II. Indications
- Severe refractory Atopic Dermatitis
III. Pharmacokinetics
- Normal topical use causes <5 ng/ml serum concentration
- Greater absorption in severely damaged skin
- Factors increasing serum concentrations
- Higher doses or greater surface area of application
- Inflamed skin
IV. Mechanism
- Macrolide with similar activity to Cyclosporine
- Specifically binds T Cell receptors
- Inhibits Cytokine production
- Inhibits IgE sensitivity
V. Precautions
- Increased risk of Skin Malignancy and Lymphoma
- FDA black box warning has been added
- Do not use for extended periods of time
- Use only in refractory Eczema
VI. Preparations
- Pimecrolimus (Elidel)
- Tacrolimus (Protopic)
VII. Dosing: Tracolimus
- Children over age 2 years: Apply 0.03% ointment bid
- Adults: Apply 0.03% or 0.1% ointment bid
VIII. Adverse Effects
- Local irritation (transient <1 week)
- Burning
- Erythema
- Pruritus
- Less common adverse effects
- Immunosuppression related adverse effects
- Increased malignancy risk in mice (see precautions)
IX. Precautions
- Protect treated areas from direct sunlight
- Systemic Tacrolimus associated with Skin Cancer
- Non-melanoma Skin Cancer
X. Advantages
- Very effective in refractory atopic cases
- Unlike Corticosteroids, does not cause skin atrophy
- May be useful on face and neck
XI. Disadvantages
- Expensive (costs per Red Book)
- Tacrolimus Ointment (0.03 or 0.1%): $60 per 30 grams
- Risk of malignancy (see prcautions)
XII. References
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Related Studies
elidel (on 4/20/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ELIDEL 1% CREAM | Generic | $4.13 per gram |
pimecrolimus (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
PIMECROLIMUS 1% CREAM | Generic | $4.13 per gram |
Ontology: Protopic (C0939455)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
English | Protopic, protopic |
Ontology: Elidel (C0971833)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C117268 |
English | Elidel, elidel, Novartis brand of pimecrolimus |
Ontology: Pimecrolimus (C1099414)
Definition (NCI) | A 33-epi-chloro-derivative of the ascomycin macrolactam with immunosuppressant property. Pimecrolimus binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. Via dephosphorylation, calcineurin is the enzyme responsible for activating nuclear factor of activated T-cells (NF-AT), a T cell transcriptional regulatory factor. As a consequence, the synthesis and release of Th1- (T helper 1) and Th2- (T helper 2) type cytokines, and other inflammatory mediators from T-cells and mast cells are blocked and the expression of signals essential for the activation of inflammatory T-lymphocytes is inhibited. However, pimecrolimus mode of action is cell-selective and does not affect Langerhans' cells/dendritic cells and primary fibroblasts. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C117268 |
SnomedCT | 385580005, 385581009 |
English | PIMECROLIMUS @ @ UNIDENTIFIED, PIMECROLIMUS UNIDENTIFIED, 15,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-((1E)-2-((1R,3R,4S)-4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-,(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-, 33-epi-Chloro-33-desoxyascomycin, pimecrolimus (medication), PIMECROLIMUS, pimecrolimus [Chemical/Ingredient], Pimecrolimus, Pimecrolimus (product), Pimecrolimus (substance), 33-epi-chloro-33-desoxyascomycin, pimecrolimus |
Spanish | pimecrolimus (sustancia), pimecrolimus, pimecrolimus (producto), pimecrolimo (sustancia), pimecrolimús, pimecrolimús (sustancia), pimecrolimo, pimecrolimús (producto) |