Investigational Drug Details
| Drug ID: | D186 |
| Drug Name: | Trazodone |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00656 |
| DrugBank Description: | Trazodone is triazolopyridine derivative from the serotonin receptor antagonists and reuptake inhibitors (SARIs) class of antidepressants.[A181180] It is used in adults and has been shown to be comparable in efficacy to other drugs such as tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), and serotonin-norepinephrine receptor inhibitor (SNRIs) in the treatment of depression.[T646] A unique feature of this drug is that it does not promote the anxiety symptoms, sexual symptoms, or insomnia, which are commonly associated with SSRI and SNRI therapy.[T646] Trazodone acts on various receptors, including certain histamine, serotonin, and adrenergic receptors, distinguishing it from other antidepressants that cover a narrow range of neurotransmitters.[T646] It was initially granted FDA approval in 1981.[L3484] |
| PubChem ID: | 5533 |
| CasNo: | 19794-93-5 |
| Repositioning for NAFLD: | Yes |
| SMILES: | ClC1=CC=CC(=C1)N1CCN(CCCN2N=C3C=CC=CN3C2=O)CC1 |
| Structure: |
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| InChiKey: | PHLBKPHSAVXXEF-UHFFFAOYSA-N |
| Molecular Weight: | 371.864 |
| DrugBank Targets: | 5-hydroxytryptamine receptor 2A; 5-hydroxytryptamine receptor 2C; Sodium-dependent serotonin transporter; 5-hydroxytryptamine receptor 1A; Histamine H1 receptor; Alpha-1A adrenergic receptor; Alpha-2A adrenergic receptor; 5-hydroxytryptamine receptor 1C |
| DrugBank MoA: | The mechanism of action of trazodone is not fully understood, however, it is known to inhibit the reuptake of serotonin and block both histamine and alpha-1-adrenergic receptors.[T646] Despite the fact that trazodone is frequently considered a selective serotonin reuptake inhibitor, several reports have shown that other mechanisms including antagonism at serotonin 5-HT1a, 5-HT1c, and 5-HT2 receptor subtypes may occur.[A181177,T646] The strongest antagonism of trazodone is reported to occur at the serotonin 5-HT21c receptors, preventing serotonin uptake.[A985] In addition to acting on serotonin receptors, trazodone has been shown to inhibit serotonin transporters.[A4334,A181457] The antidepressant effects of trazodone result from the inhibition of receptor uptake, which normally decreases circulating neurotransmitters, contributing to depressive symptoms.[A181186,A175840] |
| DrugBank Pharmacology: | Trazodone treats depressed mood and other depression-related symptoms and shows benefit in the treatment of insomnia due to its sedating effects.[T646] It is known to prolong the cardiac QT-interval.[L3484] Memory, alertness, and cognition may be decreased by trazodone, especially in elderly patients due to its central nervous system depressant effects.[A181177] A note on priapism Trazodone has been associated with the occurrence of priapism, a painful and persistent incidence of penile tissue erection that is unrelievable and can cause permanent neurological damage if left untreated. Patients must be advised to seek immediate medical attention if priapism is suspected.[A181198,L3484] |
| DrugBank Indication: | Trazodone is indicated for the treatment of major depressive disorder (MDD).[L3484] It has been used off-label for adjunct therapy in alcohol dependence, and off-label to treat anxiety and insomnia.[L3484] It may also be used off-label to treat symptoms of dementia, Alzheimer’s disease, schizophrenia, eating disorders, and fibromyalgia due to its effects on various neurotransmitter receptors.[A31634] |
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| Therapeutic Category: | |
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| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L3261 | NCT01019486 | PHASE4 | COMPLETED | YES | 2009-11 | 2015-12-14 | Details |
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