5 ms·

This article seems pretty low on detail. Almost all of it seems to be talking about, well, not the drug in question. What, exactly, does "10x more powerful" me

This article seems pretty low on detail. Almost all of it seems to be talking about, well, not the drug in question. What, exactly, does "10x more powerful" mean? Potency? Presumably it'd then be prescribed in lower doses?

13of40 8y ago
One hundredth the size of a grain of salt vs. one tenth for fentanyl? Imagine if a piece of dust from that blew into your eye.
- maverick2007 8y ago
  This is probably a stupid question but is it possible for this or for any drug to be absorbed and take effect via the eye? Or does it have to get into the circulatory/digestive system to take effect?
  - sb8244 8y ago
    One of the classic LSD stereotypes is eye drop. Here's a Reddit thread with the question https://www.reddit.com/r/LSD/comments/5aqp8s/lsd_drops_in_eye/ https://www.reddit.com/r/LSD/comments/5aqp8s/lsd_drops_in_ey...
  - mveety 8y ago
    No question is stupid! For fentanyl at least that can totally happen. On of the common ways to administer it is via a transdermal patch. It’s one of the major selling points of fentanyl and why people that need ridiculous amounts of opioids because of burns or cancer like it.
    - ddingus 8y ago
      >No question is stupid! Hear, hear! Especially in this context. I have a modest understanding of just a couple of these compounds. And that comes by way of chronic pain people in my life. Over time, doing the work to better undestand these things has paid off. They, at times, get contradictory or just bad advice, or see something that makes them worry, or think they are in danger somehow. It can be hard to get clarity, and know a change is thearaputic vs compliance related, for example. Anyway, I just liked that you said that and followed up with super easy to understand information.
  - Balgair 8y ago
    Side note: This reminds me of RedEye from Cowboy Bebop: http://cowboybebop.wikia.com/wiki/Red_Eye http://cowboybebop.wikia.com/wiki/Red_Eye
  - imsofuture 8y ago
    You can definitely put liquid LSD in your eye.
- Johnny555 8y ago
  Do they actually dispense drugs in the pure form (i.e. would anyone outside of a pharmacy have access to the drug in a medical setting), or are they diluted in liquid or maybe in a painkilling patch?
  - darpa_escapee 8y ago
    To my knowledge, all legal formulations are diluted for administration and only the manufacturer handles the substance in its pure form. Illicit fentanyl and its derivatives are usually distributed in their pure form, to people who have no training in handling hazardous substances. Sometimes first responders to fentanyl overdoses will not even be able to enter the room of the victim without hazmat suits, because accidentally breathing in fentanyl dust or touching a surface in which the dust has settled could kill them.
teilo 8y ago
It likely means a much more profitable product, since they can get the same effect in 1/10th the dose.
- koolba 8y ago
  Is making the physical product a substantial cost of any non generic medication?
  - deleted 8y ago
    [deleted]
- deleted 8y ago
  [deleted]
- dogma1138 8y ago
  Opioids are measured in binding strength (and so pain relief) with morphine as the baseline which ranges from x0.5-x1 for light opioids like Codine to x100 for Fentanyl. Non opioid pain killers like ibuprofen are usually 1/200-1/300th of morphine.
- PhasmaFelis 8y ago
  Synthesizing the active ingredient is generally very cheap regardless. Research and testing are the big costs in drug development.
  - acct1771 8y ago
    On paper, at least. Marketing's probably up there.
dogma1138 8y ago
It’s the the binding strength which has direct impact on addiction and withdrawal which is a bit scary since Fentanyl is 100 times stronger than morphine already, heroine is only 5 times as strong for comparison.
- jessriedel 8y ago
  Are you talking about binding affinity? Do you have a cite for the relationship between this and the relative addictiveness of opioids given at their normal effective doses? Everything I'm turning up suggests that, in the clinical setting, the "strength of opioids" is a statement about the relative size of the effective dose (in mg). Presumably that's correlated with molecular properties like the affinity, but I don't think that's what the article is talking about.
  - dogma1138 8y ago
    Googling comes up with a WaPo article which seems to cover it pretty well: https://www.washingtonpost.com/graphics/2017/health/opioids-scale/?utm_term=.27b1c87dc55b https://www.washingtonpost.com/graphics/2017/health/opioids-... Edit: Since you edited your question I think you might want to look at opioid agonism across the range of receptors you should probably be able to find quite few NIH studies.
    - jessriedel 8y ago
      I don't think that article answers my question. This seems to be the entire contents that might directly address the issue: > The new, deadlier drugs are altered opioids that bind in more powerful ways to the brain’s receptors and get to the brain more quickly. The combination of factors can make them thousands of times more deadly. > All opioids connect to particular brain and nervous system receptors that exist for the body’s natural painkiller, endorphins... That is the only mention of the word "bind" and the article doesn't contain the word "affinity". It doesn't discuss the relationship between effective-dose-size and potential for addiction, except in cases where it seems to go in the opposite direction of what you suggested: > Methadone is about three times stronger than morphine, but it does not produce a strong euphoric effect. It also lasts much longer and can address physical dependence on other opioids, making it the most common choice for treating opioid addiction.
DevX101 8y ago
Here is an image comparing the lethal dose of heroin vs fentanyl. https://www.statnews.com/wp-content/uploads/2016/09/Heroin-Fentanyl-vials-NHSPFL-1024x576.jpg https://www.statnews.com/wp-content/uploads/2016/09/Heroin-F...
- robbyking 8y ago
  Drugs don't look fun anymore.
- twoheadedboy 8y ago
  That is a ludicrously small amount, holy moly.
  - bootlooped 8y ago
    Wait till you see the lethal dose of one more synthetic opioid: http://mediad.publicbroadcasting.net/p/wosu2/files/styles/medium/public/201705/heroin_fentanyl_carfentanil.jpg http://mediad.publicbroadcasting.net/p/wosu2/files/styles/me...
    - vilhelm_s 8y ago
      That picture is misleading. Although the pain relief effect of carfentalin is ~35 times higher than fentanyl, the lethal dose of both drugs is about the same. So carfentanil is actually safer, in the sense that it has a higher therapeutic index. https://twitter.com/davidjuurlink/status/859227636400349184?lang=en https://twitter.com/davidjuurlink/status/859227636400349184?...
  - jcranmer 8y ago
    Botox is lethal at ~1ng per kg of body weight. It takes 20,000 times that amount of the compound in question to kill you. (These are both using LD50 numbers).
    - Pharmakon 8y ago
      Botox is a refined form of one of the most lethal substances to humans, it is a poison, and most of all it’s not a recreational drug of abuse commonly smuggled around the world. You also can’t absorb it through your skin like fentanyl and carfentanil. Brief contact with botulinum toxin won’t kill you, but brief contact with a rice-grain sized particle of carfentanil can and will.
new12345 8y ago
Power of drug could be quantified based on its impact strength on targeted body functions and side affects on non-targeted ones.
rscho 8y ago
Indeed it is potency. In iv form, sufentanyl is usually prescribed at 1/10th the dose of fentanyl, aiming at an equivalent effect.
grawprog 8y ago
https://en.m.wikipedia.org/wiki/Sufentanil https://en.m.wikipedia.org/wiki/Sufentanil This is the drug the article is talking about. >Sufentanil (R30730, brand name Sufenta) is a synthetic opioid analgesic drug approximately 5 to 10 times more potent than its parent drug, fentanyl, and 500 times as potent as morphine. Structurally, sufentanil differs from fentanyl through the addition of a methoxymethyl group on the piperidine ring (which is believed to reduce duration of action[2]), and the replacement of the phenyl ring by thiophene. Sufentanil first was synthesized at Janssen Pharmaceutica in 1974.[3] >Sufentanil is marketed for use by specialist centers under different trade names, such as Sufenta and Sufentil. Sufentanil with and without lidocaine or mepivacaine is available as a transdermal patch similar to Duragesic in Europe under trade names such as Chronogesic. It is available as a sublingual tablet under the trade name Dsuvia.[4] >Currently sufentanil is the strongest opioid painkiller available for use in humans. Although stronger narcotic pain medications do exist, all medications stronger than sufentanil are approved for veterinary use only.

13of40 8y ago

One hundredth the size of a grain of salt vs. one tenth for fentanyl? Imagine if a piece of dust from that blew into your eye.

maverick2007 8y ago
This is probably a stupid question but is it possible for this or for any drug to be absorbed and take effect via the eye? Or does it have to get into the circulatory/digestive system to take effect?
- sb8244 8y ago
  One of the classic LSD stereotypes is eye drop. Here's a Reddit thread with the question https://www.reddit.com/r/LSD/comments/5aqp8s/lsd_drops_in_eye/ https://www.reddit.com/r/LSD/comments/5aqp8s/lsd_drops_in_ey...
- mveety 8y ago
  No question is stupid! For fentanyl at least that can totally happen. On of the common ways to administer it is via a transdermal patch. It’s one of the major selling points of fentanyl and why people that need ridiculous amounts of opioids because of burns or cancer like it.
  - ddingus 8y ago
    >No question is stupid! Hear, hear! Especially in this context. I have a modest understanding of just a couple of these compounds. And that comes by way of chronic pain people in my life. Over time, doing the work to better undestand these things has paid off. They, at times, get contradictory or just bad advice, or see something that makes them worry, or think they are in danger somehow. It can be hard to get clarity, and know a change is thearaputic vs compliance related, for example. Anyway, I just liked that you said that and followed up with super easy to understand information.
- Balgair 8y ago
  Side note: This reminds me of RedEye from Cowboy Bebop: http://cowboybebop.wikia.com/wiki/Red_Eye http://cowboybebop.wikia.com/wiki/Red_Eye
- imsofuture 8y ago
  You can definitely put liquid LSD in your eye.
Johnny555 8y ago
Do they actually dispense drugs in the pure form (i.e. would anyone outside of a pharmacy have access to the drug in a medical setting), or are they diluted in liquid or maybe in a painkilling patch?
- darpa_escapee 8y ago
  To my knowledge, all legal formulations are diluted for administration and only the manufacturer handles the substance in its pure form. Illicit fentanyl and its derivatives are usually distributed in their pure form, to people who have no training in handling hazardous substances. Sometimes first responders to fentanyl overdoses will not even be able to enter the room of the victim without hazmat suits, because accidentally breathing in fentanyl dust or touching a surface in which the dust has settled could kill them.

teilo 8y ago

It likely means a much more profitable product, since they can get the same effect in 1/10th the dose.

koolba 8y ago
Is making the physical product a substantial cost of any non generic medication?
- deleted 8y ago
  [deleted]
deleted 8y ago
[deleted]
dogma1138 8y ago
Opioids are measured in binding strength (and so pain relief) with morphine as the baseline which ranges from x0.5-x1 for light opioids like Codine to x100 for Fentanyl. Non opioid pain killers like ibuprofen are usually 1/200-1/300th of morphine.
PhasmaFelis 8y ago
Synthesizing the active ingredient is generally very cheap regardless. Research and testing are the big costs in drug development.
- acct1771 8y ago
  On paper, at least. Marketing's probably up there.

dogma1138 8y ago

It’s the the binding strength which has direct impact on addiction and withdrawal which is a bit scary since Fentanyl is 100 times stronger than morphine already, heroine is only 5 times as strong for comparison.

jessriedel 8y ago
Are you talking about binding affinity? Do you have a cite for the relationship between this and the relative addictiveness of opioids given at their normal effective doses? Everything I'm turning up suggests that, in the clinical setting, the "strength of opioids" is a statement about the relative size of the effective dose (in mg). Presumably that's correlated with molecular properties like the affinity, but I don't think that's what the article is talking about.
- dogma1138 8y ago
  Googling comes up with a WaPo article which seems to cover it pretty well: https://www.washingtonpost.com/graphics/2017/health/opioids-scale/?utm_term=.27b1c87dc55b https://www.washingtonpost.com/graphics/2017/health/opioids-... Edit: Since you edited your question I think you might want to look at opioid agonism across the range of receptors you should probably be able to find quite few NIH studies.
  - jessriedel 8y ago
    I don't think that article answers my question. This seems to be the entire contents that might directly address the issue: > The new, deadlier drugs are altered opioids that bind in more powerful ways to the brain’s receptors and get to the brain more quickly. The combination of factors can make them thousands of times more deadly. > All opioids connect to particular brain and nervous system receptors that exist for the body’s natural painkiller, endorphins... That is the only mention of the word "bind" and the article doesn't contain the word "affinity". It doesn't discuss the relationship between effective-dose-size and potential for addiction, except in cases where it seems to go in the opposite direction of what you suggested: > Methadone is about three times stronger than morphine, but it does not produce a strong euphoric effect. It also lasts much longer and can address physical dependence on other opioids, making it the most common choice for treating opioid addiction.

DevX101 8y ago

Here is an image comparing the lethal dose of heroin vs fentanyl. https://www.statnews.com/wp-content/uploads/2016/09/Heroin-Fentanyl-vials-NHSPFL-1024x576.jpg https://www.statnews.com/wp-content/uploads/2016/09/Heroin-F...

robbyking 8y ago
Drugs don't look fun anymore.
twoheadedboy 8y ago
That is a ludicrously small amount, holy moly.
- bootlooped 8y ago
  Wait till you see the lethal dose of one more synthetic opioid: http://mediad.publicbroadcasting.net/p/wosu2/files/styles/medium/public/201705/heroin_fentanyl_carfentanil.jpg http://mediad.publicbroadcasting.net/p/wosu2/files/styles/me...
  - vilhelm_s 8y ago
    That picture is misleading. Although the pain relief effect of carfentalin is ~35 times higher than fentanyl, the lethal dose of both drugs is about the same. So carfentanil is actually safer, in the sense that it has a higher therapeutic index. https://twitter.com/davidjuurlink/status/859227636400349184?lang=en https://twitter.com/davidjuurlink/status/859227636400349184?...
- jcranmer 8y ago
  Botox is lethal at ~1ng per kg of body weight. It takes 20,000 times that amount of the compound in question to kill you. (These are both using LD50 numbers).
  - Pharmakon 8y ago
    Botox is a refined form of one of the most lethal substances to humans, it is a poison, and most of all it’s not a recreational drug of abuse commonly smuggled around the world. You also can’t absorb it through your skin like fentanyl and carfentanil. Brief contact with botulinum toxin won’t kill you, but brief contact with a rice-grain sized particle of carfentanil can and will.

new12345 8y ago

Power of drug could be quantified based on its impact strength on targeted body functions and side affects on non-targeted ones.

rscho 8y ago

Indeed it is potency. In iv form, sufentanyl is usually prescribed at 1/10th the dose of fentanyl, aiming at an equivalent effect.

grawprog 8y ago

https://en.m.wikipedia.org/wiki/Sufentanil https://en.m.wikipedia.org/wiki/Sufentanil This is the drug the article is talking about. >Sufentanil (R30730, brand name Sufenta) is a synthetic opioid analgesic drug approximately 5 to 10 times more potent than its parent drug, fentanyl, and 500 times as potent as morphine. Structurally, sufentanil differs from fentanyl through the addition of a methoxymethyl group on the piperidine ring (which is believed to reduce duration of action[2]), and the replacement of the phenyl ring by thiophene. Sufentanil first was synthesized at Janssen Pharmaceutica in 1974.[3] >Sufentanil is marketed for use by specialist centers under different trade names, such as Sufenta and Sufentil. Sufentanil with and without lidocaine or mepivacaine is available as a transdermal patch similar to Duragesic in Europe under trade names such as Chronogesic. It is available as a sublingual tablet under the trade name Dsuvia.[4] >Currently sufentanil is the strongest opioid painkiller available for use in humans. Although stronger narcotic pain medications do exist, all medications stronger than sufentanil are approved for veterinary use only.