Deflazacort is a synthetic glucocorticoid, with anti-inflammatory and immunomodulating properties. It is a prodrug, converts to active metabolite by plasma esterases.
It has approved by the FDA to manage Duchenne Muscular Dystrophy (DMD). With less adverse effects on bone health and weight than other steroids, it improves the lives of children with DMD by delaying the development of muscle-related problems. Although the precise method by which deflazacort exerts its therapeutic effects in DMD patients is unclear, it most likely happens as a result of its anti-inflammatory properties.
This newer steroid has a little lower glucocorticoid potency than prednisolone but no mineralocorticoid activity. Although it is asserted to have fewer side effects, it could be because of its lesser potency. It has been specifically advised for paediatric patients since in some studies it showed less growth retardation in children.
There is no information on the use of deflazacort during breastfeeding, an alternate corticosteroid may be preferred, especially while nursing a newborn or preterm infant.
Drug class
Glucocorticoid, intermediate acting
Glucocorticoid receptor agonist
Available preparation
- Tablet: 6 mg, 12 mg, 18 mg, 30 mg
- Syrup: 6 mg/5 ml
Dosage
- Adult: 12 – 30 mg daily
- Children: 6 – 18 mg daily (0.9 mg/kg/day)
Common uses
- Duchenne Muscular Dystrophy
- Inflammatory disorders
- Immunological disorders
Side effects
- Weight gain
- Deflazacort, as a steroid prodrug used over a long-term period, can cause hormone imbalance leading to diseases such as Cushing’s Syndrome and hypothalamic-pituitary-adrenal axis suppression.
- It can predispose to infection, as it promotes immunosuppression.
- Chronic use in mice for 2 years in one study resulted in a higher rate of osteoma and osteosarcomas in mice.
Pharmacological characteristics
- Half-life (t1/2): 1.1 – 1.9 hours
- Duration of action: 12-36 hours
- It is rapidly absorbed when taken orally, reaching its peak concentration in one to two hours.
- coadministration of deflazacort crushed with food or applesauce did not affect absorption or bioavailability.
- Metabolized by plasma esterases to active metabolite 21-desacetyl deflazacort (21-deflazacort). then further metabolized by CYP3A4 to inactive metabolite Deflazacort 21-OH and deflazacort 6-beta-OH to eliminate.
- About 70% excreted in urine, remainder (about 30%) excreted in faces.
- The protein binding of the active metabolite of deflazacort is approximately 40%