Doxepin low-dose (insomnia)

SILENOR

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Pronunciation: DOX-e-pin

Doxepin low-dose (insomnia) ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Doxepin low-dose (insomnia) ballicule

Doxepin low-dose (insomnia) SINEQUAN, SILENOR mascot mnemonic cartoon — Visual mnemonic: Doxepin low-dose (insomnia) mascot
**“Box with pins”**

What it isLow-dose doxepin 3/6 mg, a tricyclic whose H1 antagonism treats sleep-maintenance insomnia.

Why this oneAt insomnia exposure it acts mainly as an antihistamine, with less antimuscarinic burden than antidepressant-dose doxepin.

What limits itNext-day sedation and additive CNS depression can impair driving; the antidepressant suicidality warning remains.

Doxepin low-dose (insomnia) molecular structure (skeletal formula) — Molecular structure: Doxepin low-dose (insomnia)

FDA-approved for

insomnia (sleep maintenance) (2010)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Insomnia (sleep maintenance)	Adults	6 mg once daily (3 mg may be appropriate)	6 mg QHS	6 mg/day
Insomnia (sleep maintenance)	Elderly (≥65 y)	3 mg once daily	3 mg QHS (may increase to 6 mg)	6 mg/day

Renal Undefined (not studied; not expected to significantly alter concentrations)

Hepatic Initiate at 3 mg (hepatic impairment); monitor for daytime effects

Instructions

Take within 30 minutes of bedtime
Do not take within 3 hours of a meal
Total dose should not exceed 6 mg/day
With cimetidine, max dose 3 mg

Available strengths

tab 3, 6 mg
cap 10, 25, 50, 75, 100, 150 mg
sol 10 mg/mL
cream 5 %

Contraindications

Co-administration with monoamine oxidase inhibitors (MAOIs) — do not administer if taking MAOIs or used within the past two weeks
Untreated narrow angle glaucoma or severe urinary retention

Cautions

Evaluate for comorbid diagnoses if insomnia persists after 7-10 days
Abnormal thinking/behavioral changes including sleep-driving and hallucinations
Worsening of depression or suicidal thinking
CNS-depressant effects; avoid hazardous activities; do not use with alcohol
Additive effects with CNS depressants/sedating antihistamines
Not recommended in severe sleep apnea

Adverse reactions

Somnolence/sedation
Nausea
Upper respiratory tract infection/nasopharyngitis

Pregnancy Epidemiologic data have not established increased risk of major birth defects; third-trimester TCA exposure risks poor neonatal adaptation

Lactation Doxepin present in human milk; excess sedation, respiratory depression, hypotonia reported — breastfeeding not recommended

Cost

Doxepin low-dose (insomnia) (SILENOR)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	CostPlus
3 mg	tab	30 qd	$40	offered
6 mg	tab	30 qd	$41.15	offered

Other forms: Doxepin (SINEQUAN)

⚠ BOXED WARNING

Suicidal thoughts and behaviors in patients under 25

Classes and tags

Clinical profile

Direct muscarinic antagonism3 / 4

Serotonicity

This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.

Predominantly antihistaminic at usual doses; negligible clinically meaningful SRI activity.

Label contraindicationCo-administration with monoamine oxidase inhibitors (MAOIs) — do not administer if taking MAOIs or used within the past two weeks. The label governs prescribing; Gillman’s point concerns serotonin toxicity only.

It binds the serotonin transporter, and its SERT peg is drawn to that textbook affinity. The pale halo around the peg marks binding that, by Gillman’s human-effect criteria, does not produce clinical serotonin reuptake inhibition.

Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.