Deflazacort is used in the treatment of various conditions like allergic joint, and muscle disorders. Use with caution in diabetes, gastrointestinal disorders, and bone disorders. Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It was approved in February 2017 by the FDA for use in the treatment of Duchenne muscular dystrophy.
Mechanism of Action of Deflazacort
Deflazacort is a corticosteroid prodrug, whose active metabolite, 21-desDFZ, acts through the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects. The precise mechanism by which deflazacort exerts its therapeutic effects in patients with DMD is unknown.
Clinical studies have indicated that the average potency ratio of deflazacort to prednisolone is 0.69–0.89 and 6 mg of deflazacort is equivalent to 5 mg of prednisolone. However, the therapeutic dosage ratio has been reported to range from 1:1.2 to 1:1.5 Due to the short pharmacokinetic half-life of its active metabolite, pharmacodynamic effects of deflazacort are of shorter duration than those of methylprednisolone and prednisolone.
Indications of Deflazacort
- Duchenne’s Muscular Dystrophy
- Myesthenia Gravis
- Deflazacort is a corticosteroid indicated for the treatment of Duchenne muscular dystrophy (DMD) in patients 5 years of age and older
- Acute interstitial nephritis
- Mixed connective tissue disease (other than systemic sclerosis)
- Crohn’s disease
- Idiopathic thrombocytopenic purpura
- Juvenile chronic arthritis
- Severe hypersensitivity reactions
- Immunosuppression in transplantation
- Acute and lymphatic leukemia
- Malignant lymphoma
- Multiple myelomas
- Muscular Dystrophy
- Rheumatoid arthritis
- Polymyalgia rheumatica
- Nephrotic syndrome
- Polyarteritis nodosa
- Pyoderma gangrenosum
- Systemic lupus erythematosus
- Ulcerative colitis
- Autoimmune haemolytic anaemia
- Autoimmune haemolytic anaemia, idiopathic thrombocytopenic purpura
- Acute and lymphatic leukaemia, malignant lymphoma, multiple myeloma
- Immune suppression in transplantation
In the United States, deflazacort is also FDA-approved for the treatment of Duchenne muscular dystrophy in people over the age of 5
Contra-Indications of Deflazacort
- Serious infections
- Herpetic eye infections
- Pregnancy and lactation
- Receiving live virus immunization
- HBsAg-positive chronic active hepatitis
- Two months before and fourteen days after prophylactic vaccination
- Herpes simplex infection
- Herpes zoster infection
- Other viral infections
- Hypersensitivity to prednisolone or any of the excipients
- Systemic infections unless specific anti-infective therapy is employed.
- Ocular herpes simplex because of possible perforation.
Dosage of Deflazacort
Strengths : 6mg, 18mg ,24mg , 30mg , 36mg ;Oral suspension 22.75mg/mL
- 0.9 mg/kg orally once a day
Pediatric Muscular Dystrophy
- 5 years or older: 0.9 mg/kg orally once a day
Duchenne Muscular Dystrophy
- Indicated for Duchenne muscular dystrophy (DMD)
- 0.9 mg/kg/day
Juvenile chronic arthritis
- The usual maintenance dose is between 0.25 – 1.0 mg/kg/day.
- Initial dose of usually 1.5 mg/kg/day followed by down titration according to clinical need.
- Bronchial asthma: On the basis of the potency ratio, the initial dose should be between 0.25 – 1.0 mg/kg deflazacort on alternate days.
- The maintenance dose is usually within the range 3 – 18 mg/day. The smallest effective dose should be used and increased if necessary.
- In the treatment of an acute attack, high doses of 48-72 mg/day may be needed depending on severity and gradually reduced once the attack has been controlled.
Side Effects of Deflazacort
The most common
- Weight gain
- Swelling of the eyelids or around the eyes, face, lips, or tongue
- Mouth dryness in the early stages
- Abdominal or stomach pain
- cold or flu symptoms such as stuffy nose, sore throat, fever;
- Nausea ,vomiting,
- painful or swollen gums
- numbness or heavy feeling in the jaw
- dull, aching pain in the hip, groin, or thigh
- stomach pain,
- reversible hair loss or thinning, and
- chills or fever
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- excessive sweating
- sudden drowsiness or need to sleep
- coughing up blood
- liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite,
- change in vision
- chest pain or tightness
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- extra heartbeats
- cold and clammy skin
- fast and shallow breathing
- swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
- fast or abnormal heart rate or palpitations
- loss of appetite
- lower back, side, or stomach pain
- mental depression
- muscle pain or cramps
- Swelling of your feet or ankles
- Shortness of breath
- Nausea, fever, dark urine, loss of appetite
Drug Interactions of Deflazacort
Deflazacort may interact with following drugs, supplyments, & may change the efficacy of drugs
- “azole” antifungal medications (e.g., fluconazole, itraconazole, ketoconazole)
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., clonazepam, diazepam, lorazepam)
- beta-blockers (e.g., atenolol, metoprolol, propranolol)
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, )
May increase the anticoagulant effect of coumarins. May prolong relaxation and acute myopathy when given w/ non-depolarising muscle relaxants. Increases the renal clearance of salicylates, steroid withdrawal may lead to salicylate intoxication.
Increased serum concentrations w/ oral contraceptives. Reduced bioavailability w/ antacids. Increased risk of tendonitis and tendon rupture if concomitantly used w/ quinolones.
FDA pregnancy category: Not Assigned
The ability of corticosteroids to cross the placenta varies between individual drugs, however, deflazacort does cross the placenta. Administration of corticosteroids to pregnant animals can cause abnormalities of foetal development including cleft palate, intra-uterine growth retardation and effects on brain growth and development. There is no evidence that corticosteroids result in an increased incidence of congenital abnormalities, such as cleft palate/lip in man.
Corticosteroids are excreted in breast milk, although no data are available for deflazacort. Doses of up to 50 mg daily of deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breast feeding are likely to outweigh any theoretical risk.