Efficacy and safety profile of fexofenadine HCl: A unique therapeutic option in H1-receptor antagonist treatment

• Published in: Journal of allergy and clinical immunology Vol. 112; no. 4; pp. S69 - S77
• Main Authors: MEEVES, Suzanne G, APPAJOSYULA, Sireesh
• Format: Conference Proceeding Journal Article
• Language: English
• Published: New York, NY Elsevier 01.10.2003; Elsevier Limited
• Subjects: Allergies; Anti-Allergic Agents - therapeutic use; Biological and medical sciences; Drug therapy; Heart; Heart rate; Histamine; Histamine and antagonists. Allergy; Histamine H1 Antagonists - therapeutic use; Humans; Medical sciences; Nose; Patients; Permeability; Pharmacology. Drug treatments; Quality of life; Rhinitis, Allergic, Seasonal - drug therapy; Sleep; Studies; Terfenadine - analogs & derivatives; Terfenadine - therapeutic use; Treatment Outcome; Human; Immunopathology; Allergy; Nose disease; antiallergy; Rhinitis; Indication; Treatment efficiency; Fexofenadine; H1-receptor; nasal congestion; Antihistaminic; chronic idiopathic urticaria; Chemotherapy; Treatment; Allergic rhinitis; ENT disease; Antagonist; Mechanism of action; H1 Histamine receptor; antihistamine; non-sedating
• ISSN: 0091-6749; 1097-6825
• DOI: 10.1016/S0091-6749(03)01879-7

Results of head-to-head comparative trials suggest that fexo-fenadine might offer distinct advantages compared with other antihistamines. Fexofenadine is highly selective for peripheral H(1)-receptors and does not cross the blood-brain barrier, as shown by positron emission tomography. These data support findings that fexofenadine is nonsedating and does not impair performance or driving ability, even at very high doses. In addition, fexofenadine does not interact with muscarinic receptors, which might offer a potential advantage compared with desloratadine, the recently approved active metabolite of loratadine. Fexofenadine is devoid of adverse cardiac effects, and changes in electrocardiogram parameters are not significantly different from those observed with placebo. Fexofenadine has also been shown to have a favorable effect on nasal congestion. This therapeutic advantage might be related to its significant antiallergic properties, ie, the demonstrated ability of fexofenadine to blunt the inflammatory effects of preformed and de novo synthesized mediators at clinically relevant doses in vivo and in vitro. Cumulatively, these benefits distinguish fexofenadine from other antihistamines and make it an optimum therapeutic option for treating allergy-mediated respiratory and dermatologic diseases.