Ketoconazol
Ketoconazole
Ketoconazolum
También conocido como: Nizoral · Fungiconazole · ketoconazolum · R-41400
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 |
|---|---|---|---|---|---|
| Coccidioidomycosis (systemic form) | 5-10 mg/kg PO twice daily | PO | q12h | Minimum of 3-6 months | 🌎 NA |
| Coccidioidomycosis (CNS form) | 15-20 mg/kg PO twice daily | PO | q12h | Minimum of 3-6 months | 🌎 NA |
| Coccidioidomycosis (bony lesions or relapses) | 5 mg/kg PO every other day | PO | q48h | Lifelong | 🌎 NA |
| Coccidioidomycosis | 10-30 mg/kg PO divided twice a day | PO | q12h | 6-12 months | 🌎 NA |
| Blastomycosis | 10 mg/kg PO twice daily (15-20 mg/kg PO twice daily if CNS involvement) | PO | q12h | At least 3 months | 🌎 NA |
| Blastomycosis | 20 mg/kg/day PO once daily or divided twice daily; 40 mg/kg divided twice daily for ocular or CNS involvement | PO | q24h or q12h | At least 2-3 months or until remission | 🌎 NA |
| Histoplasmosis | 10 mg/kg PO once a day or twice a day | PO | q24h or q12h | At least 3 months | 🌎 NA |
| Histoplasmosis | 10-20 mg/day PO once daily or divided twice daily | PO | q24h or q12h | At least 2-3 months or until remission | 🌎 NA |
| Aspergillosis | 20 mg/kg PO | PO | Not specified | At least 6 weeks | 🌎 NA |
| Nasal aspergillosis | 10 mg/kg PO once daily (q24h) or 5 mg/kg PO q12h | PO | q24h or q12h | Many weeks; continue 1 month beyond last detection | 🌎 NA |
| Cryptococcosis | 10 mg/kg PO once daily or divided twice daily | PO | q24h or q12h | Maintenance | 🌎 NA |
| Fungal myocarditis | 10 mg/kg PO three times daily | PO | q8h | — | 🌎 NA |
| Candidiasis | 10 mg/kg PO once daily (q24h) or 5 mg/kg PO q12h | PO | q24h or q12h | Many weeks; continue 1 month beyond last detection | 🌎 NA |
| Sporotrichosis | 15 mg/kg PO q12h | PO | q12h | Many weeks; continue 1 month beyond last detection | 🌎 NA |
| Malassezia dermatitis (severe) | 5 mg/kg PO once daily to 10 mg/kg twice daily | PO | q24h to q12h | Until clinical signs abate and no organisms seen | 🌎 NA |
| Malassezia dermatitis | 5-10 mg/kg PO twice a day | PO | q12h | 30 days | 🌎 NA |
| Malassezia dermatitis | 5-10 mg/kg PO daily for 10 days, then every other day for an additional 10 days | PO | q24h then q48h | 20 days | 🌎 NA |
| Malassezia dermatitis | 5 mg/kg twice daily for 21-30 days, may increase to 10 mg/kg PO twice daily if poor response | PO | q12h | 21-30 days | 🌎 NA |
| Malassezia dermatitis | 2.5-10 mg/kg PO once daily (q24h) for 7-14 days; once a good response is seen taper to every other day (q48h) | PO | q24h then q48h | Until complete remission | 🌎 NA |
| Hyperadrenocorticism | 5-10 mg/kg PO twice daily initially; may increase to 15 mg/kg PO twice daily | PO | q12h | Long-term | 🌎 NA |
| Hyperadrenocorticism | 5 mg/kg q12h for 5-7 days, increase to 10 mg/kg q12h for 10-14 days; many require 15-20 mg/kg q12h | PO | q12h | Long-term | 🌎 NA |
| Hyperadrenocorticism (palliative) | 15 mg/kg PO q12h | PO | q12h | Long-term | 🌎 NA |
| Reduce cyclosporine dosage | 5-10 mg/kg PO per day | PO | q24h | Concurrent with cyclosporine | 🌎 NA |
| Perianal fistula (with cyclosporine) | 7.5 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
| Atopic dermatitis (with cyclosporine) | 5 mg/kg/day | PO | q24h | — | 🌎 NA |
| IMHA (with cyclosporine) | 10 mg/kg/day | PO | q24h | — | 🌎 NA |
- Blastomycosis: Used with amphotericin B
- Blastomycosis: Used with amphotericin B
- Histoplasmosis: Treat at least 30 days after complete resolution. Maintenance 5 mg/kg PO every other day indefinitely if relapse.
- Histoplasmosis: Used with amphotericin B
- Aspergillosis: May require long-term/maintenance therapy
- Nasal aspergillosis: Itraconazole somewhat more effective
- Cryptococcosis: Used with amphotericin B
- Malassezia dermatitis: Often used with therapeutic shampoos
- Hyperadrenocorticism: Monitor with ACTH stimulation test
- Perianal fistula (with cyclosporine): Given with cyclosporine 0.5-0.75 mg PO twice daily
- Atopic dermatitis (with cyclosporine): Given with cyclosporine 2.5 mg/kg/day
- IMHA (with cyclosporine): Allows reduction of cyclosporine dose
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Coccidioidomycosis | 10-30 mg/kg PO divided twice a day | PO | q12h | 6-12 months | 🌎 NA |
| Coccidioidomycosis | 50 mg per cat PO once daily; or 25-75 mg per cat q12-48h | PO | q24h or q12-48h | 9-12 months on average | 🌎 NA |
| Blastomycosis | 10 mg/kg q12h PO | PO | q12h | At least 60 days | 🌎 NA |
| Cryptococcosis | 10 mg/kg twice daily | PO | q12h | — | 🌎 NA |
| Aspergillosis | 10 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Dermatophytosis | 10 mg/kg PO once daily with an acidic meal | PO | q24h | Prolonged; 2 weeks beyond clinical cure and negative cultures | 🌎 NA |
| Sporotrichosis | 5-10 mg/kg PO q12-24h | PO | q12-24h | 2-4 months on average | 🌎 NA |
- Coccidioidomycosis: Use in cats is controversial
- Blastomycosis: Used with amphotericin B
- Cryptococcosis: Can produce anorexia and debility at this dosage
- Dermatophytosis: Reserved for when griseofulvin ineffective or not tolerated
Pequeños mamíferos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Susceptible infections (Rabbits) | 10-40 mg/kg per day PO | PO | q24h | 14 days | 🌎 NA |
| Systemic mycoses/candidiasis (Hamsters, Gerbils, Mice, Rats, Guinea pigs, Chinchillas) | 10-40 mg/kg per day PO | PO | q24h | 14 days | 🌎 NA |
Aves
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Severe refractory candidiasis in Psittacines | 5-10 mg/kg as a gavage twice daily | PO (gavage) | q12h | 14 days | 🌎 NA |
| Susceptible fungal infections (most species) | 200 mg/L | PO (water) | Continuous | 7-14 days | 🌎 NA |
| Susceptible fungal infections (most species) | 10-20 mg/kg | PO (feed) | Daily | 7-14 days | 🌎 NA |
| Susceptible fungal infections (Moluccan Cockatoos) | 20-30 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
| Susceptible fungal infections (Ratites) | 5-10 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
- Severe refractory candidiasis in Psittacines: Dissolve in 0.2 mL 1 N HCl and add 0.8 mL water
- Susceptible fungal infections (most species): Dissolve in acid prior to adding to water
- Susceptible fungal infections (most species): Add to favorite food or mash
Reptiles
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Susceptible infections (most species) | 15-30 mg/kg PO once daily | PO | q24h | 2-4 weeks | 🌎 NA |
| Fungal shell diseases in turtles/tortoises | 25 mg/kg PO once a day | PO | q24h | 2-4 weeks | 🌎 NA |
Caballos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Susceptible yeasts and Aspergillus spp | 5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Scopulariopsis pneumonia | 30 mg/kg q12h | NG tube | q12h | — | 🌎 NA |
- Susceptible yeasts and Aspergillus spp: Using commercial oral solution
- Scopulariopsis pneumonia: Administered via NG tube mixed with 0.2 Normal hydrochloric acid
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El ketoconazol es un agente antifúngico imidazólico de primera generación. Aunque ha sido reemplazado en gran medida por triazoles más nuevos (como el itraconazol y el fluconazol) debido a sus mejores perfiles de seguridad y mayor eficacia, el ketoconazol sigue siendo una opción rentable para el tratamiento de ciertas micosis sistémicas (p. ej., Blastomyces, Histoplasma, Coccidioides y dermatitis por Malassezia).
Perla clínica: Más allá de sus propiedades antifúngicas, el ketoconazol es un potente inhibidor de las enzimas del citocromo P450 en mamíferos. Esta característica única se aprovecha con frecuencia fuera de etiqueta (off-label) en medicina veterinaria para dos propósitos principales:
- Ahorro de fármacos: Para reducir la dosis requerida (y el costo) de medicamentos costosos como la ciclosporina al inhibir su metabolismo hepático.
- Terapia endocrina: Como opción de manejo médico para el hiperadrenocorticismo canino (enfermedad de Cushing) al inhibir de forma reversible la esteroidogénesis adrenal.
Nota: El uso de ketoconazol en gatos es altamente controvertido debido a una mayor prevalencia de toxicidad gastrointestinal y hepática; muchos clínicos prefieren el itraconazol para pacientes felinos.
Mecanismo de acción
Antifungal Action: Ketoconazole inhibits lanosterol 14α-demethylase, a fungal cytochrome P450 enzyme → blocks the conversion of lanosterol to ergosterol → depletion of ergosterol in the fungal cell membrane → accumulation of toxic intermediate sterols → increased cellular membrane permeability and cell death. It is primarily fungistatic but can be fungicidal at high concentrations or prolonged exposures.
Endocrine/Metabolic Action: It reversibly inhibits mammalian cytochrome P450 enzymes (specifically CYP11A1 and CYP17) → blocks the synthesis of adrenal and gonadal steroids → decreases cortisol and testosterone production.
Immunomodulatory Action: Inhibits 5-lipooxygenase, providing mild anti-inflammatory effects, and suppresses T-lymphocyte proliferation.
Seguridad y advertencias
Contraindicaciones
- Known hypersensitivity to ketoconazole
- Controversial/Contraindicated in cats (due to toxicity risks)
- Concurrent use with cisapride or ivermectin (in dogs)
- Hepatic insufficiency
- Pregnancy (due to possible teratogenic effects)
Efectos adversos
- Anorexia (most common, especially in cats)
- Vomiting
- Diarrhea
- Hepatic toxicity (cholangiohepatitis, increased liver enzymes)
- Thrombocytopenia (rare)
- Reversible lightening of haircoat
- Transient suppression of gonadal and adrenal steroid synthesis
- Infertility in male dogs (reversible)
- Hepatotoxicity
- Alterations in hair-coat colour
- Thrombocytopenia (at high doses)
- Adrenal insufficiency (at high doses)
- Cataract development (in dogs)
- Teratogenic effects
Precauciones
Use with caution in patients with hepatic disease or thrombocytopenia. Ketoconazole is a known teratogen and embryotoxin; weigh risks vs. benefits in pregnant animals. It may cause reversible infertility in male dogs by decreasing testosterone synthesis. Dogs undergoing high-dose antifungal therapy may need additional glucocorticoid support during periods of acute stress due to adrenal suppression.
Interacciones farmacológicas
May produce a disulfiram-like reaction (vomiting)
May reduce oral absorption of ketoconazole; administer at least 1 hour before or 2 hours after
Ketoconazole may reduce metabolism and increase adverse effects
Ketoconazole may increase levels
Plasma concentrations may be elevated
Ketoconazole may increase levels
Ketoconazole may increase levels
Ketoconazole may increase cisapride levels and possibility for toxicity; use together contraindicated
Ketoconazole may inhibit metabolism; potential for increased adverse effects
Ketoconazole may inhibit metabolism; potential for increased toxicity
Increased cyclosporine levels (often used therapeutically to reduce cyclosporine dose)
Ketoconazole may increase digoxin levels
Ketoconazole may increase fentanyl or alfentanil levels
Increased gastric pH may reduce ketoconazole absorption
Should be used cautiously together due to additive hepatotoxicity risk
May affect ketoconazole levels; concomitant use not recommended
Ketoconazole may increase risk for neurotoxicity; should never be used together in dogs
May increase ketoconazole concentrations
Not recommended together; adrenolytic effects of mitotane may be inhibited by ketoconazole
May decrease ketoconazole levels
Increased gastric pH may reduce ketoconazole absorption
Ketoconazole may increase quinidine levels
May decrease ketoconazole levels; ketoconazole may increase rifampin levels
May reduce absorption of ketoconazole
Ketoconazole may increase levels; hypoglycemia possible
Ketoconazole may decrease serum theophylline concentrations; monitor levels
Ketoconazole may inhibit vinca alkaloid metabolism and increase levels
Ketoconazole may cause increased prothrombin times
Ketoconazole increases blood levels of ciclosporin (used therapeutically to reduce ciclosporin dose requirements)
Used synergistically in systemic fungal disease, allowing for a reduced dose of amphotericin B
Increases gastric pH, which impairs the absorption of ketoconazole; stagger dosing
Increases gastric pH, which impairs the absorption of ketoconazole; stagger dosing
Increases gastric pH, which impairs the absorption of ketoconazole; stagger dosing
Ketoconazole extends the activity of methylprednisolone
Inhibits the metabolism of antihistamines (extrapolated from human data)
Inhibits the metabolism of oral hypoglycaemics (extrapolated from human data)
Inhibits the metabolism of antiepileptics (extrapolated from human data)
Monitorización
- Liver enzymes with chronic therapy (at least every 1-2 months)
- CBC with platelets
- Clinical efficacy
- Adverse effects (GI signs, jaundice)
- Liver function tests (routine monitoring recommended)
- Platelet count (if high doses are used)
- Adrenal function/clinical signs of hypoadrenocorticism
Farmacocinética
Vida media
Absorción
Highly variable oral bioavailability in dogs (4-89%). Absorption is enhanced in an acidic environment and may be increased with food. Poor oral absorption of tablets in horses, but increases to 23% if given with hydrochloric acid, and 60% with oral solution.
Distribución
Distributed into bile, cerumen, saliva, urine, synovial fluid, and CSF (CSF levels <10% of serum). High levels in liver, adrenals, and pituitary gland. 84-99% bound to plasma proteins. Crosses the placenta and is found in milk.
Metabolismo
Extensively metabolized by the liver into several inactive metabolites.
Eliminación
Metabolites are excreted primarily into the feces via the bile. About 13% is excreted into the urine (only 2-4% unchanged).
Sobredosis
No reports of acute toxicity associated with overdosage were located. The oral LD50 in dogs is >500 mg/kg. In the event of an acute overdose, employ supportive measures, including gastric lavage with sodium bicarbonate.
Productos disponibles
Formulaciones
- Oral tablets
- Oral suspension (compounded)
- Topical preparations
- 200 mg oral tablet
Veterinario
- None for systemic use
- Fungiconazole 200 mg tablet
Etiquetado para humanos
- Ketoconazole Tablets: 200 mg (scored)
Estado regulador
POM-V classification
POM-V (Prescription Only Medicine - Veterinarian)
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store tablets at room temperature in well-closed containers. Compounded oral suspensions (20 mg/mL) retain >95% potency for 60 days when stored at 5°C or 25°C and protected from light.
Información para el cliente
- Administración: Administre este medicamento con comida para aumentar la absorción y reducir el malestar estomacal. Si su mascota presenta vómitos o pérdida de apetito, dividir la dosis diaria puede ayudar.
- Efectos secundarios: Esté atento a la pérdida de apetito, vómitos o diarrea. Si ocurren, contacte a su veterinario. En gatos, estos efectos secundarios son más comunes.
- Cambios en el pelaje: Es posible que note un aclaramiento reversible del pelaje de su mascota durante el tratamiento.
- Compromiso: Las infecciones fúngicas a menudo requieren meses de tratamiento continuo. No suspenda el medicamento antes de tiempo aunque su mascota parezca estar mejor, ya que la infección puede regresar fácilmente.
- Advertencia: Informe a su veterinario sobre todos los demás medicamentos que esté tomando su mascota, ya que el ketoconazol interactúa con muchos fármacos.
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.