Low-dose doxepin for the treatment of insomnia: emerging data.
BACKGROUND
Doxepin is a tricyclic compound that has been used extensively for the treatment of depressive and anxiety disorders for approximately thirty years. It was noted early to have sedative effects and assist with the improvement of disrupted sleep patterns, but in higher antidepressant doses it was also noted to have significant anticholinergic and antinoradrenergic properties. These properties led to significant dose-limiting side effects, which at times precluded its effective use. Recently, doxepin has seen renewed interest in low doses as an H1 specific antagonist in sleep disorders.


OBJECTIVE
The review seeks systematically to examine currently published data on the use of doxepin for the treatment of insomnia, and its pharmacological basis.


METHODS
Medline articles showing from a search of 'doxepin and insomnia' were included in the review.


CONCLUSIONS
Currently available data support the use of low-dose doxepin as preferential H1 antagonist for the treatment of primary insomnia. There are likely preferential effects upon sleep maintenance insomnia compared with sleep initiation given the role of histamine in the sleep-wake cycle.
Goforth
Harold W
HW
Duke University Medical Center and Durham Veterans Affairs Medical Center, Department of Psychiatry, Durham, NC 27705, USA. harold.goforth@duke.edu
D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D004316:Doxepin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D004334:Drug Administration Schedule; D006801:Humans; D006993:Hypnotics and Sedatives / Q000494:pharmacology; D017286:Polysomnography; D011569:Psychiatric Status Rating Scales; D012720:Severity of Illness Index; D012890:Sleep / Q000187:drug effects / Q000502:physiology; D007319:Sleep Initiation and Maintenance Disorders / Q000188:drug therapy* / Q000378:metabolism; D012893:Sleep Wake Disorders / Q000188:drug therapy; D016896:Treatment Outcome; D014851:Wakefulness
D000929:Antidepressive Agents, Tricyclic; D006993:Hypnotics and Sedatives; D004316:Doxepin