Canis ISSN: 2398-2942

Tacrolimus

Synonym(s): FK506

Contributor(s): Elizabeth Atkins, Rosanna Marsella

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

Drug not FDA-approved for use in dogs.
  • One of main advantages of topical tacrolimus compared to topical glucocorticoids Therapeutics: 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.

Administration

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Pharmocokinetics

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Precautions

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Interactions

with other drugs

with diagnostic tests

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Recent references from VetMed Resource and 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),29-41 PubMed.
  • 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.

     

 


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