Drug intelligence / Profile preview

lofexidine

Development stage
Approved
Lead developer
US WorldMeds
Modality
Small Molecules
Administration
Oral
01

Overview

Lofexidine is a centrally acting alpha2-adrenergic receptor agonist used primarily for the symptomatic treatment of acute opioid withdrawal syndrome in adults. It works by stimulating alpha-2 adrenergic receptors in the brain, which reduces the release of norepinephrine and attenuates the sympathetic stress response associated with opioid withdrawal. This action helps to alleviate symptoms such as stomach cramps, muscle spasms or twitching, yawning, runny eyes, trouble sleeping, and pounding heart that occur when opioids are discontinued abruptly. Lofexidine is a non-opioid medication and does not treat opioid addiction itself but can be used as part of a comprehensive program for opioid use disorder[1][2][3][4][5]. It was originally developed as an antihypertensive agent but was repurposed due to its efficacy in managing withdrawal symptoms with fewer side effects than clonidine[4]. The drug is available by prescription only and is typically administered orally for up to 14 days during detoxification[1][7].

Brand names
Lucemyra
Other names
lofexidinelofexidine hydrochloride
02

Targets

ADRA1A (α1A)HTR7 (5-hydroxytryptamine receptor 7)HTR1D (5-hydroxytryptamine receptor 1D)ADRA2A (α2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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