Pharmacokinetic evaluation of topical calcineurin inhibitors for treatment of allergic conjunctivitis

Expert Opin Drug Metab Toxicol. 2014 Apr;10(4):543-9. doi: 10.1517/17425255.2014.884070. Epub 2014 Feb 3.


Introduction: Topical calcineurin (Cn) inhibitors delivered via ophthalmic drop is emerging as a potential treatment for severe, immune-mediated forms of allergic conjunctivitis, such as vernal keratoconjunctivitis, atopic keratoconjunctivitis and giant papillary conjunctivitis.

Areas covered: This article is based on a comprehensive literature search, with information taken from meta-analyses, systematic reviews, treatment guidelines and clinical studies in children and adults. The articles that have been selected evaluate the use of topical Cn inhibitors and their role in the treatment of allergic conjunctivitis.

Expert opinion: Ophthalmic topical Cn inhibitors have been shown to be safe for short-term use, with minimal systemic absorption and toxicity. For patients with severe, refractory forms of allergic conjunctivitis, topical Cn inhibitors offer a promising treatment option and an alternative to steroidal therapies. The safety profile and efficacy data for topical cyclosporine are more robust compared to that of tacrolimus and pimecrolimus, although larger trials will be needed for all three agents. With more randomized controlled trials involving larger sample sizes and long-term follow-up to establish both efficacy and safety, ophthalmic Cn inhibitors offer exciting treatment possibilities for the prevention of morbidity associated with refractory allergic conjunctivitis.

Publication types

  • Review

MeSH terms

  • Administration, Ophthalmic
  • Calcineurin Inhibitors*
  • Conjunctivitis, Allergic / drug therapy*
  • Cyclosporine / pharmacokinetics*
  • Cyclosporine / therapeutic use
  • Humans
  • Immunosuppressive Agents / pharmacokinetics*
  • Immunosuppressive Agents / therapeutic use
  • Tacrolimus / analogs & derivatives*
  • Tacrolimus / pharmacokinetics*
  • Tacrolimus / therapeutic use
  • Treatment Outcome


  • Calcineurin Inhibitors
  • Immunosuppressive Agents
  • pimecrolimus
  • Cyclosporine
  • Tacrolimus