Prescription drugs info

Aldara™ (imiquimod 5%) Cream is an immune response modifier for topical administration. Each gram contains 50 mg of imiquimod in an off-white oil-in-water vanishing cream base consisting of isostearic acid, cetyl alcohol, stearyl alcohol, white petrolatum, polysorbate 60, sorbitan monostearate, glycerin, xanthan gum, purified water, benzyl alcohol, methylparaben, and propylparaben.

Chemically, imiquimod is 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine. Imiquimod has a molecular formula of C14H16N4 and a molecular weight of 240.3.

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Topical overdosing of Aldara Cream could result in an increased incidence of severe local skin reactions and may increase the risk for systemic reactions.

The most clinically serious adverse event reported following multiple oral imiquimod doses of >200 mg (equivalent to imiquimod content of >16 packets) was hypotension, which resolved following oral or intravenous fluid administration.

AK and sBCC are not conditions generally seen within the pediatric population. The safety and efficacy of Aldara Cream for AK or sBCC in patients less than 18 years of age have not been established.

Safety and efficacy in patients with external genital/perianal warts below the age of 12 years have not been established.

Aldara Cream was evaluated in two randomized, vehicle-controlled, double-blind trials involving 702 pediatric subjects with molluscum contagiosum (MC) (470 exposed to Aldara; median age 5 years, range 2-12 years). Subjects applied Aldara Cream or vehicle 3 times weekly for up to 16 weeks. Complete clearance (no MC lesions) was assessed at Week 18. In Study 1, the complete clearance rate was 24% (52/217) in the Aldara Cream group compared with 26% (28/106) in the vehicle group. In Study 2, the clearance rates were 24% (60/253) in the Aldara Cream group compared with 28% (35/126) in the vehicle group. These studies failed to demonstrate efficacy.

Similar to the studies conducted in adults, the most frequently reported adverse reaction from 2 studies in children with molluscum contagiosum was application site reaction. Adverse events which occurred more frequently in Aldara-treated subjects compared with vehicle-treated subjects generally resembled those seen in studies in indications approved for adults and also included otitis media (5% Aldara vs. 3% vehicle) and conjunctivitis (3% Aldara vs. 2% vehicle). Erythema was the most frequently reported local skin reaction. Severe local skin reactions reported by Aldara-treated subjects in the pediatric studies included erythema (28%), edema (8%), scabbing/crusting (5%), flaking/scaling (5%), erosion (2%) and weeping/exudate (2%).

Systemic absorption of imiquimod across the affected skin of 22 subjects aged 2 to 12 years with extensive MC involving at least 10% of the total body surface area was observed after single and multiple doses at a dosing frequency of 3 applications per week for 4 weeks. The investigator determined the dose applied, either 1, 2 or 3 packets per dose, based on the size of the treatment area and the subject’s weight. The overall median peak serum drug concentrations at the end of week 4 was between 0.26 and 1.06 ng/ml except in a 2-year old female who was administered 2 packets of study drug per dose, had a Cmax of 9.66 ng/mL after multiple dosing. Children aged 2-5 years received doses of 12.5 mg (one packet) or 25 mg (two packets) of imiquimod and had median multiple-dose peak serum drug levels of approximately 0.2 or 0.5 ng/mL, respectively. Children aged 6-12 years received doses of 12.5 mg, 25 mg, or 37.5 mg (three packets) and had median multiple dose serum drug levels of approximately 0.1, 0.15, or 0.3 ng/mL, respectively. Among the 20 subjects with evaluable laboratory assessments, the median WBC count decreased by 1.4*109/L and the median absolute neutrophil count decreased by 1.42*109/L.

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It is not known whether imiquimod is excreted in human milk following use of Aldara Cream. Because many drugs are excreted in human milk, caution should be exercised when Aldara Cream is administered to nursing women.

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Pregnancy Category C:

Note: The Maximum Recommended Human Dose (MRHD) was set at 2 packets per treatment of Aldara Cream (25 mg imiquimod) for the animal multiple of human exposure ratios presented in this label. If higher doses than 2 packets of Aldara Cream are used clinically, then the animal multiple of human exposure would be reduced for that dose. A non-proportional increase in systemic exposure with increased dose of Aldara Cream was noted in the clinical pharmacokinetic study conducted in actinic keratosis subjects . The AUC after topical application of 6 packets of Aldara Cream was 8 fold greater than the AUC after topical application of 2 packets of Aldara Cream in actinic keratosis subjects. Therefore, if a dose of 6 packets per treatment of Aldara Cream was topically administered to an individual, then the animal multiple of human exposure would be either 1/3 of the value provided in the label (based on body surface area comparisons) or 1/8 of the value provided in the label (based on AUC comparisons). The animal multiples of human exposure calculations were based on weekly dose comparisons for the carcinogenicity studies described in this label. The animal multiples of human exposure calculations were based on daily dose comparisons for the reproductive toxicology studies described in this label.

Systemic embryofetal development studies were conducted in rats and rabbits. Oral doses of 1, 5 and 20 mg/kg/day imiquimod were administered during the period of organogenesis (gestational days 6 – 15) to pregnant female rats. In the presence of maternal toxicity, fetal effects noted at 20 mg/kg/day (577X MRHD based on AUC comparisons) included increased resorptions, decreased fetal body weights, delays in skeletal ossification, bent limb bones, and two fetuses in one litter (2 of 1567 fetuses) demonstrated exencephaly, protruding tongues and low-set ears. No treatment related effects on embryofetal toxicity or teratogenicity were noted at 5 mg/kg/day (98X MRHD based on AUC comparisons).

Intravenous doses of 0.5, 1 and 2 mg/kg/day imiquimod were administered during the period of organogenesis (gestational days 6 – 18) to pregnant female rabbits. No treatment related effects on embryofetal toxicity or teratogenicity were noted at 2 mg/kg/day (1.5X MRHD based on BSA comparisons), the highest dose evaluated in this study, or 1 mg/kg/day (407X MRHD based on AUC comparisons).

A combined fertility and peri- and post-natal development study was conducted in rats. Oral doses of 1, 1.5, 3 and 6 mg/kg/day imiquimod were administered to male rats from 70 days prior to mating through the mating period and to female rats from 14 days prior to mating through parturition and lactation. No effects on growth, fertility, reproduction or post-natal development were noted at doses up to 6 mg/kg/day (87X MRHD based on AUC comparisons), the highest dose evaluated in this study. In the absence of maternal toxicity, bent limb bones were noted in the F1 fetuses at a dose of 6 mg/kg/day (87X MRHD based on AUC comparisons). This fetal effect was also noted in the oral rat embryofetal development study conducted with imiquimod. No treatment related effects on teratogenicity were noted at 3 mg/kg/day (41X MRHD based on AUC comparisons).

There are no adequate and well-controlled studies in pregnant women. Aldara Cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

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Local Inflammatory Reactions

Intense local inflammatory reactions including skin weeping or erosion can occur after few applications of Aldara Cream and may require an interruption of dosing. Aldara Cream has the potential to exacerbate inflammatory conditions of the skin, including chronic graft versus host disease.

Administration of Aldara Cream is not recommended until the skin is completely healed from any previous drug or surgical treatment.

Systemic Reactions

Flu-like signs and symptoms may accompany, or even precede, local inflammatory reactions and may include malaise, fever, nausea, myalgias and rigors. An interruption of dosing should be considered.

Ultraviolet Light Exposure

Exposure to sunlight (including sunlamps) should be avoided or minimized during use of Aldara Cream because of concern for heightened sunburn susceptibility. Patients should be warned to use protective clothing (e.g., a hat) when using Aldara Cream. Patients with sunburn should be advised not to use Aldara 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 Aldara Cream.

Aldara Cream shortened the time to skin tumor formation in an animal photoco-carcinogenicity study. The enhancement of ultraviolet carcinogenicity is not necessarily dependent on phototoxic mechanisms. Therefore, patients should minimize or avoid natural or artificial sunlight exposure.

Unevaluated Uses: Actinic Keratosis

Safety and efficacy have not been established for Aldara Cream in the treatment of actinic keratosis with repeated use, i.e. more than one treatment course, in the same area.

The safety of Aldara Cream applied to areas of skin greater than 25 cm2 (e.g. 5 cm X 5 cm) for the treatment of actinic keratosis has not been established.

Unevaluated Uses: Superficial Basal Cell Carcinoma

The safety and efficacy of Aldara Cream have not been established for other types of basal cell carcinomas (BCC), including nodular and morpheaform (fibrosing or sclerosing) types. Aldara Cream is not recommended for treatment of BCC subtypes other than the superficial variant (i.e., sBCC). Patients with sBCC treated with Aldara Cream should have regular follow-up of the treatment site.

The safety and efficacy of treating sBCC lesions on the face, head and anogenital area have not been established.

Unevaluated Uses: External Genital Warts

Aldara Cream has not been evaluated for the treatment of urethral, intra-vaginal, cervical, rectal, or intra-anal human papilloma viral disease.

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Aldara (imiquimod) Cream, 5%, is supplied in single-use packets each of which contains 250 mg of the cream, equivalent to 12.5 mg of imiquimod. Aldara Cream is supplied in boxes of 12 packets each.

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Actinic Keratosis

Aldara Cream is indicated for the topical treatment of clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp in immunocompetent adults.

Superficial Basal Cell Carcinoma

Aldara Cream is indicated for the topical treatment of biopsy-confirmed, primary superficial basal cell carcinoma (sBCC) in immunocompetent adults, with a maximum tumor diameter of 2.0 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.

The histological diagnosis of superficial basal cell carcinoma should be established prior to treatment, since safety and efficacy of Aldara Cream have not been established for other types of basal cell carcinomas, including nodular and morpheaform (fibrosing or sclerosing) types.

External Genital Warts

Aldara Cream is indicated for the treatment of external genital and perianal warts/condyloma acuminata in patients 12 years old or older.

Limitations of Use

Aldara Cream has been evaluated in children ages 2 to 12 years with molluscumcontagiosum and these studies failed to demonstrate efficacy.

Unevaluated Populations

The safety and efficacy of Aldara Cream in immunosuppressed patients have not been established.

Aldara Cream should be used with caution in patients with pre-existing autoimmune conditions.

The efficacy and safety of Aldara Cream have not been established for patients with Basal Cell Nevus Syndrome or Xeroderma Pigmentosum.

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Along with its needed effects, Aldara may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

More common

Blisters on skin; body aches or pain; chills; cough; difficulty in breathing; ear congestion; itching in genital or other skin areas; loss of voice; nasal congestion; open sores or scabs on skin; pain or tenderness around eyes and cheekbones; redness of skin (severe); scaling; shortness of breath or troubled breathing; skin rash; sneezing; sore throat; stuffy or runny nose; tightness of chest or wheezing; unusual tiredness or weakness

Less common

Abdominal pain; ankle, knee, or great toe joint pain; blurred vision; chest pain; dizziness; bladder pain; bloody or cloudy urine; cold flu-like symptoms; difficult, burning, or painful urination; fainting; fast or irregular heartbeat; frequent urge to urinate; joint stiffness or swelling; high amount of cholesterol in the blood; hoarseness; lower back or side pain; lump in abdomen; nervousness; persistent non-healing sore; pink growth on skin; pounding in the ears; reddish patch or irritated area; severe headache; shiny bump on skin; slow or fast heartbeat; swollen, painful, or tender lymph glands in neck, armpit, or groin; white, yellow or waxy scar-like area

Incidence unknown—Observed during clinical practice, estimates of frequency can not be determined

Blurred vision; blue lips and fingernails; convulsions; coughing that sometimes produces a pink frothy sputum; difficulty breathing; dilated neck veins; dizziness; extreme fatigue; faintness; fast, irregular or pounding heartbeat; irregular breathing; headache; irregular heartbeat; nausea or vomiting ; pain in the shoulders, arms, jaw or neck; seizures; shortness of breath; slurred speech; sudden and severe inability to speak; suicide; sweating; swelling of face, fingers, feet, or lower legs; temporary blindness; weakness in arm and/or leg on one side of the body; weight gain; wheezing

Aldara Symptoms of overdose

Flu-like symptoms, including diarrhea, fatigue, fever, headache, or muscle pain

Other side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. However, check with your doctor if any of the following side effects continue or are bothersome:

More common

Burning or stinging of skin (mild); flaking of skin; mild headache; pain, soreness, or tenderness of skin (mild); rash; redness of skin (mild); swelling at place of application

Less common

Back pain; fever; lightening of the treated skin; nausea

Incidence unknown—Observed during clinical practice, estimates of frequency can not be determined

Agitation; cloudy urine; cracks in the skin ; decrease or increase in amount of urine; depression; lab results that show problems with liver; large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs; loss of heat from the body ; multiple sclerosis aggravation; pale skin; red, swollen skin; scaly skin; sleeplessness ; swelling of neck; trouble sleeping; unable to sleep

Other side effects not listed above may also occur in some patients. If you notice any other effects, check with your doctor.

If you notice severe skin irritation or flu-like symptoms (diarrhea, fatigue, fever, headache, or muscle pain), check with your doctor . It may be necessary for you to reduce the number of times a week that you use the medicine or to stop using the medicine for a short time until your skin is less irritated or your flu-like symptoms disappear.

For treatment of warts on the skin outside of the genital or rectal areas (condyloma acuminatum), avoid having genital, oral, or anal sex while Aldara is on your skin. Make sure you wash the cream off your skin before you engage in any sexual activity . Also, the medicine contains oils that can weaken latex (rubber) condoms, diaphragms, or cervical caps causing them not to work properly to prevent pregnancy.

Aldara is not a cure for genital warts. New warts may develop during treatment with Aldara

Aldara will not keep you from spreading genital warts to other people.

Do not use any other skin product on the same skin area on which you use Aldara, unless directed otherwise by your doctor.

Do not share Aldara with others , even if you think that they have the same condition you have.

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