Long-term use of topical tacrolimus ointment: a safe and effective option for the treatment of vernal keratoconjunctivitis

Abstract

To assess the compliance, efficacy, and safety of the long-term use of topical tacrolimus for the clinical management of vernal keratoconjunctivitis. Methods: The medical records of patients with vernal keratoconjunctivitis undergoing long-term treatment with 0.03% topical tacrolimus were retrospectively reviewed. The duration of tacrolimus use and the causes for drug discontinuation were used to assess treatment compliance. To assess drug efficacy, the need for and the number of times that topical corticosteroids were used to control symptoms were registered. Side effects related to tacrolimus use were monitored to determine drug safety. Results: The study cohort consisted of 21 patients who met the eligibility criteria. The mean duration of tacrolimus use was 41.3 ± 18.5 months. Fourteen patients (66.7%) continuously used tacrolimus, and three (14.3%) discontinued treatment following complete remission. Four patients (19%) did not use tacrolimus as prescribed or interrupted tacrolimus use on their own: two (9.5%) because of discomfort upon application and two (9.5%) because of the lack of improvement. Ten patients (47.6%) maintained disease control without the use of corticosteroids, whereas 11 (52.4%) required an average of 2.70 ± 1.35 corticosteroid cycles to control symptoms. The only reported side effect was discomfort upon application. Conclusions: Despite the small sample size and study design limitations, these results support the long-term use of topical tacrolimus as an effective and safe option for the treatment of vernal keratoconjunctivitis, with good compliance of patients to the treatment.

Efficacy of 0.03% Dermatological Tacrolimus Ointment for Refractory Vernal Keratoconjunctivitis.

“…6 Two being cyclosporine and tacrolimus, of which tacrolimus is strong, nonsteroidal, macrolide immunomodulator isolated from Streptomyces tsukubaensis that has 100 times more potency than cyclosporine 7 . Though uncertainty exists about its mechanism of action but it is known to interact with 12-kDa FK506-binding protein in T-cells and thus inhibits calcineurin activity that ultimately leads to reduced de-phosphorylation of the nuclear factor of activated T-cells and hence TH1 (IL-2, interferon-γ), as well as TH2 cytokines (IL-4, IL-5) production is reduced 8 . Tacrolimus is also known to inhibit histamine release from mast cells thus alleviating the symptom of itching 9 .…”

Therapeutic efficacy of tacrolimus in vernal keratoconjunctivitis: a meta-analysis of randomised controlled trials

“…Beyond a mild burning sensation, no other adverse reactions were observed. A study by Müller et al, 7 with continuously applied 0.03% TAC over a period of 41 months, showed no serious side effects in the treatment of VKC, highlighting the safety of long-term application. In brief, the data and results of these studies indicated that TAC was a safe and effective treatment for allergic conjunctivitis and an efficacious replacement for steroid therapy designed to control disease activity.…”

“…In addition, TAC also acts as a membrane stabiliser for mast cells by inhibiting histamine release and prostaglandin production. 7 Studies have shown that TAC has a superior immunosuppressive effect to cyclosporine. Moreover, because TAC ointment has a higher efficacy and fewer side effects in comparison with corticosteroid ointment, it can also be used as a replacement therapy for corticosteroids.…”

“…Its mechanism of action is similar to that of cyclosporine, targeting mainly CD4+ T lymphocytes, where it inhibits calcineurin, thereby suppressing interleukin 2 (IL-2) production and preventing the ensuing inflammatory cascade and eosinophil recruitment. In addition, TAC also acts as a membrane stabiliser for mast cells by inhibiting histamine release and prostaglandin production 7. Studies have shown that TAC has a superior immunosuppressive effect to cyclosporine.…”

Diagnosis, Management, and Treatment of Vernal Keratoconjunctivitis in Asia: Recommendations From the Management of Vernal Keratoconjunctivitis in Asia Expert Working Group

“…Tacrolimus is a strong, non-steroidal immunosuppressant that binds to FK506-binding proteins in T lymphocytes and inhibits calcineurin activity ( 49 ). Tacrolimus has been investigated in a small randomized controlled trial in VKC, where it demonstrated improvements in symptoms of itching, foreign-body sensation, and photophobia, as well as in signs of limbal inflammatory activity and keratitis, with maintenance of disease control ( 50 , 51 ). Tacrolimus may be administered as eye drops or an ointment; however, the eye drop formulation is not approved for use in many countries in Asia.…”