Trazodone (Desyrel, Oleptro)

Class

Serotonin antagonist and reuptake inhibitor (SARI)

Mechanism

Inhibits serotonin reuptake and antagonizes 5-HT2A receptors; also blocks histamine H1 and alpha-1 adrenergic receptors, contributing to sedative and hypotensive effects

FDA-Approved Use

Major depressive disorder (MDD)

Off-Label Use

Insomnia (sleep onset and maintenance), agitation and behavioral disturbances in dementia

Formulation

Oral tablets (50 mg, 100 mg, 150 mg, 300 mg; immediate and extended-release)

Titration

25–50 mg p.o. nightly for sleep or agitation; may be titrated up to 150–400 mg/day for depression

Dose Range

150–400 mg/day for MDD; 25–150 mg/night for insomnia or behavioral symptoms

Kinetics

Half-life ~6–11 hours; metabolized via CYP3A4; active metabolite (mCPP) may contribute to serotonergic effects

Common AEs

Sedation, dizziness, dry mouth, orthostatic hypotension, headache, blurred vision

Serious/Rare AEs

Priapism, QTc prolongation, cardiac arrhythmia, serotonin syndrome (with other serotonergic agents)

Monitoring

Monitor for orthostatic hypotension, ECG in patients with cardiovascular risk, and signs of priapism or serotonin syndrome

Black Box Warning

Increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults with MDD and other psychiatric disorders

Considerations

Trazodone is frequently used off-label in older adults with dementia for insomnia and agitation, though its sedating and hypotensive effects increase fall risk. It may also be beneficial in managing sleep disturbances and behavioral symptoms in patients with post-stroke conditions or traumatic brain injury (TBI). In individuals with cardiovascular disease, use caution due to the potential for orthostatic hypotension and QTc prolongation. Combining trazodone with other central nervous system (CNS) depressants should be avoided unless clinically necessary.