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DERMATOLOGICALS › ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. › ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. › Other antipruritics
doxepin
D04AX01
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: Oral 75 mg to 150 mg daily in divided doses or as a single bedtime dose up to 300 mg/max daily
- Insomnia: Oral 3 mg to 6 mg once daily within 30 minutes of bedtime
- Pruritus: Topical 5% cream applied thinly QID with at least 3-4 hours between applications, max 8 days
Pediatric Dosing
- Depression/Anxiety (Children > 12 years): Oral initially 10 mg/kg/day up to 25-50 mg daily, titrated up to 100 mg/day
- Pruritus (Children < 18 years): Safety and efficacy of topical cream not established
Indications
- Major depressive disorder
- Psychoneurotic anxiety and depression
- Insomnia characterized by difficulty with sleep maintenance
- Pruritus associated with atopic dermatitis, lichen simplex chronicus, and eczema (topical)
Mechanism of Action
- Tricyclic antidepressant inhibiting serotonin and norepinephrine reuptake at neuronal synapses
- Potent antagonist at histamine H1 receptors, mediating sedative and antipruritic effects
- Antagonist at alpha-1 adrenergic, muscarinic (M1-M5), and serotonin (5-HT2) receptors
Contraindications
- Hypersensitivity to doxepin or other dibenzoxazepine derivatives
- Untreated narrow-angle glaucoma
- Severe urinary retention or tendency to urinary retention
- Concurrent use or within 14 days of monoamine oxidase inhibitors (MAOIs)
- Acute recovery phase post-myocardial infarction
Adverse Reactions
- Somnolence, sedation, fatigue, dizziness
- Anticholinergic effects: dry mouth, blurred vision, constipation, urinary retention
- Orthostatic hypotension, tachycardia, ECG changes (QT prolongation)
- Weight gain, increased appetite
- Application site burning or stinging (topical cream)
Drug Interactions
- MAOIs: risk of severe, potentially fatal serotonin syndrome or hypertensive crisis
- CNS depressants (alcohol, opioids, sedatives): enhanced sedation and respiratory depression
- CYP2D6 inhibitors (e.g., bupropion, fluoxetine): increased doxepin plasma concentrations and toxicity
- Anticholinergic agents: additive anticholinergic toxicity (paralytic ileus, confusion)
- QT-prolonging drugs: increased risk of ventricular arrhythmias
Curated Content: Needs Vetting Before Put to Clinical Use