Topical calcineurin inhibitors

– Cat. C

  • Tacrolimus (0.1% and 0.03% ointments)
  • Pimecrolimus (1% cream)

  • Desensitize TRPV1: transient ↑ in substance P release via activation of TRPV1 🡪 burning sensation, with eventual desensitization of TRPV1
  • Block production of multiple proinflammatory cytokines (↓IL-2)

  • Atopic dermatitis

Absolute

  • Hypersensitivity to tacrolimus or ingredients

Relative

  • < 2 years of age
  • Active skin infection (at treated site)

  • Local irritation (most common & transient)
  • Transient burning (1-2 weeks)
  • Flushing after alcohol ingestion
  • Rosacea-like dermatitis
  • Acne
  • Reactivation of Herpes simplex virus
  • Eczema herpeticum
  • Possible molluscum 
  • Malignancy risk (black box warning)

  • Significant systemic absorption in patients with Netherton syndrome (Tacrolimus only)
  • Black box warning
    • Most recent literature failed to show malignancy association, so international experts recently concluded that the warning is not justified & recommended its removal