The opiate receptor will not save you.

From this week’s JAMA.

The prevalences of heroin use and use disorder have increased significantly in the US adult general population since the beginning of this millennium. Of note, increases have been greatest among men, white individuals, those with low income and educational levels, and, for heroin use disorder, younger individuals. To curb the heroin epidemic, particularly among younger adults, collective prevention and intervention efforts may be most effective. Promising examples include expansion of access to medication-assisted treatment (including methadone hydrochloride, buprenorphine hydrochloride, or injectable naltrexone hydrochloride), educational programs in schools and community settings, overdose prevention training in concert with comprehensive naloxone hydrochloride distribution programs, and consistent use of prescription drug monitoring programs that implement best practices by prescribers.

Opiates are powerful painkillers. They give a sense of euphoria, which adds to the relief you feel if the pain goes away. We understand the pharmacology of these quite well.

The electron density used to position interacting side chains is shown in light blue colored mesh depicting the 2Fo-Fc electron density contoured at 1.3 ?. Green mesh depicts an omit map of ?-FNA and K2335.39 side chain atoms contoured at 3.0 ?. b, Binding pocket viewed from the extracellular surface. Water molecules are shown as red spheres, with the accompanying electron density shown in light blue mesh. c, The binding site is diagrammed, showing the chemical structure of ?-FNA (green) covalently bound to the receptor through K2335.39 (bold). Hydrophobic interactions are shown in orange and polar contacts with red dotted lines. V3006.55 and I2966.51 form extensive hydrophobic contacts with the back face of the ligand (not shown). Two water molecules are positioned between H2976.52 and the phenolic group of ?-FNA d, The ?OR selective ligand naltrindole includes an indole group that would clash with W3187.35 in ?OR, but not with the leucine found in the equivalent position in ?OR. The indole has been described as an “address” to target the ligand to ?OR, while its efficacy (“message”) is determined by the morphinan group on the left

understanding, in this case, is not helping. The suggestions that the authors have are standard. The difference between NZ and the USA is that we have regulations for novel agents, possession of light substances is not a felony, and our customs service is so good at keeping diamorphine out that the local IV uses make their own.

What has changed is that the groups that seem to be using heroin are the groups the narrative hates. The underclass is growing: the society is hollowing out. And no use of psychopharmacology or psychotherapy can save a people without vision.

6 thoughts on “The opiate receptor will not save you.

  1. Here, while OxyContin / Oxycodone abuse has been a big social problem amongst the underclass for over a decade and a half, now some middle class kids are messing with fentanyl, carfentanil, and other opiates / opioids, and so now our politicians are declaring ‘Crisis!’ and ‘Epidemic!’, and engaging in political grandstanding over the ‘issue’ (as if it were a major issue, rather than a few idiot teens here and there).

    That’s what I was bitching about here and here.

    Some neoreactionary would-be commenter conflated my commentary on these few middle-class Canadian idiots with the wider North American working class opiate problem, and accused me of insensitivity among other things. Idiot didn’t read both posts, else he’d have known what I was talking about.

    Anyway, I would love to see politicians actually tackle the problem of opiate abuse among those in lower socioeconomic groups. But they won’t, because they only care about a few of their own kids and those of their richest supporters, not those of the hated underclass.

    • We don’t have the Oxycont issue because it is a controlled drug. Tramadol is our equivelant.

      When I go to professional meetings in Canada the smugness of the elite is nauseating: the bill of rights is seen as gospel and CANMEDs as the prophets. But the social dysfunction is high, even when I go to the Prairie.

      And in Canada, the truth is always insensitive. I’m worried I will be stopped at the border when I go to visit the family there…

      • I think crystal meth is a bigger problem than opiates, frankly, but that’s just a layman’s opinion; I could be wrong. But I remember how big that was, when I lived in western Canada…

      • Crystal is too toxic. We had an epidemic of it a decade ago. When the gangs stop pushing it because it is ruining their families, and that happened…. the drug does not last.

  2. Interesting that singleness–voluntary or otherwise–is a powerful predictor.

    I personally remember having morphine to kill the pain when I had surgery, and while it killed the pain, there was no euphoria. Asked a doctor friend of mine why some people respond to it quite differently, and one hypothesis is that the euphoric reaction seems to correlate really well with life sucking.

    Now I don’t know if that’s statistically defensible, but it strikes me that if there’s anything to that, then one could theoretically test for depression after any significant surgery with how the person responds to painkillers. Alternatively, one could adjust painkillers based on a history of depression to avoid problems.

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