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Does the Low Dose Naltrexone mechanism extend to other drugs?

S-VV

Senior Member
Messages
310
LDN works by transient antagonism of the opioid receptors, thereby tricking the body to upregulate them.

Recently, I started taking a low dose of Clonidine for sleep. Clonidine binds to presynaptic alpha2 receptors, reducing adrenaline release. However, during the day I started having random shivers, I recognized them as adrenaline driven, since I also have them when I take midrodine, a pure alpha1 agonist.

What I think happened is that the low dose of Clonidine slowly reduced the number of alpha2 receptors.

Something similar happens when I took gabapentin for sleep. The following day I started having peripheral neuropathy. Gabapentin is used to treat neuropathy by blocking calcium channels is glutamatergic neurons, so I imagine the body upregulated those channels.

Now the question is, if our bodies are so sensible to neuroactive substances, could we take a low dose of a GABAa and a D2 antagonist in order to induce receptor upregulation? Or is naltrexone somehow special?
 

Hip

Senior Member
Messages
17,976
Now the question is, if our bodies are so sensible to neuroactive substances, could we take a low dose of a GABAa and a D2 antagonist in order to induce receptor upregulation?

Possibly, but the question is, would the upregulation actually have any useful clinical effects?



LDN works by transient antagonism of the opioid receptors, thereby tricking the body to upregulate them.

LDN has a number of different mechanisms:

blocks TLR-4 on microglia (anti-inflammatory)
antagonizes TLR-9, as well as TLR-7 and TLR-8
increases levels of met-enkephalin (opioid growth factor) and its receptor
• blocks the mu-opioid, delta-opioid and kappa-opioid receptors for a short while (thought to up-regulate endorphins)
• has an effect the nociceptin system
• may reduce peroxynitrite and may thereby increase astrocyte glutamate transport

It's not known which of these mechanisms help in ME/CFS.
 

junkcrap50

Senior Member
Messages
1,353
LDN works by transient antagonism of the opioid receptors, thereby tricking the body to upregulate them.
I saw just recently headlines of low dose Ritalin being more effective than regular dose. But I didn't read the articles or look into it.
 
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