Pimecrolimus
- Atc Codes:D11AH02
- CAS Codes:137071-32-0
- PHARMGKB ID:137071-32-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
Brand Names
Europe
Austria: Elidel; Belgium: Elidel; Bulgaria: Elidel; Czech Republic: Elidel; Denmark: Elidel; Estonia: Elidel; Finland: Elidel; France: Elidel; Germany: Douglan, Elidel, Velov; Greece: Aregen, Elidel; Hungary: Elidel; Italy: Elidel; Luxembourg: Elidel; Netherlands: Elidel; Poland: Elidel; Portugal: Aregen, Elidel; Romania: Elidel; Slovakia: Elidel; Slovenia: Elidel; Spain: Elidel, Rizan; Sweden: Elidel; UK: Elidel.
North America
Canada: Elidel; USA: Elidel.
Latin America
Argentina: Elidel; Mexico: Elidel.
Asia
Japan: Elidel.
Drug combinations
Chemistry
Pimecrolimus: C~43~H~68~ClNO~11~. Mw: 810.45. (1) 15,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,17,20,21(4H,23H)-tetrone, 3-[(1E)-2-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]-1-methylethenyl]-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-, (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-; (2)(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-3-[(E)-2-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]-1-methylvinyl]-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,26,26a-hexadecahydro-5,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,17,20,21(4H,23H)-tetrone. CAS-137071-32-0 (2000).
Pharmacologic Category
Skin and Mucous Membrane Agents, Miscellaneous. Immunosuppressive Agents. (ATC-Code: D11AH02).
Mechanism of action
Penetrates inflamed epidermis to inhibit T cell activation by blocking transcription of proinflammatory cytokine genes such as interleukin-2, interferon-gamma (Th~1~-type), interleukin-4, and interleukin-10 (Th~2~-type). Pimecrolimus binds to intracellular protein FKBP-12, inhibiting calcineurin, which blocks cytokine transcription and inhibits T-cell activation. Prevents release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE.
Therapeutic use
Short-term and intermittent long-term treatment of mild to moderate atopic dermatitis in patients not responsive to conventional therapy or when conventional therapy not appropriate.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women. Use only if clearly needed. Not recommended if breast-feeding.
Unlabeled use
Contraindications
Hypersensitivity to pimecrolimus or any component of the formulation.
Warnings and precautions
May cause local symptoms (e.g. burning, soreness, stinging) during first few days of treatment. May be associated with development of lymphadenopathy. Topical calcineurin inhibitors associated with rare cases of lymphoma and skin malignancy. Use in children <2 years of age not recommended (unknown effect on immune system development). Papilloma/warts observed. Patients with atopic dermatitis predisposed to skin infections, and pimecrolimus therapy associated with risk of developing eczema herpeticum, varicella zoster, and herpes simplex. Not recommended for use in Netherton’s syndrome or skin conditions which may increase potential for systemic absorption. Should not be used in immunocompromised patients. Topical calcineurin agents should not be applied to areas of active bacterial or viral infection. Artificial or natural sunlight exposure should be avoided.