Haloperidol
| Summary sheet: Haloperidol |
| Haloperidol | |||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||
| Common names | Haldol | ||||||||||||||||||||||||||
| Substitutive name | Haloperidol | ||||||||||||||||||||||||||
| Systematic name | 4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one | ||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||
| Psychoactive class | Antipsychotic | ||||||||||||||||||||||||||
| Chemical class | Butyrophenone / Phenylpiperidine | ||||||||||||||||||||||||||
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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[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.
History and culture
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]
Chemistry
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This chemistry section is incomplete. You can help by adding to it. |
Haloperidol is a molecule of the butyrophenone class.
Pharmacology
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As a typical antipsychotic, haloperidol has a diverse pharmacological profile. Primarily, haloperidol acts on dopamine D2 receptors 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]
Subjective effects
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This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it. |
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 PsychonautWiki contributors. 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 ☠.
Physical effects 
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- Constipation
- Dehydration
- Difficulty urinating
- Excessive yawning
- Muscle tension
- Nausea suppression
- Neurotoxicity - Several lines of evidence suggest that haloperidol exhibits neurotoxicity.[6][7]
- Physical fatigue - This effect can sometimes result in an inability to perform tasks such as exercise, walking or even sitting.
- Respiratory depression
- Sedation
Experience reports
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and harm potential
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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. |
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]
It is strongly recommended that one use harm reduction practices when using this drug.
Legal status
- Australia: 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.[10]
- 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]
See also
External links
- Haloperidol (Wikipedia)
- Haloperidol (TiHKAL / Isomer Design)
- Haloperidol decanoate (Isomer Design)
- Haloperidol propionate (Isomer Design)
- Haloperidol (DrugBank)
- Haloperidol (Drugs.com)
References
- ↑ Sneader, W. (23 June 2005). Drug Discovery: A History. John Wiley & Sons. ISBN 9780471899792.
- ↑ Ravina, E. (18 April 2011). The Evolution of Drug Discovery: From Traditional Medicines to Modern Drugs. John Wiley & Sons. ISBN 9783527326693.
- ↑ http://www.who.int/medicines/publications/essentialmedicines/EML2015_8-May-15.pdf
- ↑ 4.0 4.1 4.2 4.3 López-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. ISSN 0361-9230.
- ↑ Kroeze, W. K., Hufeisen, S. J., Popadak, B. A., Renock, S. M., Steinberg, S., Ernsberger, P., Jayathilake, K., Meltzer, H. Y., Roth, B. L. (March 2003). "H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs". Neuropsychopharmacology. 28 (3): 519–526. doi:10.1038/sj.npp.1300027. ISSN 1740-634X.
- ↑ Nasrallah HA, Chen AT (August 2017). "Multiple neurotoxic effects of haloperidol resulting in neuronal death". Annals of Clinical Psychiatry. 29 (3): 195–202. PMID 28738100.
- ↑ Pierre JM. "Time to retire haloperidol?". Current Psychiatry. 19 (5): 19.
- ↑ Correll, C. U., Schenk, E. M. (March 2008). "Tardive dyskinesia and new antipsychotics:". Current Opinion in Psychiatry. 21 (2): 151–156. doi:10.1097/YCO.0b013e3282f53132. ISSN 0951-7367.
- ↑ Aia, P. G., Revuelta, G. J., Cloud, L. J., Factor, S. A. (1 June 2011). "Tardive Dyskinesia". Current Treatment Options in Neurology. 13 (3): 231–241. doi:10.1007/s11940-011-0117-x. ISSN 1534-3138.
- ↑ Anlage 1 AMVV - Einzelnorm