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Haloperidol: Difference between revisions
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{{SubstanceBox/Haloperidol}} | {{SubstanceBox/Haloperidol}} | ||
'''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> | '''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. | ||
==History and culture== | ==History and culture== | ||
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==Pharmacology== | ==Pharmacology== | ||
{{pharmacology}} | {{pharmacology}} | ||
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>H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs | | 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== | ||
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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/ | 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. | ||
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*'''Australia:''' The drug is available via prescription only.{{citation needed}} | *'''Australia:''' The drug is available via prescription only.{{citation needed}} | ||
*'''Canada:''' The drug is available via prescription only.{{citation needed}} | *'''Canada:''' The drug is available via prescription only.{{citation needed}} | ||
*'''Germany:''' Haloperidol is a prescription medicine, according to Anlage 1 AMVV.<ref>https://www.gesetze-im-internet.de/amvv/anlage_1.html</ref> | *'''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> | ||
*'''Switzerland:''' Haloperidol is listed as a "Abgabekategorie B" pharmaceutical, which requires a prescription.{{citation needed}} | *'''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 Kingdom:''' Haloperidol is a prescription-only medication.{{citation needed}} | ||