Opioids Methadone to OXY EQUIVALENT

[hwbush336]

Levomethadone is superior to methadone in every aspect. Too bad it's only prescribed in Germany. It lacks most of the nasty side effects that methadone has due to the lacking dextro enantiomer, so should be the first choice instead of methadone.

Wat is this levo methadone you speak of

 

[Hexenstahl]

Wat is this levo methadone you speak of

It's basically a twice as potent methadone without its nasty side effects. Half life is 36h instead of 24h and the high feels cleaner and more euphoric.

 

[Señor Moreno]

Methadone is dirt cheap to synthesize and manufacture, yet without my private health insurance, a sealed bottle of Metadol 25mg / 100 tablet bottle of Methadone HCL scored white long tablets are $240 CDN / $200 USD approx….with my Sunlife insurance I pay $40 ….

Its indeed cheap. Have read a study : ""Cost-Analysis of methadone program in Autonomous Community La Rioja, Spain" were they show the cost of treatment in several facilities in said place in 2012 iirc.
It ranged from 285 € and 800 € per patient/ year.
That includes everything from the drug adquisition to transport and dispensation, so the biggest clinics are also the cheapest due to concentration of patients.
The whole cost for the methadone programs in the region (315.000ppl) was 165.759€/ year, but the cost of the methadone itself was only 4% of that, it costed 6.634€ a year.
Patients get it for free, btw.
That's how cheap methadone is
Now if you take the numbers of some USA clinics who charge like 12$/day/patient, you get that a single US patient pays in a month and a half the same money that some of those clinics need to attend all of their patients for a whole year. Its a crime.

 

[Gaz_hmmmm]

Wat is this levo methadone you speak of

Regular methadone is 50/50 levo-methadone and dextro-methadone.

Levo-methadone is a mu opioid receptor agonist, like morphine, oxycodone, fentanyl etc.
It has very little NMDA receptor antagonism unlike dextro-methadone which is a NMDA receptor antagonist and has very little if any mu opioid receptor agonism.
Other NMDA receptor antagonists include DXM, ketamine, PCP and nitrous oxide (N2O / laughing gas).
The dextro-methadone is why methadone is also really good for nerve / neuropathic pain unlike straight mu opioid receptor agonists which often don’t fully help.
It also helps to lower opioid tolerance too and is being developed as a long-acting antidepressant.

The problem is however that dextro-methadone can cause heart QT prolongation above certain doses of methadone (100mg+ or 150mg+) and so in certain European countries they prescribe just the levo-methadone, which is basically methadone but with the dextro-methadone removed.
They do this cause of the QT prolongation risk.
Levo-methadone is twice as potent mg for mg than mixed isomer methadone aka standard methadone.

 

[Gaz_hmmmm]

The OP, if they could get their methadone prescribed 2 - 3x a day to use as a painkiller instead of once a day as maintenance it’d most likely be far better than oxycodone.

Also methadone short-term is around equipotent to morphine in strength but long-term is 6x to 11x as potent as morphine orally from the opioid calculators I’ve seen.

So 162mg methadone would be equivalent to (6x potent) 972mg oral morphine all the way to (11x potent) 1782mg oral morphine.

Oxycodone is apparently 1.5x to 2x as potent as oral morphine so you’d be looking at the lowest being 486mg all the way upto 1188mg.

I doubt any American doc’ is gonna give you that daily.

 

[AlsoTapered]

I've repeatedly been shocked by pain-patients in the US and Canada telling me they are given methadone once a day. In the UK Physeptone (methadone) tablets rather than linctus is used and is taken [BID[ or occasionally [TID[.

It's the fact that the methadone metabolites (normethadone and dinormethadone) still seem to prevent abstinence syndrome but they aren't very active as analgesics.

The UK figure is chronic methadone 30mg equals 80mg OxyContin. But only specialists may prescribe methadone for pain because of it's widely varying time of onset, duration of action and metabolism. In short, it's really only used when everything else has been tried.

 

[Señor Moreno]

Yes, you can dose once a day for maintenance but not for pain, analgesic effects don't last much more than 8 hours if lucky.
And no, doctors aren't very prone to use it for pain management, they would rather cover you in fentanyl patches like a egyptian mummy.

Methadone is very tricky, it's not a linear thing where 40 mg is twice the potency of 20 mg. Doesn't work like that. Being on 30 mg methadone I get pain relief and feel nice, not high, on 90 mg morphine. On 40mg methadone and based on linear charts I should get the same effects from 120 mg morphine, but no fucking way, I need way more to get the same pain relief and I don't feel that warm. Reaching 60mg methadone, morphine becomes next to useless.

 

[AlsoTapered]

As I understand it, when a UK specialist uses Physeptone for pain, initially it is prescribed [TID] but after the methadone accumulates, most patients can be shifted to the same dose [BID]. That's why it IS limited to specialists - they have to closely monitor the dose and frequency to obtain adequate analgesia without sedation becoming an issue.

But I've talked to several BLers in the US or Canada and they were prescribed a single dose daily and when asked actually stated that even on chronic administration, the analgesia didn't last for 24 hours. That's why I asked. At least two received a liquid formulation (the others didn't specify).

 

[Señor Moreno]

No, analgesia doesn't last 24 hours, never did for me not in liquid form nor in waffer
I use it for maintenance, sure had resorted to it as a pain killer hundreds of times, but my pain meds are others. Even for maintenance when you (me) are under 40 mg, it doesn't fully cover you (me) the whole 24 hours if I don't split it in 30mg morning and 10 mg night doses, and when tapering I also split the taper, as if I want to reduce 2mg, I would take 29mg morning and 9mg night.

 

[Hexenstahl]

but they aren't very active as analgesics.

The analgesia can be potentiated with the concomitant application of ultra low dose naltrexone, because it appears that naltrexone binds very strongly to the Filamin A Proteins (instead of binding to the opioid receptors directly which was erroneuously believed for a long time) at nano- to microgram dosages, which is known to modulate the coupling preference of MOR (µ-opioid receptors). This essentially means that ultra low dose naltrexone (ULDN) puts the switch from the excitatory Gs-Protein (the cause of hyperalgesia, many of the nasty side effects and most importantly the development of TOLERANCE) back to the inhibitory Gi/o-Protein (causes analgesic action and is the state that a low tolerance user is in). In other words, Naltrexone, the notorious opioid antagonist actually starts to act pharmacologically as an AGONIST of the µ-opioid receptors when taken in low enough dosages, leading to potentiated analgesia when combined simultaneously with an opioid agonist medication like Oxycodone, Methadone, Morphine or what have you + decreases side effects + reverses tolerance and keeps tolerance to opioid agonists consistently at a low level due to the above described mechanism of action.
I finally understand now why the hell I feel an opioid-like effect when I take my ULDN right before my daily ER morphine tabs at the clinic.

Naltrexone has quite possibly the most fascinating and diverse pharmacological profile out of all chemicals that I personally know of. It's essentially a pharmacological chameleon. It behaves as a normal antagonist like naloxone when taken at therapeutic dosages (50 to 25mg), acts as an immunostimulant drug at LDN doses (anywhere between 500µg up to 4.5mg) with awesome co-effects like increased production of sex hormones like testosterone, endorphin upregulation, antidepressant action, etc. (still antagonizes though, so do NOT take it while you are still physically dependent), and at ULDN doses (anywhere between 1ng up to 100µg; the hormetic zone however seems to be between 1µg and 10µg most of the time, though I know someone who had success with 150ng which is a ridiculously small dose) it acts again completely differently in that it doesn't antagonize MOR at all, and instead starts to behave like a tolerance obliterating/reducing/inhibiting, analgesia potentiating, duration of action prolonging drug when combined with an opioid agonist!!!

This study was an eye opener in that it perfectly explained to me in the most lucid manner the science behind how Naltrexone and ULDN specifically works in the brain:

https://journals.sagepub.com/doi/full/10.4137/CMT.S4870

Everything I explained above in simple language, is described in this paper in more detail.

I wonder to this day why this knowledge hasn't finally made its round in junky circles (it's obvious why it hasn't led to a revolution in pain medicine as it dramatically lowers revenue for pharma companies since their #1 profit driver in the opioid market is tolerance), not only because these studies prove without a doubt its effectiveness, but we also have countless anecdotal evidence in the form of experience reports in various forums (especially reddit). My own experience has confirmed every one of these findings, including the withdrawal obviating effects of ULDN (see this: https://pubmed.ncbi.nlm.nih.gov/16681181/). So much suffering, so much waste of money and so much lack of pleasure can be avoided by simply creating your own ULDN solution and finding the dose that's right for you. My daily morphine habit would be around 600mg if it wasn't for ULDN, but thanks to it I only need 240mg right now to get the same buzz.

Here is the study for those interested in how it affects methadone patients including the analgesic potential: https://www.jpsmjournal.com/article/S0885-3924(03)00139-8/fulltext

"Less than 24 hours after the initiation of oral naltrexone, the patient reported improvement. He had NO SYMPTOMS OF WITHDRAWAL and his PAIN DECREASED from a score of 9/10 the night prior to the initiation of the naltrexone to a 3/10 the morning after. In addition, his CHRONIC NAUSEA RESOLVED. The methadone DOSE WAS DECREASED to 50 mg four times daily and the methylphenidate dose was kept unchanged. His FATIGUE IMPROVED and the pain remained at the same level. One month later the patient remained with the same degree of pain relief, the same dose of methadone after the dose reduction and utilizing 50% of the short-acting opioid for rescues."

So it seems that even if Methadone isn't very active as an analgesic, it can be made to be so by combining it with ULDN, when other opioids are not an option for whatever reason.

If people wanna know how to create ULDN themselves, they can refer to my ULDN thread that I created back in 2022.

 

[AlsoTapered]

No, analgesia doesn't last 24 hours, never did for me not in liquid form nor in waffer
I use it for maintenance, sure had resorted to it as a pain killer hundreds of times, but my pain meds are others. Even for maintenance when you (me) are under 40 mg, it doesn't fully cover you (me) the whole 24 hours if I don't split it in 30mg morning and 10 mg night doses, and when tapering I also split the taper, as if I want to reduce 2mg, I would take 29mg morning and 9mg night.

I'm NOT arguing that it doesn't act as an analgesic for 24 hours - I'm merely stating that it was prescribed for INAPPROPRIATELY for pain to several BLers who PMed me on the issue. The BLers were complaining that it didn't work for 24 hours and asking why.

So I was wondering why doctors would dose inappropriately. Either they REALLY are that ignorant (which is a distinct possibility and why in the UK only specialists in pain management can prescribe methadone as an analgesic) OR the current crackdown on doctors prescribing opioids excludes methadone maintenance.

I make that second suggestion because I know a US lawyer who defends doctors who are prosecuted for the over-prescribing of opioids. They mentioned to me that they use a simple demographic breakdown of a doctors patient-list. If the doctors practice is in an area with a high proportion of elderly people or in a region where hard physical labour makes up a large proportion of jobs, obviously that's 2 groups who are statistically more likely to need opioid analgesia.

But I pose it as a question - why prescribe methadone for pain? Why prescribe it inappropriately?

 

[Señor Moreno]

I'm NOT arguing that it doesn't act as an analgesic for 24 hours - I'm merely stating that it was prescribed for INAPPROPRIATELY for pain to several BLers who PMed me on the issue. The BLers were complaining that it didn't work for 24 hours and asking why.

I totally got you mate, but English is not my language and maybe I used some word that made you think that I took it like you were arguing. Not at all, I just went on explaining my own thing. I am sorry

 

[Señor Moreno]

Methadone isn't a first choice in pain management. The few persons that I knew that were put on it for pain were all cancer patients that didn't respond or didn't tolerate morphine or other stuff.
Also, I think that the fact that the majority of pain patients are suffering nociceptive pain, such as oncologic or traumatic events where morphine&others work well and are well tolerated by patients, doesn't play any role in favour of a wider study/use of opi+ nmda antagonism meds like methadone or even dxm, aswell as other stuff like ketamine or memantine.
It is only a thought of mine, but maybe if another forms of pain, such as nerve related one and/or other idiopatic complex and severe pain were more prevalent, the efforts to treat them would lead to relectures of existing meds possibilities

 

[Juniper Bruhmomentius]

As I take levomethadone I can assure that its much better choice than normal. Basically no side effects + seems to work longer.

 

[AlsoTapered]

Methadone has NMDA activity so it a small number of patients, it provides adequate analgesia where other opioids have failed. But almost every nation has at least one other MOR/NMDA analgesic.

In the US Levo-Dromoran (levorphanol) is the agent. In some European nations Ketogan (ketobemidone) is used, in others Heptazone (phenadoxone) and in the UK Diconal (dipipanone + cyclizine).

That every nation keeps a MOR joint NMDA analgesic on it's books shows that their is clinical utility.

The problem with methadone (even levomethadone) is that the onset, duration of action and elimination half-life very so wildly between individuals. UK figures at least show the bioavailability of oral morphine to be anywhere from 41% to 72% which is HUGE,

So as long as the doctor is carefully monitoring analgesic efficacy against side-effects, methadone IS usable, but it does take more monitoring than most of the alternatives. Of course it is DIRT cheap. until 2017 levomethadone was produced via the partial crystalization of raecemic methadone but now their is a chiral synthesis.

Either way, it's going to cost a lot less than all of those other MOR/NMDA analgesics because they are all prescribed to a small number of people so production will be on a small scale - batch synthesis at pilot-scale, I believe.

 

[PaulAxe]

That's a lot of oxycodone. I don't know much about this topic as I deal mostly with benzos, but one of my family members (not gonna mention who for the person's privacy sake) was on a high dose of SubTex and took a full year to recover from heron addiction. That's why I've only touched heroin once and once I did fentanyl, I overdosed on it and never touched an opioid again.

 

[AlsoTapered]

That's a lot of oxycodone. I don't know much about this topic as I deal mostly with benzos, but one of my family members (not gonna mention who for the person's privacy sake) was on a high dose of SubTex and took a full year to recover from heron addiction. That's why I've only touched heroin once and once I did fentanyl, I overdosed on it and never touched an opioid again.

Absolutely avoid opioids unless their is a clinical need. John Cooper Clark summed it up nicely - 'first it's fun, then it's not, then it's hell'.

That fentanyl seems aimed almost totally at users who are already opioid tolerant seems crazy to me BUT the truth is that 99% of people who try opioids do not go on to become 'addicts' but that 1% represents 99% of the income for dealers.

Now carfentanil is turning up as well as the nitazines - and let me tell you that their are FAR more potent opioids known to science. But thankfully they aren't known to many and nobody is posting much about them. One BLer stumbled on a paper which described an opioid some x180,000 morphine in analgesic activity. But they didn't post the references. I removed an entire thread when I realized that I had just shown lurkers exactly how to make an opioid some x40,000 morphine - I don't want to be associated with the destruction such drugs can produce.

 

[Gaz_hmmmm]

It's the fact that the methadone metabolites (normethadone and dinormethadone) still seem to prevent abstinence syndrome but they aren't very active as analgesics.

Normethadone isn’t a metabolite of methadone.
I thought it was but it’d actually a different opioid and is active itself.

 

[AlsoTapered]

Normethadone isn’t a metabolite of methadone.
I thought it was but it’d actually a different opioid and is active itself.

Current Concepts in Methadone Metabolism and Transport

Methadone is a cornerstone therapy for opioid addiction and a public health strategy for HIV/AIDS and hepatitis C reduction. Methadone is also used for acute and chronic pain. As use for chronic pain has grown, so too have adverse events. Constitutive ...

www.ncbi.nlm.nih.gov

The TECHNICAL term for 'normethadone' is N-desmethyl methadone. Likewise 'dinormethadone' is 'N,N-desmethyl methadone.

That someone chose to name a related but different compound 'normethadone' is simply because it's related to methadone but lacks the alpha-methyl.

Don't rely on Wikipedia as a reliable source of technical information - DO read technical journals and understand the metabolism of methadone.

 

[Gaz_hmmmm]

Current Concepts in Methadone Metabolism and Transport

Methadone is a cornerstone therapy for opioid addiction and a public health strategy for HIV/AIDS and hepatitis C reduction. Methadone is also used for acute and chronic pain. As use for chronic pain has grown, so too have adverse events. Constitutive ...

www.ncbi.nlm.nih.gov

The TECHNICAL term for 'normethadone' is N-desmethyl methadone. Likewise 'dinormethadone' is 'N,N-desmethyl methadone.

That someone chose to name a related but different compound 'normethadone' is simply because it's related to methadone but lacks the alpha-methyl.

Don't rely on Wikipedia as a reliable source of technical information - DO read technical journals and understand the metabolism of methadone.

Thanks for the info.