Tacrolimus ointment: a review of its use in atopic dermatitis and its clinical potential in other inflammatory skin conditions

Drugs. 2005;65(6):827-58. doi: 10.2165/00003495-200565060-00011.

Abstract

Tacrolimus ointment (Protopic) is a topically applied macrolide lactone immunomodulator effective in the treatment of atopic dermatitis. Its mechanism of action primarily involves calcineurin inhibition, which interrupts cytokine gene expression and leads to the downregulation of T-cell activity. Tacrolimus ointment (0.03% and 0.1% for adults and 0.03% for children) is an effective treatment for atopic dermatitis of the trunk and limbs, as well as sensitive skin areas such as the face. Its efficacy is similar to or greater than that of hydrocortisone acetate 1%, hydrocortisone butyrate 0.1% and betamethsone valerate 0.12% ointments and pimecrolimus 1% cream. Systemic absorption of tacrolimus from the ointment is minimal, and adverse events, which are mostly associated with the application site and include skin burning and pruritus, tend to resolve early in treatment. Unlike topical corticosteroids, tacrolimus ointment is not associated with skin atrophy, and it is a well tolerated treatment for adults or children with atopic dermatitis, particularly when long-term treatment is indicated or the face or skin-fold regions are involved.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
  • Dermatitis, Atopic / drug therapy*
  • Dermatitis, Atopic / metabolism
  • Dermatitis, Atopic / pathology*
  • Humans
  • Immunosuppressive Agents / pharmacokinetics
  • Immunosuppressive Agents / therapeutic use
  • Ointments
  • Skin Diseases / drug therapy
  • Skin Diseases / metabolism
  • Skin Diseases / pathology*
  • Tacrolimus / pharmacokinetics
  • Tacrolimus / therapeutic use*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Immunosuppressive Agents
  • Ointments
  • Tacrolimus