Search

The authors present results obtained in a complex study of 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-on (ABMP). ABMP was shown to differ from existing analogues by high gestagen activity and prolonged action. The substance does not possess androgenic or mineralocorticoid activity, is not toxic when used in high doses, and possesses significant cytostatic and chemiosensitizing activity. These properties of ABMP demonstrate that the substance should be studied in clinical setting as a gestagen with anticancer and chemiosensitizing activity for further application to therapy of hyperplastic processes in the female genital system and tumors that are sensitive to female sex hormones.

The influence of ionic and non-ionic contrast media on the ex vivo hemostasis in rabbits was studied for ionic urografin (76 %), non-ionic ultravist-300, and non-ionic omnipaque-300 intravenously injected in medium and high doses (1.5 ml/kg and 3.0 ml/kg, respectively). Ionic urografin (1.5 ml/kg) almost did not influence the level of hemostasis ex vivo. Non-ionic contrast media (ultravist and omnipaque) in the medium diagnostic dose (1.5 ml/kg) activated the hemostasis, the effect being much more pronounced in the case of omnipaque. Dose-dependent action was observed for both ionic and non-ionic contrast media.

Antitumor activity of a new highly active promising gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one (butagest) was studied in mice with model cervical carcinoma (RShM-5). The reference drug was medroxyprogesteron acetate (MPA, Depo Provera) used in clinics. The new preparation introduced perorally in a dose of 1 mg per mice inhibited the model tumor growth by 73%, which was 18% (p < 0.01) more effective than the action of the reference drug MPA. The effect of the new gestagen was also studied in vitro with respect to human breast carcinoma of the MCF-7 line and human cervical carcinoma HeLa. The viability of the tumor cells was studied during a 6-day incubation with the drug at a concentration of 10(-7)-10(-5) M (MTT test). The reference compounds were progesterone and MPA. These drugs suppressed the growth of both MCF-7 and, in higher concentrations, of HeLa. Butagest inhibited the growth of HeLa in all concentrations. Thus, the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one is capable of suppressing the viability of human breast carcinoma and human cervical carcinoma, being comparable or even more effective than the reference drugs.

The results of prophylactic endoscopic treatment of 22 patients with extrahepatic portal hypertension (main group--EPH) and 76 patients with cirrhosis of the liver (a comparison group--CL) who had had variceal bleedings were analyzed. In the EPH group permanent eradication was obtained in 14 patients (63.6%), in the CL group--in 46 patients (50.5%). With the average duration of achieving the eradication the number of sessions before achieving it proved to be greater than that for CL. Recurrent bleeding during the first month of observations was noted in 7 out of 22 patients. In most cases the sources of bleedings were postligational and postinjectional ulcers of the cardial part of the stomach. Long-term results (1-5 years) were followed-up in 14 patients. In 9 patients there was no recurrent bleeding during 2-5 years of observation. Thus, it is expedient to use endoscopic interventions as the methods of the "first line" in the complex program of secondary prophylactics of variceal bleedings in extrahepatic portal hypertension.

The combined cytostatic effect of doxorubicin and gestagens progesterone, medroxyprogesterone acetate, mecigestone, and butagest on doxorubicin-resistant and doxorubicin-sensitive human breast cancer MCF-7 cells was studied by the MTT assay. On the 6th day of incubation progesterone, medroxyprogesterone acetate, mecigestone, and butagest in high concentrations (10(-5) M) potentiated the cytostatic action of doxorubicin in sensitive and resistant cells by 30-50%. Potentiation of the cytostatic effect produced by doxorubicin in sensitive cells is related to intrinsic cytotoxic activity of gestagens. In resistant cells these changes are associated with potentiation of the effect of doxorubicin.

The paper analyses current data of monomer and dimmer iodine-containing radiocontrast agents used for diagnosis of cardiovascular diseases and radiovascular interventions. Considering the risk factors of nephropathy as the most common and threatening complication of radiocontrast agents the authors conclude that non-ionic monomers are the most advisable as they demonstrate optimal balance of viscosity, water solubility, osmolality and diagnostic effectiveness.

Cervical myometrium was examined in 22 pregnant women at 39-41 weeks gestation at risk of labor abnormalities. The patients received mifegin for preparing to labor. A new component in the mechanism of mifegin effect on the uterine cervix in full-term pregnancy was revealed: mifegin elevated the content of cAMP by 50% and almost 2-fold increased the cAMP/cGMP ratio compared to the initial level.

The investigation involved 22 reproductive and menopausal women (aged 30-48) with atypical endometrial hyperplasia. In addition to general clinical examination, all the patients underwent ultrasound scanning of the organs of the small pelvis, hysteroscopy and diagnostic curettage for morphological examination both before and after treatment. All tissue samples taken before and after treatment were assayed for cytoplasmic and plasma-membrane receptor levels and a number of biochemical parameters of plasma membranes. Hormone therapy with prolonged-release gestagen-based drugs pointed to changes which occurred in: (1) sex steroid reception at cytosol and plasma-membrane levels; (2) the lipids profile of plasma membranes, and (3) activity of membrane-related enzymes. Among the beneficial results of gestagen treatment was coming most of lipid profile parameters and plasma-membrane enzymes back to normal. However, a decrease in the progesterone reception level in target tissue after 3-6 month treatment may suggest a likelihood of development of tolerance to gestagen. The data also suggest that further research continue in this area of endometrial precancer.

An analysis of observations of 250 patients with different rheumatological diseases has shown that 18% of the patients had ulcer disease with complications. The greatest risk of bleedings and perforations took place during the first year of treatment with nonsteroidal antiinflammatory drugs. The main risk factors of complications were determined. They are: male sex, high parameters of gastric secretion.

A drug composition LINCOGAP is assessed, consisting of lincomycin hydrochloride (33%), ultrahighly dispersed hydroxyapatite (HA) (33%), gelatin (7%), and water (27%). Distribution of tritium-labeled lincomycin in organs and tissues of experimental animals was studied by the radiometric method after implantation of the composition into a standard rat mandibular defect. Lincomycin concentration surpassing by orders of magnitude the minimal inhibitory concentration for the main lincomycin-sensitive microorganisms persisted at the site of implantation of the composition for at least 7 days, while the concentration in internal organs and tissues was the minimum. Microbiological findings indicate active diffusion of lincomycin from the site of injection into the adjacent bone. Thus, LINCOGAP exerts an antibacterial effect in the pathological focus while its general toxic effect is low and, therefore, side effects are minimized. Combination of the antibiotic with ultrahighly dispersed HA helps regulate the process of bone repair, stimulating the proliferative and functional activity of osteoblasts. Hence, combined drug LINCOGAP is a promising agent for the treatment of inflammatory destructive diseases of osseous tissue.

Information is presented on the classification of serotonin receptors which is based on the results of pharmacological and radioligand analysis. The genetic and biochemical characteristics of the types and subtypes of serotonin receptors are discussed. The role of serotonin receptors of the central and peripheral nervous system and the role of some effector cells and organs in the regulation of their functional activity is described.

In concentrations of > or = 10(-5) mol/liter nistranol (11 beta-nitroxy-9 alpha-hydroxy-ethynylestradiol-diacetate) demonstrated cardiac and vascular activity in vitro. It caused concentration-dependent and reversible increase of the contractile parameters of an isolated atrial appendage of rats. A three-phase effect of nistranol on a isolated rat thoracic aorta was encountered: vasodilatation-vasoconstriction-vasodilatation. Anti-ischemic and antinecrotic effects of nistranol were noted in experimental myocardial infarction.