Imiquimod

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Imiquimod
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Deepika Beereddy, MBBS [2]

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Overview

Imiquimod is an immnunologic adjuvant that is FDA approved for the treatment of actinic keratosis, external genital warts. Common adverse reactions include erythema, edema, erosion/ulceration, exudate, scabbing/crusting, headache, application site pain, application site irritation, application site pruritus, fatigue, influenza-like illness, and nausea.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Actinic Keratosis
  • ZYCLARA Cream, 2.5% and 3.75% are indicated for the topical treatment of clinically typical visible or palpable, actinic keratoses (AK), of the full face or balding scalp in immunocompetent adults.
  • Dosing Information
  • ZYCLARA Cream should be applied once daily before bedtime to the skin of the affected area (either entire face or balding scalp) for two 2-week treatment cycles separated by a 2-week no-treatment period. ZYCLARA Cream should be applied as a thin film to the entire treatment area and rubbed in until the cream is no longer visible. Up to 0.5 grams (2 packets or 2 full actuations of the pump) of ZYCLARA Cream may be applied to the treatment area at each application. ZYCLARA Cream should be left on the skin for approximately 8 hours, after which time the cream should be removed by washing the area with mild soap and water. The prescriber should demonstrate the proper application technique to maximize the benefit of ZYCLARA Cream therapy.
  • Patients should wash their hands before and after applying ZYCLARA Cream.
  • Avoid use in or on the lips and nostrils. Do not use in or near the eyes.
  • Local skin reactions in the treatment area are common [see Adverse Reactions (6.1)]. A rest period of several days may be taken if required by the patient's discomfort or severity of the local skin reaction. However, neither 2-week treatment cycle should be extended due to missed doses or rest periods. A transient increase in lesion counts may be observed during treatment. Response to treatment cannot be adequately assessed until resolution of local skin reactions. The patient should continue dosing as prescribed. Treatment should continue for the full treatment course even if all actinic keratoses appear to be gone. Lesions that do not respond to treatment should be carefully re-evaluated and management reconsidered.
  • Prescribe no more than 2 boxes (56 packets), two 7.5g pumps or one 15g pump for the total 2-cycle treatment course. Partially-used packets should be discarded and not reused.
External Genital Warts
  • ZYCLARA Cream, 3.75% is indicated for the treatment of external genital and perianal warts (EGW)/condyloma acuminata in patients 12 years or older.
  • Dosing Information
  • Patients should apply a thin layer of ZYCLARA Cream once a day to the external genital/perianal warts until total clearance or for up to 8 weeks. Patients should use up to 0.25 grams (one packet or one full actuation of the pump) at each application, which is a sufficient amount of cream to cover the wart area. ZYCLARA Cream should be applied prior to normal sleeping hours and left on the skin for approximately 8 hours, then removed by washing the area with mild soap and water. The prescriber should demonstrate the proper application technique to maximize the benefit of ZYCLARA Cream therapy.
  • Patients should wash their hands before and after applying ZYCLARA Cream.
  • Local skin reactions at the treatment site are common, and may necessitate a rest period of several days; resume treatment once the reaction subsides. Non-occlusive dressings such as cotton gauze or cotton underwear may be used in the management of skin reactions.
  • Prescribe up to 2 boxes (56 packets), two 7.5g pumps or one 15g pump for the total treatment course. Use of excessive amounts of cream should be avoided. Partially-used packets should be discarded and not reused.
Superficial basal cell carcinoma, on trunk, neck, or extremities; when surgical methods are less appropriate and follow-up is assured
  • Dosing Information
  • Tumors 0.5 cm to less than 1 cm in diameter, apply a 4 mm diameter cream droplet (10 mg); tumors 1 cm to less than 1.5 cm in diameter, apply a 5 mm diameter cream droplet (25 mg); tumors 1.5 cm to 2 cm in diameter, apply a 7 mm cream droplet (40 mg of cream)

Limitations of Use

  • Imiquimod cream has been evaluated in children ages 2 to 12 years with molluscum contagiosum and these studies failed to demonstrate efficacy.
  • Treatment with ZYCLARA Cream has not been studied for prevention or transmission of HPV.

Unevaluated Populations

  • The safety and efficacy of ZYCLARA Cream have not been established in the treatment of:
  • urethral, intra-vaginal, cervical, rectal or intra-anal human papilloma viral disease.
  • actinic keratosis when treated with more than one 2-cycle treatment course in the same area.
  • patients with xeroderma pigmentosum.
  • superficial basal cell carcinoma.
  • immunosuppressed patients.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condyloma acuminatum, external - HIV infection

  • Recommendation: Adult, Class IIb
  • Strength of Evidence: Adult, Category B
  • Dosing information
  • For the treatment of uncomplicated external genital warts in patients with human immunodeficiency virus, apply imiquimod 5% cream to the lesion at bedtime, 3 times per week on nonconsecutive nights. Wash with soap and water 6 to 10 hours after each application. Treatment may continue for up to 16 weeks.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Imiquimod in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

External Genital Warts
  • ZYCLARA Cream, 3.75% is indicated for the treatment of external genital and perianal warts (EGW)/condyloma acuminata in patients 12 years or older.
  • Dosing information
  • Zyclara(R)
  • For the treatment of children 12 years and older with external genital and perianal warts/condyloma acuminata, apply up to 1 packet or 1 pump actuation of 3.75% cream topically to warts once daily at bedtime until total clearance or up to a duration of 8 weeks. Leave on the skin for 8 hours then wash area with mild soap and water.
  • Aldara(R)
  • For the treatment of external genital and perianal warts/condyloma acuminata in patients 12 years of age or older, apply up to one imiquimod 5% cream packet to the treatment area 3 times per week until total genital and perianal wart clearance or for a maximum duration of 16 weeks. Each imiquimod packet contains enough cream to cover a wart area of up to 20 square centimeters. Apply a thin layer of cream prior to normal sleeping hours and leave on the skin for 6 to 10 hours. Following each treatment period, remove the cream by washing the treated area with soap and water. Examples of 3 times per week application schedules are: Monday, Wednesday, and Friday or Tuesday, Thursday, and Saturday.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condyloma acuminatum, external - HIV infection

  • Recommendation: Pediatric, Class IIb
  • Strength of Evidence: Pediatric, Category C
  • Dosing information
  • For the treatment of uncomplicated external genital warts in children with human immunodeficiency virus, apply imiquimod 5% cream to the lesion at bedtime, 3 times per week on nonconsecutive nights. Wash with soap and water 6 to 10 hours after each application. Treatment may continue for up to 16 weeks.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Imiquimod in pediatric patients.

Contraindications

  • None.

Warnings

Local Skin Reactions

  • Intense local skin reactions including skin weeping or erosion can occur after a few applications of ZYCLARA Cream and may require an interruption of dosing [see Dosage and Administration (2) and Adverse Reactions (6)]. ZYCLARA Cream has the potential to exacerbate inflammatory conditions of the skin, including chronic graft versus host disease.
  • Severe local inflammatory reactions of the female external genitalia can lead to severe vulvar swelling. Severe vulvar swelling can lead to urinary retention. Dosing should be interrupted or discontinued for severe vulvar swelling.
  • Administration of ZYCLARA Cream is not recommended until the skin is healed from any previous drug or surgical treatment.

Systemic Reactions

  • Flu-like signs and symptoms may accompany, or even precede, local skin reactions and may include fatigue, nausea, fever, myalgias, arthralgias, malaise and chills. An interruption of dosing and an assessment of the patient should be considered.
  • Lymphadenopathy occurred in 2% of subjects with actinic keratosis treated with ZYCLARA Cream, 3.75% and in 3% of subjects treated with ZYCLARA Cream, 2.5% [see Adverse Reactions (6)]. This reaction resolved in all subjects by 4 weeks after completion of treatment.

Ultraviolet Light Exposure Risks

  • Exposure to sunlight (including sunlamps) should be avoided or minimized during use of ZYCLARA Cream. Patients should be warned to use protective clothing (e.g., a hat) when using ZYCLARA Cream. Patients with sunburn should be advised not to use ZYCLARA Cream until fully recovered. Patients who may have considerable sun exposure, e.g. due to their occupation, and those patients with inherent sensitivity to sunlight should exercise caution when using ZYCLARA Cream.
  • In an animal photo-carcinogenicity study, imiquimod cream shortened the time to skin tumor formation. The enhancement of ultraviolet carcinogenicity is not necessarily dependent on phototoxic mechanisms. Therefore, patients should minimize or avoid natural or artificial sunlight exposure.

Increased Risk of Adverse Reactions with Concomitant Imiquimod Use

  • Concomitant use of ZYCLARA Cream and any other imiquimod products, in the same treatment area, should be avoided since they contain the same active ingredient (imiquimod) and may increase the risk for and severity of local skin reactions.
  • The safety of concomitant use of ZYCLARA Cream and any other imiquimod products has not been established and should be avoided since they contain the same active ingredient (imiquimod) and may increase the risk for and severity of systemic reactions.

Immune Cell Activation in Autoimmune Disease

  • ZYCLARA Cream should be used with caution in patients with pre-existing autoimmune conditions because imiquimod activates immune cells.

Adverse Reactions

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Clinical Trials Experience: Actinic Keratosis

  • The data described below reflect exposure to ZYCLARA Cream or vehicle in 479 subjects enrolled in two double-blind, vehicle-controlled trials. Subjects applied up to two packets of ZYCLARA Cream or vehicle daily to the skin of the affected area (either entire face or balding scalp) for two 2-week treatment cycles separated by a 2-week no treatment period.

Overall, in the clinical trials, 11% (17/160) of subjects in the ZYCLARA Cream, 3.75% arm, 7% (11/160) of subjects in the ZYCLARA Cream, 2.5% arm, and 0% in the vehicle cream arm required rest periods due to adverse local skin reactions.

Other adverse reactions observed in subjects treated with ZYCLARA Cream include: application site bleeding, application site swelling, chills, dermatitis, herpes zoster, insomnia, lethargy, myalgia, pancytopenia, pruritus, squamous cell carcinoma, and vomiting.

6.2 Clinical Trials Experience: External Genital Warts

In two double-blind, placebo-controlled studies 602 subjects applied up to one packet of ZYCLARA Cream or vehicle daily for up to 8 weeks.

The most frequently reported adverse reactions were application site reactions and local skin reactions. Selected adverse reactions are listed in Table 3.

The frequency and severity of local skin reactions were similar in both genders, with the following exceptions: a) flaking/scaling occurred in 40% of men and in 26% of women and b) scabbing/crusting occurred in 34% of men and in 18% of women.

In the clinical trials, 32% (126/400) of subjects who used ZYCLARA Cream and 2% (4/202) of subjects who used vehicle cream discontinued treatment temporarily (required rest periods) due to adverse local skin reactions, and 1% (3/400) of subjects who used ZYCLARA Cream discontinued treatment permanently due to local skin/application site reactions.

Other adverse reactions reported in subjects treated with ZYCLARA Cream include: rash, back pain, application site rash, application site cellulitis, application site excoriation, application site bleeding, scrotal pain, scrotal erythema, scrotal ulcer, scrotal edema, sinusitis, nausea, pyrexia, and influenza-like symptoms.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of imiquimod. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Application Site Disorders: tingling at the application site

Body as a Whole: angioedema

Cardiovascular: capillary leak syndrome, cardiac failure, cardiomyopathy, pulmonary edema, arrhythmias (tachycardia, supraventricular tachycardia, atrial fibrillation, palpitations), chest pain, ischemia, myocardial infarction, syncope

Endocrine: thyroiditis

Gastro-Intestinal System Disorders: abdominal pain

Hematological: decreases in red cell, white cell and platelet counts (including idiopathic thrombocytopenic purpura), lymphoma

Hepatic: abnormal liver function

Infections and Infestations: herpes simplex

Musculo-Skeletal System Disorders: arthralgia

Neuropsychiatric: agitation, cerebrovascular accident, convulsions (including febrile convulsions), depression, insomnia, multiple sclerosis aggravation, paresis, suicide

Respiratory: dyspnea

Urinary System Disorders: proteinuria, urinary retention, dysuria

Skin and Appendages: exfoliative dermatitis, erythema multiforme, hyperpigmentation, hypertrophic scar, hypopigmentation

Vascular: Henoch-Schonlein purpura syndrome

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Imiquimod in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Imiquimod during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Imiquimod with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Imiquimod with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Imiquimod with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Imiquimod with respect to specific gender populations.

Race

There is no FDA guidance on the use of Imiquimod with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Imiquimod in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Imiquimod in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Imiquimod in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Imiquimod in patients who are immunocompromised.

Administration and Monitoring

Administration

  • For topical use only; ZYCLARA Cream is not for oral, ophthalmic, intra-anal or intravaginal use.

Actinic Keratosis

  • ZYCLARA Cream should be applied once daily before bedtime to the skin of the affected area (either entire face or balding scalp) for two 2-week treatment cycles separated by a 2-week no-treatment period. ZYCLARA Cream should be applied as a thin film to the entire treatment area and rubbed in until the cream is no longer visible. Up to 0.5 grams (2 packets or 2 full actuations of the pump) of ZYCLARA Cream may be applied to the treatment area at each application. ZYCLARA Cream should be left on the skin for approximately 8 hours, after which time the cream should be removed by washing the area with mild soap and water. The prescriber should demonstrate the proper application technique to maximize the benefit of ZYCLARA Cream therapy.
  • Patients should wash their hands before and after applying ZYCLARA Cream.
  • Avoid use in or on the lips and nostrils. Do not use in or near the eyes.
  • Local skin reactions in the treatment area are common [see Adverse Reactions (6.1)]. A rest period of several days may be taken if required by the patient's discomfort or severity of the local skin reaction. However, neither 2-week treatment cycle should be extended due to missed doses or rest periods. A transient increase in lesion counts may be observed during treatment. Response to treatment cannot be adequately assessed until resolution of local skin reactions. The patient should continue dosing as prescribed. Treatment should continue for the full treatment course even if all actinic keratoses appear to be gone. Lesions that do not respond to treatment should be carefully re-evaluated and management reconsidered.
  • Prescribe no more than 2 boxes (56 packets), two 7.5g pumps or one 15g pump for the total 2-cycle treatment course. Partially-used packets should be discarded and not reused.

External Genital Warts

  • Patients should apply a thin layer of ZYCLARA Cream once a day to the external genital/perianal warts until total clearance or for up to 8 weeks. Patients should use up to 0.25 grams (one packet or one full actuation of the pump) at each application, which is a sufficient amount of cream to cover the wart area. ZYCLARA Cream should be applied prior to normal sleeping hours and left on the skin for approximately 8 hours, then removed by washing the area with mild soap and water. The prescriber should demonstrate the proper application technique to maximize the benefit of ZYCLARA Cream therapy.
  • Patients should wash their hands before and after applying ZYCLARA Cream.
  • Local skin reactions at the treatment site are common [see Adverse Reactions (6.2)], and may necessitate a rest period of several days; resume treatment once the reaction subsides. Non-occlusive dressings such as cotton gauze or cotton underwear may be used in the management of skin reactions.
  • Prescribe up to 2 boxes (56 packets), two 7.5g pumps or one 15g pump for the total treatment course. Use of excessive amounts of cream should be avoided. Partially-used packets should be discarded and not reused.

Pump Administration

  • ZYCLARA (imiquimod) Cream pumps should be primed before using for the first time by repeatedly depressing the actuator until cream is dispensed. It is not necessary to repeat this priming process during treatment.

Dosage forms and strengths

  • ZYCLARA Cream, 2.5% is a white to faintly yellow cream available in single-use packets and pump bottles. Each packet administers 0.25 grams of cream and each pump bottle, when actuated after priming, delivers 0.235 grams of cream (a similar amount as one packet).
  • ZYCLARA Cream, 3.75% is a white to faintly yellow cream available in single-use packets and pump bottles. Each packet administers 0.25 grams of cream and each pump bottle, when actuated after priming, delivers 0.235 grams of cream (a similar amount as one packet).

Monitoring

There is limited information regarding Monitoring of Imiquimod in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Imiquimod in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Imiquimod in the drug label.

Pharmacology

There is limited information regarding Imiquimod Pharmacology in the drug label.

Mechanism of Action

Structure

File:Imiquimod01.png
This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Imiquimod in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Imiquimod in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Imiquimod in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Imiquimod in the drug label.

How Supplied

Storage

There is limited information regarding Imiquimod Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Imiquimod in the drug label.

Precautions with Alcohol

  • Alcohol-Imiquimod interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Aldara, Zyclara.

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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