Cortisone Acetate
**Cortisone acetate** is an oral corticosteroid that possesses both **glucocorticoid** and **mineralocorticoid** effects. Key clinical highlights: * **Prodrug Nature**: It is biologically inactive until converted in vivo to cortisol (hydrocortisone) by the liver. * **Addison's Disease Management**: It serves as a potential alternative to prednisolone for the oral treatment of hypoadrenocorticism (Addison's disease) in dogs. Because it provides both glucocorticoid and mineralocorticoid activity, it may reduce the dosage requirements for primary mineralocorticoid drugs (like fludrocortisone), potentially lowering overall treatment costs. * **Controversy**: Its use in veterinary medicine is relatively uncommon, and whether its increased mineralocorticoid activity offers a clinically significant benefit over standard prednisolone therapy remains debated among endocrinologists. * **Safety Profile**: When used at physiologic replacement doses for Addison's disease, it is generally very well tolerated. Supra-physiologic doses will induce typical corticosteroid adverse effects (e.g., PU/PD/PP, panting, immunosuppression).
Mecanismo: Cortisone acetate is a prodrug. Upon oral absorption, it undergoes first-pass hepatic metabolism where the enzyme **11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)** converts it into the active hormone, **cortisol**. * **Glucocorticoid Action**: Cortisol diffuses across cell membranes and binds to cytosolic **glucocorticoid receptors (GR)** → the receptor-ligand complex translocates to the nucleus → binds to glucocorticoid response elements (GREs) on DNA → alters gene transcription (transactivation of anti-inflammatory proteins and transrepression of pro-inflammatory cytokines). * **Mineralocorticoid Action**: Cortisol also binds to **mineralocorticoid receptors (MR)** in the distal renal tubules → promotes sodium retention and potassium excretion, which is critical for patients with hypoadrenocorticism.
Dosificación por especie
- Long-term treatment of hypoadrenocorticism (changeover period) · 0.5-1 mg/kg PO q12-24h · PO · q12-24h · Initial stabilization · Used initially with a semi-selective mineralocorticoid (fludrocortisone).
- Long-term treatment of hypoadrenocorticism (maintenance) · 0.5 mg/kg PO q12-24h · PO · q12-24h · Long-term · Provides adequate additional glucocorticoid supplementation once stable.
Las dosis son una referencia clínica para veterinarios colegiados. Confirme siempre con la ficha técnica vigente y el paciente individual.
Vías de administración
Contraindicaciones
- Hypersensitivity to cortisone acetate
- Systemic fungal infections (general corticosteroid contraindication)
Efectos adversos
- Vomiting
- Inappetence
- Diarrhea
- Hypersensitivity reactions (rare)
- Polyuria/Polydipsia/Polyphagia (at supra-physiologic doses)
- Panting (at supra-physiologic doses)
- Immunosuppression (at supra-physiologic doses)
Interacciones farmacológicas
- Amphotericin B · Concomitant use may cause hypokalemia; risk of CHF and cardiac enlargement reported in humans.
- Aspirin · Glucocorticoids may reduce salicylate blood levels and increase risk for GI ulceration/bleeding.
- Diuretics, Potassium-Depleting (e.g., furosemide, thiazides) · Concomitant administration may cause hypokalemia.
- Estrogens · May potentiate the effects of hydrocortisone/glucocorticoids.
- Insulin and Antidiabetic Agents · Insulin requirements may increase due to glucocorticoid-induced insulin resistance.
- Mitotane · May alter steroid metabolism; higher doses of steroids may be needed to treat mitotane-induced adrenal insufficiency.
- NSAIDs · Increased risk of gastrointestinal ulceration and bleeding.
- Vaccines (Live attenuated) · Virus replication may be augmented if given at immunosuppressive doses; diminished immune response to killed vaccines/toxoids.
- Warfarin · May affect INR values; requires monitoring.
Monitorización
- Weight, appetite, signs of edema
- Serum and/or urine electrolytes (Na+, K+)
- Total plasma proteins, albumin
- Blood glucose
- Growth and development in young animals
- ACTH stimulation test (Note: Cortisone cross-reacts with cortisol assays; must test before administration)
Sobredosis
Acute ingestion is rarely a clinical problem, and severe clinical effects are unlikely with a single acute overdose. However, neuropsychiatric effects can occur. Cardiac arrhythmias and anaphylaxis are theoretically possible but very rare. Treatment is generally supportive.
La referencia de fármacos de VetSheet está destinada a veterinarios colegiados como apoyo a la decisión clínica, no sustituye el juicio profesional ni la ficha técnica vigente del fabricante.