Professional Information
Imiquimod (Topical)
VA CLASSIFICATION
Primary: IM404
Commonly used brand name(s): Aldara.
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).
Category:
Biological response modifier—
Indications
Accepted
Condyloma acuminatum (treatment)—Imiquimod is indicated for the treatment of external genital and perianal warts (condyloma acuminatum). Imiquimod is not a cure and new warts may develop during treatment; effect of imiquimod on transmission of genital warts is not known. {01}
Unaccepted
Imiquimod has not been evaluated for the treatment of urethral, intravaginal, cervical, rectal, or anal human papilloma viral disease and is not recommended for these uses {01}.
Pharmacology/Pharmacokinetics
Physicochemical characteristics:
Molecular weight—
240.31 {02}
Mechanism of action/Effect:
The mechanism of action is not known. Imiquimod does not have direct antiviral activity. Studies of mice show that imiquimod may induce cytokines, including interferon-alpha, in mouse skin; clinical significance or relevance of this finding to humans is not known. Imiquimod potentially can exacerbate inflammatory conditions of the skin {01}.
In one clinical trial that had a 4 to 6 ratio of females to males, 50% of patients, approximately 75% of females and 33% of males, experienced complete wart clearance after using imiquimod for 10 weeks (median, range 4 to 16 weeks). Of the remaining 50% of patients, 33% still had genital warts at 16 weeks and 17% withdrew from the clinical trial {01}. Of those who had complete wart clearance at 10 weeks and could be followed for 12 additional weeks, 23% of patients remained wart-free {01}.
Absorption:
Percutaneous absorption is minimal for a median wart area of 69 square millimeters (mm 2) (range, 8 to 5525 mm 2) {01}.
Precautions to Consider
Carcinogenicity
Rodent carcinogenicity data are not available {01}.
Mutagenicity
Imiquimod was not found to be mutagenic in a series of tests, including the Ames, mouse lymphoma, Chinese hamster ovary (CHO) chromosome aberration, human lymphocyte chromosome aberration, SHE cell transformation, rat and hamster bone marrow cytogenetics, and mouse dominant lethal test {01}.
Pregnancy/Reproduction
Fertility—
Daily oral administration of imiquimod to rats at eight times the human recommended (topical) daily dose, based on mg per square meter of body surface area, produced no impairment of fertility {01}.
Pregnancy—
Adequate and well-controlled studies in humans have not been done. Problems in humans have not been documented. {01}
Researchers studied imiquimod's effect on reproduction in rats and rabbits. Maternotoxicity, but not teratogenicity, as shown by reduced pup weights and delayed ossification, occurred in studies of female rats given doses 28 times the recommended human dose (based on mg per square meter of body surface area). In developmental studies, no adverse effects appeared in the offspring of pregnant rats who received eight times the recommended human dose {01}.
FDA Pregnancy Category B {01}.
Breast-feeding
It is not known whether topical imiquimod is distributed into breast milk. Problems in humans have not been documented {01}.
Pediatrics
No information is available on the relationship of age to the effects of imiquimod in pediatric patients. Safety and efficacy have not been established {01} in patients up to 18 years of age.
Geriatrics
No information is available on the relationship of age to the effects of topical imiquimod in geriatric patients.
Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).
Except under special circumstances, this medication should not be used when the following medical problems exist:
» Dermatitis, genital or
» Surgery, genital, recent (may exacerbate inflammatory conditions of skin; imiquimod is not recommended for application to areas that have recently involved surgery until genital skin has healed {01})
Risk-benefit should be considered when the following medical problem exists
Sensitivity to imiquimod
Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Those indicating need for medical attention
Incidence more frequent
Erosion or excoriation of skin (self-induced skin lesion, such as a scratch)—30%, at site of application{01}
fungal infection, including tinea cruris (itching in genital or other skin areas; scaling)—11% in females, 2% in males{01}
scabbing —4 to 13%, at site of application{01}
ulceration or vesicles on skin (blisters; open sores on skin)—3 to 5%, at site of application{01}
Incidence less frequent
Erythema, severe (redness of skin)—4%, at site of application{01}
Signs and symptoms of systemic effects
Influenza-like symptoms (diarrhea; fatigue; fever; headache; muscle pain){01}
Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
Burning or stinging of skin, mild —26%, at remote site and at site of application{01}
edema of skin (swelling of skin)—12 to 17%, at site of application{01}
erythema, mild (redness of skin)—54 to 61%, at site of application
flaking of skin, mild —18 to 25%, at site of application{01}
pain, soreness, or tenderness of skin, mild —8%, at remote site and at site of application{01}
pruritus, mild (itching of skin)—32%, at remote site and at site of application{01}
rash —at site of application{01}
Incidence less frequent
Hypopigmentation (lightening of normal skin color)—at site of application{01}
Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Imiquimod (Topical).
In providing consultation, consider emphasizing the following selected information (» = major clinical significance):
Before using this medication
» Conditions affecting use, especially:
Sensitivity to imiquimod
Other medical problems, especially genital dermatitis or recent genital surgery
Proper use of this medication
» Not using occlusive dressing, such as bandages; if covering is needed, only using nonocclusive material, such as cotton gauze or cotton underclothes
Proper administration
» Importance of washing hands before and after administration to help avoid translocation of cream. Avoiding contact with eyes
» Understanding amount to use and avoiding excessive administration
Allowing medication to remain on skin for 6 to 10 hours; removing medication by thoroughly washing area with soap and water
Discarding any unused cream from the single-dose packet
» Proper dosing
Missed dose: Wait until the next evening to apply it, and then return to the normal dosing schedule
» Proper storage
Precautions while using this medication
» Reporting severe local skin reactions and rare systemic reactions to physician
» Delaying next dose for several days when experiencing any discomfort or if severe reaction occurs
» Avoiding genital, oral, or anal sexual contact while the cream is on the skin; washing cream off before engaging in sexual activities. Also, oils in the cream may weaken latex contraceptive devices, such as cervical caps, condoms, and diaphragms
» Avoiding use of other topical medications on the same treatment area, unless recommended by physician
» Not sharing medication with others
Side/adverse effects
Erosion or excoriation of skin (at site of application); fungal infection, including tinea cruris; scabbing (at site of application); ulceration or vesicles (at site of application); erythema, severe (at site of application)
Signs or symptoms of systemic effects—Influenza-like symptoms, including myalgia
General Dosing Information
Occlusive dressings, such as bandages, should be avoided. If covering is needed, patient should use nonocclusive material, such as cotton gauze or cotton underclothes. {01}
It is important for patients to avoid transferring cream to uninvolved skin sites or to their partners during sexual contact and not to share medication with others. Patient should wash hands before and after administration to help avoid translocation of cream, especially to eyes, and should wash the treatment area thoroughly with mild soap and water before engaging in sexual activities. Also, oils in the cream can weaken latex contraceptive devices, such as cervical caps, condoms, and diaphragms, and reduce their efficacy. {01}
Patient should understand correct amount of imiquimod to use and avoid excessive administration, discarding the unused portion in the single-dose packets. When experiencing any discomfort or if severe reaction occurs, patient should delay next dose for several days, and report severe local skin reactions and rare systemic reactions to physician. {01}
For treatment of adverse effects
Recommended treatment consists of the following: • Discontinuing medication or decreasing frequency of dosing as needed {01}.
• Using nonocclusive dressing, such as gauze, or cotton underclothes to help manage skin reactions {01}.
Topical Dosage Forms
IMIQUIMOD CREAM
Usual adult dose
Condyloma acuminatum
Topical, to the wart, once every other day (three times a week) prior to normal sleeping hours{03}{04} as a thin film, rubbing in well, leaving on skin for six to ten hours, then removing medication by washing with mild soap and water. Treatment is continued until wart is gone or for up to sixteen weeks. {01}
Note: Each single-use packet containing 250 mg of cream is sufficient to cover a wart area of up to 20 square centimeters; excessive application should be avoided {01}.
Usual pediatric dose
Up to 18 years of age—Safety and efficacy have not been established {01}.
Usual geriatric dose
See Usual adult dose .
Strength(s) usually available
U.S.—
5% (Rx) [Aldara (benzyl alcohol) (cetyl alcohol) (glycerin) (isostearic acid) (methylparaben) (polysorbate 60) (propylparaben) (purified water) (sorbitan monostearate ) (stearyl alcohol) ( white petrolatum) (xanthan gum)]{01}{04}
Canada—
5% (Rx) [Aldara (benzyl alcohol) (cetyl alcohol) (glycerin) (isostearic acid) (methylparaben) (polysorbate 60) (propylparaben) (purified water) (sorbitan monostearate ) (stearyl alcohol) ( white petrolatum) (xanthan gum)]{03}
Packaging and storage:
Store below 30 °C (86 °F), preferably between 15 and 30 °C (59 and 86 °F). Protect from freezing. {01}
Auxiliary labeling:
• For external use only.
Developed: 11/13/1997
Revised: 09/20/1999
References
- Aldara package insert (3M Pharmaceuticals—US), Rev 3/97, Rec 6/97.
- Canada JR, editor. USP dictionary of USAN and international drug names 1998. Rockville, MD: The United States Pharmacopeial Convention, Inc; 1997. p. 374.
- Aldara package insert (3M Pharmaceuticals—Canada), Rev 1/99, Rec 8/99.
- Aldara package insert (3M Pharmaceuticals—US), Rev 3/98.
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