Naltrexone [BSA]

Naltrexone is a synthetic opioid receptor antagonist with a chemical molecular structure comparable to that of opioids that is mostly used for opioid dependence and alcoholism. It lessens the ecstatic and addictive properties of drugs by antagonistizing opioid receptors and preventing opioids from binding to them, thereby inhibiting neurotransmitters like dopamine. The mechanism of action of naltrexone is completely opposite to that of opioids and therefore does not trigger similar biological effects. This property is key to the action of naltrexone, which is particularly important in withdrawal treatment and relapse prevention. Also, there's an immunomodulatory component to naltrexone. Naltrexone muzzles immune cells, reduces inflammation and even some autoimmune disorders such as Crohn's and rheumatoid arthritis.

Figure 1. Naltrexone structure
(Source: Bradley ES, et al. 2019)

While naltrexone at high doses completely inhibits the action of endogenous opioids (e.g., endorphins) and the patient experiences less pain and pleasure, when given at low doses naltrexone increases endogenous opioids and this helps the immune system work better. We have observed that LDN acts not just against opioid receptors, but also on cytokines that cause neuroinflammation. LDN is available as an adjunct to opioid painkillers alone, or when combined with opioids to increase the painkiller effect and minimise side effects.

LDN is cheaper than high-dose naltrexone, less side-effect-laden, and drug-free compared with the latter. LDN is usually well tolerated and safe for most patients. The most common side effect is dreaming, with a few patients experiencing nightmares. It kicks in immediately after taking LDN, but then goes away gradually. LDN, when administered for drug addiction, does not euphoria or make a drug stronger, and it does not cause dependence or tolerance, so it's safe for the treatment of addiction.