Method of treating chronic infectious urethritis complicated by prostatitis

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely dermatovenerology and is applicable for treating chronic infectious urethritis complicated by prostatitis. That is ensured by taking azithromycin 1.0 g (sumamed) once a day in 1st-7th-14th days combined with the complex therapy. The complex therapy involves rectal suppositories Dalargex, 1 suppository daily at bedtime No.10, prostate massage, rectal laser therapy and daily application of fluoroquinolone - gemifloxacin (factive) 1 tab. (320 mg) a day for 14 days.

EFFECT: method enables prolonged remission of the disease, higher life quality of the patients, recovers the reproductive function due to improved eradication of the opportunistic flora in the prostate secretion contents.

4 ex

 

The invention relates to dermatology, namely to new methods of treatment of patients with chronic infectious urethritis, prostatitis complicated.

Academic researchers and practitioners know that today prostatitis is the most common urological disease in men younger than 50 years.

Special attention in our time should be given to infectious prostatitis, which occurs on the background of chronic urethritis, often caused C.trachomatis.

There is a method of use in the treatment of prostatilen (Nicomedia) - polypeptide, obtained by extraction of the prostate gland in cattle [1]. In the experiment, and has been clinically proven that the medication has immunomodulatory effects, anti-inflammatory effect and effect on hemostasis. The purpose of prostatilen intramuscularly 1 time per day in a dose of 10 mg diluted in 1 ml of 0.5% solution of novocaine, No. 10 has resulted in 1-3 months full recovery in 36.6% of patients [2].

The use of this technique requires daily visits to the hospital and long-term treatment.

In 2002 in the Russian market registered a new drug cytomegalovirus series - vitaprost [3]. Its advantage over prostatilen dosage form is in the form of rectal CBE is her. In the instructions to vitaprost recommendations of his appointment on 1 suppository per day for 20-30 days. The efficiency for the purpose of preparation and the influence of vitaprost not only on the condition of the prostate gland, but also to improve sexual function (71,4% of patients) [4].

However, the use of vitaprost requires a long course of therapy (20-30 days).

The closest in technical essence is a chronic infectious uretroprostatit a fluoroquinolone with ooxacin [5].

The drug has a broad spectrum of antimicrobial activity, high bactericidal activity and good pharmacokinetic (penetrates into the tissue of the prostate). Ofloxacin (Floxin-200) 200 mg 2 times a day for 4-6 weeks [6].

However, studies revealed a lack of effectiveness of ofloxacin in the treatment of chronic urethritis caused by chlamydia or associated with conditionally pathogenic flora infection, acute prostatitis [7], as confirmed by the reports of the weak activity of the drug against anaerobic bacteria and the emergence of drug resistance microbial flora found in patients uretroprostatitis to ofloxacin [8, 9]. In addition, it has a high photosensitivity.

The goal is to create the most effective treatment for patients who ironicheskim infectious uretroprostatitis, acting on etiological, pathogenetic factors, the decrease in the number of complications.

The task is carried out by use of fluoroquinolone - gemifloxacin (factive) 1 tab. (320 mg) per day for 14 days in combination with azithromycin (Sumamed) in 1.0 g once a day 1-7-14 days, rectal suppositories alergex 1 candle at night daily No. 10, prostate massage and No. 7 in a day, daily for 5 minutes rectal therapy No. 10.

The method is as follows.

The patient after diagnosis of chronic infectious urethritis, prostatitis complicated, prescribed fluoroquinolone - gemifloxacin (factive) 1 tab. (320 mg) a day for 14 days in combination with azithromycin (Sumamed) in 1.0 g once a day 1-7-14 days, as well as combined therapy, including: the appointment of Nicomedia - new rectal suppositories alergex 1 candle at night daily No. 10, prostate massage through day 7, rectal laser therapy (device Pattern) with a wavelength of 0.89 mm, generating low-intensity laser pulse radiation in the near infrared region of the spectrum daily No. 10 the duration of the procedure within 5 minutes

Gemifloxacin (factive) - a new antimicrobial drug of fluoroquinolone, appeared on the Russian market. It has a wide range of bacteria is icenova actions. Unlike other fluoroquinolones has a dual action: inhibits replication of microbial DNA by binding with topoisomerase IV and DNA Girasol, which does not allow microorganisms to form a resistance to it. Gemifloxacin (factive) is rapidly absorbed in the gastrointestinal tract, it penetrates into the tissue of the prostate, has a lower toxicity in comparison with other fluoroquinolones and assigned to 1 table. per day (ofloxacin in table 2. in the day).

Azithromycin (Sumamed) is the first representative of a new group of macrolide antibiotic of azalides. Its exceptional pharmacokinetic properties became the basis of a simple dosing schedules and a short course of treatment. Azithromycin penetrates the prostate gland, in addition has a wide antimicrobial spectrum and immunomodulatory properties [10, 11, 12]. In this connection the author has established the feasibility of the combination of this drug with a new fluoroquinolone.

Alergex individual synthetic peptide that deprives its allergenic properties characteristic of polypeptides secreted from the prostate gland of cattle, normalizes microcirculation and platelet-vascular hemostasis, reduces swelling and stagnation of the secretions in the sinuses by improving blood circulation and secretory functions of the epithelial cells in the inflamed lesion is I of the prostate, this reduces the volume of blood in the prostate secretion, regulate spermatogenesis, has a modulating effect on the state of T - and b-systems of immunity and nonspecific resistance of the organism, stimulates reparative processes. It contains dimexide has a pronounced anti-inflammatory and analgesic effect.

During task execution, the inventive method has enabled to increase the efficiency of treatment as in the near and long-term.

The object of the study were 104 patients with chronic infectious uretroprostatitis, randomized in the main group (OG) - 53 men and the comparison group (GS) - 51 man. In both groups prevailed contingent workers from 31 to 50 years, most patients were married. Duration of disease prostatitis often accounted for terms from 3 to 5 years (OG - 83,1%, HS - 84.4 per cent). Only 7.6% of men in the EXHAUST gas and 13.8% in HS remission lasted from 1 to 1.5 years. Most patients complained of short erections and decreased libido.

Patients were held ultrasound of the prostate (ultrasound), reconfirmed the diagnosis and specified the nature of the changes in her. When the etiologic evaluation of patients used the polymerase chain reaction (PCR), Real Time PCR. Spent culture for the distribution Tr.vaginalis and N.gonorrhoeae. Allocated anaerobic flora in the content of the prostate gland. Investigated the ejaculate. Enzyme-linked immunosorbent assay (ELISA) to determine the level of testosterone, follicle-stimulating hormone, prolactin.

Before treatment, 84.8% of the patients in the experimental and 81,3% in HS were serous discharge from the urethra, often abundant nature. Anterior urethritis was installed in the EXHAUST gas - to 52.9%in HS - 56,9%.

Almost half of the patients was found .trachomatis as monoinfection. In 20.8% of patients in the EXHAUST gas and to 21.6% in HS was a combination of C. trachomatis, U. urealyticum. The most frequent opportunistic flora were installed Peptostreptococcus and E. coli. In both groups prevailed patients with a significant increase in the number of cells in the discharge of the mucous membrane of the urethra.

When assessing symptoms of chronic uretroprostatit (on a scale NIH-CPSI) found that severe symptoms (30 to 43 points) was more than half of the patients in the experimental (52,8%)and HS (51,1%).

Only half of the patients were normal concentration of sperm. Almost 60% of patients in both groups was reduced volume of ejaculate, normal sperm motility observed in the EXHAUST gas only 8.3%in HS - 9.1 per cent; normal viscosity in 33.3% and 27.3%, respectively, alkaline pH - 54,2% and 45.4% of men. The normal level of testosterone was only 47.2% of men OG and 49% - TOS; FSH in 64.2% and 62.7 percent, respectively, prolactin - 66,1% and 64.7%.

Bol is by the EXHAUST gas was treated by the proposed method. Patients TOS instead of gemifloxacin (factive) received from the first day of treatment ofloxacin (Floxin-200) 200 mg 2 times a day for 14 days. In the rest of therapy was similar to the EXHAUST gas.

A comparative study demonstrated the effectiveness of the proposed method for the treatment of patients with infectious uretroprostatit both in the near and long-term.

One month after treatment, the eradication of C. trachomatis occurred in all patients in the EXHAUST gas, and GS.

When comparing the dynamics of the parameters between patients DG and GS was found that in the EXHAUST gas was statistically significant decrease in the number of conditionally pathogenic flora on four microorganisms, GS - only two. According to the results of urethroscopy patients OG 11.9% more likely to have occurred normalization of the mucosa of the urethra in its entirety (p<0,05).

When examining the content of the prostate gland in men, the EXHAUST gas does not have a single patient with a significant increase in the number of cells. Patients TOS was 6 (11.8 percent) of the 51 patients (p<0,05).

Objective indicator of the effectiveness of treatment of chronic infectious uretroprostatit was data ultrasound of the prostate gland. One month after the end of treatment in men OG improving the echostructure of the prostate occurred in 44 (83%) of the 53 patients in the HS - 33 (64,7%) of the 51 men that n is 18,3% less than in CG (p<0,05).

Reliable was the difference in favor of the EXHAUST gas positive changes to the overall assessment of symptoms of chronic uretroprostatit scale (NIH-CPSI)in the EXHAUST gas, the number of patients with low symptoms of chronic infectious uretroprostatit 31 of 53 (58,5%), HS 20, 51(39.2 per cent) (p<0,05).

Dynamics of previously impaired sexual function, indicators of the level of sex hormones in serum and semen was positive in both groups, but the number of patients with increased viscosity was reduced in the EXHAUST gas and 12.5% of the people; in the GS - 33,3% (p<0,01). The number of persons with a normal volume of ejaculate was in the EXHAUST gas 75%, HS - 68,2% (p<0,05).

Comparative analysis of the immediate outcomes of therapy developed by the scheme showed a more pronounced treatment efficiency in the EXHAUST gas compared to the GS.

All patients (CG - 53, GS - 51) were re-surveyed six months after the end of treatment.

Men of the EXHAUST gas when examined by PCR for STIs scraping with mucous urethral C. trachomatis and M. genitalium were not discovered. One patient found M. hominis (2.0%) and one (2,0%) - U. urealyticum. Among patients TOS C. trachomatis installed in 6 (11,2%) men, M. hominis - 1 (2,1%). One man TOS C. trachomatis were in Association with U. urealyticum.

The difference in the frequency of detection of C. trachomatis between men DG and GS statistically significant (p<0,05).

In the EXHAUST gas, the number of the patient is in low symptoms of chronic infectious uretroprostatit (0-14) on a scale NIH-CPSI was more of 22.8% (67,9% and 45.1%, p<0,01).

Patients OG normal number of leukocytes in the content of the prostate was often 22.2%, than men HS (p<0,05); normal echoes prostate - 26.0% (p<0,01).

Twelve months after the end of treatment were able to evaluate the results in the EXHAUST gas 48 men, GS - 46. Patients in both groups did not complain of anything, which could give rise to additional examination. In this regard, based on the effectiveness of therapy total score of symptoms of chronic prostatitis scale (NIH-CPSI). It turned out that in the EXHAUST gas, the number of patients with low symptoms increased by four and amounted to 40 (83.3%) of 48 patients in the GS - one and amounted to 24 (52.2 per cent) of the 46 men. Therefore, in the EXHAUST gas was 31.1% more patients than in HS, with a high rate of effectiveness of therapy (p<0,01), i.e. long-term in the EXHAUST gas was the increase in the number of persons with low symptoms of chronic prostatitis.

Thus, when applying the method by 11.9% more normal state of the mucosa of the urethra; 18.0% - number the number of cells from the surface, 19.3% more likely to occur among men with low symptoms of chronic uretroprostatit and restoration of sexual function (p<0,05). Receiving gemifloxacin (factive) complainte (1 time daily), ofloxacin (Floxin-200) of destinations is carried out 2 times a day.

In the long term after the end of therapy in the EXHAUST gas in comparison with GS 6 months number of patients with low symptoms of chronic uretroprostatit was more of 22.2% (p<0,05); 12 months - 40.4% (p<0,01).

This confirmed the validity of the selection scheme: combination of gemifloxacin (factive) and azithromycin (Sumamed) in combination with candles alergex, massage of the prostate and rectal laser therapy to improve the efficiency of treatment of patients with chronic infectious urethritis, prostatitis complicated.

Examples of specific performance.

Example 1 (DG). Patient A., age 28, single.

Diagnosis: Lung prostate on the background of chronic chlamydial urethritis (solid infiltration of the anterior urethra, colliculi).

Treatment: azithromycin (Sumamed) schema 1.0 g per day in 1-7-14 days, parallel to gemifloxacin (factive) 1 tab. (320 mg) per day for 14 days + complex therapy candles alergex 1 per night No. 10, prostate massage through day 7, rectal laser therapy (device Pattern) for 5 minutes daily No. 10.

Before the treatment: of iron in the form of an oval, lateral lobe asymmetrical, contours equal, echo is increased, the density is non-uniform size 45×27×33 mm in the peripheral zone of the multiple linear foci of fibrosis.

1.5 months after treatment: the pin is ture prostate smooth, echostructure homogeneous, dimensions 31×25×26 mm

12 months after treatment: a form of prostate oval, clear contours, echo and the density - regular, size 33×23×24 mm, diffuse homogeneous.

Example 2 (DG). Patient I., 42 years old, married.

Diagnosis: Lung prostate on the background of chronic chlamydial urethritis (total urethritis, mild infiltration).

Treatment: azithromycin (Sumamed) schema 1.0 g per day in 1-7-14 days, parallel to gemifloxacin (factive) 1 tab. (320 mg) per day for 14 days + complex therapy candles alergex 1 per night No. 10, prostate massage through day 7, rectal laser therapy (device Pattern) for 5 minutes daily No. 10.

Before the treatment: of iron in the form of an oval, lateral lobe asymmetrical, contours equal, echo is increased, the size of the prostate 41×26×35 mm, diffuse induration of the internal structure, a honeycomb pattern.

1.5 months after treatment: the contours of the prostate smooth, there is a significant decrease in echogenicity of the tissue, the increase in hydrophilicity of the cancer, the size of the prostate 34×25×27 mm, recovered the symmetry of the lateral lobes.

12 months after treatment: a form of prostate oval, clear contours, echo and the density of normal prostate size 34×23×24 mm, diffuse homogeneous. PTS is GI hydrophilicity was resolved.

Example 3 (OG). Patient I., aged 39, married.

Diagnosis: Lung prostate on the background of chronic chlamydial urethritis (total urethritis, mild infiltration).

Treatment: azithromycin (Sumamed) schema 1.0 g per day in 1-7-14 days, parallel to gemifloxacin (factive) 1 tab. (320 mg) per day for 14 days + complex therapy candles alergex 1 per night No. 10, prostate massage through day 7, rectal laser therapy (device Pattern) for 5 minutes daily No. 10.

Before treatment: a form of cancer rounded in the upper part of the gland focal hydrophilicity on the background of diffuse seals, more pronounced in the lower part of the gland. Viewed porous nature of the structure, sometimes with a rounded contour with hyperechogenicity. The size of the prostate 40×22×33 mm

1.5 months after treatment: the contours of the prostate smooth, echo tissue decreased. The size of the prostate 36×22×27 mm

12 months after treatment: a form of prostate oval, clear contours, echo and the density - regular, size 33×22×22 mm, diffuse homogeneous. Foci hydrophilicity was resolved.

Thus, the results of ultrasound examination of the prostate in patients OG confirm the clinical and laboratory data of the effectiveness of treatment of patients with infectious uretroprostatit on the elaborately the th method.

Other were the results of ultrasound examination of the prostate in HS.

Example 4 (HS). Patient K., aged 27, single.

Diagnosis: Lung prostate on the background of chronic chlamydial urethritis (transient infiltration of the anterior urethra, colliculi).

Treatment: azithromycin (Sumamed) schema 1.0 g per day in 1-7-14 days, in parallel ofloxacin (Floxin-200) 1 tab. (200 mg) 2 times daily for 14 days + complex therapy candles alergex 1 per night No. 10, prostate massage through day 7, rectal laser therapy (device Pattern) for 5 minutes daily No. 10.

Before treatment: the size of the prostate 44×27×34 mm, the boundaries are fuzzy, rough, diffuse heterogeneous echogenicity increased, there are multiple foci of fibrosis.

1.5 months after treatment: a form of prostate oval, echo is non-uniformly increased in the peripheral zone of the linear foci seal, size 38×29×25 mm

12 months after treatment: a form of prostate oval, fuzzy contours, increased echogenicity, size 40×24×22 mm, in the Central part there is a linear hearth seal.

As follows from the above examples, an ultrasound of the prostate in the long-term shows that the effectiveness of treatment of chronic uretroprostatit was more pronounced in the line is the cation in the complex treatment of gemifloxacin (factive) instead of ofloxacin (Floxin-200).

The application of the proposed method can improve the eradication of conditionally pathogenic flora in the content of the prostate gland secretion in the range from 4 to 11 times, enables to prolong remission of the disease, improve the quality of life of patients, to restore reproductive function, which is not only medical but also social value.

Sources of information

1. Tkachuk V.M., Gorbachev A.G., Khavinson V.H. Application of prostatilen in the treatment of patients with chronic prostatitis // Urology and Nephrology, 1991. No. 6. - P.40-43.

2. Borisenko K.K., Hilinski M., Malyshev, A.M., A.I. Medvedev experience in the application of prostatilen in the treatment of chronic prostatitis // Vestnik St.Petersburg University. dermatol. and venerol., 1991. No. 8. P.47 - 50.

3. On The Main Page. Drugs in Russia // M Attraversare, 2009. - SB-433-434.

4. Tkachuk V.M., Lotzen-Medvedev A.K. Our experience in the application of vitaprost in patients with chronic prostatitis // Nephrology, 2005. - V.9. No. 4. - P.84-88.

5. Derevyanko I.I., Kotlyarova, GA, Sinykin V.N., Kondratiev E.M. Perspectives and experience in the use of ofloxacin in urology // Antibiot. and Himyar., 1996. No. 41 (9). - S.89-94.

6. Pushkar DU Treatment of chronic bacterial prostatitis // the Plenum of the Russian society of urologists: Materials. - M., 2004. - P.289-314.

7. Ushakov MS, V.V. Chebotarev the Effectiveness of treatment regimens for patients and the infectious uretroprostatitis in short-and long-term Scientific-practical journal "Medical Bulletin of the North Caucasus". - Stavropol, 2010. - №1(17). - P.60-63.

8. Ridgway G. Management of genital chlamydial infections: problems and controversies // Clinical Microbiology, University College London Hospital, London WCJEGAU, England Proc 3rdMeet Eur Soc Chlam Res, 11-14 Sept, 1996, Vienna, Austria, 1996: 445-446.

9. Padalka E.N., Yakovlev V.P. of Antimicrobial drugs of fluoroquinolones in clinical practice. M: Lagata, 1998. - S-187.

10. Mosquitoes W., Derevianko I.I., Yakovlev and other Pharmokinetic azithromycin with urogenital infections // Infection and antimicrobial therapy, 2001. No. 3(6). - S-178.

11. A method for the treatment of chronic chlamydial urethritis, prostatitis complicated (Patent for invention dated 29.12.2000, No. 2189815. V.V. Chebotarev, N. Chebotareva, Lukyanenko AV).

12. Sukhanov SV, Mazo E.B. Possible use of azithromycin in treatment of patients with urogenital chlamydial prostatitis // Russ. The honey. journal, 2002. No. 10. - P.26.

A method for the treatment of chronic infectious urethritis, prostatitis complicated, consisting of the use of 1.0 g of azithromycin (Sumamed) once a day 1-7-14 days in combination with a fluoroquinolone, comprehensive therapy, including rectal candles, massage prostate, rectal laser therapy, characterized by daily use of fluoroquinolone - gemifloxacin (factive) 1 tab. (320 mg) per day for 14 days and Nicomedia - rectal suppositories alergex 1 candle every night on No. 10.



 

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1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to substituted heteroarylpiperidine derivatives of formula (I) and enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof, where R1 denotes -N(R10)-(C(R6)2)m-T, (C(R6)2)1-T or -O-(C(R6)2)m-T; R6 is independently selected from H, OCH3, C1-6-alkyl, possibly substituted with 1-3 substitutes which are halogen, and C3-6-cycloalkyl, possibly substituted with 1-3 substitutes which are halogen, T denotes NR7R8, , , , or ; R7 and R8 are independently selected from H, C1-6-alkyl; R9 is independently selected from OH, C1-6-alkyl, O-C1-6-alkyl, or NR12R13; R10 denotes H or C1-6-alkyl; R12 and R13 are independently selected from C1-6-alkyl, possibly substituted with OH, C2-6-alkylene-O-C1-6-alkyl and W denotes CH, O or NR10; B denotes CR2 or N; G denotes CR2 or N; D denotes CR2 or N; E denotes CR2 or N; provided that one or more of variables B, G, D and E must be N; R2 is independently selected from H, F, Cl, CH3, OCH3 and CF3; R3 denotes: H, CI, F or CH3; R4 denotes Cl, F or CH3, R5 denotes , morpholine, possibly substituted with 1-3 identical or different substitutes R14, a 4-7-member saturated or partially unsaturated heterocycle containing one nitrogen atom in the ring and possibly an additional heteroatom selected from O, N and S, where the heterocycle is possibly substituted with 1-4 identical or different substitutes R11, or NR12R13; R11 is indendently selected from halogen, OH, C1-6-alkyl, possibly substituted with 1-3 substitutes which are halogen, C2-6-alkynyl, -C0-6-alkyl-C3-6-cycloalkyl, -OC(O)C1-6-alkyl, -NH2, -NH(C1-6-alkyl) and -N(C1-6-alkyl)2; A denotes a 3-7-member saturated ring; R12 and R13 are independently selected from C1-6-alkyl, possibly substituted with OH, C2-6-alkylene-O-C1-6-alkyl; R14 denotes C1-6-alkyl; 1 equals 0, 1, 2, 3 or 4; m equals 0, 1, 2, 3 or 4; o equals 0, 1 or 2; p equals 0, 1, 2, 3 or 4; r equals 0, 1, 2, 3 or 4; s equals 1 or 2 and t equals 0 or 1. The invention also relates to use the compound of formula I to produce a drug for treating or preventing disorders, diseases or conditions responsible for inactivation or activation of the melanocortin-4 receptor in mammals, and to a pharmaceutical composition based on said compounds.

EFFECT: novel compounds which can be used as melanocortin-4 receptor modulators are obtained and described.

10 cl, 134 ex, 16 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely gynaecology, and is applicable for treating patients with refractory pregnancy loss in the first trimester. That is ensured by prescribing a water solution of the preparation Immunal 1 dosimetric pipette twice a day, tablets of nicotinic acid 50 mg twice a day, rectal enemas with 30% sodium thiosulphate 5.0 ml and 0.25% Novocain 15.0 ml once a day, and Rekicene-RD one dessertspoon twice a day. The therapeutic course makes 30 days.

EFFECT: method provides higher clinical effectiveness and prevented complications due to complex immunomodulatory, anti-inflammatory, disintoxication effect improving blood circulation.

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to azaadamantane derivatives of formula (I), to their pharmaceutically acceptable salts possessing the properties of nAChR ligands, their application, a method of treating and based pharmaceutical compositions, and also to intermediate compounds of formula (VI) and (VII) and to application of the compound of formula (V) for preparing the compound (I). In general formulas

L1 represents -O- or -NRa-; A represents -Ar1 or -Ar2-L2- Ar3; Ar1 represents 5-9-member heteroaryl wherein said heteroaryl is optionally substituted by alkoxy, alkoxycarbonyl, alkyl, alkylcarbonyl, carboxy, carboxyalkyl, cyano, halogenalkoxy, halogenalkyl, halogen, hydroxy, nitro, -NH2, (NH2)carbonyl and oxido; Ar2 represents 5-6-member heteroaryl wherein said heteroaryl is optionally substituted by alkoxy, alkoxycarbonyl, alkyl, alkylcarbonyl, carboxy, carboxy alkyl, cyano, halogenalkoxy, halogenalkyl, halogen, hydroxy, nitro, -NH2 and (NH2) carbonyl; Ar3 represents aryl, optionally substituted alkoxy, alkoxyhalogenalkyl, alkyl, aryl, halogenalkoxy, halogen, hydroxy and -NH2; or Ar3 5-9-member heteroaryl wherein said heteroaryl is optionally substituted by alkoxy, alkoxycarbonyl, alkyl, alkylcarbonyl, aryl, carboxy, carboxyalkyl, halogenalkyl, heterocyclyl and tritylaryl; L2 represents a bond, -O- or -C(O)NRa-; and Ra represents hydrogen.

EFFECT: preparing the pharmaceutically acceptable salts possessing the properties of nAChR ligands.

41 cl, 11 dwg, 162 ex

Gsk-3 inhibitors // 2449998

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns applying urea derivatives or their pharmaceutically acceptable salts characterised by formula , wherein RB is specified in: while R3, R4, R'2, R'3, R'4, R'5, and R'6 represent hydrogen as GSK-3 inhibitors, pharmaceutical compositions containing them, and using them for treating and/or preventing disorders the development of which involves GSK-3.

EFFECT: preparing the pharmaceutical compositions containing them, and using them for treating and/or preventing disorders the development of which involves GSK-3.

14 cl, 2 ex, 1 tbl, 4 dwg

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

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

FIELD: medicine.

SUBSTANCE: modeling of ADMA-like model of gestosis in laboratory pregnant rats of Wistar line is carried out by daily introduction of inhibitor of NO-synthase L-NAME in dose 25 mg/kg from 14 to 20 day of pregnancy. Correction of endothelial dysfunction is performed by L-norvalin, which at the background of modeling is introduced intragastrically daily for 7 days in dose 10 mg/kg once per day.

EFFECT: method leads to expressed dysfunction correction under conditions of specific mechanisms of pathological process course in pregnant women.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel acid-additive salts of pyrrolopyrimidinone derivative, represented by formula (1) which is selected from gentisate, maleate, citrate, fumarate and semitartrate salts, which possess improved properties in their application, in particular higher stability.

EFFECT: invention also relates to method of obtaining acid-additive salts of pyrrolopyrimidinone derivative, represented by formula (1) and to pharmaceutical composition, containing them, for treatment and prevention of erectile dysfunction, pulmonary arterial hypertension, chronic obstructive lung disease, benign prostate gland hypertrophy and diseases of lower urinary tract.

11 cl, 30 ex, 7 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely urology, is applicable for treating chronic cystitis. That is ensured by drug instillations into a bladder. In addition, the instillation is preceded by endovesical mucosal exposure to laser light of wave length 0.62 mcm. The instillation is followed by pubic exposure to laser light of wave length 0.86 mcm within a projection of the bladder. The duration of each procedure is 7 minutes; the therapeutic course is 10-12 procedures.

EFFECT: method provides higher clinical effectiveness ensured by pain pulse interruption and improved microcirculation and consequently prolonged drug staying in the bladder cavity as a result of the exposure to laser light before the instillation, and also by deeper drug penetration in bladder tissue as a result the epicutaneous exposure to laser light after the instillation.

1 dwg, 2 tbl, 2 ex

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