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PubMed1977

[Hormontal treatment of pre-tumorous diseases of the testis in rats].

Tumours and proliferates of the testes from spermatogenic epithelium were treated with estrogens, and those from the interstitial cells-with androgens and 17-hydrosyprogesterone caproate. Depression of the folliculo-stimulating function of the pituitary body with a simultaneous stimulation of the luteinizing hormones (LH) production under the effect of estrogen led to cessation of teratoma and seminoma growth, and to the resolution of the proliferates. When androgens or 17-hydroxyprogesterone caproate were used, depression of the LH led to cessation of the tumour growth, and to the resolution of proliferion of proliferates from the interstitial cells.

Animals↗
PubMed1980

[Clinico-morphological changes during treatment of endometrial cancer with progestins].

The results of the complex clinico-morphological study of the effect of 17-a-hydroxyprogesterone-caproate are reported in 71 patients aged from 37 to 75. Stage I was noted in 17 patients, stage II--in 51, stage III--in 3. A total dosage was 5,0; 10,0; 20,0 and 30,0 for the course of treatment. Following the hormonal therapy all these patients were subjected to surgery. To study the hormonal pathomorphism specimens from the uterine cavity were assayed histologically and cytologically prior to and during the hormonal therapy, the removed specimen was examined after the operation. The clinico-morphological studies indicated that 17 GPC shows the antitumor effect in endometrial cancer, so the complete tumor regression seems to be possible. The antitumor effect is mostly pronounced at initial stages of the disease and with high-differentiated tumors. The data obtained may be used to solve the problem on the purposeful application of 17 GPC either in the complex of therapeutic measures or as a separate method of treatment.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1983

Quantitation of meperidine hydrochloride in pharmaceutical dosage forms by high-performance liquid chromatography.

A high-performance liquid chromatographic (HPLC) method for the quantitative determination of meperidine hydrochloride in pharmaceutical dosage forms was developed. The method is reproducible and precise with relative standard deviations (based on six readings) of 1.2% with hydroxyzine and 0.93% with hydroxyprogesterone caproate as the internal standards. A variety of other active and inactive ingredients which were mixed with meperidine hydrochloride did not interfere with the assay procedure. Among the ingredients tested were acetaminophen, atropine sulfate, disodium edetate, metacresol, phenol, promethazine, and sodium metabisulfite. This method appears to be stability-indicating since a hydrolyzed sample of meperidine showed zero potency and a new peak with a different retention time.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1988

Effects of perinatal exposure to a synthetic estrogen and progestin on mammary tumorigenesis in mice.

The effects of perinatal exposure to synthetic estrogens and progestins on mammary tumorigenesis were studied in female C3H/HeN/MTV + mice. Mice were treated neonatally with 0.001 microgram/day diethylstilbestrol (DES), with 15 micrograms/day 17 alpha-hydroxyprogesterone caproate (HPC), or with oil on days 1-5 of life (birth = day 1). As adults, neonatally hormone-treated mice received long-term treatment with a synthetic estrogen and progestin combination or vehicle. Animals were palpated weekly for mammary gland tumors. The effect of treatment on the probability of tumor development was examined. Neonatal treatment with a low dose of DES increased the probability of mammary-gland tumor formation, whereas neonatal treatment with HPC had a slightly protective effect on tumorigenesis. Subsequent treatment of adult mice with synthetic steroids did not affect mammary gland tumorigenesis in neonatally DES-treated or oil-treated animals. There was a significant interaction between the effect of neonatal HPC treatment and subsequent steroid treatment on mammary tumorigenesis but examination of the data indicated that this interaction was due to the protective effect of HPC in the absence of subsequent exposure to synthetic steroids and the probability of tumor appearance in mice treated with both HPC and synthetic steroids as adults did not differ from that of neonatally oil-treated controls.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed2000

Noncompetitive, reversible inhibition of aminoacylase-1 by a series of L-alpha-hydroxyl and L-alpha-fluoro fatty acids: ligand specificity of aspergillus oryzae and porcine kidney enzymes.

L-lactate and L-beta-phenyllactate have been identified in the culture broth of Streptomyces sp. KY-11 as reversible noncompetitive inhibitors of Aspergillus oryzae aminoacylase-1 and porcine kidney aminoacylase I. A series of alpha-hydroxyl acids (DL-R-CH(OH)-COOH, R = Et, n-pro, n-butyl, n-pentyl, n-hexyl) also inhibited the two enzymes in reversible noncompetitive kinetics, and the inhibition potency (-log K(i)) increased with the increased hydrophobicity of the R group. The two eukaryotic enzymes showed distinct preferences to the ligand alpha-alkyl group, and the fungus enzyme was inhibited by L-beta-phenyllactate (R = benzyl) 10(3)-fold more potently than the mammalian enzyme. L-alpha-Fluoro-beta-phenyl-propionate and its D-isomer were used to show that the L-configuration of the alpha-substituent was important for potent inhibition of both the enzymes. The fungus aminoacylase-1 steeply decreased the affinity to alpha-fluoro- and alpha-hydroxy-n-caproate as pH was raised from 7 to 11, whereas the mammalian enzyme retained the affinity to these ligands under alkaline conditions. These results suggest that A. oryzae aminoacylase-1 has an acidic residue that interacts with -OH or -F, while the mammalian enzyme would have a basic residue that recognizes the alpha-substituents.

Alkylation↗
PubMed1994

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↗
PubMed1988

Ovarian tumors in pregnancy.

Thirty-eight women were operated for an ovarian tumor diagnosed during pregnancy, with an incidence of 1/2328 deliveries. The diameter of all tumors was above 5 cm. Of the 31 women operated before delivery, seven were untreated and 24 received supportive progestational therapy. The rate of abortions was 85.7% in the untreated group and 10% in the hydroxy-progesterone-caproate group (HPC) (P less than 0.02). When the women received a total dose of HPC of more than 300 mg, 9 of 10 pregnancies reached term with a live child. Two ovarian malignancies were found, 5.3% of all cases. In 42.9% of the women there were fertility problems later in life. Ovarian tumors during pregnancy should be removed as soon as possible, irrespective of the age of the pregnancy. If fully progesterone therapy is given, the danger of abortions is reduced to a minimum. Prophylactic antibiotic treatment should also be administered.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1981

Hormone mediated changes in monoamine stores and regulation of enzymes of biosynthesis and metabolism in the rat adrenal gland. Influence of progesterone, estradiol, ACTH and testosterone administration.

The influence of daily injections, for 7 days, of 17-hydroxyprogesterone caproate (8 mg/100 g body weight pro die), of estradiol-17 beta 17-undecylate (1.2 mg/100 g body weight pro die) of testosterone enanthate (2 mg/100 g body weight pro die) and of ACTH (4 IU/100 g body weight pro die) to male Wistar rats, weighing 200 g, were investigated. Monamine storage and regulation of enzymes phenylethanolamine N-methyl transferase (PNMT), monoamine oxidase (MAO) and catechol-O-methyl transferase (COMT) were studied in the adrenal glands. Results from testosterone treated rats were especially significant : the hormone administration decreased the stores of dopamine and norepinephrine (epinephrine precursors), stimulated PNMT and decreased metabolism of epinephrine by MAO and COMT. However, the adrenal content of epinephrine remained in the normal range. These findings suggest that uptake of epinephrine is accelerated in peripheral tissues by testosterone.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1995

Biosynthesis and characterization of hydroxybutyrate-hydroxycaproate copolymers.

Most polyhydroxyalkanoates (PHAs) reported to date fall into one of two broad classes: either hydroxybutyrate-hydroxyvalerate copolymers (typified by the PHA produced by Alcaligenes eutrophus), or hydroxyoctanoate-rich heteropolymers (typified by the PHA produced by Pseudomonas oleovorans). Few reports of copolymers rich in hydroxybutyrate (HB), but containing a minor proportion of a co-monomer with a higher carbon number than valerate, have appeared. Here we report on the biosynthesis and characterization of HB-rich polymers containing 2-4 mol% of hydroxycaproate (HC) units, as well as a terpolymer containing HC and hydroxyoctanoate (HO) units. These polymers were produced in good yield by Comomonas testosteroni, Bacillus cereus and an unidentified third organism when grown on caproate or octanoate. The minor co-monomers were found to be rejected from the PHB crystallites by X-ray analysis and by quantitative analysis of the melting point depression. The greatly reduced melting point, coupled with the retention of a high degree of crystallinity, could make these materials attractive as melt-processible thermoplastics.

Bacillus↗
PubMed2005

Role of progestogens for the prevention of premature birth.

Premature birth represents a major cause of perinatal morbidity and mortality. The short- and long-term sequelae of prematurity have serious consequences for newborn survival and health in later life. In addition, prematurity is a major problem with regard to health expenditure. Despite major progress in obstetrics, perinatology and neonatology, the percentage of premature birth persists and there is even a tendency towards a slight increase. Therefore, besides screening programmes for the detection of vaginal infections, additional therapeutic opportunities must be sought. According to previously published data, vaginal progesterone and intramuscular 17alpha-hydroxyprogesterone caproate should be considered possible treatment options for the prevention of preterm delivery.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1985

Congenital malformations among offspring exposed in utero to progestins, Olmsted County, Minnesota, 1936-1974.

Comparison of a cohort of 988 offspring exposed in utero to exogenous progestins with a matched cohort of unexposed offspring did not result in detection of an association of congenital anomalies with exposure. The conclusions are based primarily on outcomes of pregnancy with exposure to progesterone and 17 alpha-hydroxyprogesterone caproate, and may not apply to androgenic progestins. Offspring exposed to combinations of progestins and estrogens were excluded from this study and may have a different distribution of anomalies.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1998

Prodrugs of gestodene for matrix-type transdermal drug delivery systems.

PURPOSE: The aim of this study was to enhance the transdermal absorption of the highly active progestin gestodene from matrix type transdermal delivery systems (TDDS) by formation of prodrugs with improved matrix solubility. METHODS: Gestodene esters were synthesized via acylation of the drug with the respective carboxylic anhydrides. Subsequently TDDS were produced using the solvent cast method. Selected formulations were examined with in vitro diffusion experiments using skin of nude mice. RESULTS: One prodrug, gestodene caproate proved to be an oil at ambient temperature and showed a very high solubilty of over 10.5% in the TDDS matrix. Within in vitro penetration studies using those systems the prodrug exhibited a significantly higher transdermal penetration rate than gestodene from reference systems. Furthermore, the prodrug was hydrolyzed to the parent drug to a high extent during the passage of the skin. CONCLUSIONS: Designing prodrugs to the requirements of matrix TDDS is an efficient way of enhancing the transdermal drug flux rate.

Acylation↗
PubMed1999

Ion-pair partition of quarternary ammonium drugs: the influence of counter ions of different lipophilicity, size, and flexibility.

PURPOSE: The ion-pair partition of quaternary ammonium (QA) pharmacons with organic counter ions of different lipophilicity, size, shape and flexibility was studied to elucidate relationships between ion-pair formation and chemical structure. METHODS: The apparent partition coefficient (P') of 4 QAs was measured in octanol/pH 7.4 phosphate buffer system by the shake-flask method as a function of molar excess of ten counter ions (Y), namely: mesylate (MES), acetate (AC), pyruvate (PYRU), nicotinate (NIC), hydrogenfumarate (HFUM), hydrogenmaleate (HMAL), p-toluenesulfonate (PTS), caproate (CPR), deoxycholate (DOC) and prostaglandin E1 anion (PGE1). RESULTS: Based on 118 of highly precise logP' values (SD< 0.05), the intrinsic lipophilicity (without external counter ions) and the ion-pair partition of QAs (with different counter ions) were characterized. Linear correlation was found between the logP' of ion-pairs and the size of the counter ions described by the solvent accessible surface area (SASA). The lipophilicity increasing effect of the counter ions were quantified and the following order was established: DOC approximate to PGE1 >> CPR approximate to PTS >> NIC approximate to HMAL >> PYRU approximate to AC approximate to MES approximate to HFUM. Analyzing the lipophilicity/molar ratio (QA:Y) profile, the differences in the ion-pair formation were shown and attributed to the differences in the flexibility/rigidity and size both of QA and Y. CONCLUSIONS: Since the largest (in average, 300 X) lipophilicity enhancement was found by the influence of DOC and PGE1 and considerable (on average 40 X) increase was observed by CPR and PTS, it was concluded that bile acids and prostaglandin anions may play a significant role in the ion-pair transport of quaternary ammonium drugs and caproic acid and p-toluenesulfonic acid may be useful salt forming agents to improve the pharmacokinetics of hydrophilic drugs.

Absorption↗
PubMed1994

Rapid increase in lumbar spine bone density in osteopenic women by high-dose intramuscular estrogen-progestogen injections. A preliminary report.

This prospective pilot study has been carried out to assess the effect of high parenteral doses of estrogens and progestogens on lumbar spine bone density in osteopenic women. Thirteen osteopenic women received 40 mg estradiol valerate and 250 mg hydroxyprogesterone caproate by intramuscular injections once a week for 6 months (so called "pseudopregnancy"). One g oral calcium was added. Six out of the 13 patients (49.5 +/- 4.8 y were peri- and postmenopausal = group A. Seven patients (21.5 +/- 2.2 y) suffered from primary and secondary amenorrhea, in 4 out of them due to gonadal dysgenesis = group B. Estradiol was measured by commercial radioimmunoassay. Bone density was determined by dual-energy X-ray absorptiometry (DEXA) of the upper 4 lumbar vertebrae. Lumbar spine bone density as well as estradiol serum levels were measured before and 3 and 6 months after therapy, respectively. Estradiol increased from 34.8 +/- 7.5 pg/ml to 3226 +/- 393 pg/ml after 3 months and to 2552 +/- 254 pg/ml after 6 months, respectively, in group A. Bone density increased by 15.3 +/- 3.6% within the first 3 months to a total of 18.8 +/- 3.9% after 6 months, respectively. Two patients we have controlled for two years, maintained this increase. In group B estradiol increased from 27.8 +/- 6.5 pg/ml to 3028 +/- 728 after 3 and to 2491 +/- 684 pg/ml after 6 months. Bone density in this group increased by 11.8 +/- 1.9% within 3 and to a total of 18.2 +/- 2.8% after 6 months.(ABSTRACT TRUNCATED AT 250 WORDS)

17 alpha-Hydroxyprogesterone Caproate↗
PubMed2001

Preliminary experience with steroidal ovarian suppression for prevention of severe ovarian hyperstimulation syndrome in IVF patients.

The purpose of the study was to evaluate the efficiency of administration of high dose progesterone in combination with oestradiol during the luteal phase for the prevention of ovarian hyperstimulation syndrome in a high-risk population of patients undergoing in vitro fertilization. An observational study was carried out involving 21 women (mean age 28.6 years) undergoing controlled ovarian stimulation for in vitro fertilization. The women were identified as at risk of ovarian hyperstimulation syndrome as they had suffered from the condition when hCG was used for luteal phase support in previous cycles. Steroidal suppression of the stimulated ovary on days 2, 6, 10 and 14 after embryo transfer was achieved by intramuscular injections of 500 mg hydroxyprogesterone caproate and 10 mg oestradiol valerate. The incidence of moderate and severe ovarian hyperstimulation syndrome under steroidal ovarian suppression, serum progesterone concentration and pregnancy rates were compared with those in cycles in which human chorionic gonadotrophin was used for luteal phase support. No cases of moderate or severe ovarian hyperstimulation syndrome occurred under steroidal ovarian suppression. Despite low progesterone concentrations (mean 10.7 nmol l(-1), range 2.6-24.5), indicating almost complete ovarian suppression, the pregnancy rate was not impaired. These preliminary results indicate that steroidal ovarian suppression during the luteal phase is a promising tool for reducing the incidence and severity of ovarian hyperstimulation syndrome in a high-risk population, without compromising the pregnancy rate.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed2003

Prevention of severe ovarian hyperstimulation syndrome (OHSS) in IVF patients by steroidal ovarian suppression--a prospective randomized study.

Ovarian hyperstimulation syndrome (OHSS) is the major complication associated with artificial reproductive technologies. The aim of this study was to assess the potential of exogenous steroids to prevent OHSS without adversely affecting pregnancy rate. A prospective and randomized study including 945 consecutive cycles in 603 women (mean age 28.6 years) was carried out to evaluate the efficiency of high-dose progesterone and oestradiol administration during the luteal phase to prevent OHSS. After ovulation induction, patients were allocated by a series of computer-generated random numbers to receive either 5000 iu human chorionic gonadotrophin (hCG) 4 and 8 days after embryo transfer (group 1, n = 534) or 500 mg hydroxy-progesterone caproate and 10 mg oestradiol valerate on days 2, 6, 10 and 14 after embryo transfer (group 2, n = 411), by i.m. injection. Total pregnancy rate was 24% (97 of 411) and 23% (121 of 534), and median serum progesterone concentrations on day 15 after embryo transfer were 5.8 ng ml(-1) (range 0.1-298) and 0.1 ng ml(-1) (range 0.1-372) in groups 1 and 2, respectively (P = 0.001). One hundred and sixty-three (30.5%) women in group 1 and 22 (5.4%) women in group 2 developed signs of OHSS (P < 0.0001). These results indicate that steroidal ovarian suppression during the luteal phase is a promising tool to reduce the incidence and severity of OHSS in a high-risk population without compromising the pregnancy rate.

17 alpha-Hydroxyprogesterone Caproate↗
PubMed1992

The effect of 17 alpha-hydroxyprogesterone caproate/oestradiol valerate on the development and outcome of early pregnancies following in vitro fertilization and embryo transfer: a prospective and randomized controlled trial.

A prospective and randomized study was performed to investigate the effect of supportive hormones on the development and outcome of early pregnancies following in vitro fertilization and embryo transfer. Immediately after pregnancies were confirmed endocrinologically on day 15 after oocyte collection, 17 alpha-hydroxyprogesterone caproate and oestradiol valerate (PC/EV) was administered to half of the patients in a randomly controlled trial. One group received supportive treatment until the twelfth week of gestation, whereas the other group received no treatment at all. Both groups were followed up by measurements of serum levels of human chorionic gonadotrophin (HCG), oestradiol and progesterone every three days until day 35, when a first ultrasound examination was carried out to confirm fetal vitality. Subsequently, pregnancies were monitored sonographically at regular intervals. In cases of miscarriage, dilatation and curettage was performed and histology analysed. A total of 120 pregnant patients entered the study: 55 of them received hormone treatment and 65 patients were controls. Within the treatment group 48 (89%) clinically ongoing pregnancies were observed, five (9%) miscarriages occurred after the seventh week of gestation and one preclinical pregnancy was noted. In the control group, 38 (59%) ongoing pregnancies were observed, nine (14%) miscarriages occurred and 17 (27%) preclinical pregnancies were recorded. Two ectopic pregnancies, one in each group, were excluded from evaluation. A significantly higher percentage of pregnancies were intact at 7 weeks of gestation after treatment with PC/EV (p less than or equal to 0.01).

17 alpha-Hydroxyprogesterone Caproate↗