How does buprenorphine and naloxone interact with each other in Suboxone? I’ve heard that buprenorphine is more potent than morphine, how does the naloxone prevent this?
In: Biology
Morphine is a full opiate agonist. It fits perfectly in the mud receptors in your brain and results in pain relief and euphoria. Buprenorphine is a partial opiate agonist, meaning it fits imperfectly in the my receptors, but still provides some pain relief but not so much (or any) euphoria. Naloxone is a full opiate antagonist, which means it perfectly blocks the mu- receptors and prevents opiates from reaching them.
Buprenorphine has a high affinity for the mu-receptors, which is why – if you take it while you are dependent and intoxicated with heroin/morphine – it will cause a precipitated withdrawal. The buprenorphine essentially throws out the morphine and takes its place firmly in the receptors, causing feelings of precipitated withdrawal.
Naloxone will also displace opiates in the mu receptors due to high affinity, resulting in withdrawal.
All that being said, naloxone has poor bioavailability when administered sublingual (under the tongue.) However, if you melt down the suboxone and try to inject it, the naloxone is much more bioavailable and will cause symptoms of withdrawal.
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