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Carvedilol

COREG

What it isBeta-1, beta-2 and alpha-1 antagonist; systolic heart failure and hypertension.

Why this oneCombined beta and alpha-1 blockade gives heart-failure survival benefit plus vasodilation, but more orthostasis than beta-1-selective agents.

What limits itTake with food to limit orthostasis. Bradycardia and hypotension limit it; nonselective beta blockade can provoke bronchospasm.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Heart failureAdults3.125 mg BIDup to 25 mg BID (50 mg BID if >85 kg)50 mg BID (>85 kg)
LV dysfunction after MIAdults6.25 mg BID (3.125 mg BID if needed)25 mg BID
HypertensionAdults6.25 mg BID12.5–25 mg BID50 mg/day

Titration Heart failure: increase at intervals ≥2 weeks; post-MI: after 3–10 days; hypertension: over 7–14 days per step

Renal Undefined

Hepatic Contraindicated in severe hepatic impairment

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Insufficient data; third-trimester beta-blocker use may cause neonatal hypotension, bradycardia, hypoglycemia, respiratory depression

Lactation No human data; present in rat milk — weigh benefits vs. risk

NO BOXED WARNINGS

Principal riskBradycardia and orthostatic hypotension

Cost, est. cash$10–$300/month

Generic entry2017

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger3 / 4
Weight-gain liability1 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityBradycardia, hypotension and worsening heart failure during titration; overdose can cause shock.

Mechanism of action: Carvedilol ballicule

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

Open Carvedilol in the interactive console ↗

Memory aids: mascots and interaction avatars

Carvedilol COREG mascot mnemonic cartoon
“Corey the Carver”
Polka dots on pink → α1 blocker → syncope if titrated too quickly (hit the floor)
LOL hat → β blocker
Carvedilol CYP2D6 substrate avatar
CYP2D6 substrate

Open Carvedilol in the interactive console ↗