Application of lidocaine derivative with local anesthetic activity, for terminal anesthesia

FIELD: medicine.

SUBSTANCE: invention can be used for application of a lidocaine derivative - N-acetyl-L-glutamate 2-diethylamino-21,61-dimethyl phenylacetamide of the general formula (1)

with local anesthetic activity, for terminal anesthesia.

EFFECT: invention allows to reduce acute toxicity, increase the breadth of therapeutic action, increase the depth and duration of terminal local anesthesia without a local irritant effect compared to lidocaine.

3 tbl, 3 ex

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a pain control formulation containing 4 wt % to 10 wt % of Lidocaine and 4 wt % to 10 wt % of Tetracaine, 10 wt % to 40 wt % of polyvinyl alcohol, water and sorbitan monostearate (Span 60) as an emulsifier, wherein water/PVA mass ratio makes more than 2.5, wherein the formulation provides the transdermal delivery of Lidocaine and Tetracaine, and wherein the delivery is terminated or considerably slows down when water evaporates completely, and wherein the formulation possess an initial viscosity from approximately 28,000 centipoise to approximately 828,000 centipoise, and shows a after 3 freeze-thaw cycles at least 2 times as much as the initial viscosity; the freeze-thaw cycle is determined by placing the formulation into the environment of temperature -18°C to -22°C for the time period of 48 hours and thawing the formulation at room temperature (approximately 25°C) for the time period of 48 hours.

EFFECT: invention provides the improved long-term storage of the compositions.

16 cl, 9 ex, 7 tbl, 2 dwg

FIELD: medicine.

SUBSTANCE: catheter is inserted into the retrobulbar space and used to introduce 2% lidocaine 1 ml and 0.5% marcaine 1 ml 15-20 minutes before applicator anchoring. The catheter is left in the retrobulbar space for 1-7 days. 10-15 minutes before removing the applicator, 2% lidocaine 0.5-1 ml and 0.5% marcaine 0.5-1 ml are introduced through the catheter. 4-6 hours after anchoring and removing the applicator, 2% lidocaine 1 ml and 0.5% marcaine 1 ml are introduced respectively additionally.

EFFECT: achieving adequate and prolonged anaesthesia in a combination with reducing a risk of a retrobulbar haematoma, eyeball puncture and visual nerve damage by eliminating the retrobulbar space re-puncture.

2 ex

FIELD: medicine.

SUBSTANCE: after performing median sternotomy pericardial and mediastinal drainages are installed and sternum is sutured. After suturing sternum for length of its entire front surface, catheter is installed through skin counterpuncture, with 1.0-2.0 cm indent from lower wound edge. proximal end of catheter is fixed to subcutaneous-adipose cellular tissue with absorbable suture material, and distal part of catheter with cannula is fixed by suturing to skin with non-absorbable suture material. Local anaesthetic is introduced through installed catheter every 6 hours, with antibiotic being introduced every 8 hours. Introduction of medications is performed for 3-5 days.

EFFECT: method provides effective anaesthetics with simultaneous drainage of front sternum surface and skin wound due to introduction of anaesthetics and antibiotics via catheter into said zone, which additionally reduces quantity of exudative inflammatory complications in post-operative period.

2 dwg, 1 ex

FIELD: medicine.

SUBSTANCE: spinal anaesthesia is followed by catheterisation of an epidural space at the level of L1-L2. The spinal anaesthesia is performed at the level of L4-L5 by administering 0.5% bupivacaine. Bupivacaine is administered in a dose of 5-6 mg if the pregnant woman's height is less than 165 cm, and the dose is 6-7 mg if the pregnant woman is from 165 to 175 cm high. After the local anaesthetic is administered into the epidural space, normal saline is introduced. If the intra-abdominal pressure is ≤16 cm H2O, normal saline 15 ml is administered; if the intra-abdominal pressure is 17-21 cm H2O, an amount of normal saline is 10 ml, whereas the intra-abdominal pressure of 22-28 cm H2O requires an amount of 5 ml.

EFFECT: performing the effective spinal anaesthesia combined with reducing a probability of hypertension by dilating the epidural space preliminary in accordance with the intra-abdominal pressure.

1 tbl, 1 dwg, 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, pharmaceutics.

SUBSTANCE: invention refers to a percutaneously absorbable layer having a base and an adhesive layer which is placed on the base and which comprises an adhesive agent and a therapeutic ingredient. The adhesive agent contains a mixture of resins containing 100 portions by weight of an acrylic copolymer (A) and 0.1 to 30 portions by weight of an acrylic copolymer (B) or 0.05 to 2 portions by weight of a low-molecular polyamine compound having at least two amino groups in one molecule and non-polymerising with a polymer or an oligomer formed. The adhesive layer additionally contains an organic acid. The acrylic copolymer (A) represents an acrylic copolymer, which contains acrylic ester of (meth)acrylic acid as a main monomer ingredient and contains 3 to 45 wt % of diacetone acrylamide as a target monomer ingredient, but free from a free carboxylic group. The acrylic copolymer (B) represents an acrylic copolymer, which contains acrylic ester of (meth)acrylic acid as a main monomer ingredient and contains a primary amino group and/or carboxyhydrazidase group on side chains, but free from a free carboxylic group.

EFFECT: reducing the aging period of the adhesive layer considerably.

7 cl, 8 tbl, 39 ex

FIELD: medicine.

SUBSTANCE: therapeutic agent contains hypromellose, boric acid and a consistency base; it additionally contains anesthesin or lidocaine as an analgesic in an amount of 0.00001-0.5 g.

EFFECT: fixing a lubricating agent on the catheter enabling preventing mucosal injuries accompanying a drainage procedure, and eliminating side effects.

3 cl, 6 ex

FIELD: medicine.

SUBSTANCE: anterior chamber anaesthesia and pupil dilatation accompanying anterior eye segment surgeries experimentally involve a preoperative administration of a composition in an amount of 0.1-0.2 ml representing 0.005% 1-(3-pyrrolidinopropyl)-2-phenylimidazo[1,2-a]benzimidazole dihydrochloride into the anterior eye segment. The composition is prepared in 1% viscoelastic solution, visiton PEG.

EFFECT: prolonging anaesthetic effect and pupil dilatation with no mydriatics used.

2 ex

FIELD: veterinary medicine.

SUBSTANCE: intramesovarian blockade of ovarian and cranial uterine nerves is carried out by laparotomy and administration in the mesovarium of 0.5-1% solution of novocaine or lidocaine. Blockade is carried out by inserting the needle of the syringe into the mesovarium in the vicinity of the ovarian bursa and uterine horn at an acute angle to the surface of the ovarian mesenterium to a depth of 3-4 cm. At that 3 ml of anaesthetic is administered to small breeds of dogs and fur-bearing animals, and from 3 to 9 ml of anaesthetic is administered to large and giant breeds of dogs as from one and from the opposite side of the body.

EFFECT: effective implementation of intramesovarian blockade by taking into account the anatomical and the breed features of the animal category.

1 tbl

FIELD: medicine.

SUBSTANCE: patient is laid on his/her side opposite a block region. A guide mark is a vertical line in a projection of Petit's triangle from the twelfth rib to a wing of ilium. A needle is pricked into the skin on the vertical line at 1.5-2.5cm above the wing of ilium. 0.25% Novocaine is administered in layers into the skin and subcutaneous fat. The needle is advanced into the lumbar region from back to front in the medial direction along the lateral edge of broadest muscle of back at 6-8cm. Novocaine 120ml is administered into the lower order of the lumboiliac fossa formed in this region.

EFFECT: effective and safe pain management in the given category of patients by providing the required Novocaine concentration in the retroperitoneal space.

1 dwg, 1 ex

FIELD: medicine.

SUBSTANCE: method involves instilling the Colegel ADL gel preparation every second day from the 1st to 20th day, and then Colegel DNK L two times a week from the 21st to 56th day.

EFFECT: invention enables relieving pain symptomatic, reducing the rate and length of recurrences in the patients.

3 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, pharmaceutics.

SUBSTANCE: present invention aims at pharmaceutical compositions containing a number of microparticles with taste masking, containing high-/low-dose therapeutic agents, at dosage forms containing the above pharmaceutical compositions (such as orally dispersible tablets), and at methods for producing these pharmaceutical compositions and dosage forms.

EFFECT: dosage forms containing the pharmaceutical compositions according to the invention represent the improved homogenous mixtures of the high-dose and low-dose therapeutic agents, which enable controlling the release rate of the therapeutic agent from particles by various ways, as well as flexible correction of dosages when administering the combinations of the therapeutic agents, eg in pain management.

31 cl, 4 dwg, 12 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 3-phenylpropionic acid derivatives of formula

wherein R1A represents hydrogen, methyl, ethyl, cyclopropyl or cyclobutyl, R1B is hydrogen or methyl, R2A represents hydrogen, methyl, trifluoromethyl, ethyl or n-propyl, R2B is hydrogen or methyl or R1A and R2A are combined together, and in a combination to carbon atoms to which they are attached, form a cyclopropyl ring of formula

wherein R1B and R2B have the values as specified above, or R2A and R2B are combined together, and in a combination to a carbon atom, to which they are attached, form a cyclic group of formula or

wherein n means a number 1 or 2, R3 is hydrogen, fluorine or methyl, R4 represents hydrogen, fluorine, chlorine or a cyanogroup, R5A represents methyl, R5B is trifluoromethyl or R5A and R5B are combined together, and in a combination to a carbon atom, to which they are attached, form a difluorosubstituted cycloalkyl ring of formula or

R6 represents chlorine, alkyl with 1-4 carbon atoms, alkenyl with 2-4 carbon atoms, cyclopropyl or cyclobutyl; alkyl with 1-4 carbon atoms and alkenyl with 2-4 carbon atoms can contain up to three fluorine atoms, cyclopropyl and cyclobutyl up to three fluorine atoms as substitutes, and R7 represents hydrogen, fluorine, chlorine, methyl or a methoxy group. The invention also refers to a therapeutic agent containing the above compounds and to a method for producing the compounds of formula (I).

EFFECT: compounds of formula (I) activate the form of soluble haem-free guanylate cyclase and are applicable in the method of treating and/or preventing cardiac failure, angina, hypertension, pulmonary hypertension, ischemia, vascular diseases, disturbed microcirculation, thromboembolic diseases and arterial sclerosis.

6 cl, 4 tbl, 113 ex

FIELD: medicine.

SUBSTANCE: catheter is inserted into the retrobulbar space and used to introduce 2% lidocaine 1 ml and 0.5% marcaine 1 ml 15-20 minutes before applicator anchoring. The catheter is left in the retrobulbar space for 1-7 days. 10-15 minutes before removing the applicator, 2% lidocaine 0.5-1 ml and 0.5% marcaine 0.5-1 ml are introduced through the catheter. 4-6 hours after anchoring and removing the applicator, 2% lidocaine 1 ml and 0.5% marcaine 1 ml are introduced respectively additionally.

EFFECT: achieving adequate and prolonged anaesthesia in a combination with reducing a risk of a retrobulbar haematoma, eyeball puncture and visual nerve damage by eliminating the retrobulbar space re-puncture.

2 ex

FIELD: medicine.

SUBSTANCE: after performing median sternotomy pericardial and mediastinal drainages are installed and sternum is sutured. After suturing sternum for length of its entire front surface, catheter is installed through skin counterpuncture, with 1.0-2.0 cm indent from lower wound edge. proximal end of catheter is fixed to subcutaneous-adipose cellular tissue with absorbable suture material, and distal part of catheter with cannula is fixed by suturing to skin with non-absorbable suture material. Local anaesthetic is introduced through installed catheter every 6 hours, with antibiotic being introduced every 8 hours. Introduction of medications is performed for 3-5 days.

EFFECT: method provides effective anaesthetics with simultaneous drainage of front sternum surface and skin wound due to introduction of anaesthetics and antibiotics via catheter into said zone, which additionally reduces quantity of exudative inflammatory complications in post-operative period.

2 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to a method of manufacturing a tablet by pressing a powder mixture in a press-mould plate with the formation of a tablet form, with the powder mixture including a pharmaceutically active substance and hydrated sugars, as well as exposure of the tablet form to radiation for a period of time, sufficient for heating the hydrogen-containing material in the tablet form to a temperature higher than its dehydration temperature with the tablet formation.

EFFECT: increase of production efficiency.

21 cl, 14 dwg, 3 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine. Described is medical form for transmucousal per oral introduction of, at least, one active substance of antispasmodic and/or analgesic action, which contains said active substance in form of base and/or in form of salt, water-alcohol solution, with alcoholic content, at least, 35° of alcohol by weight, with said active substance being present in water-alcohol solution in condition of stable and complete dissolution. Invention also relates to method of said medical form preparation and its application for treating spastic attacks.

EFFECT: medical form makes it possible to realise instantaneous transmucousal per oral introduction.

10 cl

FIELD: medicine.

SUBSTANCE: invention represents an agent for treating septic wounds, pus pockets and trophic ulcers containing betaine hydrochloride, methyluracil, trimecaine, pepsin powder and polyethylene oxide 400 with the ingredients taken in certain proportions, wt %, and polyethylene oxide 400 is taken in an amount of 87.0-84.0 ml.

EFFECT: invention provides fastening necrolysis, intensifies bactericidal action, stimulates regeneration, prevents secondary infection.

4 ex

FIELD: medicine.

SUBSTANCE: introduction of endoscope into duodenum is realised. After that, "tight" filling of choledoch is performed through cholecystostoma with sterile solution, for instance, 0.25% Novocain. After that major duodenal papilla is catheterised and endoscopic papillosphincterotomy is carried out.

EFFECT: method makes it possible to provide effective surgical treatment of cholelithiasis with simultaneous reduction of probability of development of complications due to provision of possibility of fast identification and good visualisation of major duodenal papilla.

1 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I):

wherein X means group of the formula (X-1) wherein R15 means halogen atom, (lower)-alkyl and perfluoro-(lower)-alkyl; R16 means hydrogen, halogen atom and (lower)-alkyl; or X means group of the formula (X-2) wherein Het means 5- or 6-membered heteroaromatic ring comprising 1 or 2 heteroatoms as nitrogen (N) atom; R15 and R16 have values indicated above for (X-1); R30 means hydrogen atom or (lower)-alkyl; p means a whole number from 0 to 1; or X means group of the formula (X-3) wherein R18 means aryl; R19 means unsubstituted arylalkyl or heteroarylalkyl representing 6-membered heteroaromatic ring comprising nitrogen (N) atom as a heteroatom; R20 means unsubstituted (lower)-alkanoyl; Y means group of the formula (Y-1) wherein R22 and R23 mean independently from one another hydrogen atom, (lower)-alkyl, halogen atom or perfluoro-(lower)-alkyl and at least one of radicals R22 and R23 doesn't mean hydrogen atom; R24 means hydrogen atom; or Y means group of the (Y-3) wherein R25 means group of the formula: R26-(CH2)e- wherein R26 means (lower)-alkoxy-group, (lower)-alkylthio-group, (lower)-alkylsulfonyl; or R26 means group of the formula: -NR28R29 wherein R28 means hydrogen atom; R29 means (lower)-alkanoyl or (lower)-alkylaminocarbonyl; Q means -(CH2)f- wherein e means a whole number from 0 to 4; f means a whole number from 1 to 3; a bond denoted as a dotted line can be hydrogenated optionally; and to its pharmaceutically acceptable salts and esters. Also, invention proposes a pharmaceutical composition designated for treatment or prophylaxis of rheumatic arthritis, cerebrospinal sclerosis, intestine inflammatory disease and asthma and containing compound of the formula (I) or its pharmaceutically acceptable salt or ester in combination with a compatible pharmaceutical carrier. Invention proposes derivatives of thioamide inhibiting interaction between α4-comprising integrins and VCAM-1.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

20 cl, 1 tbl, 86 ex

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