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tranquilizer (trade name Haldol) used to treat some psychotic disorders and Tourettes syndrome (同)Haldol

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/09/17 19:10:06」(JST)

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Haloperidol, marketed under the trade name Haldol among others, is a typical antipsychotic medication.^[3] Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, nausea and vomiting, delirium, agitation, acute psychosis, and hallucinations in alcohol withdrawal.^[3]^[4]^[5] It may be used by mouth, as an injection into a muscle, or intravenously. Haloperidol typically works within thirty to sixty minutes. A long-acting formulation may be used as an injection every four weeks in people with schizophrenia or related illnesses, who either forget or refuse to take the medication by mouth.^[3]

Haloperidol may result in a movement disorder known as tardive dyskinesia which may be permanent. Neuroleptic malignant syndrome and QT interval prolongation may occur. In older people with psychosis due to dementia it results in an increased risk of death.^[3] When taken during pregnancy it may result in problems in the infant.^[3]^[6] It should not be used in people with Parkinson's disease.^[3]

Haloperidol was discovered in 1958 by Paul Janssen.^[7] It was made from meperidine.^[8] It is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.^[9] It is the most commonly used typical antipsychotic.^[10] The yearly cost of the typical dose of haloperidol is about 20 to 800 pounds (30 to 1,250 US dollars) in the United Kingdom.^[10]^[11] The cost in the United States is around 250 US dollars a year.^[12]

1 Medical uses
- 1.1 Pregnancy and lactation
- 1.2 Other considerations
2 Adverse effects
- 2.1 Contraindications
- 2.2 Special cautions
- 2.3 Interactions
3 Overdose
- 3.1 Symptoms
- 3.2 Treatment
- 3.3 Prognosis
4 Pharmacology
5 Pharmacokinetics
- 5.1 Oral
- 5.2 Intramuscular injections
- 5.3 Intravenous injections
- 5.4 Therapeutic concentrations
- 5.5 Distribution and metabolism
6 History
- 6.1 Brand names
7 Veterinary use
8 References
9 External links

Medical uses

Haloperidol is used in the control of the symptoms of:

Schizophrenia^[13]
Acute psychosis, such as drug-induced psychosis caused by LSD, psilocybin, amphetamines, ketamine,^[14] and phencyclidine,^[15] and psychosis associated with high fever or metabolic disease
Hyperactivity, aggression
Hyperactive delirium (to control the agitation component of delirium)
Otherwise uncontrollable, severe behavioral disorders in children and adolescents
Agitation and confusion associated with cerebral sclerosis
Adjunctive treatment of alcohol and opioid withdrawal
Treatment of severe nausea and emesis in postoperative and palliative care, especially for palliating adverse effects of radiation therapy and chemotherapy in oncology
Treatment of neurological disorders, such as tic disorders such as Tourette syndrome, and chorea
Therapeutic trial in personality disorders, such as borderline personality disorder
Treatment of intractable hiccups^[16]^[17]
Alcohol-induced psychosis
Hallucinations in alcohol withdrawal^[4]

Haloperidol was considered indispensable for treating psychiatric emergency situations,^[18]^[19] although the newer atypical drugs have gained greater role in a number of situations as outlined in a series of consensus reviews published between 2001 and 2005.^[20]^{[needs update]}^[21]^[22]^[23]

A multiple-year study suggested this drug and other neuroleptic antipsychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often make their condition worse and its withdrawal was even beneficial for some cognitive and functional measures.^[24]

Pregnancy and lactation

Data from animal experiments indicate haloperidol is not teratogenic, but is embryotoxic in high doses. In humans, no controlled studies exist. Reports in pregnant women revealed possible damage to the fetus, although most of the women were exposed to multiple drugs during pregnancy. In addition, reports indicate neonates exposed to antipsychotic drugs are at risk for extrapyramidal and/or withdrawal symptoms following delivery, such as agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder. Following accepted general principles, haloperidol should be given during pregnancy only if the benefit to the mother clearly outweighs the potential fetal risk.^[13]

Haloperidol, when given to lactating women, is found in significant amounts in their milk. Breastfed children sometimes show extrapyramidal symptoms. If the use of haloperidol during lactation seems indicated, the benefit for the mother should clearly outweigh the risk for the child, or breastfeeding should be stopped.^{[citation needed]}

Other considerations

Skeletal formula of haloperidol decanoate. The decanoate group is highlighted in red.

During long-term treatment of chronic psychiatric disorders, the daily dose should be reduced to the lowest level needed for maintenance of remission. Sometimes, it may be indicated to terminate haloperidol treatment gradually.^[25] In addition, during long-term use, routine monitoring including measurement of BMI, blood pressure, fasting blood sugar, and lipids, is recommended due to the risk of side effects.^[26]

Other forms of therapy (psychotherapy, occupational therapy/ergotherapy, or social rehabilitation) should be instituted properly.^{[citation needed]} PET imaging studies have suggested low doses are preferable. Clinical response was associated with at least 65% occupancy of D2 receptors, while greater than 72% was likely to cause hyperprolactinaemia and over 78% associated with extrapyramidal side effects. Doses of haloperidol greater than 5 mg increased the risk of side effects without improving efficacy.^[27] Patients responded with doses under even 2 mg in first-episode psychosis.^[28] For maintenance treatment of schizophrenia, an international consensus conference recommended a reduction dosage by about 20% every 6 months until a minimal maintenance dose is established.^[26]

Depot forms are also available; these are injected deeply intramuscularly at regular intervals. The depot forms are not suitable for initial treatment, but are suitable for patients who have demonstrated inconsistency with oral dosages.^{[citation needed]}

The decanoate ester of haloperidol (haloperidol decanoate, trade names Haldol decanoate, Halomonth, Neoperidole) has a much longer duration of action, so is often used in people known to be noncompliant with oral medication. A dose is given by intramuscular injection once every two to four weeks.^[29] The IUPAC name of haloperidol decanoate is [4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]piperidin-4-yl] decanoate.

Topical formulations of haloperidol should not be used as treatment for nausea because research does not indicate this therapy is more effective than alternatives.^[30]

Adverse effects

Sources for the following lists of adverse effects^[31]^[32]^[33]^[34]

As haloperidol is a high-potency typical antipsychotic, it tends to produce significant extrapyramidal side effects. According to a 2013 meta-analysis of the comparative efficacy and tolerability of 15 antipsychotic drugs it was the most prone of the 15 for causing extrapyramidal side effects.^[35]

Common (>1% incidence)

Extrapyramidal side effects including:
- Dystonia
- Muscle rigidity
- Akathisia
- Parkinsonism
Hypotension
Anticholinergic side effects such as: (These adverse effects are more common than with lower-potency typical antipsychotics, such as chlorpromazine and thioridazine.)
- Constipation
- Dry mouth
- Blurred vision
Somnolence (which is not a particularly prominent side effect, as is supported by the results of the aforementioned meta-analysis.^[35])

Unknown frequency

Prolonged QT interval
Orthostatic hypotension
Increased respiratory rate
Anemia
Visual disturbances
Headache

Rare (<1% incidence)

Jaundice
Hepatitis
Cholestasis
Acute hepatic failure
Liver function test abnormal
Hypoglycemia
Hyperglycemia
Hyponatremia
Anaphylactic reaction
Hypersensitivity
Agranulocytosis
Neutropenia
Leukopenia
Thrombocytopania
Pancytopenia
Psychotic disorder
Agitation
Confusional state
Depression
Insomnia
Seizure
Torsades de pointes
Ventricular fibrillation
Ventricular tachycardia
Extrasystoles
Bronchospasm
Laryngospasm
Laryngeal edema
Dyspnea
Nausea
Vomiting
Leukocytoclastic vasculitis
Dermatitis exfoliative
Urticaria
Photosensitivity reaction
Rash
Pruritis
Hyperhidrosis
Urinary retention
Priapism
Gynecomastia
Sudden death
Face edema
Edema
Hypothermia
Hyperthermia
Injection site abscess
Anorexia
Pulmonary embolism
Tardive dyskinesia
Cataracts
Retinopathy
Neuroleptic malignant syndrome

Contraindications

Pre-existing coma, acute stroke
Severe intoxication with alcohol or other central depressant drugs
Known allergy against haloperidol or other butyrophenones or other drug ingredients
Known heart disease, when combined will tend towards cardiac arrest^{[citation needed]}

Special cautions

Pre-existing Parkinson's disease^[36] or dementia with Lewy bodies
Patients at special risk for the development of QT prolongation (hypokalemia, concomitant use of other drugs causing QT prolongation)
Impaired liver function, as haloperidol is metabolized and eliminated mainly by the liver
In patients with hyperthyreosis, the action of haloperidol is intensified and side effects are more likely.
IV injections: risk of hypotension or orthostatic collapse
Patients with a history of leukopenia: a complete blood count should be monitored frequently during the first few months of therapy and discontinuation of the drug should be considered at the first sign of a clinically significant decline in white blood cells.^[13]
Elderly patients with dementia-related psychosis: analysis of 17 trials showed the risk of death in this group of patients was 1.6 to 1.7 times that of placebo-treated patients. Most of the causes of death were either cardiovascular or infectious in nature. It is not clear to what extent this observation is attributed to antipsychotic drugs rather than the characteristics of the patients. The drug bears a boxed warning about this risk.^[13]

Interactions

Other central depressants (alcohol, tranquilizers, narcotics): actions and side effects of these drugs (sedation, respiratory depression) are increased. In particular, the doses of concomitantly used opioids for chronic pain can be reduced by 50%.
Methyldopa: increased risk of extrapyramidal side effects and other unwanted central effects
Levodopa: decreased action of levodopa
Tricyclic antidepressants: metabolism and elimination of tricyclics significantly decreased, increased toxicity noted (anticholinergic and cardiovascular side effects, lowering of seizure threshold)
Lithium: rare cases of the following symptoms have been noted: encephalopathy, early and late extrapyramidal side effects, other neurologic symptoms, and coma.^[37]
Guanethidine: antihypertensive action antagonized
Epinephrine: action antagonized, paradoxical decrease in blood pressure may result
Amphetamine and methylphenidate: counteracts increased action of norepinephrine and dopamine in patients with narcolepsy or ADD/ADHD
Amiodarone: Q-Tc interval prolongation (potentially dangerous change in heart rhythm).^[38]
Other drugs metabolized by the CYP3A4 enzyme system: inducers such as carbamazepine, phenobarbital, and rifampicin decrease plasma levels and inhibitors such as quinidine, buspirone, and fluoxetine increase plasma levels^[13]

Overdose

Symptoms

Symptoms are usually due to side effects. Most often encountered are:

Severe extrapyramidal side effects with muscle rigidity and tremors, akathisia, etc.
Hypotension or hypertension
Sedation
Anticholinergic side effects (dry mouth, constipation, paralytic ileus, difficulties in urinating, decreased perspiration)
Coma in severe cases, accompanied by respiratory depression and massive hypotension, shock
Rarely, serious ventricular arrhythmia (torsades de pointes), with or without prolonged QT-time

Treatment

Treatment is merely symptomatic and involves intensive care with stabilization of vital functions. In early detected cases of oral overdose, induction of emesis, gastric lavage, and the use of activated charcoal can all be tried. Epinephrine is avoided for treatment of hypotension and shock, because its action might be reversed. In the case of a severe overdose, antidotes such as bromocryptine or ropinirole may be used to treat the extrapyramidal effects caused by haloperidol, acting as dopamine receptor agonists.^{[citation needed]} ECG and vital signs should be monitored especially for QT prolongation and severe arrhythmias should be treated with antiarrhythmic measures.^[13]

Prognosis

In general, the prognosis of overdose is good, and lasting damage is not known, provided the person has survived the initial phase. An overdose of haloperidol can be fatal.^[39]

Pharmacology

Haloperidol, 10-mg oral tablet

Haloperidol is a typical butyrophenone type antipsychotic that exhibits high affinity dopamine D₂ receptor antagonism and slow receptor dissociation kinetics.^[40] It has effects similar to the phenothiazines.^[17] The drug binds preferentially to D₂ and α₁ receptors at low dose (ED₅₀ = 0.13 and 0.42 mg/kg, respectively), and 5-HT₂ receptors at a higher dose (ED₅₀ = 2.6 mg/kg). Given that antagonism of D₂ receptors is more beneficial on the positive symptoms of schizophrenia and antagonism of 5-HT₂ receptors on the negative symptoms, this characteristic underlies haloperidol's greater effect on delusions, hallucinations and other manifestations of psychosis.^[41] Haloperidol's negligible affinity for histamine H₁ receptors and muscarinic M₁ acetylcholine receptors yields an antipsychotic with a lower incidence of sedation, weight gain, and orthostatic hypotension though having higher rates of treatment emergent extrapyramidal symptoms.

Haloperidol acts on these receptors: (K_i)

D₁ (silent antagonist) — Unknown efficiency^{[citation needed]}
D₅ (silent antagonist) — Unknown efficiency^{[citation needed]}
D₂ (inverse agonist) — 1.55 nM^[42]
D₃ (inverse agonist) — 0.74 nM^[43]
D₄ (inverse agonist) — 5–9 nM^[44]
σ₁ (irreversible inactivation by haloperidol metabolite HPP⁺) – 3 nM^[45]
σ₂ (agonist): 54 nM^[46]
5HT_1A receptor agonist – 1927 nM^[47]
5HT_2A (silent antagonist) – 53 nM^[47]
5HT_2C (silent antagonist) – 10,000 nM^[47]
5HT₆ (silent antagonist) – 3666 nM^[47]
5HT₇ (irreversible silent antagonist) — 377.2 nM^[47]
H₁ (silent antagonist) — 1,800 nM^[47]
M₁ (silent antagonist) — 10,000 nM^[47]
α_1A (silent antagonist) — 12 nM^[47]
α_2A (silent antagonist) — 1130 nM^[47]
α_2B (silent antagonist) — 480 nM^[47]
α_2C (silent antagonist) — 550 nM^[47]
NR1/NR2B subunit containing NMDA receptor (antagonist; ifenprodil site): IC₅₀ — 2,000 nM^[48]

Pharmacokinetics

Oral

The bioavailability of oral haloperidol ranges from 60–70%. However, there is a wide variance in reported mean T_max and T_1/2 in different studies, ranging from 1.7 to 6.1 hours and 14.5 to 36.7 hours respectively.^[1]

Intramuscular injections

The drug is well and rapidly absorbed with a high bioavailability when injected intramuscularly. The T_max is 20 minutes in healthy individuals and 33.8 minutes in patients with schizophrenia. The mean T_1/2 is 20.7 hours.^[1] The decanoate injectable formulation is for intramuscular administration only and is not intended to be used intravenously. The plasma concentrations of haloperidol decanoate reach a peak at about six days after the injection, falling thereafter, with an approximate half-life of three weeks.^[49]

Intravenous injections

The bioavailability is 100% in intravenous (IV) injection, and the very rapid onset of action is seen within seconds. The T_1/2 is 14.1 to 26.2 hours. The apparent volume of distribution is between 9.5 and 21.7 L/kg.^[1] The duration of action is four to six hours. If haloperidol is given as a slow IV infusion, the onset of action is slowed, and the duration of action is prolonged.^{[citation needed]}

Haloperidol for injection

Therapeutic concentrations

Plasma levels of four to 25 micrograms per liter are required for therapeutic action. The determination of plasma levels can be used to calculate dose adjustments and to check compliance, particularly in long-term patients. Plasma levels in excess of the therapeutic range may lead to a higher incidence of side effects or even pose the risk of haloperidol intoxication.^{[citation needed]}

The concentration of haloperidol in brain tissue is about 20-fold higher compared to blood levels. It is slowly eliminated from brain tissue,^[50] which may explain the slow disappearance of side effects when the medication is stopped.^[50]^[51]

Distribution and metabolism

Haloperidol is heavily protein bound in human plasma, with a free fraction of only 7.5 to 11.6%. It is also extensively metabolized in the liver with only about 1% of the administered dose excreted unchanged in the urine. The greatest proportion of the hepatic clearance is by glucuronidation, followed by reduction and CYP-mediated oxidation, primarily by CYP3A4.^[1]

History

Haloperidol was discovered by Paul Janssen.^[52] It was developed in 1958 at the Belgian company Janssen Pharmaceutica and submitted to the first of clinical trials in Belgium later that year.^[53]^[54]

Haloperidol was approved by the U.S. Food and Drug Administration (FDA) on April 12, 1967; it was later marketed in the U.S. and other countries under the brand name Haldol by McNeil Laboratories.^{[citation needed]}

Brand names

Haloperidol is the INN, BAN, USAN, AAN approved name.

It is sold under the tradenames Aloperidin, Bioperidolo, Brotopon, Dozic, Duraperidol (Germany), Einalon S, Eukystol, Haldol (common tradename in the US and UK), Halosten, Keselan, Linton, Peluces, Serenace and Sigaperidol.^{[citation needed]}

Veterinary use

Haloperidol is also used on many different kinds of animals. It appears to be particularly successful when given to birds, e.g., a parrot that will otherwise continuously pluck its feathers out.^[55]

References

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^ Ilyin, VI; Whittemore, ER; Guastella, J; Weber, E; Woodward, RM (1996). "Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol". Molecular Pharmacology. 50 (6): 1541–50. PMID 8967976.
^ "drugs.com".
^ ^a ^b Kornhuber, Johannes; Schultz, Andreas; Wiltfang, Jens; Meineke, Ingolf; Gleiter, Christoph H.; Zöchling, Robert; Boissl, Karl-Werner; Leblhuber, Friedrich; Riederer, Peter (1999). "Persistence of Haloperidol in Human Brain Tissue". The American Journal of Psychiatry. 156 (6): 885–90. doi:10.1176/ajp.156.6.885. PMID 10360127.
^ Kornhuber, Johannes; Wiltfang, Jens; Riederer, Peter; Bleich, Stefan (2006). "Neuroleptic drugs in the human brain: Clinical impact of persistence and region-specific distribution". European Archives of Psychiatry and Clinical Neuroscience. 256 (5): 274–80. doi:10.1007/s00406-006-0661-7. PMID 16788768.
^ Healy, David (1996). The psychopharmacologists. 1. London: Chapman and Hall. ISBN 978-1-86036-008-4. ^{[page needed]}
^ Granger, Bernard; Albu, Simona (2005). "The Haloperidol Story". Annals of Clinical Psychiatry. 17 (3): 137–40. doi:10.1080/10401230591002048. PMID 16433054.
^ Lopez-Munoz, Francisco; Alamo, Cecilio (2009). "The Consolidation of Neuroleptic Therapy: Janssen, the Discovery of Haloperidol and Its Introduction into Clinical Practice". Brain Research Bulletin. 79: 130–141. doi:10.1016/j.brainresbull.2009.01.005. PMID 19186209.
^ "Veterinary:Avian at Lloyd Center Pharmacy".

External links

Rx-List.com – Haloperidol
Medline plus – Haloperidol
Swiss scientific information on Haldol
"WHO Model List of Essential Medicines" (PDF) (16th list (updated) ed.). World Health Organization. March 2010. Retrieved 2010-09-14.
U.S. National Library of Medicine: Drug Information Portal - Haloperidol

UpToDate Contents

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1. 統合失調症に対する薬物療法：持効性抗精神病薬注射製剤 pharmacotherapy for schizophrenia long acting injectable antipsychotic drugs
2. 第1世代抗精神病剤：薬理学、投与、および副作用の比較 first generation antipsychotic medications pharmacology administration and comparative side effects
3. せん妄および急性錯乱状態：予防、治療、および予後 delirium and acute confusional states prevention treatment and prognosis
4. 危篤状態の成人における鎮静鎮痛剤：特性、投与レジメン、および副作用 sedative analgesic medications in critically ill adults properties dosage regimens and adverse effects
5. 授乳中の乳幼児：物質使用障害による抗精神病薬、リチウム、および薬剤への曝露の安全性 breastfeeding infants safety of exposure to antipsychotics lithium and medications for substance use disorders

English Journal

Cost-Effectiveness of Long-Acting Injectable Paliperidone Palmitate Versus Haloperidol Decanoate in Maintenance Treatment of Schizophrenia.

Rosenheck RA1, Leslie DL1, Sint KJ1, Lin H1, Li Y1, McEvoy JP1, Byerly MJ1, Hamer RM1, Swartz MS1, Stroup TS1.
Psychiatric services (Washington, D.C.).Psychiatr Serv.2016 Jun 1:appips201500447. [Epub ahead of print]
OBJECTIVE: This study assessed the relative cost-effectiveness of haloperidol decanoate (HD), a first-generation long-acting injectable (LAI) antipsychotic, and paliperidone palmitate (PP), a second-generation LAI antipsychotic.METHODS: A double-blind, randomized 18-month clinical trial conducted at
PMID 27247177

Cost Effectiveness of Paliperidone Long-Acting Injectable Versus Other Antipsychotics for the Maintenance Treatment of Schizophrenia in France.

Druais S1, Doutriaux A2, Cognet M2, Godet A3, Lançon C4, Levy P5, Samalin L6, Guillon P3.
PharmacoEconomics.Pharmacoeconomics.2016 Apr;34(4):363-91. doi: 10.1007/s40273-015-0348-x.
BACKGROUND: French clinical recommendations suggest prescribing long-acting injectable (LAI) antipsychotics to patients with a maintenance treatment indication in schizophrenia. Despite this, and due to their relatively high acquisition and administration costs, LAIs are still underused in clinical
PMID 26883132

Japanese Journal

^<19>F-magnetic resonance spectroscopy and chemical shift imaging for schizophrenic patients using haloperidol decanoate

Psychiatry and clinical neurosciences 56(6), 637-642, 2002-12-01
NAID 10018974982

筋肉注射で使用される持効性ハロペリドール使用中に発生した悪性症候群の1例

日本救急医学会雑誌 13(5), 269-273, 2002-05-10
NAID 10008942086

「デカン酸ハロペリドール」

Haloperidol
Systematic (IUPAC) name
	4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
Clinical data
Pronunciation	/hæloʊpɛridɒl/
Trade names	Haldol
AHFS/Drugs.com	Monograph
MedlinePlus	a682180
Pregnancy; category	AU: C; US: C (Risk not ruled out); ;
Routes of; administration	Oral, IM, IV, depot (as decanoate ester)
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	60–70% (Oral)
Protein binding	~90%
Metabolism	Liver-mediated
Biological half-life	14–26 hours (IV), 20.7 hours (IM), 14–37 hours (oral)
Excretion	Biliary (hence in feces) and in urine
Identifiers
CAS Number	52-86-8
ATC code	N05AD01 (WHO)
PubChem	CID 3559
IUPHAR/BPS	86
DrugBank	DB00502
ChemSpider	3438
UNII	J6292F8L3D
KEGG	D00136
ChEBI	CHEBI:5613
ChEMBL	CHEMBL54
Chemical data
Formula	C21H23ClFNO2
Molar mass	375.9 g/mol
	SMILES c1cc(ccc1C(=O)CCCN2CCC(CC2)(c3ccc(cc3)Cl)O)F ;
	InChI InChI=1S/C21H23ClFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2 ; Key:LNEPOXFFQSENCJ-UHFFFAOYSA-N ;
(verify)

　　[★]

英: haloperidol decanoate
関: ハロペリドール

「decanoate」

　　[★]

デカン酸、(化合物)カン酸エステル

関: capric acid、decanoic acid

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[24] Ballard, Clive; Lana, Marisa Margallo; Theodoulou, Megan; Douglas, Simon; McShane, Rupert; Jacoby, Robin; Kossakowski, Katja; Yu, Ly-Mee; Juszczak, Edmund; on behalf of the Investigators DART AD (2008). Brayne, Carol, ed. "A Randomised, Blinded, Placebo-Controlled Trial in Dementia Patients Continuing or Stopping Neuroleptics (The DART-AD Trial)". PLoS Medicine. 5 (4): e76. doi:10.1371/journal.pmed.0050076. PMC 2276521. PMID 18384230. Lay summary – BBC News (April 1, 2008). Neuroleptics provided no benefit for patients with mild behavioural problems, but were associated with a marked deterioration in verbal skills

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[APA_schizophrenia_guideline-26] Work Group on Schizophrenia. "Practice Guideline for the Treatment of Patients With Schizophrenia Second Edition". Retrieved 21 April 2014.

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[28] Tauscher, Johannes; Kapur, Shitij (2001). "Choosing the Right Dose of Antipsychotics in Schizophrenia". CNS Drugs. 15 (9): 671–8. doi:10.2165/00023210-200115090-00001. PMID 11580306.

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[AAHPMfive-30] American Academy of Hospice and Palliative Medicine. "Five Things Physicians and Patients Should Question". Choosing Wisely: an initiative of the ABIM Foundation. American Academy of Hospice and Palliative Medicine. Retrieved August 1, 2013. , which cites

Smith, Thomas J.; Ritter, Joseph K.; Poklis, Justin L.; Fletcher, Devon; Coyne, Patrick J.; Dodson, Patricia; Parker, Gwendolyn (2012). "ABH Gel is Not Absorbed from the Skin of Normal Volunteers". Journal of Pain and Symptom Management. 43 (5): 961–6. doi:10.1016/j.jpainsymman.2011.05.017. PMID 22560361.

Weschules, Douglas J. (2005). "Tolerability of the Compound ABHR in Hospice Patients". Journal of Palliative Medicine. 8 (6): 1135–43. doi:10.1089/jpm.2005.8.1135. PMID 16351526.

[31] Smith, Thomas J.; Ritter, Joseph K.; Poklis, Justin L.; Fletcher, Devon; Coyne, Patrick J.; Dodson, Patricia; Parker, Gwendolyn (2012). "ABH Gel is Not Absorbed from the Skin of Normal Volunteers". Journal of Pain and Symptom Management. 43 (5): 961–6. doi:10.1016/j.jpainsymman.2011.05.017. PMID 22560361.

[32] Weschules, Douglas J. (2005). "Tolerability of the Compound ABHR in Hospice Patients". Journal of Palliative Medicine. 8 (6): 1135–43. doi:10.1089/jpm.2005.8.1135. PMID 16351526.

[31] PRODUCT INFORMATION [Internet]. 2011 [cited 2013 Sep 29]. Available from: https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2011-PI-03532-3

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[36] Leentjens, Albert FG; Van Der Mast, Rose C (2005). "Delirium in elderly people: An update". Current Opinion in Psychiatry. 18 (3): 325–30. doi:10.1097/01.yco.0000165603.36671.97. PMID 16639157.

[37] Sandyk, R; Hurwitz, MD (1983). "Toxic irreversible encephalopathy induced by lithium carbonate and haloperidol. A report of 2 cases". South African medical journal. 64 (22): 875–6. PMID 6415823.

[38] Bush, S. E.; Hatton, R. C.; Winterstein, A. G.; Thomson, M. R.; Woo, G. W. (2008). "Effects of concomitant amiodarone and haloperidol on Q-Tc interval prolongation". American Journal of Health-System Pharmacy. 65 (23): 2232–6. doi:10.2146/ajhp080039. PMID 19020191.

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[affindata-47] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k Kroeze, Wesley K; Hufeisen, Sandra J; Popadak, Beth A; Renock, Sean M; Steinberg, Seanna; Ernsberger, Paul; Jayathilake, Karu; Meltzer, Herbert Y; Roth, Bryan L (2003). "H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs". Neuropsychopharmacology. 28 (3): 519–26. doi:10.1038/sj.npp.1300027. PMID 12629531.

[48] Ilyin, VI; Whittemore, ER; Guastella, J; Weber, E; Woodward, RM (1996). "Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol". Molecular Pharmacology. 50 (6): 1541–50. PMID 8967976.

[49] "drugs.com".

[Kornhuber1999-50] Kornhuber, Johannes; Schultz, Andreas; Wiltfang, Jens; Meineke, Ingolf; Gleiter, Christoph H.; Zöchling, Robert; Boissl, Karl-Werner; Leblhuber, Friedrich; Riederer, Peter (1999). "Persistence of Haloperidol in Human Brain Tissue". The American Journal of Psychiatry. 156 (6): 885–90. doi:10.1176/ajp.156.6.885. PMID 10360127.

[51] Kornhuber, Johannes; Wiltfang, Jens; Riederer, Peter; Bleich, Stefan (2006). "Neuroleptic drugs in the human brain: Clinical impact of persistence and region-specific distribution". European Archives of Psychiatry and Clinical Neuroscience. 256 (5): 274–80. doi:10.1007/s00406-006-0661-7. PMID 16788768.

[52] Healy, David (1996). The psychopharmacologists. 1. London: Chapman and Hall. ISBN 978-1-86036-008-4. ^{[page needed]}

[53] Granger, Bernard; Albu, Simona (2005). "The Haloperidol Story". Annals of Clinical Psychiatry. 17 (3): 137–40. doi:10.1080/10401230591002048. PMID 16433054.

[JanssenHist-54] Lopez-Munoz, Francisco; Alamo, Cecilio (2009). "The Consolidation of Neuroleptic Therapy: Janssen, the Discovery of Haloperidol and Its Introduction into Clinical Practice". Brain Research Bulletin. 79: 130–141. doi:10.1016/j.brainresbull.2009.01.005. PMID 19186209.

[55] "Veterinary:Avian at Lloyd Center Pharmacy".

v t e Antipsychotics (neuroleptics) (N05A)

Typical	Benzamides Levosulpiride Sulpiride Veralipride^‡ Butyrophenones Azaperone Benperidol Bromperidol Droperidol Fluanisone Haloperidol^# Lenperone Moperone Pipamperone Spiperone Timiperone Trifluperidol Diphenylbutylpiperidines Clopimozide Fluspirilene Penfluridol Pimozide Phenothiazines Acepromazine Acetophenazine Butaperazine Carphenazine (carfenazine) Chloracizine Chlorproethazine Chlorpromazine Cyamemazine Dixyrazine Fluacizine Fluphenazine Levomepromazine/Methotrimeprazine Mesoridazine Perazine Periciazine Perphenazine Perphenazine 4-aminobutyrate Piperacetazine Pipotiazine Prochlorperazine Promazine Promethazine Sulforidazine Thiethylperazine Thiopropazate Thioproperazine Thioridazine Trifluoperazine Triflupromazine Thioxanthenes Chlorprothixene Clopenthixol Clothixamide Flupentixol Fluprothixene Piflutixol Teflutixol Thiothixene Zuclopenthixol Tricyclics Fluotracen Loxapine Trimipramine Others Butaclamol Prothipendyl

Atypical	Benzamides Amisulpride Nemonapride Remoxipride^‡ Sultopride Tiapride Butyrophenones Cinuperone Melperone Setoperone Benzo(iso)oxazolepiperidines Iloperidone Ocaperidone^§ Paliperidone Risperidone^# Benzo(iso)thiazolepiperazines Lurasidone Perospirone Revospirone^§ Tiospirone^§ Ziprasidone Diphenylbutylpiperazines Amperozide Phenylpiperazines Aripiprazole Aripiprazole lauroxil Bifeprunox^§ Brexpiprazole Cariprazine Tricyclics Amoxapine Asenapine Carpipramine Clocapramine Clorotepine Clotiapine Clozapine^# Flumezapine Fluperlapine Gevotroline Metitepine Mosapramine Olanzapine Quetiapine Tenilapine Zotepine Others Blonanserin Lumateperone^† Molindone Pimavanserin RP5063^† Sertindole Zicronapine^§

Others	Azacyclonol Cannabidiol Oxypertine Reserpine Tetrabenazine

^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

v t e Antiemetics (A04)

5-HT₃ serotonin ion channel antagonists	Alosetron Azasetron Bemesetron Cilansetron Clozapine Dazopride Dolasetron Granisetron Lerisetron Metoclopramide Mianserin Mirtazapine Olanzapine Ondansetron Palonosetron (+netupitant) Quetiapine Ramosetron Ricasetron Tropisetron Zatosetron

5-HT serotonin G-protein receptor antagonists	Clozapine Cyproheptadine Hydroxyzine Olanzapine Risperidone Ziprasidone

CB₁ agonists (cannabinoids)	Dronabinol Nabilone Tetrahydrocannabinol (cannabis)

D₂/D₃ antagonists	Alizapride Bromopride Chlorpromazine Clebopride Domperidone Haloperidol Hydroxyzine Itopride Metoclopramide Metopimazine Prochlorperazine Thiethylperazine Trimethobenzamide

H₁ antagonists (antihistamines)	Cyclizine Dimenhydrinate Diphenhydramine Hydroxyzine Meclizine Promethazine

mACh antagonists (anticholinergics)	Atropine Diphenhydramine Hydroxyzine (very mild) Hyoscyamine Scopolamine

NK₁ antagonists	Aprepitant Casopitant Ezlopitant Fosaprepitant Maropitant Netupitant Rolapitant Vestipitant

Others	Cerium oxalate Dexamethasone Lorazepam Midazolam Propofol

v t e Sigma receptor modulators

Agonists	3-MeO-PCE 3-MeO-PCP 3-PPP 4-MeO-PCP 4-IBP 4-PPBP Afobazole Alazocine Amantadine Amitriptyline Arketamine BD-1008 BD1031 BD1052 Berberine Buprenorphine Captodiame Citalopram Clorgiline Cocaine Cutamesine Cyclazocine DHEA DHEA-S Desipramine Dextrallorphan Dextromethorphan Dextrorphan Dimemorfan DMT Donepezil DTG Escitalopram Fluoxetine Fluvoxamine Heroin Ibogaine Igmesine Imipramine JO-1784 Ketamine L-687,384 Lamotrigine Lu 28-179 MDMA Memantine Metaphit Methamphetamine Methoxetamine Methylphenidate Morphine Naluzotan Noscapine OPC-14523 Opipramol PB-28 PD-144,415 Pentazocine Pentoxyverine Phencyclidine PRE-084 Pregnenolone Pregnenolone sulfate Quetiapine RTI-55 SA-4503 Siramesine Tapentadol Tenocyclidine Tramadol UMB23 UMB82 Venlafaxine

Antagonists	AC927 AHD1 AZ66 BD1008 BD1047 BD1060 BD1063 BD1067 BMY-14802 CM156 E-5842 Haloperidol Lamotrigine LR132 LR172 MIN-101 MS-377 Naloxone Naltrexone NE-100 Panamesine PD-144418 Progesterone Quingestrone Rimcazole S1RA (E-52862) Sertraline SM-21 SR-31742A UMB100 UMB101 UMB103 UMB116 YZ-011 YZ-069 YZ-185

Unknown / unsorted	4C-T-2 5-MeO-DiPT 18-MC β-Endopsychosin Chlorpromazine Clemastine Clocapramine Cloperastine D-Deprenyl DiPT DPT Gevotroline Nepinalone Selegiline TMA; Allosteric modulators: SKF-83959

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haloperidol decanoate