normal Mexican women. 661 5

Twenty-four normal adult female volunteers were dosed orally with a solution and tablet formulation containing the contraceptive combination of norethindrone (NET, 1.0 mg) and ethinylestradiol (EE2, 0.12 mg) in a crossover bioequivalence study. Blood was sampled sequentially following single oral doses and the plasma separated for analysis of NET and EE2 by specific radioimmunoassays. Comparisons of both drugs following a dose in solution and tablets were made with respect to the following parameters: (a) plasma concentrations at each sample time; (b) maximum plasma concentration (Cpmax); (c) time to maximum plasma concentration (Tmax); (d) total area under the plasma concentration vs. time curve (AUC), and (e) plasma half-life (t1/2). It was found that the tablet and solution doses were bioequivalent with respect to EE2 absorption. However, absorption of NET from solution and tablet doses exhibited significant differences with respect to plasma levels at certain time points as well as AUC (which were higher following the tablet dose), but Cpmax, Tmax and t1/2 were not significantly different. Pharmacokinetic analysis of both drugs following the tablet dose was carried out using a two-compartment open model. The absorption rate constant (ka) and peripheral to central compartment transfer rate constant (k21) were similar for NET and EE2, but statistically significant differences were observed with respect to the distribution rate constant (alpha), the central to peripheral transfer rate constant (k12), the overall elimination rate constant (ke1), and volume of distribution (V1/F). The elimination rate constant (beta) for both drugs showed a difference of borderline statistical significance.
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PMID:Plasma levels and pharmacokinetics of norethindrone and ethinylestradiol administered in solution and as tablets to women. 664 Dec 24

Clinical trials of norethisterone enanthate (NET-EN), a long-acting, injectable progestogen, have demonstrated its short-term safety and effectiveness as a method of contraception in a controlled trial setting. Family planning programs interested in providing NET-EN need information on its efficacy and acceptability under usual field conditions. This first field study of NET-EN was conducted in family planning clinics in rural areas of Mexico. Women admitted to the study were followed up at two-month intervals to receive an injection of 200 milligrams of NET-EN, and to be asked about possible side effects of the drug. Among the 5,792 women recruited, the overall life-table discontinuation rate was 57.0 per 100 women at 12 months and 69.0 at 18 months. The single most common reason for discontinuation was amenorrhea, followed by bleeding problems. Women who were older and who already had several children were most likely to continue using NET-EN. Nine pregnancies were reported during the study, with a cumulative pregnancy rate of 0.3 per 100 women at 18 months. NET-EN appears to be an effective method of contraception that is acceptable to a substantial proportion of women from rural areas in Mexico who choose to use it, when it is provided through a national family planning program.
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PMID:A clinical study of norethisterone enanthate in rural Mexico. 674 Jul 31

5 puerperal and 20 nonpuerperal were treated with intramuscular injections of norethisterone enanthate (NET-EN) for a total of 366 months. Basal hormonal levels were measured in blood samples, and NET was also assayed in plasma from breastfed newborns. There were no pregnancies and only minor menstrual disorders. Lactation was not inhibited in breastfeeding women, and NET transfer to newborn was negligible, even when maximal levels were measured in the mothers. Ovulation was achieved in 3 patients, but with insufficient luteal function. NET-EN seems therefore to be an effective contraceptive, deprived of major side effects, and particularly advisable during puerperium.
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PMID:Norethisterone enanthate as an injectable contraceptive in puerperal and non-puerperal women. 678 16

A clinical trial was conducted with 2 types of progestogen-only contraceptives in 20 fertile Cuban women. 1/2 the group was administered NEN (norethisterone enanthate) injectable; the other 1/2 was given NET (norethisterone acetate) minipill. Daily blood samples were taken and complicated laboratory procedures followed to measure pharmacological effects and gonadotropin secretion. Although preovulatory LH (luteinizing hormone) and FSH peaks were abolished, basal levels of these 2 hormones remained constant. 8 of the 10 women on NEN had some type of menstrual disorder; 5 of those on NET experienced menstrual disorders. Despite the menstrual irregularities, both drugs were highly acceptable and the continuation rate was high. No pregnancy was reported in either group. Blood pressure, renal, hepatic, and thyroid function remained unchanged. Cholesterol levels were unchanged. Both drugs significantly reduced triglycerides. The NET group registered significant changes in their carbohydrate metabolism.
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PMID:Phase I clinical trial of two contraceptive preparations. Norethisterone enanthate (NEN) and norethisterone acetate (NET). 678 25

6 normally menstruating women were each inserted with a single silastic implant-D releasing (NETA) norethindrone acetate. The levels of endogenous hormones, FSH, LH, E2, and progesterone, were estimated by (RIA) radioimmunoassay procedures in the control and treatment cycles. In addition, the levels of drug in the serum as (NET) norethindrone which is a major metabolite of NETA were also estimated by RIA procedures in the treatment cycles. In all, 12 treatment cycles were studied. In the initial treatment cycles (1st/2nd or 3rd), the serum NET levels were either 1 ng/ml or above. The LH and FSH showed either normal or suppressed midcycle peaks, but the progesterone levels were completely suppressed. In the 6th treatment cycle, the serum NET levels were either 0.5 ng/ml or below. The FSH and LH midcycle peaks were lower but distinct while the luteal progesterone levels were of normal ovulatory type. These studies lead us to the conclusion that a serum level of NET of the order of 1 ng/ml is required to bring about suppression of luteal progesterone, either as a result of direct action on the ovary or through suppression of pituitary gonadotropins. When the serum level falls to 0.5 ng/ml or below, the suppressive effect is removed and ovulatory pattern of progesterone returns.
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PMID:Correlation between the serum norethindrone (NET) levels attained after insertion of a silastic implant releasing norethindrone acetate and the endogenous hormones particularly progesterone. 678 28


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