Dinitrato de isosorbida / Mononitrato de isosorbida
Isosorbide Dinitrate / Isosorbide Mononitrate
1,4:3,6-dianhydro-D-glucitol 2,5-dinitrate / 1,4:3,6-dianhydro-D-glucitol 5-nitrate
También conocido como: Isordil · Ismo · Imdur · Isochron · Dilatrate-SR · Monoket · Titradose · ISDN · EV-151 · sorbide nitrate · AHR-4698 · BM-22145 · IS5-MN · isosorbide-5-mononitrate
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 |
|---|---|---|---|---|---|
| Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors | Isosorbide dinitrate at 0.5-2 mg/kg PO twice daily OR isosorbide mononitrate at 0.25-2 mg/kg PO twice daily | PO | twice daily | — | 🌎 NA |
- Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors: Efficacy is unknown. It is unknown if nitrate-free periods are required to prevent nitrate tolerance.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Adjunctive treatment of heart failure associated with thyroid storm | Isosorbide dinitrate at 0.5-2 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors | Isosorbide dinitrate at 0.5-2 mg/kg PO twice daily OR isosorbide mononitrate at 0.25-2 mg/kg PO twice daily | PO | twice daily | — | 🌎 NA |
- Adjunctive treatment of heart failure associated with thyroid storm: Start at lowest level and titrate upward.
- Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors: Efficacy is unknown.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El dinitrato de isosorbida (ISDN) y el mononitrato de isosorbida (ISMN) son nitratos orgánicos que actúan como potentes venodilatadores, utilizados principalmente para reducir la precarga cardíaca.
- Uso veterinario: Aunque se utilizan ampliamente en medicina humana para la angina de pecho y la insuficiencia cardíaca congestiva (ICC), la experiencia clínica y la eficacia probada en medicina de pequeños animales siguen siendo limitadas. Se utilizan ocasionalmente como terapia adyuvante para la insuficiencia cardíaca refractaria o en pacientes que no toleran los inhibidores de la ECA.
- Matices farmacológicos: Los perros parecen requerir dosis significativamente más altas de isosorbida para lograr efectos hemodinámicos terapéuticos en comparación con los humanos.
- Perla clínica: Al igual que otros nitratos orgánicos (p. ej., nitroglicerina), el uso continuo de nitratos de isosorbida puede conducir a tolerancia a los nitratos (taquifilaxia), donde los efectos vasodilatadores disminuyen con el tiempo. En medicina humana, se requiere un intervalo "libre de nitratos" (generalmente de 10-12 horas diarias) para mantener la eficacia, aunque se desconoce el requisito exacto para esto en pacientes veterinarios.
Mecanismo de acción
Organic nitrates act as prodrugs that donate nitric oxide (NO) to vascular smooth muscle, leading to profound vasodilation (predominantly venous, with some arterial effects at higher doses).
Mechanism Pathway: Organic Nitrate → converted to free radical Nitric Oxide (NO) → activates soluble guanylate cyclase (sGC) → increases intracellular cyclic GMP (cGMP) → activates Protein Kinase G (PKG) → decreases intracellular calcium and dephosphorylates myosin light chain → Vascular Smooth Muscle Relaxation.
- Hemodynamic Effects: By dilating the venous capacitance vessels, nitrates significantly decrease venous return to the heart (reduced preload), which lowers ventricular filling pressures and helps alleviate pulmonary edema in CHF.
- Additional Effects: Nitrates functionally antagonize acetylcholine, norepinephrine, and histamine. They also relax non-vascular smooth muscle, including biliary, bronchial, gastrointestinal, ureteral, and uterine tissues.
Seguridad y advertencias
Contraindicaciones
- Cardiogenic or hypovolemic shock
- Severe hypotension
- Hypovolemia
- Use as a sole agent for treating heart failure
- Concurrent use with selective phosphodiesterase inhibitors (e.g., sildenafil)
Efectos adversos
- Postural hypotension
- Reflex tachycardia
- Lethargy or weakness (secondary to hypotension)
- Gastrointestinal upset
- Restlessness
- Headache (well-documented in humans, difficult to assess in animals)
- Hypersensitivity reactions (rare)
Precauciones
Hemodynamic Warning: Use with extreme caution in patients with low blood pressure or uncorrected hypovolemia.
- Nitrate Tolerance: Continuous exposure may lead to tolerance. Consider dosing strategies that allow for a nitrate-free interval if chronic use is intended.
- Laboratory Interference: Serum cholesterol levels may be falsely decreased by nitrates when using the Zlatkis-Zak color reaction method.
- Pregnancy: FDA Category C. Use only if the potential benefit justifies the potential risk to the fetus.
Interacciones farmacológicas
Possible additive hypotensive effects; monitor blood pressure closely.
Possible additive hypotensive effects due to alpha-adrenergic blockade.
Concurrent use with sildenafil can cause profound, life-threatening hypotension and is strictly contraindicated. Use with pimobendan (a PDE3 inhibitor) is common in vet med but requires monitoring for excessive vasodilation.
Monitorización
- Clinical efficacy (improvement in respiratory rate/effort, resolution of pulmonary edema)
- Systemic blood pressure (monitor for hypotension)
- Heart rate (monitor for reflex tachycardia)
- Renal values and electrolytes (if used concurrently with diuretics and ACE inhibitors)
Farmacocinética
Vida media
Absorción
Dogs: Isosorbide mononitrate oral bioavailability is approximately 70%. Oral doses >2 mg/kg yield peak plasma levels >100 ng/mL (believed to be the minimum required for hemodynamic effects). Humans: Both ISDN and ISMN are well absorbed orally; food may delay the rate but not the extent of absorption.
Distribución
Widely distributed. Hemodynamic effects require minimum serum concentrations of approximately 100 ng/mL, though some canine studies showed no hemodynamic changes even at much higher peak levels.
Metabolismo
Isosorbide dinitrate undergoes extensive first-pass hepatic metabolism primarily to isosorbide mononitrate. Isosorbide mononitrate is metabolized primarily in the liver but does not undergo first-pass metabolism.
Eliminación
Metabolites do not appear to have pharmacologic activity and are principally excreted in the urine.
Sobredosis
Toxicity Profile: Isosorbide mononitrate caused significant lethality in rats and mice at massive dosages (2000 mg/kg and 3000 mg/kg, respectively).
Clinical Signs of Overdose:
- Profound venous pooling
- Decreased cardiac output
- Severe hypotension
- Reflex tachycardia
- Collapse or syncope
Treatment:
- Treatment is primarily supportive.
- Avoid Epinephrine: Drug therapies with agents such as epinephrine are NOT recommended as they may exacerbate the cardiovascular collapse.
- Fluid Therapy: Increasing central fluid volume may be useful to counteract venous pooling, but in patients with pre-existing congestive heart failure (CHF), IV fluids must be administered with extreme caution to avoid precipitating fulminant pulmonary edema.
Productos disponibles
Formulaciones
- Oral tablets
- Sublingual tablets
- Extended-release tablets
- Sustained-release capsules
Etiquetado para humanos
- Isosorbide Dinitrate Oral Tablets: 5 mg, 10 mg, 20 mg, 30 mg, & 40 mg
- Isosorbide Dinitrate Sublingual Oral Tablets: 2.5 mg, & 5 mg
- Isosorbide Dinitrate Extended-Release Oral Tablets: 40 mg
- Isosorbide Dinitrate Sustained-Release Oral Capsules: 40 mg
- Isosorbide Mononitrate Tablets: 10 mg, & 20 mg
- Isosorbide Mononitrate Extended-Release Tablets: 30 mg, 60 mg, & 120 mg
Estado regulador
Sin datos reguladores para: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Isosorbide dinitrate and standard isosorbide mononitrate tablets should be stored in well-closed/tight containers below 40°C (preferably between 15°-30°C). Isosorbide mononitrate extended-release tablets should be stored between 2°-30°C. Heat and moisture accelerate the loss of potency.
Información para el cliente
- Naturaleza experimental: Existe una experiencia limitada en el uso de este medicamento en medicina veterinaria; generalmente se reserva para afecciones cardíacas avanzadas o difíciles de tratar.
- Administración: Puede administrarse con o sin alimentos. Siga exactamente el programa de dosificación de su veterinario, ya que puede ser necesario un horario específico para evitar que el cuerpo desarrolle tolerancia al fármaco.
- Qué observar: Debido a que este medicamento reduce la presión arterial, observe a su mascota de cerca para detectar signos de debilidad, letargo, tropiezos o desmayos. Si esto ocurre, comuníquese con su veterinario de inmediato.
- Almacenamiento: Mantenga el medicamento bien cerrado en su envase original, protegido del calor y la humedad, ya que estos pueden hacer que el fármaco pierda su potencia.
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.