Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects

Bibliography

• Bielory L. Allergic and immunologic disorders of the eye: part II. Ocular allergy. J Allergy Clin Immunol 2000;106(6):1019-32
   PubMed Web of Science ®Google Scholar
• Bielory L, Friedlaender MH. Allergic conjunctivitis. Immunol Allergy Clin North Am 2008;28(1):43-58
   PubMed Web of Science ®Google Scholar
• Bielory L. Ocular Allergy Overview. Immunol Allergy Clin North Am 2008;29:1-23
   Web of Science ®Google Scholar
• Leonardi A, Motterle L, Bortolotti M. Allergy and the eye. Clin Exp Immunol 2008;153(Suppl 1):17-21
   PubMed Web of Science ®Google Scholar
• Bachert C. Histamine – A major role in allergy? Clin Exp Allergy 1998;28(Suppl 6):15-9
   PubMed Web of Science ®Google Scholar
• Bielory L, Ghafoor S. Histamine receptors and the conjunctiva. Curr Opin Allergy Clin Immunol 2005;5(5):437-40
   PubMed Web of Science ®Google Scholar
• Bielory L. Ocular allergy treatment. Immunol Allergy Clin North Am 2008;28(1):189-224
   PubMed Web of Science ®Google Scholar
• Meltzer EO. The prevalence and medical and economic impact of allergic rhinitis in the United States. J Allergy Clin Immunol 1997;99:S805-28
   PubMed Web of Science ®Google Scholar
• Marshall PS, Colon EA. Effects of allergy season on mood and cognitive function. Ann Allergy 1993;71:251-8
   PubMedGoogle Scholar
• Malone DC, Lawson KA, Smith DH, et al. A cost of illness study of allergic rhinitis in the United States. J Allergy Clin Immunol 1997;99:22-7
   PubMed Web of Science ®Google Scholar
• Oppenheimer JJ, Casale TB. Next generation antihistamines: therapeutic rationale, accomplishments, and advances. Expert Opin Investig Drugs 2002;11(6):807-17
   PubMed Web of Science ®Google Scholar
• Lanier BQ, Gross RD, Marks BB, et al. Olopatadine ophthalmic solution adjunctive to loratadine compared with loratadine alone in patients with active seasonal allergic conjunctivitis symptoms. Ann Allergy Asthma Immunol 2001;86(6):641-8
   PubMed Web of Science ®Google Scholar
• Friedlaender MH. Epinastine in the management of ocular allergic disease. Int Ophthalmol Clin 2006;46(4):85-6
   PubMedGoogle Scholar
• Fügner A, Bechtel WD, Kuhn FJ, Mierau J. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung 1988;38(10):1446-53
   PubMed Web of Science ®Google Scholar
• Fügner A, Meissner C. Accumulation of granulocytes in the lung and skin of guinea pigs. Inhibition by the anti-H1 antiallergic agent epinastine. Arzneimittelforschung 1994;44(12):1338-42
   PubMed Web of Science ®Google Scholar
• Inagaki N, Nagao M, Nakamura N, et al. Evaluation of anti-scratch properties of oxatomide and epinastine in mice. Eur J Pharmacol 2000;400(1):73-9
   PubMed Web of Science ®Google Scholar
• Schilling JC, Adamus WS, Kuthan H. Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers. Int J Clin Pharmacol Ther Toxicol 1990;28(12):493-7
   PubMedGoogle Scholar
• Leroy T, van Neste D. Dermal objective pharmacodynamic profile of cetirizine and epinastine: two controlled, randomised, double-blind, crossover studies. Int J Clin Pract 2002;56(8):568-73
   PubMed Web of Science ®Google Scholar
• Grant JA, Danielson L, Rihoux JP, DeVos C. A double-blind, single-dose, crossover comparison of cetirizine, ebastine, epinastine, fexofenadine, terfenadine, and loratadine versus placebo: suppression of histamine-induced wheal and flare response for 24 h in healthy male subjects. Allergy 1999;54(7):700-7
   PubMed Web of Science ®Google Scholar
• Mita H, Shida T. Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes. Arzneimittelforschung 1995;45(1):36-40
   PubMed Web of Science ®Google Scholar
• Amon U, Gibbs BF, Buss G, Nitschke M. In vitro investigations with the histamine H1 receptor antagonist, epinastine (WAL 801 CL), on isolated human allergic effector cells. Inflamm Res 2000;49(3):112-6
   PubMed Web of Science ®Google Scholar
• Hanashiro K, Sunagawa M, Tokeshi Y, et al. Antiallergic drugs, azelastine hydrochloride and epinastine hydrochloride, inhibit ongoing IgE secretion of rat IgE-producing hybridoma FE-3 cells. Eur J Pharmacol 2006;547(1-3):174-83
   PubMed Web of Science ®Google Scholar
• Kamei C, Akagi M, Mio M, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol 1991;14(1-2):191-205
   Web of Science ®Google Scholar
• Misawa M, Kanai Y. Effect of the new antiallergic drug epinastine on chemical mediator induced bronchoconstrictions in guinea pigs. Arzneimittelforschung 1991;41(11):1145-9
   PubMed Web of Science ®Google Scholar
• Kamei C, Mio M, Kitazumi K, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (II). Antagonistic effect of epinastine on chemical mediators, mainly antihistaminic and anti-PAF effects. Immunopharmacol Immunotoxicol 1992;14(1-2):207-18
   PubMed Web of Science ®Google Scholar
• Kohyama T, Takizawa H, Akiyama N, et al. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun 1997;230(1):125-8
   PubMed Web of Science ®Google Scholar
• Matsukura M, Yajima A, Yamazaki F, et al. Epinastine inhibits eosinophil chemotaxis and adhesion molecules in atopic dermatitis. Skin Pharmacol Appl Skin Physiol 2003;16(6):405-10
   PubMedGoogle Scholar
• Kanai K, Asano K, Hisamitsu T, Suzaki H. Suppressive activity of epinastine hydrochloride on TARC production from human peripheral blood CD4+ T cells in-vitro. J Pharm Pharmacol 2005;57(8):1027-36
   PubMed Web of Science ®Google Scholar
• Kanai K, Asano K, Watanabe S, et al. Epinastine hydrochloride antagonism against interleukin-4-mediated T cell cytokine imbalance in vitro. Int Arch Allergy Immunol 2006;140(1):43-52
   PubMed Web of Science ®Google Scholar
• Galatowicz G, Ajayi Y, Stern ME, Calder VL. Ocular anti-allergic compounds selectively inhibit human mast cell cytokines in vitro and conjunctival cell infiltration in vivo. Clin Exp Allergy 2007;37(11):1648-56
   PubMed Web of Science ®Google Scholar
• Ohtani H, Kotaki H, Sawada Y, Iga T. A comparative pharmacokinetic-pharmacodynamic study of the electrocardiographic effects of epinastine and terfenadine in rats. J Pharm Pharmacol 1997;49(4):458-62
   PubMed Web of Science ®Google Scholar
• Kishimoto W, Hiroi T, Sakai K, et al. Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol 1997;98(3):273-92
   PubMed Web of Science ®Google Scholar
• Yanai K, Ryu JH, Watanabe T, et al. Positron emission tomographic study of central histamine H1-receptor occupancy in human subjects treated with epinastine, a second-generation antihistamine. Methods Find Exp Clin Pharmacol 1995;17(Suppl C):64-9
   PubMed Web of Science ®Google Scholar
• Sarashina A, Tatami S, Yamamura N, et al. Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol 2005;59(1):43-53
   PubMed Web of Science ®Google Scholar
• Toyoda M, Nakamura M, Nakagawa H. Distribution to the skin of epinastine hydrochloride in atopic dermatitis patients. Eur J Dermatol 2007;17(1):33-6
   PubMed Web of Science ®Google Scholar
• Ogiso T, Kasutani M, Tanaka H, et al. Pharmacokinetics of epinastine and a possible mechanism for double peaks in oral plasma concentration profiles. Biol Pharm Bull 2001;24(7):790-4
   PubMed Web of Science ®Google Scholar
• Whitcup SM, Bradford R, Lue J, et al. Efficacy and tolerability of ophthalmic epinastine: a randomized, double-masked, parallel-group, active- and vehicle-controlled environmental trial in patients with seasonal allergic conjunctivitis. Clin Ther 2004;26(1):29-34
   PubMed Web of Science ®Google Scholar
• Abelson MB, Gomes P, Crampton HJ, et al. Efficacy and tolerability of ophthalmic epinastine assessed using the conjunctival antigen challenge model in patients with a history of allergic conjunctivitis. Clin Ther 2004;26(1):35-47
   PubMed Web of Science ®Google Scholar
• Monson BK, Rothman JS, Raizman MB. Efficacy of epinastine ophthalmic solution for post-exposure treatment of signs and symptoms of allergic conjunctivitis in cat-sensitive subjects. Presented at Annual Meeting of the American College of Allergy, Asthma, and Immunology, November 12–17, 2004, Boston, MA
   Google Scholar
• Lanier BQ, Finegold I, D'Arienzo P, et al. Clinical efficacy of olopatadine vs epinastine ophthalmic solution in the conjunctival allergen challenge model. Curr Med Res Opin 2004;20(8):1227-33
   PubMed Web of Science ®Google Scholar
• Finegold I, Granet DB, D'Arienzo PA, Epstein AB. Efficacy and response with olopatadine versus epinastine in ocular allergic symptoms: a post hoc analysis of data from a conjunctival allergen challenge study. Clin Ther 2006;28(10):1630-8
   PubMed Web of Science ®Google Scholar
• Mah FS, Rosenwasser LJ, Townsend WD, et al. Efficacy and comfort of olopatadine 0.2% versus epinastine 0.05% ophthalmic solution for treating itching and redness induced by conjunctival allergen challenge. Curr Med Res Opin 2007;23(6):1445-52
   PubMed Web of Science ®Google Scholar
• Chachin M, Katayama Y, Yamada M, et al. Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel. Eur J Pharmacol 1999;374(3):457-60
   PubMed Web of Science ®Google Scholar
• Tasaka K, Kamei C, Nakamura S. Inhibitory effect of epinastine on bronchoconstriction induced by histamine, platelet activating factor and serotonin in guinea pigs and rats. Arzneimittelforschung 1994;44(3):327-9
   PubMed Web of Science ®Google Scholar
• Trattler WB, Luchs J, Majmudar P. Elestat (epinastine HCl ophthalmic solution 0.05%) as a therapeutic for allergic conjunctivitis. Int Ophthalmol Clin 2006;46(4):87-99
   PubMedGoogle Scholar
• Ousler GW 3rd, Workman DA, Torkildsen GL. An open-label, investigator-masked, crossover study of the ocular drying effects of two antihistamines, topical epinastine and systemic loratadine, in adult volunteers with seasonal allergic conjunctivitis. Clin Ther 2007;29(4):611-6
   PubMed Web of Science ®Google Scholar
• Torkildsen GL, Ousler GW, Gomes P. Ocular comfort and drying effects of three topical antihistamine/mast cell stabilizers in adults with allergic conjunctivitis: a randomized, double-masked crossover study. Clin Ther 2008;30(7):1264-71
   PubMed Web of Science ®Google Scholar
• Villareal AL, Farley W, Pflugfelder SC. Effect of topical ophthalmic epinastine and olopatadine on tear volume in mice. Eye & Contact Lens. Sci Clin Pract 2006;32(6):272-6
   Google Scholar