Aldara疣定寧

Aldara

imiquimod

Manufacturer:

iNova

Distributor:

Zuellig
/
Agencia Lei Va Hong
Full Prescribing Info
Contents
Imiquimod.
Description
Each gram of cream contains imiquimod 50 mg 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.
Imiquimod is 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine. It has a molecular formula of C14H16N4 and a molecular weight of 240.3.
Action
Immune response modifier.
Pharmacology: Pharmacodynamics: The mechanism of action of imiquimod in treating genital/perianal warts is unknown. Imiquimod has no direct antiviral activity in cell culture. Mouse skin studies suggest that imiquimod induces cytokines including interferon-α. However, the clinical relevance of these findings is unknown.
Pharmacokinetics: Percutaneous absorption of [14C]-imiquimod was minimal in a study involving 6 healthy subjects treated with a single topical application (5 mg) of [14C]-imiquimod cream formulation. No radioactivity was detected in the serum (lower limit of quantitation: 1 ng/mL) and <0.9% of the radiolabelled dose was excreted in the urine and feces following topical application.
Clinical Studies: In a double-blind, placebo-controlled clinical trial, 209 otherwise healthy patients ≥18 years with genital/perianal warts were treated with Aldara 5% cream or vehicle control 3 times a week for a maximum of 16 weeks. The median baseline wart area was 69 mm2 (range 8-5525 mm2).
Patient accountability is shown in the following diagram. (See diagram.)

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Data on complete clearance are listed in Table 1 (see Table 1). The median time to complete wart clearance was 10 weeks.

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Reference:1. Edwards et al. Self-Administered topical 5% Imiquimod Cream for Exrternal Anogenital Warts. Arch Dermatol.1998; 134:25-30.
Indications/Uses
Treatment of external genital and perianal warts/condyloma acuminata in adults.
Dosage/Direction for Use
Aldara cream is to be applied 3 times/week, prior to normal sleeping hours, and left on the skin for 6-10 hrs. Following the treatment period, the cream should be removed by washing the treated area with mild soap and water. Examples of 3 times/week application schedules are: Monday, Wednesday, Friday; or Tuesday, Thursday, Saturday application prior to sleeping hours. Aldara treatment should continue until there is total clearance of the genital/perianal warts or for a maximum of 16 weeks. Local skin reactions (erythema) at the treatment site are common. A rest period of several days may be taken if required by the patient's discomfort or severity of the local skin reaction. Treatment may resume once the reaction subsides. Non-occlusive dressings eg, cotton gauze or cotton underwear may be used in the management of skin reactions. The technique for proper dose administration should be demonstrated by the prescriber to maximize the benefit of Aldara therapy. Handwashing before and after cream application is recommended. Aldara 5% cream is packaged in single-use packets which contain sufficient cream to cover a wart area of up to 20 cm2; use of excessive amounts of cream should be avoided. Patients should be instructed to apply Aldara cream to external genital/perianal warts. A thin layer is applied to the wart area and rubbed in until the cream is no longer visible. The application site is not to be occluded.
Overdosage
Overdosage of Aldara in humans is unlikely due to minimal percutaneous absorption. Animal studies reveal a rabbit dermal lethal imiquimod dose of >1600 mg/m2. Persistent topical overdosing of Aldara cream could result in severe local skin reactions. The most clinically serious adverse event reported following multiple oral imiquimod doses of >200 mg was hypotension, which resolved following oral or IV fluid administration.
Contraindications
None known.
Warnings
Aldara cream has not been evaluated for the treatment of urethral, intravaginal, cervical, rectal or intra-anal human papilloma viral disease and is not recommended for these conditions.
Special Precautions
General: Local skin reactions eg, erythema, erosion, excoriation/flaking and edema are common. Should severe local skin reaction occur, the cream should be removed by washing the treatment area with mild soap and water. Treatment with Aldara cream can be resumed after the skin reaction has subsided. There is no clinical experience with Aldara cream therapy immediately following the treatment of genital/perianal warts with other cutaneously applied drugs; therefore, Aldara cream administration is not recommended until genital/perianal tissue is healed from any previous drug or surgical treatment. Aldara has the potential to exacerbate inflammatory conditions of the skin.
Information for Patients: Patients using Aldara should receive the following information and instructions: The effect of Aldara on the transmission of genital/perianal warts is unknown. Aldara may weaken condoms and vaginal diaphragms. Therefore, concurrent use is not recommended.
Aldara is to be used as directed by a physician. It is for external use only. Eye contact should be avoided.
The treatment area should not be bandaged or otherwise covered or wrapped as to be occlusive.
Sexual (genital, anal, oral) contact should be avoided while the cream is on the skin.
It is recommended that 6-10 hrs following Aldara cream application, the treatment area be washed with mild soap and water.
It is common for patients to experience local skin reactions eg, erythema, erosion, excoriation/flaking and edema at the site of application or surrounding areas. Most skin reactions are mild to moderate. Severe skin reactions can occur and should be reported promptly to the prescribing physician.
Uncircumcised males treating warts under the foreskin should retract the foreskin and clean the area daily.
Patients should be aware that new warts may develop during therapy, as Aldara is not a cure.
Carcinogenicity, Mutagenicity & Impairment of Fertility: Rodent carcinogenicity data are not available. Imiquimod was without effect in a series of 8 different mutagenicity assays including Ames, mouse lymphoma, CHO chromosome aberration, human lymphocyte chromosome aberration, SHE cell transformation, rat and hamster bone marrow cytogenetics, and mouse dominant lethal test. Daily oral administration of imiquimod to rats, at doses up to 8 times the recommended human dose on a mg/m2 basis throughout mating, gestation, parturition and lactation, demonstrated no impairment of reproduction.
Use in pregnancy: There are no adequate and well-controlled studies in pregnant women. Imiquimod was not found to be teratogenic in rat or rabbit teratology studies. In rats at a high maternally toxic dose (28 times human dose on a mg/m2 basis), reduced pup weights and delayed ossification were observed. In developmental studies with offspring of pregnant rats treated with imiquimod (8 times human dose), no adverse effects were demonstrated.
Use in lactation: It is not known whether topically applied imiquimod is excreted in breast milk.
Use in children: Safety and efficacy in patients <18 years have not been established.
Use In Pregnancy & Lactation
Use in pregnancy: There are no adequate and well-controlled studies in pregnant women. Imiquimod was not found to be teratogenic in rat or rabbit teratology studies. In rats at a high maternally toxic dose (28 times human dose on a mg/m2 basis), reduced pup weights and delayed ossification were observed. In developmental studies with offspring of pregnant rats treated with imiquimod (8 times human dose), no adverse effects were demonstrated.
Use in lactation: It is not known whether topically applied imiquimod is excreted in breast milk.
Adverse Reactions
In controlled clinical trials, the most frequently reported adverse reactions were those of local skin and application site reactions; some patients also reported systemic reactions. These reactions were usually mild to moderate in intensity; however, severe reactions were reported with 3 times a week application. These reactions were more frequent and more intense with daily application than with 3 times a week application. Overall, in the 3 times a week application clinical studies, 1.2% (4/327) of the patients discontinued due to local skin/application site reactions. The incidence and severity of local skin reactions during controlled clinical trials are shown in Table 2.

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Remote site skin reactions were also reported in female and male patients treated 3 times a week with imiquimod 5% cream. The severe remote site skin reactions reported for females were erythema (3%), ulceration (2%) and edema (1%); and for males, erosion (2%), and erythema, edema, induration and excoriation/flaking (each 1%).
Adverse events judged to be probably or possibly related to Aldara reported by >5% of patients are listed in Table 3. Also included are soreness, influenza-like symptoms and myalgia. (See Table 3.)

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Adverse events judged to be possibly or probably related to Aldara and reported by >1% of patients include:
Application Site Disorders: Wart Site Reactions: Burning, hypopigmentation, irritation, itching, pain, rash, sensitivity, soreness, stinging, tenderness. Remote Site Reactions: Bleeding, burning, itching, pain, tenderness, tinea cruris.
Body as a Whole: Fatigue, fever, influenza-like symptoms.
Central and Peripheral Nervous System Disorders: Headache.
Gastrointestinal System Disorders: Diarrhea.
Musculoskeletal System Disorders: Myalgia.
Storage
Store below 25°C. Avoid freezing.
ATC Classification
D06BB10 - imiquimod ; Belongs to the class of topical antivirals used in the treatment of dermatological diseases.
Presentation/Packing
Cream 5% x 250 mg x 12 sachets.
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