Dermatology Book

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Tacrolimus OintmentAka: Protopic, Elidel, Pimecrolimus

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  1. Indications
    1. Severe refractory Atopic Dermatitis
  2. 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
  3. Mechanism
    1. Macrolide with similar activity to cyclosporine
    2. Specifically binds T Cell receptors
      1. Inhibits cytokine production
      2. Inhibits IgE sensitivity
  4. 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
  5. Preparations
    1. Pimecrolimus (Elidel)
    2. Tacrolimus (Protopic)
  6. Dosing: Tracolimus
    1. Children over age 2 years: Apply 0.03% ointment bid
    2. Adults: Apply 0.03% or 0.1% ointment bid
  7. 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
  8. Precautions
    1. Protect treated areas from direct sunlight
    2. Systemic tacrolimus associated with skin cancer
      1. Non-Melanoma skin cancer
  9. Advantages
    1. Very effective in refractory atopic cases
    2. Unlike Corticosteroids, does not cause skin atrophy
      1. May be useful on face and neck
  10. 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
  11. References
    1. Bekersky (2001) J Am Acad Dermatol 44:S17
    2. Hanifin (2001) J Am Acad Dermatol 44:S28
    3. Kang (2001) J Am Acad Dermatol 44:S58
    4. Paller (2001) J Am Acad Dermatol 44:S47
    5. Ruzicka (1997) N Engl J Med 337:816
    6. (2001) Med Lett Drugs Ther 43(1102):33

Protopic (C0939455)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishProtopic
SourcesNCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Elidel (C0971833)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC117268
EnglishElidel, Novartis brand of pimecrolimus
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


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.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC117268
English33-epi-chloro-33-desoxyascomycin, Pimecrolimus, PIMECROLIMUS @ @ UNIDENTIFIED, PIMECROLIMUS PREPARATION, PIMECROLIMUS UNIDENTIFIED
Spanishpimecrolimo, pimecrolimus
Parent ConceptsImmunosuppressive Agents (C0021081), [DE900] DERMATOLOGICALS, TOPICAL OTHER (C0993166), Unclassified Ingredients (C1372954), Dermatologic Agents (C0011625), Calcineurin inhibitor (C1562036), Macrolide immunosuppressant (C1690933), Immunomodulators (C1527392)
SourcesMSH, MTH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)



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