Drug intelligence / Profile preview

doxepin + zopiclone

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Doxepin + zopiclone is a combination of two pharmaceutical drugs, each with distinct mechanisms of action, used primarily for their sedative and hypnotic effects. Doxepin is a tricyclic antidepressant that also acts as an H1-antihistamine at low doses and is approved for the treatment of depression, anxiety disorders, and insomnia. Its mechanism involves inhibition of the reuptake of serotonin and norepinephrine as well as antagonism at histamine H1 receptors[3][7]. Zopiclone is a non-benzodiazepine hypnotic agent (a cyclopyrrolone derivative) that acts by binding to the benzodiazepine site on GABAA receptors (specifically α1, α2, α3, and α5 subunits), enhancing GABAergic inhibitory neurotransmission to produce sedative-hypnotic effects[2]. The combination may be considered in clinical scenarios where both antidepressant/anxiolytic and hypnotic actions are desired; however, co-administration increases the risk or severity of adverse central nervous system effects such as sedation, dizziness, confusion, impaired concentration or psychomotor performance[5]. This combination should only be used under close medical supervision due to additive CNS depressant risks.

02

Targets

BZD site (GABA-A receptor benzodiazepine site)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)HRH1 (Histamine H1 Receptor)

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