Last update 01 Nov 2024

Doxepin intranasal(Winston Pharmaceuticals)

Last update 01 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Dolorac

Target

H1 receptor x SERT

Mechanism

H1 receptor agonists(Histamine H1 receptor agonists), Serotonin reuptake inhibitors

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Headache

Originator Organization

Winston Pharmaceuticals, Inc.

Active Organization-

Inactive Organization

Winston Pharmaceuticals, Inc.

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

100 Clinical Results associated with Doxepin intranasal(Winston Pharmaceuticals)

100 Translational Medicine associated with Doxepin intranasal(Winston Pharmaceuticals)

100 Patents (Medical) associated with Doxepin intranasal(Winston Pharmaceuticals)

Literatures (Medical) associated with Doxepin intranasal(Winston Pharmaceuticals)

01 Aug 2007·European Journal of AnaesthesiologyQ2 · MEDICINE

Differential neurotoxicity of tricyclic antidepressants and novel derivatives in vitro in a dorsal root ganglion cell culture model*

Q2 · MEDICINE

Article

Author: P. Gerner ; G. K. Wang ; L. Klimaschewski ; I. Haller ; P. Lirk ; C. Keller

BACKGROUND AND OBJECTIVETricyclic antidepressants are commonly employed orally to treat major depressive disorders and have been shown to be of substantial benefit in various chronic pain conditions. Among other properties they are potent Na+ channel blockers in vitro and show local anaesthetic properties in vivo. The present study aimed to determine their differential neurotoxicity, and that of novel derivatives as prerequisite for their potential use in regional anaesthesia.METHODSTo directly test neurotoxicity in adult peripheral neurons, the culture model of dissociated adult rat primary sensory neurons was employed. Neurons were incubated for 24 h with amitriptyline, N-methyl-amitriptyline, doxepin, N-methyl-doxepin, N-propyl-doxepin, desipramine, imipramine and trimipramine at 100 mumol, and at concentrations correlating to their respective potency in blocking sodium channels.RESULTSAll investigated substances showed considerable neurotoxic potency as represented in significantly decreased neuron numbers in cultures as compared to controls. Specifically, doxepin was more neurotoxic than amitriptyline, and both imipramine and trimipramine were more toxic than desipramine or amitriptyline. Novel derivatives of tricyclic antidepressants were, in general, more toxic than the parent compound.CONCLUSIONSTricyclic antidepressants and novel derivatives thereof show differential neurotoxic potential in vitro. The rank order of toxicity relative to sodium channel blocking potency was desipramine < amitriptyline < N-methyl amitriptyline < doxepin < trimipramine < imipramine < N-methyl doxepin < N-propyl doxepin.

01 Jul 2005·Regional Anesthesia and Pain Medicine

Differential Block of -Propyl Derivatives of Amitriptyline and Doxepin for Sciatic Nerve Block in Rats

Article

Author: Zhi-Ye Zhuang ; Anthony M. Zizza ; Ging Kuo Wang ; Robert R. Myers ; Shi Hua Luo ; Peter Gerner ; Alimorad G. Djalali

BACKGROUND AND OBJECTIVESThe propyl group of ropivacaine ( N -propyl-2',6'-pipecoloxylidide hydrochloride) could be responsible for conferring some sensory selectivity to this drug. Thus, adding a propyl group to experimental local anesthetics (LAs) (e.g., the tricyclic antidepressants amitriptyline and doxepin) to increase sensory selectivity may be useful. We, therefore, synthesized N -propyl amitriptyline and N -propyl doxepin and investigated a potential predominance of sensory/nociceptive block over motor block (differential block) in a rat sciatic nerve block model. In addition, tetrodotoxin (TTX), a naturally occuring Na + channel blocker, was coinjected to investigate whether it increased block duration.METHODSA 0.2-mL test dose of N -propyl amitriptyline and N -propyl doxepin, at a concentration of 1, 2.5, 5, and 10 mM, (alone or in combination with TTX at a concentration of 20 microM) was injected by the subfascial sciatic nerve approach. Motor function and sensory function (nociception) were evaluated by the force a rat's hind limb produced when pushing against a balance and the reaction to pinch, respectively.RESULTSN -propyl amitriptyline and N -propyl doxepin demonstrated prolonged block duration, with N -propyl amitriptyline displaying significant differential block at higher concentrations (5 and 10 mM). The combination of either of these drugs with TTX increased the potency as well as the efficacy. Neurotoxicity commenced at concentrations of 5 to 10 mM.CONCLUSIONSDetailed histopathologic nerve toxicity evaluations are justified to determine whether N -propyl amitriptyline has potential as a more sensory-selective local anesthetic at lower concentrations or as a predominantly sensory-selective neurolytic agent at higher concentrations.

01 Jan 1977·PsychopharmacologyQ3 · MEDICINE

Sedative properties of doxepin in comparison with diazepam

Q3 · MEDICINE

Article

Author: R Grundström ; H Ledermann ; G Holmberg ; B Livstedt

Doxepin (Quitaxon) at doses of 25, 50, and 75 mg was compared with diazepam 7.5, 15, and 22.5 mg, using as variables the percentage lowering of Critical Flicker Fusion (CFF) and the self-estimated degree of drowsiness. Single doses were given, and repeated effect determinations were made over 6 h. Clear dose-effect relations could be demonstrated. The two drugs differed in speed and duration of action and in steepness of effect increase with dose. Although there were good correlations between CFF effect and subjective drowsiness, it seemed that the two methods interrelated somewhat differently in the different types of drug. CFF was a more stable and reliable method than the subjective estimation of drowsiness. However, when comparing drugs belonging to different classes, both methods preferably should be used together.

100 Deals associated with Doxepin intranasal(Winston Pharmaceuticals)

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Headache	Phase 2	US	Winston Pharmaceuticals, Inc.	27 Mar 2009

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Doxepin intranasal(Winston Pharmaceuticals)

Overview

Basic Info

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation