Generic
Imiquimod
2 brands available in the market
At a glance
Imiquimod cream is used for the topical treatment of external genital and perianal warts, small superficial basal cell carcinomas, and actinic keratoses on the face or scalp.
Description
Imiquimod is an immune response modifier that acts as a toll-like receptor-7 agonist. It enhances both innate and acquired immune responses by inducing production of IFN-α and other cytokines. It stimulates natural killer cells, B-cell proliferation, and activates Langerhans cells. It stimulates TH-1 cells to produce IFN-γ, which activates cytotoxic T lymphocytes and provides long-term immune memory.
Indications
- External genital and perianal warts (adults)
- Small superficial basal cell carcinomas (adults)
- Actinic keratoses on face or scalp (immunocompetent adults)
Therapeutic class
Immunosuppressant, Miscellaneous topical agents
Pharmacological class
Immune Response Modifier (Toll-like Receptor 7 Agonist)
Pharmacology
Imiquimod is a toll-like receptor-7 agonist enhancing both innate and acquired immune response. It activates production of numerous compounds including IFN-α, IL-1, -6, -8, -10, -12, and TNF-α, stimulates natural killer cells and B-cell proliferation. It also activates Langerhans cells and promotes their migration to regional lymph nodes. Imiquimod stimulates TH-1 cells to produce IFN-γ, which can activate cytotoxic T lymphocytes providing long-term immune memory.
Mechanism of action
Acts as a toll-like receptor-7 agonist to activate immune cells; induces production of IFN-α and other cytokines to provide antiviral and antitumor activity.
Dosage
Adult Dose (Topical):
- External Genital & Perianal Warts (5% cream): Apply 3 times weekly (non-consecutive days) before bedtime, leave for 6-10 hours; max 16 weeks
- External Genital & Perianal Warts (3.75% cream): Apply once daily until clearance or max 8 weeks
- Superficial Basal Cell Carcinoma (5% cream): Apply 5 times weekly (consecutive days) for 6 weeks, leave for 8 hours; assess response 12 weeks after treatment
- Actinic Keratoses (2.5% or 3.75% cream): Apply daily on face/scalp for 2 weeks, 2-week break, assess response 8 weeks after 2nd course
- Actinic Keratoses (5% cream): Apply 3 times weekly for 4 weeks, 4-week break, repeat if necessary
Child Dose: Safety and efficacy not established in children <12 years
Administration
For external use only; apply to clean and dry affected area; apply thin layer and rub until cream vanishes; apply before bedtime; leave for 6-10 hours (warts) or 8 hours (BCC/AK); wash off with mild soap and water; wash hands before and after application.
Missed dose
If you miss a dose, apply it as soon as possible; do not apply more than once a day.
Side effects
Common Side Effects:
- Dry skin
- Application site itching, burning, redness, swelling, skin ulceration
Others: Pustules, genital candidiasis, vaginitis, bacterial/fungal infections, upper respiratory tract infection, headache, dizziness, migraine, nausea, diarrhea, myalgia, arthralgia
Precautions & warnings
Precautions:
- Avoid direct contact with eyes; if contact occurs, wash with water and seek immediate medical attention
- Inform doctor if pregnant, planning pregnancy or breastfeeding
- Inform doctor if any kidney or liver disease
- Caution in patients receiving immunosuppressive medication
- Application of excess cream or prolonged contact may cause severe local reactions
Contraindications
Contraindications:
- Hypersensitivity to imiquimod or cream excipients
Drug interactions
No interaction studies have been performed; caution with immunosuppressive drugs.
Food interactions
No food interaction found/established.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies have shown harmful effects; use only if potential benefit justifies potential risk to fetus.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests drug does not represent significant risk to baby.
Pediatric use
Not recommended for children below 12 years.
Geriatric use
Recommended for elderly patients.
Renal / hepatic impairment
No interaction found/established.
Overdose effects
Systemic overdosage unlikely with topical use; accidental ingestion (200 mg) may cause nausea, vomiting, headache, myalgia, fever; hypotension reported with multiple oral doses ≥200 mg.
Storage conditions
Store in a cool & dry place, protected from light; store at 4°-25°C.
Chemical structure
Imiquimod