Carvedilol
carvedilolum
También conocido como: Coreg CR · Eucardic · BM-14190 · carvedilolum · Cardilol · Cardiol · Carloc · Carvil · Carvipress · Coritensil · Coropres · Dilatrend · Dilbloc · Dimitone · Divelol · Hybridil · Kredex · Querto
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Dosis por especie
🌎 NA — North America🌍 EU — Europe
Perros
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Heart failure (adjunctive therapy) | ¼-½ of a 3.125 mg tablet PO twice daily | PO | twice daily | — | 🌎 NA |
| Early/mild heart failure or later stages of CHF | 0.2 mg/kg PO twice daily initially with slow titration upwards towards a dose of 0.8 mg/kg twice daily | PO | twice daily | — | 🌎 NA |
| Heart failure (target plasma concentration) | 0.5 mg/kg PO twice daily | PO | twice daily | — | 🌎 NA |
| Dilated cardiomyopathy | 0.3 mg/kg PO q12h | PO | q12h | 3 months | 🌎 NA |
| Chronic heart failure / Dilated Cardiomyopathy (DCM) | Start at 0.05-0.1 mg/kg, gradually increase at 2-week intervals to target dose of 0.3-0.4 mg/kg | PO | q12h | Long-term | 🌍 EU |
| ACVIM stage B2 degenerative mitral valve disease | 0.3 mg/kg, increased at intervals up to 1.1 mg/kg | PO | q12h | Long-term | 🌍 EU |
- Heart failure (adjunctive therapy): Usual starting dose. Start at the low end of the dosing range and gradually titrate upward carefully watching to avoid negative inotropic effects.
- Early/mild heart failure or later stages of CHF: Beta blockers are best employed in dogs that are minimally symptomatic. Many dogs with CHF will not tolerate this upward titration.
- Heart failure (target plasma concentration): Should result in beta-blockade, but maximum beta-blockade may require doses of >0.7-0.9 mg/kg. Because of bioavailability variations, plasma monitoring, clinical trials and uptitration protocols may be beneficial.
- Dilated cardiomyopathy: Did not produce any significant improvements in neurohormonal activation, heart size, or owner-perceived quality of life. Doses >0.3 mg/kg q12h are likely to be required to effect changes in ventricular remodeling and function.
- Chronic heart failure / Dilated Cardiomyopathy (DCM): Increase dose only if tolerated.
- ACVIM stage B2 degenerative mitral valve disease: For cardiac remodelling with no signs of cardiac failure.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El carvedilol es un betabloqueante no selectivo de tercera generación único, con propiedades de bloqueo adrenérgico alfa-1. En medicina veterinaria, se investiga principalmente como tratamiento adyuvante para la miocardiopatía dilatada canina (MDC) y la insuficiencia cardíaca crónica.
- Acción dual: A diferencia de los betabloqueantes tradicionales (como el atenolol), el carvedilol proporciona efectos vasodilatadores adicionales, reduciendo la poscarga cardíaca.
- Uso controvertido: Su uso en cardiología veterinaria sigue siendo controvertido. Aunque ha demostrado beneficios en la mortalidad en la insuficiencia cardíaca humana, los estudios en perros han mostrado resultados mixtos respecto a su eficacia para mejorar la activación neurohormonal o el remodelado ventricular a dosis estándar.
- Perla clínica: El carvedilol es un potente inótropo negativo. Puede precipitar una descompensación aguda en pacientes con insuficiencia cardíaca avanzada o altamente sintomática. Requiere un aumento de dosis extremadamente cauteloso y lento, y es mejor iniciarlo en pacientes mínimamente sintomáticos.
Mecanismo de acción
Carvedilol exerts its cardiovascular effects through multiple mechanisms:
- Non-selective Beta-Adrenergic Blockade (β1 and β2): Heart failure leads to chronic sympathetic nervous system (SNS) activation → tachycardia, renin-angiotensin-aldosterone system (RAAS) activation, beta-receptor downregulation, and myocyte necrosis. Carvedilol blocks these receptors → reverses/diminishes SNS toxicity, reduces heart rate, and decreases myocardial oxygen demand.
- Selective Alpha-1 Adrenergic Blockade: Blocks peripheral α1-receptors → vasodilation → reduces systemic vascular resistance and cardiac afterload.
- Antioxidant Properties: Carvedilol and its metabolites act as potent scavengers of reactive oxygen species (ROS) and inhibit lipid peroxidation, protecting the myocardium from oxidative stress.
- Antidysrhythmic Effects: Secondary to its beta-blocking and membrane-stabilizing properties.
Seguridad y advertencias
Contraindicaciones
- Class IV decompensated heart failure
- Bronchial asthma
- 2nd or 3rd degree AV block
- Sick sinus syndrome (unless artificially paced)
- Severe bradycardia
- Cardiogenic shock
- Hypersensitivity to the drug
Efectos adversos
- Inappetence
- Lassitude (lethargy/fatigue)
- Hypotension
- Decompensation of heart failure (if titrated too rapidly)
- Bronchospasm (reported in humans)
- Mild hepatocellular injury (rare)
Precauciones
Black Box Warning Equivalent: Too rapid beta blockade can cause decompensation in patients with heart failure; cautious dosage titration is mandatory.
- Hepatic Insufficiency: Because the drug is extensively metabolized in the liver, patients with hepatic insufficiency should receive the drug with caution.
- Pregnancy/Nursing: FDA Category C. Increased post-implantation loss seen in animal studies. Unknown if it enters canine milk, but does enter rat milk. Use with caution in nursing patients.
Interacciones farmacológicas
Use with carvedilol may cause additive effects
May rarely cause hemodynamic compromise
May decrease metabolism and increase AUC of carvedilol
Carvedilol may potentiate the cardiovascular effects of clonidine
Carvedilol may increase cyclosporine levels
Can increase digoxin plasma concentrations by approximately 15%
May increase R(+)carvedilol concentrations and increase alpha-1 blocking effects (vasodilation)
Carvedilol may enhance the blood glucose lowering effects of insulin or other antidiabetic agents
Can decrease carvedilol plasma concentrations by as much as 70%
Can cause increased bradycardia and hypotension in patients taking carvedilol
Enhanced hypotensive effect and myocardial depression
Enhanced hypotensive effect
Enhanced hypotensive effect
Enhanced hypotensive effect
Enhanced hypotensive effect
Increased risk of bradycardia, severe hypotension, heart failure, and AV block
May antagonize the hypotensive effect of carvedilol
May enhance the hypoglycaemic effect of insulin and mask signs of hypoglycaemia
Carvedilol increases plasma concentration of ciclosporin
Contraindicated; risk of severe hypertension and bradycardia
Monitorización
- Clinical efficacy (improvement in heart failure signs)
- Adverse effects (lethargy, inappetence, hypotension, worsening heart failure)
- Plasma drug levels (Target: 50-100 nanograms/mL)
Farmacocinética
Vida media
Absorción
In dogs, bioavailability after oral dosing averages about 23%, but is highly variable (ranging from 3-10% in some individuals). In humans, it is rapidly and extensively absorbed but has a high first-pass effect, resulting in ~30% bioavailability.
Distribución
In dogs, volume of distribution averages about 1.4 L/kg. In humans, it is extensively bound to plasma proteins (98%).
Metabolismo
Extensively metabolized in the liver. In dogs, hydroxylation of the carbazolyl ring and glucuronidation are the predominant processes (at least 15 metabolites identified). In humans, CYP2D6 and CYP2C9 are the primary P450 isoenzymes responsible.
Eliminación
Metabolites are primarily excreted via the bile and feces.
Sobredosis
The acute oral LD50 in healthy rats and mice is greater than 8 grams/kg.
Clinical Signs of Overdose:
- Severe hypotension
- Cardiac insufficiency
- Bradycardia
- Cardiogenic shock
- Death due to cardiac arrest
Treatment:
- Gut emptying protocols should be considered if ingestion was recent.
- Bradycardia: Treat with atropine.
- Cardiovascular Support: Support function with glucagon and sympathomimetics (e.g., dobutamine, epinephrine).
- Contact an animal poison control center for specific information.
Productos disponibles
Formulaciones
- Oral tablets
- Extended-release oral capsules
- Compounded oral suspension
Etiquetado para humanos
- Carvedilol Oral Tablets: 3.125 mg, 6.25 mg, 12.5 mg, & 25 mg (Coreg, generic)
- Carvedilol Extended-Release Oral Capsules: 10 mg, 20 mg, 40 mg & 80 mg as phosphate (Coreg CR)
Estado regulador
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Tablets and extended-release capsules should be stored below 30°C (86°F), protected from moisture, and dispensed in tight, light-resistant containers. Compounded oral suspensions (2 mg/mL or 10 mg/mL in simple syrup) should be stored in amber bottles at temperatures not exceeding 25°C and protected from light for up to 90 days. Shake well before administering.
Información para el cliente
Información importante para los propietarios de mascotas
- Dosificación estricta: Administre este medicamento exactamente como lo prescribe su veterinario. No suspenda el medicamento abruptamente sin la aprobación y guía de su veterinario, ya que esto puede causar un efecto rebote peligroso en el corazón.
- Esté atento a signos de empeoramiento: Contacte a su veterinario inmediatamente si la condición de su mascota empeora mientras recibe este medicamento (por ejemplo, aumento de la tos o dificultad para respirar).
- Monitoree los efectos secundarios: Llame a su veterinario si su mascota muestra signos de disminución del apetito, fatiga severa o letargo, mareos o inestabilidad (lo cual puede indicar presión arterial baja).
- Administración: Este medicamento se administra mejor con comida para ayudar a la absorción y reducir el riesgo de caídas repentinas de la presión arterial.
La referencia de medicamentos de VetSheet está destinada a profesionales veterinarios autorizados como ayuda para la toma de decisiones clínicas, no como sustituto del criterio profesional ni del prospecto actual del fabricante.