Limpet_Chicken
Bluelighter
Not traditional opioids, but delta-opiate receptor agonists cause seizures, well, some of them do, others do not, or at least, do so only at high doses. Makes me inclined to think that there are delta subtypes, as there are for mu (Mu1, Mu2, and a little known Mu3) and kappa (at least two subtypes are known, kappa1 and kappa2)
Delta agonists appear to have antidepressant effects, I think I read somewhere that they induce BDNF release which would make them neuroprotective, and induce neurogenesis/promote neuronal survival, and appear to be stimulating in nature, they do apparently provide analgesia, and counteract respiratory depression induced by Mu-opioid agonists, I would quite like to try a selective delta agonist, one of the ones known to possess little convulsant activity someday.
As far as traditional Mu opioid agonists go...I have suspicions of potential toxicity about meptazinol. It is scripted here in the UK for those with a requirement for a painkiller below the level which warrants morphine or pethidine etc, but who cannot take codeine/dihydrocodeine or tramadol.
My former housemate, who turned out to be a serial liar, highly manipulative, a thief, delighted, so I found out, in taking my pain meds, hiding them, and making me withdraw, only to come to the rescue with meptazinol, gain attention and look like a wonderful, helpful person.
She took my pain meds, I have a rx for dihydrocodeine, thanks to a knee problem that I have had since childhood, after falling on broken glass and getting glass in my knee, and to compound that, while that was healing, a bunch of chavscum stamped on my knee.
Ever since then, I have been left with stiffness, constant pain and chronic tendonitis, surgery to remove a piece of bone from my knee joint didn't help, and just left me with nerve damage, so my doc has no problem with, if needs be, we both know full well they are habit forming, and I would (and have) become physically dependent, but such is the price I have to pay. I'm 24, and walk with a damn cane :/
If the bitch had actually took any of the painkillers she stole it would have killed her in minutes, possibly before an ambulance could arrive as she is highly allergic to any of the morphine-related opiates, she has hypermobile joints (in my opinion Ehlers-Danloss syndrome) and they dislocate all the time, climbing stairs, walking, anything will do it, and severe arthritis in her hips and knee....although she deserves every fucking second of pain she will ever get, and then many more. Tramadol would also cause anaphylaxis....fucking slag has more allergies than the rest of BLers put together have had drug benders. Morphine related pain meds, tramadol, latex, tomato, lactose intolerant, chocolate..you name it, fucker is allergic to it.
Doc couldn't give her the first line painkillers, codeine, DHC or tramadol, before coming over on the banana boats from the US illegally to the UK she was given darvocet, but that CANNOT be prescribed here, they took it off the market thanks to its cardiotoxicity and frequent use in suicides, so they put her on meptid, the trade name for meptazinol.
Worked, 200mg would give pain relief, 400 much more so, high as a kite (atypical response methinks, she was highly sensitive to many drugs and had wierd responses...typical tryptamine psychedelic response to sumatriptan, rectal dose of maybe 40mg or so of DMT, no MAOI lasted all night, very sensitive to mushrooms etc) so I don't think those doses would do that to most people, and a couple more 200mg tablets than that made her pretty damn ill.
I'm dependent on DHC, thanks to my longterm need for it, but stable at a minimum of 60mg/d, sometimes get by on just 30mg before I sleep, (am scripted more than that however, but have been tapering to lower my tolerance and have it maintain efficacy) and meptazinol is a partial agonist, but I had some very, very bad responses to it, that were NOT precipitated withdrawal, details as follows:
Used it for tapering, as a step down from a full agonist, to partial, should make it easier to stop altogether, 200mg did fuck all to alleviate withdrawal, 400mg helped, 600mg gave me horrid heartburn and GI discomfort, 800 per os....that felt like I had swallowed battery acid, awful corrosive shits, stomach pain and nausea.
Once tried 800mg rectally, whilst pretty tolerant to DHC after using quite a bit of the stuff, and jesus...that was fucking awful, after adminstering the solution, dissolved in 10ml of water, instant, vicious pain. I assumed it was just a bit of stinging, and slightly irritating at the time (this was before my sever GI issues with the stuff), so I held it in to make sure it took effect.
Bad, bad, bad idea. I started playing a videogame to pass the time a bit, ignoring what was then mild discomfort, eventually couldn't retain the solution anymore, got rid of it, but the discomfort turned into intense pain and repeated abdominal cramping, started getting nauseous, sweating like crazy. Had to go puke, repeatedly, then collapsed on the bathroom floor, became tachycardic.
After a while just lying there hoping it would pass soon, as meptazinol is quite a short acting opioid, I eventually managed to walk to the bedroom and crash on the bed, heart still racing like fucking crazy, and pronounced diaphoresis, had to take my top off as it literally got soaked with sweat. I also noticed that my hands started twitching/jerking if I tried any fine motor movements, that extended up to the arms but went no further.
I managed to dissolve a large dose of tizanidine in water, and plug that, which stopped the twitching, and appeared to reverse all the effects, save the nausea and GI pain, although that became irrelevant, as it soon knocked me unconscious.
It was NOT precipitated withdrawal due to its partial agonist effects. I know what withdrawal feels like, and this was not it, it did share some symptoms with the opioid withdrawal syndrome, but definately wasn't withdrawal. Meptazinol orally doesn't cause precipitated withdrawal at any dose either, even those that make me feel awfully sick and cause stomach/throat pain.
Meptazinol has AWFUL bioavailability taken per os, 10% or less. I don't think the gastrointestinal effects are due to a pharmacological effect of the drug itself, but rather, of its physical chemical properties, its a funky looking benzazepine, with a phenolic hydroxy group present, unlike the -OH of an aliphatic alcohol, a phenolic hydroxy moiety is significantly acidic, so I think it quite likely that meptazinol is sufficiently acidic to irritate mucous membranes, the tablets felt like they did on my throat, when swallowed, and to further substantiate that theory, any drug at all would have to act extremely rapidly, considering the onset of the pain up my arse was felt within a minute, two at most, for it to be able to pharmacologically produce any effect, including pain.
Interestingly though, meptazinol is a highly subtype selective agonist for the Mu1 subtype, and there aren't many of those known.
Bearing in mind my theory of the physical irritation of the mucosa being due to that phenol moiety, I have been contemplating trying the propionyl and/or benzoyl esters, just as morphine is acetylated to give heroin, making it much more lipophilic (-OH is very polar indeed, a big, water loving carbuncle of a functional group that really is not conducive to passing the BBB), enabling much lower doses to be taken.
I may never get round to it though, and the crystalline meptazinol sulfate I have may well just get left to sit on the shelf, so to speak for a few years, until I eventually get so bored one day I have nothing else to do but go acylate it![:\](https://bluelight.org/xf/BL_Images/Orig_Emoji/wrygrin.gif "wry grin :\")
Not a high priority.
If I do test those derivatives out though, it will be most damn carefully, working up from a few milligrams...that plugging experience was awful.
Meptazinol is a chiral molecule....I am pretty sure the form used clinically is racemic, it would be interesting to see if one isomer is responsible for its opioid properties and one for toxic symptoms.
Structure of meptazinol:
Formal name: 3-(3-ethyl-1-methylazepan-3-yl)phenol.
I think we can also consider the superpotent opioids that are derived from fentanyl, the oripavine derivatives like etorphine, Lednicer's bromadol, and the Knaus-compounds as toxic opioids. Not because they have non-opioid effects that are toxic, but simply because they are so cunting potent, 10,000x the potency of morphine in the case of carfentanil, and even that is made to look like a shittier version of darvocet in comparison with some derivatives of ohmefentanil.
An active dose of etorphine is a mere one fucking microgram, to show some activity in humans, for the fluoro-ohmefentanyl, that would likely be active in the low nanogram range, 1mg would kill even a real tolerant, degenerate gutter smack-rat a thousand times over before the needle even left his arm.
In contrast, a lethal dosage of sarin nerve agent is between 5-10mg (although it would be much less if injected), a lethal dosage of the far more toxic VX is a little less than 1mg, and by far the deadliest nerve agents yet discovered, the novichok agents, the most potent of those, is perhaps 50-200mcg, which still makes some of those fentanyl derivatives far more toxic (although given the choice between death by nerve agent, and by fuckoff potent opiate...no contest really)
Delta agonists appear to have antidepressant effects, I think I read somewhere that they induce BDNF release which would make them neuroprotective, and induce neurogenesis/promote neuronal survival, and appear to be stimulating in nature, they do apparently provide analgesia, and counteract respiratory depression induced by Mu-opioid agonists, I would quite like to try a selective delta agonist, one of the ones known to possess little convulsant activity someday.
As far as traditional Mu opioid agonists go...I have suspicions of potential toxicity about meptazinol. It is scripted here in the UK for those with a requirement for a painkiller below the level which warrants morphine or pethidine etc, but who cannot take codeine/dihydrocodeine or tramadol.
My former housemate, who turned out to be a serial liar, highly manipulative, a thief, delighted, so I found out, in taking my pain meds, hiding them, and making me withdraw, only to come to the rescue with meptazinol, gain attention and look like a wonderful, helpful person.
She took my pain meds, I have a rx for dihydrocodeine, thanks to a knee problem that I have had since childhood, after falling on broken glass and getting glass in my knee, and to compound that, while that was healing, a bunch of chavscum stamped on my knee.
Ever since then, I have been left with stiffness, constant pain and chronic tendonitis, surgery to remove a piece of bone from my knee joint didn't help, and just left me with nerve damage, so my doc has no problem with, if needs be, we both know full well they are habit forming, and I would (and have) become physically dependent, but such is the price I have to pay. I'm 24, and walk with a damn cane :/
If the bitch had actually took any of the painkillers she stole it would have killed her in minutes, possibly before an ambulance could arrive as she is highly allergic to any of the morphine-related opiates, she has hypermobile joints (in my opinion Ehlers-Danloss syndrome) and they dislocate all the time, climbing stairs, walking, anything will do it, and severe arthritis in her hips and knee....although she deserves every fucking second of pain she will ever get, and then many more. Tramadol would also cause anaphylaxis....fucking slag has more allergies than the rest of BLers put together have had drug benders. Morphine related pain meds, tramadol, latex, tomato, lactose intolerant, chocolate..you name it, fucker is allergic to it.
Doc couldn't give her the first line painkillers, codeine, DHC or tramadol, before coming over on the banana boats from the US illegally to the UK she was given darvocet, but that CANNOT be prescribed here, they took it off the market thanks to its cardiotoxicity and frequent use in suicides, so they put her on meptid, the trade name for meptazinol.
Worked, 200mg would give pain relief, 400 much more so, high as a kite (atypical response methinks, she was highly sensitive to many drugs and had wierd responses...typical tryptamine psychedelic response to sumatriptan, rectal dose of maybe 40mg or so of DMT, no MAOI lasted all night, very sensitive to mushrooms etc) so I don't think those doses would do that to most people, and a couple more 200mg tablets than that made her pretty damn ill.
I'm dependent on DHC, thanks to my longterm need for it, but stable at a minimum of 60mg/d, sometimes get by on just 30mg before I sleep, (am scripted more than that however, but have been tapering to lower my tolerance and have it maintain efficacy) and meptazinol is a partial agonist, but I had some very, very bad responses to it, that were NOT precipitated withdrawal, details as follows:
Used it for tapering, as a step down from a full agonist, to partial, should make it easier to stop altogether, 200mg did fuck all to alleviate withdrawal, 400mg helped, 600mg gave me horrid heartburn and GI discomfort, 800 per os....that felt like I had swallowed battery acid, awful corrosive shits, stomach pain and nausea.
Once tried 800mg rectally, whilst pretty tolerant to DHC after using quite a bit of the stuff, and jesus...that was fucking awful, after adminstering the solution, dissolved in 10ml of water, instant, vicious pain. I assumed it was just a bit of stinging, and slightly irritating at the time (this was before my sever GI issues with the stuff), so I held it in to make sure it took effect.
Bad, bad, bad idea. I started playing a videogame to pass the time a bit, ignoring what was then mild discomfort, eventually couldn't retain the solution anymore, got rid of it, but the discomfort turned into intense pain and repeated abdominal cramping, started getting nauseous, sweating like crazy. Had to go puke, repeatedly, then collapsed on the bathroom floor, became tachycardic.
After a while just lying there hoping it would pass soon, as meptazinol is quite a short acting opioid, I eventually managed to walk to the bedroom and crash on the bed, heart still racing like fucking crazy, and pronounced diaphoresis, had to take my top off as it literally got soaked with sweat. I also noticed that my hands started twitching/jerking if I tried any fine motor movements, that extended up to the arms but went no further.
I managed to dissolve a large dose of tizanidine in water, and plug that, which stopped the twitching, and appeared to reverse all the effects, save the nausea and GI pain, although that became irrelevant, as it soon knocked me unconscious.
It was NOT precipitated withdrawal due to its partial agonist effects. I know what withdrawal feels like, and this was not it, it did share some symptoms with the opioid withdrawal syndrome, but definately wasn't withdrawal. Meptazinol orally doesn't cause precipitated withdrawal at any dose either, even those that make me feel awfully sick and cause stomach/throat pain.
Meptazinol has AWFUL bioavailability taken per os, 10% or less. I don't think the gastrointestinal effects are due to a pharmacological effect of the drug itself, but rather, of its physical chemical properties, its a funky looking benzazepine, with a phenolic hydroxy group present, unlike the -OH of an aliphatic alcohol, a phenolic hydroxy moiety is significantly acidic, so I think it quite likely that meptazinol is sufficiently acidic to irritate mucous membranes, the tablets felt like they did on my throat, when swallowed, and to further substantiate that theory, any drug at all would have to act extremely rapidly, considering the onset of the pain up my arse was felt within a minute, two at most, for it to be able to pharmacologically produce any effect, including pain.
Interestingly though, meptazinol is a highly subtype selective agonist for the Mu1 subtype, and there aren't many of those known.
Bearing in mind my theory of the physical irritation of the mucosa being due to that phenol moiety, I have been contemplating trying the propionyl and/or benzoyl esters, just as morphine is acetylated to give heroin, making it much more lipophilic (-OH is very polar indeed, a big, water loving carbuncle of a functional group that really is not conducive to passing the BBB), enabling much lower doses to be taken.
I may never get round to it though, and the crystalline meptazinol sulfate I have may well just get left to sit on the shelf, so to speak for a few years, until I eventually get so bored one day I have nothing else to do but go acylate it
Not a high priority.If I do test those derivatives out though, it will be most damn carefully, working up from a few milligrams...that plugging experience was awful.
Meptazinol is a chiral molecule....I am pretty sure the form used clinically is racemic, it would be interesting to see if one isomer is responsible for its opioid properties and one for toxic symptoms.
Structure of meptazinol:
Formal name: 3-(3-ethyl-1-methylazepan-3-yl)phenol.
I think we can also consider the superpotent opioids that are derived from fentanyl, the oripavine derivatives like etorphine, Lednicer's bromadol, and the Knaus-compounds as toxic opioids. Not because they have non-opioid effects that are toxic, but simply because they are so cunting potent, 10,000x the potency of morphine in the case of carfentanil, and even that is made to look like a shittier version of darvocet in comparison with some derivatives of ohmefentanil.
An active dose of etorphine is a mere one fucking microgram, to show some activity in humans, for the fluoro-ohmefentanyl, that would likely be active in the low nanogram range, 1mg would kill even a real tolerant, degenerate gutter smack-rat a thousand times over before the needle even left his arm.
In contrast, a lethal dosage of sarin nerve agent is between 5-10mg (although it would be much less if injected), a lethal dosage of the far more toxic VX is a little less than 1mg, and by far the deadliest nerve agents yet discovered, the novichok agents, the most potent of those, is perhaps 50-200mcg, which still makes some of those fentanyl derivatives far more toxic (although given the choice between death by nerve agent, and by fuckoff potent opiate...no contest really
)
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