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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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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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