Imiquimod


Generic Medicine Info
Indications and Dosage
Topical/Cutaneous
Actinic keratoses
Adult: For the treatment of clinically typical, nonhyperkeratotic, nonhypertrophic, visible or palpable cases: As 2.5% or 3.75% cream: Apply thinly onto the entire face or balding scalp once daily before bedtime for 2 weeks; after a 2-week treatment-free interval, repeat a 2nd 2-week treatment course. Assess response 8 weeks after the 2nd course. Max: 2 sachets daily or 2 full pump actuations daily. Rest periods may be taken if local skin reactions occur, but treatment period must not be extended due to missed doses or rest periods. Therapy must be continued for the full treatment course even if all actinic keratoses appear to be gone. As 5% cream: Apply onto the face or scalp 3 times each week before bedtime for 4 weeks; after a 4-week treatment-free interval, assess response then repeat another 4-week treatment course if any lesions persist. Alternatively, apply onto the face or scalp 2 times each week for 16 weeks. Max: 1 sachet at each application. Rest periods may be taken if local skin reactions occur, but the treatment period must not be extended beyond 4 weeks or 16 weeks due to missed doses or rest periods. All doses must be left on the skin for approx 8 hours, then washed with mild soap and water. Dosage and treatment recommendations may vary among individual products or between countries (refer to specific product or local guidelines).

Topical/Cutaneous
Superficial basal cell carcinoma
Adult: For the treatment of biopsy-confirmed cases with a max tumour diameter of 2 cm located on the neck, trunk (except anogenital skin), or extremities (except hands and feet) when surgical methods are less appropriate and patient follow-up can be assured: As 5% cream: Apply sufficient amount to cover the lesion and 1 cm beyond it 5 times each week (on consecutive days) before bedtime; leave on skin for approx 8 hours, then wash with mild soap and water. Treatment duration: 6 weeks. Assess response 12 weeks after treatment completion.

Topical/Cutaneous
Genital warts, Perianal warts
Adult: As 3.75% cream: Apply thinly onto the affected area(s) once daily before bedtime; leave on the skin for approx 8 hours, then wash with mild soap and water. Continue treatment until total clearance or for a Max duration of 8 weeks. As 5% cream: Apply thinly 3 times each week (on alternate days) before bedtime; leave on the skin for 6-10 hours, then wash with mild soap and water. Continue treatment until total clearance or for a Max duration of 16 weeks. Dosage and treatment recommendations may vary among individual products or between countries (refer to specific product or local guidelines).
Special Precautions
Patient with pre-existing autoimmune disorders, inherent sensitivity to sunlight or potential for considerable sun exposure (e.g. occupational reasons); reduced haematologic reserve. Immunocompromised patients, including organ transplant patients. Uncircumcised males. Not indicated for urethral, cervical, rectal, intravaginal, or intra-anal HPV disease. Not recommended to be used until the skin has healed from any previous sunburn, drug or surgical treatment. Not intended for oral, nasal, or ophthalmic use. Pregnancy and lactation.
Adverse Reactions
Significant: Intense local inflammatory reactions (e.g. skin weeping or erosion), photosensitivity, severe vulvar swelling which may lead to urinary retention; flu-like symptoms (e.g. chills, fever, fatigue, arthralgia, malaise); may exacerbate autoimmune disorders or inflammatory skin conditions (including graft-versus-host-disease).
Blood and lymphatic system disorders: Lymphadenopathy.
Cardiac disorders: Chest pain.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea.
General disorders and administration site conditions: Application site reactions (e.g. dryness, pruritus, pain, irritation, burning sensation, rash, erythema, oedema, paraesthesia, discharge, scabbing, exfoliation, ulceration).
Infections and infestations: Fungal infection, herpes simplex.
Investigations: Increased blood glucose.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Myalgia, back pain.
Neoplasms benign, malignant and unspecified: Squamous cell carcinoma.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Insomnia.
Reproductive system and breast disorders: Bacterial vaginosis.
Respiratory, thoracic and mediastinal disorders: URTI, sinusitis.
Skin and subcutaneous tissue disorders: Skin hypopigmentation or hyperpigmentation, dermatitis, erythema multiforme.
Patient Counseling Information
Avoid contact with eyes, lips, nostrils and broken skin. Avoid or minimise exposure to sunlight, UV lights, and tanning beds; use protective clothing during therapy. Avoid the use of excessive amounts of cream or occlusive dressing. Avoid sexual contact while the cream is on the skin as it may weaken condoms and diaphragms (when used for external genital or perianal warts).
Monitoring Parameters
Establish a histological basis for superficial basal cell carcinoma prior to therapy. Periodically assess response to treatment, particularly for a reduction in lesion size. Monitor for local skin reactions and signs and symptoms of hypersensitivity.
Action
Description:
Mechanism of Action: Imiquimod is an immune response modifier and a Toll-like receptor 7 agonist that activates immune cells. Its exact mechanism of action has not been determined; however, it may induce the release of interferon-α (IFN-α) and other cytokines and enhance cell-mediated cytolytic antiviral activity.
Pharmacokinetics:
Absorption: Minimal systemic absorption. Time to peak plasma concentration: 9-12 hours.
Excretion: Via urine (<3% as unchanged drug and metabolites).
Chemical Structure

Chemical Structure Image
Imiquimod

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 57469, Imiquimod. https://pubchem.ncbi.nlm.nih.gov/compound/Imiquimod. Accessed Nov. 23, 2023.

Storage
Store below 25°C. Do not freeze. Keep the cream in pump bottle upright.
MIMS Class
Other Dermatologicals
ATC Classification
D06BB10 - imiquimod ; Belongs to the class of topical antivirals used in the treatment of dermatological diseases.
References
Aldara 5% Cream (Mylan Products Ltd). MHRA. https://products.mhra.gov.uk. Accessed 11/10/2023.

Aldara Cream (Bausch Health US LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 27/06/2023.

Aldara Cream 5% w/w (iNova Pharmaceuticals [Singapore] Pte Ltd [Incorporated in Singapore] Malaysia Branch). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 27/06/2023.

Anon. Imiquimod. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 27/06/2023.

Anon. Imiquimod. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/06/2023.

Buckingham R (ed). Imiquimod. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/06/2023.

Joint Formulary Committee. Imiquimod. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/06/2023.

Orion Laboratories (NZ) Ltd. Imiquimod Cream 5% w/w Topical Cream data sheet 22 September 2017. Medsafe. http://www.medsafe.govt.nz. Accessed 29/06/2023.

Zyclara 3.75% Cream (Mylan Products Ltd). MHRA. https://products.mhra.gov.uk. Accessed 27/06/2023.

Zyclara Cream (Bausch Health US, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/10/2023.

Disclaimer: This information is independently developed by MIMS based on Imiquimod from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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