Dosing and uses of Aczone (dapsone topical)
Adult dosage forms and strengths
topical geL
- 5% (30g, 60g, or 90g tubes)
- 7.5% (30g, 60g, or 90g pump)
Acne Vulgaris
Apply thin layer to the entire face BID (5% gel) or qDay (7.5% gel); a thin layer can also be applied to other affected areas
If no improvement after 12 weeks, reassess treatment
Pediatric dosage forms and strengths
topical geL
- 5% (30g, 60g, or 90g tubes)
- 7.5% (30g, 60g, or 90g pump)
Acne Vulgaris
<12 years: Safety and efficacy not established
≥12 years: Apply thin layer to the entire face BID (5% gel) or qDay (7.5% gel); a thin layer can also be applied to other affected areas
If no improvement after 12 weeks, reassess treatment
Aczone (dapsone topical) adverse (side) effects
>10%
Dryness (16%)
Erythema (13%)
1-10%
Burning (1%)
Pruritus (1%)
Postmarketing reports
Methemoglobinemia
Warnings
Contraindications
None
Cautions
Cases of methemoglobinemia, with resultant hospitalization reported postmarketing in association with 5% gel formulation; patients with glucose-6-phosphate dehydrogenase deficiency or congenital or idiopathic methemoglobinemia are more susceptible to drug-induced methemoglobinemia; avoid use of 5% gel in those patients with congenital or idiopathic methemoglobinemia
No events of peripheral neuropathy observed with topical dapsone; peripheral neuropathy reported with oral dapsone
Serious skin reactions have not been observed with topical application, but are associated with oral therapy and include toxic epidermal necrolysis, erythema multiforme, morbilliform and scarlatiniform reactions, bullous and exfoliative dermatitis, erythema nodosum, and urticaria
Pregnancy and lactation
Pregnancy category: C
There are no adequate and well controlled studies in pregnant women; shown to have an embryocidal effect in rats and rabbits when administered orally in doses of 75 mg/kg/day and 150 mg/kg/day (approximately 800 and 500 times the systemic exposure observed in human females as a result of use of the maximum recommended topical dose, based on AUC comparisons), respectively
Lactation: Although systemic absorption of dapsone following topical application is minimal relative to oral dapsone administration, it is known that dapsone is excreted in human milk
Because of the potential for oral dapsone to cause adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the topical gel, taking into account the importance of the drug to the mother
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Aczone (dapsone topical)
Mechanism of action
Mechanism of action of dapsone gel in treating acne vulgaris is not known
Sulfone; prevents normal bacterial utilization of para-aminobenzoic acid (PABA) for the synthesis of folic acid by acting as a competitive antagonist of PABA; it is bactericidal and bacteriostatic against Mycobacterium leprae
Absorption
AUC: 415 ± 224 ng•h/mL
Exposure of single 100 mg PO dose is 100 times that of topical 5% BId
Administration
Topical Administration
For topical use only; not for oral, ophthalmic, or intravaginal use
Gently cleanse skin and pat dry
Apply pea-size amount in thin layer to acne affected area
Rub gel in gently and completely
Wash hands after application
