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|Imiquimod

Imiquimod

Trade Names:
Aldara
- Cream 5%

Mechanism of Action

Pharmacology

Unknown; however, imiquimod induces mRNA encoding cytokines, including interferon-alpha at the treatment site.

Pharmacokinetics

Absorption

Minimal percutaneous absorption.

Elimination

Less than 0.9% of topical dose excreted in urine and feces.

Indications and Usage

Treatment of external genital and perianal warts/condyloma acuminata; treatment of clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratosis on the face or scalp in immunocompetent adults; treatment of biopsy-confirmed, primary superficial basal cell carcinoma in immunocompetent adults, with a max tumor diameter of 2 cm located on the trunk, neck, or extremities.

Contraindications

Standard considerations.

Dosage and Administration

Topical Apply cream 3 times/wk (eg, Monday, Wednesday, Friday) prior to sleeping hours, and leave on skin for 6 to 10 hr. Remove cream by washing treated area with mild soap and water. Continue treatment until there is total clearance of genital/perianal warts or for a max of 16 wk. Local skin reactions in treatment area are common. Patients should contact health care provider if experiencing any sign or symptom in the treatment area that restricts or prohibits daily activity or makes continued application of the cream difficult. A rest period of several days may be taken if needed because of the patient"s discomfort or severity of the local skin reaction.

Topical 2 times/wk (eg, Monday and Thursday) for 16 wk to a defined treatment area on face or scalp (but not both concurrently). Treatment area should be 1 contiguous area of approximately 25 cm ² . Before applying, the treatment area should be washed with mild soap and water and allowed to dry thoroughly. Apply prior to normal sleeping hours and leave on skin for about 8 hr, after which time cream should be removed by washing the area with mild soap and water. Treatment should continue for the full 16 wk; however, the treatment period should not be extended beyond 16 wk because of missed doses or rest periods.

Topical 5 times/wk (eg, Monday through Friday) for 6 wk to a biopsy-confirmed superficial basal cell carcinoma. The treatment area should include a 1-cm margin of skin around the tumor. Before applying, the treatment area should be washed with mild soap and water and allowed to dry thoroughly. Apply prior to normal sleeping hours and leave on skin for about 8 hr.

General Advice

• For topical use only. Not for ophthalmic, oral, or intravaginal use.
• Do not cover with occlusive dressings. A porous gauze dressing or cotton underwear may be used to cover application site.
• Assess application site for evidence of recent surgery, or irritation or inflammation from previous or current treatment. Avoid applying cream to these areas until tissue has healed.

Storage/Stability

Store cream below 77°F. Protect from freezing.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

The following adverse reactions occurred with an incidence of at least 1% unless otherwise indicated.

Cardiovascular

Atrial fibrillation; chest pain; hypertension.

CNS

Anxiety; dizziness; fatigue; headache.

Dermatologic

Erythema (97%); flaking/scaling/dryness (93%); scabbing crusting (79%); induration (78%); edema (71%); erosion/ulceration (54%); vesicles (29%); weeping/exudates (22%); alopecia; basal cell carcinoma; dermatitis; eczema; hyperkeratosis; rash; skin disorder; squamous carcinoma.

EENT

Eye abnormality; pharyngitis; rhinitis.

GI

Diarrhea; dyspepsia; gastroesophageal reflux; nausea; vomiting.

Genitourinary

Urinary tract disorder.

Local

Bleeding at target site; burning at remote and target sites; induration at remote and target sites; infection at target site; irritation at remote site; itching at remote and target sites; pain and soreness at target site; papules at target site; procedural site reaction; stinging at target site; tenderness at target site.

Metabolic-Nutritional

Gout; hypercholesterolemia.

Musculoskeletal

Back pain; myalgia; rigors; skeletal pain.

Respiratory

Coughing; sinusitis; upper respiratory tract infection.

Miscellaneous

Abrasion; allergy aggravated; fever; flu-like symptoms; fungal infection; hernia; herpes simplex; infection; inflicted injury; pain; postoperative pain; viral infection.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy in patients with external genital/perianal warts younger than 12 yr of age have not been established. Safety and efficacy in patients with actinic keratosis or superficial basal cell carcinoma younger than 18 yr of age have not been established.

Immunosuppression

Safety and efficacy not established in immunosuppressed patients.

Sunburn

Exposure to sunlight or sunlamps should be avoided or minimized.

Patient Information

• Explain name, dosing, action, and potential side effects of drug, including potential to cause permanent hypopigmentation or hyperpigmentation of the skin.
• Teach patient proper technique for applying cream: wash area to be treated with mild soap and water and allow to dry; wash hands before and after application; open a new packet of cream just before use; apply a thin layer of cream to affected area(s); gently rub cream into affected area(s) until cream is no longer visible.
• Caution patient to avoid contact of the cream with the eyes, lips, nostrils, vagina, and anus. Advise patient if cream gets in mouth or eyes, to rinse well with water right away.
• Caution patient not to cover application site with occlusive dressings. Advise patient that a porous gauze dressing or cotton underwear may be used to cover application site.
• Advise patient that packet of cream is for single use only; discard partially-used packets of cream and do not save for use at a later time.
• Advise patient if a dose is missed, to apply the missed dose of cream as soon as remembered and then continue on the regular regimen.
• Advise patient that response to therapy is slow and may take several weeks to occur.
• Advise patient to temporarily discontinue application of cream if discomfort at application site occurs. Therapy can be restarted when reaction subsides. Instruct patient to promptly notify health care provider if experiencing any sign or symptom at the application site that restricts or prohibits daily activity or makes continued application of the cream difficult.
• Advise patient to avoid unnecessary exposure to direct and indirect sunlight or tanning lamps and to use sunscreen and wear protective clothing to avoid photosensitivity reactions during therapy.
• Advise women to notify health care provider if pregnant, planning to become pregnant, or breastfeeding.
• Instruct patient not to take any prescription or OTC medications, herbal preparations, or dietary supplements unless advised by health care provider.
• Advise patient follow-up visits will be required to monitor therapy and to keep appointments.

• Treatment of genital warts
• Remind patient that cream is applied 3 times/wk (eg, Monday, Wednesday, Friday or Tuesday, Thursday, Sunday) until there is total clearance of genital/perianal warts, or for a max of 16 wk.
• Advise patient to apply cream before bedtime and remove the cream 6 to 10 hr after application by washing with mild soap and water.
• Advise patient that medication is not a cure for genital or perianal warts, and new warts may develop during or after therapy.
• Caution patient it is not known if imiquimod can prevent the spread of genital or perianal warts to others and to practice safer sex.
• Instruct uncircumcised men treating warts under foreskin to retract the foreskin and clean the area daily.
• Caution woman applying cream near opening of vagina to take special care not to accidentally apply to vaginal mucus membranes because of risk of causing severe tissue reaction.
• Caution patient to avoid sexual (genital, anal, oral) contact while cream is on the skin.
• Caution patient that cream may weaken condoms and vaginal diaphragms and to use alternative methods of birth control while cream is on the skin.

• Treatment of actinic keratosis
• Remind patient that cream is applied 2 times/wk (eg, Monday and Thursday or Tuesday and Friday) for 16 wk, even if all of the actinic keratosis appears to be gone, unless advised to do differently by health care provider. Caution patient that treatment period should not extend beyond 16 wk because of missed doses or rest periods.
• Advise patient to apply cream before bedtime and to remove the cream 8 hr after application by washing with mild soap and water.

• Treatment of superficial basal cell carcinoma
• Remind patient that cream is applied 5 times/wk (eg, Monday through Friday) for 6 wk, even if the superficial basal cell carcinoma appears to be gone, unless advised differently by health care provider.
• Advise patient to apply cream before bedtime and to remove the cream 8 hr after application by washing with mild soap and water.