Drug intelligence / Profile preview

naltrexone + clonidine

Development stage
Phase 2
Lead developer
Allodynic Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Naltrexone + clonidine is a combination therapy used primarily for the management of opioid withdrawal. Naltrexone is a pure opioid antagonist that blocks the effects of opioids at mu, kappa, and delta receptors in the central nervous system, with highest affinity for the mu receptor. It prevents opioid-induced euphoria and can precipitate withdrawal symptoms in dependent individuals[8]. Clonidine is an alpha-2 adrenergic receptor agonist that reduces sympathetic outflow from the central nervous system, thereby attenuating symptoms such as anxiety, restlessness, sweating, lacrimation, rhinorrhea, and craving during withdrawal[6][1]. The combination has been shown to be safe and effective in reducing both subjective and objective signs of opioid withdrawal compared to either agent alone or placebo. Very low-dose naltrexone (VLNTX) combined with low-dose clonidine may further improve safety by allowing lower doses of each drug while maintaining efficacy[1][4][5]. This approach leverages functional interactions between opioid and adrenergic pathways to provide more comprehensive symptom control during detoxification.

Other names
Naltrexone and Clonidine Combination
02

Targets

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

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