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Does the Low Dose Naltrexone mechanism extend to other drugs?

S

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

Hip

Senior Member
Messages
17,858
S-VV said:
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?
Click to expand...

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



S-VV said:
LDN works by transient antagonism of the opioid receptors, thereby tricking the body to upregulate them.
Click to expand...

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

junkcrap50

Senior Member
Messages
1,333
S-VV said:
LDN works by transient antagonism of the opioid receptors, thereby tricking the body to upregulate them.
Click to expand...
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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