Carvedilol: Difference between revisions
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{{MedTemplate | {{MedTemplate | ||
| generic = Carvedilol | | generic = Carvedilol | ||
| brand | | brand = Coreg, Coreg CR | ||
| classes = Beta blocker | | structure = | ||
| | | classes = [[:Category:Beta blockers|Beta blocker (non-selective, with alpha-1 antagonism)]], [[:Category:Antihypertensives|Antihypertensive]], [[:Category:Heart failure medicines|Heart failure medicine]] | ||
| uses = <vote slug="heart-failure-reduced-ef-use">Heart failure with reduced ejection fraction (FDA; foundational guideline-directed medical therapy)</vote>, <vote slug="post-mi-lv-dysfunction-use">Left ventricular dysfunction after myocardial infarction (FDA)</vote>, <vote slug="hypertension-use">Hypertension (FDA)</vote>, <vote slug="angina-use">Stable angina (off-label)</vote> | |||
| 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) | |||
| fda_max = 50 mg BID in heart failure (or once-daily equivalent CR); 25 mg BID in hypertension | |||
| pill_id = | |||
| routes = Oral | |||
| onset = Antihypertensive effect within 1 week; heart-failure mortality benefit accrues over months of titration | |||
| duration = ~12 hours (IR); 24 hours (CR) | |||
| halflife = 7-10 hours<ref name="coreg-label">FDA Prescribing Information, Coreg (carvedilol), GSK/Woodward, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020297s039lbl.pdf</ref> | |||
| bioavailability = ~25-35% (extensive first-pass), increased by food which slows absorption and reduces orthostatic risk<ref name="coreg-label" /> | |||
| pregnancy = Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.{{citation needed}} | |||
| legal = [[USLegal:Prescription only|Rx-only]] in US | |||
| mechanism = <vote slug="carvedilol-mech-claim">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.</vote> CYP2D6 metabolism produces stereoselective clearance; CYP2D6 poor metabolizers have higher plasma exposure and may need lower doses<ref name="coreg-label" />. | |||
}} | }} | ||
== References == | |||
<references /> | |||
[[Category:Beta blockers]] | |||
[[Category:Antihypertensives]] | |||
[[Category:Heart failure medicines]] | |||