[Norethisterone enantate as a tricyclical contraceptive. Comparative study].
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Adult↗
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Experience with norethisterone enanthate as injectable contraceptive.
Norethisterone Enanthate (NE) was used in 151 women as injectable contraceptive. Pregnancy due to method failure was 2% whereas the overall pregnancy was 4%. The results have been discussed.
Adult↗
A double-blind randomised placebo controlled trial of postnatal norethisterone enanthate: the effect on postnatal depression and serum hormones.
OBJECTIVES: To determine the effect of postnatal administration of the long-acting progestogen contraceptive, norethisterone enanthate, on postnatal depression and on serum hormone concentrations, and their association with depression. DESIGN: Double-blind randomised placebo-controlled trial. SETTING: A tertiary care hospital in Johannesburg, South Africa. POPULATION Postnatal women using a non-hormonal method of contraception (n = 180). METHODS: Random allocation within 48 hours of delivery to norethisterone enanthate by injection, or placebo. MAIN OUTCOME MEASURES: Depression scores in the three months postpartum as rated by the Montgomery-Asberg Depression Rating Scale (MADRS) and the Edinburgh Postnatal Depression Scale (EPDS); 2. serum 17beta-oestradiol, progesterone, testosterone and the 17beta-oestradiol:progesterone ratio at six weeks postpartum. RESULTS: There was a chance excess of caesarean section deliveries in the progestogen group. Mean depression scores were significantly higher in the progestogen group than in the placebo group at six weeks postpartum (mean MADRS score 8.3 vs 4.9; P = 0.0111; mean EPDS score 10.6 vs 7.5; P = 0.0022). Mean serum 17beta-oestradiol and progesterone concentrations were significantly lower in the progestogen group compared with the placebo group at six weeks postpartum. There were no correlations between any of the hormone parameters and depression at six weeks except in the formula feeding subgroup of the placebo group, where formula feeding and 17beta-oestradiol concentrations were positively associated with depression. CONCLUSIONS: Long-acting norethisterone enanthate given within 48 hours of delivery is associated with an increased risk of developing postnatal depression and causes suppression of endogenous ovarian hormone secretion.
Adult↗
Long-acting contraceptive agents: structure activity relationships in a series of norethisterone and levonorgestrel esters.
A large number of esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) and levonorgestrel (D-(-)-13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) were synthesized and tested for biological activity. The test employed in these studies was the duration of estrus suppression in cycling mature rats. In the norethisterone series several esters exhibited duration of activity comparable to that of norethisterone enanthate. In the levonorgestrel series the butanoic, cyclobutylcarboxylic and cyclopropylcarboxylic esters were longer acting than medroxyprogesterone acetate (17 alpha-acetoxy-6 alpha-methylpregn-4-ene-3,20-dione) when prepared as aqueous microcrystalline suspensions.
Animals↗
Investigations upon the mechanism of inhibition of spermatogenesis in the rat by a dimeric ethynodiol-testosterone ester.
The combination of androgens and progestogens has been shown to be a suitable male contraceptive. Previous experiments revealed that injection of a dimeric testosterone-ethynodiol ester into rats and monkeys induces azoospermia for several weeks. In order to investigate the mechanism of action, we compared the endocrine effects of a single injection of 10 mg of the dimeric ester into intact male rats with that of 6 mg of norethisterone enanthate + 6 mg of testosterone enanthate. After the injection of the dimer there was a transitory reduction of serum FSH and a strong suppression of serum LH and testosterone, of testicular testosterone and of androgen-binding protein (ABP) in the testis and epididymis for at least 8 weeks, whereas spermatogenesis was totally depressed between the 4th and 8th week. Contrary to this, the enanthates caused only a slight suppression of spermatogenesis, although serum LH, testicular testosterone and ABP were profoundly reduced. The only conspicuous difference in the endocrine pattern of both groups during the first 4 weeks was in the serum testosterone level which remained normal in the rats treated with the enanthates. The results suggest that testicular testosterone and ABP concentrations are of minor significance for an intact spermatogenesis, and that some other factors produced by Sertoli cells might be involved and possibly maintained by normal serum testosterone levels.
Androgen-Binding Protein↗
Metabolic effects of once-a-month combined injectable contraceptives. The World Health Organization Task Force on Long-Acting Systemic Agents for Fertility Regulation, Geneva, Switzerland.
The results of metabolic studies on once-a-month combined injectable contraceptives are summarized, focusing on four preparations: dihydroxyprogesterone acetophenide 150 mg/estradiol enanthate 10 mg; depot-medroxyprogesterone acetate 25 mg/estradiol cypionate 5 mg; norethisterone enanthate 50 mg/estradiol valerate 5 mg; and 17 beta-hydroxyprogesterone caproate 250 mg/estradiol valerate 5 mg. Their effects on carbohydrate metabolism, lipid metabolism, hemostasis, serum prolactin, cortisol, binding globulins and liver functions are reviewed. Areas requiring further research are identified.
17 alpha-Hydroxyprogesterone Caproate↗
Effects of norethisterone enanthate on certain body functions.
Effects of Norethisterone Enanthate (an injectable contraceptive) on body weight, blood pressure, blood cell count, level of haemoglobin, fasting blood sugar and serum cholesterol were studied in 31 women. It was observed that in the successful acceptors the pregnancy rate was nil. No appreciable change could be found in the body functions studied.
Adult↗
Effect of continuous local microdose norethisterone enanthate on the epididymis of adult rat.
Unilateral implantation of a small silastic capsule containing crystalline Norethisterone Enanthate (NE, average observed rate of release, 17-22 micrograms/24 h) into the epididymal fat-pad of adult rats induced drastic impairment of epididymal functional anatomy in the adjacent epididymis six weeks later without affecting the contralateral epididymis. Tubular elements in the ipsilateral epididymis were highly shrunken with their luminal epithelial height greatly reduced and the lumen devoid of spermatozoa as compared with the normal epididymis (full of spermatozoa) on the sham operated contralateral side.
Animals↗
Alterations in blood sugar, protein, and lipid levels in Indian women by norethisterone enanthate.
Fasting levels of sugar, protein, and lipids, namely, cholesterol, triglyceride, and phospholipid, were determined in the blood of 150 women taking an injectable contraceptive, norethisterone enanthate, 200 mg every 60 days for 24 months. Triglyceride and cholesterol showed a statistically significant decrease from 10 and 16 months of use; however, both values returned to control level after use for 24 months. Serum phospholipids and total protein did not show significant changes, while the blood sugar level increased significantly from 12 months onwards and remained elevated (P less than .001) up to the end of the trial period.
Adolescent↗
Long-term regulation of male fertility by norethisterone enanthate 'epididymal' implants: effect on libido and fertility of rabbits.
Bilateral insertion of silastic capsules releasing 38-44 micrograms norethisterone enanthate/24 h into the epididymal fat-pads was found to induce complete azoospermia leading to infertility in adult male rabbits 8 weeks after insertion of the progestin implants. The treatment did not exert any inhibitory effects on the libido and sexual behaviour of the animals as judged by objective parameters of mating. Further, the failure of the hormone-releasing implants was not found to exert any adverse effects on the embryos and pregnancy as indicated by the delivery of normal pups to females mated with implant-bearing males 3 weeks after the insertion of 'epididymal' implants.
Animals↗
Interpersonal testosterone transfer after topical application of a newly developed testosterone gel preparation.
OBJECTIVE: Transdermal testosterone gel treatment is an effective androgen substitution therapy with several advantages over conventional substitution therapies. Whereas side-effects due to overdosing of hypogonadal patients are unlikely, testosterone gel application without protection may cause severe side-effects in other subjects (partners, family members) by contamination. Therefore, the risk of testosterone transfer of a newly developed 2.5% testosterone gel preparation was evaluated. DESIGN: In two clinical randomized open single-centre studies on healthy male volunteers the percentage of testosterone remaining on the skin after gel application over time (n = 12) and the possibility of a transfer of testosterone to another person (n = 28) was evaluated. In the second study the endogenous testosterone production in the receiving subjects was suppressed by injecting 400 mg norethisterone enanthate (NETE). RESULTS: After 8 h approximately 60% of testosterone applied to the skin could be recovered. When the skin had been previously washed with water, only about 14% of applied testosterone could be recovered. After intense skin contact with a volunteer who had applied testosterone before on his forearm, no increase in testosterone serum levels could be found in NETE-suppressed men. CONCLUSION: Although considerable amounts of testosterone remain on the intact skin for several hours after evaporation of the alcohol vehicle, contamination of a second, especially female or prepubertal, subject causing side-effects seems very unlikely.
Administration, Cutaneous↗
Low dose injectable contraceptive norethisterone enanthate 20mg monthly--I. Clinical trials.
Clinical trials were undertaken with an injectable low dose progestational contraceptive, norethisterone enanthate 20 mg monthly (Net-en - 20). Data from the study indicate that Net-en - 20 is an effective contraceptive with lower incidence of menstrual cycle disturbances than the currently used injectable progestogens. There was a prompt return of fertility after the withdrawal of the drug. Net-en - 20 did not have any adverse effect on maternal nutritional status as assessed by anthropometric indices of nutritional status, and clinical sign of nutritional deficiencies or on lactational performance as assessed by mothers' impression on milk output and mean duration of lactation.
Actuarial Analysis↗
Alterations in protein, sialic acid and some enzymes in cervical mucus of female rats during NET-EN treatment.
The effect of norethisterone enanthate (NET-EN) on cervical mucus protein, sialic acid and some enzymes (e.g. peroxidase, alkaline phosphatase and alpha-amylase) were studied in adult female rats. One mg NET-EN every 12 days was found to be an effective contraceptive dose of this drug in this species, acting primarily through the cervical mucus. NET-EN produced a highly significant increase in protein content and peroxidase and alkaline phosphatase activities. However, sialic acid content and amylase activity did not exhibit any definite pattern after NET-EN therapy. The increased protein content together with persistent elevated levels of peroxidase and alkaline phosphatase corroborates the hypothesis that NET-EN creates a progestogenic phase which prevents sperm penetration and thus conception.
Alkaline Phosphatase↗
Pharmacokinetics, pharmacodynamic and endometrial effects of a single dose of 200 mg norethisterone enanthate.
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.
Adult↗
Long acting contraceptives. Present status.
Long acting injectable hormonal contraceptives are among the most effective fertility regulating agents developed; yet they are also among the most controversial because of animal data indicating a possible carcinogenic potential in several species. A critical analysis of these animal findings has revealed, in all instances, the existence of specific mechanisms not occurring in the human. For this reason, most national and international scientific bodies who have reviewed this issue have concluded that there are no toxicological reasons for not using long acting hormonal contraceptives. Long acting agents can be divided into 2 separate groups: those having a duration of action of one month, which are composed of a long acting oestrogen and a progestagen, and those lasting for several months which consist of only a progestagen. Among the injectable progestagen-only contraceptives tested, only 2 have so far reached the international market: depot medroxyprogesterone acetate (DMPA), which has been administered at 3- or 6-month intervals and norethisterone enanthate, which has been injected at intervals ranging between 2 and 3 months. The most important side effect observed with these 2 agents is a complete disruption of the menstrual bleeding pattern, leading - in some cases - to total amenorrhoea, which is more frequent with depot medroxyprogesterone acetate than with norethisterone enanthate. The latter, however, has a shorter duration of action with a higher pregnancy rate than the former. Other adverse reactions are rare and of no real importance. Metabolic effects with progestagen-only injectable preparations are, in general, mild and less marked than with combined oestrogen-progestagen formulations. Recent investigations have shown that the return of fertility following their use is delayed but in no way impaired. Monthly injectable oestrogen-progestagen combinations have been tested to a more limited extent and these agents are available only in a very few countries. Their main advantage over progestagen-only preparations is that they allow a reasonable menstrual bleeding pattern in the majority of cases. Their obvious disadvantage is that they contain a long acting oestrogen.
Animals↗
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.
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.
Female↗
Bleeding patterns of adolescents using a combination contraceptive injection for 1 year.
PURPOSE: This prospective observational study evaluated the bleeding patterns of adolescents receiving a monthly injectable contraceptive containing norethisterone enanthate 50 mg plus estradiol valerate 5 mg. MATERIALS AND METHODS: The study enrolled 73 volunteers aged between 14 and 19 years; of these patients, 38 (52%) recorded their menstrual cycles during 1 year. RESULTS: After 1 year of using the contraceptive, most of the 38 women (71.1%) had adequate menstrual patterns (two to four bleeding episodes; none lasting 10 days or longer; with a range of bleeding-free intervals not exceeding 17 days), 23.7% reported prolonged bleeding episodes, 2.6% had irregular bleeding and 2.6% had amenorrhea. Only 1 of the 38 teenagers is known to have discontinued the method due to bleeding. Among these 38 adolescents, dissatisfaction with bleeding patterns was not a frequent reason given for discontinuation of the monthly injectable contraceptive.
Adolescent↗
Some metabolic and hormonal changes in women using long acting injectable contraceptives.
Some metabolic and hormonal changes in women using longacting injectables as a contraceptive method were examined. The 2 main injectables utilized were depomedroxyprogesterone acetate (DMPA), given every 90 +or- 5 days, and norethisterone enanthate (NET/EN) injected every 60 +or- 5 days. None of the studied cases became pregnant during injectable use, indicating the high contraceptive efficacy of the method. No statistically significant changes were observed in hemoglobin, hematocrit, all protein fractions including albumin, alpha1, alpha2 beta, gamma immunoglobulins IgG, IgA, and IgM after 6 and 12 months in both groups of injectable users as compared with the preinjection values. Statistically significant suppression of the estimated hormones, Follitropin, Luteotropin, and Estradiol-17beta were detected in both groups of NET/EN and DMPA users, after 6 and 12 months, as compared with the preinjection values.
Africa↗