Aldara

External genital warts, superficial basal cell carcinoma and actinic keratosis:

Less than 0.9% of a topically applied single dose of radiolabelled imiquimod was absorbed through the skin of human subjects. The small amount of drug which was absorbed into the systemic circulation was promptly excreted by both urinary and faecal routes at a mean ratio of approximately 3 to 1. No quantifiable levels (>5 ng/ml) of drug were detected in serum after single or multiple topical doses.

Systemic exposure (percutaneous penetration) was calculated from recovery of carbon-14 from [14C] imiquimod in urine and faeces.

Minimal systemic absorption of imiquimod 5% cream across the skin of 58 patients with actinic keratosis was observed with 3 times per week dosing for 16 weeks. The extent of percutaneous absorption did not change significantly between the first and last doses of this study. Peak serum drug concentrations at the end of week 16 were observed between 9 and 12 hours and were 0.1, 0.2, and 1.6 ng/mL for the applications to face (12.5 mg, 1 single-use sachet), scalp (25 mg, 2 sachets) and hands/arms (75 mg, 6 sachets), respectively. The application surface area was not controlled in the scalp and hands/ arms groups. Dose proportionality was not observed. An apparent half-life was calculated that was approximately 10 times greater than the 2 hour half-life seen following subcutaneous dosing in a previous study, suggesting prolonged retention of drug in the skin. Urinary recovery was less than 0.6% of the applied dose at week 16 in these patients.

Paediatric population

The pharmacokinetic properties of imiquimod following single and multiple topical application in paediatric patients with molluscum contagiosum (MC) have been investigated. The systemic exposure data demonstrated that the extent of absorption of imiquimod following topical application to the MC lesional skin of the paediatric patients aged 6-12 years was low and comparable to that observed in healthy adults and adults with actinic keratosis or superficial basal cell carcinoma. In younger patients aged 2-5 years absorption, based on C_max values, was higher compared to adults.

isostearic acid

benzyl alcohol

cetyl alcohol

stearyl alcohol

white soft paraffin

polysorbate 60

sorbitan stearate

glycerol

methyl hydroxybenzoate (E 218)

propyl hydroxybenzoate (E 216)

xanthan gum

purified water.

Not applicable.

2 years.

Do not store above 25 °C.

Sachets should not be re-used once opened.

Boxes of 12 or 24 single-use polyester/aluminium foil sachets, containing 250 mg of cream.

Not all pack sizes may be marketed.

Dispose of the medication in accordance with local regulations for medical waste.

Meda AB

Pipers väg 2A

170 73 Solna

Sweden

EU/1/98/080/001-002

Date of first authorisation: 18/09/1998

Date of last renewal: 03/09/2008

January 2017

• R52.1 – Chronic intractable pain
• R52.2 – Other chronic pain
• R52.9 – Unspecified pain