Keep in mind that heroin is more euphoria-inducing than morphine because it crosses the blood-brain barrier about 10 times faster than morphine, thus kicking in a LOT quicker. But it’s a pro-drug, converted to morphine in the brain, and it’s the morphine molecule that gives the effect. Heroin on its own only weakly binds to opioid receptors.
Which is why anyone who is allergic to morphine will be allergic to heroin. True Ige-mediated allergic, that is.
I wish I could dig up that story.
Could that effect be mitigated by giving a smaller time-release dose?
ETA: Even if it could, it seems to me that it would probably be more practical to just go with morphine in the first place. I’m just curious because I was talking about this a few days ago and the subject came up. (Specifically, why heroin would be more addictive than morphine, when they both end up as the same thing in the brain.)
Why is it called “schedule” 1 instead of something like “tier”, “classification”, or “level”?
The OED entry on “schedule” is illuminating:
[quote]
[ol][li] A slip or scroll of parchment or paper containing writing; a ticket, label, placard; a short note. Obs.[/li][li][list=a][*] Originally (as specific use of sense 1), a separate paper or slip of parchment accompanying or appended to a document, and containing explanatory or supplementary matter; in 16–17th century sometimes used for a codicil to a will. Obs.[/li][li] Hence (without material reference) an appendix to an Act of Parliament or a legal instrument, containing (often in tabular form) a statement of details that could not conveniently be placed in the body of the document.[/li][li]In wider sense, any tabular or classified statement, esp. one arranged under headings prescribed by official authority, as, e.g. an insolvent’s statement of assets and liabilities, a return of particulars liable to income or other tax, and the like. Also occasionally a blank form to be filled up by the insertion of particulars under the several headings.[/ol][/list][/li][/quote]
So basically: it used to be a word meaning “a slip of paper”, and then became used for “an attachment to an official document” and then “an appendix to a law” via that sense. The applicable US law presumably has various “schedules” that categorize drugs as to the penalties and regulations that apply to them.
More and faster euphoria ==> more positive reinforcement to take more, sooner.
The physical dependency and withdrawal from heroin vs. morphine isn’t all that different, however.
Yeah, that was what I meant I was discussing – my understanding is that, even for the same basic chemical (or different chemical but same receptor it is an agonist for), the higher the dose and the faster it gets to your brain, the more euphoria it creates and the more addictive it is. Which is why smoking and injecting stuff tends to be more addictive than taking it orally, because those are both very rapid routes to the brain. And why cocaine tends to be more addictive than chewing coca leaves, because you’re getting a much higher dose of active ingredient at once.
The initial discussion started because my daughter was reading a book about drug policy, and one of the chapters had a number of anecdotes from drug users, and one of them described a heroin user who described the experience of injecting some heroin and feeling waves of orgasmic pleasure washing over him, and she said “Hey, whenever I’ve had painkillers, it never felt anything at all like that, even in the hospital when I had IV morphine! And I thought heroin was basically just more fat-soluble morphine that gets through the blood-brain barrier faster before being converted back to morphine! Why would it be so different?” So we got into a discussion about … all the stuff previously mentioned.
But I did wonder if a time-release version of diacetylmorphine that released, say, 1/10 as much for 10x as long, would be pretty much equivalent to a similar dose of morphine, or if there would still be significant differences. It’s been way too long since I studied anything about the blood-brain barrier…
I"m not sure you could make a time release version of heroin, without denaturing so far that it is only gesturally relevant to call it heroin at all.
IIRC, it is the two acetyl compounds hanging off the morphine molecule (hence diacetyl morphine) that mediate the process of getting through the blood/brain barrier more quickly than morphine, as Qadgop has described. This generates the much-prized rush associated with heroin use. Slowing that down (so that it is monoacetyl morphine or maybe with another compound to replace the acetyls) prevents it being heroin at all.
Again IIRC, heroin’s half life in the body once ingested but before it metabolises into morphine is a matter of minutes. Once it is through the brain barrier, the acetyls fall off. People who die of heroin overdoses (but not immediately, on the end of the pick) tend to be found with only morphine in the body.
Morphine itself metabolises into at least two important glucoronides, the 6 and 3 variants. One (I think the 6) has much more pain killing power than morphine itself and the other is actually antagonistic to the analgesic properties being sought. Some years ago, anaesthetists who were pain specialists were treating intractable terminal pain by injecting the effective glucuronide directly into the brain (via semi-permanent catheters/needles/canulae or the like). Don’t know if they still do.
I have heard addicts describe the difference between heroin and drugs like methadone as (pardon the graphic language) as like the difference between sex and a handjob.
It’s easy enough to make a time-delay delivery for a drug taken orally: Just embed it in a matrix of something inert and slow to dissolve in the stomach. But that sort of macro-scale solution would be hard to make work in the bloodstream, because if you make your inert pellets too big, they’ll block vessels. I suppose you could put the time-delay mechanism outside of the body, though, with something like a slow IV drip.
Speaking as someone who practices addiction medicine and as a recovering opioid freak, at least part of the level of euphoria one feels from a drug is due to the situation and mindset. Some opioids are definitely more pleasure-inducing than others, but depending on circumstance, the buzz one gets over time from the same drug at same dose will change. Even before habituation sets in.
And oral heroin just doesn’t work well; it gets metabolized by the body quite rapidly, and not a lot of the resultant morphine gets to the brain. That’s why injecting, snorting, and smoking are the preferred routes.
And there’s just no need for heroin as a medicine, as noted earlier. we’ve other opioids that do everything we need such a drug to do.
What is the literal etymology? It’s “a little” sced, I’m guessing, but that’s all I got.
According to the OED it’s from the Latin scheda or scida, meaning a strip of papyrus.
Is that why crack is considered more addictive than cocaine? Because absorption thru the lungs is faster and more reinforcing than absorption thru the mucous membranes?
Regards,
Shodan
More full definition:
[ul]
[li]The drug or other substance has a high potential for abuse. [/li][li]The drug or other substance has no currently accepted medical use in treatment in the United States. [/li][li]There is a lack of accepted safety for use of the drug or other substance under medical supervision.[/li][/ul]
In terms of drugs, there’s an emotional and political stigma attached to heroin that will always supersede the medical evidence. Hardcore anti-smoking groups unstated goal is to get tobacco classified as Schedule I. And as much as I dislike their sanctimonious rhetoric all three of the above qualifications apply to it. And even though vaping meets the third criteria as a (much, much) safer form of smoking it’s still persecuted the same as tobacco.
Yep. Coke and crack are pretty much the same molecule. But crack is in a form which optimizes injection and inhalation.
Per Doctor of Pharmacy Jenni Stein:
Hombre, por mal que lo toque, no me parece justificado…
(pardon the slight hijack)
**Qadgop **- A hospice physician told me years ago that true allergies to morphine are very rare, due to (I think he said) its close resemblance to natural endorphins.
Comment?
mmm
I agree. The vast majority of ‘allergies’ to opioids in general are just side-effects like nausea, vomiting, itching, rash. All from the direct effect of the drug, NOT due to IgE mediated anaphylactoid reactions. Some people have greater reactions to one opioid and lesser to others, often depending on circumstances also.
True allergies are not impossible, but they are not common at all.