DWritten 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



What Is Naltrexone




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 has not been reported at larger dosages.1 Additionally, LDN causes an increase of 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 LDN 1


  • 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 has 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 dosages strengths for treating certain disease states.  
  • Although naltrexone has a long history of safe use with 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 nonmainstream treatment, it may not be covered by insurance plans.  


Formulations 4


  • 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 issue taking the medication orally. This allows quicker delivery of medication into the bloodstream. Drops are placed under the tongue from a dropper bottle and 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.


Connect with Us

If you have any questions or would like additional information, please contact Innovation Compounding at 1-800-547-1399, Monday-Friday, 9 a.m. to 5 p.m. EST, excluding all major holidays.

Medical Disclaimer This content is for informational and educational purposes only. It is not intended to provide medical advice or take the place of such information or treatment from a personal physician. All readers/viewers of this content are advised to consult their doctors or qualified health professionals regarding specific health questions. Neither Innovation Compounding, Inc. nor the publisher of this content takes responsibility for possible health consequences of any person or persons reading or following the information in this educational content. All viewers of this content, especially those taking prescription or over-the-counter medications, should consult their physicians before beginning any medication, nutritional supplement, diet, or health regimen. Innovation Compounding does not make or intend to make any claims to efficacy or safety of compounded products for specific conditions or disease states, as compounded products are not FDA-approved for these conditions. 


The Power of Naltrexone for Treating Addiction https://www.evergreendrugrehab.com/blog/power-naltrexone-treating-addiction


  1. Younger J, Parkitny L, McLain D. The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clinical Rheumatology. 2014;33(4):451-459. doi:10.1007/s10067-014-2517-2

  2. The Low Dose Naltrexone Homepage. http://www.lowdosenaltrexone.org/#What_is_low_dose_naltrexone.

  3. How Naltrexone Works | LDN Research Trust – Low Dose Naltrexone. https://www.ldnresearchtrust.org/how-naltrexone-works.

  4. Formulations of LDN | LDN Research Trust – Low Dose Naltrexone. https://www.ldnresearchtrust.org/types-of-ldn.

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