Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy.
Allergic rhinitis (AR) is associated with histamine-mediated physiologic events. The currently used histamine antagonists are all inverse agonists that bind and inactivate histamine H1 receptors. Second-generation antihistamines are much more H1-receptor selective with less central nervous system penetration than first-generation agents. Antihistamines typically are more effective in seasonal than perennial AR and do not demonstrate significant relief of nasal congestion. The recent availability of some second-generation antihistamines as over-the-counter products clearly places them as the preferred first-line treatment for mild to moderate AR based on safety when compared with first-generation over-the-counter antihistamines. The remaining prescription-only second-generation antihistamines, fexofenadine, desloratadine, and levocetirizine, all have unique attributes. Antihistamines in oral, intranasal, or intraocular formulations will likely remain among the mainstays of allergy therapeutics.
DuBuske
Lawrence
L
Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA. ldubuske@partners.org
Kowal
Krzysztof
K
D054314:Drug Inverse Agonism; D006632:Histamine / Q000276:immunology / Q000378:metabolism*; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000276:immunology / Q000627:therapeutic use*; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage / Q000627:therapeutic use*; D006801:Humans; D004366:Nonprescription Drugs / Q000008:administration & dosage / Q000627:therapeutic use; D055553:Prescription Drugs / Q000008:administration & dosage / Q000627:therapeutic use; D011969:Receptors, Histamine H1 / Q000187:drug effects; D012221:Rhinitis, Allergic, Perennial / Q000188:drug therapy* / Q000276:immunology; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy* / Q000276:immunology
D006634:Histamine H1 Antagonists; D039563:Histamine H1 Antagonists, Non-Sedating; D004366:Nonprescription Drugs; D055553:Prescription Drugs; D011969:Receptors, Histamine H1; D006632:Histamine