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Trazodone

Trazodone
Trazodone structure
CAS No.
19794-93-5
Chemical Name:
Trazodone
Synonyms
trazon;desyrel;TRAZODONE;trialodine;Trazodone-d6;Trazodone (base and/or unspecified salts);Trazodone Hydrochloride 2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-1,2,4-tri;2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-[1,2,4]triazolo[4,3-a]pyridin-3-one;2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-[1,2,4]triazolo[4,5-a]pyridin-3-one;1,2,4-Triazolo[4,3-a]pyridin-3(2H)-one,2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-
CBNumber:
CB3727463
Molecular Formula:
C19H22ClN5O
Formula Weight:
371.86
MOL File:
19794-93-5.mol

Trazodone Properties

Melting point:
86-870C
Boiling point:
528.5±60.0 °C(Predicted)
Density 
1.3141 (rough estimate)
refractive index 
1.5790 (estimate)
pka
pKa (50% ethanol): 6.14(at 25℃)
CAS DataBase Reference
19794-93-5(CAS DataBase Reference)
FDA UNII
YBK48BXK30
NCI Dictionary of Cancer Terms
trazodone
NIST Chemistry Reference
Desyrel(trazodone hcl salt)(19794-93-5)
EPA Substance Registry System
1,2,4-Triazolo[4,3-a]pyridin-3(2H)-one, 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]- (19794-93-5)
SAFETY
  • Risk and Safety Statements
RIDADR  3249
HazardClass  6.1(b)
PackingGroup  III

Trazodone Chemical Properties,Uses,Production

Chemical Properties

Brown Oil

Uses

Antidepressant

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.

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.

brand name

Beneficat;Bimaran;Deprax;Devidone;Manegan;Molipaxin;Pragmarel;Pragmazone;Taxagon;Thittico;Thombran;Thromban;Tombran;Tramensan;Tritico;Trittico.

World Health Organization (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.

Biological Functions

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.

Mechanism of action

Trazodone acts as an antagonist at 5-HT2A receptors and is a weak inhibitor of 5-HT reuptake at the presynaptic neuronal membrane, potentiating the synaptic effects of 5-HT. Its mechanism of action is complicated by the presence of its metabolite, m-chlorophenylpiperazine, which is a 5-HT2C agonist. At therapeutic dosages, trazodone does not appear to influence the reuptake of dopamine or NE within the CNS. It has little anticholinergic activity and is relatively devoid of toxic cardiovascular effects. The increase in serotonergic activity with long-term administration of trazodone decreases the number of postsynaptic serotonergic (i.e., 5-HT2) and β-adrenergic binding sites in the brains of animals, decreasing the sensitivity of adenylate (or adenylyl) cyclase to stimulation by β-adrenergic agonists. It has been suggested that postsynaptic serotonergic receptor modification is mainly responsible for the antidepressant action observed during long-term administration of trazodone. Trazodone does not inhibit MAO and, unlike amphetamine-like drugs, does not stimulate the CNS.
Trazodone is rapidly and almost completely absorbed from the GItract following oral administration, with an oral bioavailability of approximately 65%. Peak plasma concentrations of trazodone occur approximately 1 hour after oral administration when taken on an empty stomach or 2 hours when taken with food. At steady state, its plasma concentrations exhibit wide interpatient variation.
Trazodone is extensively metabolized in the liver by N-dealkylation to its primary active metabolite, m-chlorophenylpiperazine (m-CPP), which subsequently undergoes aromatic hydroxylation to p-hydroxy-m-CPP. In vitro studies indicate that CYP3A4 is the major isoform involved in the production of m-CPP from trazodone (and CYP2D6 to a lesser extent). The p-hydroxy-m-CPP and oxotriazolopyridine-propionic acid (the major metabolite excreted in urine) are conjugated with glucuronic acid. Less than 1% of a dose is excreted unmetabolized.

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.

Drug interactions

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.

Trazodone Preparation Products And Raw materials

Raw materials

Preparation Products


Trazodone Suppliers

Global( 85)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21837 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22625 55
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23977 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63728 58
CONIER CHEM AND PHARMA LIMITED
86-18523575427
sales@conier.com CHINA 47486 58
career henan chemical co
0086-371-86658258
0086-371-86658258 factory@coreychem.com CHINA 29643 58
Amadis Chemical Company Limited
0086-571-89925085
0086-571-89925065 sales@amadischem.com China 132149 58
Mainchem Co., Ltd. +86-0592-6210733
+86-0592-6210733 sale@mainchem.com CHINA 32444 55
LGM Pharma 1-(800)-881-8210
615-250-9817 inquiries@lgmpharma.com United States 1938 70
Nanjing Chemlin Chemical Co., Ltd 025-83697070
+86-25-83453306 info@chemlin.com.cn China 19991 64

View Lastest Price from Trazodone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-01-03 Trazodone
19794-93-5
US $7.00 / KG 1KG 99% 100KG Career Henan Chemical Co

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