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Re: Suboxone???? Is it only for Opiates or an Ad Too?

Posted by undopaminergic on May 25, 2008, at 23:08:32

In reply to Suboxone???? Is it only for Opiates or an Ad Too?, posted by Phillipa on May 25, 2008, at 13:07:47

> I know this is used for opiate addiciton no I don't take opiates but the sender of the link the link says it is good for depression too. Is that true? Love Phillipa

The article you are probably thinking of can be found at the URL addresses listed below.

Buprenorphine is a partial mu-opioid receptor agonist and a kappa-opioid receptor antagonist. Both of these properties are beneficial to dopaminergic neurotransmission, and buprenorphine is slightly more effective than morphine in activating the dopamine neurons of the ventral tegmental area (VTA), which project to the shell of the nucleus accumbens (NAc) - often referred to as the brain's pleasure or reward centre.

The stimulation of kappa-opioid receptors results in a downregulation of the density of dopamine D2-receptors and the dopamine transporter (DAT) protein. These deleterious changes reduce dopaminergic neurotransmission, and blunts responsiveness to stimulant drugs.

The endogenous kappa-agonist is dynorphin - a peptide neurotransmitter. Dynorphin is released in response to chronic stress, by a mechanism that involves corticotropin-releasing factor (CRF). As a side-note, CRF is a hypothalamic hormone that stimulates the pituitary to secrete adrenocorticotropic hormone (ACTH), which in turn causes the adrenal glands to release cortisol.

Not only cronic stress, but also chronic use of cocaine elevates dynorphin, and the resultant stimulation of kappa-opioid receptors by dynorphin may explain the downregulation of D2-receptors that follows the use of stimulants, and which accounts for at least some of the tolerance that often develops to these drugs. Buprenorphine may prevent or at least attenuate these changes.

Dynorphin, via downregulation of D2-receptors, may also be responsible for the condition of anhedonia that results from chronic mild stress, which is used as an animal model of depression.

The dynorphin-antagonism of buprenorphine makes it an excellent theoretical choice of an antidepressant. However, in practice many people don't react well do buprenorphine, but prefer other opioids like oxycodone and methadone.

In conclusion, buprenorphine and other drugs acting on the opioid system are well worth trying for those who have failed to respond to more conventional treatments.




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