Deflazacort is a synthetic, heterocyclic glucocorticoid of the oxazoline class. It is a prodrug that is rapidly hydrolyzed in vivo to its active metabolite, 21-desacetyl deflazacort. It possesses potent anti-inflammatory and immunosuppressive properties, with a claimed lower incidence of certain adverse effects (like weight gain, hypertension, and glucose intolerance) compared to equipotent doses of prednisone, though this remains a subject of clinical debate. It is widely used in India for managing various inflammatory and autoimmune conditions.
Adult: Initial dose varies by condition: Typically 24mg to 120mg per day in single or divided doses. For maintenance, the lowest effective dose should be used, often tapered to 6mg to 24mg daily.
Note: Administer orally, preferably in the morning with food to minimize GI upset. Tablets should be swallowed whole with a glass of water. Do not crush or chew unless specified (some brands offer dispersible tablets). For once-daily dosing, take in the morning to coincide with the body's natural cortisol rhythm and reduce insomnia.
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 increases the synthesis of anti-inflammatory proteins (like lipocortin-1) and decreases the synthesis of pro-inflammatory proteins (like cytokines, chemokines, adhesion molecules, and inflammatory enzymes such as COX-2). It also has profound effects on carbohydrate, protein, and fat metabolism, and influences immune cell function.
Pregnancy: Pregnancy Category C (US FDA). Glucocorticoids cross the placenta. Use only if potential benefit justifies potential fetal risk. Chronic use may be associated with low birth weight and neonatal adrenal suppression. Monitor neonate for hypoadrenalism.
Driving: May cause dizziness, vertigo, or visual disturbances. Patients should be cautioned about operating machinery or driving until they know how the drug affects them.
| Ketoconazole, Itraconazole | Potent CYP3A4 inhibitors; significantly increase deflazacort levels and effects/toxicity. | Major |
| Rifampicin, Phenytoin, Carbamazepine | Potent CYP3A4 inducers; significantly decrease deflazacort levels, reducing efficacy. | Major |
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of gastrointestinal ulceration and bleeding. | Moderate |
| Warfarin | Altered anticoagulant response (may increase or decrease INR); monitor closely. | Moderate |
| Diuretics (e.g., Furosemide, Hydrochlorothiazide) | Enhanced potassium loss, leading to severe hypokalemia. | Moderate |
| Antidiabetic drugs (Insulin, Metformin) | Corticosteroids antagonize hypoglycemic effect; increased dosage of antidiabetics may be needed. | Moderate |
| Live Vaccines (MMR, Varicella, OPV) | Risk of disseminated infection due to immunosuppression; contraindicated. | Major |