DE2356091A1 - MEDICINAL PRODUCTS WITH PSYCHOTROPIC EFFECT - Google Patents

Description

■ WSESOJUSNYJ NAUTSCHNO-ISSLEDOWATELSKIJ CHIMIKO-FARMAZEWTICHESKIJ INSTITUT IMENI SERGO ORDSCHONIKIDSE, USSR
Moscow

MEDICINAL PRODUCTS WITH PSYCHOTROPIC EFFECTS

Priority dated 11/28/1972 USSR No. 1850615 '

The present invention relates to a remedy with psychotropic effects, which is used for the treatment of depressive Conditions and other mental illnesses is determined.

At present, a variety is psychotropic and in particular antidepressant agents such as decipramine, imipramine, etc. are known. Although these funds are pronounced therapeutic Have an effect, as they cause a number of side effects, such as dryness in the mouth, constipation, and accommodation disorders etc., which their application in some crane r limit.

The object of the present invention was to develop a new remedy with a psychotropic effect, which in the Effectiveness is not inferior to any known agent, but causes fewer side effects.

This task was accomplished by 'developing a cure

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solved with psyehotropic effect, according to the invention a therapeutically effective amount of the active substance, which a Salt of 3-methyl-8-methoxy- (3H) -1,2,5,6-tetrahydropyrazine- [i , 2,3-abJ-ß-karbo.lins is of the following structural formula,

contains, wherein A is an organic or inorganic acid and a pharmaceutical carrier therefor.

The hydrochloride of the specified agent is below Called "Inkasan".

This substance is an odorless, white-yellowish powder with a bitter taste, which is easily soluble in water, has a molecular weight of 291.5 and a melting point of 305 to 308 ^° C. (with decomposition). The hemihydrate bitartrate of the specified compound is yellowish, easily soluble in water crystals with a molecular weight of 339 and a melting point of 220 to 222 ^° C.

The medicinal product is recommended for ingestion in the form of tablets, in which the carrier substance is a pharmaceutical filler such as lactose, starch and calcium stearate. The amount of active substance in tablets is 0.025 g.

The medicinal product in which the carrier substance is a pharmaceutical solvent, for example water for injections, is recommended for parenteral use. The amount of the active substance is 0.0125 to 0.025 g. An aqueous solution with a concentration of 1.25 % is used.

The pharmacological properties of the hydrochloride of the

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specified compound (Xnkasan) and its other salts, E.g. of hemihydrate bitartrate "are peculiar to preparations, that have antidepressant activity. The remedy according to the invention intensifies the central effects of phenamine and 5-oxytryptophan as well as the peripheral effects of adrenaline, phenylethylamine, tyramine, serotonin and tryptamine. . "·

The remedy of the invention weakens the depressing Effects of reserpine and tetrabenazine as well as the cataleptic Activity of phenothiazine or metherazine derivatives. In addition to similarities with well-known antidepressants (imipramine, decipramine etc.) the proposed remedy also has a number of differences. It does not exercise cholinolytic Effect from and does not increase the soporific effect of Hexanal, the analgesic effect of Promedol and the local anesthetic activity of novocaine.

The suggested remedy boosts that more than Imipramine Phenylethylamine, tyramine and tryptamine effects. According to dates Biochemical research calls the proposed remedy in doses that achieve an unmistakable pharmacological Effect are sufficient, a moderate inhibition of the monoamine oxidase activity only in the kidney tissue. this supports the assumption that the pharmacological effect of the medicament according to the invention is not due to an antimonoaminoxidase effect is based. - ^

The proposed remedy has only low toxicity. The LD ^ _{0 of} the preparation for mice when injected (per os) is 445 mg / kg.

A toxicological study of the proposed medicinal product, carried out in mice, rats and rabbits with one or more introductions (over the course of a month) has been shown that the preparation in doses that the

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for clinical treatment recommended doses around the 30-bis Exceed 50 times, does not have a toxic effect on animals.

The proposed remedy is used to treat depressive states in 46 sick people (13 men and 33 women) been. 33 patients were treated as inpatients and 13 outpatients. At the time of treatment, the patients were of the following age: up to 21 years - 2 sick, from 21 to 30 years - 20 sick, from 31 to 40 years - 10 sick, from 41 to 50 years - 11 Sick, over 50 years - 3 sick. According to the nosological affiliation, the patients had the following distribution:

I. Schizophrenia of which periodic relapsing sluggish

II. Manic-depressive psychosis

III. Reactive depression

The remedy was given in tablets of 25 mg 1 to 2 times administered daily (morning and evening). The average daily dose was 25 to 150 mg each according to the depth and structure of the depression, the duration of treatment from 1 to 2 weeks to 4 months.

As a result of the treatment carried out, it was complete disappearance of depression characteristics in 14 patients and a reduction in the severity of depression in 18 patients. The best therapeutic effect could be observed in patients with depressive symptoms that are related to Refer to disturbances of the anergetic pole. There are good results when treated with the suggested remedy also with neurotic and hypochondriac depression and

40 Sick 1 30th 9 4th Sick 2 Sick

A 0 9 8 2 7/1 0 6 * 7

OBiGIMAL

mild depression with depressive delusions has been observed.

This has been suggested for patients with troubled depression Remedies given in small doses of 25 to 50 mg / day, because larger doses increase anxiety was found and combined it with preparations of sedative effects (Tryphtasin, Sonapax, etc.).

When treated with the suggested remedies were the following side effects were noted: agitated depression - 1 case, increased restlessness and fear of restlessness - 3 cases, dermatitis - 2 cases, headache - 1 case. It should be noted that headaches and phenomena of the Dermatitis has been temporary (without discontinuation of the product).

Based on the conducted clinical investigations of the proposed Remedy "is to be found that Ihkasan is a for the treatment of sluggish, apatic, adynamic, neurotic, hypochondriac and depressive states is a suitable antidepressant agent.

Given the few side effects, the remedy can recommended for treatment in both inpatient and outpatient conditions. The proposed Remedies can be used in combined treatment with neuroleptics (Triphtasin, Äthaperasin, Sonapax, etc.).

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Claims (7)

Claims (Aj> remedy with psychotropic effects, characterized in that it contains a therapeutically effective amount of the active substance, which is a salt of 3-methyl-8-methoxy- (3H) -1,2,5,6-tetrahydropyrazine ^ [i , 2,3-ab ^ jf -ß-carbolins of the following structural formula contains, wherein A is an organic or inorganic acid and a pharmaceutical carrier therefor. 2. Remedy according to claim 1, characterized that it contains a pharmaceutical filler for tablets as a carrier substance. 3. Remedy according to Claims 1 and 2, characterized that it contains lactose, starch and calcium stearate as fillers. 4. Remedy according to Claims 1 to 3, characterized that it contains 0.025 g of active substance. 409827/1067 5. Remedy according to claim 1, characterized in that that it is a pharmaceutical carrier substance Contains solvent. ,. 6. Remedy according to Claims 1 and 5, characterized that it contains water for injections as a solvent. 7. Remedy according to claims 1, 5 and 6, characterized characterized as being 0.0125 Ms 0.025 g active Contains substance. 4 09827/1067