ABSTRACT
Imiquimod cream 5%, a toll-like receptor 7 agonist, induces alpha-interferon upon topical application, prompting off-label usage to treat children with molluscum contagiosum. We conducted an open-label study to measure serum drug concentration in children aged 2-12 years with extensive molluscum contagiosum (> or = 10% total body surface area). Dependent on extent of subject disease and weight, one to three packets (12.5 mg imiquimod per packet) were applied per dose, three times per week for 4 weeks. Serum imiquimod and metabolite concentrations were measured at pre dose and 2, 4, and 8 hours postdose 1 and dose 12. Thirty children were screened; 22 children (64% boys; 91% white; mean age 6.2 +/- 2.87 years; median involved body area treated 13.5%) were enrolled. Peak serum imiquimod concentrations following single and multiple dosing were low (< 10 ng/mL). Imiquimod concentrations increased 2- to 3.5-fold with multiple dosing. After single and multiple dosing, peak serum imiquimod (Pearson correlation r = 0.4989 and 0.7219, p < 0.05 both, respectively) and area under the serum concentration-time curve values (r = 0.4989 and 0.7219, p < 0.05 both, respectively) correlated with dose normalized for body weight (mg/kg). Systemic drug levels were low after single and multiple doses of imiquimod 5% cream in children.
Subject(s)
Aminoquinolines/pharmacokinetics , Aminoquinolines/therapeutic use , Molluscum Contagiosum/diagnosis , Molluscum Contagiosum/drug therapy , Administration, Topical , Age Factors , Aminoquinolines/blood , Area Under Curve , Child , Child, Preschool , Dose-Response Relationship, Drug , Drug Administration Schedule , Female , Follow-Up Studies , Humans , Imiquimod , Interferon Inducers/blood , Interferon Inducers/pharmacokinetics , Interferon Inducers/therapeutic use , Male , Maximum Tolerated Dose , Probability , Risk Assessment , Severity of Illness Index , Sex Factors , Single-Blind Method , Treatment OutcomeABSTRACT
BACKGROUND: A shorter dosing regimen of imiquimod for the treatment of actinic keratosis may be effective, with long-term clinical benefits. OBJECTIVE: Imiquimod in one or two shorter courses of treatment was evaluated. METHODS: Patients with actinic keratosis lesions on the head applied imiquimod or vehicle cream 3x/wk for 4 weeks (course 1). Patients with remaining lesions received another course of treatment. Complete and partial clearance rates were evaluated after course 1, after course 2 (overall), and 1 year later. RESULTS: Complete clearance rates were 26.8% (course 1) and 53.7% (overall). Partial clearance rates were 36.6% (course 1) and 61.0% (overall). One-year follow-up recurrence rates were 39% (imiquimod) and 57% (vehicle). LIMITATIONS: Blinded investigators may have been biased toward patients treated with imiquimod identified by treatment site reactions. CONCLUSION: Imiquimod 3x/wk in one or two courses of treatment appears to be effective for the treatment of actinic keratoses on the head, providing long-term clinical benefits. Some recurrences do occur, so long-term follow-up is recommended.
