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 is widely used in the Indian market for its potent anti-inflammatory and immunosuppressive properties, with a claimed better side-effect profile regarding weight gain, glucose metabolism, and bone mineral density compared to other corticosteroids like prednisone, though this is subject to ongoing clinical evaluation.
Adult: Initial dose: 0.25 to 1.5 mg/kg/day (or 6 to 90 mg/day), adjusted based on disease severity and response. Maintenance: Lowest effective dose. For the 6mg/5ml suspension, this translates to variable volumes (e.g., 30 mg dose = 25 ml).
Note: Shake the oral suspension well before each use. Use the calibrated measuring cup or oral syringe provided. Can be taken with or without food, but taking with food may reduce GI upset. Administer preferably in the morning to mimic the body's natural cortisol rhythm and reduce insomnia.
Deflazacort, via its active metabolite, binds to the cytosolic glucocorticoid receptor. The receptor-ligand complex translocates to the nucleus, where it binds to glucocorticoid response elements (GREs) in DNA, leading to modulation of gene transcription. This results in the synthesis of anti-inflammatory proteins (lipocortin-1) and inhibition of the synthesis of pro-inflammatory mediators (cytokines, chemokines, adhesion molecules, enzymes like COX-2).
Pregnancy: Pregnancy Category C (US FDA). Glucocorticoids cross the placenta. Use only if potential benefit justifies potential risk to the fetus. Chronic use may lead to fetal adrenal suppression. Monitor neonates for hypoadrenalism.
Driving: May cause dizziness, vertigo, or visual disturbances. Patients should be cautioned about operating machinery or driving if they experience such effects.
| Ketoconazole, Itraconazole | Inhibit CYP3A4, increasing deflazacort levels and toxicity | Major |
| Rifampicin, Phenytoin, Carbamazepine | Induce CYP3A4, decreasing deflazacort efficacy | Major |
| Warfarin | Altered anticoagulant effect (may increase or decrease) | Moderate |
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of GI ulceration and bleeding | Moderate |
| Diuretics (e.g., Furosemide, Hydrochlorothiazide) | Enhanced potassium loss, leading to severe hypokalemia | Moderate |
| Antidiabetics (Insulin, Metformin) | Corticosteroids increase blood glucose, requiring dose adjustment | Moderate |
| Live Vaccines (MMR, Varicella, OPV) | Risk of disseminated infection due to immunosuppression | Major |