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Opioids Which has a more affable hold on opiate receptors, Methadone or Buprenorphine?

velocity92c

Bluelighter
Joined
Jun 29, 2009
Messages
82
Trying to settle a dispute, and I'm not talking about mg vs. mg, I'm referring to a typical daily dosage. Let's say 8mg Bupe vs. 80mg Methadone. This is actually a harm reduction question because I've got a friend that doses on top of Methadone which I think is dangerous. He claims to be able to get high after taking Methadone but I'm pretty sure Methadone has one of, if not the most affable hold on opiate receptors.
 
Buprenorphine, just because buprenorphine has better binding affinity than Narcan.

Narcan can reverse a methadone OD, but can't reverse a buprenorphine OD...

Somebody correct me if I'm wrong...
 
no you are correct i know i am new but you are right you can most certaintly get high while on methadone i have done by doing my DOC oxy after i already took some meth

However you are right it is very dangerouse because it increases the chance of OD and i knew this when i did it
 
Narcan can reverse a methadone OD, but can't reverse a buprenorphine OD...

Is a buprenorphine OD even possible? I've used it to revive people, I suppose if norbuprenorphine, it's direct metabolite, is a full agonist then yeah, but its more quirky in bodily metabolism aligning more correctly than with other simple full agonists to OD on I'm guessing?
 
Is a buprenorphine OD even possible? I've used it to revive people, I suppose if norbuprenorphine, it's direct metabolite, is a full agonist then yeah, but its more quirky in bodily metabolism aligning more correctly than with other simple full agonists to OD on I'm guessing?

if it was a pure bupe OD I'd imagine the person would have to be very sensitive to opiates, but it's definitely possible when mixed with benzos, barbituates, or alcohol
 
Methadone is also an NMDA antagonist, and buprenorphine also works on other receptors which include other opiate receptors and other non-opiate receptors.

Because of this, to compare each with respect to just the mu-opioid receptor, may not really be that great of a comparison in the first place.

Comparing 8mg of buprenorphine to 80mg of methadone is not great to compare because some people would say 80mg of methadone is "a lot", others would say it's "enough but I could go for more" and yet others would say "that's way too little for me".

8mg of buprenorphine would be far more than needed for many, many opiate users. Some people would find it to be "not enough", especially if they are early in their recovery.

if it was a pure bupe OD I'd imagine the person would have to be very sensitive to opiates, but it's definitely possible when mixed with benzos, barbituates, or alcohol

Extremely sensitive or possibly not in good health, but yes your answer was very well stated.
 
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Buprenorphine, just because buprenorphine has better binding affinity than Narcan.

Narcan can reverse a methadone OD, but can't reverse a buprenorphine OD...

Somebody correct me if I'm wrong...

You may be right.

This is what I got from wiki:

Buprenorphine is a thebaine derivative with powerful analgesia and its analgesic effect is due to partial agonist activity at μ-opioid receptors, i.e., when the molecule binds to a receptor, it is less likely to transduce a response in contrast to a full agonist such as morphine. Buprenorphine also has very high binding affinity for the μ receptor such that opioid receptor antagonists (e.g. naloxone) only partially reverse its effects. These two properties must be carefully considered by the practitioner, as an overdose cannot be easily reversed. Overdose is unlikely in addicted patients or people with tolerance to opioids who use the drug sublingually as meant in the case of Subutex/Suboxone, especially if there is no alcohol involved. Concomitant use of alcohol with any opioid increases the risk of overdose. One French study showed a higher incidence of fatal overdose in patients who injected both buprenorphine and benzodiazepines, specifically, temazepam, together. Buprenorphine can be safely taken with prescribed benzodiazepines at normal dosage, as long as the patient is tolerant to either opioids or benzodiazepines, and the drugs are taken in the dosages prescribed and by the route of administration prescribed, and not injected.
 
Bupe has a much stronger affinity at the mu opioid receptor than methadone and will displace methadone, fent, and even compete with naloxone when taken at the same time.
 
Speaking from a purely biochemical point of view, buprenorphine has a Ki (dissociation constant) of 1 to 1.5 nanomolar vs methadone's ~3 nmol in human tissue. Smaller numbers indicate better binding (higher affinity).

Edit: This is basically what amapola said.
 
Damn, oxycodone has a Ki of 13.345 nmol, morphine has a Ki of 2.55 nmol.

EDIT: Codeine has a Ki of 3513.5 nmol and hydrocodone has a Ki of 11.1 nmol.
 
OK, so I was wrong about it having the most affable hold on opiate receptors - but according to the data posted it still has a very affable hold on receptors. Doesn't this mean it still acts as a blockade against other opiates, especially at a higher dosage (80mg+)? I know that's not an insanely high dosage, but shouldn't that be enough to 'block' other opiates ? For one, I don't want my friend to endanger himself. 2, I don't want him to waste his money dosing on top of methadone when I feel that it is pointless.

I have been on methadone for about 6 months, and not only could I not feel anything after a fairly low daily dosage of methadone (40mg), I couldn't feel anything for DAYS after stopping dosing.
 
Methadone has a very long half life which is why you didn't feel anything for days. The blockade effect as you mentioned is well documented and it takes a lot more of a drug to feel the effects but it often is possible to break through it especially at lower doses.
 
Damn, oxycodone has a Ki of 13.345 nmol, morphine has a Ki of 2.55 nmol.

EDIT: Codeine has a Ki of 3513.5 nmol and hydrocodone has a Ki of 11.1 nmol.

The fact that codeine's Ki is so high (meaning low affinity) is a bit deceptive. Remember that codeine is largely metabolized into morphine so while it's true that codeine's affinity is extremely low, it's active metabolie morphine has a very high affinity.

And something for everyone to keep in mind-binding affinities have nothing to do with potency or level of euphoria. For example, while Bupe has an incredibly high affinity, it is is only a partial agonist with a low level of euphoria.
 
Remember that codeine is largely metabolized into morphine so while it's true that codeine's affinity is extremely low, it's active metabolie morphine has a very high affinity.
This just came up in a thread in OD where someone could break through low dose bupe or methadone on codeine but not hydrocodone and I mentioned this. I'll add though that codeine being "largely" metabolized to morphine is wishful thinking...:(
 
def bupe, its affinity last for days depending on the dose. Im on 8mg 2 times a day and if I take my whole dose I cant do opiates and get a buzz for at least 24 hours. Unless its something like phynt. bc that has a really high affinity aswell. enough to "break through" the sub
 
OK, so I was wrong about it having the most affable hold on opiate receptors - but according to the data posted it still has a very affable hold on receptors. Doesn't this mean it still acts as a blockade against other opiates, especially at a higher dosage (80mg+)? I know that's not an insanely high dosage, but shouldn't that be enough to 'block' other opiates ? For one, I don't want my friend to endanger himself. 2, I don't want him to waste his money dosing on top of methadone when I feel that it is pointless.

I have been on methadone for about 6 months, and not only could I not feel anything after a fairly low daily dosage of methadone (40mg), I couldn't feel anything for DAYS after stopping dosing.

I guess i should have stated that i was only on 40 mg's of methadone which i was tollerant to it but it only took me about 60 mg's of oxycodone to feel high as opposed to about 250 it usually takes
 
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