Pharmacokinetics of amineptine after single-dose, repeated treatment and study of the at-risk populations.
In this paper, three different studies are discussed. First, pharmacokinetics of the tricyclic antidepressant amineptine (Survector) and its main metabolite were investigated in young healthy adults. Amineptine was rapidly absorbed. Mean peak plasma concentrations of amineptine and its metabolite occurred 1 and 1.5 h, respectively, after drug administration. The mean apparent volume of distribution was large: 2.4 L/kg. Elimination was rapid. T 1/2 (half-life) was 0.8 h for amineptine and 2.5 h for the metabolite. The mean apparent plasma clearance of amineptine was high (124.8 L/h). In a second study in young patients, no change in pharmacokinetic parameters was observed after a 10-day course of repeated treatment with the drug. Finally, pharmacokinetics of amineptine and its main metabolite were studied in elderly patients on day 1 and after a repeated administration for 15 days. There was no significant age-linked change in the pharmacokinetics of amineptine even if half-life and area under the curve of the metabolite were all greater in the elderly subjects than in young adults. Pharmacokinetic parameters of amineptine and its metabolite were not affected by repeated administration over 15 days. The pharmacokinetic characteristics of amineptine in elderly subjects do not necessitate any dosage alteration for this population.
Riché
C
C
C.H.U. Dupuytren, Limoges, France.
Lachatre
G
G
Guedes
Y
Y
Mocaër
E
E
Nicot
G
G
D000328:Adult; D000368:Aged; D000375:Aging / Q000378:metabolism*; D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003986:Dibenzocycloheptenes / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004285:Dogs; D005260:Female; D006801:Humans; D008297:Male; D015201:Meta-Analysis as Topic; D015337:Multicenter Studies as Topic; D051381:Rats; D012737:Sex Factors
D000929:Antidepressive Agents, Tricyclic; D003986:Dibenzocycloheptenes; C011597:amineptin