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Most pleasurable opioid based on pharmacology?

FlyingDutchman342

FlyingDutchman342

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I've seen many posts on this message board where users descibed heroin/morphine as the best opioid.

I found this excerpt in the wikipedia article on morphine. The parcipitants in the study (→below) clearly prefered morphine and it's ester diamorphine over any other opioid. Is there a pharmacological reason for the more pleasurable effects of the two drugs, despite similar mechanism of action to other opioids? Or was the only reason for this outcome that the participants were former heroin users?

"Morphine is a highly addictive substance. In controlled studies comparing the physiological and subjective effects of heroin and morphine in individuals formerly addicted to opiates, subjects showed no preference for one drug over the other. Equipotent, injected doses had comparable action courses, with no difference in subjects' self-rated feelings of euphoria, ambition, nervousness, relaxation, drowsiness, or sleepiness. [...] When compared to the opioids hydromorphone, fentanyl, oxycodone, and pethidine/meperidine, former addicts showed a strong preference for heroin and morphine, suggesting that heroin and morphine are particularly susceptible to abuse and addiction. Morphine and heroin were also much more likely to produce euphoria and other positive subjective effects when compared to these other opioids."
-Source: https://en.wikipedia.org/wiki/Morphine#Reinforcement_disorders (The links to the mentioned studies are given there.)
 
It is evident that some medications can be more addictive than others, but we must not forget the subjective variables of each individual. In my case, I have tried Oxycodone, Tramadol, Morphine, Fentanyl, Meperidine and Kratom. I have never been addicted to any of them, perhaps over time the one I liked the most is Tramadol, despite what many may think, for me it is a very pleasant substance.
But I always take opioids like any other drug, that is, I like to experience one day and then go back to my job and my responsibilities. If you go through a bad time in life, you have no motivation or you are depressed, maybe you can not resist the pleasure provided by opiates, so I think you should not get close to drugs without first solving this important issues.

Drugs are not a toy, they all deserve the same respect, but obviously this is a very difficult type of education to apply to society for a multitude of reasons.

On pharmacology I am not an expert, but I think that depressants (benzo, opiates, alcohol, etc ...) are easier to abuse.


DocLad
 
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how do heroin and morphine differ? im always curious to know because they seem to be the same thing but yet not really perhaps heroin is more diluted with other crap and therefore nobody can be sure what they get high on? and morphine is purification of an opiate to the highest standard possible with zero filler and therefore maybe perhaps the best painkiller and addictive compound out there? correct me if im wrong, i could never get morphine because thats what rich people used to get in the past and only really sick people before their death get now so hard to compare in any way.
about tramadol, its just an antidepressant for me. i dont get high on that thing, just keeps you going is all. interesting to find you get a high off it, good job, do you take like 10 50mgs or what?
 
how do heroin and morphine differ? im always curious to know
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From what I remember, studies seem to indicate that morphine and heroin differ only in potency; that is to say heroin is mainly a high-BA prodrug for morphine.[ref] Esterases convert heroin in the blood to 6-MAM and morphine quite rapidly so the major difference is in potency alone.

That's for purified diamorphine, the stuff sold on the streets is not necessarily "heroin" at all.

It's also worth noting that there are also the delta, kappa, and nociceptin receptors and activity as a histamine releaser to consider. Possibly also mu-dopamine receptor dimers to consider too.
 
not sure why, any idea by the professionals here - since i started using alcohol aggressively, heroin has been more of a super stimulant and panic inducer than anything ive experienced before i started abusing alcohol. any clue as to why? to try to explain better i guess, when i abused heroin years ago, i hardly drank and i felt super relaxed on heroin alone, so i never needed much booze. now days its the opposite, i abuse alcohol, and whenever i do heroin which is very rare, i get panics and weird annoying stimulation, like... small coke dose without the high. very bizarre case...
 
For me opiates were always enough, but there were moments when I tried something else hoping to get away from all the meds, heroin, especially when I IV’ed even when it was prescribed. At some point I felt that Coke was a good distraction and it somehow interfered with my opiate addiction. Like I recently mentioned in another post, I started to have allergies and for an instance I thought I could not do opiates the way I was doing.

I am not a professional but I find it possible that other stimulants may change the reaction we have with this or that drug but at the end, from my experience, eventually we end up going back to our drug of choice even if that makes us feel bad or sick.

Alcohol is obviously underestimated by a lot of people in different cultures but it can be as devastating and strong as most of strong drugs imho, and that may lead some of us to experience various degrees of collateral effects, socially but also physically. So I think it has a great potential to make us feel different, especially when we associate it with other drugs even if they once made us feel good and complete. Depending on how much you are drinking I assume this could happen.
 
asecin said:
not sure why, any idea by the professionals here - since i started using alcohol aggressively, heroin has been more of a super stimulant and panic inducer than anything ive experienced before i started abusing alcohol. any clue as to why? to try to explain better i guess, when i abused heroin years ago, i hardly drank and i felt super relaxed on heroin alone, so i never needed much booze. now days its the opposite, i abuse alcohol, and whenever i do heroin which is very rare, i get panics and weird annoying stimulation, like... small coke dose without the high. very bizarre case...
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To some degree the effects of opiates (agonists at Mu Opioid Receptors) are due to inhibition of GABAergic neurons, which normally alcohol will tend to increase the excitability of. So a partial explanation may lie therein
 
I thought that diamorphine was only stronger and more potent due to its ability to cross the BBB much faster and fill receptors more quickly than morphine?
 
I haven't done any real research regarding this, but I have seen said by a few posters whom I trust that ethanol can switch certain populations of opioid receptors from inhibitory to excitatory,
 
Diconal, Ketogan, Levo-Dromaran & Piritamide - μ/NMDA activity results in a massive and long rush. Adding methylphenidate was common in the 1970s. People have mixed antihistamines & DRIs with opioids for a similar effect but it's both inferior and very, very hazardous.

Since nortilidine has μ/NMDA/DRI, reports state a very similar subjective effect. Long, highly euphoric, stimulating rush from insuffusion but it was only available for about 6 weeks and the supplier never restocked.

I should also point out that these drugs are just about the most destructive known to man.

http://michaellinnell.org.uk/michael_linnell_archive/mc_dermotts_guides/pdf/M6 MCDERMOTT.pdf

I've worked with Michael for 26 years and of course, McDeromott is quite famous. Delia Venus Wyn (listed in the credits) created the Eunoia Disc so people like the DEA have copies. A 'level playing field' was the explanation. 'Since everyone knows everything, the war on drugs is doomed...' which is an odd idea, but it does mean something like 35000 compounds would need to be watched and without a CAS, deviation from IUPAC naming makes the stuff impossible to spot. A strange person but I cannot fault the work.
 
Opioids bind to specific opioid receptors in the nervous system and other tissues. There are three principal classes of opioid receptors, μ, κ, δ (mu, kappa, and delta), although up to seventeen have been reported, and include the ε, ι, λ, and ζ (Epsilon, Iota, Lambda and Zeta) receptors.

from wikipedia
my quick guess morphine e.g heroine has a balanced opiate receptor pharmacology,that exceed the 3 main opioid receptors,that most people here know,but extends to the other minor opioid receptors,that also play a role in how euphoric a opioid can be.
High mu affinity is the main factor,as is lipid solubillity,but on the other side,fentanyl has both a higher affinity to mu receptors and is more lipid soouble and has more rapid BBB penetration,but anyway is consiered to be much less euphoric than say IV heroine,morphine and pretty much all phenanthrenes,because thy tend to have a balanced pharmalogical profile
 
Neithman said:
Opioids bind to specific opioid receptors in the nervous system and other tissues. There are three principal classes of opioid receptors, μ, κ, δ (mu, kappa, and delta), although up to seventeen have been reported, and include the ε, ι, λ, and ζ (Epsilon, Iota, Lambda and Zeta) receptors.

from wikipedia
my quick guess morphine e.g heroine has a balanced opiate receptor pharmacology,that exceed the 3 main opioid receptors,that most people here know,but extends to the other minor opioid receptors,that also play a role in how euphoric a opioid can be.
High mu affinity is the main factor,as is lipid solubillity,but on the other side,fentanyl has both a higher affinity to mu receptors and is more lipid soouble and has more rapid BBB penetration,but anyway is consiered to be much less euphoric than say IV heroine,morphine and pretty much all phenanthrenes,because thy tend to have a balanced pharmalogical profile
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We know.

μ2 is responsible for most of the euphoric effects but the more promiscuous ligands interact with 2 or more different groups of receptors.
 
I really liked that link CC, and found most of it surprisingly on the level...except for this part about injecting hydrophone.

Anyone who has seen the film ‘Drugstore
Cowboy’, specifically the fatal overdose
scene, is on nodding terms with
hydromorphone (Dilaudid), the active
principle in these capsules. Potency is
about 10 times that of morphine. The
high is clearer and the euphoria greater
than that of heroin although it doesn’t
have the rush. As Nadine in the film
found out the hard way, a little goes a
long way. The strongest of these capsules
has the narcotic punch of a gram of
morphine and since it takes a little while
to come on, the user might turn blue
some minutes after injection rather than
then and there. If you must use them
then crush them and snort them – slowly.
Only recently they were removed from
the US market because combining these
capsules with alcohol could result in the
whole dose being released immediately,
often with fatal results.
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As far as I know, hydromorphone/oxymorphone are up there almost with fentanyl in terms of potency. From what I recall they have rather short duration but are very strong opioids indeed.
 
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