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Re: Temgesic 0.2mg Tablets

Posted by undopaminergic on June 25, 2008, at 8:27:27

In reply to Re: Temgesic 0.2mg Tablets » undopaminergic, posted by Crotale on June 20, 2008, at 18:17:55

>
> > No nausea or itching for me, but it's somewhat sedating in a special way when I take higher doses - even though I always take stimulants too.
>
> Err...what do you mean by "a special way?"
>

I mean that it's unlike normal sedation or tiredness, because there is no exhaustion, and little, if any, cognitive impairment. The main effect is the strong tendency of the extraocular muscles to relax, so that the visual axes are parallel and double vision results at near distances (such as the computer screen and books). To a lesser extent, a tendency for the muscles of the neck to relax is also present, but not enough so to result in "nodding" (unless I were to *really* take too much).

> I suspect the itching is the result of stimulation of histamine release, an effect common to mu-agonists
>

I don't think histamine release is due to mu-opioid receptor stimulation, but due to the direct diffusion of the morphine-like molecules into mast cells, resulting in the displacement of histamine through the cell membrane into the extracellular space where it can reach and stimulate histamine H1 receptors. I don't think itching occurs with synthetic opioids like methadone and fentanyl, which are structurally quite different from poppy alkaloids.

> (BUP is effectively a morphine-like agonist at low doses).
>

Partial agonist, and kappa-antagonist. It probably doesn't have much of an effect on delta-opioid receptors at low doses, but at higher concentrations, it acts as an antagonist, and this is a reason why higher doses may be disadvantageous (delta-agonism is generally beneficial, so antagonism is scarcely desirable).

> > I haven't noticed a clear analgesic effect - perhaps a little, though.
>
> Even when you first started taking it?

Including then.

> > I'm now introducing a MAOI too.
>
> Which one? Let me know how the combo works for you.
>

Just low doses of rasagiline. It doesn't appear to have pronounced effects. Maybe I'll try higher doses at some future point.


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