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Subject: Naloxone sucks

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Suboxone or Subutex, what is better?
  Suboxone
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smallville

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Joined: 24 May 2009
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Question Naloxone sucks Reply with quote
 
Naloxone is a ingredient in Suboxone to prevent people from shooting it up.
Naloxone stopes endorphins from producing naturally in the brain
or from activity's like eating, exercise,sex,etc.
Suboxone helps my withdraw a lot.
But Suboxone gives me a bad mood.
Ive been in this mess for six years. (oxy, sub, perks etc.)
And doing hard research the whole time.
But I always have a open mind. Laughing
 
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alaskagirl

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Joined: 22 Jul 2009
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Note maybe it isnt the suboxone? Reply with quote
 
maybe it isnt the suboxone putting you in a bad mood- if your taking all this stuff at the same time, even if it isnt putting you in actuall withdrawal- the suboxone is probably doing what its supposed to do which is fight the other drugs running around in your brain. try JUST taking the subs for a while- like a month and see how you feel. you may also need something to go with your suboxone like a anti depresant or anxiety medication, but you cant do that if your still taking all these other things. Be honest with yourself and your doctor about your feelings. thats about the best advice I can give. naloxone is (while the addict in us may not want to agree) a god send. get serious about being really "clean" and being just on suboxone without the other drugs is something you will be able to feel really good about!
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StaffWriter

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Naloxone remains an inactive substance when Suboxone is taken sublingually or even snorted. It is used as a deterent against having people shoot it up and even then, the naloxone in Suboxone remains inactive. It was a scare tactic by RB to discourage abuse and encourage the FDA to allow suboxone to be prescribed in an office setting. So basically it is a placebo effect for the FDA and DEA. It doesn't do anything. Completely inactive. Although some who are sensitive to it may get a headache. If it causes a headache, switch to Subutex. Many people think it's the naloxone that causes precipitated withdrawal. It's actually the properties of an agonist/antagonist that is Suboxone.
 
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Derek

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Joined: 23 Oct 2009
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StaffWriter wrote:
Naloxone remains an inactive substance when Suboxone is taken sublingually or even snorted. It is used as a deterent against having people shoot it up and even then, the naloxone in Suboxone remains inactive. It was a scare tactic by RB to discourage abuse and encourage the FDA to allow suboxone to be prescribed in an office setting. So basically it is a placebo effect for the FDA and DEA. It doesn't do anything. Completely inactive. Although some who are sensitive to it may get a headache. If it causes a headache, switch to Subutex. Many people think it's the naloxone that causes precipitated withdrawal. It's actually the properties of an agonist/antagonist that is Suboxone.

Good Info!
 
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IrishSubs35

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Joined: 04 Feb 2010
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I agree that it is inactive. Thats what I always thought. What is this I hear that it blocks natural endorphines? Is that true or is that person confused? I still feel good after a nice meal!!! Smile I could not find anything like that online.
 
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jdhammond1982

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Joined: 02 Nov 2009
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No naloxone is absorbed into the body from using Suboxone sublingually and/or swallowing saliva with buprenorphine and naloxone in it. Here's why:

This is a quote from Suboxdoc's posted answer in the thread "Doc swiched me from Suboxone to Subutex" in the forum topic room "Dosing Discussion":

"We also know what happens when a person takes Suboxone vs. Subutex. Buprenorphine is very lipophylic i.e. dissolvable in oil vs. water. It passes easily through lipid membranes (cell membranes are lipids, and so oil-soluble drugs pass through them more quickly than water-soluble drugs). This phenomenon is why injected fentanyl has an effect in about 20 seconds, whereas morphine has an onset time fo 10 minutes evern after IV injection.

On the other hand, naloxone is 'hydrophylic', or water soluble. It does not pass through mucous membranes, instead going down the esophagus and being absorbed in the first part of the small intestine, the duodenum. The naloxone is take to the liever where it is almost entirely destroyed by something called 'first pass metabolism;' the liver has the capacity to easily destroy all of the naloxone that reaches it, so that no naloxone makes it out the other side, to the blood leaving the liver.

When I was an anesthesiologist, it was fairly common to inject naloxone intravenously. If a patient had a narcotic-based anesthetic, sometimes a tiny sprinkle of naloxone was needed to get the person breathing again at the end of the case. There were a couple rists to giving even small doses of IV naloxone; one was that even a small IV dose could precipitate pulmonary edema by effects on pressures in the pulmonary venous circulation. Too much naloxone could result in the patient awakening in pain. Finally, naloxone is a very short-acting medication, so there was risk of 'renarcotization', where the naloxone got the person breathing, but then wore off as you waled the patient to the ICU or recovery room, causing the patient to stop breathing. Gosh, I sometimes miss those days!

The primarly point of relevance here is that naloxone is a very short-acting drug. It lasted about 15-20 minutes in small doses-- and the doses in Suboxone are also small doses. It wears off by being metabolized by the liver, and also by 'redistributing' throughout the body and becoming very diluted in the bloodstream. I also (ick) injected naloxone by accident into myself during a desperate weekend search for narcotics-- so desperate that I injected the contents of an unlabelled syringe that tasted like an opiate (I would taste the things I found to try to avoid dying of an injection of a paralyzing agent-- pretty dumb stuff).

Suboxone and Subutex are equal when taken orally. The naloxone is not going to be absorbed, because the lipid nature of cell membranes is universal. So everyone who takes Suboxone ends up swallowing naloxone, and almost everyone gets no effect from it.... but let's imagine for the sake of argument that the original writer of this thread WAS getting an effect from the naloxone... maybe it was not completely broken down at the liver. If that was the case, the person would get withdrawal symptoms from the naloxone for maybe 20 minutes-- which is how long naloxone lasts, even when INJECTED, and in much higher doses than what is found in Suboxone. There is just no way that the naloxone in Suboxone is going to have a prolonged effect in the body-- of ANYONE." -Suboxdoc

Hope that helps (I had to cut and paste manually and add my own quotations, because I didn't know how to "really" quote Suboxdoc the way we're supposed to.)
james
 
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Schrodinger's Cat

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Joined: 19 Mar 2010
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Quote:
Completely inactive.


Are you saying that injecting 2 mg of naloxone will not have any effect? How is that even possible? I would say that it's highly improbable that injecting 2 mg of naloxone will have no effect. Perhaps no outwardly measurable effect, maybe--even then though I think it unlikely.

I think that not all of the buprenorphine is "blocked" by the naloxone (i.e. buprenorphine has a higher binding affinity) but it should still have some effect.

I'm curious. The molar mass of buprenorphine is 467.64 g/mol and naloxone is 327.27 g/mol. This means that there are 6.022 x 10^23 molecules of buprenorphine in every 467.64 g of it. So, in an 8/2 Suboxone there are:

((467.64 g/mol)/(0.008 g))^-1 --> (1.7107 × 10^-5 moles) * (6.022 x 10^23) = 1.0302 × 10^19 molecules o' buprenorphine

((327.27 g/mol)/(0.002 g))^-1 --> (6.1112 × 10^-6 moles) * (6.022 x 10^23) = 3.6801 × 10^18 molecules of naloxone

So, in each pill there are 6.62185822 × 10^18 more molecules of buprenorphine than naloxone. (This is the comparison to be used because mass/weight really has nothing to do with it). But ahhhhh! This is only 2.8 times more bupe (2.8:1) than naloxone! The ratio this way is less than with mass (which is 4:1). This is interesting although it doesn't really mean much without knowing precise details about each drugs reactivity with the different receptors.

What do you guys think? Surely the chemists and drug designers thought about this when they made the pill; I wonder what the implications are...
 
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johnbeatingopioids

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Joined: 14 Jun 2010
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I would like to ask. I too seem to exhibit measurable irritability very soon after dosin. Now I read a post about naloxone in some people isn!t eliminated by first pass metabolism but makes its way into the brain and aspinal chord deminishing buprenprphic effect. I always felt the effects of any pill in a quarter of the normal time of onset of efficacy. Like i metabolize very quickly. I am on Lamictal I don!t know if that effects me or nor or if I am one of those unlucky few that the naloxone gives problems. P.S. I will continue to take my Sub. Otherwise I would be jailed or dead. I need advice please. Also. Can suboxone cause swollen throat and sore throat cause i am suffering that as well as severe headaches anxiety and insomnia. My dr. Gave me clonazepam but it doesnt help.
 
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hatmaker510

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Joined: 29 Apr 2009
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Hi john and welcome to the forum,

As it sounds like you've read, a small number of people have trouble with the naloxone. They usually spit out what's left of the dissolved pill (after the appropriate amount of time) instead of swallowing. This can help reduce headaches. I also take Lamictal and don't have any problems taking it with the suboxone. As for the swollen and sore throat, I doubt it's related to the suboxone. Perhaps you have a virus or infection?

Personally I don't have any problems sleeping (that I didn't have before starting sub), but nor does it make me terribly sleepy. But people report both side effects. When do you take your sub? Maybe you can adjust your schedule or even lower your dose to lower some of the side effects.

Good luck and keep us posted.
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