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Imiquimod

Generic Medicine
Indications

Imiquimod cream is used for:

  • Treatment of external genital and perianal warts in adults.
  • Treatment of small superficial basal cell carcinoma in adults.
  • Treatment of clinically typical, non-hyperkeratotic, non-hypertrophic actinic keratosis on the face or scalp in immunocompetent adults, especially when cryotherapy or other topical treatments are not suitable or effective due to the size or number of lesions.
Pharmacology

Imiquimod is a toll-like receptor-7 (TLR-7) agonist that enhances both innate and adaptive immune responses. It stimulates the production of cytokines such as: Interferon-alpha (IFN-α), Interleukins (IL-1, IL-6, IL-8, IL-10, IL-12), Tumor necrosis factor-alpha (TNF-α). It also: Activates natural killer (NK) cells, Promotes proliferation of B-cells. Activates Langerhans cells and helps them migrate to lymph nodes. Stimulates TH-1 cells to produce interferon-gamma (IFN-γ), which activates cytotoxic T lymphocytes. These immune responses help destroy infected or abnormal cells and provide long-term immune memory against viruses or tumors.

Dosage Administration

External genital warts in adults: Imiquimod cream should be applied 3 times per week (example: Monday, Wednesday, and Friday; or Tuesday, Thursday, and Saturday) prior to normal sleeping hours, and should remain on the skin for 6 to 10 hours. Imiquimod cream treatment should continue until the clearance of visible genital or perianal warts or for a maximum of 16 weeks per episode of warts.

Imiquimod cream should be applied in a thin layer and rubbed on the clean wart area until the cream vanishes. Only apply to affected areas and avoid any application on internal surfaces. Imiquimod cream should be applied prior to normal sleeping hours. During the 6 to 10 hour treatment period, showering or bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Application of an excess of cream or prolonged contact with the skin may result in a severe application site reaction. A single use sachet is sufficient to cover a wart area of 20 cm² (approx. 3 inches²). Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream. Uncircumcised males treating warts under the foreskin should retract the foreskin and wash the area daily.

Superficial basal cell carcinoma in adults: Apply Imiquimod cream for 6 weeks, 5 times per week (example: Monday to Friday) prior to normal sleeping hours, and leave on the skin for approximately 8 hours. Before applying Imiquimod cream, patients should wash the treatment area with mild soap and water and dry thoroughly. Sufficient cream should be applied to cover the treatment area, including one centimetre of skin surrounding the tumour. The cream should be rubbed into the treatment area until the cream vanishes. The cream should be applied prior to normal sleeping hours and remain on the skin for approximately 8 hours. During this period, showering and bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream. Response of the treated tumour to Imiquimod cream should be assessed 12 weeks after the end of treatment. If the treated tumour shows an incomplete response, a different therapy should be used. A rest period of several days may be taken if the local skin reaction to Imiquimod cream causes excessive discomfort to the patient, or if infection is observed at the treatment site. In this latter case, appropriate other measures should be taken.

Actinic keratosis in adults: Treatment should be initiated and monitored by a physician. Imiquimod cream should be applied 3 times per week (example: Monday, Wednesday and Friday) for four weeks prior to normal sleeping hours, and left on the skin for approximately 8 hours. Sufficient cream should be applied to cover the treatment area. After a 4-week treatment-free period, clearance of Actinic Keratosis should be assessed. If any lesions persist, treatment should be repeated for another four weeks. An interruption of dosing should be considered if intense local inflammatory reactions occur or if infection is observed at the treatment site. In this latter case, appropriate other measures should be taken. Each treatment period should not be extended beyond 4 weeks due to missed doses or rest periods. If the treated area does not show complete clearance at a follow-up examination about 8 weeks after the last 4-weeks course of treatment, an additional 4-weeks course of Imiquimod treatment may be considered. A different therapy is recommended if the treated lesion(s) shows insufficient response to Imiquimod. Actinic keratosis lesions that have cleared after one or two courses of treatment and subsequently recur can be re-treated with one or two further courses of Imiquimod cream following an at least 12 weeks treatment pause. Before applying Imiquimod cream, patients should wash the treatment area with mild soap and water and dry thoroughly. Sufficient cream should be applied to cover the treatment area, including one centimetre of skin surrounding the tumour. The cream should be rubbed into the treatment area until the cream vanishes. The cream should be applied prior to normal sleeping hours and remain on the skin for approximately 8 hours. During this period, showering and bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream.

Information applicable to all indications: If a dose is missed, the patient should apply the cream as soon as he/she remember and then he/she should continue with the regular schedule. However the cream should not be applied more than once a day.

Interactions

No formal interaction studies have been conducted, including with immunosuppressive drugs. Systemic drug interactions are expected to be minimal due to low skin absorption of imiquimod. However, caution is advised when using imiquimod with immunosuppressive medications because of its immune-stimulating effects.

Contraindications

Imiquimod cream should not be used in patients who are hypersensitive to imiquimod or any of the excipients in the formulation.

Side Effects

Reported side effects include infections (bacterial, fungal, upper respiratory), genital and vaginal disorders, lymphadenopathy, loss of appetite, insomnia, depression, irritability, headache, dizziness, migraine, drowsiness, eye irritation, tinnitus, flushing, throat irritation, nasal congestion, nausea, abdominal pain, diarrhea, vomiting, rectal discomfort, dry mouth, itching, rash, eczema, increased sweating, urticaria, redness, swelling, skin ulcer, muscle pain, joint pain, back pain, urinary symptoms, sexual dysfunction, and various application site reactions such as burning, irritation, redness, inflammation, bleeding, papules, ulcer, warmth, fever, fatigue, and discomfort.Changes in skin pigmentation (hypopigmentation or hyperpigmentation) have been reported. Hair loss at the application site (about 0.4%) has also been observed. Some patients showed reductions in blood counts (hemoglobin, white cells, neutrophils, platelets).

Pregnancy & Lactation

No adequate human studies are available. Imiquimod should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Similarly, during breastfeeding, use only if benefits outweigh risks to the infant.

Precautions & Warnings

Avoid use in patients with hypersensitivity to the drug or its components.

Special Populations

Children: Not recommended for children under 12 years.

Elderly: Can be used in elderly patients.

Driving & machinery: Unlikely to affect ability.

Overdose Effects

Systemic overdose is unlikely due to low skin absorption. However, excessive topical use may cause severe local skin reactions. Accidental ingestion may cause nausea, vomiting, headache, muscle pain, and fever. High oral doses may lead to low blood pressure, which can be treated with fluids.

Therapeutic Class

Immunosuppressant, miscellaneous topical agent

Storage Conditions

Store in a cool, dry place, protected from light, at 4°C–25°C.

Common Questions

What is Imiquimod for?

What does Imiquimod do?

What are the side effects of Imiquimod?

What happens if you use too much Imiquimod?

Can Imiquimod be used during pregnancy?

No available drugs found

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