Posted 22 September 2018 - 03:26 PM
Can you provide a link to back your claim?
To anyone who is unaware of this, ALKS-5461 is a new antidepressant drug that may come out in 2019. The mechanism of how it works involves the opioid system which is a very different approach than any other anti-depressant drug on the market. The reason why this is relevant to us depersonalization sufferers is that this drug blocks the kappa opioiod receptor which is the reason why the drugs naloxone and naltrexone are thought to reduce depersonalization disorder symptoms. However, ALKS-5461 will supposedly act as a more potent kappa opioid receptor antagonist than naloxone or naltrexone and be much easier to get and tolerable to take.
In short ALKS-5461 could be the first "anti-depersonalization drug" but there is only hope and speculation at this point.
Here is the more detailed explanation of all this:
The hypothesis is out there that depersonalization symptoms may have to do with a specific opioid receptor called the kappa opioid receptor. A possible dysfuntion of this receptor may be the cause of symptoms in depersonalzation disorder. This idea is backed up by two small clinical trials where depersonalization patients were given naloxone in one study done in Russia, and naltrexone in another study in the U.S.A. The results of the naloxone treatment resulted in three of 14 patients having depersonalization symptoms disappearing entirely and seven patients showed a marked improvement. In the naltrexone study there was an average 30% reduction of symptoms with treatment, as measured by 3 validated dissociation scales. It is still unknown why this treatment may help, but since a naloxone injection or a very high dose of naltrexone acts as a μ-opioid receptor and a δ-opioid receptor antagonist, but more importantly as a partial kappa opioid receptor antagonist, it may be the effect on the kappa receptor that results in improvement. This is because kappa opioid receptor agonists are known to produce side effects such as dysphoria, hallucinations, and dissociation, which has limited their clinical usefulness. Centrally active KOR agonists have hallucinogenic or dissociative effects, as exemplified by salvinorin A(the active constituent in Salvia divinorum). The kappa receptor agonist enadoline has been shown to induce “pure” depersonalization in health volunteers according to Dr. Simeon. Some other evidence that it may be the kappa to blame is how a very high dose of naltrexone (250mg) was needed for DPD patients to experience any relief from naltrexone, and naltrexone only becomes a kappa opiod recptor antagonist at high doses of 200mg or more. The Wikipedia page for Naltrexone even states:
“Naltrexone is sometimes used in the treatment of dissociative symptoms such as depersonalization and derealization. Some studies suggest it might help. Other small, preliminary studies have also shown benefit. Blockade of the KOR by naltrexone and naloxone is thought to be responsible for their effectiveness in ameliorating depersonalization and derealization. Since these drugs are less efficacious in blocking the KOR relative to the MOR, higher doses than typically used seem to be necessary.”
Here are links to the two trials:
Posted 05 November 2018 - 11:51 AM
Are we looking at a 2019 January release date?
Posted 05 November 2018 - 11:52 AM
They are being taken orally in two 50 mg pills in am.
I saw the study and wiki post that it can help - but I’m not sure how high the dose was - I don’t think I’d mind to go up to 150/mg daily.
However, Naltrexone is VERY hard on the liver
Posted 04 January 2019 - 02:34 PM
By 'gets approved' what do you mean? Gets the green light for a wider study or is set for release for public use? I thought we were years away from this one being available...
Posted 05 January 2019 - 07:12 PM
In November 2018, an FDA advisory committee voted overwhelmingly against recommending approval, finding that evidence of efficacy was insufficient
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