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Doxepin, a tricyclic antidepressant, is a potent histamine H1 antagonist [1]. The histamine receptors belong to a family of G protein–coupled receptors activated by their primary endogenous ligand histamine. The H1 receptor has been expressed in smooth muscles, vascular endothelial cells, heart, and the central nervous system [2].

In vitro: Doxepin was a moderately potent competitive inhibitor of serotonin uptake in human blood platelets in vitro, with an inhibitory constant Ki of ～0.2 μM. Doxepin (100 μM) rapidly increased the efflux of serotonin from platelets [1].

In vivo: In rats and dog, oral administration of doxepin was well absorbed and quickly appeared in the blood. Numerous metabolites of doxepin were observed in liver and in urine, only doxepin and demethyl doxepin were found in the rat brain[3]..

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