5 ms·

From Wikipedia: "In veterinary medicine, the alpha-2 antagonist atipamezole is used to reverse the effects of xylazine or the related drug dexmedetomidine, but

From Wikipedia: "In veterinary medicine, the alpha-2 antagonist atipamezole is used to reverse the effects of xylazine or the related drug dexmedetomidine, but while this has been tested in humans in Phase I trials, it is not an approved medical treatment for xylazine overdose.

A_D_E_P_T 4y ago
"Not approved" simply because it hasn't gone through the drug approval process -- because, among other reasons, xylazine isn't approved for use in humans in the first place. Not because it doesn't necessarily work or would necessarily be harmful. Granted, atipamezole seems somewhat "cleaner" than yohimbine, which is a natural product with quite a few off-target effects.
- mbreese 4y ago
  Also probably not approved because of a lack of randomized, double blind studies. But it would be really hard to run a study for a treatment like this. I can’t even imagine trying to get informed consent to try and enroll someone on the trial. So, without that, the best you could do would be to find a drug that is approved for something else that can be used off label. I don’t think there are any easy answers here.
  - A_D_E_P_T 4y ago
    > So, without that, the best you could do would be to find a drug that is approved for something else that can be used off label. Xylazine has a very rapid onset and a short half-life. So, as it can take >40 minutes for orally-administered drugs to be absorbed, there are really only two options that _might_ be legal and effective. 1) Administer an FDA-approved alpha-2 antagonist intravenously. There are no good options here. AFAIK, the only FDA-approved alpha-2 antagonist that's available as an intravenous injection is Thorazine -- and it does a hell of a lot besides counteract alpha-2 adrenoceptor activation. It's also an alpha-1 antagonist, dopamine antagonist, serotonin antagonist, and more. This likely makes it a little bit unpredictable in drug overdose scenarios. 2) Sidestep FDA approval with a fast-acting yohimbine nasal spray, administered as a "dietary supplement." The FDA process is a terrible roadblock in situations like this. Intravenous atipamezole, which would be much better than either of the two options above, is available for veterinary use, but would be totally illegal for use in humans. (Like xylazine itself!)
- jharbison 3y ago
  Does it really matter if it hasn't gone through any testing? Have we forgotten about the Covid shot not going through any trials? We have people dropping dead left and right due Narcan not reversing the effects. The FDA NEEDS to come up with something that acts both like Narcan and Atipamezole, so we can start saving lives!

A_D_E_P_T 4y ago

"Not approved" simply because it hasn't gone through the drug approval process -- because, among other reasons, xylazine isn't approved for use in humans in the first place. Not because it doesn't necessarily work or would necessarily be harmful. Granted, atipamezole seems somewhat "cleaner" than yohimbine, which is a natural product with quite a few off-target effects.

mbreese 4y ago
Also probably not approved because of a lack of randomized, double blind studies. But it would be really hard to run a study for a treatment like this. I can’t even imagine trying to get informed consent to try and enroll someone on the trial. So, without that, the best you could do would be to find a drug that is approved for something else that can be used off label. I don’t think there are any easy answers here.
- A_D_E_P_T 4y ago
  > So, without that, the best you could do would be to find a drug that is approved for something else that can be used off label. Xylazine has a very rapid onset and a short half-life. So, as it can take >40 minutes for orally-administered drugs to be absorbed, there are really only two options that _might_ be legal and effective. 1) Administer an FDA-approved alpha-2 antagonist intravenously. There are no good options here. AFAIK, the only FDA-approved alpha-2 antagonist that's available as an intravenous injection is Thorazine -- and it does a hell of a lot besides counteract alpha-2 adrenoceptor activation. It's also an alpha-1 antagonist, dopamine antagonist, serotonin antagonist, and more. This likely makes it a little bit unpredictable in drug overdose scenarios. 2) Sidestep FDA approval with a fast-acting yohimbine nasal spray, administered as a "dietary supplement." The FDA process is a terrible roadblock in situations like this. Intravenous atipamezole, which would be much better than either of the two options above, is available for veterinary use, but would be totally illegal for use in humans. (Like xylazine itself!)
jharbison 3y ago
Does it really matter if it hasn't gone through any testing? Have we forgotten about the Covid shot not going through any trials? We have people dropping dead left and right due Narcan not reversing the effects. The FDA NEEDS to come up with something that acts both like Narcan and Atipamezole, so we can start saving lives!