Deflazacort is a synthetic, oxazoline derivative of prednisolone, classified as a glucocorticoid. It is a prodrug that is rapidly hydrolyzed in vivo to its active metabolite, 21-desacetyl deflazacort. It exhibits potent anti-inflammatory and immunosuppressive activity with a potentially improved side effect profile compared to other corticosteroids, particularly regarding lower propensity for weight gain, fluid retention, and hypertension. It is widely used in India for managing inflammatory and autoimmune conditions.
Adult: Initial dose: 0.25 to 1.5 mg/kg/day (typically 6mg to 90mg daily), adjusted based on disease severity. Maintenance: Lowest effective dose. For chronic conditions, often started at 30-60 mg/day, tapered by 3-6 mg every 5-7 days.
Note: Administer orally, preferably in the morning with food to minimize GI upset. Tablet should be swallowed whole with a glass of water. Do not crush or chew. For DMD, administration in the evening may be considered to minimize behavioral side effects.
Deflazacort, via its active metabolite, binds to the cytosolic glucocorticoid receptor (GR). The drug-receptor complex translocates to the nucleus, where it modulates gene transcription. It binds to glucocorticoid response elements (GREs), leading to increased transcription of anti-inflammatory proteins (transactivation) and interacts with transcription factors like NF-ÎșB and AP-1 to repress the transcription of pro-inflammatory genes (transrepression).
Pregnancy: Pregnancy Category C (US FDA). Glucocorticoids cross the placenta. Use only if potential benefit justifies potential fetal risk. Chronic use may lead to fetal adrenal suppression. Monitor neonates for hypoadrenalism. Avoid high doses in first trimester.
Driving: May cause dizziness, vertigo, or visual disturbances. Patients should not drive or operate machinery if they experience these effects.
| Ketoconazole, Itraconazole | Inhibits CYP3A4, increasing Deflazacort levels and toxicity risk. | Major |
| Rifampicin, Phenytoin, Carbamazepine | Induces CYP3A4, decreasing Deflazacort efficacy. | Major |
| Warfarin | Effect may be potentiated or inhibited; monitor INR closely. | Moderate |
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of GI ulceration and bleeding. | Moderate |
| Diuretics (e.g., Furosemide, Hydrochlorothiazide) | Enhanced potassium depletion and hypokalemia. | Moderate |
| Antidiabetic drugs (Insulin, Metformin) | Corticosteroid-induced hyperglycemia may require dose adjustment. | Moderate |
| Live Vaccines (MMR, Varicella, OPV) | Risk of disseminated infection; contraindicated. | Major |
| Digoxin | Risk of digitalis toxicity due to hypokalemia. | Moderate |