Felis ISSN 2398-2950

Tacrolimus

Synonym(s): FK506

Contributor(s): Elizabeth Atkins, Rosanna Marsella, Gigi Davidson

Introduction

Name

  • Tacrolimus.

Class of drug

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

Description

Molecular formula

  • C44H69NO12.H2O.

Molecular weight

  • 822 kilodaltons.

Physical properties

  • Lipid soluble.

Uses

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Indications

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:
    • Perianal fistulas.
    • Atopic dermatitis.
    • Keratoconjunctivitis sicca (KCS).
    • Discoid lupus erythematosus.
    • Vasculitis.
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. 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.

In cats

Drug not FDA-approved for use in cats.
  • FDA recommends for use in humans only when other drugs have failed; veterinary ophthalmologists observe this same caution.
  • Avoid use of topical products (Protopic®) in the eye as contains known corneal toxin, propylene carbonate.

Administration

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Pharmocokinetics

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Precautions

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Interactions

with other drugs

with diagnostic tests

  • Previous or concurrent treatment with cyclosporine A Ciclosporin and other drugs may interfere with laboratory assays to determine tacrolimus blood concentrations.
  • High tryglicerides also would interfere with ELISA tests Enzyme linked immunosorbent assay (ELISA) to measure blood levels of tacrolimus.

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Recent references from VetMed Resource and PubMed.
  • Chung T H, Ryu M H, Kim D Y, Yoon H Y & Hwang C Y (2009) Topical tacrolimus (FK506) for the treatment of feline idiopathic facial dermatitis. Aus Vet J 87 (10), 417-420 PubMed.
  • Marsella R, Nicklin C F, Saglio S & Lopez J (2004) Investigation on the efficacy and safety of 0.1% tacrolimus ointment (Protopic®) in canine atopic dermatitis: a randomized, double blinded, placebo controlled, cross over study. Vet Dermatol 15(5), 294-303 PubMed.
  • Marsella R, Nicklin C F, Saglio S & Lopez J (2004) Investigation on the effects of topical therapy with 0.1% tacrolimus ointment (Protopic®) on intradermal skin test reactivity in atopic dogs. Vet Dermatol 15(4), 218-224 PubMed.
  • Griffies J D, Mendelsohn C L, Rosenkrantz W S, Muse R, Boord M J & Griffin C E (2004) Topical 0.1% tacrolimus for the treatment of discoid lupus erythematosus and pemphigus erythematosus in dogs. J Am Anim Hosp Assoc 40(1), 29-241PubMed.
  • Marsella R & Nicklin C F (2002) Investigation on the use of 0.3% tacrolimus lotion for canine atopic dermatitis: a pilot study. Vet Dermatol 13(4), 203-210 PubMed.
  • Marsella, R & Olivry T (2001) The ACVD task force on canine atopic dermatitis (XXII): nonsteroidal anti-inflammatory pharmacotherapy. Vet Immunol Immunopathol 81, 331-345. Review PubMed.
  • Paller A et al(2001) A 12-week study of tacrolimus ointment for the treatment of atopic dermatitis in pediatric patients. J Am Acad Dermatol 44, S47-57.
  • Misseghers B S, Binnington A G & Mathews K A (2000) Clinical observations of the treatment of canine perianal fistulas with topical tacrolimus in 10 dogs. Can Vet J 41, 623-627.PubMed
  • Plosker G L & Foster G H (2000) Tacrolimus, a further update of its pharmacology and therapeutic use in the management of organ transplantation. Drugs 59,323-389 PubMed.
  • Vaden S L (1997) Cyclosporine and tacrolimus. Semin Vet Med & Surg (Small Anim) 12(3), 161-166 Review PubMed.
  • Kelly P A, Burckart G J & Venkataramanan R (1995) Tacrolimus: a new immunosuppressive agent. Am J Health-Syst Pharm 52, 1521-1535 PubMed.
  • Thomson A W, Bonham C A & Zeeva A (1995) Mode of action of tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit 17,584-591 PubMed.
  • Fukuse T et al (1993) Combined therapy with FK-506 and cyclosporine for canine lung allotransplantation: immunosuppressive effects and blood trough levels. J Heart Lung Transplant 12, 941-947 PubMed.

Other sources of information

  • Hovda L & Brutlag A (2016) Blackwell's Five-Minute Veterinary Consult Clinical Companion: Small Animal Toxicology. John Wiley & Sons.
     

 


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