Drug intelligence / Profile preview

Lofexidine + naltrexone

Development stage
Phase 2
Lead developer
Britannia Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Lofexidine + naltrexone is a combination of two pharmaceutical agents used primarily in the management of opioid dependence and withdrawal. Lofexidine is a centrally acting alpha-2 adrenergic receptor agonist that reduces the release of norepinephrine, thereby alleviating symptoms associated with acute opioid withdrawal such as muscle spasms, stomach cramps, insomnia, and anxiety[1][5][8]. Naltrexone is an opioid receptor antagonist that blocks the effects of opioids at their receptors and is used to prevent relapse after detoxification[2][4]. In some clinical settings—particularly in the United Kingdom—lofexidine has been combined with naltrexone for rapid detoxification protocols to manage both withdrawal symptoms (via lofexidine) and block opioid effects (via naltrexone)[6]. This combination does not treat addiction itself but facilitates safe discontinuation from opioids.

02

Targets

ADRA2A (α2A)ADRA2B (α2B)ADRA2C (α2C)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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