Novel therapeutic usage of low-dose doxepin hydrochloride

  title={Novel therapeutic usage of low-dose doxepin hydrochloride},
  author={Haramandeep Singh and Philip M. Becker},
  journal={Expert Opinion on Investigational Drugs},
  pages={1295 - 1305}
  • H. Singh, P. Becker
  • Published 1 August 2007
  • Medicine, Psychology
  • Expert Opinion on Investigational Drugs
Low-dose doxepin hydrochloride (1, 3 and 6 mg) is a tricyclic antidepressant currently being investigated for the treatment of primary insomnia in adult and geriatric patients. Although it has been used at much higher doses to treat depression effectively for a number of decades, it offers a unique potency and selectivity for antagonizing the H1 (histamine) receptor at low doses. This mechanism of action may prove to be advantageous compared with other medications currently approved for the… 

Low-dose doxepin for the treatment of insomnia: emerging data

  • H. Goforth
  • Medicine, Psychology
    Expert opinion on pharmacotherapy
  • 2009
Current available data support the use of low-dose doxepin as preferential H1 antagonist for the treatment of primary insomnia and there are likely preferential effects upon sleep maintenance insomnia compared with sleep initiation given the role of histamine in the sleep–wake cycle.

Low-Dose Doxepin

In three large, well designed, phase III trials in adult or elderly patients with chronic primary insomnia, oral, low-dose doxepin 3 or 6 mg once daily improved wake time after sleep onset, total sleep time and sleep efficiency to a significantly greater extent than placebo.

Low-dosedoxepinforthe treatmentofinsomnia: emergingdata

Current available data support the use of low-dose doxepin as preferen- tial H1 antagonist for the treatment of primary insomnia and there are likely preferential effects upon sleep maintenance insomnia compared with sleep initiation given the role of histamine in the sleep-wake cycle.

Evaluation of central and peripheral effects of doxepin on acetic acid-induced colitis in rat and the involved mechanisms

Doxepin as an ancient antidepressive drug has anti-colitis and anti-inflammatory properties which are mainly exerted peripherally so it could be introduced as a good candidate for depressed people who suffered from IBD disorders.

The expanding role of H1 antihistamines: a patent survey of selective and dual activity compounds 2005 – 2010

The development of multiple activity H1 antihistamines in allergy has met with limited success due in part to a competitive commercial environment and new sedative hypnotics may show potential but will need to demonstrate significant benefits in an increasingly competitive landscape.

Evaluation of the central and peripheral effects of doxepin on carrageenan-induced inflammatory paw edema in rat

Although the exact mechanism of the anti-inflammatory effect of doxepin is not clear, it seems that reduced leukocyte migration and pro-inflammatory cytokines play important role in its anti- inflammation effect.

Can we use psychoactive drugs to treat pruritus?

The role of H1‐antihistamines, antidepressants, antipsychotics and antiepileptics in managing pruritus is summarized.

Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake time

Current understanding of how hypnotic drugs act is reviewed, and how new, more effective drugs and treatment strategies for insomnia might be achieved by taking into consideration the daytime consequences of disrupted sleep is discussed.

Role of serendipity in the discovery of classical antidepressant drugs: Applying operational criteria and patterns of discovery

The role played by serendipity in the origin of modern psychopharmacology has proven to be controversial in scientific literature. In its original meaning (Walpole), serendipity refers to discoveries



Long-term treatment of chronic depression: 15-year experience with doxepin HCl.

  • F. Ayd
  • Medicine, Psychology
    The Journal of clinical psychiatry
  • 1984
Advantages of doxepin therapy include its lack of adverse interactions with prescription and non-prescription drugs taken by these patients and the high degree of safety seen in patients with concomitant cardiovascular and other physical disorders.

Double-blind comparison of amoxapine and imipramine in the treatment of depressed patients.

A 5-week double-blind study compared amoxapine to imipramine (2:1 dosage ratio) in the treatment of depressed outpatients. The two agents were similar in anti-depressant efficacy and rapidity of

Pharmacokinetic factors affecting antidepressant drug clearance and clinical effect: evaluation of doxepin and imipramine--new data and review.

At doses approaching the upper range recommended for the treatment of depression, Cpss appear to approach, in at least a few individuals, the maximum metabolic capacity of the patient, leading to greater-than-expected increases in concentrations for a given dosage increment.

Antidepressants in the treatment of migraine headache

In patients who are depressed with severe migraine, a tricyclic antidepressant may treat both conditions; however, the addition of a newer atypical antidepressant may be needed.

Effective Low Dose Tricyclic Antidepressant Treatment for Depressed Geriatric Rehabilitation Patients: A Double‐Blind Study

The patients treated with doxepin had a significantly greater reduction in depressive symptoms than did those who received a placebo and no side effects were found.

Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study.

The results support the effectiveness of low doses of doxepin to improve sleep and working ability in chronic primary insomniacs, although subjective effects were light to moderate, and in some patients, rebound insomnia and specific side effects have to be considered.

Efficacy and safety of doxepin 1 mg, 3 mg, and 6 mg in elderly patients with primary insomnia: a randomized, double-blind, placebo-controlled crossover study.

In this 2-night study of elderly adults with primary insomnia, doxepin doses of 1 mg, 3 mg, and 6 mg were well tolerated and produced significant improvement in objective and subjective sleep maintenance and duration endpoints that persisted into the final hour of the night.

Pharmacokinetics of doxepin and desmethyldoxepin: an evaluation with the population approach

The analysis indicates that the factors age and, to some extent, body weight may be a guidance for individual doxepine dose regimens, which however needs confirmation in prospective clinical trials linking pharmacokinetics and therapeutic effect.

The effects of doxepin HCl on sleep and depression.

Doxepin in doses of 75 and 150 mg/day significantly improved sleep efficiency, as evidenced by decreased sleep latency and increased total sleep time and after 2 weeks of treatment, REM latency and percent REM time were dramatically changed.