[Amineptine, a new antidepressant: pharmacological review (author's transl)].
Amineptine is a tricyclic derivative with a 7-carbon chain of aminoacids. Chemical alterations of the aminoacid chain have revealed its importance in the shaping of the pharmacological effects. The drug is rapidly absorbed. Amineptine is metabolised principally by beta-hydroxylation of the chain. The pharmacological profile at different doses is as follows: a. 0.1 mg/kg: reduction of exploratory behaviour, b. 1 mg/kg: reduction of serum prolactin level, c. 5 mg/kg: potentiation of L-5 HTP, d. 10 mg/kg: antagonism of the effects of reserpine and of tetrabenazine, e. increased activity and social behaviour, EEG alerting effect limited to 1 hour and increase in paradoxical sleep (15 to 20 mg/kg). This pharmacological profile suggests an effect of amineptine upon certain dopamine structures. At synapse, neurobiochemistry confirms a mechanism of inhibition of DA incorporation and inhibition of uptake and/or release of 5 HT. Amineptine is virtually devoid of peripheral activity, particularly anticholinergic Amineptine may be indicated for the treatment of depression where retardation is dominant.
D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000097:blood / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001711:Biotransformation; D001831:Body Temperature / Q000187:drug effects; D001921:Brain / Q000187:drug effects; D003986:Dibenzocycloheptenes / Q000097:blood / Q000494:pharmacology*; D004569:Electroencephalography; D005071:Evoked Potentials / Q000187:drug effects; D006801:Humans; D018377:Neurotransmitter Agents / Q000378:metabolism; D012110:Reserpine / Q000494:pharmacology
D000929:Antidepressive Agents, Tricyclic; D003986:Dibenzocycloheptenes; D018377:Neurotransmitter Agents; C011597:amineptin; D012110:Reserpine
Revue pharmacologique sur l'amineptine.