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Discussion => Newbie discussion => Topic started by: HenryC0833 on July 07, 2013, 04:44 pm

Title: Suboxone and naloxone misconceptions
Post by: HenryC0833 on July 07, 2013, 04:44 pm
Post-whoring my way to 50....

A lot of people are confused by the apparent opiate-blocking effect of Suboxone, and what naloxone has to do with it.

Buprenorphine itself can have antagonistic qualities in some situations; the naloxone has nothing to do with it.

As you know, psychotropic drugs work by binding to receptors in the cell membranes of brain cells.  There are a number of different ways of describing this binding.  For example, how specific is it?  Will the drug bind to numerous receptors or just a small subset?  How long does the binding last for?  How "sticky" is the binding?  Is it easy, hard, or impossible to knock the drug off the receptor? 

Any number of drugs can bind a given receptor, and may have similar effects (eg, morphine, heroin, oxycodone).  Some bind a receptor and have no effect at all; and to the extent they displace effective chemicals, they can block the effect of a drug. 

So let's consider three actions at the opiate receptor:
1.  Heroin:  binds and activates.
2.  Naloxone:  binds and does nothing, thereby taking that receptor out of action for a while
3.  Buprenorphine:  binds but doesn't do all that much.

Buprenorphine is high affinity and low potency.  By high affinity I mean it will knock heroin or oxycodone off the receptor, and keep them off.  It does stimulate the receptor, just not as much as heroin does.

So if you're drug-naive, burprenorphine can give you opiate effects.  You can use it for pain control, for example.

But if you have a head full of heroin, the buprenorphine is not going to have nearly the effect you're used to.   It will feel like withdrawal to you. 

It will likely be an all-or-nothing effect.  12mg of buprenorphine is enough to cover every single opiate receptor in your brain.  Fortunately this is a one-way street.  If you have a head full of heroin or methadone, and take a bunch of buprenorphine on top of that, you will not likely have a very pleasant day as you suddenly and massively exchange one drug for another.  But if you have a head full of buprenorphine, taking heroin or oxycodone won't make you sick, because it is difficult for those drugs to displace the buprenorphine off the receptors.    More likely you will at least partially block their effects, although I'm told that if you take enough opiates, you can power through the buprenorphine effect.  Still, that's a useful property.  Helps guard against relapses. 

Naloxone is not orally active.  It's in Suboxone as a public health service to punish people for shooting it up.  I'm told there's a way of cooking it up to remove all or most of the naloxone, so I guess it's not totally effective in this regard.

There's a civil liberties angle on this, and a good practices angle.  You shouldn't prescribe two drugs when one will do, and you shouldn't force someone to take something they don't need to satisfy the ambivalence of some politician about drug treatment.  But that's what it is.

Note: naloxone and naltrexone are two different things.  Naltrexone is an oral opioid antagonist, and can be used to treat addiction and other things, like certain forms of autism.  Naloxone doesn't do anything if you swallow it, you have to snort it or inject it to experience that pain. 

Moral of the story:  generic Subutex is gonna basically be the same from the consumer's viewpoint as brand-name Suboxone.  The rest is politics. 
Title: Re: Suboxone and naloxone misconceptions
Post by: Garrincha on July 08, 2013, 09:55 pm
"Naloxone doesn't do anything if you swallow it, you have to snort it or inject it to experience that pain."

Isn't Suboxone the same as Subutex, in that you dissolve it under the tongue? Why would anyone want to shoot it up?