トラゾドン 化學(xué)特性,用途語,生産方法
効能
トランキライザー, 抗うつ薬, セロトニン受容體拮抗?再取り込み阻害薬
化學(xué)的特性
Brown Oil
使用
It is believed that trazodone, in therapeutic doses, inhibits the neuronal reuptake of serotonin. It is not a MAO inhibitor or a CNS stimulator. It has a minor influence on the reuptake of norepinephrine and dopamine. In addition, it does not bind with cholinergic or
α-adrenergic receptors.
適応癥
Trazodone (Apothecon) is also classified as an antidepressant
agent. It is a selective serotonin reuptake inhibitor
(SSRI), partial agonist at postsynaptic 5-HT1A
receptors, and exhibits α-adrenoceptor blocking actions.
Trazodone may cause priapism and enhance libido,
and it prolongs nocturnal erections. This drug has been
used both orally and by intracavernosal injection. It can
be used alone or in combination with yohimbine.
Overall, trazodone has not been as effective in treating
ED as other available agents. However, it may be an option
for selected patients, particularly those with performance
anxiety or low libido.
定義
ChEBI: An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.
世界保健機(jī)関（WHO）
Trazodone, an antidepressant indicated for the treatment of a
wide range of depressive illness, was introduced in 1973. Although it is registered
for use in many countries with highly evolved regulatory authorities, approval for
registration was not granted in Norway because of a suspicion of carcinogenicity
in a two-year rat study.
生物學(xué)の機(jī)能
Trazodone (Desyrel) was introduced in the early 1980s
as a second-generation antidepressant. It blocks the
neuronal reuptake of serotonin and is an antagonist at
the 5HT2-receptor. Also, its major metabolite, mchlorophenylpiperazine
(mCPP), is a postsynaptic serotonin
receptor agonist. When compared to the TCAs,
trazodone is relatively free of antimuscarinic side effects,
but it does block the α-adrenoceptor. Common
side effects include marked sedation, dizziness, orthostatic
hypotension, and nausea. Priapism is
an uncommon but serious side effect requiring surgical
intervention in one-third of the cases reported. Because
of trazodone’s sedating quality, it is often used in low
doses to counter the insomnia associated with the
newer antidepressants, such as the SSRIs.
臨床応用
Trazodone is a phenylpiperazine–triazolopyridine antidepressant that is structurally unrelated to most of the
other antidepressant classes.Trazodone is used primarily in the treatment of insomnia, mental depression, or depression/anxiety disorders.
The drug also has shown some efficacy in the treatment of benzodiazepine or alcohol dependence, diabetic
neuropathy, and panic disorders.
薬物相互作用
Trazodone possesses serotonergic activity; therefore, the possibility of developing 5-HT syndrome should be
considered in patients who are receiving trazodone and other SSRIs or serotonergic drugs concurrently.
When trazodone is used concurrently with drugs metabolized by CYP3A4, caution should be used to avoid
excessive sedation. Trazodone can cause hypotension, including orthostatic hypotension and syncope;
concomitant administration of antihypertensive therapy may require a reduction in dosage of the
antihypertensive agent.
トラゾドン 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品