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Full characterization of a concentration– effect relationship requires determination of the EC50, the maximally possible effect (Emax), and the slope at the point of inflection. In order to elicit their effect, drug molecules must be bound to the cells of the effector organ. Binding commonly occurs at specific cell structures, namely, the receptors.
In healthy subjects, absorbed glucose and insulin released from the pancreas simultaneously reach the liver in high concentration, whereby effective presystemic elimination of both substances is achieved. In the diabetic, s. c. injected insulin is uniformly distributed in the body. Since insulin concentration in blood supplying the liver cannot rise, less glucose is extracted from portal blood.


Indroduction of a small alkyl residue at the carbon atom adjacent to the amino group (ephedrine, methamphetamine) confers resistance to degradation by MAO (p. 80), as does replacement on the amino groups of the methyl residue with larger substituents (e. g. , ethyl in etilefrine).
Central: Motor restlessness, progressing to maniacal agitation, psychic disturbances, disorientation, and hallucinations. Elderly subjects are more sensitive to such central effects. In this context, the diversity of drugs producing atropine-like side effects should be borne in mind: e.g., tricyclic antidepressants, neuroleptics, antihistamines, antiarrhythmics, antiparkinsonian agents.


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