Trazodone
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| Trade names | Many brand names worldwide |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a681038 |
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| Routes of administration |
By mouth (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | 65% (Oral) |
| Protein binding | 89–95% |
| Metabolism | Hepatic (CYP3A4) |
| Onset of action | 1 hour (oral) |
| Biological half-life | 7 hours (immediate-release), 10 hours (extended-release) |
| Excretion | Urine (70–75%), feces (21%) |
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| ECHA InfoCard | 100.039.364 |
| Chemical and physical data | |
| Formula | C19H22ClN5O |
| Molar mass | 371.8641 g/mol |
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Trazodone (sold under many brand names worldwide) is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects. Its side-effect profile and potential toxicity are considerably different from those of the original antidepressants (i.e., the monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants (TCAs)).
The primary use of trazodone is the treatment of major depression. Data from open and double-blind trials suggest the antidepressant efficacy of trazodone is comparable to that of amitriptyline, doxepin, and mianserin. Also, trazodone showed anxiolytic properties, low cardiotoxicity, and relatively mild side effects. Because trazodone has minimal anticholinergic activity, it was especially welcomed as a treatment for geriatric patients with depression when it first became available. Three double-blind studies reported trazodone has antidepressant efficacy similar to that of other antidepressants in geriatric patients. However, a side effect of trazodone, orthostatic hypotension, which may cause dizziness and increase the risk of falling, can have devastating consequences for elderly patients; thus, this side effect, along with sedation, often makes trazodone less acceptable for this population, compared with newer compounds that share its lack of anticholinergic activity but not the rest of its side-effect profile. Still, trazodone is often helpful for geriatric patients with depression who have severe agitation and insomnia. Trazodone has also been reported to have antianxiety properties. In a randomized, double-blind, placebo-controlled trial, the anxiolytic efficacy of trazodone was comparable to that of diazepam in weeks 3–8 of treatment for generalized anxiety disorder, although patients treated with diazepam had greater improvement during the first 2 weeks of treatment. Early case reports had indicated that trazodone is associated with improvement in obsessive-compulsive disorder, but a double-blind, placebo-controlled study found that trazodone lacked antiobsessional effects. Many clinicians use low-dose trazodone as an alternative to benzodiazepines for the treatment of insomnia. Two recent reviews found that trazodone is the second most prescribed agent for insomnia, but as most studies have been limited to patients with depression, few studies actually support trazodone's use in primary insomnia.
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