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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.
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.
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.
