Pimecrolimus

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Contents

[edit] BRAND NAMES

[edit] MECHANISM OF ACTION

The mechanism of action of pimecrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T cells. In addition, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE.

[edit] INDICATIONS

Pimecrolimus 1% cream is indicated for patients 3 months of age and older with atopic dermatitis (eczema) for:

  • short term treatment of signs and symptoms
  • intermittent long-term treatment of emerging and resolving lesions in atopic dermatitis where the use of a topical corticosteroid is not yet warranted, no longer needed, or is inadvisable.

[edit] DOSAGE

The patient or care giver should apply a thin layer of pimecrolimus Cream 1% to the affected skin twice daily. The patient or caregiver should stop using when signs and symptoms (e.g., itch, rash and redness) resolve and should be instructed on what actions to take if symptoms recur.

  • If signs and symptoms persist and beyond 6 weeks, patients should be re-examined by their health care provider to confirm the diagnosis of atopic dermatitis.
  • Continuous long-term use of pimecrolimus Cream should be avoided, and application should be limited to areas of involvement with atopic dermatitis.

The safety of pimecrolimus Cream under occlusion, which may promote systemic exposure, has not been evaluated. Pimecrolimus Cream should not be used with occlusive dressings.

[edit] CONTRAINDICATIONS

pimecrolimus Cream 1% is contraindicated in individuals with a history of hypersensitivity to pimecrolimus or any of the components of the cream.

[edit] WARNINGS AND PRECAUTIONS

Long-term Safety of Topical Calcineurin Inhibitors Has Not Been Established

Although a causal relationship has not been established, rare cases of malignancy (e.g., skin and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including pimecrolimus Cream. Therefore:

  • Continuous long-term use of topical calcineurin inhibitors, including pimecrolimus Cream, in any age group should be avoided, and application limited to areas of involvement with atopic dermatitis.
  • pimecrolimus Cream is not indicated for use in children less than 2 years of age.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

Pregnancy Category C (US)

[edit] SIDE EFFECTS

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES