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?

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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

Naloxone is a competitive antagonist. That’s fancy for it is fighting buprenorphine for the same receptor sites, it is just way better at getting them. Naloxone (Narcan) is essentially a much better version of buprenorphine, but it doesn’t get you high.

Naloxone is not well absorbed orally while buprenorphine is. At high enough dosage, the effect of naloxone (which blocks opioid effects) does start to become significant, which decreases the effect from dose escalation. The biggest reason is for injection though, as naloxone is fully active there, and injecting will not give you a significant high, and might even precipitate withdrawal.

To a drug user, potency just means more difficulty in metering out a hit (whereas pharma companies have the tech to do so). It doesn’t necessarily translate into good shit mang.

The opiates that are more potent than heroin – fentanyl, U-47700, many of them are regarded as simply not as enjoyable, mostly used by existing addicts too deep to seek pleasure but rather withdrawal’s relief.

Buprenorphine isn’t one of those drugs some would commend like heroin. It is to stop those urges had from withdrawal. The naloxone isn’t actually active through the prescribed route, but rather by injection only – in order to dissuade users from injecting the Suboxone.

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.