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Most published research suggests a daily dosage of 4.5 mg, but this can vary by a few milligrams. [1] Low-dose naltrexone has been studied for the treatment of multiple chronic pain disorders including fibromyalgia, multiple sclerosis, Crohn’s disease, and complex regional pain syndrome. [2]
Naltrexone/bupropion, sold under the brand name Contrave among others, is a fixed-dose combination medication for the management of chronic obesity in adults in combination with a reduced-calorie diet and increased physical activity. [4] [6] It contains naltrexone, an opioid antagonist, and bupropion, an aminoketone atypical antidepressant. [4]
Methylnaltrexone is a peripheral acting mu-opioid receptor antagonist, and does not cross the blood brain barrier. [9] Methylnaltrexone has restricted access through the blood brain barrier because it is a quaternary amine, which carries a positive charge when in a solution.
The plasma protein binding of naltrexone is about 20% over a naltrexone concentration range of 0.1 to 500 μg/L. [6] [3] Its apparent volume of distribution at 100 mg orally is 16.1 L/kg after a single dose and 14.2 L/kg with repeated doses.
In a 2001 study with naloxone, three of fourteen patients lost their depersonalization symptoms entirely, and seven showed marked improvement. [4] The findings of a 2005 naltrexone study were slightly less promising, with an average of a 30% reduction of symptoms, as measured by three validated dissociation scales. [5]
It is unknown if GLP-1 agonists or dual/triple agonists of GLP-1 and/or the glucagon or GIP receptors act solely by reducing energy intake or if they also increase energy expenditure. [ 15 ] Setmelanotide is an agonist of the melanocortin 4 receptor and is used in people with certain rare genetic conditions that cause obesity.
It has been found to produce antidepressant-like effects in mice (similarly to the case of buprenorphine alone or in combination with samidorphan) [3] [4] and (at a buprenorphine dosage of 16 mg/day but not 4 mg/day) has recently been found to be effective in the treatment of cocaine dependence in a large clinical trial. [5] [6]
[2] [3] It is a major active metabolite of naltrexone formed by hepatic dihydrodiol dehydrogenase enzymes. [2] [3] With naltrexone therapy, 6β-naltrexol is present at approximately 10- to 30-fold higher concentrations than naltrexone at steady state due to extensive first-pass metabolism of naltrexone into 6β-naltrexol. [4]