Itraconazol
Itraconazole
También conocido como: Sporanox · Intrafungol · Itrafungol · itraconazolum · oriconazole · R-51211
Revisado por el equipo veterinario de VetSheetActualizado 15 may 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 |
|---|---|---|---|---|---|
| Malassezia dermatitis | 5 mg/kg PO once daily | PO | q24h | 3 weeks | 🌎 NA |
| Pulse therapy for Malassezia dermatitis | 5 mg/kg for 2 consecutive days per week | PO | 2 consecutive days per week | 3 weeks | 🌎 NA |
| Dermatophytosis | 5 mg/kg PO once daily | PO | q24h | Prolonged course required | 🌎 NA |
| Dermatophytosis (Pulse therapy) | 5 mg/kg PO once daily on an every other week schedule | PO | q24h (pulse) | Three 'pulses' of one week on, one week off | 🌎 NA |
| Blastomycosis | 5 mg/kg PO once daily | PO | q24h | At least 30 days after all signs resolve (total 60-90 days) | 🌎 NA |
| Histoplasmosis | 10 mg/kg daily PO | PO | q24h | At least 30 days after all signs resolve (total at least 90 days) | 🌎 NA |
| Blastomycosis (Alternative) | 5 mg/kg PO once a day or divided twice a day | PO | q24h or q12h | 2-3 months or until active disease is not apparent | 🌎 NA |
| Coccidiomycosis | 5-10 mg/kg PO once daily | PO | q24h | 6-12 months | 🌎 NA |
| Sporotrichosis | 5-10 mg/kg once daily | PO | q24h | 30 days beyond complete resolution of detectable lesions | 🌎 NA |
| Pythiosis or lagendiosis (after lesion resection) | 10 mg/kg PO once daily | PO | q24h | At least 2 months after surgery | 🌎 NA |
| Zygomycosis | 5-10 mg/kg PO q24h | PO | q24h | 3-6 months for non-resectable lesions | 🌎 NA |
| Idiopathic lymphoplasmacytic (chronic) rhinitis (LPR) | 5 mg/kg PO q12h | PO | q12h | Minimum of 3-6 months | 🌎 NA |
| Nasal aspergillosis | 5 mg/kg PO q12h | PO | q12h | 3-6 months | 🌎 NA |
| Coccidioidomycosis | 5-10 mg/kg PO q24h or 5 mg/kg PO q12h | PO | q24h or q12h | — | 🌎 NA |
| General use (fungal infections) | 5 mg/kg | PO | q24h | 4-20 weeks of treatment may be needed, dependent upon culture results | 🌍 EU |
- Malassezia dermatitis: Fair evidence supports recommendation
- Dermatophytosis: Begin taking cultures after 4 weeks. Continue therapy for 2 weeks beyond clinical cure and when 2-3 negative cultures are obtained at weekly intervals.
- Dermatophytosis (Pulse therapy): Toxicity problems are rare with this protocol.
- Blastomycosis: Give with food.
- Histoplasmosis: Give with food. If intestinal histoplasmosis, treat with amphotericin B initially.
- Blastomycosis (Alternative): A loading dose of 10 mg/kg once a day (or divided twice a day) for the first three days may reduce the 'lag' phase.
- Pythiosis or lagendiosis (after lesion resection): Given with terbinafine at 5-10 mg/kg PO q24h.
- Zygomycosis: After aggressive surgical resection or for non-resectable lesions.
- Idiopathic lymphoplasmacytic (chronic) rhinitis (LPR): Has shown dramatic beneficial improvement in some dogs.
- Nasal aspergillosis: May cure up to 60-70% of dogs, although some studies show marginal efficacy.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Histoplasmosis | 10 mg/kg daily PO | PO | q24h | At least 2-4 months | 🌎 NA |
| Cryptococcosis | 50-100 mg per cat per day PO | PO | q24h | Many months (mean 8.5 months) | 🌎 NA |
| Blastomycosis | 10 mg/kg PO once a day or divided twice a day | PO | q24h or q12h | 2-3 months or until active disease is not apparent | 🌎 NA |
| Coccidiomycosis | 5-10 mg/kg PO once daily | PO | q24h | 6-12 months | 🌎 NA |
| Sporotrichosis | 5-10 mg/kg once daily | PO | q24h | 30 days beyond complete resolution of detectable lesions | 🌎 NA |
| Cryptococcosis (mild to moderate, no CNS involvement) | Cats <= 3.5 kg: 50 mg PO once daily or 100 mg PO every other day; Medium/large cats: 100 mg PO once daily | PO | q24h or q48h | 3-12 months | 🌎 NA |
| Coccidioidomycosis | 25-50 mg (total dose) per cat q12-24h | PO | q12-24h | — | 🌎 NA |
| Generalized dermatophytosis (Microsporum canis) | 5 mg/kg PO once daily preferably between meals for 7 days on, 7 days off; repeat 3 times | PO | q24h (pulse) | 5 weeks (treated weeks 1, 3, 5) | 🌎 NA |
| Generalized dermatophytosis (Alternative) | 5 mg/kg PO twice daily or 10 mg/kg | PO | q12h or q24h | Generally 3-5 weeks | 🌎 NA |
| Dermatophyte granuloma | 10 mg/kg PO once daily | PO | q24h | Weeks to months | 🌎 NA |
| Dermatophytosis (Pulse therapy) | 5 mg/kg PO once daily on an every other week schedule | PO | q24h (pulse) | Three 'pulses' of one week on, one week off | 🌎 NA |
| General use (fungal infections) | 5 mg/kg | PO | q24h | 4-20 weeks of treatment may be needed, dependent upon culture results | 🌍 EU |
| Dermatophytosis (Microsporum canis) | 5 mg/kg | PO | q24h | Pulse dosing: 7 days on, 7 days off repeated x3 | 🌍 EU |
- Histoplasmosis: Given with food. Can also be divided twice daily.
- Cryptococcosis: If response inadequate, may add flucytosine.
- Blastomycosis: Cats usually require longer treatment than dogs.
- Cryptococcosis (mild to moderate, no CNS involvement): Give with food. Monitor ALT. Continue until completely normal, then check antigen titer.
- Generalized dermatophytosis (Alternative): Give with food. Give until culture is negative 2 times at two week intervals.
- Dermatophyte granuloma: At least one month beyond clinical resolution and until brush culture is negative x 2.
- Dermatophytosis (Microsporum canis): Authorized in the form of an oral solution. Used successfully to treat ringworm in Persian cats without the need for clipping.
Pequeños mamíferos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Blastomycosis (Mice) | 50-150 mg/kg q24h | PO | q24h | — | 🌎 NA |
| Vaginal candidiasis (Rats) | 2.5-10 mg/kg q24h | PO | q24h | — | 🌎 NA |
| Systemic candidiasis (Guinea pigs) | 5 mg/kg q24h | PO | q24h | — | 🌎 NA |
Aves
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Fungal infections in Ratites | 6-10 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Fungal diseases | 5-10 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Aspergillosis (Amazon parrots) | 5-10 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Aspergillosis (African grey Parrots) | 2.5-5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
- Fungal infections in Ratites: If neuro signs develop reduce dose or discontinue.
- Fungal diseases: Use with caution in African grey parrots.
Caballos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Guttural pouch mycosis, mycotic rhinitis or osteomyelitis | 5 mg/kg PO q24h | PO | q24h | — | 🌎 NA |
- Guttural pouch mycosis, mycotic rhinitis or osteomyelitis: Using the oral solution should be sufficient for treatment.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El itraconazol es un agente antifúngico triazol oral sintético altamente lipofílico, utilizado extensamente en medicina veterinaria para el tratamiento de micosis sistémicas (tales como aspergillosis, criptococosis, blastomicosis e histoplasmosis), así como dermatofitosis superficiales e infecciones por Malassezia.
Perlas clínicas y perfil farmacológico:
- Eficacia superior: Generalmente se considera más eficaz y con menos efectos secundarios endocrinos en comparación con los imidazoles antiguos como el ketoconazol, ya que no suprime de manera apreciable la síntesis de hormonas en mamíferos.
- Distribución tisular: Debido a que es altamente lipofílico y queratinofílico, se concentra fuertemente en la piel, el sebo y el pus, lo que lo hace excepcionalmente efectivo para infecciones fúngicas dermatológicas.
- La formulación importa: La absorción del itraconazol depende en gran medida de la formulación. Las cápsulas disponibles comercialmente requieren un entorno gástrico ácido y alimento para una absorción óptima. La solución oral comercial contiene ciclodextrina para mejorar la solubilidad y se absorbe mejor con el estómago vacío.
- Advertencia sobre formulaciones magistrales: Se desaconseja encarecidamente la formulación a partir de polvo a granel, ya que a menudo resulta en niveles sanguíneos subterapéuticos o indetectables, lo cual puede ser fatal en infecciones fúngicas sistémicas.
Mecanismo de acción
Itraconazole is a fungistatic triazole.
Mechanism of Action:
- Enzyme Inhibition: Itraconazole selectively inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase.
- Pathway Disruption: This inhibition blocks the conversion of lanosterol to ergosterol (the primary sterol in fungal cell membranes) → leads to the accumulation of toxic 14α-methylsterols.
- Membrane Permeability: The lack of ergosterol alters the cellular membrane structure → increases membrane permeability → allows leakage of cellular contents and impairs the uptake of purine and pyrimidine precursors.
- Immunomodulation: Itraconazole also exhibits mild immune-suppressing activity, likely via the suppression of T-lymphocyte proliferation.
Seguridad y advertencias
Contraindicaciones
- Hypersensitivity to itraconazole or other azole antifungals
- Hepatic impairment (relative contraindication)
- Achlorhydria or hypochlorhydria (relative contraindication)
- Reduced cardiac function (relative, due to potential negative inotropic effects)
- Pregnancy
- Liver disease (avoid use if present)
Efectos adversos
- Anorexia (most common in dogs)
- Hepatotoxicity (increased ALT, jaundice)
- Ulcerative skin lesions/vasculitis (dogs at high doses)
- Limb edema (dogs at high doses)
- Erythema multiforme (rare)
- Toxic epidermal necrolysis (rare)
- Vomiting
- Weight loss
- Depression (especially in cats and African grey parrots)
- Diarrhoea
- Salivation
- Depression and apathy
- Abdominal pain
- Hepatic toxicosis
- Ulcerative dermatitis
- Limb oedema
- Serious cutaneous drug eruptions (occasional)
- Dose-related suppression of adrenal function
Precauciones
Use with caution in patients with hepatic impairment, achlorhydria, or reduced cardiac function (due to potential negative inotropic effects). African grey parrots are extremely sensitive to itraconazole and can develop severe anorexia and depression; reduced dosages or alternative antifungals are recommended. Do not use compounded capsules from bulk powders, as they may not yield an absorbable dosage form, leading to treatment failure in life-threatening infections. Safety during pregnancy is not established (teratogenic and embryotoxic in lab animals at high doses).
Interacciones farmacológicas
May be antagonistic against Aspergillus or Candida; clinical importance unclear.
May reduce oral absorption of itraconazole; administer itraconazole at least 1 hour before or 2 hours after antacids.
Itraconazole may increase benzodiazepine levels.
Plasma concentrations may be elevated.
Itraconazole may increase levels.
Itraconazole may increase levels.
Increased cisapride levels and possibility for toxicity; concurrent use contraindicated in humans.
May decrease metabolism and increase clomipramine levels.
May inhibit the metabolism of corticosteroids; potential for increased adverse effects.
May inhibit metabolism of cyclophosphamide and its metabolites; potential for increased toxicity.
Increased cyclosporine levels.
May increase digoxin levels; concurrent use considered contraindicated in humans.
May increase fentanyl or alfentanil levels.
Increased gastric pH may reduce itraconazole absorption.
May increase risk for neurotoxicity.
May increase itraconazole concentrations.
May decrease itraconazole levels.
Increased gastric pH may reduce itraconazole absorption.
Increased risk for quinidine toxicity.
May decrease itraconazole levels; itraconazole may increase rifampin levels.
May increase levels; hypoglycemia possible.
May inhibit vinca alkaloid metabolism and increase levels.
May cause increased prothrombin times in patients receiving warfarin or other coumarin anticoagulants.
Extends the activity of methylprednisolone
Inhibits metabolism, potentially leading to toxicity
Inhibits metabolism
Inhibits metabolism
Increases bioavailability and blood levels of ciclosporin (well-documented in cats)
Inhibits metabolism and increases plasma concentrations
Reduces the absorption of itraconazole
Reduces the absorption of itraconazole
Reduces the absorption of itraconazole
Increases plasma concentrations of benzodiazepines
Increases plasma concentrations of vincristine
Datasheet advises against concurrent administration in cats
Datasheet advises against concurrent administration in cats
Monitorización
- Clinical Efficacy
- Liver function tests (monthly ALT recommended with long-term therapy)
- Appetite (anorexia is often the first sign of toxicity)
- Physical assessment for ulcerative skin lesions in dogs
- Liver enzymes (ALT, AST, ALP, Bilirubin) prior to and during prolonged treatment
- Clinical signs of hepatotoxicity (anorexia, vomiting, jaundice)
- Resolution of clinical signs and negative fungal cultures
Farmacocinética
Absorción
Highly dependent on gastric pH and presence of food. Empty stomach bioavailability may be <50%; with food, it approaches 100%. The oral solution is better absorbed on an empty stomach and possesses adequate bioavailability. Compounded capsules from bulk powders may not be absorbed.
Distribución
Very high protein binding. Widely distributed to lipid-rich tissues (highly lipophilic). Skin, sebum, female reproductive tract, and pus have concentrations greater than serum. Minimal concentrations in CSF, urine, aqueous humor, and saliva.
Metabolismo
Metabolized by the liver to many different metabolites, including the active metabolite hydroxyitraconazole.
Eliminación
Elimination may be a saturable process. Because of its long half-life, steady-state plasma levels are not reached for at least 6 days without a loading dose.
Sobredosis
There is very limited information on acute toxicity.
- Decontamination: Giving oral antacids may help reduce absorption. If a large overdose occurs, consider gut emptying and provide supportive therapy.
- Clearance: Itraconazole is not removed by dialysis.
- Chronic Toxicity: In studies, dogs receiving 40 mg/kg PO daily for 3 months demonstrated no overt toxicity.
Productos disponibles
Formulaciones
- Capsules
- 100 mg capsule
- 10 mg/ml oral solution
Veterinario
- Intrafungol® (Janssen) oral liquid 10 mg/mL (Available in UK/select countries)
- Itrafungol 10 mg/ml oral solution
Etiquetado para humanos
- Sporanox® Capsules 100 mg (and generics)
- Sporanox® Oral Solution 10 mg/mL
- Sporanox 100 mg capsule
Estado regulador
POM-V
POM-V, POM
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Capsules should be stored between 15-25°C and protected from light and moisture. Oral solution should be stored at temperatures less than 26°C, and protected from freezing.
Información para el cliente
Instrucciones importantes de administración:
- Cápsulas: Deben administrarse con alimento para asegurar una absorción adecuada. En gatos y perros pequeños, las cápsulas pueden abrirse y los gránulos mezclarse con una pequeña cantidad de comida apetecible (ej. mantequilla, queso, dieta enlatada).
- Solución líquida: Idealmente debe administrarse con el estómago vacío en mamíferos.
Qué observar:
- La pérdida de apetito suele ser el primer signo de que el medicamento está afectando el hígado. Contacte a su veterinario inmediatamente si su mascota deja de comer, comienza a vomitar o si nota una coloración amarillenta en los ojos/encías (ictericia).
- En perros, observe si aparecen llagas inexplicables en la piel o hinchazón en las patas.
Advertencias de seguridad:
- No utilice versiones de este fármaco formuladas a partir de polvo a granel. Se absorben mal y pueden llevar al fracaso del tratamiento, lo cual es peligroso en infecciones fúngicas graves.
- No administre junto con otros medicamentos (especialmente antiácidos) sin la aprobación de su veterinario.
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.