Method for preventing acute exposure to organophosphates
SUBSTANCE: what is presented is a method for acute exposure to organophosphates with pronounced non-anticholinesterase mode of toxicity. A method consists in preventive administration of β-oestradiol 100 mg/kg 20-60 min prior to application of the toxic agent organophosphate.
EFFECT: reducing the manifestations of first signs of the exposure, developing convulsions and complete elimination of animals' death experimentally, administering β-oestradiol 5 days or 1 day before the exposure has not been producing such an effect.
The present invention may find application in medicine as a prophylactic agent in acute poisoning cholinesterase poisons with nervously-paralytic action.
At present time for emergency aid in cases of poisoning by substances with marked anticholinesterase activity recommended anticholinergics and reaktivatory cholinesterase (e.g. 1-methyl-5-[2'-benzyldimethylammonium)ethyl]carbamoyl-pyridine-2-aldoxime dichloride in the form of a 15% aqueous solution (patent RF №2243770, publ. 10.01.2005, A61K 31/4425, A61K 31/455, A61P 39/02) whose action is directed primarily to the blockade of cholinergic effects of toxicants. However, despite the relief of a number of manifestations of intoxication, their introduction is only partially addresses the development of seizures, masking the true severity of the lesion [Kolbasov S. E. Comparative efficacy pantethine and atropine under experimental simulation of an emergency situation on objects on chemical weapon destruction / S. E. S. Kolbasov, P. Nechiporenko, M. B. Melikhov [et al.] / / Proceedings of Institute of toxicology, dedicated to the 75th anniversary of the Foundation day: Sat. article edited by Professor S. P. Paciorek. - SPb.: ELBI-SPb, 2010. - S. 160-163, Mohort N. And. The modern condition of development of antidotal remedies for the treatment of lesions of the nerve agents / N. And. Mohort, Etc�ula // Modern problems ciï - 2003. - No. 2. - P. 49-55].
At the same time, long-term persistent cramps define high risk of death struck and disability, as well as the formation of neurodegenerative changes in an intoxication distant period [Prozorovsky V. B. New data on not sinaps (distant) effects of organophosphorus cholinesterase inhibitors (Review of literature.) / Prozorovsky V. B., S. V. Chepur // Tox. Vestn. 2001. No. 4. C. 2-7].
Lack of effect of available therapeutic agents allows to make a conclusion about the importance neholinergichesky mechanisms in the pathogenesis of poisoning by organophosphates and emphasizes the necessity of correction that determines the relevance of search for new means of pathogenetic therapy of lesions. Mostly it relates to acute poisoning with compounds with anticholinesterase activity, which has a pronounced pantyhosepictures mechanism of toxic action, such as Malathion, metaphos, etc. In this regard, the search continues for ways to improve the efficiency of emergency treatment of poisoning with organophosphates pronounced pantyhosepictures mechanism of toxic action, one of which is the study of compounds of steroid structure, including estrogenic hormones with FAMK-mimetic and glutamatemediated effect.
The basis for invented�I put the task of creating an effective method of prevention of acute poisonings with organophosphates pronounced pantyhosepictures mechanism of toxic action.
A solution to a technical problem is provided in that prophylactically for 20-60 min before the application of toxic substances used β-estradiol at a dose of 100 mg/kg.
To simulate intoxication as an example used metaphos, which was injected intramuscularly once the rate of 0.1 ml/kg of body weight of the animal.
Working solutions of β-estradiol was prepared in 4% aqueous solution of tween-80 ex tempore and injected intramuscularly once in doses of 25 to 100 mg/kg of body weight of the animal.
Observation of experimental animals was carried out for 15 days. During the period of observation in experimental animals was recorded the time of occurrence of the main symptoms (lockjaw, tremors, convulsions) and time to onset of death.
The findings of the experimental data were subjected to standard statistical analysis with calculation of average value and the average error. A quantitative estimate of the death rate of animals was performed using probit analysis (Finney). The assessment of differences of mean values was performed using t-student criterion. The average value of the indicators and its error were determined using the tables of interest and their errors in Genes V. S. (1967). To assess the significance of intergroup differences of indicators used Fisher's exact test. Evaluation of the protective activity prep�preparations was carried out by examining the latent period of onset of the first symptoms of intoxication, the latent period for the development of seizures, the time until death of animals, the case-fatality rate (LD50).
To determine the effectiveness of β-estradiol on the model of acute poisoning metafoam was an optimal effective dose and the optimal time of drug administration.
Studies to determine the optimal effective dose of β-estradiol was found that the prophylactic use of the drug had an impact on the dynamics of poisoning caused by metafoam at a dose of 1 LD50,and helped reduce the severity of symptoms (table 1).
From the data presented in table 1. it follows that the use of β-estradiol at doses of 75 and 100 mg/kg 20 min before the injection of the poison is in the dose 1-LD50contributed to a significant increase in NO50development of the first signs of intoxication and ET50start convulsing all degrees compared with the control group. At the same time, the use of the drug in the doses of 25 and 50 mg/kg did not significantly affect these indicators. In addition, it was shown that the introduction of high doses of estrogen were associated with decreased frequency of seizures in the acute poisoning metafoam at a dose of 1 LD50. In the control group cramps 1-5 degrees, developed at 100-17% of specimens, and preventive �primenenie β-estradiol at a dose of 100 mg/kg reduced the likelihood of seizures 1-2 and 3-4 degrees to 17±11% (differences from control are significant at p< 0,05). The introduction of the drug in doses of 75 mg/kg and 100 mg/kg prevent the development of seizures 5-th degree in all animals.
Results analysis of the dynamics and frequency of death of the animals suggests that the prophylactic use of β-estradiol for 20 min to acute poisoning metafoam at a dose of 1 LD50was accompanied by dose-dependent change of the pattern of intoxication, reducing its severity and reduce the frequency of death. The maximum protective effect was observed against the background of preventive applications of the drug in a dose of 100 mg/kg, which completely prevented the death of poisoned animals (p<0,05).
To determine the optimal time for application of β-estradiol was administered at a dose of 100 mg/kg for 5 days, 1 day, 1 hour, 20 mins to poisoning and in the development of the first signs of intoxication, caused by the introduction of metaphase in doses of 1 LD50, 1,25 LD50and 1.5 LD50. Obtained in the course of this experiment the data presented in table 2.
Found that prophylactic use of the drug intramuscularly single dose of 100 mg/kg for 5 days or 1 day before the injection of metaphase in all tested doses had no effect on the dynamics of signs of intoxication and death of animals.
The introduction of the drug for 20 minutes before application of the poison to animals at a dose of 1 LD50increased NO50development of the first signs of into�ikali and seizures, warned the convulsions 1-4 degrees at 83,3±17% of the individuals of the group (differences from control are significant at p<0,05), and completely prevented the development of seizures 5 degrees (p<0.01) and mortality (p<0,05). In rats, which metaphos was introduced in doses of 1.25 LD50or 1.5 LD50increased NO50development of the first signs of poisoning, ET50the development of seizures and the occurrence of death (all differences were significant when compared with the control group).
The use of β-estradiol for 1 h to defeat metafoam at a dose of 1 LD50contributed to the increase of ET50development of the first signs of intoxication (significantly difference at p<0.05) and ET50of seizures 1-2 and 3-4 degrees and completely prevented the appearance of seizures 5 degrees and the death of animals. In rats, which metaphos was introduced in doses of 1.25 LD50or 1.5 LD50increased NO50development of the first signs of intoxication, ET50the development of seizures and ET50the occurrence of death (all differences were significant when compared with the control group), however, the complete prevention of seizures 5 degrees and deaths were noted.
The introduction of β-estradiol in the development of the first symptoms of intoxication with poison in the dose of 1 LD50contributed to the reduction in the frequency of death, but were not warned of convulsions Shin�Roma. Increasing the dose of toxicant completely neutralized the protective effect of the drug.
When assessing the frequency of death is established that the introduction of the drug for 5 days and 1 day before the poisoning metafoam not affect the value of this index compared with the control group animals. Prophylactic use of the drug for 1 h before the injection of metaphase at a dose of 1 LD50completely prevented the death of animals. When you increase the dose of toxicant to 1.25 LD50registered a reduction in the frequency of death in the early period after exposure (up to 1 day), however further significant differences in this indicator from the control group were noted. With the introduction of metaphase in the dose of 1.5 LD50the prophylactic use of β-estradiol for 1 h before toxicity had no effect on the frequency of death of the experimental animals.
The introduction of β-estradiol for 20 min to poisoning metafoam at a dose of 1 LD50contributed to the prevention of destruction of animals throughout the observation period (15 days), at a dose of 1.25 LD50the probability of death was 17±17%, in the dose of 1.5 LD50- 83,3+17% (the differences with the control group are not significant).
The introduction of the drug when the first signs of intoxication warned the death of animals after poisoning metafoam at a dose of 1 LD50but when you increase the dose of toxicant killed all the ex�erimentale animals. It should be noted that only by the use of β-estradiol for 1 h and 20 min before the application of toxicant death of animals occurred significantly later than individuals in the control group.
Similar data were obtained when assessing the effectiveness of the prophylactic use of β-estradiol on the model of acute poisoning by other organophosphate - Malathion (table 3).
It is established that the introduction of the drug for 20 minutes before application of the poison to animals at a dose of 1 LD50increased NO50development of the first signs of intoxication, convulsions, warned the convulsions 1-4 degrees at 83,3±17% of the individuals of the group (differences from control are significant at p<0,05), and completely prevented the development of seizures 5 degrees (p<0.05) and mortality (p<0,05). In rats, which Malathion was introduced in doses of 1.25 LD50or 1.5 LD50increased NO50development of the first signs of poisoning, ET50the development of seizures and the occurrence of death (all differences were significant when compared with the control group). It should be noted that the introduction of β-estradiol for 20 min to poisoning by Malathion at a dose of 1.25 LD50almost completely prevented the development of seizures 5 degrees and significantly (p<0,05) reduced the frequency of death. When assessing the frequency and dynamics of death of the animals shown, �the introduction of β-estradiol in a dose of 100 mg/kg 20 min before poisoning Malathion significantly influenced the rate of mortality, reducing it only in the groups of animals that received the poison in doses of 1 LD50and 1.25 LD50(all differences were significant, p<0,05, when compared with the control group).
Thus, prophylactic administration of β-estradiol in a dose of 100 mg/kg for 20 min and 1 hour before poisoning metafoam and Malathion in the dose range up to 1,0-1,5 LD50helped reduce the severity of intoxication and frequency of death.
The data indicate that prophylactic administration of β-estradiol to acute poisoning by organophosphates contributed to a significant reduction in the severity of intoxication, severity of seizures and probability of death of the experimental animals.
Method of prevention of acute poisoning with organophosphates, wherein the prophylactically for 20-60 min to acute poisoning used β-estradiol.
SUBSTANCE: invention relates to mixed cobalt (II) salts of ketocarboxylic and mercaptocarboxylic acids of general formula (I):
where R=Alk, R'=H, Alk, NH2, NHCOCH3, m=0-3, R"=H, Alk, COOH, n=0-3, where Alk=alkyl C1-C3, or to such compounds as a cobalt (II) salt of mercaptoacetic acid and pyruvic acid, a cobalt (II) salt of mercaptoacetic acid and α-ketoglutaric acid, a cobalt (II) salt of N-acetyl-L-cysteine and pyruvic acid, a cobalt (II) salt of α-ketoglutaric acid and L-cysteine, a cobalt (II) salt of pyruvic acid and 2-mercaptopropionic acid or hydrates or solvates thereof. A method of producing salts of general formula (I) is also disclosed.
EFFECT: invention enables to obtain mixed cobalt (II) salts of ketocarboxylic and mercaptocarboxylic acids, having cyanide antidote activity.
7 cl, 7 ex
SUBSTANCE: preparation shows an antitoxic activity, and can be used as an antidote for nitrite and nitrate poisoning. A complex compound of 5-hydroxy-6-methyluracil with ascorbic acid (5-hydroxy-6-methyluracil ascorbate) is described by formula: The preparation contains the complex compound in an amount of 0.3-0.4 wt %, and ascorbic acid - the rest. The method for producing the preparation consists in a reaction of 5-hydroxy-6-methyluracil and ascorbic acid taken in the relation of ascorbic acid: 5-hydroxy-6-methyluracil equal to 1:(0.0015-0.0022), in water as a solvent at a temperature of 20-40°C for 30-60 minutes. The complex compound is produced as shown by infra-red and NMR spectra. The antitoxic activity of 5-hydroxy-6-methyluracil on nitrite has been unknown before.
EFFECT: water removal from the reaction mixture under low pressure.
2 cl, 2 tbl, 1 ex
FIELD: veterinary medicine.
SUBSTANCE: invention is intended for treatment of acute poisoning of animals with neonicotinoid insecticides. The method comprises intravenous administration of diazepam, Ringer's solution and unitiol.
EFFECT: method improves effectively the survival of animals, reduces the concentration of neonicotinoid insecticides in the body.
3 tbl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmacology and medicine and concerns the use of dihydrobromide 9-(2-diethylaminoethyl)-2-(3,4-dioxyphenyl)imidazo[1,2-a]benzimidazole of formula as a biologically active compound possessing high antihypoxic, actoprotective, nootropic activities and having a positive effect on physical efficiency, and a based pharmaceutical composition.
EFFECT: preparing the compound possessing high antihypoxic, actoprotective, nootropic activities and having a positive effect on physical efficiency, and the based pharmaceutical composition.
2 cl, 8 tbl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to veterinary science. A detoxicant of polysilicic acid derivatives is specified in a group of reversed-phase sorbents.
EFFECT: using the detoxicant enables practically eliminating toxic effects accompanying animal's poisoning.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention concerns veterinary science. A polyfunctional enterosorbent contains schungite-containing minerals comprising silicon dioxide 15.0-70.0 wt %, with an average median particle size 15.0*10-6 m.
EFFECT: invention provides higher efficacy on a wide spectrum of toxic substances, including mycotoxines, nitrates, nitrites, heavy metal salts, and also as an antibacterial and antioxidant agent.
14 tbl, 14 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to zinc-containing antidote of lethal and severe poisonings with carbon monoxide. Claimed antidote represents intramolecular tricyclic complex of triethanolamine with zinc salts of inorganic or organic acids (2, 8, 9-trihydrozincatrane) with ratio of triethanolamine to zinc salts being 1:1. Invention also relates to method of protection against poisoning by carbon monoxide by peroral introduction into organism of zinc-containing antidote in 5 vol. % ethanol in dose range 20-60 mg/kg of body weight.
EFFECT: prevention of lethal poisoning with carbon monoxide, higher efficiency and reducing acute toxicity of zinc-containing antidote.
9 cl, 5 ex.
SUBSTANCE: invention refers to medicine, namely to toxicology, and can be used for treating rats with acute verapamil intoxications. That is ensured by administering sodium thiosulphate 15-20 mg per 100 g of rat's weights as a cardioprotector.
EFFECT: method provides improved central venous pressure value.
3 ex, 1 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to zinc-containing antidote of lethal and severe poisonings with ethanol. Claimed antidote represents intramolecular tricyclic complex of triethanolamine with zinc salts of inorganic or organic acids (2, 8, 9-trihydrozincatran), the ratio of triethanolamine to zinc salts being 1:1. Invention also relates to method of treating ethanol poisoning by introduction into organism of zinc-containing antidote in 5 vol.% ethanol in dose range 30-60 mg/kg of body weight.
EFFECT: prevention of lethal outcome in case of ethanol poisoning and reduction of acute toxicity of zinc-containing antidote.
9 cl, 5 ex
SUBSTANCE: Chinese magnolia is extracted with liquefied carbon dioxide. The obtained CO2 extract undergoes chromatographic separation on aluminium oxide and eluated with hexane. After eluation the obtained hexane fractions are frozen and recrystallised from the chloroform-hexane mixture in ratio of 1:10-3:10.
EFFECT: high output of product.
SUBSTANCE: invention relates to medicine, namely to gynaecology, and can be used for the treatment of urogenital disorders at the background of hypothyroidism in women in postmanopause. The method consists in the application of local hormonal therapy. Depending on a degree of expression of clinical symptoms in the determination of the Modified Menopausal Index (MMI) and the Vaginal Health Index (VHI) in case of a mild degree of severity an intake of the medication Estrocard is administered vaginally in a dose of 1 suppository per night for 3 weeks, then 1 suppository per week for a year. In case of a severe degree an intake of the medication Angelic is administered with an additional daily intake of the medication Estrocard in the form of vaginal suppositories for 3 weeks continuously. Then, 1 suppository per week is prescribed for 12 months with administration of a daily intake of 50 mg of L-thyroxine.
EFFECT: method ensures the elimination of clinical manifestations of a urogenital disorder, normalisation.
SUBSTANCE: invention relates to medicine. Described are transdermal oestrogen delivery systems which include a polymer matrix and oestrogen. Also described are methods of producing and using said systems.
EFFECT: transdermal oestrogen delivery systems have a smaller active surface area without detriment to daily dosage of oestrogen.
16 cl, 1 dwg, 1 ex
SUBSTANCE: invention refers to medicine, namely to gynaecology. The method involves the daily transcranial electrical stimulation and drug administration. The transcranial electrical stimulation is characterised by current intensity 1.0÷1.5 mA, 20 - 30 minutes for 10÷15 days. In addition, the patients intakes the phytocomposition 'Myrrasyl-1'. The phytocomposition is taken 15÷20 minutes before meals 2 tablets 2 times a day for 10÷15 days. Thereafter, the phytocomposition 'Myrrasyl-1' is administered daily for 20÷30 days, 1 tablet 2 times a day; the preparation 'Sagenit' is administered before meals 1 tablet a day.
EFFECT: method provides higher clinical effectiveness in the patients suffering the hepatobiliary system by reducing the current intensity during the transcranial electric stimulation.
2 ex, 2 cl
FIELD: medicine, pharmaceutics.
SUBSTANCE: what is presented is the use of oestriol for preparing a pharmaceutical composition for vaginal administration for preventing and/or treating urogenital atrophy due to estrogen deficiency in women, wherein said composition is administered so that the patient receives a dose of oestriol 0.3 mg/day or less with this administration being daily or once every two days, once every three days or once a week for at least 3 weeks and a related method for preventing and/or treating. It is shown that the administration of oestriol in a dose of 10 times less than the standard one; it eliminates the state of vaginal atrophy.
EFFECT: invention provides the therapeutic effectiveness similar to the responses to the modern methods of treating, but with greater safety leading to a better quality of life.
14 cl, 10 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: pharmaceutical composition contains as a first active agent, 6β, 7β; 15β, 16β-dimethylenene-oxo-17α-pregn-4-ene-21,17-carbolactone (drospirenone) in an amount according to a daily dose after the administration of the composition and making approximately 2 to approximately 4 mg, and as a second active agent, 17a-ethinylestradiol (ethinylestradiol) in an amount according to a daily dose and making approximately 0.01 mg to approximately 0.05 mg together with one or more pharmaceutically acceptable carriers or additives. The composition contains drospirenone applied on inert carrier particles. A method for preparing a pharmaceutical composition involves spraying of the drospirenone and ethinylestradiol solution on the inert carrier particles. The pharmaceutical preparation according to the invention contains a number of separately packed and individually taken daily dosage units of the described compositions in a single package used for oral administration for at least 21 days running with said daily dosage units containing the combination of drospirenone and ethinylestradiol. The composition may additionally contain 7 and less daily dosage units containing no active agent, or containing ethinylestradiol only.
EFFECT: invention provides higher oral bioavailability of drospirenone.
20 cl, 5 dwg, 5 ex
SUBSTANCE: invention refers to medicine, namely obstetrics and gynaecology, and may be used for treating benign hyperplastic processes of the female reproductive system. That is ensured by the introduction of gonadotropin-releasing hormone agonist for 6 months once monthly in a combination with the oral administration of the preparation for hormonal replacement therapy. It is preceded by specifying the initial metabolic, vegetative and gynaecologic status of the patient which along with an age group provides a basis to assess an adequacy of initiating hormonal add-back therapy. If the patient belongs to the age group of under 40 years of age, and in case of observing additional burdening of the metabolic and vegetative status, the introduction of gonadotropin-releasing hormone agonist with no hormonal add-back therapy prescribed. For the purpose of preventing potential negative symptoms, it is combined with underlying prescription of a complex of phytoestrogens and vitamins with required intake of calcium and vitamin D3. Each injection of gonadotropin-releasing hormone agonist, starting with the second one, is followed by clinical assessment of hypestrogenism symptoms and blood chemistry analysis, and if observing hypestrogenism symptoms, additional hormonal add-back therapy is prescribed. If the patient appears to belong to the age of 40 years old and more, and in case of observing the presence of burdened metabolic and vegetative status regardless of the age group, 2 years after the first injection of gonadotropin-releasing hormone agonist, hormonal add-back therapy is started. When selecting the preparation included in the hormonal add-back therapy regimen: there are differentiated: if the patient belongs to a younger group under 35 years of age, a therapeutic add-back preparation is presented by a combine oral contraceptive containing ethinyl estradiol 30 mg and dienogest 2 mg in each tablet. The oral contraceptive is prescribed 1 tablet a day in the continuous regimen which is recommended to be used after termination of the therapeutic course with gonadotropin-releasing hormone agonist if pregnancy prevention is required. If the patient belongs to the age group of 35 years and older, a therapeutic hormonal add-back preparation is presented by a preparation for hormonal replacement therapy containing micronised 17-p estradiol 1 mg and dydrogesterone 5 mg or a preparation containing drospirenone 2 mg instead of dydrogesterone in each tablet 1 tablet a day in the continuous regimen. An initial or underlying tendency to increase of blood pressure, a combined preparation for hormonal replacement therapy containing drospirenone is prescribed. The therapeutic course is followed by recommended administration of the preparation of hormonal replacement therapy if the patient belongs to the age group of 50 years and older in the continuous regimen.
EFFECT: method enables providing an evident therapeutic effect that is manifested in stable elimination of estrogenic deficiency symptoms accompanying gonadotropin-releasing hormone agonist therapy with preserved clinical effectiveness and improved patient's quality of life.
SUBSTANCE: invention relates to medicine, namely to dentistry, and can be used in orthopedic treatment of women in post-menopausal period in case of complete or partial defects of dentitions by means of removable plate dentures. For this purpose cream "Ovestin" is applied on surface of denture basis in thin uniform 0.5-1.0 mm thick layer. Treatment is carried out daily once during 10 days from the moment of application.
EFFECT: method also ensures reduction of bleeding, keratinisation, improvement of microcirculation in mucosa of denture bed and as a result acceleration of socially-psychological adaptation of said contingent of patients.
2 dwg, 1 ex
SUBSTANCE: invention relates to substituted extratriene derivatives of general formula (values of radicals are given in the claim), useful in therapy, especially for treating and/or preventing steroid hormone-dependent disorders which require inhibition of 17β-hydroxysteroid dehydrogenase (17-HSD) enzyme type 1, type 2 and/or type 3, as well as salts thereof, pharmaceutical preparations containing said compounds, as well as methods of producing said compounds.
EFFECT: improved method.
41 cl, 98 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: as a first active agent a pharmaceutical composition contains drospirenone in the amount equal to a daily dose when administering the composition and making 2 to 4 mg, and as a second active agent - ethinylestradiol in the amount equal to a daily dose and making 0.01 mg to 0.05 mg, together with one or more pharmaceutically acceptable carriers or additives. Drospirenone as a part of the pharmaceutical composition has a particle surface area more than 10000 cm2/g. Preferentially, drospirenone is fine-grained or sprayed from a drospirenone solution by inert carrier particles. The preparation contains a number of separately packed and individually taken daily dosage units in a single package used for oral administration for at least 21 days running with said daily dosage units containing a combination of drospirenone and ethinylestradiol. The preparation may additionally contain 7 and less daily dosage units containing no active agent, or containing ethinylestradiol only.
EFFECT: combination of drospirenone and ethinylestradiol provides reliable contraceptive activity ensured by the use of a maximum dose of drospirenone which causes no side effects, particularly, excess diuresis.
29 cl, 5 dwg
SUBSTANCE: invention refers to medicine, namely gynaecology, and is applicable for the purpose of prevention of hormone resistance in endometrial hyperplasia. That is ensured by prescribing a depot synthetic analogue of gonadotrophin releasing hormone by 1 injection on the 1st-2nd day of menstrual cycle once every 28 days. Nine injections in all. It is combined with an oestrogen-gestagen drug by 1 tablet a day starting with the 14th day after the second injection of the gonadotrophin releasing hormone analogue and up to the 28th day after the ninth injection.
EFFECT: method enables prevention of hormone resistance in endometrial hyperplasia.
FIELD: organic chemistry, steroids, pharmacy.
SUBSTANCE: invention describes unsaturated 14,15-cyclopropanoandrostanes of the general formula (I):
wherein R1 means hydrogen atom (H), hydroxy-group (OH); R2 means hydroxy-group (OH), hydrogen atom (H); R3 means hydrogen atom (H), (C1-C10)-alkyl at α- or β-position; R4 means halogen atom (F, Cl, Br) or pseudohalogen group (azide, rhodanide), hydroxy-group (OH), perfluoroalkyl; R5 means (C1-C4)-alkyl; if double bond is at 1,2-position then R4 can mean hydrogen atom (H). Also, invention relates to a method for preparing these compounds and pharmaceutical compositions containing these compounds. Compounds of the formula (I) are compounds eliciting gestagenic and/or androgenic effect.
EFFECT: improved preparing method, valuable medicinal properties of compounds.
11 cl, 1 tbl, 9 ex