Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1990-06-18
1992-09-29
Friedman, S. J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514317, 514646, A61K 3154, A61K 31135, A61K 31445
Patent
active
051514192
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the treatment of schizophrenia characterized by negative symptoms by selegiline (1-Deprenyl) (-)-N-(1-phenylisopropyl)-N-methyl-propynylamine and to a composition for this treatment.
About one third of the schizophrenic patients amounting to 1% of the total population is characterized by negative symptoms, i.e. said patients suffer from schizophrenia of type II. according to Crow., i.e. they loose interest about themselves and their environment, their cognitive function gets damaged and their orientation to the future is characterized by ambivalence and ambitendency. The conventional neuroleptica as such are not successful, on the other hand, they may be harmful due to their side effects. (Ideggyogyaszati Szemle 1983, Psych. Res. 1984.)
Several compounds were tested for the treatment of these patients in order to find an effective drug and in order to be able to send home the patients treated for a long time in mental social homes.
Morphological changes are supposed to be observed in schizophrenic patients characterized by negative symptoms. (Brit. J. Psych. 1980, Brit. Med. J. 1983. Psychopharmacology Basic Aspects 1980, Schizophr. Bull. 1982, Arch. Gen. Psych. 1982, Arch. Gen. Psych. 1982, Arch. Gen. Psych. 1986.)
It is known that within the nerve system the dopamine hypofunction is in connection with the Parkinson disease (Klin. Wschr. 1960.) leading to the treatment with 1-DOPA (Canad. med. Ass. J. 1969.). But the increase of the dopaminerg tone concerning the whole organism, was accompanied by several side effects (hypertonic crisis, tremor, gastrointestinal disorders etc.).
It is further known that 1-deprenyl inhibits the monoamino-oxydase-B (MAO-B) enzyme, i.e. it acts as dopamine agonist (Arch. Intern. Pharmacodyn. 1965.).
Schizophrenia is characterized according to our present knowledge by the hyperactivity of the mesocortical system, which can be located mainly to the nucleus accumbens. This hyperactivity is decreased by neuroleptica. Post-mortem investigations have proved that the number of dopamine receptors of the above brain parts increases upon long neuroleptic treatment. (A pszichiatria alapjai, Akademia Kiado Budapest 1986. p. 168.).
On the basis of this knowledge it could not be expected that selegiline is suitable for the treatment of schizophrenia.
The psychiatric indications of the successfully tested selegiline are given on the basis of the New Haven Schizophrenia index, the Carpenter-Strauss-Bartko WHO Flexible System and the DSM III systems. In each case the precondition is the confirmation of the diagnosis of the schisophrenia and the exclusion of organic, toxic (drug, alcohol), affective pathological forms.
Considering these results the selegiline is suggested for the following symptoms: slow and almost symptomless beginning, deficiency in impulses, introversion, lack of rapport ability, hesitating speech, poor associations, insensibility, asthenia, lack of feeling of joy, instinct dynamical fading, poor social and working connections, isolation.
The group of symptoms can appear at the beginning of the pathological process of schisophrenia or at its subchronic or chronic period as well.
Selegiline is applied at a daily dosage of 10-50 mg on each occasion at 5-10 mg, preferably orally or intramuscularly. It may be administered together with one or more neuroleptica. It is suggested to carry on with the treatment for at least one month, but depending on the condition of the patient the treatment may be prolonged for a longer period.
The used selegiline can be prepared by methods disclosed in HU PS 154 655 and 187 775. The most preferred drug forms are the tablets and capsules.
Neuroleptica are a group of compounds defined in the Dictionary of Pharmacology (Blackwell Scientific. Publ. Oxford 1985, p. 143), the best known representatives of this group are chlorpromazine, thioridazine, flufenazine, haloperidol and pimozide. The maintaining neuroleptic treatment is carried out with the usual therapeutic doses.
The pharmaceutical compositions according to
REFERENCES:
Parsad, E., Rakodd, V.: Use of Drugs in Psychiatry, A Handbook, Hans Huber Publ., Toronto, 1987, p. 3.
Bernstein, J. G., Handbook of Drug Therapy in Psychiatry, Second Ed., PSG Publishing Co., Inc., Littleton, MA (1988), pp. 112-113.
Chem. Abst. 113-145354e (1990) refers to 1988 article.
Arato Mihaly
Bela D. Arpad
Frescka Ede
Knoll Jozsef
Perenyi Andras
Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara RT.
Dubno Herbert
Friedman S. J.
Myers Jonathan
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