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)

Daily levels of LH (luteinizing hormone) were measured in 29 healthy women and compared with in vitro bioassays and immunological assays (radioimmunoassay) to determine the effect of NET (norethisterone), administered as a low-dose formulation (.3 mg/day), on levels of biologically and immunologically active LH. Measurements of NET were made daily throughout the menstrual cycle in the women before and during the 2nd month of NET administration. All 29 control cycles showed the characteristic midcycle LH surge; however, only 10 treated cycles exhibited this surge; even in those cycles showing the LH surge, the level of LH was noticeable depressed (P.001) throughout the menstrual cycle. A biological-to-immunological ratio (B/I) was quantified, and among these 10 treatment cycles with LH surge, there was no difference of statistical significance in B/I between control and treatment cycles. In the 19 remaining cycles in which no midcycle LH peak occurred, both biological and immunological activities of LH were significantly reduced (P.05) compared with those in the follicular phase of controls and were significantly higher than in control luteal phase (P.05). For these 19 subjects, the B/I ratio was significantly lower in treatment periods than in control cycles (P.001); still, the article concludes that even during treatment with NET, both biological and immunological LH behave irregularly, but the irregular patterns are of similar kind.
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PMID:Effect of the norethisterone minipill on the plasma levels of biologically and immunologically active luteinizing hormone in women. 51 47

Norethisterone oenanthate (NET-OEN) was given as an injectable contraceptive to 295 healthy women over 1606 woman-months. A modified injection schedule was used. There were no pregnancies, and the 12-month, life-table, use-related discontinuation rate was 39.1/100 users. Menstrual disturbance (10.8/100 women), minor side effects (13.5/100 women), and personal reasons (12.0/100 women) were the main causes of use-related discontinuation. There was no difference in use-related discontinuation rates between women receiving their first injection during a normal menstrual period and those receiving it immediately after a pregnancy. There were no serious side effects. The use of NET-OEN in certain groups of women is recommended, particularly in those in need of highly effective contraception, who cannot or do not wish to take oral contraceptives, who are lactating, or who are awaiting hospital admission for sterilisation.
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PMID:Norethisterone oenanthate as an injectable contraceptive: use of a modified dose schedule. 65 65

The effect of 2 long-acting injectables on the plasma protein-bound carbohydrate components and serumucoid when taken for different periods, was illustrated in 100 women of childbearing age. 40 acted as controls, 30 took depot-medroxyprogesterone acetate (DMPA), and 30 took norethisterone enanthate (NET-EN). DMPA was given in a dose of 150 mg and NET-EN in a dose of 200 mg im. The 1st injections were given on Day 5 of the menstrual cycles. Repeat injections were given every 84 + or -5 days for a total of 850 cycles. Serum samples were taken while the women were fasting and immediately before the next injection. There was no statistical difference between any group of women using the injectable contraceptives for different periods of 2-8 injections and the controls for protein-bound carbohydrate components. The seromucoid showed a significant decrease in all the groups, as compared with controls.
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PMID:Serium protein-bound carbohydrate and seromucoid levels during long-acting progestational contraceptive therapy. 92 50

The kinetics and metabolism of 17 beta-heptanoyl-17 alpha-ethinyl-4-oestren-3-one-7-3H (7-3H-norethisterone enanthate, NET-En) after i.m. injection in two female subjects is described. 177.4 mg and 174.5 mg NET-En were injected. Maximum 3H-activity in plasma was reached 8 to 14 days after the injection. In terms of NET-En it amounted to 70-100 mug/100 ml. Maximum NET concentration was reached on the 4th to 8th day and amounted to about 1 mug/100 ml. After 4 weeks NET concentration was still about 0.05 to 0.1 mug/100 ml and even after 6 weeks NET was still detectable in plasma. In 14 days the two subjects excreted about 13% of the administered dose in the urine and about 15% and 21%, respectively, in the faeces. On the basis of a rough calculation, the subjects eliminated about 60% and 55% of the radioactivity with urine and faeces within 42 days.
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PMID:Studies of the kinetics and metabolism of 17 beta-heptanoyl-17 alpha-ethinyl-4-oestren-3-one-7-3H (norethisterone enanthate) in humans following intramuscular injection. 103 62

Reduction of the oral contraceptive estrogen burden by alternate-day estrogen administration was studied. 3 regimens: 1) 1 mg norethindrone acetate (NET-Ac) plus .05 mg ethinyl estradiol (EE) on alternate days, 2) .05 mg NET plus .03 mg EE daily, and 3) .05 mg NET daily plus .06 EE on alternate days, were compared. Studies with the 1st regimen were prematurely terminated due to gross cycle irregularities; the 2nd regimen provided better cycle control but inadequate pregnancy protection apparently because of inconsistent inhibition of ovulation. Studies with the last regimen, expanded to include 1090 women for 12,942 patient-months, had clinically acceptable bleeding patterns with a bleeding discontinuation rate after the 1st year of 10.5 and after the 2nd year of 11.9. 2 of 8 pregnancies which occurred were attributed to method failure.
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PMID:Reduction of the oral contraceptive estrogen burden by alternate day estrogen administration. 113 55

Norethisterone-3-oxime (NETO) was administered to 3 female cynomolgus monkeys intragastrically and, after a wash-out period of 2-5 weeks, intravenously at a dose of 1 mg/kg. The radioactive dose of tritiated NETO was 20 microCi/kg for both treatments. For i.v. injection, a 30% propylene glycol/water solution and for i.g. administration an aqueous microcrystalline suspension was used. Excretion of radiolabel in urine and feces was followed for 5 days and plasma samples were obtained up to 2 days after administrations. In all samples (urine, feces and plasma) radioactivity was determined. Extracts from plasma samples were subjected to HPLC separation of drug and metabolites, as well as NETO and NET (metabolite of NETO after hydrolysis of the oxime group) levels were determined. In addition, EE2 (ethinylestradiol, A-ring aromatised metabolite of NET) levels were estimated using a specifically designed HPLC system for separation. Quantification of EE2 was achieved by radioimmunoassay (RIA) of specific eluate fractions. The results demonstrate that [3H]-NETO was absorbed completely at a dose level of 1 mg/kg, and excreted predominantly via the kidneys. A urinary to fecal excretion ratio of 1.5 (i.v.) or 1.0 (i.g.) was found. Renal excretion of total radiolabel proceeded with a half-life of about 0.8 (i.v.) or 1.1 (i.g.) days. Balances were incomplete, probably due to technical reasons. Orally administered NETO was highly bioavailable (84.0 +/- 16.9% of dose) but rapidly cleared from plasma (total clearance corresponded to 97% of plasma liver flow). The clearance from plasma is equivalent to the metabolic clearance because almost no unchanged NETO is excreted. Extensive metabolism of the parent drug was observed leading to at least two pharmacologically active metabolites (NET, EE2). The main progestogenic metabolite was NET reaching similar high plasma levels as NETO. EE2 turned out to be a metabolite of NETO and a conversion rate of below 0.5% of dose was estimated. However, due to its high estrogenic potency EE2 might contribute to the overall pharmacological pattern of NETO in the cynomolgus monkey.
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PMID:Pharmacokinetics, hydrolysis and aromatisation of norethisterone-3-oxime in female cynomolgus monkey. 130 58

The effect of reducing the dose of peroral lynestrenol by half on serum sex-hormone, lipid and lipoprotein status was studied in 21 mentally retarded women with therapeutic amenorrhea (TA). They had previously received 5 or 10 mg peroral lynestrenol daily for periods ranging from 32 to 196 months. Dose halving of lynestrenol resulted in an increase in serum total testosterone (T) by 16% (p less than 0.05), sex-hormone binding globulin (SHBG) by 39% (p less than 0.01) and high-density lipoprotein cholesterol (HDL-C) by 28% (p less than 0.001). Both the mean serum total and free concentrations of norethisterone (NET and fNET) decreased by 60% (p less than 0.001). The serum concentrations of 17-beta-estradiol (E2), its free fractions (fE2) and free T (fT) were not significantly altered. Significant correlations were observed between the change in HDL-C and the change in T (r = 0.45, p less than 0.05), between the change in SHBG and the change in T (r = 0.62, p less than 0.01), fT (r = 0.43, p less than 0.05) and E2 (r = 0.51, p less than 0.05). The elevation of HDL-C was probably caused by the reduced serum NET concentrations. This also resulted in an increase in serum SHBG concentration, which is regarded as an indicator of the overall estrogen/androgen ratio.
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PMID:Lynestrenol induced therapeutic amenorrhea: effects of dose reduction on serum sex-hormones and lipids. 131 38

The World Health Organization recommends the use of fixed reference periods for quantification of the incidence and severity of vaginal bleeding when patients use various forms of contraception. Ninety- and 110-day reference periods were used in the analysis of data from daily menstrual diaries kept by 72 healthy women in a one-year study of oral contraceptive agents containing ethinyl estradiol and either norethindrone or levonorgestrel. Analysis of bleeding patterns reported during both 90-day and 110-day periods revealed fewer days of bleeding and/or spotting overall with norethindrone than with levonorgestrel (e.g., a mean of 16.06 vs. 19.55 days, respectively, over the first 90-day period; P = .013) and significantly shorter bleeding and/or spotting episodes with the norethindrone preparation. This trend persisted when data were adjusted for a day-1 pill start. Using either method of analysis, duration of bleeding episodes was shorter among subjects taking norethindrone than levonorgestrel. Pills were missed in both study groups, but more women in the LNG/EE group missed from 1 to 3 pills in at least one cycle (31 vs. 21 in the NET/EE group). The between-group difference in bleeding events may be due to intrinsic hormonal differences in regimens or to the greater number of pills missed among levonorgestrel users.
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PMID:Reference period analysis of vaginal bleeding with triphasic oral contraceptive agents containing norethindrone or levonorgestrel: a comparison study. 135 65

This randomized double-blind study of the metabolic effects of two low-dose oral contraceptives was conducted in 58 randomly selected Singaporean women. Study subjects were divided into two treatment groups: 1) norethisterone 1 mg/ethinyl estradiol 35 mcg (NET/EE) or levonorgestrel 150 mcg/ethinyl estradiol 30 mcg (LNG/EE) were given to 35 women; 2) a control group of 23 women using IUDs. Blood samples were taken on admission and at 3 and 12 months after pills or insertion of IUDs. Findings demonstrate a significant decrease in mean fasting glucose and in 2-hour glucose loading, while triglycerides were increased throughout the treatment period in the NET/EE group. The LNG/EE group only showed significant suppression of the 2-hour glucose loading at 12 months and low-density lipoprotein/high-density lipoprotein (LDL/HDL) cholesterol was significantly reduced by 12 months. Both groups had no change in hemoglobin, hematocrit and total protein levels, but alkaline phosphatase, bilirubin and aspartate transaminase (SGOT) were decreased. Decreased albumin was observed in the NET/EE group, but not in the LNG/EE group. Changes in total HDL and LDL cholesterol and SGOT were not significantly different in the treatment group compared to the IUD group, except for the 2-hour glucose loading. There was no increase in the number of abnormal parameters after treatment. On the contrary, there was a reduction of abnormal values in most liver function parameters. Thus, except for glucose intolerance, the observed changes in metabolic parameters may not be of any clinical significance.
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PMID:Lipid and biochemical changes after low-dose oral contraception. 145 19

We report on a new method of stimulating the facial nerve through Stensen's duct. Electrical resistance of the skin and subcutaneous tissue is one of the major problems of neurophysiological facial nerve testing. To overcome this disadvantage, the authors show that the facial nerve can be stimulated with far less current through Stensen's duct. The NET, ENoG, and antidromic facial nerve responses are recordable at less than a third of the current required for conventional percutaneous stimulation. It is our belief that nerve stimulation through Stensen's duct will be a new and useful method for assessing facial nerve dysfunction in the early stage of palsy.
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PMID:Facial nerve stimulation through Stensen's duct. 148 54


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