The Use of Topical Tacrolimus 0.1% Skin Ointment for Anterior Segment Conditions: A Case Series

Abstract

Tacrolimus (FK 506) is a macrolactam derivative with immunomodulatory and anti-inflammatory activity. Topical tacrolimus 0.03% has been used for inflammatory conditions of the anterior segment. This article adds to the literature on the off-license application of tacrolimus ointment, by describing the safe and effective use of the higher strength of 0.1% topical tacrolimus skin ointment in four patients. To our knowledge this is the first report of topical tacrolimus 0.1% ointment applied to the conjunctival sac for the treatment of atopic keratoconjunctivitis, vernal keratoconjunctivitis and the post-operative management of trabeculectomy and graft rejection in steroid responders.

Tacrolimus for the Treatment of Subepithelial Infiltrates Resistant to Topical Steroids After Adenoviral Keratoconjunctivitis

“…A denoviral keratoconjunctivitis (AK), which is caused most commonly by adenoviral serotypes 8,19, and 37, is characterized by a large spectrum of clinical manifestations with variable durations. This conjunctival infection is considered the most common external ocular infection in the world; and as a contagious disease, it has been associated with epidemic outbreaks.…”

Effect of Topical Tacrolimus in the Treatment of Thygeson's Superficial Punctate Keratitis

“…Tacrolimus has a more potent immunosuppressant action, 15 and initial evidence indicates that it may be more effective for treating some ocular surface diseases with fewer side effects than cyclosporine A (burning sensation and pain on application). 16 Tacrolimus generally is an effective alternative for specific ocular inflammatory conditions refractory to traditional treatments such as dry eye, 17 ocular surface inflammation in patients with graft versus host disease, 18,19 allergic 10,16,[20][21][22][23][24][25][26][27][28][29] lens-induced papillary conjunctivitis, 30 corneal subepithelial infiltrates secondary to adenoviral keratoconjunctivitis, 31 superior limbic keratoconjunctivitis, 32 refractory phlyctenular keratoconjunctivitis, 33 ocular cicatricial pemphigoid, 34,35 and anterior segment inflammatory disorders. [5][6][7]9 In addition, patients who are intolerant of cyclosporine can be treated effectively with topical tacrolimus.…”

“…[5][6][7]9 In addition, patients who are intolerant of cyclosporine can be treated effectively with topical tacrolimus. 18 The commercially available tacrolimus ointment is a dermatologic formulation (Protopic, tacrolimus ointment 0.03% and 0.1%, Protopic, Astellas Pharma Tech Co., Toyama, Japan) and has been used to treat atopic eczema and ocular surface diseases without side effects or patient intolerance 9,10,19,21,23,24,26,[32][33][34] (Table 2). The Protopic ointment contains either 0.03% or 0.1% of tacrolimus in a base of mineral oil, paraffin, propylene carbonate, white petrolatum, and white wax.…”

Evaluation of the Pharmacokinetics and Ocular Tolerance of a Microemulsion Containing Tacrolimus

“…This can increase the absorption surface area, and therefore, the ocular bioavailability of the drug. 9 The microemulsion presented small droplets size probably due to the presence of the cosurfactant molecules that act by decreasing the radius of curvature of the droplets. 15 The formulation presented low viscosity, which is mainly because of the small average size of the droplets.…”

“…6,8 Topical tacrolimus ointment has been demonstrated to be effective to treat inflammatory conditions of anterior segment eye at a concentration of 0.03% as well as in cases of keratoconjunctivitis and graft rejection at concentration of 0.1%. 9 Although ointments are able to ensure adequate ocular drug bioavailability, they have been related with blurred vision, lachrymation, and reflex blinking. These undesirable effects have a negative impact on patient compliance and may limit the drug administration during nighttime or when the inflammatory site is located outside or at the edges of eyelids.…”