II. Indications

  1. Severe refractory Atopic Dermatitis

III. Pharmacokinetics

  1. Normal topical use causes <5 ng/ml serum concentration
    1. Greater absorption in severely damaged skin
  2. Factors increasing serum concentrations
    1. Higher doses or greater surface area of application
    2. Inflamed skin

IV. Mechanism

  1. Macrolide with similar activity to Cyclosporine
  2. Specifically binds T Cell receptors
    1. Inhibits cytokine production
    2. Inhibits IgE sensitivity

V. Precautions

  1. Increased risk of skin malignancy and Lymphoma
    1. FDA black box warning has been added
  2. Do not use for extended periods of time
  3. Use only in refractory Eczema

VI. Preparations

  1. Pimecrolimus (Elidel)
  2. Tacrolimus (Protopic)

VII. Dosing: Tracolimus

  1. Children over age 2 years: Apply 0.03% ointment bid
  2. Adults: Apply 0.03% or 0.1% ointment bid

VIII. Adverse Effects

  1. Local irritation (transient <1 week)
    1. Burning
    2. Erythema
    3. Pruritus
  2. Less common adverse effects
    1. Skin Tingling
    2. Acne
    3. Hyperesthesia
    4. Alcohol intolerance
  3. Immunosuppression related adverse effects
    1. Varicella zoster increased Incidence
    2. Eczema herpeticum
  4. Increased malignancy risk in mice (see precautions)
    1. Skin cancer
    2. Lymphoma

IX. Precautions

  1. Protect treated areas from direct sunlight
  2. Systemic Tacrolimus associated with skin cancer
    1. Non-Melanoma skin cancer

X. Advantages

  1. Very effective in refractory atopic cases
  2. Unlike Corticosteroids, does not cause skin atrophy
    1. May be useful on face and neck

XI. Disadvantages

  1. Expensive (costs per Red Book)
    1. Tacrolimus Ointment (0.03 or 0.1%): $60 per 30 grams
  2. Risk of malignancy (see prcautions)
    1. Skin cancer
    2. Lymphoma

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Cost: Medications

elidel (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ELIDEL 1% CREAM $8.28 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)