Many people out there are aware of the "blocking effect" of buprenorphine. This supposedly happens because buprenorphine while being a partial agonist, has a higher affinity for the receptors in the brain. Basically if an opiate with a weaker affinity has already binded itself to the receptor and buprenorphine is introduced it will knock that opiate off of the receptor and take its place. Or if buprenorphine is already binded to the receptor and other opiates are taken, they are not able to bind because the buprenorphine essentially blocks them from doing so.
This made me wonder about how binding affinity comes into play when the opiates in question are those other than buprenorphine. Suppose you are taking full agonists... Two chronic pain patients may be given the same time-release opiate for pain control but different breakthrough pain meds. Surely there would have to be some logic in which particular medication would be used for breakthrough pain, and I can't help but wonder how much binding affinity would come into play in such a situation. I'm no doctor or pharmacologist however binding affinity is rarely mentioned outside of when discussing buprenorphine. Surely it's possible for one full agonist to compete with other full agonists for a spot on a receptor.
It also makes me wonder about our natural endorphins and their binding affinity in comparison with different artificial opiates. Does morphine knock our natural endorphins off of the receptors? This is something that is probably a bit over my head but even so, I'm curious.
05-07-2007, 06:54
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