Drug intelligence / Profile preview

scopolamine + naltrexone

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous, Oral, Transdermal, Intramuscular
01

Overview

Scopolamine + naltrexone is a combination of two FDA-approved drugs, each with distinct mechanisms of action. Scopolamine is an antimuscarinic agent that acts as a non-selective competitive antagonist at muscarinic acetylcholine receptors (M1-M5), primarily blocking the effects of acetylcholine in the central and peripheral nervous systems. It is traditionally used to prevent nausea and vomiting associated with motion sickness and surgical procedures, but has also demonstrated rapid antidepressant effects in clinical studies[2][6][8]. Naltrexone is an opioid receptor antagonist that competitively binds to μ, κ, and δ opioid receptors, blocking the effects of endogenous opioids. It is approved for treating opioid use disorder (OUD) and alcohol use disorder (AUD), reducing cravings by inhibiting euphoric and sedative effects from opioids[3][4]. The combination has been studied off-label for major depressive disorder (MDD), where pilot data suggest it may provide rapid symptom reduction in treatment-resistant depression[1]. Additionally, this combination has been explored as part of detoxification protocols for heroin addiction[5].

Other names
Scopolamine and naltrexone combinationNaltrexone/Scopolamine buccal drops
02

Targets

KOR (Kappa opioid receptor)MOR (Mu opioid receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM4 (M4)CHRM3 (M3)DOR (Opioid Receptor Delta 1)CHRM5 (M5)CHRM2 (M2)

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