In one study, the majority of sexual offenders reported a strong reduction in sexual urges and fantasies which reverted to baseline once the medication was discontinued. Case reports have also shown cessation of gambling and other compulsive behaviors, for as long as the medication was taken. Available forms
Naltrexone is available and most commonly used in the form of an oral tablet (50 mg). Vivitrol, a naltrexone formulation for depot injection containing 380 mg of the medication per vial, is also available. Additionally, naltrexone subcutaneous implants that are surgically implanted are available. While these are manufactured in Australia, they are not authorized for use within Australia, but only for export. By 2009, naltrexone implants showed superior efficacy in the treatment of heroin dependence when compared to the oral form.When taken at much smaller doses, a regimen known as Low Dose Naltrexone (LDN), naltrexone may reduce pain and help to address neurological symptoms. Some patients report that LDN helps reduce their symptoms of ME/CFS, multiple sclerosis (MS), fibromyalgia (FMS), or autoimmune disease. Although its mechanism of action is unclear, some have speculated that it may act as an anti-inflammatory. LDN is also being considered as a potential treatment for Long COVID. Contraindications
Naltrexone should not be used by persons with acute hepatitis or liver failure, or those with recent opioid use (typically 7–10 days). Side effects
The most common side effects reported with naltrexone are gastrointestinal complaints such as diarrhea and abdominal cramping.
In accordance with its partial agonism, although naltrexone is described as a pure opioid receptor antagonist, it has shown some evidence of weak opioid effects in clinical and preclinical studies.By itself, naltrexone acts as an antagonist or weak partial agonist of the opioid receptors. In combination with agonists of the MOR such as morphine however, naltrexone appears to become an inverse agonist of the MOR. Conversely, naltrexone remains a neutral antagonist (or weak partial agonist) of the KOR and DOR. In contrast to naltrexone, 6β-naltrexol is purely a neutral antagonist of the opioid receptors. The MOR inverse agonism of naltrexone when it is co-present with MOR agonists may in part underlie its ability to precipitate withdrawal in opioid-dependent individuals. This may be due to suppression of basal MOR signaling via inverse agonism.Occupancy of the opioid receptors in the brain by naltrexone has been studied using positron emission tomography (PET). Naltrexone at a dose of 50 mg/day has been found to occupy approximately 90 to 95% of brain MORs and 20 to 35% of brain DORs. Naltrexone at a dose of 100 mg/day has been found to achieve 87% and 92% brain occupancy of the KOR in different studies. Per simulation, a lower dose of naltrexone of 25 mg/day might be expected to achieve around 60% brain occupancy of the KOR but still close to 90% occupancy of the MOR.