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.
- 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.
- 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.
Effects of overdosage
- Nephrotoxocity can occur with overdosage.
- In experimental treatment, pancreatitis, gastrointestinal, hepatic and renal disease and death can occur.
Other reported reactions
- With systemic administration:
- Musculoskeletal problems.
- For dermal application:
- Mild pruritus.
- Burning sensation that resolves >15 mins, occurs occasionally.
- Hemolytic anemia.
- Topical application well tolerated and pruritus is an uncommon adverse effect.