Deflazacort; Uses, Dosage, Side Effect, Interactions ,Pregnancy

Deflazacort; Uses, Dosage, Side Effect, Interactions ,Pregnancy

Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It is used in the treatment of Duchenne muscular dystrophy.D eflazacort is a Corticosteroid. The mechanism of action of deflazacort is as a Corticosteroid Hormone Receptor Agonist.

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 

In the United States, deflazacort is also FDA-approved for the treatment of Duchenne muscular dystrophy in people over the age of 5

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Contra-Indications of Deflazacort 

  • Serious infections
  • Herpetic eye infections
  • Hypersensitivity
  • 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

Muscular Dystrophy

  • 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.

Nephrotic syndrome

  • 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.

Rheumatoid arthritis 

  • The maintenance dose is usually within the range 3 – 18 mg/day. The smallest effective dose should be used and increased if necessary.

Bronchial asthma

  • 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

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Common

Rare

Drug Interactions of Deflazacort 

Deflazacort may interact with following drugs, supplyments, & may change the efficacy of drugs

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.

Pregnancy and Lactation of Deflazacort 

FDA pregnancy category: Not Assigned 

Pregnancy

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.

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Lactation

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.

References

  1. Deflazacort

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