Dapsone is a sulfone antimicrobial agent. The mechanism of action of the sulfones is similar to that of the sulfonamides, but the sulfones are predominantly used in the treatment of leprosy. Sulfonamides are competitive antagonists of paraaminobenzoic acid (PABA) and prevent normal bacterial utilization of PABA for the synthesis of folic acid. In the treatment of dermatological diseases, the anti-inflammatory action of dapsone is not fully understood, but it does not appear to be associated with its antibacterial action.
藥動學
Dapsone is acetylated in the liver and 85% renal excretion. Patients may have slow or fast acetylation rates.Elimation half-life is 10 to 50 hours, average 28 hours.
禁忌症
Hypersensitive to dapsone
懷孕分類
C [FDA]
哺乳分類
Enters breast milk/not recommended
副作用
Abdominal pain, nausea and vomiting, reticulocyte increase and hemolysis (dose related; associated with G6PD deficiency), Agranulocytosis, anemia, Erythema nodosum, Cholestatic jaundice syndrome (rare), Toxic hepatitis, Inflammation of skin and subcutaneous tissue, Peripheral neuropathy, Blurred vision, Acute renal failure.
劑量和給藥方法
Dermatitis herpetiformis:initial, 50 mg QD orally; maintenance 50 to 300 mg QD or higher to achieve full control; reduced to minimum maintenance dose as soon as symptom improvement occurs.
Leprosy: 100 mg QD in combination with one or more anti-leprosy drugs (rifampin, clofazimine or ethionamide) for 3 to 10 year.
Pediatrics: 1-2 mg/kg/day, up to a maximum of 100 mg/day, in combination with other antileprosy agent. Do not give with antacids, alkaline foods.