ブプロピオン 化学特性,用途語,生産方法
効能
抗うつ薬, ノルアドレナリン・ドパミン再取り込み阻害薬
説明
Bupropion hydrochloride, an aminoketone structurally unrelated to tricyclics or
tetracyclics, is a dopamine uptake blocker with antidepressant activity. Its clinical
efficacy is reportedly comparable to that of amitriptyline, yet unlike most conventional
antidepressants, bupropion hydrochloride is not associated with orthostatic hypotension or
other cardiovascular side-effects.
使用
vasoconstrictor;non-selective agonist of all adrenergic receptors
生物学の機能
Bupropion (Wellbutrin) is a pharmacologically unique
antidepressant, since it is a weak inhibitor of both dopamine
and norepinephrine neuronal reuptake. However,
its actual antidepressant activity is not well understood.
Bupropion is generally well tolerated and does
not block muscarinic, histaminergic, or adrenergic receptors.
Unlike the SSRIs and venlafaxine, bupropion
does not cause sexual side effects. However, it can cause
CNS stimulation, including restlessness and insomnia.
High doses of bupropion, given as its original formulation,
were associated with a risk of seizures in 0.4% of
patients. However, this risk is lower with slow-release
bupropion (Wellbutrin SR). This formulation still requires
dosing twice a day, and bupropion is contraindicated
in patients with a history of seizures. Bupropion
inhibits the cytochrome P450 2D6 isoenzyme and may
elevate blood levels of drugs metabolized by this route.
一般的な説明
The mechanism of action of bupropion (Wellbutrin) is consideredcomplex and reportedly involves a block of DA reuptakevia the dopamine transporter (DAT), but the overallantidepressant action is noradrenergic. A metabolite thatcontributes to the overall action and its formation can beeasily rationalized. Oxidation of one of the methyl groupson the t-butyl substituent yields hydroxybupropion, an activemetabolite. Reduction of the keto group also occurs,yielding threohydrobupropion and erythrohydrobupropion.Both of these metabolites are also active.
Hydroxybupropion is half as potent as the parent bupropion,and the hydrobupropion isomers are five times less potent.The presence of these metabolites, especially hydroxybupropionwhich is formed by cytochrome P450 2D6(CYP2D6), suggests that there will be a myriad of drug interactionswith bupropion.
薬理学
Bupropion is an α-aminoketone that is structurally related to amphetamines, and it exhibits
unique activity comparable to that of other antidepressants. It is believed that bupropion
restores the total amount of norepinephrine in the body. This compound is a poor reuptake
inhibitor of dopamine, and does not exhibit anticholinergic activity or inhibit MAO. Its
efficacy as an antidepressant is comparable to that of tricyclic antidepressants, and as a
serotonin uptake inhibitor it is comparable to fluoxetine.
ブプロピオン 上流と下流の製品情報
原材料
準備製品