H1-receptor antagonists: safety issues.

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Estelle F, Simons R

H1-receptor antagonists: safety issues.

Ann Allergy Asthma Immunol. 1999 Nov;83(5):481-8.

PubMed ID

10582735 [ View in PubMed

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Abstract

Histamine is an important neurotransmitter. Old (first-generation) H1-receptor antagonists such as chlorpheniramine, diphenhydramine, or triprolidine produce histamine blockade at H1-receptors in the central nervous system (CNS) and frequently cause somnolence or other CNS adverse effects. New (second generation) H1-antagonists such as cetirizine, fexofenadine, and loratadine represent an advance in therapeutics; in manufacturers' recommended doses, they enter the CNS in smaller amounts, produce relatively little somnolence or other CNS adverse effects, and do not exacerbate the adverse CNS effects of alcohol or other CNS-active chemicals. Two H1-antagonists, astemizole and terfenadine, have been found to prolong the QTc interval and, rarely, to cause cardiac dysrhythmias after overdose or under other specific conditions. This has led to withdrawal of regulatory approval for them. An H1-antagonist absolutely free from adverse effects under all circumstances is not yet available for use.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Triprolidine	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details