Opioids Toxic Opioids

[Knarf]

Toxicity: Using Little-Known Opioids

I was curious as to the toxicity of certain opioids, knowing already the specific dangers of a select few.

How and why do certain chemicals of this grouping cause ill effects beyond that of say, morphine? What are some common issues of this nature, for example seizures from tramadol, with regards to opioids? If anyone with some knowledge could put it into layman's terms, a general overview of the subject would be greatly appreciated; unfortunately my formal education has not yet covered this material.

If investigating relatively unknown opioids with only a basic material fact sheet, what kind of things should I look for in order to gauge safety, and discern whether or not to stay away? These sheets do contain, albeit sometimes limited, toxicological and structural information, but as I said my current knowledge hinders my interpretation. What could one expect for example, given the oral and IPR(??) LD 50's in rats? How would this information translate to potential human dosing? Are there structural properties that I should be aware of?

I know this is a very broad topic and that I'm asking a lot, but it is in the pursuit of safety.

To sum it up:

How can one, armed with technical data and material safety fact sheets, ensure safety when imbibing relatively unknown opioids?


Thanks a lot!

 

[perKeceT]

im clueless on most of what youd like to know, but i will say that the seizure threshold lowering action of tramadol has to do with how it effects either serotonin or norepinephrine(dont remember which) not its weak opiate effects.

 

[HdoubleODeezy]

darvon (dont remember generic name) is toxic at high doses

 

[amapola]

To infer biological action from similarities and variability in chemical structure requires extensive experience and is well beyond the skill of most people including myself. If you go over into ADD where we have some of the best people in the world in the field, you will still see at most general theories on how it could influence the behaviour of the drug.

I really don't know where to start. Are you familiar with the opioid receptors (mu, delta, kappa, etc.)? How the blood brain barrier works? How the liver might try and metabolize the drugs?

To make a point using your example, tramadol is only a weak mu opioid receptor agonist and also has effects on serotonin, nicotine and muscarinic acetylcholine receptors, is an NERI, and the only way we know how all of these things interact is by the results not the method.

If you are sitting with a bag of powder and an MSDS that just holds the LD50 for rats, all you can safely determine is how much to give a group of rats if you want to kill half of them.

 

[sekio]

That's tox testing for you.
The safest way to figure out their efficacy as a drug is to not ingest them...

 

[RedRum OG]

you can go deep into science and chemistry and biology to figure the answer. but honestly the best method of being safe is to know your body and how it reacts. also, know your dope. do extensive research and then do a dose a little below what you believe is safe.

if youre doing something like heroin with inconsistent purity, always do a tiny test hit to see how good it is. if its a pharm, well you always know its the exact dose. just be aware of your tolerance changing.

every person is different. there is no constant safe dose to take. be aware of your limits, and always do less than you think you should. you can always take more, you can never take less once the drugs inside you.

 

[NeighborhoodThreat]

^This, and take HOOD's advice, don't take darvocet.

The generic name is dextropropoxyphene, thankfully they finally took it off the market (here in the U.S., and was withdrawn from the U.K. market in 2007 per the wiki article for it).

 

[titstypedthis]

demerol

 

[caseface99]

A chick i went to rehab with got bad heart toxicity/problems from 900+mgs of methadone a day, had to get a pace maker put in and she gained like 300 pounds. She sued the doctor and won by the way, like seriously, he had her on almost a gram of methadone that's fucking nuts.

 

[sir_thizzalot]

^
That's so unbelievable that I would assume she's lieing.

Knarf- We don't know about exact toxicities of many opiates, and I think there's more and more people having problems from taking their prescribed opiates for years now(NOT talking about withdrawal problems).

It's hard to find out the exact toxicity a complicated drug has. I'm having trouble wording what I mean.... but look at EVERY part of your brain and body a drug COULD have effect/toxicity on, and think about how impossible it is for us to do some rat/monkey trials to try to understand every bit of toxicity. Time will show us better, give it a few more years and see the problems people who've been using or abusing a certain opiate for years may have.

 

[Captain.Heroin]

A chick i went to rehab with got bad heart toxicity/problems from 900+mgs of methadone a day, had to get a pace maker put in and she gained like 300 pounds. She sued the doctor and won by the way, like seriously, he had her on almost a gram of methadone that's fucking nuts.

I know that people have had toxicity from methadone at a lower dosage as well, though how frequently I do not know.

^
That's so unbelievable that I would assume she's lieing.

A definite possibility, although typically she would have paperwork about this sort of thing. Maybe caseface has seen some of the documentation?

 

[DuckSauce]

is that really a possibility, a person being given by a doctor or even taking on their own 900 or more mgs of methadone a day? holy shitballs that is nuts. imagine the w/d from that shit

 

[Knarf]

These little known opioids I'm talking about are not on the pharmaceutical market and there is a lack of information regarding human ingestion; from what I can tell via internet research atleast.

If dosing a, highly potent selective mu-agonist, the question is really how much should one start with, assuming that there is no other activity in the body.
Dilution is obviously possible, so based on the potency of known ultra-potent opioids, how many micrograms would be a safe starting dose?

Or is there really no safe way to go about it, and should these compounds be avoided all together?

 

[NeighborhoodThreat]

^^

A chick i went to rehab with got bad heart toxicity/problems from 900+mgs of methadone a day, had to get a pace maker put in and she gained like 300 pounds. She sued the doctor and won by the way, like seriously, he had her on almost a gram of methadone that's fucking nuts.

C.H: I imagine some sort of documentation exists, that dose is insane.

I remember when I could get high off 5mg of methadone.

So here's what we have so far:

pethidine/meperidine (Demerol)
dextropropoxyphene/propoxyphene (Darvocet and many others)
methadone

any others?

 

[amapola]

These little known opioids I'm talking about are not on the pharmaceutical market and there is a lack of information regarding human ingestion; from what I can tell via internet research atleast.

If dosing a, highly potent selective mu-agonist, the question is really how much should one start with, assuming that there is no other activity in the body.
Dilution is obviously possible, so based on the potency of known ultra-potent opioids, how many micrograms would be a safe starting dose?

Or is there really no safe way to go about it, and should these compounds be avoided all together?

You should ask on a case by case basis in ADD but the final answer is if you are the first person taking them it's not going to be completely safe.

 

[daddysgone]

These little known opioids I'm talking about are not on the pharmaceutical market and there is a lack of information regarding human ingestion; from what I can tell via internet research atleast.

If dosing a, highly potent selective mu-agonist, the question is really how much should one start with, assuming that there is no other activity in the body.
Dilution is obviously possible, so based on the potency of known ultra-potent opioids, how many micrograms would be a safe starting dose?

Or is there really no safe way to go about it, and should these compounds be avoided all together?

I am going to refrain from even attempting to be polite or sensitive here because based on what you have said here, there is a good chance you are going to kill yourself if you plan on experimenting.

What I mean by this is the question you posed above displays such a profound ignorance that you have NO business attempting to dose yourself with any of these compounds.

You are asking us how many micrograms of an ultra-potent opioid you should take....you don't even mention which opioid you are referring to. You make it seem as if all of these ultra-potent opioids have a similar dosage range. They don't. Depending on what compound you are talking about, a "proper" dose might be hundreds of micrograms or more, or just a few micrograms could be enough to kill you.

Seriously man, this has bad news written all over it. Don't be stupid.

 

[Mora Fiend]

I agree with Daddysgone, if you do have 'highly potent selective mu-agonists' then you need to dilute them down with a method that has been proven effective for the opiate you are working with. You are talking about dosing in the scale of micrograms, so let's say the dose you are after is 500 micrograms to get high. Let's put that into perspective:

That would be similar to cutting a gram of coke into 2,000 equal lines.

 

[Limpet_Chicken]

Some of those uber-potent mu-opioid agonists are highly prone to causing severe respiratory depression, take as an example, carfentanil, its used to drop large animals such as rhino, lions, and other large animals.

Potency approximately 10,000 times that of morphine, starts being active at a dose of a single microgram!

Etorphine, another real brute of an opioid is perhaps a third as potent as carfentanil, yet still so strong that before it is even loaded into a dart, a second person has to be standing there with a pre-loaded syringe full of an opioid antagonist, diprenorphine, that makes naloxone look like kids candy.

It doesn't take an accidental needlestick to kill somebody working with the stuff, skin contact is quite sufficient.

Some of the hyper-potent synthetic opioids of that nature may have a binding affinity for the the MOR that exceeds that of naloxone, which means naloxone would NOT be able to bring a person who had overdosed back, buprenorphine is an example of an opioid with a higher binding affinity, IIRC, that of course is far, far less potent and well known in human use (added safety is granted by its being a partial agonist)

Then there is a fluorinated analog of ohmefentanyl, that is roughly 18000x the strength of morphine, by weight. I imagine in a human subject its active dose would be somewhere very roughly the tens of nanograms, to perhaps low hundreds of nanograms (1ng is a thousandth of a microgram)

This is an educated estimate, not an exact figure, nor guaranteed to be correct in practise.

Problems with using these sorts of opioids, discounting completely the difficulty in measuring a dose, a scale accurate to 1mg could be out by a thousandfold, even with volumetric dilution, and on opening a vial of something like this as a powder, some is bound to aerosolize, and that could well be enough to kill not just the intended user, but everybody else in the room at the time. They cause pronounced, rapid tachyphylaxis, this is evident with fentanyl itself, very rapid tolerance, receptor desensitization and internalization. And quite possibly wouldn't even get the user high, but rather, act as a rapid general anaesthetic, causing unconsciousness.

There are two realistic uses of these kinds of compounds, one being in research binding assays using radiolabelled material to determine SAR of opioid receptors and their pharmacology, and the other, is as chemical weapons, on a basis of lethal dosage by weight, many of them are not just many times, but many orders of magnitude more toxic than VX nerve agent, or even the novichok nerve agents.

Russki special forces used some sort of high-potency opioid dispersed in a gas during a hostage siege, then simply walked in and shot the terrorists as they were out cold, they haven't revealed exactly what the drug was, but its likely to be some sort of potent fentanyl derivative, etorphine type compound maybe. Killed a fair few hostages too, due to them being secretive bastards and withholding the nature of the agent, leaving the paramedics attending the hostages not knowing how to treat those affected.

Interestingly though, the chinese use dihydroetorphine in the form of sublingual tablets as a painkiller, and maintainance opioid much as western countries use methadone or bupe, active dose according to wiki is something like 20ug.

Now that I would give a try, at least once, having access to a known, measured pharmaceutical dosage unit. Not without somebody standing by me with a preloaded syringe of narcan and O2 on hand though.

 

[Nagelfar]

I've read (nearly about to ironically write 'heard' for it's colloquial meaning but then stopped myself ;-p) that hydromorphone can cause spectrum hearing loss and tinnitus.

 

[HdoubleODeezy]

^^

So here's what we have so far:

pethidine/meperidine (Demerol)
dextropropoxyphene/propoxyphene (Darvocet and many others)
methadone

any others?

isn't norbuperenorphine toxic at doses that would be needed for pain relief?
but of course that's only a metabolite and not a drug that you can just take a pill of.. as far as i know.