imiquimod (Rx)

>10%

Application site reaction (33%)

URTI (15%)

Erythema (54-61%)

Erosion (29-31%)

Excoriation/flaking (18-25%)

Edema (12-17%)

Itching (20%)

1-10%

Sinusitis (7%)

Burning (6%)

Headache (5%)

Carcinoma squamous (4%)

Diarrhea (3%)

Bleeding (3%)

Stinging (3%)

Pain (3%)

Eczema (2%)

Induration (2%)

Tenderness (2%)

Irritation (2%)

Back pain (1%)

Fatigue (1%)

Atrial fibrillation (1%)

Viral infection (1%)

Dizziness (1%)

Vomiting (1%)

UTI (1%)

Fever (1%)

Rigor (1%)

Alopecia (1%)

Frequency Not Defined

Headache

Flu-like symptoms

Myalgia

Contraindications

None

Cautions

Avoid or minimize exposure to sunlight, including sunlamps; wear protective clothing

Do not use until skin has fully healed from previous drug or surgical treatment

Avoid use in patients with pre-existing autoimmune conditions

Safety and efficacy not established for other forms of BCC besides sBCC Safety and efficacy not established for sBCC lesions on head, face or anogenital area

Dosage is different for different indications

Avoid sexual contact while cream is on skin

Aldara: Safety when applied to skin area >252 cm in treatment of actinic keratosis have not been determined

Intense local skin reactions including skin weeping or erosion may occur after few applications; may require interruption of dosing

May exacerbate inflammatory skin conditions such as chronic graft versus host disease

Severe local inflammatory reactions of female external genitalia can lead to severe vulvar swelling, which may lead to urinary retention; dosing should be interrupted or discontinued

A transient increase in lesion counts may be observed during treatment

Not recommended for oral, ophtalmic, urethral, intravaginal, cervical, rectal, or intra-anal human papilloma viral disease

Do not use in children aged 2-12 years with molluscum contagiosum due to studies failing to demonstrate efficacy

Safety and efficacy not established in immunosuppressed patients or those with basal cell nevus syndrome or xeroderma pigmentosum

Caution in patients with pre-existing autoimmune conditions

Flu-like signs and symptoms may accompany or precede local skin reactions (eg, fatigue, fever, nausea, malaise, arthralgias, chills); interrupt treatment and reassess

Pregnancy Category: C

Lactation: Unknown if distributed in breast milk; use caution

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.

Mechanism of Action

Unknown mechanism in treating actinic keratosis and external genital warts; immune response modifier, stimulates release of inflammatory cytokines and proliferation/migration of immune cells

No direct antiviral activity

Absorption

Appears to be dependent on area of application rather than amount applied

Peak plasma concentration (Aldara): 0.1-3.5 ng/mL

Peak plasma concentration (Zyclara): 0.323 ng/mL

Elimination

Excretion: Urine

Topical Administration

External genital warts: Apply prior to normal sleeping hours and leave on skin for approximately 6-10 hr; then wash with mild soap and water; nonocclusive dressings such as cotton gauze/underwear may be used in management of skin reactions

Do not bandage application area

Wash hands before and after application

Zyclara Pump: Prime before first use only by repeatedly depressing actuator until cream is dispensed

Avoid use in or on lips, nostrils or eyes