Dermatology Book

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Tacrolimus Ointment

Aka: Tacrolimus Ointment, Protopic, Elidel, Pimecrolimus
  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 [PubMed]
    2. Hanifin (2001) J Am Acad Dermatol 44:S28 [PubMed]
    3. Kang (2001) J Am Acad Dermatol 44:S58 [PubMed]
    4. Paller (2001) J Am Acad Dermatol 44:S47 [PubMed]
    5. Ruzicka (1997) N Engl J Med 337:816 [PubMed]
    6. (2001) Med Lett Drugs Ther 43(1102):33-34 [PubMed]
Medication Costs
elidel (on 2/22/2017 at Medicaid.Gov Pharmacy Drug pricing)
ELIDEL 1% CREAM $8.28 per gram
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Protopic (C0939455)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
English Protopic, protopic
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Elidel (C0971833)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C117268
English Elidel, elidel, Novartis brand of pimecrolimus
Sources
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.
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)
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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