Opioids SURVEY ON BUPRENORpHINES BEST ANALGESIC DOSE

[CfZrx]

A study reported this "Opiate agonist effects appear with up to 1 mg sublingually and doses of more than 1 mg have predominant antagonist activity; therefore, the agonist/antagonist effects are a linear
function of dose. Sublingual buprenorphine produces typical dose-related opiate agonist effects, which are limited by this ceiling effect and maximal at 8 to 16 mg.



Sounds contradictory. What dose do you think is best? I found relief at .5 mg 4X/day, and I found maybe a bit more relief at 2mg 4X/day. I truly wonder if 32 mg might even be better. There's many online who claim that low dose is best, but how many of them have experimented with high dose Sub, like 32...or shit, even 64. There was some study I read that said although the euphoria and respiratory effects have a ceiling, the analgesia does not. However, then why the heck are the buprenorphine patches for severe pain in just a few mg at the most per day size!?

So much confusion on this topic, and I think ewe need some experimenters to try high dose to see if it is better imho.

 

[Prescottdave]

I found the analgesic effects level off after you reach the 4 mg mark. Given the drug produces both agonist and at higher doses antagonistic effects I would go with the lower doses for daily pain control.

The research is extremely clear on the fact that bupe has a ceiling at 32 mg. In my state Medicaid will now not cover more then 24 mg per day.

They switched to this dose because they had a significant amount of evidence to clearly show there was no point in going above 24 mg. I found doses above 9 mg do nothing for both pain control or keeping WD's at bay. I used to take 16 mg but stopped due to serious side effects.

 

[CfZrx]

I found the analgesic effects level off after you reach the 4 mg mark. Given the drug produces both agonist and at higher doses antagonistic effects I would go with the lower doses for daily pain control. I found doses above 6-8 mg do nothing for both pain control or keeping WD's at bay. I used to take 16 mg but stopped due to serious side effects.

interesting PD!
For me it is hard to accurately assess bupes powers because I take gabapentin, which itself is super powerful. I agree that at 4 mg it is a force to be reckoned with. I'm still so curious. Why did the higher doses not help for WDs??! So it is just a better agonist in every way under 8mg? I will say thc helps.

 

[Prescottdave]

Higher doses helped with WD but doses of 4-8 mg helped almost just as much. These lower doses caused far less side effects while producing more euphoria.

 

[Sertürner]

I found that 2mg IV bupe was the perfect dose for pain relief, and it had an antidepressant effect for me that made me feel okay about life. Anything above that and it started to feel very dirty and unpleasant. 1mg IV was ok as well but I would still have minor WDs

 

[CfZrx]

I found that 2mg IV bupe was the perfect dose for pain relief, and it had an antidepressant effect for me that made me feel okay about life. Anything above that and it started to feel very dirty and unpleasant. 1mg IV was ok as well but I would still have minor WDs

Higher doses helped with WD but doses of 4-8 mg helped almost just as much. These lower doses caused far less side effects while producing more euphoria.

The trick to bupe analgesia is dose low until the evening then take more. I do 1 mg sublingual in the am, 1 mg at lunch, .5 mg at 2pm, .5 mg at 4 pm, 2 mg @ 7pm. Anyone else use this type of strategy??

 

[Prescottdave]

The trick to bupe analgesia is dose low until the evening then take more. I do 1 mg sublingual in the am, 1 mg at lunch, .5 mg at 2pm, .5 mg at 4 pm, 2 mg @ 7pm. Anyone else use this type of strategy??

I specifically do not take a dose past 4pm. The side effects keep me up and cause stomach issues. For me I find dosing in the am and then again at 3pm works the best.

I stick to a strict schedule and feel much better. Bupe reduces my appetite, causes sleep disturbances and constipation.

Dosing before 3 pm insures my ability to minimize the side effects while controlling my pain for most of the day. Been following his method for 15 years.

 

[G_Chem]

So the first time I tried Suboxone was a full 8mg after a solid 1month opiate break. Didn't feel anything for 3hours so decided to call it a night and fall asleep, woke up 14hours later dizzy as fuck with my phone ringing off the hook froma pissed off boss. Zero euphoria or feel good effect and initially gave me a very bad impression of the drug.

Didn't use it for a long time until of course that day came where my heroin stash had run dry, I was at work and decided to give it another try with just the tiniest amount off those old 8mg hexs insufflated. At exactly one hour I felt a wave of relief wash over me and from there the rest is history...

I don't think I'd ever had quit heroin if I had tried to use suboxone at the recommended doses. And mind you even at my highest heroin tolerance dropping at least 100-200$ a day IV, I still only need 1mg a day.

I've been on suboxone about 10yrs now and have settled around 1mg after going up to 6mg at one point. Less is definitely more.

I had friends who were prescribed and would dose 32mg. My buddy looked so faded when he would but he said it wasn't that great still, more physical than euphoric.

-GC

 

[apocalypse_when]

A study reported this "Opiate agonist effects appear with up to 1 mg sublingually and doses of more than 1 mg have predominant antagonist activity; therefore, the agonist/antagonist effects are a linear
function of dose. Sublingual buprenorphine produces typical dose-related opiate agonist effects, which are limited by this ceiling effect and maximal at 8 to 16 mg.



Sounds contradictory. What dose do you think is best? I found relief at .5 mg 4X/day, and I found maybe a bit more relief at 2mg 4X/day. I truly wonder if 32 mg might even be better. There's many online who claim that low dose is best, but how many of them have experimented with high dose Sub, like 32...or shit, even 64. There was some study I read that said although the euphoria and respiratory effects have a ceiling, the analgesia does not. However, then why the heck are the buprenorphine patches for severe pain in just a few mg at the most per day size!?

So much confusion on this topic, and I think ewe need some experimenters to try high dose to see if it is better imho.

Temgesic sublingual tabs come in 200mcg strength IIRC and the dose on the box usually says 1-2 tabs or 200-400mcg. Based off that i would dsy maximum analgesic action is around the 0.5mg ballpark (although this is for non tollerant individuals)

 

[CfZrx]

I specifically do not take a dose past 4pm. The side effects keep me up and cause stomach issues. For me I find dosing in the am and then again at 3pm works the best.

Interesting! I too have tried doing my last dose at 4:30pm, but felt wide awake at midnight until I put .5 mg under my tongue, and felt tired instantly when it kicked in BTW has it rotted your teeth?

I don't think I'd ever had quit heroin if I had tried to use suboxone at the recommended doses. And mind you even at my highest heroin tolerance dropping at least 100-200$ a day IV, I still only need 1mg a day.

I've been on suboxone about 10yrs now and have settled around 1mg after going up to 6mg at one point. Less is definitely more.

I had friends who were prescribed and would dose 32mg. My buddy looked so faded when he would but he said it wasn't that great still, more physical than euphoric.

-GC

Hi GC, I am still not sure which dose is best for pain, but I'll be damned if I can actually get anything more than .5 mg to dissolve properly without a bunch of saliva fucking it up So 2morrow, I'll go back to .5 mg doses through the day until 2mg at 5pm, and .5 right before bed Hope to stick around 4mg total eventually this month, but prob closer to 6 for a few days while I shake this insufflation trap. ---p.s. I know what you mean about the high doses making the person look FUCKED UP, but subjectively they aren't ecstatic.

Temgesic sublingual tabs come in 200mcg strength IIRC and the dose on the box usually says 1-2 tabs or 200-400mcg. Based off that i would dsy maximum analgesic action is around the 0.5mg ballpark (although this is for non tollerant individuals)

I would have to agree that at .5mg my pain is covered. Higher doses do provide a certain sedated euphoria that is nice. Sometimes it's hard to tell the difference between Sub high and Cannabis high,lol.

 

[Prescottdave]

Suboxone has not rotted my teeth.

 

[CfZrx]

Suboxone has not rotted my teeth.

great news!! Today I did my stretches and took .5 mg.

 

[OpiumKing]

I guess I'm the odd ball, cause the higher the dose the better ANALGESIC effect I get, and I've been on Subutex for 3 years. I start off with 8 mg, and go up to 32 mg in about 12 hours when I'm in serious pain, and that takes care of me. Yes I tried the low dose thing to see if it would work for several weeks, and No Go.! So if I'm in serious pain I add 4mg every hour or so.

 

[CfZrx]

I guess I'm the odd ball, cause the higher the dose the better ANALGESIC effect I get, and I've been on Subutex for 3 years. I start off with 8 mg, and go up to 32 mg in about 12 hours when I'm in serious pain, and that takes care of me. Yes I tried the low dose thing to see if it would work for several weeks, and No Go.! So if I'm in serious pain I add 4mg every hour or so.

Thanks Your Highness! At some point I hope to figure this out. Today about 3 mg total, all in .5 mg dose, prob dose a couple mg for bedtime, maybe just another .5 actually on second thought...I always waste so much when I go over .5. Don't you, especially when you dose 8 MILLIGRAMS OR MORE AT ONCE!!!???

 

[CfZrx]

I seem to be settling down at 4 or 5 mg daily. It covers my pain equally as did methadone. It is still so important to not let web-surfing or film watching keep me away from the floor for stretches as the night progresses towards bedtime. Where's the Pain Posse tonight? What dose are you at? I'm grateful that I stopped insufflating my liquid bupe mixture. Too much highs n lows, intact, sublingual is a better ROA all things considered.

 

[adder]

A study reported this "Opiate agonist effects appear with up to 1 mg sublingually and doses of more than 1 mg have predominant antagonist activity; therefore, the agonist/antagonist effects are a linear
function of dose. Sublingual buprenorphine produces typical dose-related opiate agonist effects, which are limited by this ceiling effect and maximal at 8 to 16 mg.

What is it supposed to mean that above 1 mg buprenorphine have predominant antagonist activity? Is it meant that KOP antagonistic effects start to dominate over partial MOP agonistic effects? Or does its mode of binding at MOP receptors change above some level from agonistic to antagonistic? I don't think it does, it just has a ceiling dose and the dose-response curve flattens which is typical of a partial agonist. In my opinion the term "mixed agonist/antagonist" is very misleading, it's used for opioids like buprenorphine, butorphanol, nalbuphine etc. which have different pharmacodynamics. It seems as though "mixed agonist/antagonist" is sometimes used to denote a partial agonist that administered over a full agonist will behave as if it was an antagonist, i.e. decrease opioidergic neurotransmission, but administered over another partial agonist can either substitute for it or cause withdrawal, and sometimes it's used to denote an opioid which is predominantly an agonist at MOP or KOP and predominantly an antagonist at KOP or MOP. In short, it's an old and very mixed up term which without additional information may be confusing.

 

[CfZrx]

What is it supposed to mean that above 1 mg buprenorphine have predominant antagonist activity? Is it meant that KOP antagonistic effects start to dominate over partial MOP agonistic effects? Or does its mode of binding at MOP receptors change above some level from agonistic to antagonistic? I don't think it does, it just has a ceiling dose and the dose-response curve flattens which is typical of a partial agonist. In my opinion the term "mixed agonist/antagonist" is very misleading, it's used for opioids like buprenorphine, butorphanol, nalbuphine etc. which have different pharmacodynamics. It seems as though "mixed agonist/antagonist" is sometimes used to denote a partial agonist that administered over a full agonist will behave as if it was an antagonist, i.e. decrease opioidergic neurotransmission, but administered over another partial agonist can either substitute for it or cause withdrawal, and sometimes it's used to denote an opioid which is predominantly an agonist at MOP or KOP and predominantly an antagonist at KOP or MOP. In short, it's an old and very mixed up term which without additional information may be confusing.

Idk. It looks like a misprint, because I took 6mg today and it had great analgesia. I'm still uncertain that small doses are better. However, I better think about continuing to try for 4mg and under because i will have more pills. However, other than hoarding, I see no reason to stockpile these. Well, maybe for a crisis natural disaster? One nice thing about the higher doses is that it is undeniably more sedating. With thc it is simply a miracle drug, with much of the analgesia of any powerful opioid, but with much better mood effects it seems. I am getting stuff done and noticed that when something falls, I can grab it out of mid-air! Like Mr. Miogi. Is that the Sub?? Lol g'nite BL

 

[CfZrx]

Yesterday took 2mg 3X at even intervals 8am/12/4pm and 1mg at 9pm and got good analgesia/stable buzz. Today took .5mg doses in the AM hours, basically 1.5mg by 2pm, then took 4MG ALL AT ONCE at 4pm. Crashed hard by 7. I guess all the random doses don't do the trick! The fucked thing is that actually internal is the best method, but I am trying hard to just use it as intended. Anyone else out there messing around with their sub dose for pain/maintenance?

 

[G_Chem]

Dude I feel you 100%, I too started using bupe up the nose back when they had the sublingual 8mg tablets that tasted horrid! To be fair they were absolutely shit for sublingual admin anyways because they'd create a lot of saliva which is detrimental to a bupe buzz via sublingual.

Once they switched over to the strips I tried snorting those for awhile and while it did work it was too time consuming and hard to do in certain situations so I gradually switched to sublingual and once I did I realized it truly is superior.

It sounds like your doing some experimentation, well as someone that's been doing that very thing for 10yrs let me lay out what I've found works best.

Biggest rule! Dose with as dry of a mouth as possible, and do no eat or drink for 1 to 1 1/2hrs after dosing. The best time is while your still sleeping or right when you get up as it will just sit there in a dry mouth unmoved giving it time to absorb. If you smoke cannabis, take it after you smoke and have a dry mouth. The goal is to maximize time it's sitting there.

This is so important, if I dose and forget then drink or eat something 30min later it strongly negates the effect and I'll go into wd after awhile.

Next is when you dose and how often you dose. I've tried everything from once a day to many times a day. Once and twice a day I found too up and down for me. Four times a day worked but I felt it was a bit too much, whereas 3 times a day feels perfect.

Here's how I dose these days, for the most part this has been my regimen for the past 4-5yrs.

1am: .25mg
8-9am: .5mg
1-4pm: .25mg

Its good to have the bulk of your dosage being in the morning/day as bupe can be energizing and having lower levels in your system at night.

Besides that, i can't say for pain but I just found overall I just enjoy life more on the lower dosage. It takes work to get there but once your there it feels good.

As your pain mgmt I'd suggest only dropping to 2-4mg depending.. Getting down to 1mg you definitely start to loose the analgesic effect but the euphoric stimulating aspect gets better once you adjust.

-GC

 

[CfZrx]

As your pain mgmt I'd suggest only dropping to 2-4mg depending.. Getting down to 1mg you definitely start to loose the analgesic effect but the euphoric stimulating aspect gets better once you adjust.

-GC

Thanks so much for that! And the rest of the post, it was all really helpful I think a good long term goal would be to get to 2.5mg/day. Today I snorted my liquid bupe mixture and just like you, I realized that for an all day use, sublingual is better. With snorting you can end up dysphoric, which is something I've never come close to while dosing 3 to 6mg/day. Tomorrow I will try to begin a new stable dose. The addict in me keeps saying "take the whole 2mg pill" lol. But I admit that My pain is ok at .5 mg morning dose. It could very well be the gabapentin I take? That shit sure changed the face of pain management. Shit, it beats opiates in a lot of respects for pinched spinal nerves!
ok, let's see if that last 1mg at 7pm keeps me up as I try to go to sleep at 11pm Thanks again GC!!!