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NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTIDEPRESSANTS › Non-selective monoamine reuptake inhibitors
doxepin
N06AA12
Forms & Strengths
- Capsules: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg
- Oral Concentrate: 10 mg/mL
- Cream (topical): 5%
Adult Dosing
- Depression/Anxiety: Initial 75 mg/day orally in divided doses or as single hs dose; titrate up to 150 mg/day (max 300 mg/day)
- Insomnia (low dose): 3 to 6 mg orally once daily within 30 minutes of bedtime
- Pruritus (topical): Apply thin film qid with at least 3-4 hours between applications, max 8 days
Pediatric Dosing
- Depression/Anxiety (Children < 12 years): Safety and efficacy not established
- Depression/Anxiety (Adolescents >= 12 years): Initial 25 to 50 mg/day orally; titrate up to 100 mg/day
Indications
- Major depressive disorder
- Anxiety neurosis
- Depression and/or anxiety associated with organic disease or alcoholism
- Insomnia characterized by difficulties with sleep maintenance
- Short-term management of moderate pruritus in adult patients with atopic dermatitis or lichen simplex chronicus
Mechanism of Action
- Tricyclic antidepressant that inhibits serotonin and norepinephrine reuptake at presynaptic neuronal membranes
- Potent antagonist at histamine H1 receptors, contributing to sedative effects
- Significant antagonist activity at alpha-1 adrenergic, muscarinic (M1-M5), and serotonin (5-HT2) receptors
Contraindications
- Hypersensitivity to doxepin or other dibenzoxepines
- Uncorrected narrow-angle glaucoma
- Severe urinary retention or risk of urinary retention
- Concurrent use with or within 14 days of MAOI therapy
- Acute recovery phase following myocardial infarction
Adverse Reactions
- Drowsiness, sedation, fatigue
- Anticholinergic effects: dry mouth, blurred vision, constipation, urinary retention
- Orthostatic hypotension, dizziness, tachycardia
- Weight gain, increased appetite
- Sexual dysfunction
Drug Interactions
- Monoamine Oxidase Inhibitors (MAOIs): risk of severe, potentially fatal serotonin syndrome or hypertensive crisis
- CNS depressants (alcohol, opioids, sedatives): enhanced CNS depression and sedation
- CYP2D6 and CYP2C19 inhibitors (e.g., fluoxetine, bupropion): may increase doxepin plasma concentrations
- Sympathomimetic agents: potential for enhanced cardiovascular effects such as arrhythmias or severe hypertension
- Anticholinergic drugs: additive anticholinergic toxicity including paralytic ileus and acute glaucoma
Curated Content: Needs Vetting Before Put to Clinical Use