Pimecrolimus
Drug Info:
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Pimecrolimus
Brand names: Elidel®
Chemical formula:
- Drug Forms:
- Pimecrolimus skin cream (below)
- Pimecrolimus Topical cream
Pimecrolimus skin cream
What is pimecrolimus skin cream?
PIMECROLIMUS (Elidel®) is used to treat certain skin conditions including atopic dermatitis (eczema). Generic pimecrolimus cream is not 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:
• cold sores or shingles
• Netherton's syndrome
• receiving any form of light therapy (phototherapy, UVA, or UVB) to your skin
• skin infection
• an unusual or allergic reaction to pimecrolimus, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I use this medicine?
Pimecrolimus cream is applied to the skin; avoid contact with the eyes. Apply a thin layer to the affected areas. Rub in gently and completely. Usually, you will continue using the cream until the areas heal. Wash your hands before and after use, unless you are treating your hands. Do not cover the treated skin with bandages or other dressings. Do not use your medicine more often than directed or for other types of skin conditions unless directed by your health care provider.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What drug(s) may interact with pimecrolimus cream?
• alcoholic beverages or medications containing high percentages of alcohol
Tell your prescriber or health care professional about other skin products you are using. Do not apply pimecrolimus at the same site as other skin preparation without advice.
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. 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 pimecrolimus cream?
Improvements to your skin may occur after the first few weeks of treatment. Even though your skin looks better, it is important to keep using the cream as instructed by your health care provider. If you do not notice an improvement in your condition or if your condition gets worse within the first few weeks of treatment, tell your health care professional.
Avoid sunlight, sun lamps, tanning beds and treatment with UVA or UVB light while using pimecrolimus cream. If you need to be outdoors after applying the cream, wear loose fitting clothing that protects the treated area from the sun. Ask your health care provider what other type of sun protection you should use.
Do not cover the skin being treated with bandages, dressings, or wraps. Unless otherwise instructed by your health care provider, do not apply another type of skin product on top of pimecrolimus cream. However, you can wear normal clothing over the treated areas.
Do not bathe, shower, or swim right after applying pimecrolimus cream. This could wash off the cream.
While you are using pimecrolimus cream, drinking alcohol may cause the skin or face to become flushed or red and feel hot. Let your prescriber know if you notice such reactions.
What side effects may I notice from using pimecrolimus cream?
Side effects that you should report to your prescriber or health care professional as soon as possible:
• chickenpox infection
• cold sores or shingles
• extreme tiredness
• hives
• infection at site of application
• skin bleeding or change in your skin's appearance (color, change in a mole or freckle, new growth)
• swollen glands (lymph nodes)
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• irritation at the site or sites where you apply pimecrolimus including stinging, feeling of warmth or burning
• runny nose
Where can I keep my medicine?
Keep out of reach of children.
Store the skin cream at room temperature, 15—30 degrees C (59—86 degrees F).
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.
Oxford A-Z of Medicinal Drugs:
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pimecrolimus
A drug that affects the immune response, used in the treatment of mild to moderate eczema when topical corticosteroids cannot be given. It works by modulating the inflammatory chemicals secreted by some white blood cells. Pimecrolimus is available as a cream on prescription only.
Side effects:
include skin irritation, itching, and skin infection.
Precautions:
the cream should not be applied to skin that is infected, reddened, or flaking or to skin tumours. It should not be used by people with immune deficiency. Excessive exposure to sunlight or sun lamps and consumption of alcohol should be avoided as these can cause skin irritation. Pimecrolimus is not recommended for children under two years of age.
Proprietary preparation:
Elidel.
| pilocarpine, phytomenadione, phosphodiesterase inhibitors | |
| pimozide, pindolol, pioglitazone |
Wikipedia on Answers.com:
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Pimecrolimus
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|---|---|
| Systematic (IUPAC) name | |
| (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS) |
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| Clinical data | |
| Trade names | Elidel |
| AHFS/Drugs.com | monograph |
| Pregnancy cat. | C (US) |
| Legal status | ℞-only (US) |
| Routes | topical |
| Pharmacokinetic data | |
| Bioavailability | low systemic absorption |
| Protein binding | 74%–87% |
| Metabolism | Hepatic CYP3A |
| Identifiers | |
| CAS number | 137071-32-0  |
| ATC code | D11AH02 |
| PubChem | CID 16051947 |
| DrugBank | DB00337 |
| ChemSpider | 10482089 |
| UNII | 7KYV510875 |
| ChEMBL | CHEMBL1200686  |
| Chemical data | |
| Formula | C43H68ClNO11 |
| Mol. mass | 810.453 g/mol |
| SMILES | eMolecules & PubChem |
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 (what is this?) (verify) |
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Pimecrolimus is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). It is currently available as a topical cream, once marketed by Novartis (however, Galderma has been promoting the compound in Canada since early 2007) under the trade name Elidel.
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Contents
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Pharmacology
Pimecrolimus is an ascomycin macrolactam derivative. It has been shown in vitro that pimecrolimus binds to macrophilin-12(also referred to as FKBP-12) and inhibits calcineurin. Thus pimecrolimus inhibits T-cell activation by inhibiting the synthesis and release of cytokines from T-cells. Pimecrolimus also prevents the release of inflammatory cytokines and mediators from mast cells.
General characteristics
Pimecrolimus, like tacrolimus, belongs to the ascomycin class of macrolactam immunosuppressives, acting by the inhibition of T-cell activation by the calcineurin pathway and inhibition of the release of numerous inflammatory cytokines, thereby preventing the cascade of immune and inflammatory signals.[1] Pimecrolimus has a similar mode of action to that of tacrolimus but is more selective, with no effect on dendritic (Langerhans) cells.[2] It has lower permeation through the skin than topical steroids or topical tacrolimus[3] although they have not been compared with each other for their permeation ability through mucosa. In addition, in contrast with topical steroids, pimecrolimus does not produce skin atrophy.[4] It has been proven to be effective in various inflammatory skin diseases, e.g., seborrheic dermatitis,[5] cutaneous lupus erythematosus,[6] oral lichen planus,[7] vitiligo,[8] and psoriasis.[9][10] Tacrolimus and pimecrolimus are both calcineurin inhibitors and function as immunosuppressants.[11]
Side effects
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This section may require cleanup to meet Wikipedia's quality standards. (Consider using more specific cleanup instructions.) Please help improve this section if you can. The talk page may contain suggestions. (September 2009) |
See also: Immunomodulators in the treatment of eczema
In January 2006, the United States Food and Drug Administration (FDA) announced that Elidel packaging would be required to carry a black box warning regarding the potential increased risk of lymph node or skin malignancy, as for the similar drug tacrolimus. Whereas current practice by UK dermatologists is not to consider this a significant real concern and they are increasingly recommending the use of such new drugs.[12]
Importantly, although the FDA has approved updated black-box warning for tacrolimus and pimecrolimus, the recent report of the American Academy of Dermatology Association Task Force finds that there is no causal proof that topical immunomodulators cause lymphoma or nonmelanoma skin cancer, and systemic immunosuppression after short-term or intermittent long-term topical application seems an unlikely mechanism.[13] Another recent review of evidence concluded that postmarketing surveillance shows no evidence for this systemic immunosuppression or increased risk for any malignancy.[14] However, there are still some strong debates and controversies regarding the exact indications of immunomodulators and their duration of use in the absence of active controlled trials.[15] Dermatologists' and Allergists' professional societies, the American Academy of Dermatology[1], and the American Academy of Allergy, Asthma, and Immunology, have protested the inclusion of the black box warning. The AAAAI states "None of the information provided for the cases of lymphoma associated with the use of topical pimecrolimus or tacrolimus in AD indicate or suggest a causal relationship."[2].
Footnotes
- ^ Allen BR, Lakhanpaul M, Morris A, Lateo S, Davies T, Scott G, Cardno M, Ebelin ME, Burtin P, Stephenson TJ (2003). "Systemic exposure, tolerability, and efficacy of pimecrolimus cream 1% in atopic dermatitis patients". Arch Dis Child 88 (11): 969–973. doi:10.1136/adc.88.11.969. PMC 1719352. PMID 14612358. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1719352.
- ^ Meingassner JG, Kowalsky E, Schwendinger H, Elbe-Bürger A, Stütz A (2003). "Pimecrolimus does not affect Langerhans cells in murine epidermis". Br J Dermatol 149 (4): 853–857. doi:10.1046/j.1365-2133.2003.05559.x. PMID 14616380.
- ^ Billich A, Aschauer H, Aszódi A, Stuetz A (2004). "Percutaneous absorption of drugs used in atopic eczema: pimecrolimus permeates less through skin than corticosteroids and tacrolimus". Int J Pharm 269 (1): 29–35. doi:10.1016/j.ijpharm.2003.07.013. PMID 14698574.
- ^ Firooz A, Solhpour A, Gorouhi F, Daneshpazhooh M, Balighi K, Farsinejad K, Rashighi-Firoozabadi M, Dowlati Y (2006). "Pimecrolimus cream, 1%, vs hydrocortisone acetate cream, 1%, in the treatment of facial seborrheic dermatitis: a randomized, investigator-blind, clinical trial". Archives of Dermatology 142 (8): 1066–1067. doi:10.1001/archderm.142.8.1066. PMID 16924062.
- ^ Firooz A, Solhpour A, Gorouhi F, Daneshpazhooh M, Balighi K, Farsinejad K, Rashighi-Firoozabadi M, Dowlati Y (2006). "Pimecrolimus cream, 1%, vs hydrocortisone acetate cream, 1%, in the treatment of facial seborrheic dermatitis: a randomized, investigator-blind, clinical trial". Archives of Dermatology 142 (8): 1066–1067. doi:10.1001/archderm.142.8.1066. PMID 16924062. http://www.ncbi.nlm.nih.gov/pubmed/16924062.
- ^ Kreuter A, Gambichler T, Breuckmann F, Pawlak FM, Stücker M, Bader A, Altmeyer P, Freitag M (2004). "Pimecrolimus 1% cream for cutaneous lupus erythematosus". J Am Acad Dermatol 51 (3): 407–410. doi:10.1016/j.jaad.2004.01.044. PMID 15337984.
- ^ Gorouhi F, Solhpour A, Beitollahi JM, Afshar S, Davari P, Hashemi P, Nassiri Kashani M, Firooz A (2007). "Randomized trial of pimecrolimus cream versus triamcinolone acetonide paste in the treatment of oral lichen planus". J Am Acad Dermatol 57 (5): 806–813. doi:10.1016/j.jaad.2007.06.022. PMID 17658663.
- ^ Boone B, Ongenae K, Van Geel N, Vernijns S, De Keyser S, Naeyaert JM (2007). "Topical pimecrolimus in the treatment of vitiligo". Eur J Dermatol 17 (1): 55–61. doi:10.1111/j.1610-0387.2006.06124.x. PMID 17081269.
- ^ Kreuter A, Sommer A, Hyun J, Bräutigam M, Brockmeyer NH, Altmeyer P, Gambichler T (2006). "1% pimecrolimus, 0.005% calcipotriol, and 0.1% betamethasone in the treatment of intertriginous psoriasis: a double-blind, randomized controlled study". Arch Dermatol 142 (9): 1138–1143. doi:10.1001/archderm.142.9.1138. PMID 16983001.
- ^ Jacobi A, Braeutigam M, Mahler V, Schultz E, Hertl M (2008). "Pimecrolimus 1% cream in the treatment of facial psoriasis: a 16-week open-label study". Dermatology 216 (2): 133–136. doi:10.1159/000111510. PMID 18216475.
- ^ Scheinfeld N (2004). "The use of topical tacrolimus and pimecrolimus to treat psoriasis: a review". Dermatol. Online J. 10 (1): 3. PMID 15347485.
- ^ N H Cox and Catherine H Smith (December 2002). "Advice to dermatologists re topical tacrolimus" (DOC). Therapy Guidelines Committee. British Association of Dermatologists. http://www.bad.org.uk/healthcare/guidelines/Advice_re_topical_tacrolimus.doc.
- ^ Berger TG, Duvic M, Van Voorhees AS, VanBeek MJ, Frieden IJ; American Academy of Dermatology Association Task Force (2006). "The use of topical calcineurin inhibitors in dermatology: safety concerns Report of the American Academy of Dermatology Association Task Force". J Am Acad Dermatol 54 (5): 818–823. doi:10.1016/j.jaad.2006.01.054. PMID 16635663. http://www.ncbi.nlm.nih.gov/pubmed/16635663.
- ^ Spergel JM, Leung DY (2006). "Safety of topical calcineurin inhibitors in atopic dermatitis: evaluation of the evidence". Curr Allergy Asthma Rep 6 (4): 270–274. doi:10.1007/s11882-006-0059-7. PMID 16822378.
- ^ Stern RS (2006). "Topical calcineurin inhibitors labeling: putting the "box" in perspective". Archives of Dermatology 142 (9): 1233–1235. doi:10.1001/archderm.142.9.1233. PMID 16983018.
External links
- Elidel official homepage
- FDA News
- NPS RADAR
- Article about American Academy of Dermatology speaking out against black box warning
- Report of the Calcineurin Task Force of the ACAAI and AAAAI
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