What is the recommended dosage and management strategy for Naltrexone (opioid receptor antagonist) in pain control?

Medical Advisory BoardAll articles are reviewed for accuracy by our Medical Advisory Board
Educational purpose only • Exercise caution as content is pending human review
Article Review Status
Submitted
Under Review
Approved

Last updated: June 3, 2025View editorial policy

Personalize

Help us tailor your experience

Which best describes you? Your choice helps us use language that's most understandable for you.

From the Guidelines

Naltrexone is not recommended for pain control in its standard dosage, but low-dose naltrexone (LDN) at 1-4.5mg daily can be considered for certain chronic pain conditions, with a recommended starting dose of 1.5mg at bedtime, gradually increasing to a maximum dose of 4.5mg daily, as supported by the most recent study 1. The use of naltrexone for pain control is complex, and its standard dosage can worsen pain or precipitate withdrawal in patients on opioid medications, as noted in a study from 2013 1. However, low-dose naltrexone (LDN) has emerged as an alternative approach for managing certain chronic pain conditions, including neuropathic pain, fibromyalgia, and complex regional pain syndrome. Some key points to consider when using LDN for pain control include:

  • Starting with a low dose of 1.5mg at bedtime and gradually increasing by 1.5mg every 1-2 weeks to a maximum dose of 4.5mg daily, as recommended in a 2017 study 1
  • Taking LDN consistently at the same time each day, preferably at night, to minimize potential side effects such as insomnia
  • Being aware that LDN requires compounding by a pharmacy, as commercial preparations are not available at these low doses
  • Monitoring for common side effects, including vivid dreams, headache, and initial sleep disturbances, which typically resolve within days to weeks
  • Avoiding concurrent use of LDN with opioid medications due to potential interference with pain control and risk of withdrawal symptoms, as highlighted in a 2021 consensus statement 1. It's essential to weigh the potential benefits and risks of LDN for pain control and to consider the individual patient's needs and medical history before initiating treatment.

From the FDA Drug Label

When Reversal of Naltrexone Hydrochloride Blockade is Required:- for Pain ManagementIn an emergency situation in patients receiving fully blocking doses of naltrexone hydrochloride, a suggested plan of management is regional analgesia, conscious sedation with a benzodiazepine, use of non-opioid analgesics or general anesthesia

The FDA drug label does not provide a specific recommended dosage of Naltrexone for pain control. Instead, it suggests alternative methods for pain management in patients taking Naltrexone, such as regional analgesia, conscious sedation, or non-opioid analgesics 2.

From the Research

Naltrexone Dosing for Pain Control

  • The recommended dosage of Naltrexone for pain control is typically considered low-dose, with studies showing effectiveness in chronic pain management at doses as low as 5.4 mg 3.
  • Low-dose Naltrexone (LDN) has been shown to reduce symptoms related to chronic pain conditions such as fibromyalgia, inflammatory bowel conditions, and multiple sclerosis 4.
  • The mechanism of LDN appears to be modulation of neuro-inflammation, specifically, the modulation of the glial cells and release of inflammatory chemicals in the central nervous system 4.

Management Strategy

  • Naltrexone can complicate postoperative pain management, and multiple studies have found that the use of naltrexone can increase the opioid requirement for postoperative pain control 5.
  • Multimodal pain regiments should be employed in patients, including non-pharmacological management and other modalities such as ketamine, lidocaine/bupivacaine, and duloxetine 5.
  • Low-dose naltrexone has been shown to be effective in chronic pain management, with a superior safety profile compared to other treatments such as amitriptyline 3.

Key Findings

  • Low-dose naltrexone significantly reduced pain by 32% in inflammatory conditions and 44% in neuropathic conditions 3.
  • Doses as low as 5.4 mg were found to reduce pain in 95% of patients with fibromyalgia 3.
  • Naltrexone is a mu-opioid receptor antagonist with a long half-life, and has been approved for the treatment of opioid and alcohol abuse 6, 7.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Is low-dose naltrexone effective in chronic pain management?

The Journal of family practice, 2023

Research

Low-Dose Naltrexone for Chronic Pain: Update and Systemic Review.

Current pain and headache reports, 2020

Research

Medication Treatment of Opioid Use Disorder.

Biological psychiatry, 2020

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

Have a follow-up question?

Our Medical A.I. is used by practicing medical doctors at top research institutions around the world. Ask any follow up question and get world-class guideline-backed answers instantly.