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Cimetidine

TAGAMET

What it isH2 receptor antagonist suppressing gastric acid; GERD and ulcer disease.

Why this oneIts antiandrogen action can cause gynecomastia, a peculiar liability not shared by famotidine.

What limits itIt inhibits multiple CYP enzymes and tubular creatinine secretion, creating interactions and a false creatinine rise; famotidine has replaced it.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Heartburn relief (OTC)Adults & children ≥12 yr200 mg (1 tablet) with water PRN200 mg PRN2 tablets/24h
Heartburn prevention (OTC)Adults & children ≥12 yr200 mg (1 tablet) up to 30 min before trigger food/drink200 mg PRN2 tablets/24h

Renal Undefined

Hepatic Undefined

Instructions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskInhibits four CYP enzymes; famotidine has replaced it

Cost, est. cash$20–$1,500/dose or month

Generic entry1994

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryB

Defining liabilityLong-term infection, magnesium/B12 and bone risks; selected agents have clinically important CYP interactions.

Mechanism of action: Cimetidine ballicule

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

Open Cimetidine in the interactive console ↗

Memory aids: mascots and interaction avatars

Cimetidine TAGAMET mascot mnemonic cartoon
“Cy, Tag a Met”
Cimetidine (left) increases levels of metformin (Mr Met, right)
Cimetidine CYP1A2 inhibitor avatar
CYP1A2 inhibitor (moderate)
Cimetidine CYP2C19 inhibitor avatar
CYP2C19 inhibitor (moderate)
Cimetidine CYP3A4 inhibitor avatar
CYP3A4 inhibitor (weak)
Cimetidine OCT2/MATE1 inhibitor avatar
OCT2/MATE1 inhibitor

Open Cimetidine in the interactive console ↗