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  • Tacrolimus.

Class of drug

  • Macrolide lactone antibiotic with potent immunosuppressive activity.
  • Produced by Streptomyces tsukubaensis.



  • Reduces T cell proliferation.
  • Inhibits interleukin-2 gene expression in CD4+ T-helper cells by blocking phosphatase action of calcineurin and preventing nuclear translocation of nuclear factor of activated T cells.
  • Also inhibits transcription of pro-inflammatory cytokines including IL-1, TNFa, IL-3, IL-4, IL-5, IL-6, IL-8 and GM-CSF by interacting with glucocorticoid and progesterone receptors.


In humans

  • Approved for use in prevention of liver, kidney, heart, lung, pancreas, intestinal and bone marrow transplant rejection.
  • Treatment of atopic dermatitis in topical formulation.
  • Experimental uses include prevention of corneal transplant rejection and treatment of various types of uveitis.

In dogs

  • Topically, routinely used in treatment of:

  • Drug not FDA-approved for use in dogs.
  • One of main advantages of topical tacrolimus compared to topical glucocorticoids is the lack of atrophogenic properties.
  • Additionally, topical tacrolimus appears to decrease cutaneous colonization of bacteria on atopic skin therefore decreasing incidence of secondary bacterial infections.
  • Proven very effective topically for localized atopic dermatitis [Skin: atopy]. Well tolerated and improvement is usually seen within first few weeks of treatment. Dogs with generalized disease do not have the same significant clinical improvement.

Adverse reactions

Effects of overdosage

In humans

  • Nephrotoxocity can occur with overdosage.

In dogs

  • In experimental treatment, pancreatitis, gastrointestinal, hepatic and renal disease and death can occur.

Other reported reactions

In humans

  • With systemic administration:
    • Headache.
    • Tremors.
    • Insomnia.
    • Hyperesthesia.
    • Musculoskeletal problems.
  • For dermal application:
    • Mild pruritus.
    • Burning sensation that resolves >15 mins, occurs occasionally.

In humans

  • Hemolytic anemia.

In dogs

  • Topical application well tolerated and pruritus is an uncommon adverse effect.
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