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Diphenhydramine

BENADRYL

What it isFirst-generation H1 antagonist; allergy, insomnia, motion sickness and acute dystonia.

Why this oneIt reverses acute dystonic reactions within minutes and is available without prescription.

What limits itHeavy anticholinergic burden and sedation — it is on every deprescribing list for the elderly. Tolerance to the hypnotic effect is rapid.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Nighttime pain relief / sleep aid (OTC combination)Adults & children ≥12 yr2 caplets QHS2 caplets QHS2 caplets/24h

Renal Undefined

Hepatic Undefined

Instructions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskAnticholinergic burden; on every elderly deprescribing list

Cost, est. cash$10–$300/month

Generic entry1982

Classes and tags

Clinical profile

Therapeutic safety burden0 / 4
Overdose danger0 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism3 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryB

Defining liabilityLocal irritation, sensitization or administration-site injury; negligible systemic toxicity at usual use.

Mechanism of action: Diphenhydramine ballicule

Diphenhydramine ballicule: receptor binding, kinetics and half-life diagram

Open Diphenhydramine in the interactive console ↗

Memory aids: mascots and interaction avatars

Diphenhydramine BENADRYL mascot mnemonic cartoon
“Dippin’ hydra’s mean Bean drill”
“wears two hats” – max antihistamine and antimuscarinic
Diphenhydramine CYP2D6 substrate avatar
CYP2D6 substrate

Open Diphenhydramine in the interactive console ↗