Low Dose Naltrexone (LDN): Alternative Treatment for Pain and Inflammation

Low Dose Naltrexone (LDN): Alternative Treatment for Pain and Inflammation

By: Sobia Khan, M.D., EdD • Posted on April 10, 2023

What is Naltrexone and Naloxone?

Naltrexone belongs to a class of drugs called opioid antagonist. In 1984, Naltrexone was first approved as a treatment for opioid addiction. In 2006, it was studied for treatment of alcohol abuse, and it was effective in decreasing alcohol cravings - 70% of clinical trials indicated benefit with its use.

Naloxone (Narcan) is also an opioid antagonist. Naloxone is fast acting to assist with opioid overdose. Naltrexone is slow acting and blocks the effects of opiates and alcohol.

What is Low Dose Naltrexone (LDN)?

Low-dose naltrexone, also known as LDN, is taken in doses much smaller than the size of a traditional dose. In 1985, Dr. Bernard Bihari identified that use of low dose naltrexone (LDN) 3mg at bedtime can enhance the immune system's response against HIV infection.

Symptoms of a poor immune system

A malfunctioning immune system can be expressed as vague bodily symptoms, including:

  • Atypical pain
  • Myalgia
  • Arthralgia
  • Rash
  • Fatigue
  • Sleep disorder
  • Depression
  • Maldigestion
  • Sensitivities to food and environment

Off label use of Low Does Naltrexone (LDN) for modulating immune response

The immune system is regulated by endorphins, and they have prime effect on opiate receptors. If opiate receptors are temporarily blocked by low dose naltrexone, it upregulates the production of endorphins. This can help improve immune function by immune modulation and symptom improvement by reduction in inflammatory cytokines.

Since its use in HIV patients, LDN use has been studied for several neurodegenerative diseases such as Multiple Sclerosis and autoimmune conditions like lupus (SLE), rheumatoid arthritis and fibromyalgia. It has gained popularity as an alternative, off label treatment that improves inflammation by immunomodulation.

LDN treatment for women's health conditions

In women’s health, LDN is used as an alternative treatment for inflammatory pain due to endometriosis, suppress inflammation to improve fertility, gut dysbiosis, fibromyalgia and pelvic pain due to endometritis. Its use is off label for such conditions, and it needs to be ordered by a physician and can only be compounded at reputable pharmacies. The only commercially available dose is 25-50mg, therefore it's best to compound the low dose naltrexone.

LDN dosage

LDN dosing starts from 1.5mg at night orally for 4 weeks and titrated up gradually to 4.5mg. Taking it at bedtime can block opioids receptors between 2am and 4 am and potentiate the upregulation of immune response by increasing endorphins and enkephalin.

The cost for compounding LDN three month prescription can range according to patients requirement for dose adjustment. For more information on pricing and details for compounding prescriptions, patients and clinicians can visit

LDN side effects

Its potential side effects are insomnia and nightmares. If observed, LDN can be taken during the daytime to avoid such side effects. If any gastrointestinal side effects are noted such as diarrhea, abdominal pain, nausea, the titration of LDN should be halted at the dose best tolerated. It usually takes consistent use for 3-6 months to give the maximum benefit.

It is not a controlled substance, but prescribed only by licensed physicians. There is insufficient data on LDN use during pregnancy, as there has been no adequate controlled studies on pregnant women. It's contraindicated to be used in patients with organ transplantation and on immunosuppressive medications.

Be Strong, Be Healthy, Be in Charge!

- Sobia Khan, MD, EdD

About Sobia Khan, MD, EdD

Dr. Sobia Khan is board certified in internal medicine physician and holds a doctoral degree in Professional Leadership and Health Science Education by University of Houston, Texas.

Prior to joining Cleveland Clinic as Menopause and Functional Medicine specialist she served as Director of Center of Women's Center for Comprehensive Care at Baylor College of Medicine for ten years.

She is a certified Functional Medicine practitioner and now offering Women's Health Functional Medicine consultation at Center of Specialized Women's Health, Women's Health Institute, Cleveland Clinic.

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