Low Dose Naltrexone: An Overview

Before we discuss how LDN works, we need to go over the role of endorphins in the body. Endorphins are opiate-like molecules in the body. They are produced in most cells in the body and are important regulators of cell growth and the immune system. Disorders of the immune system, like autoimmune disorders, can occur with unusually low levels of endorphins. The particular endorphin that has been found to influence cell growth is called Opioid Growth Factor (OGF). For an endorphin such as OGF to exert its beneficial effects, it must interact with the body’s cells. It does this by binding to a receptor on the surface of the cells.

Naltrexone is an orally administered drug that binds to opioid receptors. In doing so, it displaces the endorphins which were previously bound to the receptors. Specifically, by binding to the OGF receptors, it displaces the body’s naturally produced OGF. As a consequence of this displacement, the affected cells become

deficient in OGF and three things happen:

1) Receptor production is increased, in order to try to capture more OGF.

2) Receptor sensitivity is increased, also to try to capture more OGF.

3) Production of OGF is increased, in order to compensate for the perceived shortage of OGF.

Since LDN blocks the OGF receptors only for a few hours before it is naturally excreted, what results is a rebound effect; in which both the production and utilization of OGF is greatly increased. Once the LDN has been metabolized, the elevated endorphins produced as a result of the rebound effect can now interact with the more-sensitive and more-plentiful receptors and assist in regulating cell growth and immunity. The elevated level of endorphins can result in an enhanced feeling of well-being as well as a reduction in pain and inflammation. The duration of the rebound effect varies from person to person but generally lasts about one day. This effect can only be utilized by taking a low dose of naltrexone and not a high dose or extended-release naltrexone.