Last reviewed 2026-04-23 · How we verify

Naltrexone plus Gabapentin

Naltrexone blocks opioid receptors while gabapentin modulates calcium channels and GABA neurotransmission to reduce pain and cravings in opioid use disorder.

Naltrexone blocks opioid receptors while gabapentin modulates calcium channels and GABA neurotransmission to reduce pain and cravings in opioid use disorder. Used for Opioid use disorder, Opioid withdrawal symptoms and pain management.

At a glance

Mechanism of action

Naltrexone is an opioid antagonist that prevents opioid binding to mu, delta, and kappa receptors, reducing euphoric effects and cravings. Gabapentin enhances GABAergic inhibitory neurotransmission and modulates voltage-gated calcium channels, reducing neuropathic pain and anxiety. The combination targets both the reward pathway and pain/withdrawal symptoms associated with opioid dependence.

Approved indications

• Opioid use disorder
• Opioid withdrawal symptoms and pain management

Common side effects

• Nausea
• Dizziness
• Headache
• Somnolence
• Hepatotoxicity (naltrexone)

Key clinical trials

• Emergency Department-Initiated Medications for Alcohol Use Disorder (PHASE3)
• IV Ketamine Vs. in Esketamine for MDD TRD
• St. PETERsburg Pain and Alcohol Intervention With Naltrexone and Gabapentin (PHASE2)
• Effectiveness of Gabapentin When Used With Naltrexone to Treat Alcohol Dependence Compared to Placebo and Naltrexone Alone (PHASE3)

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Naltrexone plus Gabapentin CI brief — competitive landscape report
• Naltrexone plus Gabapentin updates RSS · CI watch RSS
• Medical University of South Carolina portfolio CI