Ciclosporina
Cyclosporine
Cyclosporin A
También conocido como: Optimmune · Restasis · Atopica · Cyclavance · Modulis · Sporimmune · Cyclosporin A · Ciclosporin · Cyclosporine
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Evidencia posológica v13 auditada
Evidencia estructurada para el cálculoAllergic dermatitis (extra-label)
Requiere verificación veterinaria
- q24-48h
NA
Contexto clínico obligatorio (3)
- NOTE: Dosages are for cyclosporine (modified), Atopica®, Cyclavance®, Neoral®, or equivalent; these dosages are not interchangeable with Sandimmune® (or equivalent) dosages.
- ■ Consider therapeutic drug monitoring (pharmacokinetic and pharmacodynamic) to assess effectiveness of therapy, particularly when response is poor or when adverse effects occur. Therapeutic drug monitoring can also be considered when changing brands or manufacturers, especially if response to therapy changes in the individual patient. Cyclosporine blood concentrations are not typically monitored when treating atopic dermatitis 93 or inflammatory bowel disease 9 because the blood concentrations were found to not correlate with clinical efficacy, but this may be warranted in some cases. 50
- ■ This medication is considered to be a hazardous drug as defined by the National Institute for Occupational Safety and Health (NIOSH). Talk with your veterinarian or pharmacist about the use of personal protective equipment when handling this medicine.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
La ciclosporina es un agente polipeptídico altamente lipofílico aislado originalmente del hongo Tolypocladium inflatum. En oftalmología veterinaria, es el tratamiento fundamental para la queratoconjuntivitis seca (KCS), comúnmente conocida como ojo seco, y la queratitis superficial crónica (Pannus) en perros.
Más allá de sus propiedades estimulantes de la producción lagrimal, la ciclosporina reduce la pigmentación corneal y la granulación asociada con la inflamación crónica. Perla clínica: Debido a que es extremadamente hidrofóbica, las formulaciones oftálmicas requieren vehículos específicos (como aceite de maíz u oliva en gotas magistrales, o bases de ungüento específicas) para lograr la penetración corneal. Por lo general, es segura para el uso tópico a largo plazo sin efectos secundarios inmunosupresores sistémicos.
Mecanismo de acción
Cyclosporine is a calcineurin inhibitor. It binds to cyclophilin within T-lymphocytes, inhibiting the enzyme calcineurin → prevents dephosphorylation of Nuclear Factor of Activated T-cells (NFAT) → blocks transcription of interleukin-2 (IL-2) and other inflammatory cytokines.
In the eye, this halts local inflammatory mediator production, arresting self-perpetuating lacrimal adenitis. It also acts as a prolactin analog, fitting onto lacrimal prolactin receptors to directly stimulate tear production. Furthermore, it increases conjunctival mucin stores, improving the overall quality of the tear film.
Seguridad y advertencias
Contraindicaciones
- Feline keratoconjunctivitis sicca associated with active herpes virus infection
- Feline eosinophilic keratitis (historically, though newer evidence varies, the monograph notes it is not promising)
Efectos adversos
- Mild ocular irritation upon application
- Aggravation of ophthalmic herpes virus infections (especially in cats)
Precauciones
Important: Discontinuation of therapy usually results in the return of clinical signs of KCS within a few days.
Use with caution in the face of ulcerative keratitis, although it is generally considered safe when concurrent antibiotic therapy is administered. Compounded formulations should be avoided if an approved commercial product (Optimmune) is available and effective.
Interacciones farmacológicas
Inhibits cytochrome P450 metabolism of ciclosporin, increasing blood concentrations up to five-fold. Dose reduction (halving dose or doubling interval) is required.
Inhibits cytochrome P450 metabolism of ciclosporin, significantly increasing blood concentrations.
Competitively inhibits enzymes involved in ciclosporin metabolism, increasing serum levels.
Inhibits enzymes involved in ciclosporin metabolism, increasing serum levels.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of hyperkalaemia.
Ciclosporin inhibits MDR1 P-glycoprotein, decreasing the efflux of macrocyclic lactones from the blood-brain barrier, potentially resulting in CNS toxicity.
Monitorización
- Schirmer Tear Test (STT) after 1 month of therapy, then periodically
- Fluorescein staining to monitor for corneal ulceration
- Resolution of corneal pigmentation and neovascularization
Farmacocinética
Vida media
Absorción
Poor systemic absorption across the GI tract. When delivered topically to the eye, it reaches very low systemic concentrations. Trace levels may be detected in blood but clinical implication is uncertain.
Distribución
Concentrates locally in the cornea, conjunctiva, and lacrimal glands.
Metabolismo
Hepatic (Cytochrome P450 3A4) if absorbed systemically.
Eliminación
Primarily biliary/fecal if absorbed systemically.
Sobredosis
Systemic toxicity has not been noted in dogs given this drug chronically via the topical ophthalmic route. Even if 100% of the ophthalmic dose were absorbed, it is well below the systemic therapeutic/toxic dose.
Productos disponibles
Formulaciones
- 0.2% ophthalmic ointment
- 0.05% ophthalmic emulsion
- 1% ophthalmic solution (compounded)
Veterinario
- Cyclosporine Ophthalmic Ointment 0.2% (Optimmune)
Etiquetado para humanos
- Cyclosporine 0.05% Ophthalmic Emulsion (Restasis)
Estado regulador
POM-V classification
POM-V classification
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store at room temperature away from moisture and heat. Keep the tube tightly closed.
Información para el cliente
Manejo del ojo seco de su mascota
- La paciencia es clave: Pueden pasar de 3 a 8 semanas de uso constante antes de observar una mejora notable en la producción de lágrimas. ¡No suspenda el medicamento antes de tiempo!
- Tratamiento de por vida: El ojo seco (KCS) suele ser una afección crónica. Si deja de aplicar el ungüento, es probable que los síntomas de ojo seco regresen en pocos días.
- Aplicación: Aplique una pequeña tira (aproximadamente 1/4 de pulgada) de ungüento directamente en el ojo. Si también está usando lágrimas artificiales, aplique primero las lágrimas artificiales, espere 5-10 minutos y luego aplique el ungüento de ciclosporina.
- Seguridad: Este medicamento es muy seguro para los ojos y no causa los efectos secundarios sistémicos que pueden provocar los esteroides.
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.