J Korean Med Assoc.  2013 Mar;56(3):231-239. 10.5124/jkma.2013.56.3.231.

An overview and considerations in prescribing H1-antihistamine

• Choi YS
• Park YM
• Rha YH
• Choi SH

• KMID: 2064828
• DOI: http://doi.org/10.5124/jkma.2013.56.3.231

Abstract

H1-antihistamines have been prescribed widely for the treatment of allergic diseases, such as rhinitis, atopic dermatitis, and urticaria besides common colds since the 1940s. H1-antihistamines are classified by chemical structures (akylamine, piperazine, piperidine, ethanolamine, ethylendiamine, and phenothiazine) or functionally by permeability through blood brain barrier (first or second generation). The first generation antihistamines have been prescribed up to now with several adverse effects such as central nervous system dysfunction, anticholinergic and antiserotonic action and cardiotoxicity with overdose. Hence second generation antihistamines are recommended for the treatment of allergic rhinitis and urticaria. Physicians should consider concomitant diseases or medications when prescribing first generation antihistamines.

Keyword

Antihistamine; First generatione; Second generation; Adverse effects

MeSH Terms

Blood-Brain Barrier
Central Nervous System
Common Cold
Dermatitis, Atopic
Ethanolamine
Histamine Antagonists
Histamine H1 Antagonists, Non-Sedating
Permeability
Piperazines
Piperidines
Rhinitis
Rhinitis, Allergic, Perennial
Urticaria
Ethanolamine
Histamine Antagonists
Histamine H1 Antagonists, Non-Sedating
Piperazines
Piperidines

Figure

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  Figure 1 Anti-inflammatory effect of H1-antihistamine. H1-antihistamines directly inhibit the action of histamine through H1-receptors on neuron and small vessels. Furthermore, they show anti-inflammatory effects through NF-κB and calcuim ion channels (From Simons FE, et al. J Allergy Clin Immunol 2011;128:1139.e4-1150.e4, with permission from Elsevier) [1]. DAG, 1,2-diacylglycerol; ER, endoplasmic reticulum; GDP, guanosine diphosphate; DTP, guamosine triphosphate; IP3, inositol 1,4,5-triphosphate; PIP2, phosphatidylinositol 4,5-bisphosphate; PKC beta, protein kinase C beta; PLC beta, phospholipate C beta.

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