Anaesthetic composition

FIELD: chemistry.

SUBSTANCE: invention relates to medicine and represents anaesthetic composition, which contains neuroactive steroidal anaesthetic, composed with cyclodextrin, where neuroactive steroidal anaesthetic is selected from the group, consisting of alphadolone, alphaxalone and pregnanolone. Cyclodextrin represents (7) sulphobutyl ether of beta-cyclodextrin. Molar ratio of steroidal anaesthetic to cyclodextrin is within the interval from 1:1.6 to 1:2.5, except alphadolone, where it constitutes from 1:2 to 1:2.5. Invention also relates to methods for induction of anaesthesia and sedative effect by means of composition.

EFFECT: low toxicity and reduced content of sulphoalkyl ether of beta-cyclodextrin.

7 cl, 11 ex, 7 tbl, 12 dwg

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, in particular to phytomixture with sedative effect. Phytomixture contains mixture of Leonurus cardiaca herb, hop cones, Origanum vulgare herb, and hawthorn fruit, taken in specified quantity.

EFFECT: claimed phytomixture possesses increased sedative effect, improved organoleptic properties, as well as reduced side effects.

3 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical composition for treating insomnia. Said composition includes root of Polygonum multiflorum and/or its extracts, seeds of Ziziphus spinosa and/or its extracts, mulberry fruit and/or its extracts, Ganoderma and/or its extracts, lily bulb and/or its extracts, Anemarrhena rhizome and/or its extracts, root of Salvia miltiorrhiza and/or its extracts, chrysanthemum flower and/or its extracts, Poria and/or its extracts and Albizia flower and/or its extracts. Invention also relates to application of said composition.

EFFECT: claimed invention provides sedative and soporific effect, contributes to memory stimulation.

17 cl, 6 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts, wherein A is thiazolyl, oxazolyl, thienyl, furyl, imidazolyl, pyrazolyl or oxadiazolyl (structures of which are presented in cl.1 of the patent claim), R1 represents C1-6alkyl; R2 represents (i) phenyl substituted by halogen; C1-6alkyl optionally substituted by morpholine or C1-6dialkylamino; C1-6alkoxy optionally substituted by halogen; or heterocyclyl, wherein a heterocyclyl substitute is specified in morpholine; pyrazolyl optionally substituted by C1-6alkyl; piperidinyl; pyrrolidinyl; oxadiazolyl substituted by C1-6alkyl; furyl substituted by C1-6alkyl; dioxydoisothiazolidinyl; triazolyl; tetrazolyl substituted by C1-6alkyl, tridiazolyl substituted by C1-6alkyl; thiazolyl substituted by C1-6alkyl; pyridyl; or pyrazinyl; (ii) substituted or unsubstituted heterocyclyl specified in quinolinyl; pyridyl substituted by C1-6alkoxy or morpholinyl; or benzo [d] [1, 2, 3] triazolyl substituted by C1-6alkyl; R3 represents phenyl substituted by 2 or 3 substitutes specified in halogen; C1-6alkyl; C1-6alkoxy optionally substituted by halogen; hydroxy group; cyano; or -C(=O)ORa, wherein Ra represents phenyl; R4 represents hydrogen, C1-6alkyl or C1-6halogenalkyl. The invention also refers to a pharmaceutical composition containing the compounds of formula (I), a method for PDE10 inhibition, a method of treating neurological disorders, and to intermediate compounds: 2-(4-chlor-3,5-dimethoxyphenyl)furan and 4-(5-methyl-1,3,4-thiadiazol-2-yl)benzaldehyde.

EFFECT: compounds of formula (I) as PDE10 inhibitors.

39 cl, 13 ex, 2 tbl, 77 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly to experimental pharmacology, and can be used as a method for rat sedation with an api-phytocomposition. The method for rat sedation with the api-phytocomposition involving single and daily one-week administration of a sedative agent, which is administered intragastrically through a probe in a dose of 200 mg/kg of animal's body weight, wherein the api-phytocomposition contains honey, bee-bread, lime pollen, propolis, valerian extract in a ratio of 10:2:1:1:1, and represents an aqueous suspension.

EFFECT: method described above is effective for rat sedation and causes no side effects.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and medicine and concerns using comenic acid potassium salt as a preventive and therapeutic antioxidant, stress- and neuroprotective agent in the amount of 2 to 8 mg per 1 kg of body weight daily on the empty stomach for 3 days.

EFFECT: agent possess high efficacy.

4 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyranyl aryl methylbenzoquinazolinone compounds of formula (I), which are positive allosteric modulators of the M1 receptor and which can be used to treat diseases associated with the M1 receptor, such as Alzheimer's disease, schizophrenia, pain disorders or sleep disturbance. In formula (I) X-Y are selected from a group comprising (1) -O-CRARB-, (2) -CRARB-O-, (3) -CRARB-SRC-, (4) -CRARB-NRC- and (5) -NRC-CRARB-, where each RA and RB is a hydrogen atom, and RC is selected from a group comprising (a) hydrogen, (b) -C(=O)-C1-6alkyl, (c) -C1-6alkyl, (d) -C(=O)-CH2-C6H5, (e) -S(=O)2-C1-6 alkyl, R1 is a hydroxy group, R2 is selected from a group comprising (1) -phenyl, (2) - heteroaryl, where the phenyl or heteroaryl group R2 is optionally substituted; the rest of the values of the radicals are given in the claim.

EFFECT: obtaining novel pyranyl aryl methylbenzoquinazolinone compounds.

28 cl, 12 tbl, 37 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and pharmacology and concerns using comenic acid sodium salt as a preventive and therapeutic antioxidant, stress and neuroprotective agent in the amount of 1 to 4 mg per 1 kg of body weight daily on the empty stomach for 3 days.

EFFECT: invention provides the high clinical effectiveness.

3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly to pharmacology and pharmaceutics, and concerns a sedative agent representing glycine immobilised on detonation nanodiamond particles 2-10 nm in size, and to a method for preparing it.

EFFECT: preparing the sedative agent.

4 cl, 7 dwg, 13 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention discloses crystalline form of S-zopicone with spectrum of powder X-ray diffraction with application of Cu-Ka radiation, with characteristic peaks, expressed under conditions 20 approximately at 11.08°, approximately 12.38°, approximately 15.86°, approximately 17.88°, approximately 19.98°C and approximately 20.58°, DSC-thermogram, on which peak is observed approximately at 207.7°C, and infrared spectrum of absorption (IR) with characteristic peaks approximately at 3078 cm-1, approximately 2942-2838 cm-1, approximately 2790 cm-1, approximately 1716 cm-1, approximately 1463 cm-1, approximately 1372 cm-1 and approximately 757 cm-1.

EFFECT: claimed are: method of preparation of crystalline form of eszopiclone, pharmaceutical preparation and its application in manufacturing medication for treatment of sleep disorder.

8 cl, 8 dwg, 10 ex

FIELD: medicine.

SUBSTANCE: present group of inventions refers to medicine, namely therapy and neurology, and concerns a melatonin agonist therapy. As the above melatonin agonist, (lR-Trans)-N-[[2-(2,3-dihydro-4-benzofuranyl)cyclopropyl]methyl]propanamide is administered in effective doses that provides treating or preventing disruption of circadian rhythm or sleep disturbance.

EFFECT: invention provides treating or preventing disruption of circadian rhythm or sleep disturbance.

9 cl, 2 ex, 4 tbl

FIELD: medicine.

SUBSTANCE: anaesthetising patients with chronic pain syndrome undergoing a cyclophotocoagulation surgery involves the intravenous administration of the hormonal preparation dexamethasone in a dose of no more than 8 mg followed by the anxiolytic droperidol in a dose of no more than 2.5 mg 5 minutes prior to the operation before the peribulbar anaesthesia. A peripheral block in the form of the peribulbar anaesthesia involving administration of no more than 6 ml of a local anaesthetic follows. At the moment the surgical procedure starts, benzodiazepin, e.g. diazepam, is administered in a dose of no more than 5 mg.

EFFECT: achieving adequate anaesthesia in the given category of patients by blocking all the links of a pathological pain chain.

1 ex

FIELD: medicine.

SUBSTANCE: dexamethasone 8 mg and ketoprofen 100 mg is administered intravenously once prior to the operation. A lumbar plexus is blocked in a combination with a parasacral block and inserting perineural catheters to administer weak 0.2% Ropivacaine, local anaesthetic 20 ml. Paracetamol 1,000 mg is administered intravenously 30 minute before the operation is completed. After the operation is completed, the perineural catheter of the lumbar plexus is used to infuse 0.2% Ropivacaine 300 ml at 6-8 ml/hour for 4-5 days. Ketoprofen 100 mg is administered intramuscularly twice a day for 3 days. Through the perineural catheter of the parasacral plexus, 0.2% Ropivacaine 10 ml is administered twice every 12 hours.

EFFECT: method provides the adequate anaesthesia in the given category of patients by having an effect on primary pain components, as well as ensures the continuous and prolonged anaesthesia both intra-, and postoperatively, prevents the stable and chronic pain syndrome and the motor block of the extremities, reduces a rate of toxic complications.

1 ex

FIELD: medicine.

SUBSTANCE: preanaesthetic medication preceding gynaecological surgeries under general anaesthesia is ensured by prescribing diazepam 10mg, nefopam 10mg and ketoprofen 100mg intramuscularly 30-40 min before the surgery.

EFFECT: method enables reaching the sedative and analgesic effect of the preanaesthetic medication by the complementary action of preparations with no undesired side effects, requiring no time consumption and expensive equipment.

3 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: as active component pharmaceutical composition contains dihydrochloride of 9-(2-morpholine ethyl)-2-(4-fluorophenyl)imidazo[1,2-α]benzimidasol, and as additional substances - fillers, binding, sliding and film coatings, in quantities, given in the invention formula. Composition can be made in form of solid medication form, mainly in form of tablets and capsules.

EFFECT: obtained solid medication forms satisfy the requirements of the State Pharmacopoeia.

7 cl, 2 dwg, 3 tbl, 14 ex

FIELD: medicine.

SUBSTANCE: at the initial stage of the intraoperative period, immediately before the local anaesthesia and the femoral artery puncture, ketorolac tromethamine is administered intravenously as an analgesic, and propofol as a sedative agent. Ketorolac tromethamine is administered in a dose of 15-75 mg, while propofol is administered in a dose of 50-250 mg.

EFFECT: method prevents developing pain and psychoemotional responses caused by the given interventions, including postoperatively by the fast development of the adequate analgesic effect accompanied by the controlled sedation level.

1 tbl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole derivatives of general formula (I) and to their pharmaceutically acceptable salts, mixed stereoisomers and enantiomers, wherein R1 is L1C(O)OL2C(O)OT; R2 is unsubstituted C1-C10alkyl; L1 is a bond; L2 is unsubstituted C2-C10alkylene; T is C1-C10alkyl. Also, the invention refers to a pharmaceutical composition of the compound of formula (I) and a method of anaesthetising on the basis of using the compound of formula (I).

EFFECT: there are prepared new imidazole derivatives effective as an anaesthetising agent.

15 cl, 9 dwg, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new compound, namely to (S)-enantiomer of 1'-{[5-(trifluoromethyl)furan-2-yl]methyl}spiro[furo[2,3-f][1,3]benzodioxol-7,3'-indole]-2'(1'H)-one of formula (I), and a method for preparing it which is effective for treating diseases and conditions, such as pain, an intensity of which can be reduced or relieved by modulating potential-dependent sodium channel gatings.

EFFECT: invention refers to the pharmaceutical composition of the above compound, methods of treating and a method of relieving an ion flux through the potassium channel gating in a cell.

10 cl, 5 tbl, 6 dwg, 11 ex

FIELD: biotechnology.

SUBSTANCE: aqueous composition for anaesthesia is proposed, which comprises propofol as an active agent, the PEG-660-12-hydroxystearate as a solubiliser, benzyl alcohol, or chloroethanol or parabens as preservative, the tocopherol and arginine or glycine at a specific content of components wt %. The GABA agonists can be additionally added to the composition, e.g. aminophenyl-butyric acid, local anesthetics such as lidocaine, alpha-2-adrenoceptor agonists such as xylazine. The method is proposed for implementing anaesthesia comprising administering to a patient of an effective amount of the claimed composition.

EFFECT: invention provides low toxicity of dosage form and high efficiency.

5 cl, 3 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: what is involved is infusion therapy with crystalloid solutions at 15 ml/kg of a patient's body weight. That is followed by puncturing and catheterising an epidural space at the level of ThVII-ThVIII according to the standard practice and introducing a test dose of 2% lidocaine 3 ml. If observing no signs of intrathecal introduction of local anaesthetics 10 minutes later, a basic dose containing 0.75-1% naropin 10 ml or 0.25-0.5% marcaine 10 ml and clofelin 3-5 mcg/kg is introduced. Total intravenous anaesthesia follows 20 minutes after pre-medication with atropine 0.01 mg/kg, 1% diphenylhydramine 1 ml and relanium 10 mg and urethral catheterisation. A narcosis is induced with propofol in a dose of 2 mg/kg. Anaesthesia is maintained with propofol 2-4 mg/kg·h. After that, within the first hour following the detoxification, naloxone 12 mg is introduced intravenously; a naloxone measurement rate is supposed to make 0.8 mg/h for 4-5 following hours of general anaesthesia. The repeated introduction of 0.75-1% naropin 6 ml or 0.25-0.5% marcaine 6 ml and clofelin 2-3 mcg/kg into the epidural space is performed 90 minutes later. After the procedure is terminated, and the patient recovers, prolonged epidural analgesia is conducted by introducing 0.2% naropin 10 ml and clofelin 1 mcg/kg into the epidural space every 4 hours for 24-48 hours.

EFFECT: method provides safety of ultrafast opioid detoxification and prolongs the remission in the given category of patients.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to anaesthesiology and resuscitation, and may be used in epidural anaesthesia. That is ensured by administering slowly intravenously a basic dose of the local anaesthetic: 0.2-1% naropin or 0.2-0.5% marcaine, or 1-2% lidocaine; 1% Sol. Nicotini acidi 1% - 0.5-1 ml into the epidural space 10-20 minutes later. After 5-10 minutes, nicotine test results are visually evaluated by determining a clear interface of skin colour - hyperemic and normal - along an axillary line from both sides. The normal skin interface corresponds to the sympathetic block.

EFFECT: method provides higher accuracy and simplification of measuring the sympathetic block.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry and describes a peroral combined medication for the treatment of arterial hypertension in patients with diabetes mellitus. The medication is made in the form of a tablet. The combined tablet contains perindopril erbumine, amlodipine besylate, sorbitol, microcrystalline cellulose, sodium carboxymethyl starch, povidone, magnesium stearate in quantities, given in the invention formula.

EFFECT: combination of perindopril, amlodipine and sorbitol in the composition of one tablet provides enhancement of the therapeutic effect.

6 tbl

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