Posted by ed_uk2010 on April 11, 2010, at 7:21:47
In reply to Re: TCA's With Opioid Actions?, posted by bulldog2 on April 10, 2010, at 17:25:22
Amitriptyline (Elavil) is believed to be one of the most effective TCAs for chronic pain. It's very widely used for this purpose. I don't believe that its efficacy in pain has much (if anything) to do with opioids, however. NE reuptake inhibition is thought to be an important mechanism. Its activity at sodium channels in the nervous system may also be relevent. Also, sleep is usually disturbed in patients with severe pain - amitriptyline can certainly help in this department. Nortriptyline is also effective for neuropathic pain. It may be slightly less effective than amitriptyline but generally better tolerated. Imipramine is another TCA which has been used for pain relief. It is considerably less sedating than amitriptyline, but may have similar efficacy. It hasn't received as much study for pain as amitriptyline.
> > Yeah, like you mentioned the TCA's do have some (direct) NMDA antagonist effects. They are also sigma1 receptor agonists (especially imipramine) which elevates synaptic neurite outgrowth. Amitriptyline (in addition to these actions) is a direct agonist at TRKa and TRKb receptors. This activity promotes neurogenesis and induces neuroprotection.
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> > Oh, also, the TCA's have some effect on monoamine oxidase. Generally, they exert stronger effects on MAO-b than MAO-a. I think trimipramine is also a dopamine reuptake inhibitor.
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> > The SSRI's were initially lauded as the product of "rational" drug design - as if they identified "the" mechanism. The notion that the TCA's were working solely in their capacity as serotonin reuptake inhibitors in nonsense. I think between this post (and the one below) we have identified like 15 different antidepressant like targets of the TCA's. Better go back to the drawing board.
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> > Linkadge
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> I guess we all remember Peter Kramer's book "Listening to Prozac". Even if we weren't depressed but just a little bored we wanted Prozac. So everyone is now running to their GP and feeling depressed and so the flood begins. Definiltely some indoctrination going on to market the product. Recently met some friends who flew in, mother,daugher, father are on ads.
> Now that we have such a safe product in that you can't die because of overdose there is a campaign to find depression in every nook and cranny. You have to wonder how much Eli Lilly knew or pushed the inappropriate diagnosis of depression for profit. After all the product was so safe compared to the dangerous and side effct riddled tcas and maois.
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> So the success of the tcas in severe depression is the fact they are dirty and touch every corner of the brain or almost do.
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> Right now I'm looking for the best tca for both depression and pain. Need something that will work with percocet for both sciatica and severe hip arthritis (not the repaired hip). Is there a best tca for pain? Right now I find elavil better than nortriptyline for both pain and arthritis.
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poster:ed_uk2010
thread:942955
URL: http://www.dr-bob.org/babble/20100406/msgs/943046.html