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haloperidol thoughts

T

toxide

Bluelighter
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Mar 21, 2006
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I was very curios about this. I have a mixed understanding of it. I heard it's an nmda antagonist(nonselective?)which I assume means it can be dissociative at the right dose. It's a sigma agonist which means what?---absolutely nothing?? what are sigma agonists? and it's either a dopamine agonist or antagonist? My question is, at a high enough dose which should be(anyone know??) would this have atleast some semi-interesting dissociative effects. I've heard alot of people talk about it sucking alot in intended doses, but what about at much higher doses? Altho if it does blocks dopamine then it may be nasty stuff. It's chem structure is similar to other nmda antagonists like ifenprodil and similar chems.
 
Haloperidol is an old neuroleptic/antipsychotic, it's a Dopamine D1 and D2 antagonist.
I don't think it has dissociative properties, and I don't think it's a NMDA antagonist.
It is used for the treatment of schizophrenic disorders, severe psychotic conditions, manic states, behavioral anomalies, Huntington's chorea and Tourette's disorder; IT SHOULDN'T BE USED FOR ANY OTHER PURPOSE!

It is dangerous to take doses higher than the dose prescribed (usually 5mg).
It has many unpleasant and dangerous side-effects (extrapyramidal syndrom, dyskinesia, akathisia....), so if you use it, stay not far from your doctor or from an hopital center.

And don't forget that older neuroleptics like Haloperidol cause Neuroleptic Malignant Syndrome in 1% of the persons using it. This syndrom is often lethal/deadly, and if it doesn't kill you, it causes very strong and unpleasant symptoms.
Be careful and don't use Haloperidol unless you have schizophrenic or psychotic disorders.
 
well i am sort of surprised to see that according to this site:http://pdsp.cwru.edu/pdsp.phphaloperidol does seem to have some affinity for some glutamate-nmda receptors....but that site tells only affinity and not whether it is antagonistic or agonistic.

however, since the typical antipsychotics (thorazine or chlorpromazine, haloperidol, stelazine and so forth) were used in mega doses (often much,much larger than the 5 mg dose jason noted:\ ) to control the behavior of many severely mentally ill patients when the drugs first came out, i think we can safely assume that the drugs didn't have strong dissociative properties...i doubt the doctors wanted people that were already difficult to control in a dissociated state. in fact, the main effect of those drugs was indifference. chlorpromazine was initially tried as part of an anesthetic concoction before surgery, and the doctors noted that the patients seemed to be more indifferent to the pain though the drug was not a good anesthetic. in the papers written up, the doctors even suggested briefly that chlorpromazine might have an application in mental health because of its indifference-producing qualities. thus, i think these drugs would be more known for their ability to produce indifference rather than dissociation.http://pdsp.cwru.edu/pdsp.php
 
Well it is an nmda antagonist but I guess there is alot of confusion as to it works as NMDAaa, it's related to 4substitutedphenylpiperidines like ifenprodil of which some are dissociative but haldol i think might be selective and doesn't directly block, I assume that means it's more of a modulater like magnesium
 
If your intent is to get some dissociative activity out of it, forget it as the dose required would entail stopping thinking alltogether. The major tranquillizer aspect would mean that you'd 'not be there' to experience any effects, but 'chemically coshed' into an automaton/zombie state
 
I just looked up the structure of haldol a couple weeks ago for the first time. It has a horrendous reputation for EPA (extrapyramidal axis) side effects, the most notorious of which being tardrive dyskinesia. A thought that I had, which is probably untrue, is that there might be a possibility some of these effects come from an elimination of the tertiary alcohol to create a double bond, which in effect would create a species with chemical similarity to MPTP. Anyone have any thoughts to refute this?
 
Here is an article that seems to agree that some of the 4-hydroxy-4-aryl-piperidine based compounds do carry certain risks that arent always taken seriously. I think the take home message is that even if these problems arent always addressed there is still a certain level of hidden danger.
 
Given that kind of damning information I wonder why haldol is still on the market. That sounds like some pretty huge liability.
 
hussness said:
Given that kind of damning information I wonder why haldol is still on the market. That sounds like some pretty huge liability.
Click to expand...

Because I think it's the only neuroleptic/antipsychotic that works 1 month after only 1 or 2 injections....
 
risperidone is also available in an injection that lasts a month (there may be a few others as well)

the reason why it is still available is because despite the risks, it's the best option for some portion of the people who need psychiatric medications....granted, it may be more a second line medication at this point due to TD risk, but everyone responds so differently to medications that having a lot of options means that more people find something that works
 
Smyth, Thanks for the article. It's great.
some of the 4-hydroxy-4-aryl-piperidine based compounds do carry certain risks that arent always taken seriously. I think the take home message is that even if these problems arent always addressed there is still a certain level of hidden danger.
Click to expand...
BTW the same metabolites are determined from haloperidol, as you suggested. I don't have the articles, but the refs are:
H. Rollema, M. Skolnick, J. D'Engelbronner et al. J. Pharmacol. Exp. Ther. 1994 (268), p. 380
and
J. Fang, D. Zuo and P.H. Yu; Psychopharmacology(Berl) 1995 (121); p. 373

Beta carbolines might undergo the same metabolism.
 
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