Carvedilol
Carvedilol
Coreg, Coreg CR
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Summary
Classes
Common uses
Heart failure with reduced ejection fraction (FDA; foundational guideline-directed medical therapy)0, Left ventricular dysfunction after myocardial infarction (FDA)0, Hypertension (FDA)0, Stable angina (off-label)0
Pharmacy
Starting dose
Heart failure: 3.125 mg PO BID, doubling every 2 weeks as tolerated to target 25 mg BID (50 mg BID if >85 kg). Hypertension: 6.25 mg PO BID, titrate to 25 mg BID
Preparations
IR tablets 3.125, 6.25, 12.5, 25 mg; Coreg CR capsules 10, 20, 40, 80 mg (once-daily)
US FDA Max
50 mg BID in heart failure (or once-daily equivalent CR); 25 mg BID in hypertension
Pharmacology
Routes
Oral
Onset
Antihypertensive effect within 1 week; heart-failure mortality benefit accrues over months of titration
Duration
~12 hours (IR); 24 hours (CR)
Half-life
7-10 hours[1]
Bioavailability
~25-35% (extensive first-pass), increased by food which slows absorption and reduces orthostatic risk[1]
Pregnancy
Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Non-selective β1/β2-adrenergic receptor antagonist with additional α1-adrenergic antagonism, giving combined heart-rate-and-contractility blunting plus peripheral vasodilation. The α1 blockade and ancillary antioxidant activity distinguish carvedilol from cardioselective β-blockers, and explain its strong mortality benefit in heart failure with reduced ejection fraction shown in COPERNICUS, CAPRICORN, and US Carvedilol Heart Failure Trials.0 CYP2D6 metabolism produces stereoselective clearance; CYP2D6 poor metabolizers have higher plasma exposure and may need lower doses[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Coreg (carvedilol), GSK/Woodward, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020297s039lbl.pdf