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Rate of Downregulation and subsquent Upregulation with Opiates.

7ca5p

Bluelighter
Joined
May 22, 2009
Messages
277
Location
England
Okay, firstly, I know how ambiguous that is, and secondly, I also am aware that it will vary for each person.

My point and question is as follows.

I am on prescription analgesics every day.

However, the four DHC's I am prescribed is great for pain management, but ultimately lead to a summer in which I noticed minor withdrawals, so decided to stop the regularity of it to give my receptors some proverbial breathing space.

At current, I am having 15mg of DHC every two days. One day I will have it, then the next I will not. For example, tonight, despite being in considerable discomfort, I am not going to take any opiate medications, because I had 15mg DHC last night. I know 15mg is very small dose, but it does go some way to relieve the pain without making me feel spacey. I think this may be due, in part, to having very sensitive opiate receptors.

I also interrupt the cycle but using other opiates, in the form of Tramadol. Never taking the two within two days of each other. As far as I am aware, the two have a slightly different mechanism of action, but attempts of finding a disambiguation of this has been near impossible to find. Are they both active at the μ-opioid receptor?

I am wondering what the sustainable rate of opiate intake is, reaching a upregluation/downregulation equilibrium. I.e. reaching a point where by the intake of my painkillers is not downregulating my receptors. This is because my health has not shown any signs of getting better any time soon, and thus need to really plan my painkiller usage for the long term. I am undergoing treatments though, so perhaps will be better in a year or two. But for now, I don't want to

Such information is difficult to find, and my doctor is seemingly clueless about the matter, so I would appreciate any opinions.

Thanks for any help.
 
Nobody can tell you, it's variable for every individual.

Yes I am aware of that, as I mentioned in my post!

There is a plethora of points in my post, and as I said, a guideline figure is more helpful than absolutely 0. Heck, even a complete estimate from an informed individual is helpful to me at this point, as I'm really working blind.

Your post is word for word what my doctor has said numerous times, and with respect, it doesn't provide an iota of help for someone not wanting to get dragged in to a potentially dark world of opiate use.
 
It's simple. Empirical observations have shown that essentially nobody can use opioids daily without developing tolerance. Tolerance development always occurs to some extent, especially with daily usage... it's just a question of when and how severe. Hence why many doctors are hesistant to rely on opioids for anything but pallative care.

The only way to get around this is severe limitation of opioid analgesic use (as an adjunct, not the "main ingredient") and reliance on "alternative" painkilling methods (NSAIDs, cannabinoids, local anesthetics) as well as lifestyle adjustment. If you use opioids daily, you will eventually find they lose efficacy at current dose levels. It could take 3 days, it could take 3 years. But it will inevitably happen in the long term, especially if the underlying condition causing pain gets worse.

BTW, Dihydrocodeine and tramadol (& their metabolites) are both active at the mu opioid receptor. Tramadol actually has other mechanisms (such as serotonin/norepinephrine reuptake inhibition) that make it a more attractive painkiller and should theoretically make it more effective for longer, at least on paper.
 
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