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'''Haloperidol''' (trade name '''Haldol''') is an [[antipsychotic]] drug used to treat a variety of mental disorders, such as schizophrenia, [[mania]], bipolar disorder, [[delirium]], [[psychosis]], Tourette syndrome, as well as other disorders. It was first synthesized in 1958 by Paul Janssen<ref>{{cite book | vauthors=((Sneader, W.)) | date=23 June 2005 | title=Drug Discovery: A History | publisher=John Wiley & Sons | isbn=9780471899792}}</ref> from [[meperidine]]<ref>{{cite book | vauthors=((Ravina, E.)) | date=18 April 2011 | title=The Evolution of Drug Discovery: From Traditional Medicines to Modern Drugs | publisher=John Wiley & Sons | isbn=9783527326693}}</ref>. Haloperidol is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.<ref>http://www.who.int/medicines/publications/essentialmedicines/EML2015_8-May-15.pdf</ref> It is also one of the most frequently prescribed typical antipsychotics and is sometimes carried by medical services as an emergency sedative.
According to Francisco López-Munoz, the "discovery of haloperidol at the end of the 1950s constitutes one of the greatest advances of 20th century psychiatry."<ref name="López-MuñozAlamo2009">{{cite journal|last1=López-Muñoz|first1=Francisco|last2=Alamo|first2=Cecilio|title=The consolidation of neuroleptic therapy: Janssen, the discovery of haloperidol and its introduction into clinical practice|journal=Brain Research Bulletin|volume=79|issue=2|year=2009|pages=130–141|issn=03619230|doi=10.1016/j.brainresbull.2009.01.005}}</ref> This [[antipsychotic]] drug has their origin in the research process of central [[analgesic]] molecules derived from [[pethidine]] and [[methadone]], carried out by the Belgian company Janssen Phamaceutica. After the synthesis of [[phenoperidine]], numerous analogues of this compound were studied, and chemists at Janssen took the decision to substitute the propiophenone group for a butyrophenone group. One of these compounds went the R-1625, a stronger agent with specifically neuroleptic properties but lacking [[morphine]]-like activity.
'''Haloperidol''' (trade name '''Haldol''') is an [[antipsychotic]] drug used to treat Tourette Syndrome, as well as other mental disorders, such as schizophrenia, mania, bipolar disorder, [[delirium]], [[psychosis]] as well a variety of other symptoms. It was first synthesized in 1958 by Paul Janssen<ref>https://books.google.ca/books?id=Cb6BOkj9fK4C&pg=PA124#v=onepage&q&f=false</ref> from [[meperidine]]<ref>https://books.google.ca/books?id=iDNy0XxGqT8C&pg=PA62#v=onepage&q&f=false</ref>. Haloperidol is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.{{citation needed}} It is also one of the most frequently prescribed typical antipsychotics and is sometimes carried by emergency medical services as an emergency sedative.
Haloperidal was synthesized on the 11th February 1958 and received the generic name of haloperidol because of the two halogenated substitutes incorporated into the molecule. Clinical development of haloperidol was conducted, primarily, by psychiatric research team at the University of Liège that confirmed its efficacy in the treatment of various psychiatric disorders such as acute and chronic paranoid [[psychosis]], mania, or chronic treatment-resistant schizophrenia. Under the brand name Haldol((R)), haloperidol was licensed and marketed in Belgium in October 1959.<ref name="López-MuñozAlamo2009" />
Haloperidol is claimed to have contributed substantially to the development of biological psychiatry and currently neuroscience, because it made possible the development of new experimental models for predicting the effects of antipsychotics, and allowed the postulate of the firsts biological hypotheses about the schizophrenia etiology.<ref name="López-MuñozAlamo2009" /> It is included in the World Health Organisation's List of Essential Medicines.<ref name="López-MuñozAlamo2009" />
==Chemistry==
==Chemistry==
{{Chemistry}}
{{Chemistry}}
Haloperidol is a molecule of the [[Butyrophenone]] class.
Haloperidol is a molecule of the [[butyrophenone]] class.
==Pharmacology==
==Pharmacology==
{{pharmacology}}
{{pharmacology}}
As a typical antipsychotic, haloperidol has a diverse pharmacological profile. Primarily, haloperidol acts on [[dopamine]] D<sub>2</sub> receptors as an [[antagonist]], as well as a D<sub>3</sub> inverse [[agonist]]. Haloperidol is also an antagonist of the [[serotonin |5-HT]]<sub>2A</sub> receptor, although this effect is not as powerful as that of quetiapine. Unlike many antipsychotcs, haloperidol has negligible affinity for the muscarinic acetylcholine receptors as well as the histamine receptors, which results in less sedation, weight gain and hypotension.<ref>H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs | http://www.nature.com/npp/journal/v28/n3/full/1300027a.html</ref>
As a typical antipsychotic, haloperidol has a diverse pharmacological profile. Primarily, haloperidol acts on [[dopamine]] D<sub>2</sub> [[receptor]]s as an [[antagonist]], as well as a D<sub>3</sub> inverse [[agonist]]. Haloperidol is also an antagonist of the [[serotonin |5-HT]]<sub>2A</sub> receptor, although this effect is not as powerful as that of [[quetiapine]]. Unlike many antipsychotcs, haloperidol has negligible affinity for the muscarinic acetylcholine receptors as well as the histamine receptors, which results in less sedation, weight gain and hypotension.<ref>{{cite journal | vauthors=((Kroeze, W. K.)), ((Hufeisen, S. J.)), ((Popadak, B. A.)), ((Renock, S. M.)), ((Steinberg, S.)), ((Ernsberger, P.)), ((Jayathilake, K.)), ((Meltzer, H. Y.)), ((Roth, B. L.)) | journal=Neuropsychopharmacology | title=H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs | volume=28 | issue=3 | pages=519–526 | date= March 2003 | url=https://www.nature.com/articles/1300027 | issn=1740-634X | doi=10.1038/sj.npp.1300027}}</ref>
==Subjective effects==
==Subjective effects==
{{effectStub}}
{{effectStub}}
The effects listed below are based upon the [[subjective effects index]] and personal experiences of [[PsychonautWiki]] [[Special:TopUsers|contributors]]. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
{{Preamble/SubjectiveEffects}}
===Physical effects===
{{effects/base
|{{effects/physical|
*'''[[Effect::Constipation]]'''
*'''[[Effect::Constipation]]'''
*'''[[Effect::Dehydration]]'''
*'''[[Effect::Dehydration]]'''
*'''[[Effect::Difficulty urinating]]'''
*'''[[Effect::Difficulty urinating]]'''
*'''[[Effect::Excessive yawning]]'''
*'''[[Effect::Excessive yawning]]'''
*'''[[Effect::Muscle stiffness]]'''
*'''[[Effect::Muscle tension]]'''
*'''[[Effect::Nausea suppression]]'''
*'''[[Effect::Nausea suppression]]'''
*'''[[Effect::Neurotoxicity]]''' - Several lines of evidence suggest that haloperidol exhibits neurotoxicity.<ref name="pmid28738100">{{cite journal | vauthors = Nasrallah HA, Chen AT | title = Multiple neurotoxic effects of haloperidol resulting in neuronal death | journal = Annals of Clinical Psychiatry | volume = 29 | issue = 3 | pages = 195–202 | date = August 2017 | pmid = 28738100 | doi = }}</ref><ref>{{cite journal | vauthors = Pierre JM | title = Time to retire haloperidol? | journal = Current Psychiatry | volume = 19 | issue = 5 | page = 19 | url = https://www.mdedge.com/psychiatry/article/221293/schizophrenia-other-psychotic-disorders }}</ref>
*'''[[Effect::Physical fatigue]]''' - This effect can sometimes result in an inability to perform tasks such as exercise, walking or even sitting.
*'''[[Effect::Physical fatigue]]''' - This effect can sometimes result in an inability to perform tasks such as exercise, walking or even sitting.
Haloperidol [[Toxicity::can have serious side effects at higher dosages]], such as [[Toxicity::risk of having severe extrapyramidal symptoms and muscle rigidity]], which can last for hours.
Haloperidol [[Toxicity::can have serious side effects at higher dosages]], such as [[Toxicity::risk of having severe extrapyramidal symptoms and muscle rigidity]], which can last for hours.
Both typical and atypical antipsychotics can cause tardive dyskinesia.<ref>Tardive dyskinesia and new antipsychotics | http://journals.lww.com/co-psychiatry/pages/articleviewer.aspx?year=2008&issue=03000&article=00012&type=abstract</ref> According to one study, rates are lower with the atypicals at 3.9% as opposed to the typicals at 5.5%.<ref>Tardive dyskinesia and new antipsychotics | http://journals.lww.com/co-psychiatry/pages/articleviewer.aspx?year=2008&issue=03000&article=00012&type=abstract</ref> Switching to these atypicals is an option to minimize symptoms of tardive dyskinesia caused by other atypicals.<ref>Tardive Dyskinesia | http://link.springer.com/article/10.1007%2Fs11940-011-0117-x</ref>
Both typical and atypical antipsychotics can cause tardive dyskinesia.<ref>{{cite journal | vauthors=((Correll, C. U.)), ((Schenk, E. M.)) | journal=Current Opinion in Psychiatry | title=Tardive dyskinesia and new antipsychotics: | volume=21 | issue=2 | pages=151–156 | date= March 2008 | url=http://journals.lww.com/00001504-200803000-00012 | issn=0951-7367 | doi=10.1097/YCO.0b013e3282f53132}}</ref> Rates are lower with the atypicals at 3.9% as opposed to the typicals at 5.5%. Switching to these atypicals is an option to minimize symptoms of tardive dyskinesia caused by other atypicals.<ref>{{cite journal | vauthors=((Aia, P. G.)), ((Revuelta, G. J.)), ((Cloud, L. J.)), ((Factor, S. A.)) | journal=Current Treatment Options in Neurology | title=Tardive Dyskinesia | volume=13 | issue=3 | pages=231–241 | date=1 June 2011 | url=https://doi.org/10.1007/s11940-011-0117-x | issn=1534-3138 | doi=10.1007/s11940-011-0117-x}}</ref>
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.
==Legal issues==
==Legal status==
*'''Australia:''' The drug is available via prescription only.
*'''Australia:''' The drug is available via prescription only.{{citation needed}}
*'''Canada:''' The drug is available via prescription only.
*'''Canada:''' The drug is available via prescription only.{{citation needed}}
*'''United States:''' The drug is available via prescription only.
*'''Germany:''' Haloperidol is a prescription medicine, according to Anlage 1 AMVV.<ref>{{Citation | title=Anlage 1 AMVV - Einzelnorm | url=https://www.gesetze-im-internet.de/amvv/anlage_1.html}}</ref>
*'''United Kingdom:''' Haloperidol is a prescription-only medication.
*'''Switzerland:''' Haloperidol is listed as a "Abgabekategorie B" pharmaceutical, which requires a prescription.{{citation needed}}
*'''United Kingdom:''' Haloperidol is a prescription-only medication.{{citation needed}}
*'''United States:''' The drug is available via prescription only.{{citation needed}}
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Haloperidol (trade name Haldol) is an antipsychotic drug used to treat a variety of mental disorders, such as schizophrenia, mania, bipolar disorder, delirium, psychosis, Tourette syndrome, as well as other disorders. It was first synthesized in 1958 by Paul Janssen[1] from meperidine[2]. Haloperidol is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.[3] It is also one of the most frequently prescribed typical antipsychotics and is sometimes carried by medical services as an emergency sedative.
According to Francisco López-Munoz, the "discovery of haloperidol at the end of the 1950s constitutes one of the greatest advances of 20th century psychiatry."[4] This antipsychotic drug has their origin in the research process of central analgesic molecules derived from pethidine and methadone, carried out by the Belgian company Janssen Phamaceutica. After the synthesis of phenoperidine, numerous analogues of this compound were studied, and chemists at Janssen took the decision to substitute the propiophenone group for a butyrophenone group. One of these compounds went the R-1625, a stronger agent with specifically neuroleptic properties but lacking morphine-like activity.
Haloperidal was synthesized on the 11th February 1958 and received the generic name of haloperidol because of the two halogenated substitutes incorporated into the molecule. Clinical development of haloperidol was conducted, primarily, by psychiatric research team at the University of Liège that confirmed its efficacy in the treatment of various psychiatric disorders such as acute and chronic paranoid psychosis, mania, or chronic treatment-resistant schizophrenia. Under the brand name Haldol((R)), haloperidol was licensed and marketed in Belgium in October 1959.[4]
Haloperidol is claimed to have contributed substantially to the development of biological psychiatry and currently neuroscience, because it made possible the development of new experimental models for predicting the effects of antipsychotics, and allowed the postulate of the firsts biological hypotheses about the schizophrenia etiology.[4] It is included in the World Health Organisation's List of Essential Medicines.[4]
As a typical antipsychotic, haloperidol has a diverse pharmacological profile. Primarily, haloperidol acts on dopamine D2receptors as an antagonist, as well as a D3 inverse agonist. Haloperidol is also an antagonist of the 5-HT2A receptor, although this effect is not as powerful as that of quetiapine. Unlike many antipsychotcs, haloperidol has negligible affinity for the muscarinic acetylcholine receptors as well as the histamine receptors, which results in less sedation, weight gain and hypotension.[5]
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
There are currently 0 experience reports describing the effects of this substance in our experience index. You can also submit your own experience report using the same link.
This toxicity and harm potential section is a stub.
As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. Note: Always conduct independent research and use harm reduction practices if using this substance.
Haloperidol can have serious side effects at higher dosages, such as risk of having severe extrapyramidal symptoms and muscle rigidity, which can last for hours.
Both typical and atypical antipsychotics can cause tardive dyskinesia.[8] Rates are lower with the atypicals at 3.9% as opposed to the typicals at 5.5%. Switching to these atypicals is an option to minimize symptoms of tardive dyskinesia caused by other atypicals.[9]
↑ 4.04.14.24.3López-Muñoz, Francisco; Alamo, Cecilio (2009). "The consolidation of neuroleptic therapy: Janssen, the discovery of haloperidol and its introduction into clinical practice". Brain Research Bulletin. 79 (2): 130–141. doi:10.1016/j.brainresbull.2009.01.005. ISSN0361-9230.
↑Nasrallah HA, Chen AT (August 2017). "Multiple neurotoxic effects of haloperidol resulting in neuronal death". Annals of Clinical Psychiatry. 29 (3): 195–202. PMID28738100.
