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Antihistamines Comparogram
1.
1 st
Generation * Anticholinergic (non-selective) * Highly sedative Less sedating Cetirizine* Somnolence(%) Cetirizine 13.7 Placebo 6.3 *Zyrtec Prescribing Information Potentially sedative/ cardiotoxic ? Loratadine Potential blockage of K + channels 2 nd Generation Cetirizine, Loratadine,Fexofenadine Non-sedating Loratadine, Fexofenadine Fexofenadine *Non- cardiotoxic *No anticholinergic side effects *Wide therapeutic index Antihistamines 3rd Generation !! Desloratadine * *Anticholinergic side effects Levocetirizine * *Profile similar to cetirizine *Somnolence 4 times that of placebo *Xyzal Prescribing Information *Ellis et al, AAAAI 2002 H1 Antihistamines: Generation Concept
2.
3.
Shamsi Z, et
al. Hum Psychopharmacol 2000; 15 (suppl 1): S3-S30 Welch MJ, et al. H1-Antihistamines in Allergic Disease, 2nd ed, 2002;337 HD = higher than recommended dose; +/- = exhibits effects Antihistamines: Side effects & Impairment 0 0 0 Fexofenadine +/-,+(HD) 0 +/-,+(HD) Cetrizine 0,+(HD) +/- 0,+(HD) Desloratadine 0,+(HD) 0 0,+(HD) Loratadine +++ +++ +++ Clemastine ++ +++ ++ Brompheniramine ++ +++ ++ Chlorpheniramine +++ +++ +++ Diphenhydramine Impairment Anticholinergic effect Drowsiness
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