The H1-receptor antagonists are among the most widely used medicationsin the world. We review here the molecular basis of their actionand their clinical pharmacology, efficacy in allergic disorders,and adverse effects. Although we will discuss the first-generation,relatively sedating H1-receptor antagonists briefly, we willemphasize the role of the second-generation, relatively nonsedatingH1 antagonists (Figure 1) and will identify future directionsfor research of these agents.
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Figure 1. Chemical Structure of Histamine and Representative H1-Receptor-Antagonist Drugs.
For practical purposes, H1 antagonists are now often divided into first-generation, relatively sedating medications and second-generation, relatively nonsedating medications. . . . [Full Text of this Article]
Molecular Basis of Action
Mechanisms of Action
H1-Receptor Blockade
Antiallergic Effects of H1 Antagonists
Absorption, Distribution, Metabolism, and Excretion
Pharmacodynamic Activity
Efficacy in Allergic Disorders
Allergic Rhinoconjunctivitis and Other Upper Respiratory Tract Disorders
Asthma
Chronic Urticaria
Anaphylaxis
Atopic Dermatitis
Adverse Effects
First-Generation H1-Antagonist Drugs
Second-Generation H1 Antagonists
Use of H1-Antagonist Drugs during Pregnancy
Summary
Source Information
From the Faculty of Medicine (F.E.R.S.) and the Faculties of Pharmacy, Medicine, and Science (K.J.S.), University of Manitoba, Winnipeg.
Address reprint requests to Dr. F.E.R. Simons at Rm. AE101, Children's Hospital of Winnipeg, 840 Sherbrook St., Winnipeg, MB R3A 1S1, Canada.
References
Related Letters:
Histamine H1 Antagonists
Fleischer A. B., Weintraub M., Walls R. M., Barr D. A., Simons F. E. R., Simons K. J.
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Full Text
N Engl J Med 1994;
331:1019-1020, Oct 13, 1994.
Correspondence
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