Clinical pharmacology of new histamine H1 receptor antagonists

Clinical Pharmacokinetics

Volumn 36, Issue 5, 1999, Pages 329-352

  Simons, F Estelle R ^a,c   Simons, Keith J ^b  

^a UNIVERSITY OF MANITOBA   (Canada)

^b UNIVERSITY OF MANITOBA   (Canada)

^c CHILDREN S HOSPITAL RESEARCH INSTITUTE OF MANITOBA   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ACRIVASTINE; ASTEMIZOLE; AZELASTINE; CETIRIZINE; EBASTINE; FEXOFENADINE; HISTAMINE H1 RECEPTOR ANTAGONIST; LEVOCABASTINE; LORATADINE; MIZOLASTINE;

ALLERGY; CLINICAL PHARMACOLOGY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG METABOLISM; DRUG STRUCTURE; HUMAN; INTRANASAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; REVIEW; RHINOCONJUNCTIVITIS; TOPICAL DRUG ADMINISTRATION; URTICARIA;

AREA UNDER CURVE; HALF-LIFE; HISTAMINE H1 ANTAGONISTS; HUMANS; INTESTINAL ABSORPTION; METABOLIC CLEARANCE RATE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032977626     PISSN: 03125963     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003088-199936050-00003     Document Type: Review

References (164)

1. 1 receptor antagonist drugs. N Engl J Med 1994; 330: 1663-70
2. 2. Simons FER. Antihistamines. In: Middleton Jr E, Reed CE, Ellis EF, et al., editors. Allergy principles and practice. St Louis: Mosby-Year Book, Inc., 1998: 612-37
3. 3. Chauhan AJ, Holgate ST. Histamine receptors and antihistamines. In: Townley RG, Agrawal DK, editors. Immunopharmacology of allergic diseases. New York: Marcel Dekker, Inc., 1996: 605-38
4. 1-receptor antagonists: comparative tolerability and safety. Drug Saf 1994; 10: 350-80
5. 5. Simons FER. The eternal triangle: benefit, risk, and cost of therapeutic agents. Ann Allergy Asthma Immunol 1996; 77: 337-40
6. 1-receptor antagonists in allergic disease. New York: Marcel Dekker Inc., 1996: 175-213
7. 1-antihistamines. Clin Pharmacokinet 1995; 28: 419-32
8. 8. Woosley RL. Cardiac actions of antihistamines. Annu Rev Pharmacol Toxicol 1996; 36: 233-52
9. 9. Woosley RL, Chen Y, Freiman JP, et al. Mechanism of the cardiotoxic actions of terfenadine. JAMA 1993; 269: 1532-6
10. 10. Brogden RN, McTavish D. Acrivastine: a review of its pharmacological properties and therapeutic efficacy in allergic rhinitis, urticaria and related disorders. Drugs 1991; 41: 927-40
11. 11. Chang SY, Nelson FR, Findlay JWA, et al. Quantitative gas chromatographic-mass spectrometric analysis of acrivastine and a metabolite in human plasma. J Chromatogr 1989; 497: 288-95
12. 12. Cohen AF, Hamilton MJ, Liao SHT, et al. Pharmacodynamics and pharmacokinetics of BW 825C: a new antihistamine. Eur J Clin Pharmacol 1985; 28: 197-204
13. 1-antagonist, following ascending doses. J Clin Pharmacol 1985; 25: 629-37
14. 14. Balasubramanian R, Klein KB, Pittman AW, et al. Pharmacokinetics of acrivastine after oral and colonic administration. J Clin Pharmacol 1989; 29: 444-7
15. 15. Liao SHT, Fleck RJ, Blum MR, et al. Clinical pharmacokinetics and safety of acrivastine with pseudoephedrine in geriatric volunteers [abstract]. J Pharm Sci 1987; 76: S113
16. 1-receptor) antagonism in skin and central actions in man. Br J Clin Pharmacol 1985; 20: 283P-4P
17. 17. Petersen LJ, Bindsley-Jensen C, Poulsen LK, et al. Time of onset of action of acrivastine in the skin of pollen-allergic subjects: a double-blind, randomized, placebo-controlled comparative study. Allergy 1994; 49: 27-30
18. 18. Lahti A, Haapaniemi T. Initiation of the effects of acrivastine and cetirizine on histamine-induced wheals and itch in human skin. Acta Derm Venereol (Stockh) 1993; 73: 350-1
19. 1-antagonism with acrivastine and terfenadine by histamine bronchial challenge in volunteers. J Int Med Res 1989; 17 Suppl. 2: 35B-9B
20. 20. Janssens MM-L. Astemizole: a nonsedating antihistamine with fast and sustained activity. Clin Rev Allergy 1993; 11: 35-63
21. 21. Al-Deeb OA, Abdel-Moety EM, Bayomi SM, et al. Spectrophotometric quantification of astemizole and its demethylated metabolite in urine after TLC separation. Eur J Drug Metab Pharmacokinet 1992; 17: 251-5
22. 22. Mangalan S, Patel RB, Gandhi TP, et al. Detection and determination of free and plasma protein-bound astemizole by thinlayer chromatography: a useful technique for bioavailability studies. J Chromatogr 1991; 567: 498-503
23. 23. Meuldermans W, Hendrickx J, Lauwers W, et al. Excretion and biotransformation of astemizole in rats, guinea-pigs, dogs and man. Drug Develop Res 1986; 8: 37-51
24. 24. 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: 71-8
25. 25. Laine K, Kivistö KT, Neuvonen PJ.The effect of activated charcoal on the absorption and elimination of astemizole. Human Exp Toxicol 1994; 13: 502-5
26. 26. Möller C, Andlin-Sobocki P, Blychert L-O. Pharmacokinetics of astemizole in children. Rhinology 1992; 13: 21-5
27. 27. Zazgornik J, Scholz N, Heykants J, et al. Plasma concentrations of astemizole in patients with terminal renal insufficiency, before, during and after hemodialysis. Int J Clin Pharmacol Ther Toxicol 1986; 24: 246-8
28. 28. Lavrijsen K, Van Houdt J, Meuldermans W, et al. The interaction of ketoconazole, itraconazole and erythromycin with the in vitro metabolism of antihistamines in human liver microsomes [abstract]. Allergy 1993; 48: 34
29. 29. Holmes GB, Adams MA, Hunt TL, et al. Eighteen-week, steady-state astemizole/pseudoephedrine bioequivalency study [abstract]. Pharmacotherapy 1991; 11: 109
30. 30. Lefebvre RA, Van Peer A, Woestenborghs R. Influence of itraconazole on the pharmacokinetics and electrocardio graphic effects of astemizole. Br J Clin Pharmacol 1997; 43: 319-22
31. 31. Gendreau-Reid L, Simons KJ, Simons FER. Comparison of the suppressive effect of astemizole, terfenadine, and hydroxyzine on histamine-induced wheals and flares in humans. J Allergy Clin Immunol 1986; 77: 335-40
32. 32. Janssens MM-L, Caers LI. Onset of action of astemizole. Int J Clin Pharm Res 1991; 11: 219-29
33. 33. Humphreys F, Hunter JAA. The effects of astemizole, cetirizine and loratadine on the time course of weal and flare reactions to histamine, codeine and antigen. Br J Dermatol 1991; 125: 364-7
34. 34. Simons FER, McMillan JL, Simons KJ. 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: 540-7
35. 35. Berkowitz RB, Dockhorn R, Lockey R, et al. Comparison of efficacy, safety, and skin test inhibition of cetirizine and astemizole. Ann Allergy Asthma Immunol 1996; 76: 363-8
36. 36. Simons FER, Watson WTA, Becker AB, et al. Histamine blockade after astemizole in children: a single-dose, placebo-controlled study. Pediatr Allergy Immunol 1994; 5: 214-7
37. 1-antagonist astemizole on the skin reactions induced by histamine, codeine and allergens. Curr Ther Res 1990; 47: 683-92
38. 38. Day JH, Briscoe MP, Clark RH, et al. Onset of action and efficacy of terfenadine, astemizole, cetirizine, and loratadine for the relief of symptoms of allergic rhinitis. Ann Allergy Asthma Immunol 1997; 79: 163-72
39. 1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine-induced skin weal responses and relationship to serum levels. Br J Clin Pharmacol 1984; 18: 1-8
40. 1-antihistamines, terfenadine and astemizole, for hay fever. Thorax 1984; 39: 668-72
41. 41. Malo J-L, Fu CL, L' Archevêque J, et al. Duration of the effect of astemizole on histamine-inhalation tests. J Allergy Clin Immunol 1990; 85: 729-36
42. 42. Benoît C, Malo J-L, Ghezzo H, et al. Single-dose effect of astemizole on bronchoconstriction induced by histamine in asthmatic subjects, chest 1992; 101: 1318-25
43. 43. McNeely W, Wiseman LR. Intranasal azelastine: a review of its efficacy in the management of allergic rhinitis. Drugs 1998; 56: 91-114
44. 44. McTavish D, Sorkin EM. Azelastine: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs 1989; 38: 778-800
45. 45. Pivonka J, Segelman FH, Hartman CA, et al. Determination of azelastine and desmethylazelastine in human plasma by high-performance liquid chromatography. J Chromatogr 1987; 420: 89-98
46. 46. Tatsumi K, Ou T, Yamada H, et al. Studies on metabolic fate of a new antiallergic agent, azelastine (4-(p-chlorobenzyl)-2-[N-methylperhydroazepinyl-(4)]-1-(2H)-phthalazinone hydrochloride). Jpn J Pharmacol 1980; 30: 37-48
47. 47. Weliky I, Howard JR, Wichmann JK. Absolute bioavailability and pharmacokinetics of azelastine [abstract]. Pharm Res 1990; 7: S247
48. 48. Ricthmüller-Winzen H, Peter G, Büker KM, et al. Tolerability, pharmacokinetics and dose linearity of azelastine hydrochloride in healthy subjects. Arzneimittel Forschung Drug Res 1994; 44: 1136-40
49. 49. Peter G, Romeis P, Borbe HO, et al. Tolerability and pharmacokinetics of single and multiple doses of azelastine hydrochloride in elderly volunteers. Arzneimittel Forschung Drug Res 1995; 45: 576-81
50. 50. Morganroth J, Lyness WH, Perbach JL, et al. Lack of effect of azelastine and ketoconazole coadministration on electrocardiographic parameters in healthy volunteers. J Clin Pharmacol 1997; 37: 1065-72
51. 51. Atkins P, Merton H, Karpink P, et al. Azelastine inhibition of skin test reactivity in humans [abstract]. J Allergy Clin Immunol 1985; 75: 167
52. 2-macroglobulin into human nasal airways. Clin Exp Allergy 1997; 27: 438-44
53. 53. McItzer EO, Storms WW, Pierson WE, et al. Efficacy of azelastine in perennial allergic rhinitis: Clinical and rhinomanometric evaluation. J Allergy Clin Immunol 1988; 82: 447-55
54. 1 histamine-receptor antagonist in human airways and skin. J Allergy Clin Immunol 1988; 82: 1113-8
55. 1-receptor antihistamines in the airways and skin of subjects with asthma. J Allergy Clin Immunol 1993; 91: 1005-14
56. 56. Albazzaz MK, Patel KR. Effect of azelastine on bronchoconstriction induced by histainine and leukotriene C4 in patients with extrinsic asthma. Thorax 1988; 43: 306-11
57. 57. Rafferly P, Ng WH, Phillips G, et al. The inhibitory actions of azelastine hydrochloride on the early and late bronchoconstrictor responses to inhaled allergen in atopic asthma, J Allergy Clin Immunol 1989; 84: 649-57
58. 58. Spencer CM, Faulds D, Peters DH. Cetirizine: a reappraisal of its pharmacological properties and therapeutic use in selected allergic disorders. Drugs 1993; 46: 1055-80
59. 59. Baltes E, Coupez R, Brouwers L, et al. Gas chromatographic method for the determination of cetirizine in plasma. J Chromatogr 1988; 430: 149-55
60. 60. Pandya KK, Bangaru RA, Gandhi TP, et al. High-performance thin-layer chromatography for the determination of cetirizine in human plasma and its use in pharmacokinelic studies. J Pharm Pharmacol 1996; 48: 510-3
61. 14 C-cetirizine in humans. Ann Allergy 1987; 59: 31-4
62. 62. Muscara MN, De Nucci G. Comparative bioavailabilily of single doses of tablet formulations of cetirizine dihydrochloride in healthy male volunteers. Int J Clin Pharmacol Ther 1995; 33: 27-31
63. 1-receptor antagonist. J Med Chem 1998; 41: 853-63
64. 64. Watson WTA, Simons KJ, Chen XY, et al. Certirizine: a pharmacokinetic and pharmacodynamic evaluation in children with seasonal allergic rhinitis. J Allergy Clin Immunol 1989; 84: 457-64
65. 1-receptor antagonist cetirizime in very young children. Clin Pharmacol Ther 1993; 53: 431-5
66. 66. Pariente-Khayat A, Rey E, Dubois MC, et al. Pharmacokinetics of cetirizine in 2-to 6-year-old children. Int J Clin Pharmacol Ther 1995; 33: 340-4
67. 67. Spicak V, Dab I, Hulhoven R, et al. Pharmacokinetics and pharmacodynamics of cetirizine in infants and toddlers. Clin Pharmacol Ther 1997; 61: 325-30
68. 68. Lefebvre RA, Rosseel MT, Bernheim J. Single dose pharmacokinetics of cetirizine in young and elderly volunteers. Int J Clin Pharm Res 1988; 8: 463-70
69. 69. Matzke GR, Yeh J, Awni WM. et al. Pharmacokineties of cetirizine in the elderly and patients with renal insufficiency. Ann Allergy 1987; 59: 25-30
70. 70. Simons FER, Watson WTA, Minuk GY, et al. Cetirizine phar macokineties and pharmacodynamics in primary biliary cirrhosis. J Clin Pharmacol 1993; 33: 949-54
71. 71. Horsmans Y, Desager JP, Hulhoven R, et al. Single-dose pharmacokinetics of cetirizine in patients with chronic liver disease. J Clin Pharmacol 1993; 33: 929-32
72. 72. Awni WM, Yen J, Halstenson CE, et al. Effect of haemodialysis on the pharmacokineties of cetirizine. Eur J Clin Pharmacol 1990; 38: 67-9
73. 1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria. J Allergy Clin Immunol 1995; 95: 685-93
74. 1-receptor antagonists in skin and scrum. J Allergy Clin Immunol 1995; 95: 759-64
75. 75. Juhlin L, de Vos C, Rihoux J-P. Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria. J Allergy Clin Immunol 1987; 80: 599-602
76. 76. Rivest J, Despontin K, Ghys L, et al. Pharmacological modulation by cetirizine and ebastine of the cutaneous reactivity to histamine. Dermatologica 1991; 183: 208-11
77. 77. Sannita WG, Critni E, Riela S, et al. Cutaneous antihistaminic action of cetirizine and dose-related EEG concomitants of sedation in man. Eur J Pharmacol 1996; 300: 33-41
78. 78. Perzanowska M, Malhotra D, Skinner SP, et al. The effect of cetirizine and loratadine on codeine-induced histamine release in human skin in vivo assessed by cutaneous microdialysis. Inflamm Res 1996; 45: 486-90
79. 79. Tasnkin DP, Brik A, Gong Jr H. Cetirizine inhibition of histamine-induced bronchospasm. Ann Allergy 1987; 59: 49-52
80. 1-antagonist, on airway dynamics and responsiveness to inhaled histamine in mild asthma. J Allergy Clin Immunol 1987; 80: 51-6
81. 81. Wiseman LR, Flauds D. Ebastine: a review of its pharmacological properties and clinical efficacy in the treatment of allergic disorders. Drugs 1996; 51: 260-77
82. 82. Martinez-Tobab A, Tarrus E, Seguru J, et al. Pharmacokinetic studies in rats, dogs and man. Drugs Today 1992; 28 Suppl. B: 57-67
83. 1-receptor antagonist cbastine and its active metabolite carebastine in healthy subjects. Arzneimittel Forschung Drug Res 1994; 44: 59-64
84. 84. Vincent J, Liminana R, Meredith PA, et al. The pharmacokinetics, antihistamine and concentration-effect relationship of ebustine in healthy subjects. Br J Clin Pharmacol 1988; 26: 497-502
85. 85. Marino EL, Jansat JM, March MA, et al. Parametrization by nonlinear regression analysis of the active acid metabolite of ebastine using different weighting methods. Int J Clin Phar macol Ther 1996; 34: 546-9
86. 86. Simons FER, Watson WTA, Simons KJ. Pharmacokinetics and pharmacodynamics of ebastine in children. J Pediatr 1993; 122: 641-6
87. 87. Huang M-Y, Argenti D, Wilson J, et al. Single dose and steady-state pharmacokinetics of carebastine following administration of 10 mg ebastine tablets once daily in healthy elderly and young adults [abstract]. Pharm Res 1993; 10: S-391
88. 88. Wilson J, Huang M-Y, Argenti D, et al. Comparative pharmacokinetics of carebastine/ebastine in moderately renally impaired and healthy volunteers following a single 10mg dose of ebastine [abstract]. Pharm Res 1993; 10: S-391
89. 89. Huang M-Y, Wilson J, Argenti D, et al. Comparative pharmacokinetics of ebastine/carebastine in liver cirrhosis and healthy volunteers following administration of a 10mg ebastine tablet [abstract]. Pharm Res 1993; 10: S-390
90. 90. Hashizume T, Mise M, Terauchi Y, et al. N-dealkylation and hydroxylation of ebastine by human liver cytochrome P450. Drug Metab Dispos 1998; 26: 566-71
91. 1-receptor antagonist ebastine to its active metabolite carebastine. Eur J Clin Pharmacol 1993; 35: 661-3
92. 92. Mattila MJ, Kuitunen T, Plétan Y. Lack of pharmacodynamic and pharmacokinetic interactions of the antihistamine ebastine with ethanol in healthy subjects. Eur J Clin Pharmacol 1992; 43: 179-84
93. 93. Nelson HS, Bucher B, Buchmeier A, et al. Suppression of the skin reaction to histamine by ebastine. Ann Allergy Asthma Immunol 1995; 74: 442-7
94. 1-histamine antagonist, ebastine, against histamine and methacholine-induced bronchoconstriction in patients with asthma. Agents Actions 1990; 30: 284-6
95. 95. Markham A, Wagstaff AJ. Fexofenadine. Drugs 1998; 55: 269-74
96. 96. Hoechst Marion Roussel. Telfast Product Monograph. Oxford: The Medicine Group (Education) Ltd., 1997
97. 97. Stoltz M, Arumugham T, Lippert C, et al. Effect of food on the bioavailability of fexofenadine hydrochloride (MDL 16455A). Biopharm Drug Dispos 1997; 18: 645-8
98. 98. Lippert C., Ling J, Brown P, et al. Mass balance and pharmacokinetics of MDL 16,455A in healthy, male volunteers [abstract]. Pharm Res 1995, 12: S-390
99. 99. Russell T, Stoltz M, Weir S. Pharmacokinetics, pharmacodynamics, and tolerance of single-and multiple-dose fexofenadme hydrochloride in healthy male volunteers. Clin Pharmacol Ther 1998; 64: 612-21
100. 100. Robbins DK, Castles MA, Pack DJ, et al. Dose proportionality and comparison of single and multiple dose pharmacokinetics of fexofenadine (MDL 16455) and its enantiomers in healthy male volunteers. Biopharm Drug Dispos 1998; 19: 455-63
101. 101. Simons FER, Bergman JN, Watson WTA, et al. The clinical pharmacology of fexofenadine in children. J Allergy Clin Immunol 1996; 98: 1062-4
102. 102. Rao N, Weilert DR, Grace MCA, et al. Pharmacokinetics of terfenadine-acid-metabolite, MDL 16,455A, in healthy geriatric subjects [abstract]. Pharma Res 1995; 12 Suppl.: S386
103. 1-blockade effect of fexofenadine. Ann Allergy Asthma Immunol 1997; 79: 530-2
104. 104. Harris Ag, Iezzoni DG, Hubbell JP, et al. Comparative pharmacokinetic and pharmacodynamic crossover study seldane tablets and allegra capsules [abstract]. J Allergy Clin Immunol 1999; 103: S253
105. 105. Day JH, Briscoe MP, Welsh A, et al. Onset of action, efficacy, and safety of a single dose of fexofenadine hydrochloride for ragweed allergy using an environmental exposure unit. Ann Allergy Asthma Immunol 1997; 79: 533-40
106. 106. Bernstein DI, Schoenwetter WE, Nathan RA, et al. Efficacy and safety of fexofenadine hydrochloride for treatment of seasonal allergic rhinitis. Ann Allergy Asthma Immunol 1997; 79: 443-8
107. 107. Paul E, Berth-Jones J, Ortonne J-P, et al. Fexofenadine hydrochloride in the treatment chronic idopathic urticaria: a placebo-controlled, parallel-group, dose-ranging study. J Dermatol Treat 1998; 9: 143-9
108. 108. Pratt CM, Mason J, Russell T, et al. Cardiovascular safety of fexofenadine HCI, Am J Cardiol 1999. In press
109. 109. Vermeeren A, O'Hanlon JF. Fexofenadine's effects, alone and with alcohol, on actual driving and psychomotor performance. J Allergy Clin Immunol 1998; 101: 306-11
110. 110. Reilly MC, Tanner A, Meltzer EO. Work, classroom and activity impairment instruments: validation studies in allergic rhinitis. Clin Drug Invest 1996; 11: 278-88
111. 111. Heykants J, Van Peer A, Van de Velde V, et al. The pharmacokinetic properties of topical levocabastine: a review. Clin Pharmacokinet 1995; 29: 221-30
112. 112. Dechant KL, Goa KL. Levocabastine: a review of its pharmacological properties and therapeutic potential as a topical antibistamine in allergic rhinitis and conjunctivitis. Drugs 1991; 41: 202-24
113. 113. Heykants J, Van Peer A, Woestenborghs R, et al. Pharmacokinetics and bioavailability of levocabastine (R 50547) in man. Arch Int Pharmacodyn Ther 1985; 274: 329-30
114. 114. Zazgornik J, Huang ML, Van Peer A, et al. Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency. J Clin Pharmacol 1993; 33: 1214-8
115. 115. Pesco-Koplowitz L, Hassall A, Lee P, et al. Lack of effect of erythromycin and ketoconazole on the pharmacokinetics and pharmacodynamics of study-state intranasal levocabastine. J Clin Pharmacol 1999; 39: 76-85
116. 116. Haria M, Fitton A, Peters DH. Loratadine: a reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs 1994; 48: 617-37
117. 117. Martens J. Determination of loratadine and pheniramine from human scrum by gas chromatography-mas spectrometry. J Chromatogr B 1995; 673: 183-8
118. 118. Johnson R, Christensen J, Lin C-C. Sensitive gas-liquid chromatographic method for the determination of loratadine and its major active metabolite, descarboethoxyloratadine, in human plasma using a nitrogen phosphorus detector. J Chromatogr B 1994; 657: 125-31
119. 14C-SCH 29851 in humans [abstrac]. Ann Allergy 1985; 55: 393
120. 120. Hilbert J, Radwanski E, Weglein R, et al. Pharmacokinetics and dose proportionality of loratadine. J Clin Pharmacol 1987; 27: 694-8
121. 121. Nomeir AA, Mojaverian P, Kosoglou T, et al. Influence of food on the oral bioavailability of loratadine and pseudoephedrine from extended-release tablets in healthy volunteers. J Clin Pharmacol 1996; 36: 923-30
122. 122. Radwanski E, Hilbert J. Symchowicz S, et al. Loratadine: multiple-dose pharmacokinetics. J Clin Pharmacol 1987; 27: 530-3
123. 123. Lin CC, Radwanski E, Affrime MB, et al. Pharmacokinetics of loratadine in pediatric subjects. Am J Ther 1995; 2: 504-8
124. 124. Hilbert J, Moritzen V, Parks A, et al. The pharmacokinetics of loratadine in normal geriatric volunteers. J Int Med Res 1988; 16: 50-60
125. 125. Matzke GR, Halstenson CE, Opsahl JA, et al. Pharmacokinetics of loratadine in patients with renal insufficiency. J Clin Pharmacol 1990; 30: 364-71
126. 126. Hilbert J, Radwanski E, Affrime MB, et al. Excretion of loratadine in human breast milk. J Clin Pharmacol 1988; 28: 234-9
127. 127. Kosoglou T, Radwanski E, Batra VK, et al. Pharmacokinetics of loratadine and pseudoephedrine following single and multiple doses of once versus twice-daily combination tablet formulations in healthy adult males. Clin Ther 1997; 19: 1002-12
128. 128. Parkinson A, Clement RP, Casciano CN, et al. Evaluation of loratadine as an inducer of liver microsomal cytochrome P450 in rats and mice. Biochem Pharmacol 1992; 43: 2169-80
129. 129. Yumihe N, Huie K, Chen K-J, et al. Identification of human liver cytochrome P450s involved in the microsomal metabolism of the antihistaminic drug loratadine. Int Arch Allergy Immumol 1995; 107: 420
130. 130. Yumihe N, Huie K, Chen K-J, et al. Identification of human liver cytochrome P450 enzymes that metabolize the non-sedating antihistamine loratadine. Formation of descarboethoxyloratadine by CYP3A4 and CYP2D6. Biochem Pharmacol 1996; 51: 165-72
131. 131. Brannan MD, Reidenberg P, Radwanski E, et al. Loratadine administered concomitantly with erythromycin: pharmacokinetic and electrocardiogiaphic evaluations. Clin Pharmacol Ther 1995; 58: 269-78
132. 132. Carr RA, Edmonds A, Shi H, et al. Steady-state pharmacokinetics and electrocardiographic pharmacodynamics of clarithromycin and loratadine after individual or concomitant administration. Antimicrob Agents Chemother 1998; 42: 1176-80
133. 133. Van Peer A, Crabbé R, Woestenborghs R, et al. Ketoconazole inhibits loratadine metabolism in man [abstract]. Allergy 1993; 48: 34
134. 134. Brannan MD, Affrime MB, Reidenberg P, et al. Evaluation of the pharmacokinetics and electrocardiographic pharmacokinetics of loratadine with concomitant administration of cimetidine [abstract]. Pharmacotherapy 1994; 14: 347
135. 135. Kassem N, Roman T, Gural R, et al. Effects of loratadine (SCH 29851) in suppression of histamine-induced skin wheals. Ann Allergy 1988; 60: 505-7
136. 136. Labrecque M, Ghezzo H, L'Archevêque J, et al. Duration of effect of loratadine and terfenadine administered once a day for one week on cutaneous and inhaled reactivity to histamine. Chest 1993; 103: 777-81
137. 1-receptor antagonists loratadine and terfenadine versus placebo in children. J Pediatr 1991; 118: 298-300
138. 138. 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: 253-6
139. 139. Kontou-Fili K, Paleologos G, Herakleous M. Suppression of histamine-induced skin reactions by loratadine and cetirizine diHCI. Eur J Clin Pharmacol 1989; 36: 617-9
140. 140. Fadel R, Herpin-Richard N, Dufresne F, et al. Pharmacological modulation by cetirizine and loratadine of antigen and histamine-induced skin weals and flares, and late accumulation of eosinophils. J Int Med Res 1990; 18: 366-71
141. 141. Town GI, Holgate ST. Comparison of the effect of loratadine on the airway and skin responses to histamine, methacholine, and allergen in subjects with asthma. J Allergy Clin Immunol 1990; 86: 886-93
142. 142. Debelic M. Protection against histamine-induced bronchocon-striction by loratadine. Allergol Immunopathol (Madr) 1992; 20: 97-100
143. 143. Bousquet J, Chanal I, Skassa-Brociek W, et al. Lack of subsensitivity to loratadine during long-term dosing during 12 weeks. J Allergy Clin Immunol 1990; 86: 248-53
144. 144. Simons FER. Mizolastine: antihistaminic activity from preclinical data to clinical evaluation. Clin Exp Allergy 1999; 29: 1-8
145. 145. Arbilla S, Besserve A, Chaufour S, et al. Mizolastine: core scientific brochure. Paris: Synthélabo Groupe, Medical and Regulatory Affairs Direction, 1998
146. 146. Ascalone V, Guinebault P, Rouchouse A. Determination of mizolastine, a new antihistaminic drug, in human plasma by liquid-liquid extraction, solid-phase extraction, and column-switching techniques in combination with high-performance liquid chromatography. J Chromatogr 1993; 619: 275-84
147. 147. Rosenzweig P, Thebault JJ, Caplain H, et al. Pharmacodynamics and pharmacokinetics of mizolastine (SL 85.0324), a new nonsedative H1 antihistamine. Ann Allergy 1992; 69: 135-9
148. 148. Mesnil F, Dubruc C, Mentre F, et al. Pharmacokinetic analysis of mizolastine in healthy young volunteers after single oral and intravenous doses: noncompartmental approach and compartmental modeling. J Pharmacokinet Biopharm 1997; 25: 125-47
149. 149. Patat A, Gram LF, Dubruc C, et al. Effects of mizolastine, a new antihistamine, on psychomotor performance and memory in elderly subjects. Int Clin Psychopharmacol 1994; 9: 101-8
150. 1-antihistamine, and erythromycin [abstract]. Clin Pharmacol Ther 1998; 63: 214
151. 151. Chaufour S, Le Coz F, Denolle T, et al. Lack of effect of mizolastine on the safety and pharmacokinetics of digoxin administered orally in repeated doses to healthy volunteers. Int J Clin Pharmacol Ther 1998; 36: 286-91
152. 152. Mesnil F, Mentre F, Dubruc C, et al. Population pharmacokinetic analysis of mizolastine and validation from sparse data on patients using the nonparametric maximum likelihood method. J Pharmacokinet Biopharm 1998; 26: 133-61
153. 153. Chosidow O, Dubruc C, Danjou P, et al. Plasma and skin suction-blister-fluid pharmacokinetics and time course of the effects of oral mizolastine. Eur J Clin Pharmacol 1996; 50: 327-33
154. 154. Pinquier J-L, Caplain H, Cabanis M - J, et al. Inhibition of histamine-induced skin wheal and flare after 5 days of mizolastine. J Clin Pharmacol 1996; 36: 72-8
155. 155. Rosenzweig P, Caplain H, Chaufour S, et al. Comparative wheal and flare study of mizolastine vs terfenadine, cetirizine, loratadine and placebo in healthy volunteers. Br J Clin Pharmacol 1995; 40: 459-65
156. 156. Prakash A, Lamb HM. Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. Biodrugs 1998; 10: 41-63
157. 157. Bousquet J, Chanal I, Murrieta M, et al. Lack of subsensitivity to mizolastine over 8-week treatment. Allergy 1996; 51: 251-6
158. 158. Zhang M-Q, Walczynski K, Ter Laak AM, et al. Optically active analogues of ebastine: synthesis and effect of chirality on their antihistaminic and antimuscarinic activity. Chirality 1994; 6: 631-41
159. 159. Qucralt M, Merlos M, Giral M, et al. Dual effect of a new compound, rupatadine, on edema induced by platelet-activating factor and histamine in dogs: comparison with antihistamines and PAF antagonists. Drug Dev Res 1996; 39: 12-8
160. 2-reccptor antagonists containing diphenhydramine and cyproheptadine derivatives. Arch Pharm Pharm Med Chem 1996; 329: 87-94
161. 1-antihistamines: an in vitro study. Inflamm Res 1997; 46: S93-4
162. 162. Tohda Y, Nakajima S, Shizawa T, et al. The inhibitory effect of TMK688, a novel anti-allergic drug having both 5-lipoxygenase inhibitory activity and anti-histamine activity, against bronchoconstriction, leukotriene production and inflammatory cell infiltration in sensitized guinea pigs. Clin Exp Allergy 1997; 27: 110-8
163. 1-receptor antagonists in allergic disease. New York: Marcel Dekker, Inc., 1996: 1-32
164. 1-receptor gene [abstract]. Am J Respir Crit Care Med 1998; 157: A773