Abstract
Azatadine (6–11-dihydro-11-[1-methyl-4-piperclylidene]-5H{5,6}cyclohepta{1,2-b}pyridine maleate {1∶2}), a nitrogen analog of cyproheptadine has been studied for its antiallergy properties. It was compared in vivo and in vitro to cyproheptadine and seven (7) standard antihistamines: chlorpheniramine, promethazine, diphenhydramine, phenindamine, chloropyriline, tripelennamine and chlorcylizine; an antiserotonin, methysergide; and an anticholinergic, atropine.
Azatadine possesses potent antihistaminic, anticholinergic, antiserotinin and antianaphylactic properties. In vitro, azatadine's antihistamine potency is equal to chlorpheniramine, cyproheptadine, phenindamine, chloropyrilene and greater than the rest of the antihistamines studied. Its anticholinergic potency is 1/3 that of atropine, equal to promethazine and cyproheptadine and greater than the rest of the antihistamines studied. Its antiserotonin potency is 1/4 that of methysergide, equal to promethazine and greater than the rest of antihistamines studied.
In vivo, azatadine's ability to protect guinea-pigs from histamine lethality (i.v.) and histamine-induced dyspnea is greater than all of the antihistamines studied. Its ability to protect guinea-pigs from acetylcholine-induced dyspnea is equal to atropine and greater than all of the antihistamines studied. Its ability to protect guinea-pigs from serotonin-induced dyspnea is 1/6 that of cyproheptadine, 1/8 that of methysergide and greater than all of the antihistamines studied.
Azatadine is a more potent antianaphylactic agent and has greater therapeutic indices than cyproheptadine in both mice and guinea-pigs.
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Tozzi, S., Roth, F.E. & Tabachnick, I.I.A. The pharmacology of azatadine, a potential antiallergy drug. Agents and Actions 4, 264–270 (1974). https://doi.org/10.1007/BF01965229
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DOI: https://doi.org/10.1007/BF01965229