Several of the tricyclic compounds and maprotiline have clinically significant antihistaminic effects. Doxepin is the most potent Hi receptor blocker in this group. It is more potent than the commonly administered antihistamine diphenhydramine. More recently, however, it has been surpassed by mirtazapine and olanzapine, which are even more potent antihistamines. Central H1 receptor blockade can contribute to sedation and delirium and also appears to be related to the increased appetite and associated weight gain that patients may develop with chronic treatment. Because of their sedating effects, the tricyclic antidepressants, especially amitriptyline, have been used as hypnotics. Given their cardiac effects and the frequency of lethal overdose, this practice should be discouraged.
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