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At least 19 recordsLinked to original sources

Treatment of benign prostatic hyperplasia with hydroxyprogesterone-caproate: placebo-controlled study.

A placebo-controlled study with progesterone compound, 17-alpha-hydroxyprogesterone 17-n-caproate (Primostat), in 39 patients with benign enlargement of the prostate is reported. Statistical analysis of the results showed no evidence of significant improvement in patients receiving hydroxyprogesterone-caproate. No evidence of an effect as compared with the placebo was found when the residual urine, prostatic size, and histologic and ultrastructural changes of the removed prostatic gland in 6 of the patients, and in the luteinizing hormone, follicle-stimulating hormone, and estrogen urine levels in 21 patients were examined. Subjective effects, when carefully analyzed, provided some beneficial evidence, however not substantiated, when the patients' mode of voiding was carefully watched. The reported beneficial subjective improvement might be attributed to the enhancement of the beta-adrenergic response by the progesterone compound of the adrenergic receptors in the posterior urethra and bladder, presumably causing relaxation of its smooth muscle. The problems associated with the choice and measurement of parameters to be used in this type of investigation are discussed, and the absolute necessity of proper controls, statistical analysis, and close follow-up of the patients is pointed out.

Aged

Testosterone metabolism in benign prostatic hypertrophy: in vivo studies of gestonorone caproate and cyproterone acetate.

18 patients with obstructive benign prostatic hypertrophy were studied. A 5-day treatment with gestonorone caproate (200 mg daily and 200 mg on alternate days) and cyproterone acetate (300 mg daily) suppressed the plasma LH and serum LH levels. Subsequently, H3-testosterone was injected intravenously and its elimination from plasma and uptake and metabolism in the BPH tissue studied. The elimination of total radioactivity and H3-testosterone from plasma was not altered after the 3 treatment regimens as compared to the control group. The uptake of total radioactivity into BPH tissue and its intraprostatic metabolism particularly to dihydrotestosterone was significantly suppressed in the patients with daily injections of gestonorone. Cyproterone acetate and gestonorone caproate on alternate days did not cause this effect.

Aged

The influence of the progestogen gestonorone caproate on testosterone turnover in renal cell carcinoma. An in vitro study.

To investigate the effect of gestagens on renal cell carcinoma 300-mg slices of normal, human kidney, renal cell carcinoma (RCC), and preoperatively irradiated RCC were subjected to a short term incubation with 200 pmoles of 3H-testosterone and 1 and 2 mug of gestonorone caproate. In the normal kidney 61.4 per cent of the testosterone added was metabolized, the oxidation products androstenedione and epitestosterone outweighing by 6:1 the reduction products 5alpha-dihydrotestosterone and androstanediol. In RCC only 22 per cent of the testosterone was metabolized, with 8.5 per cent being converted to 5alpha-androstanes. Gestonorone caproate essentially did not influence testosterone turnover. This can be explained by its action as an inhibitor of the reductive pathway of the testosterone metabolism only, which is insignificant in these tissues.

Adenocarcinoma

Prevention of premature labor by 17 alpha-hydroxyprogesterone caproate.

Eighty pregnant women at high risk of giving birth prematurely were divided randomly into two groups. Treatment with either 17 alpha-hydroxyprogesterone caproate, 250 mg by intramuscular injection once a week, or a placebo was given in a double-blind fashion. Imminent premature labor occurred in 29.0% of the treated group and in 59.4% of the control group (p less than 0.025). The rate of premature deliveries was also significantly lower in the treated group (16.1%) than in the control group (37.82%) (p less than 0.05). There were no cases of perinatal death or fetal malformations in either group. The mean birth weight of all infants of the treated group was significantly higher than in those of the control group (3111.9 +/- 905 gm versus 2680 +/- 813.4 gm, p less than 0.05). The results support treatment with progesterone caproate for the prevention of premature labor.

17-alpha-Hydroxyprogesterone

Embryotoxicity of sex steroidal hormones in nonhuman primates: II. Hydroxyprogesterone caproate, estradiol valerate.

Two sex steroid compounds which have been used clinically for parenteral supportive therapy of pregnancy were examined for embryotoxic effects in rhesus and cynomolgus macaques. Hydroxyprogesterone caproate (HPC) alone or in combination with estradiol valerate (EV) were administered intramuscularly (i.m.) to pregnant monkeys at 7-day intervals between 20 and 146 days of gestation and fetuses were examined following cesarean section at 150 +/- 2 days. HPC alone was tested in both species at doses ranging from 0.01 X to 10 X the human dose equivalent (HDE); only rhesus monkeys were exposed to the HPC + EV combination at 0.1 X to 10 X HDE. Total embryolethality resulted following the administration of HPC alone and combined with EV at 1 X and 10 X HDE in rhesus monkeys; the level of abortions in cynomolgus monkeys exposed to HPC (0.1 X to 1 X HDE) was comparable to controls. A small number of nonspecific malformations and developmental variations observed in cynomolgus fetuses after HPC exposure were considered to be incidental findings. No anomalies were found in surviving rhesus monkey fetuses treated with HPC + EV. The results indicate that long-term in utero exposure to the progestin, HPC, alone or in combination with EV in rhesus and cynomolgus monkeys, is embryolethal but not teratogenic at doses up to ten times the human therapeutic dose.

17 alpha-Hydroxyprogesterone Caproate

Endocrine effects of 17 alpha-hydroxyprogesterone caproate during early pregnancy: a double-blind clinical trial.

The clinical and endocrine effects of progestogen therapy in early pregnancy were investigated using a double-blind randomized trial in 64 patients who had a viable fetus at 6 weeks gestation and had an increased risk of miscarriage. The patients were randomly allocated to receive either 17 alpha-hydroxyprogesterone caproate or a placebo between 7 and 12 weeks gestation. Four fetal ultrasonographic variables and 17 maternal endocrine variables were studied in each woman. Only four maternal serum variables (17 alpha-hydroxyprogesterone, prolactin, thyroxin and thyroxin binding globulin) rose significantly. The serum progesterone levels in the hormone supplemented group were on average 20% higher than in the placebo group but the difference was not statistically significant. However, the relation between the progesterone levels and the fetal outcome was not clear. Therefore it is not advisable to prescribe 17-OHP-C during early pregnancy to prevent a miscarriage.

17 alpha-Hydroxyprogesterone Caproate

Serum lipids and lipoproteins in patients with endometrial carcinoma receiving adjuvant treatment with hydroxyprogesterone caproate.

Serum levels of triglycerides, total cholesterol, and HDL-cholesterol were determined in 57 patients who were undergoing treatment for stage I endometrial carcinoma. The patients belonged to a clinical trial where group A (control) was treated with surgery plus intravaginal irradiation, whereas group B in addition was treated with hydroxyprogesterone caproate (5000 mg i.m. as a loading dose followed by 1000 mg every 2 weeks for one year). In group B patients followed during the first 13 weeks of treatment, the level of serum triglycerides remained stable, whereas the level of total cholesterol and HDL-cholesterol increased significantly. This increase could not, however, have been caused by the progestogen treatment, as similar changes were seen in group A patients followed for the same period of time. Long-term effects were looked for in patient groups examined 3-12 months after the start of treatment and in groups examined 3-6 months after the hormone therapy was stopped. In neither group could any significant difference in cholesterol or HDL-cholesterol be found. It is concluded that this type of progestogen treatment causes no significant change in the levels of triglycerides, cholesterol, and HDL-cholesterol.

17 alpha-Hydroxyprogesterone Caproate

Intramuscular administration of hydroxyprogesterone caproate in patients with endometrial carcinoma. Pharmacokinetics and effects on adrenal function.

A radio-immunoassay for the determination of the serum concentration of hydroxyprogesterone caproate (HPC) was established. After a single intramuscular injection of 1000 mg, the mean serum level reached its maximum (44-81 nmol/l) after 2-7 days. Patients on long-term adjuvant HPC treatment (consisting of 1000 mg daily for 5 days followed by 1000 mg every 2 weeks) presented peak hormone levels 2 weeks after commencing treatment. After a drop at 5 weeks, the mean serum level slowly increased again to 130 nmol/l after 25 weeks of treatment. Patients being treated with weekly injections had significantly higher serum levels than those treated every 2 weeks. Considerable inter-individual differences were observed. The serum concentrations of HPC measured in this study compare favorably with those previously found in patients treated with medroxyprogesterone acetate. The patients on adjuvant HPC showed no significant change in the levels of cortisol, dehydroepiandrosterone sulphate, androstenedione, or estrone during the first 25 weeks of treatment.

17 alpha-Hydroxyprogesterone Caproate

Trial of 17-hydroxyprogesterone caproate (Proluton Depot) in women with long-standing infertility; failure of estrogen positive feedback the following cycle.

In open and double-blind studies 40 women with long-standing unexplained infertility were investigated and treated with 17 alpha-hydroxyprogesterone caproate (17HPC, Proluton Depot). In the open study, 16 women with a high index of suspicious abortions were given 500 mg 17HPC imtramuscularly (i.m.) weekly for 6-16 weeks. Six of the women received the drug from a time preceding the expected date of a period; 2 of these conceived that cycle and their pregnancies continued to term, while 4 were not pregnant. Ten women (9 with definite previous abortions) were given 17HPC when they suspected (correctly) that they were pregnant. Their pregnancies continued to term in all but 1, who had a premature delivery (still-birth) at 34 weeks. In the double-blind study 24 women were given injections of 17HPC or placebo i.m. at weekly intervals, from about 4 days before the expected period (day -4), provided that the level of progesterone (Prog) (on days -9 to -7) was greater than 10 nmol/l. After placebo no delay in menstruation or disruption of the succeeding cycle was observed. In 14 of 16 cycles in 14 women given 500 mg 17HPC the withdrawal period was delayed by a few days, and then followed by highly erratic bleeding over the next 1-3 months. The dose was therefore reduced to 250 mg 17HPC but the same problem resulted in 8 of 29 cycles in 16 women (including the above studied in later cycles). Regular cycles were eventually restored in all cases but in 3 this necessitated treatment with the contraceptive pill (Microgynon). In most of the post-treatment cycles there was a progressive and prolonged estradiol (E2) rise, which was not preceded by changes either in serum FSH concentration or in the LH/FSH ratio nor associated with the expected positive feedback rise in LH. We conclude that 17HPC disrupts the following cycle, probably by allowing follicular development while interfering with positive LH feedback. None of the patients of the double-blind study had conceived (as evidenced by undetectable hCG levels). Our study confirmed that this progestogen exerts no direct luteolytic effect. However, in order to establish the efficacy or otherwise of 17HPC given before the end of the cycle, women should be selected with a very high index of suspicion of recurrent early implantation failure or abortion.

17 alpha-Hydroxyprogesterone Caproate

Effect of oxyprogesterone caproate, tamoxifen and their combination on the level of steroid hormone receptors in the tumor, and some parameters of the reproductive system in patients with endometrial cancer.

The results of preoperative use of oxyprogesterone caproate (OPC), Tamoxifen and their combination in 165 patients suffering from primary endometrial carcinoma are presented. It was shown that Tamoxifen was able to increase concentrations cytoplasmatic receptors to progesterone in the tumor. The incidence of specific hormonal pathomorphosis in the tissue of the tumor in patients who received a combination of OPC and Tamoxifen was significantly higher (80% of cases) as compared to the separate use of OPC (60%) or Tamoxifen (57%).

17 alpha-Hydroxyprogesterone Caproate

A comparative study of the efficiency of hydroxyprogesterone caproate and of chlormadinone acetate in the prevention of premature labor.

The efficacy of caproate of hydroxyprogesterone and acetate of chlormadinone in preventing premature labore was compared in a controlled trial. The survey was based on 211 pregnant women with a high risk of premature delivery discovered during clinical examination. There are no significant differences between the two groups in either length of gestation, delay between the beginning of treatment and delivery or other parameters related to prematurity. The absence of evidence suggesting any significant difference between the two treatments can have three possible causes (which are discussed): the methodology, the inefficacy of the two products or the equivalent efficacy of the two products.

Chlormadinone Acetate

Efficacy of 17alpha-hydroxyprogesterone caproate in the prevention of premature labor.

We conducted a double-blind study to determine the efficacy of 17alpha-hydroxyprogesterone caproate in preventing premature delivery in 43 high-risk patients. Premature delivery did not occur in 18 patients receiving the progestational agent, whereas 41 per cent of the 22 receiving the palcebo had premature delivery (P less than 0.01). The mean duration of pregnancy and the mean birth weight in the former group (38.6 weeks +/- 1.6 S.D., and 2836 g +/- 412 S.D.) were both significantly greater (P less than 0.025) than that in the latter (35.2 weeks +/- 6.7 S.D.; 2361 g +/- 1085 S.D.). The perinatal mortality rate in the group given the progestational agent (O per cent) was significantly less than that observed in the placebo group (27 per cent) (P less than 0.05). Although there were no complications attributable to the progestational drug, the study population was too small for assessment of immediate or long term safety. However, the results indicate a possible obstetric use for this drug.

Adult

Allergic contact dermatitis from fluocortolone, flucocortolone pivalate and fluocortolone caproate.

Two patients with contact allergy to Ultralan preparations are reported. Each Ultralan preparation contains two of three related fluocortolone derivatives. The first patient reacted to all three derivatives. The second patient reacted to flucortolone and when retested 4 months later also to fluocortolone pivalate but ot to flucortolone caproate. The negative reaction to fluocortolone pivalate at the first examination was probably false negative due to a low test concentration. In order to avoid false negative patch test reactions the fluorinated steroids should possibly be applied in concentrations higher than 1%. No cross sensitivity to the other steroids for topical use was found.

Aged

Anti-androgen TSAA-291. II. Manifestation of the anti-androgenic action of a steroid ester TSAA-330 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one caproate) and elucidation of its long-lasting mechanism using a simple steroid determination technique.

Using a simple steroid determination technique, in situ steroid absorption from a subcutaneously injected sesame oil solution in rats was pursued following the time-course changes in the steroid concentration. Based on the knowledge thus obtained, the anti-androgenic effect of a steroidal compound, TSAA-330, could be manifested in the subcutaneous route. (1) Anti-androgenic steroid TSAA-291 and its esters in the subcutaneously injected sesame oil solution were selectively absorbed into the general circulation at different rates according to their chemical nature and structures, while the oil itself remained at the injected site for a considerably long period. At the injected site where subcutaneous doses of steroids molar equivalent to 50 mg of TSAA-291 were administered in 5 ml/rat of sesame oil, TSAA-291 decreased to the level of 10% of the initial concentration on the 4th day. TSAA-328 decreased slowly to the 50% and 20% levels on the 7th and 21st day, respectively. TSAA-335 decreased more slowly to the 50% level on the 14th day. TSAA-330 decreased most slowly only to the 70% level on the 49th day. (2) A single subcutaneous administration of 200 mg of TSAA-330 suppressed the weight increase of the accessory sex organs caused by a single subcutaneous injection of testosterone caproate (10 mg) in the immature orchiectomized rat. The suppressive effect was obvious from 2 weeks after the administration, and seemed to last for more than two weeks. The levator ani weight was not affected by the administration of TSAA-330. (3) Dose-dependent inhibitions of the accessory sex organs were obtained three weeks after a single subcutaneous administration of 50 to 400 mg of TSAA-330 in the adult male rat. (4) Daily oral administrations of 50 mg of TSAA-291 or TSAA-330 to the adult male rat for 8 days resulted in depression of the accessory sex organs to almost the same extent obtained with either agent. One week after the last administration, however, the weight of the accessory sex organs of the TSAA-291-administered animals recovered to almost the comparable level with the control, whereas a significant after-effect of the inhibition was still evident in the TSAA-330-administered animals.

Absorption

Prophylactic use of hydroxyprogesterone caproate in abdominal surgery during pregnancy. A retrospective evaluation.

Abdominal surgery (unrelated to delivery) during pregnancy is not common. Review of a recent 17-year experience at our institution revealed 112 surgical procedures among 25,189 deliveries--an incidence of 0.44% (1 case for every 225 deliveries). Progestational agents have been used prophylactically in such procedures, but few studies have adequately assessed the effectiveness of these drugs to prevent onset of premature labor. The present study involved 35 gravid patients who had been treated with various doses of hydroxyprogesterone caproate before and after operations unrelated to delivery. These 35 patients were matched with 35 gravid control patients who had undergone similar operations but who had not received progestational compounds. Analysis revealed no significant difference in the abortion rate between these two groups.

Abortion, Spontaneous

A comparative multicentre trial of halometasone ointment and fluocortolone plus fluocortolone caproate ointment in the treatment of psoriasis.

A multicentre, between-patient, comparative trial was carried out by nine dermatologists in the Federal Republic of Germany to compare the efficacy and tolerability of 0.05 halometasone ointment with those of an ointment, containing 0.25% fluocortolone + 0.25% fluocortolone caproate, in patients with psoriasis vulgaris. The evaluable trial population consisted of 182 patients, 115 males and sixty-seven females. Halometasone ointment yielded a higher success rate ('good' to 'very good' results), namely 56.4% than that obtained with the comparative ointment (45.4%). Halometasone ointment also produced a higher cure rate, namely 26.6%, than that reported with the comparative preparation (19.3%). An improvement of one score over the pre-treatment clinical status of the psoriatic lesions reported at the Day 10 visit was significantly higher (p = 0.04), namely 48.9%, with halometasone ointment than that with the comparative preparation (35.2%). The percentages of patients obtaining an early cure, i.e. in less than 30 days, and onset of action were practically identical in both treatment groups. No adverse effects were reported in any of the ninety-four patients treated with halometasone ointment, while unwanted reactions were observed in three of the eighty-eight patients treated with the comparative preparation.

Administration, Topical