The effect of ketotifen on inflammatory markers in allergic conjunctivitis: an open, uncontrolled study

Abstract

BackgroundThe efficacy and safety of ketotifen eye drop treatment in allergic conjunctivitis (AC) management is perfectly known by several studies, but the mechanism of action at the biochemical levels is poorly understood so we decided to perform an open, uncontrolled study in order to investigate the effect of the topical administration of ketotifen fumarate 0.05% on biochemical markers of inflammation on conjunctival cells in patients with AC.MethodsNineteen patients with symptoms and signs of AC (itching, discharge, burning, redness, increase in the watery discharge, swelling and follicles) and with a history of allergy were prescribed with two daily instillation of one drop of eyewash ketotifen fumarate 0,05% in both eyes during thirty days. They were studied by measuring clinical and immunologic parameters.ResultsKetotifen fumarate treatment significantly reduced the total symptoms and signs score for each patient as well as each symptoms and signs at all time points compared with day 0 (p < 0.0001 and p < 0.016, respectively). Although the percentage of HLA-DR+ epithelial cells diminished only in 58% of patients, the numbers of CD29+ and eotaxin+ epithelial cells dropped significantly in 68% and 73 % of them (p < 0.0062 and <0.0082, respectively) as a consequence of the treatment. In 9 out of 19 patients a simultaneous decrease in the percentage of epithelial cells positive for CD29 and eotaxin was observed.ConclusionKetotifen besides the well-known effect in reducing signs and symptoms of AC significantly diminished production of eotaxin and expression of CD29 by epithelial cells in patients with seasonal AC.

Evaluating the Anti-nociceptive and Anti-inflammatory Effects of Ketotifen and Fexofenadine in Rats

“…This finding is in conformity with a research published in 2003 suggesting some novel mechanisms such as diminishing production of eotaxin and expression of CD29, in addition to the former well known mast-cell stabilizing effect of ketotifen, in management of inflammatory symptoms of allergy. 27 Besides it has been reported recently that ketotifen is able to decrease pro-inflammatory mediators, including nitric oxide, interleukin-1beta, and interleukin-6, production in rats with gouty inflammation. 28 The delay in responses to ketotifen might be because of its different mechanism with diclofenac in controlling the acute inflammation, but more studies needed to fulfill this claim.…”

Comparative study of topical anti-allergic eye drops on human conjunctiva-derived cells: responses to histamine and IFNγ and toxicological profiles

“…Moreover, it reduces histamine-induced production of IL-6 and IL-8 by conjunctival epithelial cells and inhibits conjunctival mast cell upregulation of ICAM-1 driven by anti-IgE on conjunctival epithelial cells in vitro [24]. Similarly, azelastine was shown to have dual properties [21][22][23] and ketotifen fumarate to antagonize histamine H 1 -receptors, stabilize mast cells, and inhibit chemotaxis and eosinophil activation [45,55]. Epinastine is a high-affinity H 1 -receptor antagonist that also shows mast cell-stabilizing activities and anti-inflammatory effects [5,46].…”

Formulation and evaluation of doxepin hydrochloride by fast dissolving buccal film

“…(vi)Improved patient compliance. (vii)Enhanced balance [8].Dissadvantages of fast dissolving film (i)Drugs whose healing dose is more than 40mg can't be included in the Strips. (ii)Challenge of keeping dose uniformity in Strips [9].…”