Imiquimod

Topical overdosing of Aldara Cream could result in an increased incidence of severe local skin reactions and may increase the risk for systemic reactions.

The most clinically serious adverse event reported following multiple oral imiquimod doses of >200 mg (equivalent to imiquimod content of >16 packets) was hypotension, which resolved following oral or intravenous fluid administration.

Imiquimod is an immune response modifier. Imiquimod topical is used to treat actinic keratosis (a condition caused by too much sun exposure) on the face and scalp.

Imiquimod topical (for the skin) is also used to treat a minor form of skin cancer called superficial basal cell carcinoma, when surgery would not be an appropriate treatment.

Imiquimod topical also treats genital warts that appear on the outside of the body, but this medicine is not a cure for genital warts. Imiquimod may be used in adults and children who are at least 12 years.

Imiquimod topical may also be used for purposes not listed in this medication guide.

Apply imiquimod cream exactly as prescribed. Follow the directions on your prescription label carefully.

For external genital and perianal warts imiquimod cream is usually used once a day for 3 days a week for 16 weeks.

For actinic keratosis imiquimod cream is usually used once a day for 2 days a week, 3 to 4 days apart for 16 weeks.

For superficial basal cell carcinoma imiquimod cream is usually used once a day for 5 days a week for 6 weeks.

Leave the cream on the affected area or areas for the time your doctor recommends. The length of time that imiquimod cream is left on the skin is not the same for the different skin conditions that imiquimod cream is used to treat. Do not bathe or get the treated area wet before the right time has passed. Do not leave imiquimod cream on your skin longer than prescribed.

Absorption

Bioavailability

Absorbed systemically following topical application to skin.1 Systemic exposure appears to be related to surface area of application site rather than total applied dose.1

Distribution

Not known whether crosses placenta following topical application.1

Not known whether distributed into milk following topical application.1

Elimination

Elimination Route

Following topical application to the skin in adults with actinic keratosis (75-mg doses 3 times weekly for 16 weeks), 0.08–0.15% of topical dose is eliminated in urine as unchanged drug and metabolites.1

Following topical application in patients with HPV warts, 0.11 or 2.41% of topical dose is eliminated in urine as unchanged drug and metabolites in men or women, respectively.1

Half-life

Apparent half-life following topical application is approximately 10 times greater than that reported following sub-Q administration (2 hours); this indicates prolonged retention in skin.1

Storage

Topical

4–25°C; avoid freezing.1

(i mi KWI mod)

• Aldara
• Zyclara
• Zyclara Pump

• Skin and Mucous Membrane Agent
• Topical Skin Product

Note: Frequency of reactions vary and are related to the degree of inflammation associated with the treated disease, number of weekly applications, product formulation, and individual sensitivity.

>10%:

Dermatologic: Localized erythema (58% to 100%; remote: 2%), xeroderma (local; including flaking, scaling; 18% to 93%; remote: 1%), crusted skin (local; 4% to 93%), skin sclerosis (local; 5% to 84%), dermal ulcer (local; 4% to 62%; remote: 2%), localized vesiculation (2% to 31%), excoriation (local; remote: 1%)

Infection: Fungal infection (2% to 11%)

Local: Localized edema (12% to 78%; remote: 1%), application site discharge (22% to 51%), local pruritus (3% to 32%), localized burning (9% to 26%)

Respiratory: Upper respiratory tract infection (15% to 33%)

1% to 10%:

Cardiovascular: Chest pain, localized blanching

Central nervous system: Headache (2% to 6%), fatigue (1% to 4%), dizziness (<1% to 3%), local discomfort (soreness; ≤3%), rigors (1%), anxiety, pain, tingling of skin (local)

Dermatologic: Skin pain (local; 1% to 8%), skin hypertrophy (local; 3%), skin infection (local; 1% to 3%), eczema (2%), cheilitis (≤2%), alopecia (1%), dermal hemorrhage (local), localized rash, papule (local), seborrhoeic keratosis, skin tenderness (local), stinging of the skin (local), tinea (cruris)

Endocrine & metabolic: Increased serum glucose

Gastrointestinal: Nausea (1% to 4%), diarrhea (1% to 3%), anorexia (≤3%), vomiting (1%), dyspepsia

Genitourinary: Bacterial vaginosis (3%), urinary tract infection (1%)

Hematologic & oncologic: Squamous cell carcinoma (4%), lymphadenopathy (2% to 3%)

Infection: Herpes simplex (≤3%)

Local: Local irritation (3% to 6%)

Neuromuscular & skeletal: Arthralgia (1% to 3%), myalgia (≥1%), back pain

Respiratory: Sinusitis (7%), flu-like symptoms (<1% to 4%), cough, pharyngitis, rhinitis

Miscellaneous: Fever (≤3%)

Postmarketing and/or case reports (Limited to important or life-threatening): Acute exacerbations of multiple sclerosis, anemia, angioedema, atrial fibrillation, capillary leak syndrome, cardiac failure, cardiomyopathy, cerebrovascular accident, depression, erythema multiforme, erythema (scrotal), exacerbation of ulcerative colitis, exfoliative dermatitis, febrile seizures, hepatic insufficiency, Henoch-Schönlein purpura (IgA vasculitis), herpes zoster, hyperpigmentation, immune thrombocytopenia (ITP), ischemia, leukopenia, malignant lymphoma, myocardial infarction, pain (scrotal), palpitations, pancytopenia, paresis, proteinuria, psoriasis (onset or exacerbated), pulmonary edema, scrotal edema, seizure, squamous cell carcinoma, supraventricular tachycardia, syncope, tachycardia, thrombocytopenia, thyroiditis, ulcerative colitis, ulcer (scrotal), urinary retention, vertebral disk disease (spondylitis onset or exacerbated)

3.75% cream: Apply a thin layer topically to external genital/perianal warts once a day prior to bedtime. Up to 0.25 g (1 packet or 1 full actuation of the pump) may be applied to the treatment area at each application. The cream should be left on for approximately 8 hours and then removed by washing with mild soap and water.

Treatment should continue until total clearance of genital/perianal warts or for up to 8 weeks. The treatment period should not be extended beyond 8 weeks due to rest periods or missed doses.

5% cream: Apply topically to external genital/perianal warts 3 times per week prior to bedtime. The cream should be applied as a thin layer to the wart area and rubbed in until it disappears. The cream should be left on for 6 to 10 hours and then removed by washing with mild soap and water.

Treatment should continue until total clearance of genital/perianal warts or for a maximum of 16 weeks.

Data not available