Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis

Abstract

Allergic disorders of the ocular surface are primarily characterized as IgE- and/or T-lymphocyte-mediated disorders that affect the cornea, conjunctiva, and eyelid. Approximately 40% of individuals in the developed countries have allergic conjunctivitis, and as such, it is the most common form of ocular allergy. Seasonal allergic conjunctivitis is the most prevalent type of allergic conjunctivitis that impacts the quality of life of patients. This article reviews the pharmacology, pharmacodynamics, pharmacokinetics, clinical trials, clinical efficacy, and safety of alcaftadine. Histamine and the pathological mechanism of ocular allergy will be briefly reviewed with the intent of providing a background for the detailed discussion on the clinical utility of alcaftadine in allergic conjunctivitis. The Medline PubMed, Elsevier Science Direct, and Google Scholar databases were used to search for evidence-based literature on histamine and immunopathological mechanism of allergic conjunctivitis, as well as on pharmacology, pharmacodynamics, pharmacokinetics, clinical trials, and clinical efficacy of alcaftadine. The treatment and management goals of allergic conjunctivitis are to prevent or minimize the inflammatory cascade associated with allergic response in the early stages of the pathological mechanism. It is of note that activation of histamine receptors on immune and nonimmune cells are associated with allergen-induced inflammation of the conjunctiva and its associated ocular allergic manifestations, including itching, edema, hyperemia, and tearing. Alcaftadine is an efficacious multiple action antiallergic therapeutic agent with inverse agonist activity on H1, H2, and H4 receptors, as well as anti-inflammatory and mast cell stabilizing effects that could provide therapeutic benefits to patients with allergic conjunctivitis.

Enigmatic Histamine Receptor H4 for Potential Treatment of Multiple Inflammatory, Autoimmune, and Related Diseases

“…Antagonists of H 4 R (JNJ7777120, JNJ39758979, INCB38579, and others) reduced pruritus in a number of animal studies [59] as well as itching sensation in different conditions in human patients. Alcaftadine, a topical ophthalmic drug indicated for the prevention of itching associated with allergic conjunctivitis, is a potent H 1 R and H 2 R antagonist (in fact, inverse agonist) with weak inverse agonistic activity also towards H 4 R [60]. Administration of H 1 R/H 4 R antagonists or co-administration of H 1 R and H 4 R antagonists will probably be effective also in humans.…”

Allergic contact dermatitis of both eyes caused by alcaftadine 0.25%: a case report

“…Currently, alcaftadine 0.25% is one of the most prescribed antihistamine agents for allergic conjunctivitis, and is used worldwide [10, 11, 16, 17]. Alcaftadine 0.25% is an H 1 - and H 2 -receptor antagonist [11].…”

“…Alcaftadine 0.25% is an H 1 - and H 2 -receptor antagonist [11]. There are some reports of side effects related to alcaftadine 0.25% usage [10, 11, 17], and previous studies reported fewer than 4% of subjects had side effects [12, 13]. Its side effects are usually related to ocular problems such as ocular itching, conjunctival redness, chemosis, lid swelling, and tearing [10, 11, 17].…”

“…Its side effects are usually related to ocular problems such as ocular itching, conjunctival redness, chemosis, lid swelling, and tearing [10, 11, 17]. An atypical symptom of bronchitis was also reported [17]. However, there have been no reports to date that alcaftadine 0.25% induces ACD.…”

Therapeutic effects of Houttuynia eye drops combined with olopatadine hydrochloride eye drops on vernal keratoconjunctivitis

“…The reason for this is that binding of VK to the IgE receptor on surface of the cell conjunctiva can cause the release of the original cytochemical mediator (histamine) and the newly formed mediators (leukotrienes and prostaglandins), and intracellular H1 and H2 in this case bind to each other, resulting in increased permeability of the conjunctival blood vessels in order to trigger an inflammatory response, eventually leading to VK conjunctival vascular congestion, expansion, eye itching and eye tingling and other symptoms (17,18). Olopatadine hydrochloride has a strong inhibitory effect on selective H1 receptor, which can prevent the release of edematous medium from mast cells in blood vessels to directly prevent H1 receptor-induced inflammation phenomenon from inside the cell (19). Houttuynia yellow oil has a very strong bactericidal ability.…”