Disease relevance of Emadine

• CONCLUSION: The results of this study suggest that emedastine and ketotifen are not significantly different with respect to anti-itching efficacy in the CAC model of acute allergic conjunctivitis [1].
• In the between-group efficacy comparison at visit 3, the difference in itching and hyperemia scores between emedastine and loratadine was statistically significant at all time points (all, P < 0.05) [2].
• After 7 days of use, and throughout the remainder of the study, emedastine was statistically superior to levocabastine (P <.006) in preventing and alleviating the signs and symptoms (itching, redness, chemosis, and eyelid swelling) of allergic conjunctivitis [3].
• Emedastine also inhibited passive peritoneal anaphylaxis in rats and guinea pigs [4].
• Therefore, we here set out to compare the pharmacokinetics of emedastine difumarate in patients suffering from different degrees of renal failure with a control group of healthy volunteers [5].

High impact information on Emadine

• Emedastine is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis [1].
• Emedastine is registered in its country of origin (Japan) as an antihistamine for the indication of seasonal allergic rhinitis [6].
• Preincubation of the eosinophils with emedastine did not alter the expression of the CCR3 receptor, although a decrease in the concentration of intracellular calcium ions was observed after stimulation with 100 ng/ml of eotaxin [7].
• In addition, protein kinase A and protein kinase C activities in eotaxin-stimulated EoL-1 cell supernatants decreased significantly with emedastine pretreatment [7].
• These findings suggest that emedastine inhibits CC chemokine-elicited eosinophil migration by decreasing the activities of tyrosine kinase or protein kinases but does not alter CCR3 expression [7].

Chemical compound and disease context of Emadine

• METHODS: In a prospective, multicenter, randomized, double-masked, parallel group study, 222 patients with allergic conjunctivitis were randomized (221 received treatment) to either emedastine or levocabastine, instilled twice daily for 6 weeks [3].
• Prednisolone and emedastine are effective against IL-5-induced eosinophilia [8].
• Comparison of the topical ocular antiallergic efficacy of emedastine 0.05% ophthalmic solution to ketorolac 0.5% ophthalmic solution in a clinical model of allergic conjunctivitis [9].
• CONCLUSIONS: Emedastine 0.05% appeared superior to nedocromil 2% in producing immediate relief when subjects with allergic conjunctivitis were exposed to the offending allergen [10].

Biological context of Emadine

• There were no gender differences in the pharmacokinetics of emedastine [11].
• Thus emedastine appears to possess a potent and selective inhibitory effect on eosinophils chemotaxis, an action which is probably unrelated to its anti-histamine properties [12].
• The time courses of disappearance of total radioactive compound and unchanged emedastine from the liver were analyzed using a compartment model for the examination of the efflux and metabolic processes [13].
• METHODS: The effects of multiple ketoconazole administration on emedastine kinetics were evaluated by comparing values obtained for pharmacokinetic parameters at steady state, with and without ketoconazole [14].
• Estimation of in vivo percutaneous absorption of emedastine from bile excretion data using a deconvolution method [15].

Anatomical context of Emadine

• However, the effect of emedastine on the selective migration of eosinophils that have been stimulated with CC chemokines has not been examined [7].
• Tyrosine kinase activity in the cytosol supernatant of eosinophils obtained after stimulation with eotaxin significantly decreased when the eosinophils were preincubated with emedastine [7].
• Emedastine significantly reduced cytokine and ICAM-1 expression from H-stimulated fibroblasts [16].
• Adhesive explant culture of allergic nasal mucosa: effect of emedastine difumarate, an anti-allergic drug [17].
• At concentrations of 10(-8) M or higher, emedastine significantly inhibited SP-induced Ca2+ release from intracellular Ca stores and SP-induced 45Ca uptake into mast cells [4].

Associations of Emadine with other chemical compounds

• These results suggest that the inhibition by emedastine of substance P-induced itch-associated response is mediated by the blockade of leukotriene B(4) action [18].
• It has been reported that emedastine can significantly inhibit the migration of eosinophils elicited by classical chemoattractants, including LTB4 or PAF [7].
• METHODS: The clinical trial compared the efficacy and safety of emedastine 0.05% and levocabastine 0.05%, both twice daily, for 42 days, using ocular redness, itching, days without symptoms and clinical failure as outcome measures [19].
• RESULTS: Emedastine steady state pharmacokinetics were slightly altered as a result of the ketoconazole co-treatment [14].
• At pharmacokinetic steady-state levels, no significant difference could be found in the potency between cetirizine and emedastine (2 mg b.i.d.). CONCLUSION: Emedastine displays pharmacodynamic properties comparable with cetirizine and therefore qualifies as a safe and alternative compound with H1-receptor antagonist properties [20].

Gene context of Emadine

• Effect of emedastine difumarate on CC chemokine-elicited eosinophil migration [7].
• Emedastine was the most potent in ligand binding, phosphatidylinositol turnover, and IL-6 secretion, with dissociation constant and 50% inhibitory concentrations of 1-3 nmol/L [21].
• Emedastine at concentrations of 10 nM or higher strongly inhibited the eosinophil migration elicited by CC chemokines, including eotaxin, RANTES and MCP-3 [7].
• A novel controlled release system, the PVA swelling controlled release system, was evaluated in vitro and in vivo using emedastine difumarate as a model drug [22].
• Pharmacokinetics and pharmacodynamics of the novel H1-receptor antagonist emedastine in healthy volunteers [20].

Analytical, diagnostic and therapeutic context of Emadine

• Intradermal injection of substance P increased the cutaneous concentration of leukotriene B(4), which was not affected by emedastine [18].
• CONCLUSION: Through a model based on a randomised clinical trial and cost estimates of treatment failure derived from practitioner interviews, emedastine is a cost-effective treatment of AAC [19].
• Transdermal administration of emedastine [23].
• Emedastine difumarate (2 mg b.i.d.) was compared to loratadine (10 mg o.d.) in a randomized, double-blind, multicentre trial for 4 weeks in 192 patients with idiopathic chronic urticaria [24].
• METHODS: A total of 130 patients suffering from grass pollen allergic rhinitis were randomly assigned to 14 days treatment with either emedastine difumarate (2 mg b.i.d.) or terfenadine (60 mg b.i.d.) in a double-blind, randomised, crossover design [25].

References