Abstract
Histamine is a ubiquitous autacoid with particular importance to allergic reaction, inflammation, and gastric acid secretion, and it is also a neurotransmitter in both the peripheral and central nervous systems. Due to its extensive and varied effects throughout the body, histamine itself has little therapeutic value. However, antihistamine drugs that inhibit histamine receptors are very important in the treatment of mild allergy, nausea and vomiting, and gastric acid disorders. Antihistamines are also used frequently to treat the common cold and insomnia, but these applications are not well supported by evidence of efficacy. Similarly, antihistamines are not important for the management of asthma or shock, despite common misconceptions. Over-the-counter availability of many different antihistamine formulations contributes to their widespread use. Although four histamine receptor subtypes are known, all clinically relevant antihistamines act on either H1 or H2 receptors. This chapter mainly discusses those drugs that target H1 receptors.
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