Naloxone...

[blase deviant]

...okay, this isn't an advanced Q, but no one in OD knows, and I can't find it on pubmed so... (sorry)

What's the threshold dose for oral naloxone, where it begins to become an active opiate antagonist?

 

[BilZ0r]

Well that depends, the higher to dose of opioids, the lower the dose of antagonist you need to get to get a noticable antagonism.

But the question doesn't make sense. If you ate like 100 molecules of naloxone, you'd likely block an opioid receptor or two... You know what Im saying? You can some effect with a minute dose.

 

[hussness]

Isn't oral naloxone not active on the CNS? I thought I remember reading somewhere that it's administered orally to combat opiate induced constipation.

 

[BilZ0r]

Naloxone is orally active. And Naloxone permiates to the brain.

 

[blase deviant]

So like, what's a threshold dose for a dude with no tolerance taking 16mg of naloxone, or twelve, I forget... with a buzz equal to about 25-30mg OC...

And no, I'm not on bupe and the naloxone isn't in the bupe, if you're wondering.

 

[BilZ0r]

huh? You can't get a buzz equal to 25mg of OC with naloxone.

What are you trying to achieve with the naloxone?

 

[blase deviant]

Nothing, I'm trying to see if I can get high on pills orally that have them...

They're 8/100 naloxone/tilidine... I'd probably take 4 since I have no tolerance?

 

[Hater]

if this shit is similar to naltrexone (an opiate receptor antagonist) theres no way u can possibly get high off it further more if u like ur opiates and take some they wont even work while your on it when your prescribed it u have to carry a little card around in your wallet so if u get hit by a bus or something they wont give you morphine because it wont work this is what is says on the card:

In an emergancy situation requring pain relief in patients receiving doses of reVia (naltrexone hydrochloride) a suggested plan of management is regional analgesia, concious sedation with a benzodiazepine, use of non-opiate analgesics or general anaesthesia

i have to ask for the sake of it do u know what the word antagonist means?

 

[jasoncrest]

if this shit is similar to naltrexone (an opiate receptor antagonist) theres no way u can possibly get high off it further more if u like ur opiates and take some they wont even work while your on it when your prescribed it u have to carry a little card around in your wallet so if u get hit by a bus or something they wont give you morphine because it wont work this is what is says on the card:

In an emergancy situation requring pain relief in patients receiving doses of reVia (naltrexone hydrochloride) a suggested plan of management is regional analgesia, concious sedation with a benzodiazepine, use of non-opiate analgesics or general anaesthesia

i have to ask for the sake of it do u know what the word antagonist means?

An opiate antagonist puts in withdrawal someone addicted to an Opioid.
But I think that with no tolerance, you can really get high with pills containing Naloxone (or Naltrexone) + an Opioid.

 

[Hater]

u think haha i'd like to prove you wrong but it would be a waste of money can somebody who actually knows what their talking about answer this question

can u still get high off opiates while using an opiate antagonist?

from my understanding of the word "antagonist" i believe not but i dont really know what im talking about considering my knowledge or lack thereof of neurochemistry

 

[Hater]

Off Erowid:
Naltrexone is an opiate antagonist used in the treatment of opiate and alcohol addiction. It blocks the effects of opiates so that if a user chooses to take an opiate after taking naltrexone, they do not experience much (any) effect. This helps improve abstinence in those who can maintain taking the daily dose of naltrexone.

case closed

EDIT: narcan (naloxone) does the same thing as naltrexone

 

[BilZ0r]

Yeah, you can not get high on these pills man. As you said, they are antagonists... not agonists. If you are high on opioids, and you take these pills, they will bring you back down.

 

[Hater]

im confused why would u combine an antagonist (partial or not) with an agonist with the purpose of getting high how can you get high off an antagonist (partial or not)

oh and if one were to overdose on an opiate would an antagonist reverse the effect (i dont use opiates apart from the rare codiene extraction so im not planning on doing anything stupid but i have friends who would)

i might explain at this point that the reason i have naltrexone is for alcohol dependancy it has a very interesting effect on alcohol consumption ie you feel a lot more alert and when u start getting drunk u feel the tiniest bit of nausea which makes you not want to drink anymore (not that its ever stopped me)

 

[blahblahblahblah]

if one were to overdose on an opiate would an antagonist reverse the effect

Most definetly, time is of the essense. Once the brain stops receiving oxygen, the more likely you are going to be in a coma. Sometimes multiple doses of an antagonist is needed to achieve the desired effect of keeping one alive.

im confused why would u combine an antagonist (partial or not) with an agonist with the purpose of getting high how can you get high off an antagonist (partial or not)

Some people can get high off of weak'ish strange opiates. Buprenorphine perfect example as it seems to have quite the abuse potential to some.

that the reason i have naltrexone is for alcohol dependancy it has a very interesting effect on alcohol consumption ie you feel a lot more alert and when u start getting drunk u feel the tiniest bit of nausea which makes you not want to drink anymore (not that its ever stopped me)

So they have you on Revia [Naltrexone] as it is not aversive therapy [when compared to Antabuse]. Still I could not stomach drinking on Naltrexone, I was sick as a dog after a beer. Have you looked into Antabuse [disulfiram] I know its a bit more of a deterrent physically and might help cutting back. Which brings me to another question. Is Disulfiram a opiate antagonist or does it just act as one?

 

[blase deviant]

1. Why would I get high on these pills?

They were cheap (guess this is why), and I'd never done them.

2. The Hater? I thought naloxone was destroyed orally, and just put in to keep people from IVing the pills, I've heard this many times. I guess not enough is. I wanted to make sure, and I guess it's good I did.

3. Bilzor? Thanks man.

 

[blahblahblahblah]

Did you try them I am curious about Tilidine as I have not tried it.

I dont know if you will be able to acheive a significant high but maybe a low-key buzz. I am pretty unfamiliar with Tilidine/Naloxone from what I understand its more of a time release formula. The opiate antagonist naloxone, which is added as a part of the industrially produced preparation Valoron N solution to minimise oral abuse* You can take the pills as long as you are not taking a opiate agonist [oxycodone, heroin, fentanyl] as that could trigger w/d. What exactly are these pills used for I am curious as its a rather odd/high ratio combination*. These pills should not throw you into w/d if taken by themself with no other opiates in your system, there might be a plateau where the Naloxone will be active orally but 1-2 pills will surely not trigger any negative response? Why would the pills be made?

Obviously its an inferior drug used mainly in Germany:
For moderate pain, a combination of non-opioid analgesics and opioid analgesics with moderate pain relief properties (e.g. oxycodone, codeine, tramadol and tilidine/naloxone) is recommended link.

I would give these a shot if your system is clean 100mg of Tilidine might conjure up a warm feeling. Snorting might be the route to take, slowly. As the bioavailability of Tilidine is a whopping 6% orally. I am not about to attempt to search for the availability when snorted as the info is sparce. I believe the coating can be altered to achieve a quicker release. I have snorted 8mg of Naloxone and had no ill-effects what so ever. I see you dug up an old post in OD concerning Tilidine. The OP said he gets diminishing returns at the ?12-18mg? Naloxone mark, I forget.

I would say go for it and snort some as a 6% oral bio-aval. route is nuts as its drastically cut by first pass metabolism. You shouldnt have any issues if you snorted 50mgs of Tilidine as thats just 4mg of Naloxone nasally [which will have no effect IME]. I am curious as how you stumbled on these pills and what they were scripted for? Do you know?

I spent the better part of a couple hours trying to figure out this drug. As it seems pretty worthless. Although its recomended for stage 2 pain, so there is some abuse potential and I think that lies in nasal administration.

Take one for the team? See what a Tilidine buzz is all about? You are not getting into dangerous waters with nasal absorbsion of Naloxone around 6-8mg but I am one to test the waters, you might not be.

My conclusion Tilidine is much like a tramadol like drug that can produce a buzz if gone about it in the right manner, in non-tolerent opiate ppl.

And for the record: Naloxone has a very low bioavailability of about 3% link

Thats my 2 cents...

 

[rnd.id.]

Tildin/Naloxone 100mg/8mg is definitely active orally. The naloxone is more ore less inactive orally up to a threshold which is supposed to be about 24-32mg IIRC [*]. The naloxone is in it to prevent parenteral and very high-dose oral application.

I'd probably take 4 since I have no tolerance?

Don't do this. If you want to take this drug, IMO one is plenty without tolerance.

I would say go for it and snort some as a 6% oral bio-aval. route is nuts as its drastically cut by first pass metabolism.

I think snorting would be a bad idea. First, the 6% figure probably refers to what is left after the first-pass metabolism to Nortilidin, which is the substance which is actually active (well, I don't know if Tilidin itself is totally inactive). Second, this will probably prevent the inactivation of the naloxone.

Other partial agonists are: ... Tilidine [when combined with Naloxone but plain tilidine is not, i.e. [Valoron]

I don't quite get what you are saying, but Tilidin is a full agonist (AFAIK), and adding naloxone doesn't turn it into a partial agonist.

Also, I don't find Tilidine an "inferior drug" at all. It gave me strong euphoria and I have heard of quite a few people who are addicted to it - don't underestimate it, please be careful. But I have never tried H or other strong opioids, so I can't compare.


[*]: Don't take my word on this if you are opioid-dependant, as any naloxone which gets through could cause withdrawals . I have never tried more than one or maybe two tablets at once, myself.

 

[dayobUK]

u think haha i'd like to prove you wrong but it would be a waste of money can somebody who actually knows what their talking about answer this question

can u still get high off opiates while using an opiate antagonist?

from my understanding of the word "antagonist" i believe not but i dont really know what im talking about considering my knowledge or lack thereof of neurochemistry

i had a 16 year heroin addiction which i beat using subutex and then naltrexone(which i believe is the same as naloxone)i remember people without opiate addiction trying the naltrexone in high dose,it didn't give them any high,as that is not what its meant for.only thing your going to achieve is overdose if taken in really high doses.and the anwser to your question.you can not get high one bit off of opiates while your on naltrexone and drugs similar to.your system has to be clear of it for a minimum of 12 hours for opiates to have any effect at all.now subutex is a different story all together.

 

[blahblahblahblah]

I think snorting would be a bad idea. First, the 6% figure probably refers to what is left after the first-pass metabolism to Nortilidin, which is the substance which is actually active (well, I don't know if Tilidin itself is totally inactive). Second, this will probably prevent the inactivation of the naloxone.

It would increase the activation of naloxone, but when dealing with a substance with a 6% oral bio avail. It makes sense to me that most likely that would increase when insufflated.

I don't quite get what you are saying, but Tilidin is a full agonist (AFAIK), and adding naloxone doesn't turn it into a partial agonist.

Tilidine is and agonist but when you add naloxone into the tablet an pure antagonist you have a partial/mixed agonist/antagonist. It might not be a partial agonist in the true definition of the word but it is definetly a mixed agonist/antagonist. Tilidine is an agonist when in pure form such as with Valoron drops/caps link.

Also, I don't find Tilidine an "inferior drug" at all. It gave me strong euphoria and I have heard of quite a few people who are addicted to it - don't underestimate it, please be careful. But I have never tried H or other strong opioids, so I can't compare.

I was speaking on its strength compared to other opiates. In a double blind study tramadol drops were picked as a better 'analgesic' over Tilidine drops [w/ out the Naloxone]. It is commonly used for stage 2 pain [tramadol, hydrocodone, etc]. I suppose inferior was not the best choice in words. I was not underestimating it, I was actually encouraging the OP to give it a try as it looks like it has potential. It seemed people were telling him not to try it. It seems perfectly safe to me in 1-2 tablets oral or 50mg snorted and was affirmed with this old post:
link

naltrexone(which i believe is the same as naloxone)

Different drug, similar properties. Naltrexone pills/implants are usually given to opiate addicts that have been clean for awhile so that if they do use there use will be blocked and it is worthless attempt. Its so easy not to take a pill so thats when they came out with the Naltrexone implant so you cant skip a dose and get high.

you can not get high one bit off of opiates while your on naltrexone and drugs similar to.your system has to be clear of it for a minimum of 12 hours for opiates to have any effect at all

Untrue, with Naltrexone a long lasting orally active antagonist you will have trouble getting high off anything. With Naloxone [a whole different story] you can get high off other opiates as it is so short acting. See my post above concerning methadone patient being administered Narcan/Naloxone, the naloxone will wear off and the high from methadone will still be present. Thats why its common in methadone OD's for the patient to have multiple infusions of naloxone in order to clear out the receptors completely. Also according to the Buprenophine Bible 'Treatment Improvement Protocol (TIP) Series 40' that Buprenorphine binds to the mu receptors so strongly that it is not dislodged even by Naloxone injections. OD'ing on bupe while extremely hard is also extremly hard to reverse because of buprenorphines high affinity to the opiate receptor sites.

Also, a substantial percentage of individuals currently abusing heroin or other opiates do not show any evidence of withdrawal when challenged with naloxone. Between 34 and 61 percent of patients applying for methadone maintenance may have minimal or no response to intravenous or intramuscular naloxone in doses ranging from 0.2-1.2 mg. link

So yes it is possible to get high [off other drugs ] with Naloxone. In my personal experience one time I OD'd got a shot of naloxone and was shooting heroin again but 1-2 hrs later and getting high. While this might be a play on semantics it is possible disregarding Naltrexone, even though I have had friends that have shot dope on Naltrexone and gotten sick and continued shooting dope and broke thru past the blocking effects and gotten the sickness to subdue and a mellow buzz to occur, dangerous extemely. Would I try that? Fuck no.

Blase:

Have you tried the pills yet? I am curious as to what you get off 1-2 pills orally or 50mg tilidine/4mg Naloxone insufflated.

 

[RandomClean3]

It would increase the activation of naloxone, but when dealing with a substance with a 6% oral bio avail. It makes sense to me that most likely that would increase when insufflated.



Tilidine is and agonist but when you add naloxone into the tablet an pure antagonist you have a partial/mixed agonist/antagonist. It might not be a partial agonist in the true definition of the word but it is definetly a mixed agonist/antagonist. Tilidine is an agonist when in pure form such as with Valoron drops/caps link.



I was speaking on its strength compared to other opiates. In a double blind study tramadol drops were picked as a better 'analgesic' over Tilidine drops [w/ out the Naloxone]. It is commonly used for stage 2 pain [tramadol, hydrocodone, etc]. I suppose inferior was not the best choice in words. I was not underestimating it, I was actually encouraging the OP to give it a try as it looks like it has potential. It seemed people were telling him not to try it. It seems perfectly safe to me in 1-2 tablets oral or 50mg snorted and was affirmed with this old post:
link


Different drug, similar properties. Naltrexone pills/implants are usually given to opiate addicts that have been clean for awhile so that if they do use there use will be blocked and it is worthless attempt. Its so easy not to take a pill so thats when they came out with the Naltrexone implant so you cant skip a dose and get high.



Untrue, with Naltrexone a long lasting orally active antagonist you will have trouble getting high off anything. With Naloxone [a whole different story] you can get high off other opiates as it is so short acting. See my post above concerning methadone patient being administered Narcan/Naloxone, the naloxone will wear off and the high from methadone will still be present. Thats why its common in methadone OD's for the patient to have multiple infusions of naloxone in order to clear out the receptors completely. Also according to the Buprenophine Bible 'Treatment Improvement Protocol (TIP) Series 40' that Buprenorphine binds to the mu receptors so strongly that it is not dislodged even by Naloxone injections. OD'ing on bupe while extremely hard is also extremly hard to reverse because of buprenorphines high affinity to the opiate receptor sites.

Also, a substantial percentage of individuals currently abusing heroin or other opiates do not show any evidence of withdrawal when challenged with naloxone. Between 34 and 61 percent of patients applying for methadone maintenance may have minimal or no response to intravenous or intramuscular naloxone in doses ranging from 0.2-1.2 mg. link

So yes it is possible to get high [off other drugs ] with Naloxone. In my personal experience one time I OD'd got a shot of naloxone and was shooting heroin again but 1-2 hrs later and getting high. While this might be a play on semantics it is possible disregarding Naltrexone, even though I have had friends that have shot dope on Naltrexone and gotten sick and continued shooting dope and broke thru past the blocking effects and gotten the sickness to subdue and a mellow buzz to occur, dangerous extemely. Would I try that? Fuck no.

Blase:

Have you tried the pills yet? I am curious as to what you get off 1-2 pills orally or 50mg tilidine/4mg Naloxone insufflated.

So this is 17 years old, but fuck it lol. The bioavailability, that's for the pro-drug, when you consider that oral availability is almost 100%. This thread is all you find when looking for tildine, isn't that surprising lol...