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Trazodone

(Synonyms: AF-1161) 目录号 : GC26002

Trazodone (AF-1161) is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders.

Trazodone Chemical Structure

Cas No.:19794-93-5

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产品描述

Trazodone (AF-1161) is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders.

Chemical Properties

Cas No. 19794-93-5 SDF Download SDF
别名 AF-1161
分子式 C19H22ClN5O 分子量 371.86
溶解度 DMSO: 45 mg/mL (121.01 mM);Water: Insoluble;Ethanol: 17 mg/mL (45.72 mM) 储存条件 Store at -20°C
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1 mM 2.6892 mL 13.4459 mL 26.8918 mL
5 mM 0.5378 mL 2.6892 mL 5.3784 mL
10 mM 0.2689 mL 1.3446 mL 2.6892 mL
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Research Update

Treatment of insomnia - effect of Trazodone and hypnotics on sleep

Psychiatr Pol 2021 Aug 31;55(4):743-755.PMID:34994734DOI:10.12740/PP/125650.

Sedative antidepressants are commonly used drugs in the treatment of insomnia. However, some recommendations claim that only hypnotics have been proven effective in the treatment of sleep initiation and maintenance disorders. The aim of this article is to compare the effect of hypnotics and Trazodone on sleep, and to analyse the evidence for the use of Trazodone in the treatment of insomnia. Three studies investigated the effects of Trazodone on sleep in primary insomnia, 5 studies on insomnia in the course of affective disorders and 6 studies on insomnia in other indications (PTSD, Alzheimer's disease, alcohol and opiate dependence, somatoform disorder, and insomnia during pregnancy). In the treatment of insomnia, Trazodone is less effective than hypnotics in the treatment of sleep onset insomnia (i.e., disorders of falling asleep). For this indication it needs to be administered earlier than hypnotics, at least 1 hour before bedtime. It is, however, very effective in the treatment of sleep-maintenance insomnia, especially in patients with comorbid mental disorders or patients treated with activating antidepressants. Hypnotics and Trazodone have the opposite effect on deep sleep. Trazodone increases the duration of deep sleep, which is associated with better sleep quality as assessed by patients. In contrast, hypnotics decrease slow-wave activityin sleep EEG, which is the biomarker of deep sleep. The main mechanism through which Trazodone promotes sleep is its antagonistic effect on 5-HT2 serotonin receptors, while hypnotics are agonists of gamma-aminobutyric acid GABAA receptors, and other sedative antidepressants block H1 histamine receptors. This is associated with a low risk of weight gain, which is rare with Trazodone treatment.

A review of Trazodone use in psychiatric and medical conditions

Postgrad Med 2017 Jan;129(1):140-148.PMID:27744763DOI:10.1080/00325481.2017.1249265.

Trazodone is an antidepressant that is FDA-approved for the treatment of depression. It has been used by mental health and primary care providers for the treatment of multiple psychiatric and medical conditions .This review describes Trazodone mechanism of action, formulation, dosage and adverse effects and then summarizes the beneficial effects of Trazodone in the treatment of various psychiatric and medical conditions such as major depression, as well non-approved FDA indications such as insomnia,anxiety disorders, posttraumatic stress disorder, obsessive compulsive disorder, feeding and eating disorders, substance use disorders, behavioral disturbances associated with cognitive dysfunction, sexual dysfunction, certain pain conditions, and rehabilitation after acute ischemic stroke. Despite Trazodone's favorable effects in the treatment of FDA-unapproved psychiatric and medical conditions, large, randomized controlled clinical trials are still needed to confirm its efficacy in the treatment of the multiple conditions for which it is often used in clinical practice.

The effects of Trazodone on human cognition: a systematic review

Eur J Clin Pharmacol 2021 Nov;77(11):1623-1637.PMID:34097124DOI:10.1007/s00228-021-03161-6.

Trazodone is a widely used antidepressant that is also useful in the control of agitation and insomnia in Alzheimer's disease. This drug is now recognized as having a new mechanism of action, an effect on the unfolded protein response (UPR) pathway, restoring protein translation and slowing neurodegenerative progression in mice. This mechanism may have a role in dementia-modifying treatment. To explore the effects of Trazodone on human cognition and to search for clinical evidence of its putative benefits in human neurodegenerative diseases, a systematic review was conducted for studies that evaluated the effect of a minimum dose of 25 mg of Trazodone daily, for at least 1 week, on cognition in adult humans. The search was run in MEDLINE, Web of Science, and CENTRAL from the Cochrane databases, yielding a total of 16 studies after selection. Overall, seven studies showed no effect of Trazodone on cognition, five showed a beneficial effect by improving or reducing cognitive decline, and four evidenced impaired cognitive function. Our analysis highlights the possibility of a dose-independent dual effect of Trazodone on human cognition, with acute utilization associated with impaired cognitive function and long-term use with preventing cognitive deterioration. There was no clinical evidence that Trazodone could be used as a specific treatment of neurodegenerative diseases. Future studies should explore the role of Trazodone in the UPR pathway and the implications in neurodegenerative diseases in humans.

Rediscovering Trazodone for the treatment of major depressive disorder

CNS Drugs 2012 Dec;26(12):1033-49.PMID:23192413DOI:10.1007/s40263-012-0010-5.

Trazodone is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). The drug is approved and marketed in several countries worldwide for the treatment of major depressive disorder (MDD) in adult patients. In clinical studies, Trazodone has demonstrated comparable antidepressant activity to other drug classes, including tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs) and serotonin-noradrenaline (norepinephrine) reuptake inhibitors (SNRIs). Moreover, the SARI action of Trazodone may overcome the tolerability issues that are often associated with second-generation antidepressants such as SSRIs (i.e. insomnia, anxiety and sexual dysfunction). Recent focus has been placed on the development of a new prolonged-release once-a-day formulation of Trazodone (TzCOAD), which may provide improved tolerability over the conventional immediate-release formulation of Trazodone. Clinical studies have led to the recent approval in the USA of TzCOAD (as Oleptro™; Angelini Labopharm LLC, Princeton, NJ, USA), which may see resurgence of interest in the drug for the management of patients with MDD. Although Trazodone is approved for the treatment of depression, evidence supports the use of low-dose Trazodone as an off-label hypnotic for the treatment of sleep disorders in patients with MDD. The most common adverse effects reported with Trazodone are drowsiness (somnolence/sedation), headache, dizziness and dry mouth. Other events reported, albeit with low incidence, include orthostatic hypotension (particularly in elderly patients or those with heart disease), minimal anticholinergic activity, corrected QT interval prolongation and torsade de pointes, cardiac arrhythmias, and rare occurrences of priapism and suicidal ideation. Overall, Trazodone is an effective and well tolerated antidepressant (SARI) with an important role in the current treatment of MDD both as monotherapy and as part of a combination strategy. Trazodone is effective in controlling a wide range of symptoms of depression, while avoiding the negative effects on sleep seen with SSRI antidepressants. The recently approved prolonged-release formulation should provide further optimization of this antidepressant and may be useful for enabling an appropriate therapeutic dose to be administered with improved patient compliance.

Off-Label Trazodone Prescription: Evidence, Benefits and Risks

Curr Pharm Des 2015;21(23):3343-51.PMID:26088119DOI:10.2174/1381612821666150619092236.

Although Trazodone is approved and marketed in most countries worldwide for the sole treatment of Major Depressive Disorder, the use for this medication is very common for many other conditions, such as primary or secondary insomnia, Generalised Anxiety Disorder, Panic Disorder, Post-Traumatic Stress Disorder and Obsessive- Compulsive Disorder. Other, not officially approved, uses of Trazodone include: the treatment of bulimia, benzodiazepine and/or alcohol dependence or abuse, fibromyalgia, degenerative diseases of the central nervous system such as dementia and other organic disorders, schizophrenia, chronic pain, and diabetic neuropathy. In addition, due to its 5HT2A receptor antagonistic action, Trazodone may be used to prevent the occurrence of initial and long-term side effects of SSRI, such as anxiety, insomnia and sexual dysfunction. Despite the favorable clinical experience and the encouraging results from the studies that have tested the efficacy of Trazodone for some of its off-label indications, it is paramount that large, randomized and controlled clinical trials be conducted in the near future to evaluate which of the many off-label indications are supported by a strong scientific evidence.