Abstract

We developed mathematical models allowing us to calculate the parameters of pharmacokinetics of exogenous ligands based on the analysis of their pharmacodynamics under the direct influence of a pharmacological agent (agents), PhA, on tissues possessing the receptor–effector system for this PhA, i.e., on the biophase of action of this PhA. The dynamics of the paroxysmal activity induced by application to the rat brain cortex of convulsant drugs (modulators of the GABAA transmitter system) in different doses were studied. It has been demonstrated that the pharmacokinetic scheme of physiologically active substances, in the case of their direct application, can be interpreted using a chain-chamber model, whose parameters are determined by two irreversible processes of the first order: entry and elimination. The hypothesis supposing the irreversibility of the kinetic scheme of PhA mass transfer under conditions of direct application of these agents was experimentally verified.

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