Trazodon Chemische Eigenschaften,Einsatz,Produktion Methoden
Chemische Eigenschaften
Brown Oil
History
Trazodone was developed in Italy, in the 1960s, by Angelini Research Laboratories as a second-generation antidepressant. It was developed according to the mental pain hypothesis, which was postulated from studying patients and which proposes that major depression is associated with a decreased pain threshold. In sharp contrast to most other antidepressants available at the time of its development, trazodone showed minimal effects on muscarinic cholinergic receptors.
It was approved by the Food and Drug Administration (FDA) in 1981 and was the first non-tricyclic or MAOI antidepressant approved in the US. In 2023, it was the 21st most commonly prescribed medication in the United States and the fifth most common antidepressant, with more than 24 million prescriptions.
Verwenden
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.
Indications
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.
Definition
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.
Weltgesundheitsorganisation (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.
Biologische Funktion
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.
Clinical Use
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.
Arzneimittelwechselwirkung
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.
Trazodon Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
