Esmolol
Esmolol hydrochloride
También conocido como: Brevibloc · Miniblock · ASL-8052 · Esmolol HCl · Esmololum · Esmolol hydrochloride
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 |
|---|---|---|---|---|---|
| Ultra-short acting beta blockade (ventricular arrhythmias) - Normal cardiac function | An initial loading dose of 0.25-0.5 mg/kg (250-500 micrograms/kg) administered IV as slow bolus over 1-2 minutes, then followed by a constant rate infusion of 10-200 micrograms/kg/minute; or Start CRI at 10-200 micrograms/kg/minute without the bolus loading dose. | IV | CRI | — | 🌎 NA |
| Ultra-short acting beta blockade - Severe dilated cardiomyopathy or severe mitral regurgitation | Start CRI at 10-20 micrograms/kg/min and titrate upward every 10 minutes to an effective endpoint. | IV | CRI | — | 🌎 NA |
| SVTs | 0.05-0.1 mg/kg (50-100 micrograms/kg) IV bolus over 2 minutes; repeat every 5 minutes to a maximum of 0.5 mg/kg (500 micrograms/kg). | IV | q5m | — | 🌎 NA |
| Arrhythmia conversion | Give in incremental IV bolus doses of 0.05-0.1 mg/kg every 5 minutes up to a maximum dose of 0.5 mg/kg. | IV | q5m | — | 🌎 NA |
- Ultra-short acting beta blockade (ventricular arrhythmias) - Normal cardiac function: If no loading dose, maximal effect should occur in 10-20 minutes.
- Ultra-short acting beta blockade - Severe dilated cardiomyopathy or severe mitral regurgitation: Do not give loading dose.
- Arrhythmia conversion: Because esmolol's effects are short-lived, if arrhythmia conversion does not occur, other negative inotropes (e.g., diltiazem, or verapamil) can be safely used 30 minutes after esmolol.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| HCM (to determine if beta-blockers will reduce dynamic left-ventricular outflow tract obstruction) | An initial loading dose of 0.25-0.5 mg/kg (250-500 micrograms/kg) administered IV as slow bolus over 1-2 minutes, then followed by a constant rate infusion of 10-200 micrograms/kg/minute. | IV | CRI | — | 🌎 NA |
| Critical Arrhythmias | Loading dose of 200-500 micrograms/kg IV over 1 minute; followed by a constant rate IV infusion of 25-200 micrograms/kg/minute | IV | CRI | — | 🌎 NA |
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El esmolol es un antagonista de los receptores adrenérgicos beta-1 cardioselectivo de acción ultracorta.
En medicina veterinaria, se utiliza principalmente mediante infusión intravenosa para el manejo agudo y a corto plazo de taquiarritmias supraventriculares (TSV), como la fibrilación auricular, el aleteo auricular y la taquicardia sinusal. También es de gran valor como fármaco de prueba diagnóstica para determinar si la terapia con betabloqueantes será efectiva y bien tolerada antes de realizar la transición del paciente a un betabloqueante oral de acción prolongada. Esto es particularmente útil en gatos con miocardiopatía hipertrófica (MCH) para evaluar si el bloqueo beta reducirá la obstrucción dinámica del tracto de salida del ventrículo izquierdo.
Perla clínica: Debido a que el esmolol es metabolizado rápidamente por las esterasas de los glóbulos rojos, sus efectos desaparecen en un lapso de 10-20 minutos después de suspender la infusión, lo que lo hace excepcionalmente seguro para terapias de prueba en pacientes en estado crítico.
Mecanismo de acción
Esmolol competitively blocks beta-1 adrenergic receptors in the myocardium with minimal to no effect on beta-2 receptors at clinical doses.
- Negative Chronotropy: Decreases heart rate by slowing sinoatrial (SA) node firing and increasing sinus cycle length.
- Negative Dromotropy: Slows conduction velocity through the atrioventricular (AV) node and prolongs sinus node recovery time.
- Negative Inotropy: Decreases myocardial contractility, which reduces myocardial oxygen demand.
Unlike propranolol, esmolol lacks intrinsic sympathomimetic activity (ISA) and does not possess membrane-stabilizing (quinidine-like) or bronchoconstrictive effects.
Seguridad y advertencias
Contraindicaciones
- Overt cardiac failure
- 2nd or 3rd degree AV block
- Sinus bradycardia
- Cardiogenic shock
- Second or third-degree AV block
- Uncompensated congestive heart failure
- Hypotension
Efectos adversos
- Hypotension
- Bradycardia
- Heart block
- Exacerbation of congestive heart failure
- Bronchospasm (at high doses where beta-1 selectivity is lost)
Precauciones
Use with caution (weigh benefit vs. risk) in patients with congestive heart failure (CHF), bronchoconstrictive lung disease, or diabetes mellitus. Esmolol may mask certain clinical signs of developing hypoglycemia (such as increased heart rate or blood pressure).
Interacciones farmacológicas
Esmolol may increase serum digoxin levels up to 20%, but these drugs have been used together safely and effectively.
Concurrent use is not recommended due to potential risk of hypertension.
May increase steady-state esmolol serum concentrations up to 50%; titrate esmolol dosage carefully.
May see additive effects (hypotension, bradycardia) if used with esmolol.
If systemic vascular resistance is high, there is an increased risk for blocked cardiac contractility; esmolol is not recommended to control SVTs in patients receiving these drugs.
In humans, particularly with severe cardiomyopathy, cardiac arrest has occurred (rarely).
Additive negative inotropic and chronotropic effects; risk of severe bradycardia and hypotension
Increased risk of severe bradycardia
Mutual antagonism
Additive negative inotropic and chronotropic effects, increasing risk of severe bradycardia and hypotension.
Monitorización
- Continuous Electrocardiogram (ECG)
- Direct or indirect blood pressure
- Heart rate and rhythm
- Clinical signs of heart failure
Farmacocinética
Vida media
Absorción
Steady-state blood levels occur in about 5 minutes if a loading dose was given or about 30 minutes if no load was given.
Distribución
Rapidly and widely distributed but not appreciably to the CNS, spleen or testes. The distribution half-life is about 2 minutes. It is unknown whether the drug crosses the placenta or enters milk.
Metabolismo
Rapidly metabolized in the blood by esterases to a practically inactive metabolite.
Eliminación
Renal or hepatic dysfunction do not appreciably alter elimination characteristics.
Sobredosis
The IV LD50 in dogs is approximately 32 mg/kg.
- 2 mg/kg/min for 1 hour: No adverse effects.
- 3 mg/kg/min for 1 hour: Produced ataxia and salivation.
- 4 mg/kg/min for 1 hour: Caused muscular rigidity, tremors, seizures, ptosis, vomiting, hyperpnea, vocalizations, and prostration.
Management: These effects all resolved within 90 minutes of the end of infusion. Because of the short duration of action of the drug, discontinuation or dosage reduction may be all that is required; otherwise, symptomatic and supportive treatment may be initiated.
Productos disponibles
Formulaciones
- Injection
- Injectable: 10 mg/ml solution
Etiquetado para humanos
- Esmolol HCl Injection: 10 mg/mL regular & preservative free in 10 mL vials
- Esmolol HCl Injection: 20 mg/mL preservative free in 5 mL vials & 100 mL bags
- Esmolol HCl Injection: 250 mg/mL in 10 mL ampules
- Brevibloc 10 mg/ml solution for injection
Estado regulador
POM (Prescription Only Medicine). Human-approved drug used under the cascade.
POM (Prescription Only Medicine). Human-approved drug used under the cascade.
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
The concentrate for injection should be stored at room temperature; do not freeze and protect from excessive heat. After diluted to a concentration of 10 mg/mL esmolol HCl is stable (at refrigeration temperatures or room temperature) for at least 24 hours in commonly used IV solutions.
Información para el cliente
El esmolol es un medicamento de emergencia de acción ultracorta que se administra exclusivamente en un entorno hospitalario veterinario.
- Monitoreo continuo: Su mascota será monitoreada de cerca con un ECG (electrocardiograma) y equipo de presión arterial mientras recibe este medicamento.
- Propósito: Se utiliza a menudo para estabilizar rápidamente ritmos cardíacos peligrosos o como una "prueba" para ver si la afección cardíaca de su mascota responderá bien a los betabloqueantes orales de acción prolongada.
- Seguridad: Debido a que se elimina del torrente sanguíneo en cuestión de minutos, cualquier efecto secundario (como presión arterial baja o frecuencia cardíaca lenta) generalmente desaparece muy rápidamente una vez que se suspende la infusión.
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.