Misc Most recreational prescription medications? (Legal in the US)

[Them Witches]

I've never had levorphanol personally but hands down vaporized oxymorphone one was one of the best euphorias I've ever experienced. not a rush like vaporized fentanyl, the bolus isn't large enough but it had legs and felt incredible

Word

 

[4DQSAR]

I've never had levorphanol personally but hands down vaporized oxymorphone one was one of the best euphorias I've ever experienced. not a rush like vaporized fentanyl, the bolus isn't large enough but it had legs and felt incredible

Well, unless you first freebase the oxymorphone, I'm uncertain how much will pyrolize given that the MP of oxymorphone hydrochloride is 248 to 249°C. But I suppose if someone simply exploits the expedient use of 'more' then I suppose it might provide a rush somewhat like injection of the drug (a bad idea on oh so many levels).

But I recall one person whose wife gave him a 40mg Opana as one of his birthday presents. Which was interesting.

Who on earth failed to note that upon parentheral administration, oxymorphone is five times more potent than when consumed orally?

 

[Them Witches]

Equianalgesic ratio of oxymorphone (79.4 mg) to oxycodone (155 mg) was 1:2. That is how I judge narcotics right there. The buzz shit is out the window after years and decades.

 

[Them Witches]

Who on earth failed to note that upon parentheral administration, oxymorphone is five times more potent than when consumed orally?

It's hella Lipid and stays in the liver. and is broken down by it not the kidneys.. After IV dosing for a week for someone highly dependent is every 2hrs. PO is supposed to be linear.

PO 10mg equals 30mme. IV it is 10 times stronger than Morphine.

 

[4DQSAR]

Equianalgesic ratio of oxymorphone (79.4 mg) to oxycodone (155 mg) was 1:2. That is how I judge narcotics right there. The buzz shit is out the window after years and decades.

ORAL bioequivelence.

Now compare oral bioavailability.

 

[Them Witches]

ORAL bioequivelence.

Now compare oral bioavailability.

https://www.sciencedirect.com/science/article/pii/S0885392409011403#:~:text=17%2C%2018%2C%2019%2C%2020,as%20morphine%20after%20intravenous%20administration.&text=Oxymorphone%20is%20more%20lipid%20soluble%20than%20both%20oxycodone%20and%20morphine.

I know plenty of long-term Oxymorphone dependent patients. They would rather have Oxycodone for PO bioavailablity. But take both medications for pain.

Me on the other hand know that doctors think Oxymorphone is so much stronger than Oxycodone for pain PO (oral). So I do not fall for that bull crap, I ask for Oxycodone IR : 4hrs (main daily opioid). Instead of Oxymorphone for breakthru pain during the day & night, I choose Methadone 10mg tablets. Instant release but "sustained release" Methadone works from heavy physical dependence issues that come up and provides better sleep for long-term opioid patients.

An example, when I wake up at 4-5am, my eyes water like a hose and I am sneezing 10 times in a row. I need an extra Roxi in the morning to make it even stop some. Methadone takes 52 minutes flat to work. It keep the Roxi 30mg from dropping below a linear baseline physically. I add the Clonidine to extend this baseline reduction.

Doctor just added the Cyclobenzaprine back in the evening with the Lunesta, Clonidine, and Vistaril PAM. I am perfectly fine keeping my MME right where it is at and using other drugs for relief. The longer the MME stays the same increases the opportunity to medically titrate 20% at once. I haven't increased in two years from 180-210mg Oxycodone HCL and 40mg Methadone. 20% would be another 90-120MME worth of Methadone's "sustained release action" less waking in the morning with water eyes and sneezing. That sounds better than adding 2qty Roxi 30mg.

 

[4DQSAR]

Well, your reference does give a value of just 10% oral bioavailability for oxymorphone.

Oxycodone is actually MORE complex because between 10-19% of any oral dose is converted to oxymorphone via first-pass metabolism.

Oxycodone Therapy and CYP2D6 Genotype - Medical Genetics Summaries - NCBI Bookshelf

I did post a bunch of references for someone else in a thread concerning oxycodone. But this paper cites them all. So while we always knew a certain fraction of any oral dose of oxycodone would be O-demethylated to oxymorphone, it was assumed not to be significant in the analgesic activity until the last decade in which human studies suggested up to half of the analgesia is due to the (far more) active metabolite (oxymorphone). Of course, each study has it's limitations and only provides a weight of evidence but I could never work out how the conclusion that the oxymorphone we always knew was present was considered inactive.

The problem with taking more than two medications is that each one can impact on liver enzyme activity. Methadone will likely reduce N-demethylation of oxycodone and oxymorphone. One would need to find the data for each medication but the truth is, it's impossible to predict as everyone is different.

If that mix works for you, that's fine.

I've noted various people in North America stating that they are prescribed methadone to treat visceral pain... but as one single large dose each day. I always understood that UK specialists prescribe methadone either [BID] or even [TID] to treat pain. My hypothesis is that the DEA has clamped down on the prescribing opioids for visceral pain BUT somehow a loophole exists that means that methadone is sometimes excepted from that ridiculous rule.

I say this because to the best of my knowledge clonazepam was (and still is in most nations) only prescribed to control certain types of epilepsy. But I note that it also seems to be prescribed for anxiety and similar in North America. So again, is this a loophole? The DEA may wish to stop benzodiazepine prescribing for anxiety but stopping epilepsy medication could have severe outcomes so again, are doctors fudging the paperwork?

 

[yubacity]

Lyrica and Adderal and some diazepam

 

[4DQSAR]

Lyrica and Adderal and some diazepam

Well SKF-118s (dexedrine) and diazepam were commonly termed 'the sidewinder'.

I believe older formulations of (meth)amphetamine and older sedative/hypnotics (typically barbiturates) were also mixed for similar results. I don't know if there was ever an official slang term for such combinations.

 

[yubacity]

Well SKF-118s (dexedrine) and diazepam were commonly termed 'the sidewinder'.

I believe older formulations of (meth)amphetamine and older sedative/hypnotics (typically barbiturates) were also mixed for similar results. I don't know if there was ever an official slang term for such combinations.

I love a lyrica buzz but my tolerance so high I like to add some diazepams or temazzies I've never done a barbiurates

 

[Octave77]

Really? I would consider clomethiazole to be the more potent. But then clomethiazole is a hypnotic, not so much an anxiolytic.

A friend once advised me 'never take more than two or you will just wake up six hours later wondering where you are'. But that friend was injecting the liquid from inside the capsules and as they noted 'you have to be quick as it melts plastic'. The dose-response curve appears to be very steep which combined with the fact it produces anteriorgrade amnedia, is a hazard. You forget how many you consumed.

It certainly seems to produce tolerance and dependence much faster than benzodiazepines. It's more like a barbiturate in both the subjective effects and action. I can easily imagine someone taking clomethiazole as a recreational drug only to discover that they have developed physical dependence. Fatal overdoses were not uncommon. Even a small quantity of alcohol makes clomethiazole deadly.

I've talked about clomethiazole elsewhere but I admit to being surprised that it's stil being prescribed as a hypnotic. It's certainly effective, but known to be highly abusable.

I assumed that like barbiturates, clomethiazole has only remained in the BNF because there are some people who were prescribed those medications for years, are now elderly and detoxification is more hazardous that just continuing to prescribe the medication.

It demands the same amount of respect as a barbiturate.

Thank you 4DQSAR for your reaction. Yes I confirm that the equivalence in potency of clomethiazole capsules is the following to me : 1 capsule of 192 mg clomethiazole = 9 mg diazepam, after having tried this medication seven times before going to bed. On patient leaflets the recommended dosage is 1 to 2 capsules or 2 capsules before going to bed. I find this posology too high, as the standard dosage of an hypnotic medication is 10 mg diazepam. Basically the effect of clomethiazole is anxiolytic and relaxant too, but less euphoric than that of benzodiazepines. Having tried phenobarbital a couple times, I guess that the effect of clomethiazole is much more pleasant than that of barbiturates. But is clomethiazole really useful, given that a large choice of benzodiazepines are available on the market ? I don't know. Perhaps there is a historical reason : clomethiazole is marketed since the 1930's. But people who are used to take clomethiazole could just as well switch to a benzodiazepine. Anyway I'm happy to have tried clomethiazole, trying a medication is always interesting.

For 13 years I have occasionnaly tried the following GABA-A downers : 15 benzodiazepines, one barbiturate (phenobarbital), zopiclone, zaleplon, zolpidem, meprobamate, carisoprodol, clomethiazole. Phenobarbital, carisoprodol, zolpidem were strangely unefficient and unpleasant, I've never understood why. All the other medications were very efficient as hypnotics and anxiolytics at the same time. One particular thing : lorazepam is the only benzodiazepine that makes me nauseous, I have no explanation for this neither.

 

[Them Witches]

The problem with taking more than two medications is that each one can impact on liver enzyme activity. Methadone will likely reduce N-demethylation of oxycodone and oxymorphone. One would need to find the data for each medication but the truth is, it's impossible to predict as everyone is different.

PO /=/ The way it works is to take 70% Oxycodone and 30% Methadone. Methadone at 70% and/or 70mg+ will block the Oxycodone at 30% in almost every way.

A) Currently my Oxycodone HCl MME = 315 ]
>>> (A) high mg IR benefits : 4hrs combined with (B) lower mg IR/SR : 8hrs /=/ Linear baseline B/T (A):4hr & constant pain relief climb
B) Currently my Methadone HCl MME = 120 ]

This PO combo is popular with high physically dependent patients mixed with high opioid tolerance.

====================================================================================

I have already tried (it did not work well) :

A) Methadone 70% MME ]
>>> (A) Methadone blocked the effects of (B) Oxycodone
B) Oxycodone 30% MME ]

 

[4DQSAR]

@Octave77 - as I mentioned, it was my experience and the experience of others who consumed clometiazole that the dose-response curve is far steeper than most if not all benzodiazepines. For decades it was quite commonly used for alcohol detoxification because whatever it's precise action, it not only deals with the physical symptoms but also stops the cravings. That it had significant drawbacks was only really addressed in the 1970s but I do know that Addenbrookes had a ward for clomethiazole detoxification. I don't know quite what the outcomes were. Possibly similar to the barbiturates which if you check the BNF, should only be prescribed to people physically dependent ON barbiturates.

@Them Witches - As I concluded, if it works for you, fine. But be aware that those other medications may also interact with the opioids.

 

[Octave77]

Thank you. You wrote "the dose-response curve is far steeper than most if not all benzodiazepines" : by this do you mean that the onset of action of clomethiazole is faster than that of most if not all benzodiazepines ? If so, I would have agreed a few weeks ago, but after having tried clomethiazole seven times it turned out to have fairly an intermediate rapidity of action and some benzodiazepines tablets I've tried so far had a more rapid onset of action than clomethiazole : midazolam, triazolam, brotizolam for examples.

Rearding alcohol withdrawal : yes indeed, from wikipedia (no reliable source) I read : "Clomethiazole is a potent CYP2E1 enzyme inhibitor which slows down the metabolism of ethanol, hence its use in alcohol withdrawal."

Clomethiazole seems to bind to the barbiturate site on the GABA-A receptor, this could explain why according to the BNF it should only be prescribed to people physically dependent ON barbiturates.

 

[4DQSAR]

@Octave77 - No, not the onset time. The fact that one capsule is a reasonable anxiolytic, two capsules are a reasonable hypnotic but three capsules can produce blackouts i.e. people are not sleeping but rather are somewhere on the Glasgow Coma Scale. Ten will generally prove fatal.

So it's just my opinion that clomethiazole still has a place within the in-patient detoxification of people physically dependent on alcohol, like barbiturates, accidental overdoses are far too common and the outcomes are far to serious for it's use in out-patient treatment. A TI of less than 10 is quite narrow when compared with benzodiazepines.

 

[red22]

Well it's really hard to get a script for it, but Desoxyn is pure Dextromethamphetamine hydrochloride.

There's also Didrex, which metabolizes into methamphetamine.

 

[Octave77]

I confirm : 1 capsule is anxiolytic, maximum two capsules is hypnotic ; that is what the patient's leaflet mentions for that matter. And that is what happened to me during my last try (on Monday) : a slight blackout one hour and a half after taking 3 capsules of 192 mg clomethiazole at once in the evening. Not unpleasant actually, but I don't plan to experiment with this too high dosage again.

I guess I got what you meant by steep dose-response curve : when one takes 2 capsules of clomethiazole, the effect may be supposed to be twice stronger than that of 1 capsule, 3 capsules three times stronger, etc... The dose-response curve of clomethiazole may be proportional as that of barbiturates is because they are agonists of the GABA transmission. Conversely, benzodiazepines are allosteric modulators, not agonists of the GABA transmission : the dose-response curve is not proportional but asymptotic. 2 tablets may have an effect just 1.5 times stronger than that of 1 tablet. And so on until a plateau is reached. This could explain why benzodiazepines taken without other drugs or alcohol are rarely fatal in cases of overdosage.

 

[4DQSAR]

@Octave77 - Exactly right. I'm always glad to see people who take the time to understand the medications they are prescribed.

As I mentioned, clomethiazole can produce amnesia and loss of executive function so too often we would read a coroners court giving an open verdict in cases where people had taken say six Seconal (or other intermediate-acting barbiturate) or clomethiazole when they had 56 capsules. If it was an intentional overdose, wouldn't someone take ALL of their sleepers? Often small amounts of alcohol were also found in PM fluids. I mean 2-4 units i.e. 1-2 pints or 1-2 large glasses of wine.

Based on the few interviews of people who survived, the most common sequence would be someone taking their usual dose of sleepers with a drink, falling asleep for a bit, waking and up not remembering they had already taken their dose and repeat. In the morning they would be found dead with asperation of vomit or simply respiratory collapse being stated as the immediate COD.

It also seems that clomethiazole might not have reliable pharmokinetics. We also noted among people who were dependent on the sfuff (duck eggs only cost 50p back then) would find their level, take the same dose every day until one day it killed them. Being such an old drug nobody is ever likely to confirm that hypothesis, but it did strike us as being odd.

 

[BourbonMac]

Isn't that a Non sequitur?

I only know I was VERY briefly prescribed gabapentin and then pregabalin. This was long before anyone mentioned them being 'drugs of abuse' or whater term is now used.

I just kept falling over. I told the doctor I kept falling over and wasn't it perhaps a bad idea to give someone on crutches a medication that messes around with balance? It got brushed off but I think I maybe managed to take them for a few days, take a fall and realize WHY I was falling over.

As @someguyontheinternet notes - everyone I knew in the US said that oxymorpone was the best opioid although none had sampled levorphanol... although that only ever comes in 2mg tablets, not the terrible idea 40mg Opana tablets. An opioid with 20% oral bioavilability... in a tablet. I've been given ketamine after a severe injury and before a surgery. Odd stuff. I wasn't scared but I couldn't even communicate with the clinicians which I consider a problem.

Not exactly, it's just I only sometimes have those periods where I'm like getting high every night unintentionally off of it. Lol @ Lyrica rails though, I actually really dislike how Lyrica feels a lot and prefer Gabapentin. Lyrica tended to hit me like Phenibut did and I ultimately grew to really hate that stuff

 

[silver_lining]

Well you can get ketamine scripted in the US. Also dilaudid. Those 2 are pretty euphoric.

'King benzo' lmfao. Benzos are so mid bruh they're literally the least euphoric downer I've ever experienced.

Ya Soma is epic. Especially if a benzo accidently is taken shortly after. The fact that it is a "pro drug" that metabolizes into another active drug makes it a lot of fun. Empty stomach and a1 1/2 grams is my go to, perfect buzz starts it up and no comedown, just mellowed out downer. And really helps sleep, anxiety, muscle and bone pain.