The Use of Compounded Low Dose Naltrexone

Written by: Jaydee Robles, DACM, L.Ac

Medically Reviewed by: Dat Nguyen, PharmD, CPh

Current medical treatment for inflammatory conditions includes the use of steroidal anti-inflammatory drugs, NSAIDs, immunosuppressants, and other invasive types of drug therapies. Oftentimes these types of drugs have negative side effects that cannot be tolerated by certain patients. Recently the drug Naltrexone, a non-selective pure opioid antagonist, has been the focus of research for inflammatory conditions such as fibromyalgia, Crohn’s disease, multiple sclerosis, complex-regional pain syndrome, Hailey-Hailey disease, and cancer.

Compounded Low-dose naltrexone (LDN), taken in a daily dose of 1 to 5 mg, has been shown to decrease symptoms and modify the course of various inflammatory diseases. This is in part of the LDNs ability to reduce immune cells' inflammatory responses throughout the body. Another benefit to the drug's ability to combat inflammation is the drug's half-life and high absorption. Naltrexone’s half-life is 4 hours and it is a highly metabolized (>98%) drug, with very low potential for negative side effects.

In discrete compounded ‘low-doses’ ranging from 1 to 5 mg, naltrexone blocks cells from releasing pro-inflammatory chemicals. LDN is normally prescribed to be taken at bedtime as this is when our body produces pain-relieving and anti-inflammatory chemicals. This occurs between the hours of 2 am - 4 am in most individuals. These effects make compounded LDN an attractive tool for modulating the body's nervous system and immune system. These systems further bridge the central nervous system to the rest of the body. This is vital for regulating the body's response to inflammation.

One of the earliest studies of the use of compounded LDN was a study involving 17 patients with Crohn’s disease and Crohn’s disease activity index (CDAI) score of 220–450. Low-dose naltrexone was given in a 4.5 mg daily dose over 12 weeks. After the treatment, 89% of the patients were deemed responders with a decrease in CDAI score by 70 points, while 67% achieved disease remission.

The potential for compounded LDN as a means of treatment is becoming more understood and accepted, especially for patients who cannot tolerate more invasive therapies and alternative means of treatment are needed. Compounded LDN offers a viable pharmaceutical option with limited negative side effects and almost no potential for abuse.