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Imiquimod

 
Drug Info: Imiquimod

Brand names: Aldara™

Chemical formula:



Imiquimod skin cream

What is imiquimod skin cream?

IMIQUIMOD (Aldara™) cream is used to treat skin conditions including external genital or anal warts. Because imiquimod does not kill the virus (HPV virus) that causes genital or anal warts, new warts may appear during or after treatment. This drug is also effective at treating other skin conditions such as actinic keratosis and superficial basal cell cancers. Generic imiquimod skin cream is not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• an unusual or allergic reaction to imiquimod, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Apply imiquimod cream to the affected areas as directed on the prescription label. Wash hands before and after applying cream. Imiquimod cream should be applied just before bedtime. A thin layer of the cream should be applied topically with the fingers; the cream should be massaged gently into the affected areas until no longer visible. Avoid contact with lips, eyes, or nose. Use imiquimod cream only on the affected area as directed by your health care provider. Do not use imiquimod cream longer than prescribed. Using too much imiquimod cream or using it too often, or for too long can increase your chances for having a severe skin reaction or other side effect. Discard packet after applying to affected area; partial packets should not be saved or reused.

• For treatment of genital or anal warts: You will usually apply this cream every other day (3 times a week) until the warts are gone, for a maximum of 16 weeks. Do not use the cream inside the vagina or rectum. Avoid getting imiquimod cream in your eyes. Uncircumcised men treating warts under the foreskin of the penis should pull back the foreskin and clean the area daily. Women should take special care if applying the cream at the opening of the vagina because local skin reactions on the delicate moist surfaces can cause pain and swelling, and may cause problems passing urine. Do not bandage or wrap the treated area. The treated area should be washed with mild soap and water 6—10 hours after applying the cream (usually upon waking).

• For the treatment of actinic keratosis: You will apply the cream to the affected area twice weekly, 3—4 days apart, for 16 weeks. Leave on skin for about 8 hours as directed, after which time the cream should be washed off using mild soap and water usually upon waking. The area you treat with imiquimod cream should be no larger than the size of your forehead or one cheek (for example, 2 inches by 2 inches).

• For the treatment of superficial basal cell cancer: You will apply the cream to the affected area 5-times per week for 6 weeks (such as Monday through Friday before going to bed). Leave the cream on your skin for about 8 hours, as directed, after which time the cream should be washed off using mild soap and water.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed. This drug has been used in adolescents for the treatment of genital or anal warts.

What if I miss a dose?

If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use only that dose. Do not use double or extra doses.

What drug(s) may interact with imiquimod?

Imiquimod treatment is not recommended until the skin has healed from any previous drug (example: podofilox or podophyllin resin) or surgical skin treatment.

Tell your prescriber or health care professional about all other medicines you are using or taking, including non-prescription medicines. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking imiquimod?

• During the treatment of genital or anal warts:
Visit your health care professional for regular checks on your progress. Females should receive regular pelvic exams as recommended by their prescribers.

You will notice improvement in your condition gradually. Most patients experience improvement within 4 weeks. However, it may take up to 16 weeks to see a full clearing of the warts. Imiquimod cream is not a cure. New warts may develop during or after treatment.

Sexual (genital, anal, oral) contact should be avoided while the cream is on the skin.

Imiquimod cream will not cure genital or anal warts. It is also not known if imiquimod cream can stop you from spreading genital or anal warts to other people. The only way to prevent infecting others with the HPV virus (the virus that causes genital warts) is to avoid direct skin-to-skin contact. If warts are visible in the genital area, sexual contact should be avoided until the warts are treated. Experts advise that using latex condoms during sexual contact may reduce, but not entirely prevent, infecting others.

Do not rely on condoms, diaphragms, cervical caps or other 'barrier' devices as your sole method of birth control. Imiquimod cream may weaken these devices and make them less effective at birth control.

Do not cover the treated area with an airtight bandage. Cotton gauze dressings can be used. Cotton underwear can be worn after applying imiquimod cream to the genital or anal area.

• During the treatment of actinic keratosis or superficial basal cell cancer:
Visit your health care provider for regular checks on your progress. Actinic keratoses that were not seen before may appear during treatment and may later go away. The treatment area and surrounding area may lighten or darken after treatment with imiquimod cream. These skin color changes may be permenant in some patients.

It is common for patients to have skin reactions in areas treated. These reactions may extend beyond the application site onto the surrounding skin. Skin reactions generally decrease in intensity or resolve after stopping imiquimod therapy. If you experience a severe reaction or any sign or symptom at the treatment site that interferes or prevents you from doing any daily activity, contact your health care provider to discuss whether you require a rest period from treatment. Treatment may resume once the reaction has improved as recommended by your prescriber.

Use sunscreen during treatment and minimize or avoid exposure to natural or artificial sunlight (tanning beds or UVA/B treatments).

Do not cover the treated area with an airtight bandage. Cotton gauze dressings can be used.

What side effects may I notice from receiving imiquimod?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• open sores with or without drainage
• skin infection
• skin rash
• unusual or severe skin reaction

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• back pain
• burning or itching
• changes in skin color that do not always go away
• diarrhea
• feeling like you have the flu
• headache
• muscle aches
• redness of the skin (very common but is usually not painful or harmful)
• scabbing and crusting
• skin peeling
• skin that becomes hard or thickened
• swelling of the skin

Where can I keep my medicine?

Keep out of the reach of children.

Store between 4 and 25 degrees C (39 and 77 degrees F). Do not freeze. Throw away any unused portion after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Veterinary Dictionary: imiquimod
Top

A topical immune response modifier with antiviral and antineoplasia effects. Used in veterinary medicine to treat squamous cell carcinomas and viral papillomas.

Wikipedia: Imiquimod
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Imiquimod
Systematic (IUPAC) name
3-(2-methylpropyl)-3,5,8-triazatricyclo[7.4.0.02,6]trideca-1(9),2(6),4,7,10,12-hexaen-7-amine
Identifiers
CAS number 99011-02-6
ATC code D06BB10
PubChem 57469
DrugBank APRD01030
Chemical data
Formula C14H16N4 
Mol. mass 240.304 g/mol
SMILES eMolecules & PubChem
Synonyms 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 30 hours (topical dose), 2 hours (subcutaneous dose)
Excretion  ?
Therapeutic considerations
Licence data

EU EMEA:linkUS FDA:link

Pregnancy cat.

B1(AU) C(US)

Legal status

POM(UK) -only(US)

Routes Topical
 Yes check.svgY(what is this?)  (verify)

Imiquimod (INN) is a prescription medication that acts as an immune response modifier. It is marketed by MEDA AB, Graceway Pharmaceuticals and iNova Pharmaceuticals under the trade name Aldara and by Mochida as Beselna.

Contents

History

The original FDA approval was on February 27, 1997, FDA Application No. (NDA) 020723, by 3M. Imiquimod is approved to treat actinic keratosis, superficial basal cell carcinoma, and external genital warts. Adverse side effects have been reported, in some cases serious and systemic, resulting in the revision of warning labels.

Uses

Imiquimod is a patient-applied cream used to treat certain diseases of the skin, including skin cancers (basal cell carcinoma, Bowen's disease,[1] superficial squamous cell carcinoma, some superficial malignant melanomas, and actinic keratosis) as well as genital warts (Condylomata acuminata). It has also been tested for treatment of molluscum contagiosum, vulvar intraepithelial neoplasia, common warts that have proven difficult to treat, [2] and vaginal intraepithelial neoplasia.[3] Outstanding cosmetic result has resulted from the treatment of both large superficial basal cell carcinoma and squamous cell carcinoma in-situ, but the morbidity and discomfort of the treatment can be severe. Focal recurrence of tumor has been seen after imiquimod treatment, but appear to be amenable to surgical excision.

Imiquimod can also cause subclinical lesions to become visible. This unmasking effect is felt to be of clinical benefit as lesions that may have otherwise have been missed are being treated. Photographs of actinic keratosis and basal cell carcinomas before, during and after treatment show the unmasking of subclinical disease.[4]

Mechanism of action

The exact mechanism of action in which imiquimod and its analogs activate the immune system is not yet known. Nevertheless, it is known that imiquimod activates immune cells through the toll-like receptor 7 (TLR7), commonly involved in pathogen recognition, on the cell surface.[5] Cells activated by imiquimod via TLR-7 secrete cytokines (primarily interferon-α (IFN-α), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α)). [6] There is evidence that imiquimod, when applied to skin, can lead to the activation of Langerhans cells, which subsequently migrates to local lymph nodes to activate the adaptive immune system.[7] Other cell types activated by imiquimod include natural killer cells, macrophages and B-lymphocytes.[7]

New research has shown that imiquimod's anti-proliferative effect is totally independent of immune system activation or function. Imiquimod exerts its effect by increasing levels of the opioid growth factor receptor (OGFr). Blocking OGFr function with siRNA technology resulted in loss of any antiproliferative effect of imiquimod.[8]

Disadvantages

Non specific inflammation and dermatitis can occur during use of imiquimod for genital warts and molluscum.[citation needed] This often occurs where the skin is traumatized from scratching, or between skin folds. Blisters, bloody dry eschar, pain and discomfort often follows the use of imiquimod for skin cancers and precancerous growths.[citation needed] During the treatment of large superficial basal cell carcinoma or squamous cell cancer in situ, areas of black dried crust often form.[citation needed] Many individuals with extensive actinic keratosis cannot tolerate the resulting reaction either.[citation needed] Fortunately, after completion of the therapy, the skin often heals with barely any scarring.

Recurrence of skin cancer has been noted with Imiquimod, but often appears to be localized. It is more common when there are deeply penetrating nests of tumor cells such as in nodular basal cell carcinoma. Recurrence can be treated surgically by local excision. The recurrence rate depends on the condition being treated and the frequency of topical imiquimod application. A 6-week study on 99 patients with superficial basal cell carcinomas found success rates of 100%, 88%, 73% and 70% for twice daily, once daily, 6 times weekly and 3 times weekly application, respectively [9].

Other side effects include reoccurring severe headaches, back pain, muscle aches, tiredness, flu-like symptoms, swollen lymph nodes, diarrhea, and fungal infections.[10]

See also

References

  1. ^ van Egmond S, Hoedemaker C, Sinclair R (2007). "Successful treatment of perianal Bowen's disease with imiquimod". Int J Dermatol 46 (3): 318–9. doi:10.1111/j.1365-4632.2007.03200.x. PMID 17343595. 
  2. ^ van Seters M, van Beurden M, ten Kate FJ, et al. (April 2008). "Treatment of vulvar intraepithelial neoplasia with topical imiquimod". The New England journal of medicine 358 (14): 1465–73. doi:10.1056/NEJMoa072685. PMID 18385498. http://content.nejm.org/cgi/content/full/358/14/1465. 
  3. ^ Buck HW, Guth KJ (October 2003). "Treatment of vaginal intraepithelial neoplasia (primarily low grade) with imiquimod 5% cream". Journal of lower genital tract disease 7 (4): 290–3. doi:10.1097/00128360-200310000-00011. PMID 17051086. 
  4. ^ Photographs before, during, and after imiquimod therapy for actinic keratosis and basal cell carcinoma
  5. ^ Hemmi, H., et al. Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway. Nat Immunol.. 2002 3(2):196-200. PMID 11812998.
  6. ^ Sauder, D.N., Imiquimod: modes of action. British Journal of Dermatology. 2003 149(Suppl. 66):5-8. PMID 14616337
  7. ^ a b Miller, R.L., et al. Imiquimod applied topically: a novel immune response modifier and a new class of drug. Int J Immunopharmacol. 1999 Jan;21(1):1-14. PMID 10411278
  8. ^ Zagon IS, Donahue RN, Rogosnitzky M, McLaughlin PJ (August 2008). "Imiquimod upregulates the opioid growth factor receptor to inhibit cell proliferation independent of immune function". Exp. Biol. Med. (Maywood) 233 (8): 968–79. doi:10.3181/0802-RM-58. PMID 18480416. 
  9. ^ Advances in the use of topical imiquimod to treat dermatologic disorders
  10. ^ Aldara website, What are the possible side effects of Aldara Cream?

External links


 
 

 

Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Imiquimod" Read more