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INTRODUCTION

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This chapter will be most useful after having a basic understanding of the material in Chapter 32, Histamine, Bradykinin, and Their Antagonists in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here, the 12th Edition contains:

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  • Table 32-1 Characteristics of Histamine Receptors, which shows the biochemical properties, tissue distribution, and representative agonists and antagonists of the 4 histamine receptors (H1, H2, H3, and H4)

  • Table 32-2 Preparations and Dosage of Representative H1-Receptor Antagonists

  • The molecular structures of histamine and drugs that are agonists and antagonists of the various histamine receptors

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LEARNING OBJECTIVES

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  • Understand the role of histamine and bradykinin in different physiological and pathophysiological processes.

  • Understand the mechanisms of action of drugs that act as antagonists of the H1 receptor.

  • Know the therapeutic utility of H1-receptor antagonists, alone and in combination with other agents.

  • Know the important adverse effects of H1-receptor antagonists, and the difference between first- and second-generation H1 antihistamines with regard to adverse effects.

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DRUGS INCLUDED IN THIS CHAPTER

  • Acrivastine (SEMPREX-D*)

  • Aprotinin (TRAYSYLOL)

  • Azelastine (ASTELIN)

  • Brompheniramine maleate (BROMPHEN, others)

  • Carbinoxamine (RONDEC*, others)

  • Cetirizine (ZYRTEC)

  • Chlorpheniramine (CHLOR-TRIMETON, others)

  • Clemastine fumarate (TAVIST, others)

  • Cyclizine (MAREZINE)

  • Cyproheptadine (PERIACTIN)

  • Desloratadine (CLARINEX, AERIUS)

  • Dimenhydrinate (combination of diphenhydramine and 8-chlorotheophylline; DRAMAMINE, others)

  • Diphenhydramine (BENADRYL, others)

  • Doxepin (SINEQUAN)

  • Ebastine (EBASTEL)

  • Fexofenadine (ALLEGRA, TELFAST)

  • Hydroxyzine (ATARAX, others)

  • Hydroxyzine (VISTARIL)

  • Icatibant (FIRAZYR)

  • Ketotifen fumarate (ZADITOR)

  • Levocabastine (LIVOSTIN)

  • Levocetirizine (XYZAL)

  • Loratadine (CLARITIN)

  • Meclizine (ANTIVERT, others)

  • Mizolastine (MIZOLLEN)

  • Olopatadine (PATANOL, PATANASE, others)

  • Phenindamine (NOLAHIST)

  • Promethazine (PHENERGAN, others)

  • Pyrilamine (POLY–HISTINE-D*)

  • Tripelennamine (PBZ)

* Trade-name drug that contains other medications.

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Table Graphic Jump Location
MECHANISMS OF ACTION OF HISTAMINE RECEPTOR AND BRADYKININ ANTAGONISTS

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