Imiquimod

Uses

Imiquimod Cream is used for the topical treatment of:

• Clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses (AK) on he face or scalp in immunocompetent adults
• Biopsy-confirmed, primary superficial basal cell carcinoma (sBCC) in immunocompetent adults; maximum tumor diameter of 2.0 cm on trunk, neck, or extremities (excluding hands and feet), only when surgical methods are medically less appropriate and patient follow-up can be reasonably assured
• External genital and perianal warts/condyloma acuminata

Imiquimod is also used to associated treatment for these conditions: Actinic Keratoses of the face, Actinic Keratoses of the scalp, Condylomata Acuminata, Herpes Simplex Infection, Molluscum Contagiosum, Superficial Basal Cell Carcinoma

How Imiquimod works

Imiquimod's mechanism of action is via stimulation of innate and acquired immune responses, which ultimately leads to inflammatory cell infiltration within the field of drug application followed by apoptosis of diseased tissue. Imiquimod does not have direct antiviral activity. Studies of mice show that imiquimod may induce cytokines, including interferon-alpha (IFNA) as well as several IFNA genes (IFNA1, IFNA2, IFNA5, IFNA6, and IFNA8) as well as the IFNB gene. Imiquimod also induced the expression of interleukin (IL)-6, IL-8, and tumor necrosis factor alpha genes. In the treatment of basal cell carcinoma, Imiquimod appears to act as a toll-like receptor-7 agonist, and is thought to exert its anti-tumor effect via modification of the immune response and stimulation of apoptosis in BCC cells. In treating basal cell carcinoma it may increase the infiltration of lymphocytes, dendritic cells, and macrophages into the tumor lesion.

Dosage

Imiquimod dosage

Imiquimod Cream is not for oral, ophthalmic, or intravaginal use

• Actinic keratosis: 2 times per week for a full 16 weeks
• Superficial basal cell carcinoma: 5 times per week for a full 6 weeks
• External genital warts (EGW): 3 times per week until total clearance or a maximum of 16 weeks

Side Effects

Most common adverse reactions (incidence >28%) are application site reactions or local skin reactions: itching, burning, erythema, flaking/scaling/dryness, scabbing/crusting, edema, induration, excoriation, erosion, ulceration. Other reported reactions (≥ 1%) include fatigue, fever, and headache

Toxicity

Symptoms of overdose include flu-like symptoms, such as fever, fatigue, headache, nausea, diarrhoea and muscle pain.

Precaution

Intense local inflammatory reactions can occur (e.g., skin weeping, erosion). Dosing interruption may be required

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.

Flu-like systemic signs and symptoms including malaise, fever, nausea, myalgias and rigors may occur. Dosing interruption may be required

Avoid exposure to sunlight and sunlamps. Wear sunscreen daily

Safety and efficacy have not been established for repeat courses of treatment to the same area for AK

Aldara Cream is not recommended for treatment of BCC subtypes other than the superficial variant, i.e., sBCC

Treatment of urethral, intra-vaginal, cervical, rectal or intra-anal viral disease is not recommended

Safety and efficacy in immunosuppressed patients have not been established

Food Interaction

• Take with or without food.

Elimination Route

Well absorbed through skin (as a cream)

Half Life

20 hours (topical dose), 2 hours (subcutaneous dose)

Pregnancy & Breastfeeding use

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

Special Warning

Pediatric Use: AK and sBCC are not conditions generally seen within the pediatric population. The safety and efficacy of Imiquimod 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

Storage Condition

Store at 4 - 25°C

Innovators Monograph

You find simplified version here Imiquimod