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Imiquimod

Pronunciation

Pronunciation: im-I-kwi-mod
Class: Immunomodulator, topical

Trade Names

Aldara
- Cream, topical 5%

Zyclara
- Cream, topical 3.75%

Pharmacology

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

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Pharmacokinetics

Absorption

C max of 0.323 ng/mL following application of 18.75 mg/day for patients with actinic keratosis; T max occurred 9 h after dosing, and steady state occurred by day 7. C max of 0.488 ng/mL following application of up to imiquimod 9 mg on external genital warts patients; T max occurred 12 h after dosing, and steady state occurred by day 7.

Elimination

Plasma half-life is 29.3 ± 17 h and 24.1 ± 12.4 h in actinic keratosis and external genital warts patients, respectively. Approximately 0.11% to 2.41% of topical dose is excreted in the urine in patients with genital/perianal warts.

Special Populations

Renal Function Impairment

No data available.

Hepatic Function Impairment

No data available.

Indications and Usage

Treatment of external genital and perianal warts (condyloma acuminata) in patients 12 y and older; treatment of clinically typical, nonhyperkeratotic, nonhypertrophic, visible or palpable actinic keratosis on the face or balding 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 (excluding anogenital skin), neck, or extremities (excluding hands and feet), only when surgical methods are medically less appropriate and patient follow-up can be reasonably assured ( Aldara only).

Contraindications

None well documented.

Dosage and Administration

External Genital Warts
Adults and Children 12 y and older 3.75% Cream

Topical Apply cream once daily prior to bedtime and leave on the skin for approximately 8 h. Remove cream by washing the area with mild soap and water. No more than 1 packet should be applied to the treatment area at each application. Continue treatment until there is total Cl or for up to 8 wk.

5% Cream

Topical Apply cream 3 times per week (eg, Monday, Wednesday, Friday) prior to bedtime, and leave on skin for 6 to 10 h. Remove cream by washing treated area with mild soap and water. Continue treatment until there is total Cl of genital/perianal warts, or for a max of 16 wk.

Actinic Keratosis
Adults 3.75% cream

Topical Apply once daily before bedtime to the skin of the affected area (face or balding scalp) for two 2-wk treatment cycles separated by a 2-wk no-treatment period. Up to 2 packets may be applied to the treatment area at each application. Cream should be left on the skin for approximately 8 h, after which time the cream should be removed by washing the area with mild soap and water.

5% cream

Topical Apply 2 times per week (eg, Monday and Thursday) before bedtime 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 . No more than 1 packet should be applied to the contiguous treatment area at each application. Leave cream on skin for about 8 h, after which time cream should be removed by washing the area with mild soap and water.

Superficial Basal Cell Carcinoma (5% Cream Only)
Adults

Topical Apply cream once per day before bedtime 5 times per week for 6 wk. The treatment area should include a 1 cm margin of skin around the tumor. Leave cream on skin for approximately 8 h. Following treatment period, remove the cream by washing the area with mild soap and water.

General Advice

  • For topical use only. Not for ophthalmic, oral, or intravaginal use. Avoid contact with the eyes, lips, and nostrils.
  • Before applying the 5% cream on actinic keratosis or superficial basal cell carcinoma patients, wash the treatment area with mild soap and water and allow it to dry thoroughly.
  • 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.
  • Wash hands before and after cream application.
  • Local skin reactions in treatment area are common. A rest period of several days may be taken if needed because of the patient's discomfort or severity of the local skin reaction; treatment may resume once reaction subsides.
  • Do not extend treatment periods because of missed doses or rest periods.

Storage/Stability

Store between 39° and 77°F for the 5% cream or between 59° and 86°F for the 3.75% cream. Protect from freezing. Discard unused or partially used packets.

Drug Interactions

None well documented.

Adverse Reactions

Cardiovascular

Atrial fibrillation (1%); arrhythmias (palpitations, supraventricular tachycardia), capillary leak syndrome, cardiac failure, cardiomyopathy, cerebrovascular accident, Henoch-Schönlein purpura syndrome, ischemia, MI, pulmonary edema, syncope (postmarketing).

CNS

Headache (8%); fatigue (4%); dizziness (3%); anxiety (1%); agitation, convulsions (including febrile convulsions), depression, insomnia, multiple sclerosis aggravation, paresis, suicide (postmarketing).

Dermatologic

Eczema (2%); alopecia (1%); erythema multiforme, exfoliative dermatitis, hyperpigmentation, hypertrophic scar (postmarketing).

GI

Nausea (4%); anorexia, diarrhea, (3%); dyspepsia (2%); vomiting (1%); abdominal pain (postmarketing).

Genitourinary

Bacterial vaginitis (3%); UTI (1%); dysuria, proteinuria, urinary retention (postmarketing).

Hematologic

Decreases in RBC, WBC, and platelet counts (including idiopathic thrombocytopenic purpura), lymphoma (postmarketing).

Local

Erythema (100%); flaking/scaling/dryness, scabbing/crusting (93%); induration (84%); edema (78%); erosion (66%); erosion/ulceration (62%); weeping/exudate (51%); application-site reaction (33%); itching (32%); vesicle (31%); burning, excoriation/flaking (26%); pain (8%); irritation (6%); bleeding, soreness, stinging (3%); papule, tenderness (2%); hypopigmentation, rash, tinea cruris, sensitivity (more than 1%); infection (1%); tingling (postmarketing).

Musculoskeletal

Back pain (4%); myalgia, rigors (1%); arthralgia (postmarketing).

Respiratory

Upper respiratory tract infection (15%); sinusitis (7%); rhinitis (3%); coughing (2%); pharyngitis (1%); dyspnea (postmarketing).

Miscellaneous

Fungal infection (11%); carcinoma squamous (4%); herpes simplex, influenza-like symptoms, lymphadenopathy, pain, pyrexia (3%); chest pain (2%); viral infection (1%); abnormal liver function, angioedema, thyroiditis (postmarketing).

Precautions

Monitor

Periodically assess and document response to therapy. Assess application site and surrounding areas for local skin reaction (eg, edema, erosion, erythema, excoriation).


Pregnancy

Category C .

Lactation

Undetermined.

Children

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

Photosensitivity

Avoid or minimize exposure to sunlight or sunlamps.

Immunosuppression

Safety and efficacy not established in immunosuppressed patients; use with caution in patients with preexisting autoimmune conditions.

Local inflammatory reactions

May exacerbate inflammatory conditions of the skin, including chronic graft versus host disease.

Lymphadenopathy

May occur.

Systemic reactions

Flu-like symptoms may accompany or precede local inflammatory reactions and may include arthralgia, chills, fever, malaise, myalgias, nausea, and rigors. Consider an interruption of dosing if this occurs.

Overdosage

Symptoms

Severe local skin reactions, hypotension.

Patient Information

  • Explain name, dosing, action, and potential adverse 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, and nostrils. 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 the packet of cream is for single use only, and to discard partially used packets of cream and 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 patients that response to therapy is slow and may take several weeks to occur.
  • Inform patients that it is common to experience local skin reactions (ranging from mild to severe in intensity) during treatment with imiquimod cream, and that these reactions may extend beyond the application site onto the surrounding skin. Inform patients that potential local skin reactions include erythema, edema, vesicles, erosion/ulceration, weeping/exudate, flaking/scaling/dryness, and scabbing/crusting. Patients may also experience application-site reactions, such as pain, itching, and/or burning.
  • Advise patients to temporarily discontinue application of cream if discomfort at application site occurs. Therapy can be restarted when reaction subsides. Instruct patient to promptly notify their health care provider if they experience any sign or symptom at the application site that restricts or prohibits daily activity or makes continued application of the cream difficult.
  • Advise patients that because of local skin reactions, the treatment area is likely to appear noticeably different from healthy skin during treatment and until healed.
  • 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.
  • Inform patients that localized hypopigmentation and hyperpigmentation following imiquimod use have been reported and that these skin color changes may be permanent in some patients.
  • Treatment of genital warts
  • Remind patient that the 5% cream is applied 3 times per week (eg, Monday, Wednesday, and Friday, or Tuesday, Thursday, and Sunday) or once daily for the 3.75% cream until there is total clearance of genital/perianal warts, or for a max of 16 wk for the 5% cream or for up to 8 wk for the 3.75% cream.
  • Advise patient to apply cream before bedtime and remove the cream 6 to 10 h after application by washing with mild soap and water.
  • Advise patient that medication is not a cure for genital or perianal warts, and that 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 safe sex.
  • Instruct uncircumcised men treating warts under foreskin to retract the foreskin and clean the area daily.
  • Caution women applying cream near opening of vagina to take special care not to accidentally apply to vaginal mucous membranes because of the 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 patients that the 5% cream strength is applied 2 times per week (eg, Monday and Thursday, or Tuesday and Friday) for 16 wk, even if all of the actinic keratosis appears to be gone, unless advised differently by their health care provider. Caution patient that treatment period should not extend beyond 16 wk because of missed doses or rest periods.
  • Remind patient that the 3.75% cream strength is applied once daily for two 2-wk treatment cycles separated by a 2-wk no-treatment period. Treatment should continue for the full treatment course even if all actinic keratoses appear to be gone.
  • Advise patient to apply cream before bedtime and to remove the cream 8 h after application by washing with mild soap and water.
  • Treatment of superficial basal cell carcinoma
  • Remind patient that cream is applied 5 times per week (eg, Monday through Friday) for 6 wk, even if the superficial basal cell carcinoma appears to be gone, unless advised differently by their health care provider.
  • Advise patient to apply cream before bedtime and to remove the cream 8 h after application by washing with mild soap and water.

Copyright © 2009 Wolters Kluwer Health.

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