H1-receptor antagonists. Comparative tolerability and safety.

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Simons FE

H1-receptor antagonists. Comparative tolerability and safety.

Drug Saf. 1994 May;10(5):350-80.

PubMed ID

7913608 [ View in PubMed

]

Abstract

First-generation histamine H1-receptor antagonists, such as diphenhydramine, triprolidine, hydroxyzine or chlorpheniramine (chlorphenamine), frequently cause somnolence or other CNS adverse effects. Second-generation H1-antagonists, such as terfenadine, astemizole, loratadine and cetirizine, represent a true advance in therapeutics. In manufacturers' recommended doses, they have a more favourable benefit/risk ratio than their predecessors with regard to lack of CNS effects, and do not exacerbate the adverse CNS effects of alcohol or other CNS-active chemicals. Rarely, some of the newer H1-antagonists may cause cardiac dysrhythmias after overdose or under other specific conditions. The concept of a risk-free H1-antagonist is proving to be an oversimplification. An H1-antagonist absolutely free from adverse effects under all circumstances is not yet available for use. The magnitude of the beneficial effects of each H1-antagonist should be related to the magnitude of the unwanted effects, especially in the CNS and cardiovascular system, and a benefit-risk ratio or therapeutic index should be developed for each medication in this class.

DrugBank Data that Cites this Article

Drugs

Triprolidine

Drug Targets

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