Amlodipino
Amlodipine
Amlodipine besylate
También conocido como: Norvasc · Lotrel (combination) · Caduet (combination) · Amodip · Istin · Amlodipini besilas · UK-48340-26 · UK-48340-11 · Amlodipine maleate · Amlodipine besylate · Amlodipino
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 |
|---|---|---|---|---|---|
| Adjunctive therapy for refractory heart failure (advanced mitral valve degeneration as an afterload reducer) | 0.2-0.4 mg/kg PO twice daily. Initiate therapy at 0.1 mg/kg PO twice daily and up-titrate weekly while monitoring blood pressure. | PO | q12h | — | 🌎 NA |
| Arterial vasodilator for refractory CHF secondary to mitral regurgitation | 0.1 mg/kg q12-24h initially; titrate up as needed to 0.25 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Systemic hypertension in dogs with chronic renal disease | 0.1-0.5 mg/kg PO once daily (q24h) | PO | q24h | — | 🌎 NA |
| Systemic hypertension (2nd step drug) | 0.1 mg/kg q24h; step up to 0.2 mg/kg q24h if needed | PO | q24h | — | 🌎 NA |
| Systemic hypertension | 0.05-0.1 mg/kg (titrate upwards weekly as required, up to 0.5 mg/kg) | PO | q12-24h | Long-term | 🌍 EU |
- Adjunctive therapy for refractory heart failure (advanced mitral valve degeneration as an afterload reducer): After ACE inhibitor maintenance therapy has been established.
- Arterial vasodilator for refractory CHF secondary to mitral regurgitation: Monitor blood pressure.
- Systemic hypertension in dogs with chronic renal disease: Most often combined with an ACE inhibitor. May require weeks to months to achieve satisfactory control.
- Systemic hypertension (2nd step drug): Used after enalapril/benazepril. Each step added if after 1-2 weeks systolic BP > 160 mmHg.
- Systemic hypertension: Monitor blood pressure regularly. Consider concurrent ACE inhibitor.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Systemic hypertension (1st step drug) | 0.625 mg per cat q24h, if cat greater then 6 kg, 1.25 mg/cat q24h | PO | q24h | — | 🌎 NA |
| Systemic hypertension | 0.625-1.25 mg (total dose) PO once daily | PO | q24h | — | 🌎 NA |
| Systemic hypertension | 0.625-1.25 mg/cat | PO | q24h (may increase slowly or increase frequency to q12h if necessary) | Long-term | 🌍 EU |
- Systemic hypertension (1st step drug): Add ACE inhibitor if proteinuric.
- Systemic hypertension: Drug of choice; often successful as a single agent. Maximum effect seen within 7 days.
- Systemic hypertension: Blood pressure monitoring is essential. Appears safe even with concurrent renal failure.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El amlodipino es un bloqueador de los canales de calcio (BCC) de tipo dihidropiridina utilizado principalmente en medicina veterinaria como un potente vasodilatador arterial periférico.
- Medicina felina: Se considera el estándar de oro y la terapia de primera línea para el manejo de la hipertensión sistémica felina, que a menudo es secundaria a enfermedad renal crónica (ERC), hipertiroidismo o miocardiopatía hipertrófica. Es altamente eficaz como agente único en gatos.
- Medicina canina: En perros, se utiliza típicamente como un reductor de la poscarga adyuvante en la insuficiencia cardíaca congestiva (ICC) refractaria o como agente antihipertensivo de segunda línea. Cuando se usa solo en perros a dosis más altas, puede activar el sistema renina-angiotensina-aldosterona (SRAA), por lo que frecuentemente se combina con un inhibidor de la ECA (p. ej., enalapril) para mitigar este efecto.
- Perla clínica: Tiene un inicio de acción relativamente lento, lo que ayuda a prevenir crisis hipotensivas agudas, pero omitir dosis puede provocar un rápido rebote hipertensivo.
Mecanismo de acción
Amlodipine selectively inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle by blocking L-type voltage-gated calcium channels.
- Vascular Smooth Muscle → Relaxation and vasodilation → Significant reduction in peripheral vascular resistance (afterload) → Decreased systemic blood pressure.
- It has a much higher affinity for vascular smooth muscle than cardiac muscle, meaning it produces profound vasodilation with minimal negative inotropic (contractility) or chronotropic (heart rate) effects at therapeutic doses.
- Cardiac Muscle → Mildly depresses impulse formation (automaticity) and conduction velocity.
Seguridad y advertencias
Contraindicaciones
- Patients with cardiogenic shock
- Advanced aortic stenosis (relative contraindication)
- Use with caution in patients with heart failure (due to slight negative inotropic effects)
- Use with caution in patients with hepatic dysfunction
Efectos adversos
- Cats: Infrequent azotemia, lethargy, hypokalemia, reflex tachycardia, weight loss
- Dogs: Gingival hyperplasia (with long-term use)
- Anorexia and hypotension (early in therapy)
Precauciones
Renal Considerations in Cats: There is concern that using amlodipine alone for treating hypertension in cats with renal disease may expose glomeruli to higher pressures secondary to efferent arteriolar constriction (caused by localized RAAS activation). Using an ACE inhibitor concurrently may help prevent this, though routine use of ACE inhibitors with amlodipine in cats with CKD remains somewhat controversial.
- Cardiac Disease: Use cautiously in patients with heart failure due to slight negative inotropic effects.
- Hepatic Disease: Use cautiously as the drug is extensively metabolized in the liver; half-life may be prolonged.
- Pregnancy: Fetotoxic in laboratory animals at very high doses; prolonged labor in rats. FDA Category C.
Interacciones farmacológicas
Concomitant use may cause additive hypotension.
Concomitant use may cause additive hypotension.
Concomitant use may cause additive hypotension.
May cause hypotension if used concurrently.
May alter bioavailability of amlodipine.
May impair hepatic metabolism of amlodipine, increasing circulating levels
May impair hepatic metabolism of amlodipine, increasing circulating levels
May impair hepatic metabolism of amlodipine, increasing circulating levels
May impair hepatic metabolism of amlodipine, increasing circulating levels
CYP3A4 inducer; may reduce circulating amlodipine levels
Increased risk of hypotension when combined
Monitorización
- Systemic blood pressure (frequent monitoring during dose titration)
- Ophthalmic exam (to assess for hypertensive retinopathy/retinal detachment)
- Renal values and electrolytes (especially if combined with ACE inhibitors)
- Clinical signs of hypotension (lethargy, weakness)
Farmacocinética
Vida media
Absorción
Slowly but almost completely absorbed after oral administration. Bioavailability is not altered by food.
Distribución
Very high plasma protein binding characteristics (approximately 93%).
Metabolismo
Slowly but extensively metabolized to inactive compounds in the liver.
Eliminación
Hepatic metabolism and subsequent excretion.
Sobredosis
Overdoses pose a significant risk for profound hypotension and reflex tachycardia (though bradycardia is also possible). Common clinical signs in dogs and cats include lethargy and vomiting.
Treatment:
- When possible, massive overdoses should be managed with gut emptying (emesis/lavage) and activated charcoal.
- Provide aggressive supportive treatment (IV fluids).
- Specific therapies may include beta-agonists, intravenous lipid emulsion (ILE) therapy, and intravenous calcium to counteract the calcium channel blockade.
Productos disponibles
Formulaciones
- Oral tablets
- Oral suspension (compounded)
Etiquetado para humanos
- Amlodipine Oral Tablets: 2.5 mg, 5 mg, & 10 mg (Norvasc, generic)
- Fixed-dose combination products with benazepril (Lotrel) or atorvastatin (Caduet)
Estado regulador
Amodip is approved for cats in the EU.
POM-V, POM.
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store tablets at room temperature in tight, light-resistant containers. Compounded oral suspensions (1 mg/mL in Ora-Plus/Ora-Sweet) retain >90% potency for 91 days at 5°C and 25°C, but must be protected from light.
Información para el cliente
- Administración: Puede administrarse con o sin alimentos.
- La constancia es clave: La presión arterial alta es un "asesino silencioso". Omitir dosis puede causar un rápido reaparecimiento de la hipertensión, lo que puede derivar en ceguera aguda, convulsiones o daño renal grave.
- Monitoreo: Se requieren visitas veterinarias regulares para medir la presión arterial de su mascota y asegurar que la dosis sea la correcta.
- Efectos secundarios: Esté atento a signos de letargo, debilidad o pérdida de apetito, especialmente al comenzar la medicación. En perros, el uso a largo plazo puede causar un crecimiento excesivo de las encías (hiperplasia gingival).
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.
