Written by: Chettana Sanasith, PharmD. Candidate Class of 2019

What is Naltrexone?

FDA approved in 1984, naltrexone is an orally active opioid receptor antagonist, blocking the reception of the opioid hormones that our brain and adrenal glands produce (beta-endorphin and metenkephalin).1,2 It is structurally and functionally similar to naloxone.1 Naltrexone is FDA indicated for the treatment of opioid addiction at normal dosages (50-100 mg daily) helping those who addicted to heroin or opium products.1

Why Low Dose Naltrexone?

Low dose naltrexone has helped alleviate pain in conditions such as fibromyalgia and reduce autoimmune symptoms in conditions such as multiple sclerosis. Low dose naltrexone or LDN refers to dosages of naltrexone that are 1/10th to 1/50th of the normal strengths. At low dosages, naltrexone exhibits analgesic and anti-inflammatory properties that have not been reported at larger dosages.1 Additionally, LDN causes an increase in endorphin release resulting in an immune response.3 On the other hand, larger doses of naltrexone seem to negate the immunomodulatory effect by overwhelming the receptors.3 Physicians and researchers have described beneficial effects of LDN on a variety of diseases.

  • Cancers (lymphoma, multiple myeloma, etc.)
  • Neurodegenerative diseases (Alzheimer’s, multiple sclerosis, Parkinson’s, etc.)
  • Autoimmune diseases (celiac disease, systemic lupus, rheumatoid arthritis, etc.)
  • Other diseases such as HIV/AIDS (reported to improve CD4+ count)2

Advantages of LDN1

  • While pricing may vary, as a compounded product it is relatively inexpensive.
  • LDN displays a low side effect profile. There has been no reports of withdrawal symptoms when treatment is stopped. However, approximately 37% of patients have reported vivid dreams. As a side effect, this develops rapidly and decreases over time.1 This is unlikely to disrupt normal sleep patterns.
  • No reported cases of misuse or abuse. It is also not seen to develop dependence or tolerance with LDN.1 Cessation of LDN is generally followed by a slow return of symptoms to baseline levels.

Disadvantages of LDN 

  • Patients may need to individualize dosages.1 Many physicians may not be educated in dosage strengths for treating certain disease states. 
  • Although naltrexone has a long history of safe use with a wide range of large dosages, there is very little about long-term safety use when it is chronically used in low dosages.1
  • Since LDN is an off-label and non-mainstream treatment, it may not be covered by insurance plans. 


  • Oral liquid at 1 mg/1 mL is most commonly used. Taken daily and dosed using a baby oral syringe.
  • Capsules or tablets in a variety of strengths are available from compounding pharmacies.
  • Sublingual drops are designed for those who have issues taking the medication orally. This allows quicker delivery of medication into the bloodstream. Drops are placed under the tongue from a dropper bottle, and the dose is increased and decreased by the number of drops taken.
  • Creams are most typically available in 0.5 mg/mL. This formulation is helpful for children or those who are allergic to coloring, flavoring, or any excipients that may be found in other formulations of LDN.

Our Approach to Wellness

We believe that our patients' health should be managed with a healthcare team that includes the physician, pharmacist, and patient. We choose to utilize a collaborative, hands-on, and consultative approach in helping our patients find a solution to feeling better and safer.

Contact our team of pharmacists to review your medications and find an optimal treatment regimen for you. Physicians should also contact our pharmacists to speak about the best compounding options for patients.