Tacrolimus (Protopic)

Tacrolimus ointment (Protopic)

• a topical immunomodulators licensed to treat moderate-to-severe atopic eczema in adults and children who are not adequately responsive to or are intolerant of conventional therapies (1,2,3,4)
  • is a very potent anti-T-lymphocyte, macrolide, and immunosuppressant medicine produced from the fungus Streptomyces tsukubaensis; it was discovered in 1984 (5)
• however it has been stated that topical tacrolimus can be used as first-line therapy when there is extensive facial or periocular involvement or pigmented skin (1)
  
  
• tacrolimus ointment may be initiated by GPs if they have experience in managing patients on topical immunomodulatory therapy, such as topical corticosteroids (1)
  
  
• a review (1) concluded that tacrolimus ointement would appear to be a useful second-line agent for the treatment of atopic eczema
  
  • the selective mode of action of tacrolimus ointment results in effective treatment for moderate-to-severe atopic eczema with a good safety profile
    
    
• a Drug and Therapeutics review (2) states that tacrolimus ointment is as effective as topical steroids in the treatment of moderate-to-severe atopic dermatitis
  
  • concludes that short-term studies have established the efficacy of tacrolimus ointment in children and adults with atopic dermatitis
  • also concluded that it is an effective topical treatment, appropriate for use under the guidance of a specialist
  • tacrolimus can be used on areas of thin skin, such as the face and flexures, where avoidance of potent topical steroids is desirable
  • the 0.03 per cent formulation is licensed for use in children and is more effective than less potent steroids, such as 1 per cent hydrocortisone acetate
  • the 0.1 per cent formulation is licensed for use in the over-16s and is as effective as potent steroids, such as 0.1 per cent hydrocortisone butyrate
    
    
• a commentary by Dr Berth-Jones, Consultant Dermatologist in the UK, compared tacrolimus and pimecrolimus (3)
  • "tacrolimus is more potent than pimecrolimus"
  • .."while tacrolimus seems likely to be used mainly in the treatment of moderate and severe atopic eczema, pimecrolimus is likely to prove most useful in mild disease and when used to suppress further flares of eczema once the condition has been brought under control with topical steroids"
  • "both compounds are initially applied twice daily, but with tacrolimus it is often possible to reduce the frequency of application after a week or two"
  • "tacrolimus is available in two concentrations: 0.03 per cent for children and 0.1 per cent for adults"
  • "..like corticosteroids, application of the new immunomodulators is generally best avoided on infected skin, including areas affected by warts or molluscum"
    
    
• SIGN have stated (4):
  • topical tacrolimus should be considered, in patients aged two years and older, for short term, intermittent treatment of moderate to severe atopic eczema that has not been controlled by topical corticosteroids or where there is a serious risk of important adverse effects from further topical corticosteroid use, particularly skin atrophy
  • as a precaution against the possibility that the normal immunological response to infection may be suppressed, topical calcineurin inhibitors should not be applied to skin which appears actively infected
    
    
• topical tacrolimus is an effective and safe non-corticosteroid substitute treatment for atopic dermatitis (5)
  • adverse effect profiles of both long-term and short-term corticosteroids are more serious than tacrolimus
  • most frequent adverse effect of topical tacrolimus includes a burning sensation on the skin or irritation
    • burning skin-related adverse effects most frequently appear in the early part of the pharmacological intervention and usually exist for short periods
    • reported that skin irritation stops within the first few days of therapy
  • topical tacrolimus does not cause skin atrophy, which occurs during the treatment with topical corticosteroids

Reference:

1. Prescriber (2003): 14 (9): 53-58.
2. Drug and Therapeutics Bulletin (2002); 40:73-5.
3. Prescriber (2004); 15 (10): 57-61.
4. SIGN (March 2011). Management of atopic eczema in primary care.
5. Umar BU, Rahman S, Dutta S, Islam T, Nusrat N, Chowdhury K, Binti Wan Ahmad Fakuradzi WFS, Haque M. Management of Atopic Dermatitis: The Role of Tacrolimus. Cureus. 2022 Aug 18;14(8):e28130. doi: 10.7759/cureus.28130. PMID: 35990561; PMCID: PMC9387362