Pentoxifilina
Pentoxifylline
1-(5-oxohexyl)-3,7-dimethylxanthine
También conocido como: Trental · BL-191 · oxpentifylline · pentoxifyllinum · Oxypentifylline
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Evidencia posológica v13 auditada
Evidencia estructurada para el cálculoInflammatory/autoimmune dermatologic conditions (extralabel)
- q8-12h
NA
Contexto clínico obligatorio (4)
- NOTE: The commercially available pentoxifylline product is a 400 mg extended-release tablet. Cutting or crushing the tablets may negate the extended-release characteristics and alter pharmacokinetics but splitting tablets may be necessary to administer or accurately dose. Avoid crushing tablets for small animal use.
- ■ Give this medicine with food.
- ■ Extended-release tablets can be split if necessary to give the appropriate dose. Crushing the tablets may increase the risk for side effects and should be avoided when possible.
- The commercially available tablets should be stored in well-closed containers, protected from light at 20°C to 25°C (68°F -77°F).
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
La pentoxifilina es un derivado de la metilxantina sintético (estructuralmente relacionado con la teofilina y la cafeína) con propiedades hemorreológicas e inmunomoduladoras únicas.
- Perros: Se utiliza principalmente para tratar afecciones dermatológicas mediadas por el sistema inmunitario con compromiso microvascular subyacente, como la dermatomiositis canina familiar, la seborrea/necrosis del margen auricular y la vasculitis cutánea (p. ej., Alabama rot). También se utiliza como terapia adyuvante para la dermatitis atópica y se está investigando para la miocardiopatía dilatada (MCD).
- Caballos: Se utiliza como terapia adyuvante para la vasculitis cutánea, endotoxemia, enfermedad navicular y placentitis.
- Gatos: Se utiliza ocasionalmente junto con prednisolona para disminuir la vasculitis asociada con la Peritonitis Infecciosa Felina (PIF).
Perla clínica: Debido a que sus efectos sobre la remodelación tisular y la inflamación requieren tiempo, es posible que los beneficios clínicos en afecciones dermatológicas no se observen hasta después de 4 a 8 semanas.
Mecanismo de acción
The exact mechanisms are multifaceted, combining rheological improvement with anti-inflammatory effects:
- Phosphodiesterase (PDE) Inhibition: Inhibits erythrocyte PDE → increases intracellular cAMP → increases erythrocyte flexibility and deformability, allowing red blood cells to navigate compromised microvasculature.
- Blood Viscosity Reduction: Reduces plasma fibrinogen and increases fibrinolytic activity.
- Immunomodulation: PDE inhibition in leukocytes decreases the production of inflammatory cytokines, notably TNF-α, reducing the negative effects of endotoxemia.
- Enzyme Inhibition: In horses, it acts as a potent inhibitor of matrix metalloproteinase-9 (MMP-9) and a modest inhibitor of MMP-2, which may aid in preventing tissue degradation.
Seguridad y advertencias
Contraindicaciones
- Intolerance or hypersensitivity to pentoxifylline or other xanthines (e.g., theophylline, caffeine, theobromine)
- Cerebral hemorrhage
- Hypersensitivity to methylxanthines (e.g., theophylline, caffeine)
- Cerebral or retinal hemorrhage
- Severe hepatic or renal impairment (use with caution)
Efectos adversos
- Vomiting
- Inappetence
- Loose stools
- Excitement
- Nervousness
- Dizziness (humans)
- Headache (humans)
- Erythema multiforme (rare in dogs)
- Transient leukocytosis (horses IV)
- Muscle fasciculations (horses IV)
- Sweating on shoulders/flanks (horses IV)
- Mild increases in heart rate (horses IV)
- Anorexia
- Diarrhea
- Restlessness
- Tachycardia
- Tremors
Precauciones
Caution in patients with severe hepatic or renal impairment, or those at risk for hemorrhage.
- Pregnancy: FDA Category C. May be teratogenic at high dosages.
- Nursing: Excreted in maternal milk. Use cautiously in nursing patients due to potential tumorigenicity seen in rats.
Interacciones farmacológicas
May increase hypotensive effect when used concurrently
Controversial in horses; may negate beneficial effects for endotoxemia, though some studies show superior efficacy when used with flunixin
Increased risk for bleeding
Serum levels of theophylline may be increased when used concurrently
Increased risk of bleeding; use together with enhanced monitoring and caution
May increase pentoxifylline levels
Potential for additive hypotensive effects
Monitorización
- Clinical efficacy (resolution of dermatologic or vascular signs)
- Adverse effects (GI upset, CNS signs)
- Clinical response (resolution of skin lesions/improved blood flow)
- Gastrointestinal tolerance
- Signs of bleeding
Farmacocinética
Vida media
Absorción
Horses: Rapidly absorbed after PO administration of crushed sustained-release tablets, with wide interpatient variation (bioavailability ~68%). Dogs: Bioavailability is approximately 50% with peak levels occurring 1-3 hours after dosing. Humans: Rapid and almost complete absorption, but undergoes a significant first-pass effect.
Distribución
Distributive characteristics are not fully described, but it is known that the drug enters maternal milk.
Metabolismo
Metabolized both in the liver and erythrocytes; all identified metabolites appear to be active.
Eliminación
Excreted primarily via urine (inferred from human data).
Sobredosis
Signs of overdose in humans include flushing, seizures, hypotension, unconsciousness, agitation, fever, somnolence, GI distress, and ECG changes. One patient who ingested 80 mg/kg recovered completely. Overdoses should be treated using standard methods of appropriate gut emptying (emesis/lavage) and supportive therapies.
Productos disponibles
Formulaciones
- Tablets (sustained-release / controlled-release)
- Injection (IV)
- 400 mg tablet (often modified-release)
Etiquetado para humanos
- Pentoxifylline Controlled/Extended Release Tablets: 400 mg; Trental® (Hoechst Marion Roussel); generic
- Trental 400 mg modified-release tablets
Estado regulador
Human POM used off-label under the cascade.
Human POM used off-label under the cascade.
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Commercially available tablets should be stored in well-closed containers, protected from light at 15-30°C.
Información para el cliente
- Administración: Administre este medicamento con comida para reducir significativamente la posibilidad de malestar estomacal (vómitos o pérdida de apetito).
- La paciencia es clave: Para afecciones cutáneas y vasculares, puede tomar varias semanas (hasta 6-8 semanas) ver una mejoría notable. No suspenda el medicamento antes de tiempo a menos que su veterinario se lo indique.
- Efectos secundarios: Esté atento a vómitos, diarrea o nerviosismo/excitación inusual. Comuníquese con su veterinario si estos ocurren.
- Expectativas: Los clientes deben comprender que la experiencia veterinaria con este medicamento es limitada y que el perfil de riesgo frente al beneficio no está completamente definido.
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.