Doxepin (Silenor, Sinequan)

Class

Tricyclic antidepressant (TCA)

Mechanism

Inhibits reuptake of serotonin and norepinephrine; at lower doses, acts as a potent H1 histamine receptor antagonist with minimal anticholinergic effects.

FDA-Approved Use

Major depressive disorder (MDD), anxiety disorders, insomnia (low-dose formulation for sleep maintenance).

Off-Label Use

Chronic urticaria, pruritus, post-traumatic stress disorder (PTSD), augmentation in depression, post-stroke depression (PSD)

Formulation

Oral tablets, capsules, solution; low-dose formulation (Silenor) for insomnia.

Titration

For depression/anxiety, 25–50 mg p.o. daily, divided BID or taken at bedtime; titrate to 75–300 mg/day as tolerated. For insomnia, 3–6 mg nightly (FDA-approved) or off-label 10–25 mg p.o. nightly.

Dose Range

75–300 mg/day for mood and anxiety; 3–25 mg/day for sleep or pruritus.

Kinetics

Metabolized by CYP2C19 and CYP2D6; half-life 8–24 hours depending on dose and formulation.

Common AEs

Sedation, dry mouth, constipation, blurred vision, dizziness, weight gain.

Serious/Rare AEs

Cardiac arrhythmias, orthostatic hypotension, urinary retention, cognitive impairment, overdose toxicity.

Monitoring

Baseline ECG in patients over 40 or with cardiac risk factors; monitor orthostasis and anticholinergic burden.

Black Box Warning

Increased risk of suicidal ideation in children, adolescents, and young adults.

Considerations

Low-dose doxepin is often better tolerated in older adults with insomnia due to reduced anticholinergic effects. Higher doses should be avoided in patients with dementia, traumatic brain injury (TBI), or significant cognitive impairment due to sedation, fall risk, and delirium potential. ECG monitoring is advised in older or cardiac patients before initiating high-dose therapy.