CLASSIFICATION AND DETERMINATION OF CEREBRAL BIOAVAILABILITY OF PSYCHOTROPIC-DRUGS BY QUANTITATIVE PHARMACO-EEG AND PSYCHOMETRIC INVESTIGATIONS (STUDIES WITH AX-A411-BS)

  • 1 January 1977
    • journal article
    • research article
    • Vol. 15  (10) , 449-459
Abstract
Utilizing computerized quantitative analysis of the human scalp recorded EEG, it is possible to classify psychotropic drugs. While neuroleptic compounds produce an increase of slow and decrease of fast activities, anxiolytic substances induce an augmentation of fast waves, decrease of .alpha. waves and, according to the sedative properties of the drug, an increase or decrease of slow waves. Antidepressants produce a concomitant augmentation of slow and fast activities as well as an attenuation of .alpha. waves. Neotropic substances attenuate slow activities, augment .alpha. and slow .beta. waves and decrease fast .beta. waves. The latter alterations are opposite to age-related changes. Since the main psychopharmacological classes seem to have characteristic pharmaco-EEG profiles, the method proved to be useful for determination of psychoactivity and cerebral bioavailability of newly developed substances, e.g., AX-A411-BS (7-chlor-5-(2-chlorphenyl)-1,3-dihydro-1-methyl-3-(morpholino)methylene-2H-1,4-benzodiazepine-2-one), a new benzodiazepine. The latter substance was CNS-active and was classified as anxiolytic. It induced dose-dependent changes, which were barely visible in the 2nd h post-drug, became obvious in the 4th h and increased until the 8th h after oral administration of 1 single dose. In the higher dosage range, slow activities came to the fore, indicating additional sedative properties. Psychometric tests measuring attention, psychomotor activity, mood, vigilance, extroversion, concentration and personality dimensions showed that AX-A411-BS is a psychoactive compound with a long-lasting effect. The implications of these methods are discussed.

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