Aczone, Avlosulfon , DDS
Classifications: antileprosy (sulfone) agent; Therapeutic: antileprosy; sulfone; immunosuppressant
Pregnancy Category: C
25 mg, 100 mg tablets; 5% gel
Sulfone derivative chemically related to sulfonamides, with bacteriostatic and bactericidal activity similar to that group.
Interferes with bacterial cell growth by competitive inhibition of folic acid synthesis by susceptible organisms. It also
interferes with alternative pathways of complement system.
Drug is effective against dapsone-sensitive multibacillary (borderline, borderline lepromatous, or lepromatous) leprosy,
and dapsone-sensitive paucibacillary (indeterminate, tuberculoid, or borderline tuberculoid) leprosy.
Drug of choice for treatment of all forms of leprosy (unless organism is dapsone resistant). Used in dapsone-sensitive multibacillary
leprosy (with clofazimine and rifampin) and in dapsone-sensitive paucibacillary leprosy (with rifampin, clofazimine, or ethionamide).
Also used prophylactically in contacts of patients with all forms of leprosy except tuberculoid and indeterminate leprosy.
Used for treatment of dermatitis herpetiformis. Gel used for acne vulgaris.
Chemoprophylaxis of malaria (with pyrimethamine), systemic and discoid lupus erythematosus, pemphigus vulgaris, dermatosis
(especially those associated with bullous eruptions, mucocutaneous lesions, inflammation or pustules); rheumatoid arthritis,
allergic vasculitis; treatment of initial episodes of P. carinii pneumonia (with trimethoprim) in limited number of adults with AIDS.
Hypersensitivity to sulfones or its derivatives; advanced renal amyloidosis, anemia, methemoglobin reductase deficiency;
pregnancy (category C).
Sulfonamide hypersensitivity; chronic renal, hepatic, pulmonary, or cardiovascular disease, refractory anemias, albuminuria,
G6PD deficiency, lactation.
Route & Dosage
|Tuberculoid and Indeterminate-type Leprosy
Adult: PO 100 mg/d (with 6 mo of rifampin 600 mg/d) for a minimum of 3 y
Lepromatous and Borderline Lepromatous Leprosy
Adult: PO 100 mg/d for ≥10 y
Child: PO 12 mg/kg/d once daily in combination therapy (max: 100 mg/d)
Adult: PO 50 mg/d, may be increased to 300 mg/d if necessary (max: 500 mg/d)
Prophylaxis for Close Contacts of Patient with Multibacillary Leprosy
Adult: PO 50 mg/d
Child: PO <6 mo, 6 mg 3 times/wk; 623 mo, 12 mg 3 times/wk; 25 y, 25 mg 3 times/wk; 612 y, 25 mg/d
P. carinii Pneumonia Prophylaxis
Adult: PO 50 mg b.i.d. or 100 mg q.d.
Child: PO 2 mg/kg once daily (max: 100 mg/d)
Apply pea-sized amount of gel to affected area b.i.d.
- Give with food to reduce possibility of GI distress.
- Store in tightly covered, light-resistant containers at 15°30° C (59°86° F). Drug discoloration
apparently does not indicate a chemical change.
- Clean skin with soap and water before application.
Adverse Effects (≥1%)Body as a Whole:
Hypersensitivity (cutaneous reactions); erythema multiforme, exfoliative dermatitis, toxic epidermal necrolysis
(rare), allergic rhinitis, urticaria, fever, infectious mononucleosis-like syndrome. CNS:
Headache, nervousness, insomnia
, vertigo; paresthesia, muscle weakness. CV:
Anorexia, nausea, vomiting, abdominal pain; toxic hepatitis,
(reversible with discontinuation of drug therapy); increased ALT, AST, LDH; hyperbilirubinemia. Hematologic:
In patient with or without G6PD deficiency; dose-related hemolysis,
Heinz body formation, methemoglobinemia with cyanosis,
hemolytic anemia; aplastic anemia
(rare), agranulocytosis. Skin:
Drug-induced lupus erythematosus, phototoxicity. Special Senses:
Blurred vision, tinnitus. Other:
Male infertility; sulfone syndrome (fever, malaise, exfoliative dermatitis, hepatic necrosis with jaundice
InteractionsDrug: Activated charcoal
decreases dapsone absorption and enterohepatic circulation; pyrimethamine, trimethoprim
increase risk of adverse hematologic reactions; rifampin
decreases dapsone levels 710 fold.
Rapidly and nearly completely absorbed from GI tract. Peak:
28 h. Distribution:
Distributed to all body tissues; high concentrations in kidney, liver, muscle, and skin; crosses placenta; distributed into
breast milk. Metabolism:
In liver by CYP3A4. Elimination:
7085% in urine; remainder in feces; traces of drug may be found in body for 3 wk after repeated doses. Half-Life:
Assessment & Drug Effects
- Monitor for therapeutic effectiveness that may not appear for leprosy until after 36 mo of therapy. Skin lesions respond
well; recovery from nerve involvement is usually limited.
- Lab tests: Perform baseline then weekly CBC during the first month of therapy, at monthly intervals for at least 6 mo, and
- Determine periodic dapsone blood levels.
- Perform liver function tests in patients who complain of malaise, fever, chills, anorexia, nausea, vomiting, and have jaundice.
Dapsone therapy is usually suspended until etiology is identified.
- Monitor severity of anemia. Nearly all patients demonstrate hemolysis. Manufacturer states that Hgb level is generally decreased
by 12 g/dL; reticulocytes increase by 212%; RBC life span is shortened; and methemoglobinemia occurs in
most patients receiving dapsone.
- Monitor temperature during first few weeks of therapy. If fever is frequent or severe, leprosy reactional state should be
ruled out. Reduction of or interruption of therapy may be sufficient for improvement.
- Report cyanotic appearance or mucous membranes with brownish hue to physician as possible methemoglobinemia.
Patient & Family Education
- Report symptoms of leprosy that do not improve within 3 mo or get worse to physician.
- Report the appearance of a rash with bullous lesions around elbows and other joints promptly. Drug-induced or worsening skin
lesions require withdrawal of dapsone.
- Report symptoms of peripheral neuropathy with motor loss (muscle weakness) promptly.