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oaslam oaslam
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12 years ago
Converted to morphine and crossed the BBB, it binds to the opiate receptor sites leading to inhibition of GABA which in turn leads to a flood of dopamine.

So the paramedics arrive with their neat little box kit of naloxone and the overdosing casualty wakes to consciousness (hopefully)

What exactly happens to all that morphine that's still flowing around?
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12 years ago
IIRC (it's late), then Naloxone is a competitive antagonist with a high affinity for the opiate receptor. Basically. It fills up the overwhelming majority of the opiate receptors in the central nervous system.

Since those opiate receptors are occupied, an opiate, such as morphine, cannot provoke a physiological reaction. The site it needs is already occupied by a higher affinity molecule, which produces no reaction. So it sits there, inert, and is removed by the same body processes that would remove it if its effects weren't blocked.

Basically, the usefulness of naloxone is to block the effect of an overdosed opiate until the body can remove all of it.
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