Chapter References

1. Windaus A, Vogt W. Syntheses des imidazolylathylamines. Ber Dtsch Chem Ges 1907;3:3691.

2. Fried JP, ed. Dorland's illustrated medical dictionary. Philadelphia: WB Saunders, 1974.

3. Simons FE. Antihistamines. In: Middleton E, Reed CE, Ellis EF, et al, eds. Allergy principles and practice. St. Louis: CV Mosby, 1998.

4. Dale HH, Laidlaw PP. The physiological action of a-imidazolylethylamine. J Physiol 1953;120:528.

5. Pearce FL. Biological effects of histamine: an overview. Agents Actions 1991;33:4-7.

6. Ishizaka T. Analysis of triggering events in mast cells for immunoglobulin E-mediated histamine release. J Allergy Clin Immunol 1981;67:90.

7. Ash ASF, Schild HO. Receptors mediating some actions of histamine. Br J Pharmacol Chemother 1966;27:427.

8. Black JW, Duncan WAM, Durant CJ, et al. Definition and antagonism of histamine H 2 receptors. Nature 1977;236:385.

9. Arrang JM, Garbarg M, Lancelot JC, et al. Highly potent and selective ligands for histamine H 3 receptors. Nature 1987;327:117.

10. Simons FER. H1 receptor antagonists: clinical pharmacology and therapeutics. J Allergy Clin Immunol 1989;84:845.

11. Kozlowski T, Raymond RM, Korthuis RJ, et al. Microvascular protein efflux: interaction of histamine and H 1 receptors. Proc Soc Exp Biol Med 1981;166:263.

12. Dobbins DE, Swindall BT, Haddy FJ, et al. Blockade of histamine-mediated increased in microvascular permeability by H 1- and H2-receptor antagonists. Microvasc Res 1981;21:343.

13. Duncan WAM, Parsons ME. Reminiscences of the development of cimetidine. Gastroenterology 1980;78:620.

14. Ganellin CR. Medicinal chemistry and dynamic structure-activity analysis in the discovery of drugs acting as histamine H 2-receptors. J Med Chem 1981;24:913.

15. Lipsy RJ, Fennerty B, Fagan TC. Clinical review of histmanine 2 receptor antagonists. Arch Intern Med 1990;150:745.

16. Simons FER, Simons KJ. H1 receptor antagonists: clinical pharmacology and use in allergic disease. Pediatr Clin North Am 1983;30:899.

17. Simons FER, Simons KJ. The pharmacology and use of H ^receptor-antagonist drugs. N Engl J Med 1994;330:1663.

18. Simons FER, Luciuk GH, Simons KJ. The pharmacokinetics and antihistaminic effects of brompheniraine. J Allergy Clin Immunol 1982;70:458.

19. Simons FER, Frith EM, Simons KJ. The pharmacokinetics and antihistaminic effects of brompheniramine. J Allergy Clin Immunol 1982;70:458.

20. Simons KJ, Singh M, Gillespie CA, et al. An investigation of the H 1-receptor antagonist triprolidine. Pharmacokinetics and antihistaminic effects. J Allergy Clin Immunol 1986;77:326.

21. Simons FER, Simons KJ, Frith EM. The pharmacokinetics and antihistaminic of the H 1 receptor antagonist hydroxyzine. J Allergy Clin Immunol 1984;73:69.

22. Simons FER, Simons KJ. H1 receptor antagonist treatment of chronic rhinitis. J Allergy Clin Immunol 1988;81:975.

23. Church MK, Gradidge CG. Inhibition of histamine release from human lung in vitro by antihistamines and related drugs. Br J Pharmacol 1980;69:663.

24. Physicians' desk reference. 49th ed. Montvale, NJ: Oradell Medical Economics Company Inc., 2000.

25. Fowle ASE, Hughes DTD, Knight GJ. The evaluation of histamine antagonists in man. Eur J Clin Pharmacol 1971;3:215.

26. Kotzan JA, Vallner JJ, Stewart JT, et al. Bioavailability of regular and controlled release chlorpheniramine products. J Pharm Sci 1982;71:919.

27. Yacobi A, Stoll RG, Chao GG, et al. Evaluation of sustained-action chlorpheniramine-pseudoephedrine dosage form in humans. J Pharm Sci 1980;69:1077.

28. Brandon ML, Weiner M. Clinical investigation of terfenadine, a non-sedating antihistamine. Ann Allergy 1980;44:71.

29. Laduron PM, Janssen PFM, Gommeren W, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol 1982;21:294.

30. Simons FER, Simons KJ. New H1 receptor antagonists: a review. Am J Rhinol 1988;2:21.

31. Grant JA. Molecular pharmacology of second-generation antihistamines. Allergy Asthma Proc 2000;21:135-140.

32. Okerholm RA, Weiner DL, Hook RH, et al. Bioavailability of terfenadine in man. Biopharm Drug Dispos 1981;2:185.

33. Heykants J, Van Peer A, Woestenborghs R, et al. Dose-proportionality, bioavailability and steady-state kinetics of astemizole in man. Drug Dev Res 1986;8:71.

34. Rihoux JP, DeVos C, Baltes E, et al. Pharmacoclinical investigation of cetirizine, a new potent and well tolerated anti-H 1. Ann Allergy 1985;55:392 (abst).

35. Wood SG, John GA, Chasseaud JF, et al. The metabolism and pharmacokinetics of 14C-cetirizine in humans. Ann Allergy 1987;59:31.

36. Watson WTA, Simons KJ, Chen XY, et al. Cetirizine: a pharmacokinetic and pharmacodynamic evaluation in children with seasonal allergic rhinitis. J Allergy Clin Immunol 1989;84:457.

37. Hilbert J, Radwanski E, Weglein R, et al. Pharmacokinetics and dose proportionality of loratadine. J Clin Pharmacol 1987;27:694.

38. Rodrigues AD, Mulford DJ, Lee RD, et al. In vitro metabolism of terfenadine by a purified recombinant fusion protein containing cytochrome p4503A4 and NADPH P450 reductase: comparison to human liver microsomes and precision cut liver tissue slices. Drug Metab Dispos 1995;23:765-775.

39. Richards DM, Brogden RN, Heel RC, et al. Astemizole: a review of its pharmacodynamic properties and therapeutic efficacy. Drugs 1984;28:38.

40. Garteiz DA, Hook RH, Walker BJ, et al. Pharmacokinetics and biotransformation studies of terfenadine in man. Arzneimittelforschung 1982;32:1185.

41. Simons FER, Watson WTA, Simons KJ. The pharmacokinetics and pharmacodynamics of terfenadine in children. J Allergy Clin Immunol 1987;80:884.

42. Meltzer EO, Baraniuk, JN, Barbey J, et al. Antihistamine update: consensus conference. Hosp Pract 1995;31:s1.

43. Honig PK, Wortham DC, Lazarev A, et al. Grapefruit juice alters the systemic bioavailability and cardiac repolarization of terfenadine in poor metabolizers of terfenadine. J Clin Pharmacol 1996;36:345-351.

44. Simons FER, et al. A double-blind, single-dose, crossover comparison of cetirizine, terfenadine, loratadine, astemizole and chlorpheniramine versus placebo: suppressive effects on histamine-induced wheals and flares during 24 hours in normal subjects. J Allergy Clin Immunol 1990;86:540.

45. Roth T, Roehrs T, Koshorck G, et al. Sedative effects of antihistamines. J Allergy Clin Immunol 1987;80:94.

46. Chu TJ, Yamate M, Biedermann AA, et al. One versus twice daily dosing of terfenadine in the treatment of seasonal allergic rhinitis: US and European studies. Ann Allergy 1989;63:12.

47. Russell T, Burgess G, Donahue R, et al. A comparison of peripheral H 1 blockade between single doses of fexofenadine HCl and terfenadine. Ann Allergy Asthma Immunol 2000;84:146.

48. Fields DA, Pillar J, Diamantis W, et al. Inhibition by azelastine of nonallergic histamine release from rat peritoneal mast cells. J Allergy Clin Immunol 1984;74:400.

49. Chand N, Pillar J, Diamantis W, et al. Inhibition of IgE-mediated allergic histamine release from rat peritoneal mast cells by azelastine and selected anti-allergic drugs. Agents Actions 1985;16:318.

50. Tasaka K, Mio M, Okamoto M. Intracellular calcium release induced by histamine releasers and its inhibition by antiallergic drugs. Ann Allergy 1986;56:464.

51. Lowe DA, Richardson BP, Taylor P, et al. Increasing intracellular sodium triggers calcium release from bound pools. Nature 1976;260:337.

52. Busse W, Randlex B, Sedgwick J. The effect of azelastine on neutrophil and eosinophil generation of superoxide. J Allergy Clin Immunol 1989;83:400.

53. Phillips MJ, Meyrick-Thomas RH, Moodley I, et al. A comparison of the in vivo effects of ketotifen, clemastine, chlorpheniramine and sodium cromoglycate on histamine and allergen induced wheals in human skin. Br J Clin Pharmacol 1983;15:277.

54. Armour C, Temple DM. The modification by ketotifen of respiratory responses to histamine and antigen in guinea pigs. Agents Actions 1982;12:285.

55. Chand N, Harrison JE, Rooney SM, et al. Inhibition of passive cutaneous anaphylaxis (PCA) by azelastine: dissociation of its antiallergic activities from antihistaminic and antiserotonin properties. Int J Immunopharmacol 1985;7:833.

56. Van Nueten JM, Xhouneux R, Janssen PAJ. Preliminary data on antiserotonin effects of oxatomide, a novel antiallergic compound. Arch Int Pharmacodyn Ther 1978;232:217.

57. Bechel HJ, Broch N, Lenke D, et al. Pharmacologic and toxicological properties of azelastine, a novel antiallergic agent. Arzneimittelforschung 1981;31:1184.

58. Ney U, Bretz U, Gradwohl P, et al. Further characterization of the antianaphylactic action of ketotifen. Allergol Immunopathol (Madr) 1980;8:380.

59. Diamantis W, Chand N, Harrison JE, et al. Inhibition of release of SRS-A and its antagonism by azelastine, an H1 antagonist-antiallergic agent. Pharmacologist 1982;24:200.

60. Ohmori K, Ishii H, Kubota T, et al. Inhibitory effects of oxatomide on several activities of SRS-A and synthetic leukotrienes in guinea pigs and rats. Arch Int Pharmacodyn Ther 1985;275:139.

61. Van Ganse E, Kaufman L, Derde MP, et al. Effects of antihistamines in adult asthma: a meta-analysis of clinical trials. EurRespir J 1997;10:2216-2224.

62. Roquet A, Dahlen B, Kumlin M, et al. Combined antagonism of leukotrienes and histamine produces predominant inhibition of allergen induced early and late phase airway obstruction in asthmatics. Am J Respir Crit Care Med 1997;155:1856-1863.

63. Schwartz JC, Garbarg M, Quach TT. Histamine receptors in brain as targets for tricyclic antidepressants. TIPS 1981.

64. Goldsobel AB, Rohr AS, Siegel SC, et al. Efficacy of doxepin in the treatment of chronic idiopathic urticaria. J Allergy Clin Immunol 1986;78:867.

65. Drouin MA. H1 antihistamines: perspective of the use of the conventional and new agents. Ann Allergy 1985;55:747.

66. Connell JT, Howard JC, Dressler W, et al. Antihistamines: findings in clinical trials relevant to therapeutics. Ann J Rhin 1987;1:3.

67. Wong L, Hendeles L, Weinberger M. Pharmacologic prophylaxis of allergic rhinitis: relative efficacy of hydroxyzine and chlorpheniramine. J Allergy Clin Immunol 1981;67:223.

68. Schaaf L, Hendeles L, Weinberger M. Suppression of seasonal allergic rhinitis symptoms with daily hydroxyzine. J Allergy Clin Immunol 1979;3:129.

69. Empey DW, Bye C, Hodder M, et al. A double-blind crossover trial of pseudoephedrine and triprolidine: alone and in combination, for the treatment of allergic rhinitis. Ann Allergy 1975;34:41.

70. Diamond L, Gerson K, Cato A, et al. An evaluation of triprolidine and pseudoephedrine in the treatment of allergic rhinitis. Ann Allergy 1981;47:87.

71. Guill MF, Buckley RH, Rocha W, et al. Multicenter, double blind, placebo-controlled trial of terfenadine suspension in the treatment of fall-allergic rhinitis in children. J Allergy Clin Immunol 1986;78:4.

72. Sooknundun M, Kacker SK, Sundaran KR. Treatment of allergic rhinitis with a new long-acting H 1 receptor antagonist: astemizole. Ann Allergy 1987;58:78.

73. Kreutner W, Chapman RW, Gulbenkian A, et al. Antiallergic activity of loratadine, a nonsedating antihistamine. Allergy 1987;42:57.

74. Meltzer EO, Weiler JM, Widlitz MD. Comparative outdoor study of the efficacy, onset and duration of action and safety of cetirizine, loratadine and placebo for seasonal allergic rhinitis. J Allergy Clin Immunol 1996;97:617.

75. Juniper EF, White J, Dolovich J. Efficacy of continuous treatment with astemizole (Hismanal) and terfenadine (Seldane) in ragweed pollen-induced rhinoconjunctivitis. J Allergy Clin Immunol 1988;82:670.

76. Boland N. A double-blind study of astemizole and terfenadine in the treatment of perennial rhinitis. Ann Allergy 1988;61:18.

77. Dockhorn RJ, Bergner A, Connell JT, et al. Safety and efficacy of loratadine (Sch-29851): a new non-sedating antihistamine in seasonal allergic rhinitis. Ann Allergy 1987;58:407.

78. Bruttman G, Charpin D, Germouty J, et al. Evaluation of the efficacy and safety of loratadine in perennial allergic rhinitis. J Allergy Clin Immunol 1989;83:411.

79. Bruno G, D'Amato G, Del Giacco GS, et al. Prolonged treatment with acrivastine for seasonal allergic rhinitis. J Int Med Res 1989;17:41B.

80. Gervais P, Bruttman G, Pedrali P, et al. French multicentre double-blind study to evaluate the efficacy and safety of acrivastine as compared with terfenadine in seasonal allergic rhinitis. J Int Med Res 1989;17:47B.

81. Falliers CJ, Brandon ML, Buchman E, et al. Double blind comparisons of cetirizine and placebo in treatment of seasonal rhinitis. Ann Allergy 1991;66:257.

82. Skassa-Brociek W, Bousquet J, Montes F, et al. Double-blind placebo-controlled study of loratadine mequitazine, and placebo in the symptomatic treatment of seasonal allergic rhinitis. J Allergy Clin Immunol 1988;81:725.

83. Gutkowski A, Bedard P, Del Carpio JB, et al. Comparison of the efficacy and safety of loratadine, terfenadine and placebo in the treatment of seasonal allergic rhinitis. J Allergy Clin Immunol 1988;81:902.

84. Zuber P, Pecoud A. Effect of levocabastine, a new H1 antagonist, in a conjunctival provocation test with allergens. J Allergy Clin Immunol 1988;82:590.

85. Simons FER, Simons KJ, Becker AB, et al. Pharmacokinetics and antipruritic effects of hydroxyzine in children with atopic dermatitis. J Pediatr 1984; 104:123.

86. Wanderer AA, St. Pierre JP, Ellis EF. Primary acquired cold urticaria: double blind study of treatment with cryproheptadine, chlorpheniramine and placebo. Arch Dermatol 1977;113:1375.

87. Bernstein IL, Bernstein DI. Efficacy and safety of astemizole, a long-acting and nonsedating H1 antagonist for the treatment of chronic idiopathic urticaria. J Allergy Clin Immunol 1986;77:37.

88. Fox RW, Lockey RF, Burkantz SC, et al. The treatment of mild to severe chronic idiopathic urticaria with astemizole: double-blind and open trials. J Allergy Clin Immunol 1986;78:1159.

89. Sly MR, Kemp JP, Anderson JA, et al. Position statement: the use of antihistamines in patients with asthma. J Allergy Clin Immunol 1988;82:481.

90. Pierson WE, Virant FS. Antihistamines in asthma. Ann Allergy 1989;63:601.

91. Rafferty P. The European experience with antihistamines in asthma. Ann Allergy 1989;63:389.

92. Rafferty P, Holgate ST. Histamine and its antagonists in asthma. J Allergy Clin Immunol 1989;84:144.

93. Ollier S, Gould CAL, Davies RJ. The effect of single and multiple dose therapy with azelastine on the immediate asthmatic response to allergen provocation testing. J Allergy Clin Immunol 1986;78:358.

94. Rafferty P, Harrison J, Aurich R, et al. The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. J Allergy Clin Immunol 1988;82:1113.

95. Cantekin EL, Mandel EM, Bluestone CD, et al. Lack of efficacy of a decongestant-antihistamine combination of otitis media with effusion in children. N Engl J Med 1987;316:432.

96. Mandel EM, Rockette HE, Bluestone CD, et al. Efficacy of amoxicillin with and without decongestant antihistamine for otitis media with effusion in children. N Engl J Med 1987;316:432.

97. Gaffey MJ, Gwaltney JM, Sastre A, et al. Intranasally and orally administered antihistamine treatment of experimental rhinovirus colds. Am Rev Respir Dis 1987;136:556.

98. Dykewicz MS, Fineman S, Nicklas R, et al. Diagnosis and management of rhinitis. Parameter documents of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology 1998;81:501.

99. Schuller DE, Turkewitz D. Adverse effects of antihistamines. Postgrad Med 1986;79:75.

100. Simons FER, Watson WTA, Chen XY, et al. The pharmacokinetics and pharmacodynamics of hydroxyzine in patients with primary biliary cirrhosis. J Clin Pharmacol 1989;29:809.

101. Nicholson AN. Antihistamines and sedation. Lancet 1982;2:211.

102. Simons FER, Kesselman MS, Giddens NG, et al. Astemizole-induced torsades de pointes. Lancet 1988;2:624.

103. Burns JJ, Conney AH, Koster R. Stimulatory effect of chronic drug administration on drug and metabolizing enzymes in liver microsomes. Ann N Y Acad Sci 1963;104:881.

104. Simons KJ, Simons FER. The effect of chronic administration of hydroxyzine on hydroxyzine pharmacokinetics in dogs. J Allergy Clin Immunol 1987;79:928.

105. Kemp JB. Tolerance to antihistamines: is it a problem? Ann Allergy 1989;63:621.

106. Taylor RJ, Long WF, Nelson HS. The development of subsensitivity to chlorpheniramine. J Allergy Clin Immunol 1985;76:103.

107. Bantz EW, Dolen WK, Chadwick EW, et al. Chronic chlorpheniramine therapy: Subsensitivity, drug metabolism and compliance. Ann Allergy 1987;59:341.

108. Simons FER, Watson WTA, Simons KJ. Lack of subsensitivity to terfenadine during long-term terfenadine treatment. J Allergy Clin Immunol 1988;82:1068.

109. Roman IJ, Kassem N, Gural RP, et al. Suppression of histamine-induced wheal response by loratadine (SCH 29851) over 28 days in man. Ann Allergy 1986;57:253.

110. Hendeles L. Selecting a decongestant. Pharmacotherapy 1993;13:129S-134S.

111. Durant GJ, Parsons ME, Black JW. Potential histamine H2 receptor antagonists: 2N a-guanylhistamine. J Med Chem 1975;18:830.

112. Forest JAH, Shearman DJC, Spence R, et al. Neutropenia associated with metiamide [Letter]. Lancet 1975;1:392.

113. Holmberg K, Pipkorn U, Bake B, et al. Effects of topical treatment H 1 and H2 antagonists on clinical symptoms and nasal vascular reactions in patients with allergic rhinitis. Allergy 1989:44:281.

114. Norm S, Permin H, Skov PS. H 2 antihistamines (cimetidine) and allergic-inflammatory reactions. Allergy 1980;35:357.

115. Gonzalez H, Ahmed T. Suppression of gastric H2-receptor mediated function in patients with bronchial asthma and ragweed allergy. Chest 1986;4:491.

116. Ahmed T, King MM, Krainson JP. Modification of airway histamine-receptor function with methylprednisolone succinate. J Allergy Clin Immunol 1983;71:224.

117. Festen HPM, DePauw BE, Smeulders J, et al. Cimetidine does not influence immunological parameters in man. Clin Immunol Immunopathol 1981;21:33.

118. Thomas RHM, Browne PD, Kirby JDT. The effect of ranitidine, alone and in combination with clemastine, on allergen induced cutaneous wheal and flare reactions in human skin. J Allergy Clin Immunol 1985;76:864.

119. Nathan RA, Segall N, Schocket AL. A comparison of the actions of H 1 and H2 antihistamines on histamine-induced bronchoconstriction and cutaneous wheal response in asthmatic patients. J Allergy Clin Immunol 1981;67:171.

120. Havas TE, Cole P, Parker L, et al. The effects of combined H 1 and H2 histamine antagonists on alterations in nasal airflow resistance induced by topical histamine provocation. J Allergy Clin Immunol 1986;78:856.

121. Secher C, Kirkegaard J, Borum P, et al. Significance of H 1 and H2 receptors in the human nose: rationale for topical use if combined antihistamine preparations. J Allergy Clin Immunol 1982;70:211.

122. Harvey RP, Schocket AL. The effect of H 1 and H2 blockade on cutaneous histamine response in man. J Allergy Clin Immunol 1980;65:136.

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