Тразодон

Химические свойства

Brown Oil

Использование

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.

Показания

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.

Определение

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.

Всемирная организация здравоохранения(ВОЗ)

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.

Биологические функции

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.

Клиническое использование

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.

взаимодействия лекарств

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.