-
効能
抗うつ薬, セロトニン・ノルアドレナリン再取り込み阻害薬
-
使用
Desipramine is used for depression of various etiology and in particular for endogenous
depression.
-
定義
ChEBI: A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.
-
作用機序
Its antidepressant effect results from increases in the level of NE in CNS synapses, and long-term
administration causes a downregulation of α1-adrenoceptors and desensitization of presynaptic α2-receptors, equilibrating
the noradrenergic system and, thus, correcting the dysregulated output of depressed patients. The SSRIs do
not produce this effect. Desipramine also downregulates the NET, but not the 5-SERT . Substantial loss of NE
transporter–binding sites takes 15 days to occur and is accompanied by a marked reduction of NET function
in vivo. Desipramine has weak effects on 5-HT reuptake.
-
代謝
Desipramine is a dihydrodibenzazepine secondary amine TCA that also is the active metabolite of imipramine. Desipramine appears to have a bioavailability comparable to the other secondary TCAs. Desipramine is distributed into milk in concentrations similar to those present at steady state in
maternal plasma. This drug is metabolized primarily by CYP2D6 to its 2-hydroxy metabolite and by CYP1A2
and CYP2C19 to its N-demethylated (primary amine) metabolite .
Desipramine exhibits a greater potency and selectivity for the NET than the other secondary TCAs do.
