Carvedilol
- Atc Codes:C07AG02
- CAS Codes:610309-89-2
- PHARMGKB ID:610309-89-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Carvedilol, Dilatrend; Belgium: Carvedilol, Dimitone, Kredex; Bulgaria: Atram, Avedol, Avernol, Carvedigamma, Carvedil, Carvedilol, Carvetrend, Carvilex, Coryol, Dilatrend; Cyprus: Avernol, Carvedilol, Carvepen, Dilatrend; Czech Republic: Apo-Carve, Atram, Carvedigamma, Carvedilol, Carvesan, Carvetrend, Coryol, Dilatrend, Talliton; Denmark: Carvedilol, Dimitone; Estonia: Atram, Avedol, Cardiostad, Carvedilol, Carvetrend, Coryol, Dilatrend; Finland: Cardiol, Carvedilol, Karvedilol; France: Carvedilol, Kredex; Germany: CarLich, Carve TAD, Carve-Q, Carvedigamma, Carvedilol, Dilatrend, Dimetil, Querto; Greece: Carvedilol, Carvepen, Coryol, Dilatrend, Hycal; Hungary: Atram, Carvedigamma, Carvedilol, Carvetrend, Carvol, Coryol, Dilatrend, Talliton; Ireland: Biocard, Carvedilol, Eucardic; Italy: Caravel, Carvedilolo, Carvipress, Colver, Curcix, Dilatrend, Omeria, Trakor; Latvia: Atram, Avedol, Cardiostad, Carloc, Carvedigamma, Carvedilol, Carvetrend, Coryol, Dilatrend, Karvidil; Lithuania: Atram, Avedol, Cardiostad, Carvedilol, Carvetrend, Coryol, Dilatrend, Talliton; Luxembourg: Kredex; Malta: Biocard, Carvedilol, Eucardic; Netherlands: Carvedilol, Eucardic; Poland: Atram, Avedol, Carvedigamma, Carvedilol, Carvetrend, Carvewin, Carvilex, Coryol, Dilatrend, Hypoten, Symtrend; Portugal: Carbetesil, Carvedilol, Dibloc; Romania: Atram, Carvedigamma, Carvedilol, Coryol, Dilatrend, Gladycor, Kallidol, Miocarvil, Talliton; Slovakia: Atram, Avedol, Carvedigamma, Carvedilol, Coryol, Dilatrend, Talliton; Slovenia: Carvedigamma, Carvetrend, Coryol, Dilatrend; Spain: Carvedilol, Coropres; Sweden: Carvanja, Carvedilol, Carveratio, Carvsanna, Karveacta, Karvedilol, Kravol, Kredex, Symtrend; UK: Eucardic.
North America
Canada: Carvedilol; USA: Carvedilol, Coreg.
Latin America
Argentina: Antibloc, Bidecar, Cardionorm, Carvedil, Carvedilol, Corafen, Coritensil, Corubin-Lazar, Dicarpen, Dilatrend, Duobloc, Filten, Hipoten Klonal, Isobloc, Kollosteril, Nexocardil, Pluscor-Sandoz, Rodipal, Rudoxil, Veraten, Vicardol; Brazil: Cardilol, Carvedilat, Carvedilol, Coreg, Divelol, Ictus, Karvil.
Asia
Japan: Anisto, Artione, Artist, Atenote, Carvedilol.
Drug combinations
Carvedilol and Hydrochlorothiazide
Chemistry
Carvedilol Phosphate: C~24~H~26~N~2~O~4~ H~3~O~4~P ½H~2~O. Mw: 513.48. 2-Propanol, 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-, phosphate (salt), hydrate (2:2:1). CAS-610309-89-2 (2004).
Pharmacologic Category
Sympatholytic (Adrenergic Blocking) Agents; Selective α-Adrenergic Blocking Agents. Cardiovascular Drugs; α-Adrenergic Blocking Agents; β-Adrenergic Blocking Agents. (ATC-Code: C07AG02).
Mechanism of action
Nonselective β-adrenergic blocker with α-adrenergic blocking activity. Available as a racemic mixture. Does not possess intrinsic sympathomimetic activity. Has calcium channel blocking activity at higher dose (30 times the normal dose). In hypertensive patients, reduces cardiac output, exercise- or β-agonist-induced tachycardia, reflex orthostatic tachycardia, vasodilatation, peripheral vascular resistance (especially in standing position), renal vascular resistance, plasma renin activity, and increases levels of atrial natriuretic peptide. In congestive heart failure, decreases systemic blood pressure, pulmonary capillary wedge pressure, pulmonary artery pressure, heart rate, systemic vascular resistance, right arterial pressure, and increases stroke volume index and left ventricular ejection fraction.
Therapeutic use
Mild-to-severe heart failure of ischemic or cardiomyopathic origin (usually in addition to standard therapy). Left ventricular dysfunction following myocardial infarction (clinically stable with LVEF ≤40%). Management of hypertension.
Pregnancy and lactiation implications
Postimplantation losses observed in animal studies. No data available on whether carvedilol crosses the placenta. β-Blockers have been associated with persistent bradycardia, hypotension, and intrauterine growth retardation. Neonatal hypoglycemia reported following maternal use of β-blockers at parturition or during breast-feeding. Use during pregnancy only if the potential benefit justifies the risk. Not recommended during lactation.
Unlabeled use
Angina pectoris.
Contraindications
Severe liver dysfunction. Serious hypersensitivity to carvedilol or any component of the formulation. Decompensated cardiac failure requiring intravenous inotropic therapy. Bronchial asthma or related bronchospastic conditions. Second- or third-degree AV block, sick sinus syndrome and severe bradycardia (except in patients with a functioning artificial pacemaker). Cardiogenic shock. Severe hepatic impairment.
Warnings and precautions
Use caution in history of severe anaphylaxis to allergens (patients taking β-blockers may become more sensitive; treatment of anaphylaxis (e.g. epinephrine) may be ineffective or promote undesirable effects). Symptomatic hypotension with or without syncope might occur (usually within the first 30 days of therapy). Consider pre-existing conditions such as sick sinus syndrome before initiating. May precipitate or aggravate symptoms of arterial insufficiency in peripheral vascular disease and Raynaud’s disease (use with caution). Heart failure patients may experience a worsening of renal function (risk factors: ischemic heart disease, diffuse vascular disease, underlying renal dysfunction, and systolic BP <100 mmHg). Worsening heart failure or fluid retention may occur during upward titration. Patients with bronchospastic disease should not receive β-blockers. Use with caution in diabetes mellitus (may potentiate hypoglycemia and/or mask signs and symptoms). May mask signs of hyperthyroidism (e.g. tachycardia); abrupt withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm. Use with caution in mild-to-moderate hepatic impairment (contraindicated in severe hepatic impairment), myasthenia gravis and in history of psychiatric illness (may cause or exacerbate CNS depression). Use with caution in patients receiving anesthetic agents which decrease myocardial function. β-Blocker therapy should not be withdrawn abruptly (particularly in patients with CAD).