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Clorazepate

TRANXENE

What it isLong-acting benzodiazepine prodrug converted to desmethyldiazepam; anxiety and alcohol withdrawal.

Why this oneGastric acid drives the conversion, giving a smooth onset and a long tail.

What limits itAccumulates in the elderly and in liver disease. Dependence as for the class; antacids blunt conversion.

FDA-approved for

FDA label

BOXED WARNING Concomitant use with opioids: profound sedation, respiratory depression, coma, death. Benzodiazepine abuse, misuse, and addiction (overdose/death). Physical dependence; abrupt discontinuation or rapid dose reduction can cause life-threatening withdrawal.
FDA dosingPopulationStartTargetMax
AnxietyAdult30 mg/day divided (or 15 mg QHS single dose)15-60 mg/day
AnxietyElderly/debilitated7.5-15 mg/dayindividualized
Acute alcohol withdrawalAdultDay 1: 30 mg, then 30-60 mg dividedTaper: Day 2 45-90 mg, Day 3 22.5-45 mg, Day 4 15-30 mg, then 7.5-15 mg90 mg/day
Adjunct to antiepileptic drugsAdult / >12 yr7.5 mg TIDincrease <=7.5 mg/week90 mg/day
Adjunct to antiepileptic drugsChildren 9-12 yr7.5 mg BIDincrease <=7.5 mg/week60 mg/day

Titration Epilepsy adjunct: increase by no more than 7.5 mg per week

Renal Undefined

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Undefined

Lactation Undefined

⚠ BOXED WARNINGS

Cost, est. cash$10–$300/month

Generic entry1987

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySedation, falls, dependence and additive respiratory depression with opioids or other CNS depressants.

Active metabolites

Mechanism of action: Clorazepate ballicule

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

Open Clorazepate in the interactive console ↗

Memory aids: mascots and interaction avatars

Clorazepate TRANXENE mascot mnemonic cartoon
“(Cloraze)peyton Trancing”
hot pink → benzo theme
Clorazepate CYP3A4 substrate avatar
CYP3A4 substrate

Open Clorazepate in the interactive console ↗