question on how it works

A board to discuss Low Dose Naltrexone (LDN) as a treatment for Multiple Sclerosis

question on how it works

Postby CureOrBust » Mon Sep 05, 2005 4:28 am

hi all,

Ok, i understand the theory, if i am not wrong:

Naltrexone blocks opioid receptors and by shutting them down for a short period, with only a low dose, the body kicks in and produces more endorphines (the bodys own opioid). And it is these endorphines that "correct" the immune system.

Now, that bit is all clear to me, and also why its taken at night. The bit I am wondering about is: Naltrexone only blocks the receptors, not the actual production of endorphines. So, if the receptors were blocked all day long, wouldn't the body try and produce endorphines all day long (thinking there are none in the blood)?

Or is it a case of the body can only be fooled for a little while, after which it corrects itself? i.e. stops making excess endorphines.

I just want to understand this point.

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Postby rasnet6 » Mon Sep 05, 2005 7:06 am

Difficult on to explain - the numbers below are just for example

say you have 1 million of the required receptors in your body

After an hour of having your tablet you will have perhaps 100 000 molecules of naltrexone in the blood, but only a % of these will be at the site of action (the receptors) lets say 10 000 molecules of naltrexone for instance.

these 10 000 molecules will bind to the receptors in a REVERSIBLE fashion, they will flit in and out of the receptor blocking its natural action.

However not all of the 1 million receptors are targetted at the same time, only 10 000 of them. Therefore there will be a bit of 'normal' behavior, but there will be some binding to the receptors by the naltrexone so the body will produce the endorphins.

In the meantime the blood is continually pumping around the body, taking the naltrexone with it. Every time the blood passes through the liver some of the naltrexone is removed. After about 2-6 hours there wont be enough naltrexone left to bind to enough receptors to produce a response. The body will then think it has returned to normal service and stop producing the excess of endorphins, and they will drop back to normal levels.

Most drugs are reversible binders, so they flit in and out of the receptor to cause a response, the blood then takes 'free durg' to the liver to be metabolised and rendered inactive for excretion. This allows the body to return to normal after the required response has been made.

If drugs were to bind permenantly the receptor would be in effect dead, no more normal service and will result in a side effects untill new receptors can be synthesised.

I really hope I havent confused you further

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Postby watergypsy » Wed Sep 21, 2005 12:51 pm

Hi there,

Sorry to jump in here but you have definitely confused me further! I’ve been puzzling about this for a while now and agree that your explanation would certainly account for some of the effects I am getting.

The weirdest thing about what is happening to me is that whilst the stiffness increases from just after lunch, it lessens as the afternoon goes on. Thus, by about 8 pm it has virtually gone.

What do you think about splitting the dose? Having experimented with 1, 2, 3 and 4.5 mg, I have now abandoned the 4.5 (way too much stiffness) and gone back to 3 mg. However, I have 30 or so 1 mg left and was wondering what you think about taking a 3 mg at say 11 pm and a 1 mg at 2 pm?

4.5 was seriously too much but 3 mg seems not enough. Dr. Lawrence is looking into getting some 3.8 mg but that may take a while yet. If I tried my suggested split dose, would I need to have a short nap at 2 pm? Does the naltrexone only work when you sleep?

Oh, what I’d give for the answers to all this! BTW, has anyone heard any good reports on the Milk Thistle yet?
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