The treatment for alcohol intoxication

 

(57) Abstract:

The invention relates to medicine, namely to create tools for the treatment of alcohol intoxication. The invention lies in the fact that the proposed product contains pikamilon, lipoic acid, pyridoxine hydrochloride and panthenol or calcium Pantothenate and can be used in the form of capsules or tablets. The invention provides the use of a tool that is effective for relief of symptoms of acute alcohol intoxication, as well as for the treatment of alcohol and drug dependence.

The invention relates to medicine, specifically to the pharmaceutical industry, namely, to obtain the metabolic therapy in acute poisoning with ethyl alcohol for relief of symptoms in chronic alcohol intoxication, for rehabilitation treatment of drug and alcohol addiction.

Known use as a tool for the treatment of chronic and acute alcohol poisoning drug metadoxine [1]. The drug acts on enzymes involved in ethanol metabolism, accelerating its excretion from the body. Metadoxine also improves neuropsychiatric and polednak in ampoules of metadoxine contains sodium metabisulfite, which causes an allergic reaction, especially in people with asthma (severe asthma). In addition, metadoxine incompatible with drugs L-DOPA and is contraindicated in patients with Parkinson's disease.

It is also known the use of the drug pikamilon (sodium salt of N-nicotinoyl-gamma-aminobutyric acid) in complex therapy to relieve withdrawal symptoms in individuals suffering from alcoholism [2]. In the treatment of pikamilon persons with chronic alcoholism was observed: strong sedative effect, weakening the vegetative and somatoliberin symptoms, reduction of anxiety and withdrawal symptoms, activating and improving sleep. In therapy of acute alcohol intoxication revealed the ability of this drug to recover in the short term mental and physical performance, to normalize the conditioned reflex activity. therapeutic effect is manifested in the form of disappearance or significant reduction in anxiety, aggressiveness, irritability, internal stress and hyperesthesia. The drug improves hemodynamics in patients, reduces pulmonary hypertension and increases cardiac output.

However, pikamilon has no hepatotoxicity.

The present invention is the creation of the drug on the basis of picamilone elevated detoxifying effect, and also has hepatoprotective properties.

The problem is solved as follows:

In the composition of the drug, in addition to picamilone include lipoic acid, pyridoxine hydrochloride and panthenol or calcium Pantothenate in the following ratio of components, wt.%:

lipoic acid - 5-40

pyridoxine hydrochloride - 5 -10

panthenol or calcium Pantothenate - 15-25

pikamilon - rest

The pikamilon corresponds to FS 42-2862-98.

Lipoic acid (corresponding to FS 42-1918-94), entered into the composition of the drug involved in the oxidative decarboxylation of a-ketoacids and participates in the formation of acetyl-coenzyme A. Under her influence, the improvement tarifitsirujutsja liver, increases bile secretion and diuresis.

Pyridoxine hydrochloride (corresponding GF X, p 566) accelerates the metabolic oxidation of ethanol and thus reduces the damaging effect of acetaldehyde on cell function, promote the excretion of ketones with urine.

Pantothenic acid (used in the non participation in the transfer of acetyl groups, as part of the multienzyme system oxidative decarboxylation. Pantothenic acid (panthenol) restores the level of coenzyme A, helps to normalize the metabolism of phospholipids in the liver and brain, while significantly attenuated narcotic effect of ethanol by increasing utilization of acetaldehyde and acetate via acetyl-coenzyme-A - synthetase and N-acetyltransferase reaction.

Thus, the high efficiency of the proposed drug is a wide range and features of psychotropic and metabotropic effect of its components, which are mutually enhanced by the use of the proposed combination.

Members of the drug components of regulation piruvatdegidrogenazy system affect the metabolism of the decay products of ethanol and thereby contribute to detoxification at the cellular level.

The proposed drug is water-soluble, all components are compatible and can be used in the form of injection solutions or tablets.

The method of obtaining the proposed framework is illustrated by the following examples:

Example No. 1.

Dissolve 40 g of picamilone, 4 g pyridoxine added a solution of 4 g of lipoic acid in 150 ml of water, purified for injection containing 2 ml of 70% aqueous solution of Ethylenediamine (reagent-grade), bring water to 1 l, poured into ampoules of 5 ml, sterilized by autoclaving at 120oC for 5 minutes the Drug is a clear slightly yellow liquid.

Example N 2

Mix 90 g picamilone, 10 g of lipoic acid, 10 g of pyridoxine hydrochloride, 30 g of calcium Pantothenate, add 2 g of calcium stearate and 7.5 ml of water, homogenize. The resulting mixture was passed through a sieve with the hole diameter of 2 mm, dried to a residual moisture content of 6%. The dried granulate is sieved and tabletirujut in the form of cylindrical tablets with beveled edges, the weight of 0.26 g

The specific study of the effectiveness of the proposed drug was carried out at the Institute of toxicology of Ministry of health of the Russian Federation, St.-Petersburg, Russia) according to the Methodical recommendations for a pilot study of drugs proposed for clinical testing as a means for the treatment and prevention of alcoholism (Pharm. the Committee 8.07.1979 g, Protocol No. 12). Drug comparison was selected pikamilon recommended Pharm. Committee for the treatment of alcohol intoxication.

Experiments were performed on 86 white rats-males weighing 200-230 g Pikantanya.

A comparative study of picamilon and the proposed drug for the duration of the drug action of ethanol found that pikamilon virtually no effect on the duration of ethanol sleep. The proposed drug has reliable stimulative effect.

Research to identify the effectiveness of picamilon and proposed integrated product on the survival of animals following acute ethanol poisoning found that both drugs increase the number of surviving animals. Protective effect of probiotic preparation significantly exceeds pikamilon in identical conditions of this pathology.

In severe poisoning with ethanol development violations of the electric conductivity of the myocardium introduction picamilon improves heart function, but remain phenomenon aritmogennosti. Reduction of disturbances in the electrical conductivity of the heart under the action of a complex of the drug is more pronounced. Morphological studies have confirmed the disappearance of dystrophic changes in myofibrils, there was a decrease in body inclusions in myocytes and restoring the ultrastructure of mitochondria.

The study showed that pikamilon CII. However, the normalization of cerebral blood flow is not continuous and requires maintenance doses. Morphological studies have documented the disappearance of patogennogo edema, however, the destruction of the neurons remained.

The proposed introduction of the drug provides a more stable and long-term normalization of cerebral circulation. Increasing the intensity of circulation was larger and more lasting than monotherapy pikamilon. Morphological studies revealed the structural stabilization hemolymphoreticular barrier reduction patogennogo and cytotoxic brain edema, the normalization of the structure of dendrites.

The proposed comprehensive drug is longer than the introduction of picamilone, compensation of metabolic acidosis, and also has a hepatoprotective effect. It normalizes the activity of aspartate-alanineaminotransferase, stabilizes the intensity of lipid peroxidation in MDA the MDA in liver tissue. The drug restores the ultrastructure of mitochondria with the disappearance of lipid droplets in the cytoplasm of hepatocytes, normalizes the structure of cells.

The study is the first alcohol intoxication, set a time reduction of hospital stay and duration of rehabilitation of patients. The inclusion of the drug in the complex standard detoxification therapy provides access patient of the serious condition with less severe neurological symptoms, activating vegetative sphere and fewer complications. The drug is injected intravenously infusion at a rate of 40-60 drops per minute, a daily dose of up to 20-25 ml of a standard solution (10 ml diluted in 400 ml of physiological solution). Treatment within 24-48 hours.

Thus, the proposed comprehensive drug represents a new pharmacological tool for relief of symptoms of acute alcohol intoxication and acute rehabilitation of drug addicts.

Bibliography:

1. Annoni G. Metdadoxine (Metadoxil) in alcoholic liver diseases: Its Theraputic role, Clin. Trials J., 1988, 25 (5) R. 333-41.

2. Sobolev, E., A. Ovsyannikov, A. Sidorov P. the Use of picamilon in the treatment of alcoholism. Sat. Grew up with. proc. Pikamilon in modern neurological and psychiatric practice, 1997, S. 131-35.

The treatment for alcohol intoxication, containing pikamilon, characterized in that it additionally sterivent, wt.%:

Lipoic acid - 5 - 40

Pyridoxine hydrochloride - 5 - 10

Panthenol or calcium Pantothenate - 15 - 25

Pikamilon - Rest

 

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