Opioids If an opiate is blocked by methadone will it still raise your tolerance?

[ohhheyy123]

I'm currently on 70mg of methadone daily and it is my understanding that after a dose is higher than around 50mg, a "blocking" mechanism starts to take place.

If I take another opiate after my dose, are most of every molecule of that second opiate "blocked" from ever reaching my opiate receptors?


And if that is the case then would it be reasonable to assume that your tolerance would be unaffected?


I have also wondered the same thing about Suboxone.


Thanks.

 

[tightlywound]

I don't think you have to worry about the other opioids you may want to get high off of raising your tolerance ...methadone and suboxone (at least suboxone I know, I would assume the same for methadone) in themselves raise your tolerance to crazy levels.

 

[Raysu]

I've learned that yes some opiates like Suboxone, methadone, and loperamide do block your receptors at high doses and due to their long half life prevent the uptake of shorter lived opioids. I wouldn't say they block 100% except maybe at peak plasma levels but until they are well out of your system you won't feel much if anything from dosing too early. Tolerance is something I'm curious about myself or rather cross tolerance of similar drugs. To me methadone and Suboxone and loperamide act very differently than oxycodone, hydrocodone, hydromorphone, and codeine acts differently from all the above but they all are opiates/opioids. Having a high personal tolerance and after much trial and error I've had the best success in breaking up use with clean time and not using opiates for more than a week at a time. So say for example I use dilaudid for a week, loperamide a few doses over the following week then nothing for a week or two. Doing so has kept my tolerance low and at the two week mark lowers it from previous use in fact. I've noticed if I didn't wait almost three days following loperamide that it not only blocked a good bit of the dilaudid but I come out of the gate using almost four times the amount and cannot cut back. This is perplexing because it takes more than a day or so to build up tolerance. If I take the clean time break my tolerance remains low and doesn't even reach the halfway point for doses that were preceded by an opiate. It's as if taking higher doses just for the time that the opiate was blocking them doubled my tolerance. Can anyone shed light on this phenomenon? Feel free to correct my contribution as I am only speaking from personal experience and not research here! What can I say-it's a lazy day!

 

[ohhheyy123]

You're positive that your doubled tolerance isn't just a result of taking a higher dose than usual? Or are you saying it rose significantly because you took the dose while the blocking mechanism was in effect?

In other words, my theory was that if you take an opiate while there's some kind of opiate blocking taking place in your brain (from methadone, bupe or lope), the blocked opiate would not interact with your receptors and therefor not affect your tolerance right?

But you're saying you experienced the opposite of that basically?

 

[ohhheyy123]

Update: I went out and procured 0.5 g of some H.
I've used about 0.1g so far roughly 9 hours after taking my 70mg dose of meth.
While there's certainly a large chunk of the high missing, I do feel a buzz and it's much stronger than I thought it would be on the off chance that I would feel anything...

Now relating my question, if instead the methadone DID completely block all my attempts to get high, would my brain react (e.g. adjust tolerance) as if I never used any extra opiates in the first place? Since they were all blocked and never had a chance to react with my receptors?

 

[Raysu]

I'm wondering if despite attaching to receptors because of blocking a tolerance can still build. Here's the scenario I experienced: the day following regular doses for about a week or better of taking lope my usual dose of dilaudid did nothing so thinking it was a case of higher tolerance not that it was blocked by the long acting lope I waited until the next dose and doubled it...nothing so next dose I quadrupled it, sure that it was a case of tolerance due to mega doses of lope. The next day and doses of dilaudid were quadrupled again still nothing and so I went the remainder of the week to the point where I was thinking I got fake pharm from the pharmacy. I mean how could my usual dose be that off that quick I thought. So I went back to lope another week and felt those effects then took two weeks off and suddenly my usual dose of dilaudid worked again. So I was left thinking either the pills were no good, two weeks off is what it takes to decrease my tolerance, or lope allowed my tolerance to increase while it was blocking and by the time it was done the dose was insufficient. I mean I know tolerance builds fast but I can't explain how I was able to jump around so much in the course of about a month. My meds were the same manufacturer and same source as always. Thoughts?

 

[BigG]

While the blocking action of buprenorphine is well understood due to it being a partial agonist/antagonist not so for methadone (pure mu receptor agonist). There are lots of theories but it's not 100% understood why methadone does this. Also the dose at which methadone blocks other opiates varies and also does the amount of other opiate needed to "break through" this blockade (note trying to break through methadone blockade by taking huge amounts of another opiate is a very easy way to overdose so please don't try).

Personally a few years ago I was on 180mg methadone for pain and when the doctor changed me to fentanyl it took almost a week of being off the methadone before I felt the fentanyl.

Its a really interesting subject when I like hearing other people's experiences ....

 

[Raysu]

It's funny you mention that because when I compare lope to other drugs for me it most closely resembles methadone. In particular the benefit I got from lope initially was waking up the following morning and realizing I'd gone since it had taken effect without the desire to use again, which for me, does not occur with other drugs including Suboxone. For me even mid rush I could be thinking about the next dose so it was odd to suddenly realize hours had gone by since fantasizing about the next one. I had thought methadone would be done blocking by 36 hours but clearly as you say it can go a week. Fascinating to hear how that may be the key to solving my confusion. Thank you for that info! Awesome!

 

[BigG]

It's funny you mention that because when I compare lope to other drugs for me it most closely resembles methadone. In particular the benefit I got from lope initially was waking up the following morning and realizing I'd gone since it had taken effect without the desire to use again, which for me, does not occur with other drugs including Suboxone. For me even mid rush I could be thinking about the next dose so it was odd to suddenly realize hours had gone by since fantasizing about the next one. I had thought methadone would be done blocking by 36 hours but clearly as you say it can go a week. Fascinating to hear how that may be the key to solving my confusion. Thank you for that info! Awesome!

Yeah mate I think it depends a lot on how much methadone you've been on and for how long. For me it was 180mg (60mg three times a day) for about 8 years. Obviously for someone on 60mg for a few weeks it might be different.

I think the sign that something is blocking successfully is as you say when you wake up and realise you're feeling ok and not thinking about immediately having to redose.

 

[manboychef]

suboxone increased my tolerance to epic levels on its own. I only tried using on it a couple times, and it didn't work, even at heroic doses of heroin.

 

[John4444]

People on this thread, Infact almost the whole thread is saying that Methadone has a blocking agent in it to block other opiates. And even mentioning it about other opioids.

As far as I know. And I Know ALOT about these meds. The Absolute ONLY Drug Mentioned in this thread that has ANY Kind of Opiate Blocking with it, is Suboxone. It contains Naloxone & Buprenorphine. The Buprenorphine is the drug that Helps with the Withdrawl from ACTUAL OPIATES (As itself is Not an Opiate) But the "Naloxone" is the drug that is in NARCAN. Paramedics give to Overdosing Heroin Patients to Bring them Back to Life. IT Completely and Immediately Counteracts ANY Opiate in your System... So for instance, if you were taking Methadone for a week, Ran out and Started Snorting 20ea 15mg Oxy's a Day for a few days and then took Suboxone - It would throw you into IMMEDIATE Withdrawls... DETOX CITY... That is why when you start on Suboxone, you doctor actually requires you to be in Actual Withdrawl (From the Opiates you were previously taking) Before they will administer the FIRST Dose IN Office, prior to actually giving you a prescription to have filled at the pharmacy....????

Thoughts??? Oppinions????

John4444
Maricopa County, Az

 

[kleinerkiffer]

People on this thread, Infact almost the whole thread is saying that Methadone has a blocking agent in it to block other opiates. And even mentioning it about other opioids.

As far as I know. And I Know ALOT about these meds. The Absolute ONLY Drug Mentioned in this thread that has ANY Kind of Opiate Blocking with it, is Suboxone. It contains Naloxone & Buprenorphine. The Buprenorphine is the drug that Helps with the Withdrawl from ACTUAL OPIATES (As itself is Not an Opiate) But the "Naloxone" is the drug that is in NARCAN. Paramedics give to Overdosing Heroin Patients to Bring them Back to Life. IT Completely and Immediately Counteracts ANY Opiate in your System... So for instance, if you were taking Methadone for a week, Ran out and Started Snorting 20ea 15mg Oxy's a Day for a few days and then took Suboxone - It would throw you into IMMEDIATE Withdrawls... DETOX CITY... That is why when you start on Suboxone, you doctor actually requires you to be in Actual Withdrawl (From the Opiates you were previously taking) Before they will administer the FIRST Dose IN Office, prior to actually giving you a prescription to have filled at the pharmacy....????

Thoughts??? Oppinions????

John4444
Maricopa County, Az

The Bioavailability of naloxone is negligible and the dose is to small, what throws you into precipitated withdrawal is the buprenorphine itself, because it's a partial agonist

 

[John4444]

Absolutely NOT Questioning you. I know ALOT about these Meds, but I am not above knowing there are others out there that know more than me.

With that said, I completely disagree with this. I would love to have you send me any links that you have or could show to support your claim. Nothing I have read about Buprenorphine has any Opiate Blocking Ability. Infact there is a drug that contains ONLLY The Buprenorphine Alone. My Understanding is that they went on to ADD The Naloxone to the Suboxone To Keep People from being able to Abuse other Opiates while taking Suboxone to GET OFF of the Opiates and deal with the W/D / Detox Side Effects at the same time. ie: the Buprenorphine Dealing with the W/D / Detox (from Opiates) Side Effects and the "Naloxone" to keep you from being able to abuse any other Narcotic (Which by taking the Suboxone) You are trying to get off of anyways...

Good discussion either way, but id like to see documentation of what you claim.

John4444
Maricopa County, Az

 

[kleinerkiffer]

Buprenorphines affinity for the opioid receptor is way higher than say heroin, so if all your receptors are saturated with buprenorphine heroin won't do anything.
Buprenorphine is a partial agonist, that means it won't open the channels as much as a full agonist.

The bioavailability of oral naloxone is more or less 0,because it's metabolized before it reaches your BBB and people are able to shoot suboxone without going into withdrawal, just read through the forum, enough evidence (ssorry, but I have no time to link sources)

 

[kleinerkiffer]

There you have it
https://narcoticdreams.wordpress.com/2010/05/06/suboxone-myth-sublingual-is-the-only-roa/

Contrary to the belief that doctors and some patients hold, Suboxone can in fact be IV’ed/snorted/plugged without going into terrible withdrawals. The commonly held belief is that the naloxone in Suboxone will put you into withdrawals if the medication is snorted or intravenously injected. That isn’t true, plain and simply. However, if one uses a full agonist opioid such as Oxycodone, Hydrocodone, Codeine, Morphine, Methadone etc. and uses Suboxone before they are in withdrawal, or have let the medication leave their system (in the case of the opiate naive) they will be sent directly into what’s called precipitated withdrawal. This will happen no matter what route of administration is used. Precipitated withdrawals are not caused by the naloxone in the pill, but rather the buprenorphineitself. This is because buprenorphine (bupe) has a higher affinity for the opioid receptors in one’s brain than most full agonist opioids. What effectively happens is the bupe shoves it’s way into the receptors throwing the other opioid molecules out. This results in a fast, full-on withdrawal kicking in. I’ve never experienced it myself, but it is hellish, from what I hear. Instead of taking 1-3 days to peak in withdrawal it happens in minutes. Very unpleasant.

However, if you’re on a Suboxone maintenance program it doesn’t matter which ROA you use. The naloxone in the pill is essentially there as a psychological deterrent. I can attest personally that you can snort, shoot or plug and you will not go into any sort of withdrawal as long as you’re stabilized on Suboxone. Some of the other ROAs may be more favorable than because of the higher bioavailability (BA). Sublingually bupe has a BA of approximately 30%. While snorting and plugging have a BA of ~50% and ~70%, respectively.

 

[Raysu]

No I'm not suggesting there is a blocking "agent". If you search methadone blocking it pulls up plenty about a 60mg dose that is high enough to fill receptors and thus reduce cravings at length. Attempting to take anything before those receptors are freed up "blocks" the drug on standby because it cannot be picked up until the space is available. I've known others in mm who use despite and if they don't dump a dose and wait long enough their other DOC is not felt in full. This is what I was trying to describe that perhaps loperamide has the same issue as it has many similarities to methadone for me anyway. Hopefully that makes sense but it's late and I'm spent.

 

[Znegative]

Ok, methadone does not block other opiates, not really, like how buprenorphine and naloxone can. And in an answer to the question posted, yes you can definitely raise your tolerance if you use enough opiates. I know many idiots that have done this, I am one of them. Methadone just saturates your receptors, your basically in a constant state of inebriation, but you get used to it so you don't feel much more then some sedation. Your blood levels at a high enough dosage don't ever decline enough (unless you stop taking your dose for days) that you can 'recognize' a change when you take a different opiate. However if you shoot enough dope, you will feel a rush, especially if you haven't dosed that day, and it's even possible to get sedated. I knew one guy that was on 120mg of methadone and he'd be shooting the same $20 piece of tar as the rest of us and amazingly he was getting more fucked up then we were. I used to think (based on my own experiences on high dosages of methadone) that anyone saying they could nod off heroin while on 'done were lying, but I've seen it plenty of times now with my own eyes.

I've also people just shoot massive amounts of dope, not feel anything but a rush, which they start to chase, and then their methadone becomes less effective and starts wearing off by 2pm.

 

[Raysu]

Ok good that's what I meant but lacked the right term for. Saturated fits better with the mechanism of action I was envisioning. Thanks for that.