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Review Article
Drug Therapy
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Volume 330:1663-1670 June 9, 1994 Number 23
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The Pharmacology and Use of H1-Receptor-Antagonist Drugs
F. Estelle R. Simons, and Keith J. Simons

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The H1-receptor antagonists are among the most widely used medications in the world. We review here the molecular basis of their action and their clinical pharmacology, efficacy in allergic disorders, and adverse effects. Although we will discuss the first-generation, relatively sedating H1-receptor antagonists briefly, we will emphasize the role of the second-generation, relatively nonsedating H1 antagonists (Figure 1) and will identify future directions for 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.
Extract | Full Text  
N Engl J Med 1994; 331:1019-1020, Oct 13, 1994. Correspondence

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