Identification
- Summary
Haloperidol is an antipsychotic agent used to treat schizophrenia and other psychoses, as well as symptoms of agitation, irritability, and delirium.
- Brand Names
- Haldol
- Generic Name
- Haloperidol
- DrugBank Accession Number
- DB00502
- Background
Haloperidol is a high potency first-generation (typical) antipsychotic and one of the most frequently used antipsychotic medications used worldwide.7 While haloperidol has demonstrated pharmacologic activity at a number of receptors in the brain,10 it exerts its antipsychotic effect through its strong antagonism of the dopamine receptor (mainly D2), particularly within the mesolimbic and mesocortical systems of the brain. Haloperidol is indicated for the treatment of the manifestations of several psychotic disorders including schizophrenia, acute psychosis, Tourette syndrome, and other severe behavioural states.16 It is also used off-label for the management of chorea associated with Huntington's disease and for the treatment of intractable hiccups as it is a potent antiemetic. Dopamine-antagonizing medications such as haloperidol are though to improve psychotic symptoms and states that are caused by an over-production of dopamine, such as schizophrenia, which is theorized to be caused by a hyperdopaminergic state within the limbic system of the brain.9
Use of the first-generation antipsychotics (including haloperidol) is considered highly effective for the management of the "positive" symptoms of schizophrenia including hallucinations, hearing voices, aggression/hostility, disorganized speech, and psychomotor agitation. However, this class of drugs is also limited by the development of movement disorders induced by dopamine-blockade such as drug-induced parkinsonism, akathisia, dystonia, tardive dyskinesia, as well as other side effects including sedation, weight gain, and prolactin changes. While there are limited high-quality studies comparing haloperidol to lower-potency first-generation antipsychotics such as Chlorpromazine, Zuclopenthixol, Fluphenazine, and Methotrimeprazine, haloperidol typically demonstrates the least amount of side effects within this class, but demonstrates a stronger disposition for causing extrapyramidal symptoms (EPS).6,7,8 These other low‐potency antipsychotics are limited by their lower affinity for dopamine receptors, which requires a higher dose to effectively treat symptoms of schizophrenia. In addition, they block many receptors other than the primary target (dopamine receptors), such as cholinergic or histaminergic receptors, resulting in a higher incidence of side effects such as sedation, weight gain, and hypotension.
Interestingly, in vivo pharmacogenetic studies have demonstrated that the metabolism of haloperidol may be modulated by genetically determined polymorphic CYP2D6 activity. However, these findings contradict the findings from studies in vitro with human liver microsomes and from drug interaction studies in vivo. Inter-ethnic and pharmacogenetic differences in haloperidol metabolism may possibly explain these observations.3
First-generation antipsychotic drugs have largely been replaced with second- and third-generation (atypical) antipsychotics such as Risperidone, Olanzapine, Clozapine, Quetiapine, Aripiprazole, and Ziprasidone. However, haloperidol use remains widespread and is considered the benchmark for comparison in trials of the newer generation antipsychotics.8
The efficacy of haloperidol was first established in controlled trials in the 1960s.5
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Haloperidol (DB00502)
- Weight
- Average: 375.864
Monoisotopic: 375.140134897 - Chemical Formula
- C21H23ClFNO2
- Synonyms
- 1-(3-p-fluorobenzoylpropyl)-4-p-chlorophenyl-4-hydroxypiperidine
- 4-(4-(para-chlorophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
- 4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)-butan-1-one
- 4'-fluoro-4-(4-(p-chlorophenyl)-4-hydroxypiperidinyl)butyrophenone
- 4'-fluoro-4-(4-hydroxy-4-(4'-chlorophenyl)piperidino)butyrophenone
- Haloperidol
- Haloperidolum
- γ-(4-(p-chlorophenyl)-4-hydroxpiperidino)-p-fluorbutyrophenone
- External IDs
- MCN-JR-1625
- NSC-170973
- NSC-615296
- R-1625
Pharmacology
- Indication
Haloperidol is indicated for a number of conditions including for the treatment of schizophrenia, for the manifestations of psychotic disorders, for the control of tics and vocal utterances of Tourette’s Disorder in children and adults, for treatment of severe behavior problems in children of combative, explosive hyperexcitability (which cannot be accounted for by immediate provocation). Haloperidol is also indicated in the short-term treatment of hyperactive children who show excessive motor activity with accompanying conduct disorders consisting of some or all of the following symptoms: impulsivity, difficulty sustaining attention, aggressivity, mood lability, and poor frustration tolerance. Haloperidol should be reserved for these two groups of children only after failure to respond to psychotherapy or medications other than antipsychotics.16
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Aggression ••• ••••• Management of Delirium ••• ••••• Treatment of Huntington's chorea ••• ••••• Treatment of Nausea and vomiting ••• ••••• •••••••••• •••• Management of Obsessive compulsive disorder ••• ••••• - Contraindications & Blackbox Warnings
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Use of the first-generation antipsychotics (including haloperidol) is considered highly effective for the management of the "positive" symptoms of schizophrenia including hallucinations, hearing voices, aggression/hostility, disorganized speech, and psychomotor agitation. However, this class is limited by the development of movement disorders such as drug-induced parkinsonism, akathisia, dystonia, and tardive dyskinesia, and other side effects including sedation, weight gain, and prolactin changes. Compared to the lower-potency first-generation antipsychotics such as Chlorpromazine, Zuclopenthixol, Fluphenazine, and Methotrimeprazine, haloperidol typically demonstrates the least amount of side effects within class, but demonstrates a stronger disposition for causing extrapyramidal symptoms (EPS).6,7,8 Low‐potency medications have a lower affinity for dopamine receptors so that a higher dose is required to effectively treat symptoms of schizophrenia. In addition, they block many receptors other than the primary target (dopamine receptors), such as cholinergic or histaminergic receptors, resulting in a higher incidence of side effects such as sedation, weight gain, and hypotension.
The balance between the wanted drug effects on psychotic symptoms and unwanted side effects are largely at play within dopaminergic brain pathways affected by haloperidol. Cortical dopamine-D2-pathways play an important role in regulating these effects and include the nigrostriatal pathway, which is responsible for causing extrapyramidal symptoms (EPS), the mesolimbic and mesocortical pathways, which are responsible for the improvement in positive schizophrenic symptoms, and the tuberoinfundibular dopamine pathway, which is responsible for hyperprolactinemia.
A syndrome consisting of potentially irreversible, involuntary, dyskinetic movements may develop in patients. Although the prevalence of the syndrome appears to be highest among the elderly, especially elderly women, it is impossible to rely upon prevalence estimates to predict, at the inception of antipsychotic treatment, which patients are likely to develop the syndrome.16
Cases of sudden death, QT-prolongation, and Torsades de Pointes have been reported in patients receiving haloperidol. Higher than recommended doses of any formulation and intravenous administration of haloperidol appear to be associated with a higher risk of QT-prolongation and Torsades de Pointes. Although cases have been reported even in the absence of predisposing factors, particular caution is advised in treating patients with other QT-prolonging conditions (including electrolyte imbalance [particularly hypokalemia and hypomagnesemia], drugs known to prolong QT, underlying cardiac abnormalities, hypothyroidism, and familial long QT-syndrome).16
A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with antipsychotic drugs. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status (including catatonic signs) and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmias). Additional signs may include elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis) and acute renal failure.16
- Mechanism of action
While haloperidol has demonstrated pharmacologic activity at a number of receptors in the brain, it exerts its antipsychotic effect through its strong antagonism of the dopamine receptor (mainly D2), particularly within the mesolimbic and mesocortical systems of the brain. Schizophrenia is theorized to be caused by a hyperdopaminergic state within the limbic system of the brain.9 Dopamine-antagonizing medications such as haloperidol, therefore, are thought to improve psychotic symptoms by halting this over-production of dopamine. The optimal clinical efficacy of antipsychotics is associated with the blockade of approximately 60 % - 80 % of D2 receptors in the brain.9
While the exact mechanism is not entirely understood, haloperidol is known to inhibit the effects of dopamine and increase its turnover. Traditional antipsychotics, such as haloperidol, bind more tightly than dopamine itself to the dopamine D2 receptor, with dissociation constants that are lower than that for dopamine.4 It is believed that haloperidol competitively blocks post-synaptic dopamine (D2) receptors in the brain, eliminating dopamine neurotransmission and leading to the relief of delusions and hallucinations that are commonly associated with psychosis. It acts primarily on the D2-receptors and has some effect on 5-HT2 and α1-receptors, with negligible effects on dopamine D1-receptors. The drug also exerts some blockade of α-adrenergic receptors of the autonomic system.13
Antagonistic activity regulated through dopamine D2 receptors in the chemoreceptive trigger zone (CTZ) of the brain renders its antiemetic activity. Of the three D2-like receptors, only the D2 receptor is blocked by antipsychotic drugs in direct relation to their clinical antipsychotic abilities.
Clinical brain-imaging findings show that haloperidol remains tightly bound to D2 dopamine receptors in humans undergoing 2 positron emission tomography (PET) scans with a 24h pause in between scans.4 A common adverse effect of this drug is the development of extrapyramidal symptoms (EPS), due to this tight binding of haloperidol to the dopamine D2 receptor.
Due to the risk of unpleasant and sometimes lifelong extrapyramidal symptoms, newer antipsychotic medications than haloperidol have been discovered and formulated. Rapid dissociation of drugs from dopamine D2 receptors is a plausible explanation for the improved EPS profile of atypical antipsychotics such as Risperidone. This is also consistent with the theory of a lower affinity for D2 receptors for these drugs. As mentioned above, haloperidol binds tightly to the dopamine receptor, potentiating the risk of extrapyramidal symptoms,4 and therefore should only been used when necessary.
Target Actions Organism A5-hydroxytryptamine receptor 2C Not Available Humans ADopamine D2 receptor antagonistHumans U5-hydroxytryptamine receptor 2A other/unknownHumans UDopamine D3 receptor inverse agonistHumans UMelanin-concentrating hormone receptor 1 Not Available Humans USynaptic vesicular amine transporter Not Available Humans USigma non-opioid intracellular receptor 1 Not Available Humans UHistamine H1 receptor Not Available Humans UMuscarinic acetylcholine receptor M3 Not Available Humans UAlpha-1A adrenergic receptor Not Available Humans UAlpha-2A adrenergic receptor Not Available Humans UAlpha-2B adrenergic receptor Not Available Humans UAlpha-2C adrenergic receptor Not Available Humans U5-hydroxytryptamine receptor 1A Not Available Humans U5-hydroxytryptamine receptor 6 Not Available Humans U5-hydroxytryptamine receptor 7 Not Available Humans UGlutamate receptor ionotropic, NMDA 2B antagonistHumans UDopamine D1 receptor antagonistHumans - Absorption
Haloperidol is a highly lipophilic compound and is extensively metabolized in humans, which may cause a large interindividual variability in its pharmacokinetics.3
Studies have found a wide variance in pharmacokinetic values for orally administered haloperidol with 1.7-6.1 hours reported for time to peak plasma concentration (tmax), 14.5-36.7 hours reported for half-life (t1⁄2), and 43.73 μg/L•h [range 14.89-120.96 μg/L•h] reported for AUC.3 Haloperidol is well-absorbed from the gastrointestinal tract when ingested orally, however, the first-pass hepatic metabolism decreases its oral bioavailability to 40 - 75%.
After intramuscular administration, the time to peak plasma concentration (tmax) is 20 minutes in healthy individuals or 33.8 minutes in patients with schizophrenia, with a mean half-life of 20.7 hours.3 Bioavailability following intramuscular administration is higher than that for oral administration.
Administration of haloperidol decanoate (the depot form of haloperidol for long-term treatment) in sesame oil results in slow release of the drug for long-term effects. The plasma concentrations of haloperidol gradually rise, reaching its peak concentration at about 6 days after the injection, with an apparent half-life of about 21 days. Steady-state plasma concentrations are achieved after the third or fourth dose.16
- Volume of distribution
The apparent volume of distribution was found to range from 9.5-21.7 L/kg.3 This high volume of distribution is in accordance with its lipophilicity, which also suggests free movement through various tissues including the blood-brain barrier.
- Protein binding
Studies have found that free fraction of haloperidol in human plasma is 7.5-11.6%. This was found to be comparable among healthy adults, young adults, elderly patients with schizophrenia, and even in patients with liver cirrhosis.3
- Metabolism
Haloperidol is extensively metabolised in the liver with only about 1% of the administered dose excreted unchanged in urine.3
In humans, haloperidol is biotransformed to various metabolites, including p-fluorobenzoylpropionic acid, 4-(4-chlorophenyl)-4-hydroxypiperidine, reduced haloperidol, pyridinium metabolites, and haloperidol glucuronide. In psychiatric patients treated regularly with haloperidol, the concentration of haloperidol glucuronide in plasma is the highest among the metabolites, followed, in rank order, by unchanged haloperidol, reduced haloperidol and reduced haloperidol glucuronide.
The drug is thought to be metabolized primarily by oxidative N-dealkylation of the piperidine nitrogen to form fluorophenylcarbonic acids and piperidine metabolites (which appear to be inactive), and by reduction of the butyrophenone carbonyl to the carbinol, forming hydroxyhaloperidol.
The enzymes involved in the biotransformation of haloperidol include cytochrome P450 (CYP) including CYP3A4 and CYP2D6, carbonyl reductase and uridine di-phosphoglucose glucuronosyltransferase enzymes. The greatest proportion of the intrinsic hepatic clearance of haloperidol is performed by glucuronidation and followed by the reduction of haloperidol to reduced haloperidol and by CYP-mediated oxidation.
In studies of cytochrome-mediated disposition in vitro, CYP3A4 appears to be the major isoform of the enzyme responsible for the metabolism of haloperidol in humans. The intrinsic clearance of the back-oxidation of reduced haloperidol to the parent compound, oxidative N-dealkylation and pyridinium formation are of the same order of magnitude. This suggests that the same enzyme system is responsible for the above three metabolic reactions.
In vivo human studies on haloperidol metabolism have shown that the glucuronidation of haloperidol accounts for 50 to 60% of haloperidol biotransformation and that approximately 23% of the biotransformation was accounted for by the reduction pathway. The remaining 20 to 30% ofthe biotransformation of haloperidol would be via N-dealkylation and pyridinium formation.3
Hover over products below to view reaction partners
- Route of elimination
In radiolabeling studies, approximately 30% of the radioactivity is excreted in the urine following a single oral administration of 14C-labelled haloperidol, while 18% is excreted in the urine as haloperidol glucuronide, demonstrating that haloperidol glucuronide is a major metabolite in the urine as well as in plasma in humans.3
- Half-life
Following oral administration, the half-life was found to be 14.5-36.7 hours. Following intramuscular injection, mean half-life was found to be 20.7 hours.3
- Clearance
Following intravenous administration, the plasma or serum clearance (CL) was found to be 0.39-0.708 L/h/kg (6.5 to 11.8 ml/min/kg). Following oral administration, clearance was found to be 141.65 L/h (range 41.34 to 335.80 L/h).3
Haloperidol clearance after extravascular administration ranges from 0.9-1.5 l/h/kg, however this rate is reduced in poor metabolizers of CYP2D6 enzyme. Reduced CYP2D6 enzyme activity may result in increased concentrations of haloperidol. The inter-subject variability (coefficient of variation, %) in haloperidol clearance was estimated to be 44% in a population pharmacokinetic analysis in patients with schizophrenia 14.
Genetic polymorphism of CYP2D6 has been demonstrated to be an important source of inter-patient variability in the pharmacokinetics of haloperidol and may affect therapeutic response and incidence of adverse effects.3
- Adverse Effects
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Acute oral toxicity (LD50): 71 mg/kg in rats MSDS.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Haloperidol is combined with 1,2-Benzodiazepine. Abacavir Haloperidol may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Haloperidol can be increased when it is combined with Abametapir. Abatacept The metabolism of Haloperidol can be increased when combined with Abatacept. Abemaciclib The serum concentration of Haloperidol can be increased when it is combined with Abemaciclib. - Food Interactions
- Avoid alcohol. Alcohol may potential hypotension and CNS adverse effects.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Haloperidol decanoate AC20PJ4101 74050-97-8 GUTXTARXLVFHDK-UHFFFAOYSA-N Haloperidol lactate 6387S86PK3 53515-91-6 BVUSNQJCSYDJJG-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Aloperidin (Janssen-Cilag) / Bioperidolo (Firma) / Brotopon (Pfizer) / Dozic (Rosemont) / Duraperidol / Einalon S / Eukystol (Merckle) / Halosten (Shionogi Seiyaku) / Keselan (Sumitomo) / Linton (Tanabe Mitsubishi Pharma) / Peluces (lsei) / Serenace (Pfizer) / Sigaperidol (Siegfried)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Haldol Injection 5 mg/1mL Intramuscular Janssen Pharmaceuticals, Inc. 1971-05-18 2050-08-02 US 
Haldol Injection, solution 5 mg/1mL Intramuscular McNeil Pharmaceuticals 1971-05-18 2011-07-31 US Haldol Decanoate Injection 50 mg/1mL Intramuscular Janssen Pharmaceuticals, Inc. 1986-01-14 Not applicable US Haldol Decanoate Injection 100 mg/1mL Intramuscular McNeil Pharmaceuticals 1986-01-14 2011-05-31 US Haldol Decanoate Injection 50 mg/1mL Intramuscular Physicians Total Care, Inc. 1986-01-14 2012-06-30 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo Haloperidol Tab 0.5mg Tablet .5 mg Oral Apotex Corporation 1980-12-31 Not applicable Canada 
Apo Haloperidol Tab 1mg Tablet 1 mg Oral Apotex Corporation 1980-12-31 Not applicable Canada Apo-haloperidol LA Injectable Liquid 100 mg / mL Intramuscular Apotex Corporation 2000-06-30 2013-08-02 Canada Apo-haloperidol LA Injectable Liquid 50 mg / mL Intramuscular Apotex Corporation 2000-06-30 2013-08-02 Canada Apo-haloperidol Liq 2mg/ml Solution 2 mg / mL Oral Apotex Corporation 1983-12-31 2019-05-04 Canada
Categories
- ATC Codes
- N05AD01 — Haloperidol
- Drug Categories
- Agents that reduce seizure threshold
- Anti-Dyskinesia Agents
- Antiemetics
- Antipsychotic Agents
- Antipsychotic Agents (First Generation [Typical])
- Autonomic Agents
- Butyrophenone Derivatives
- Butyrophenones
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (moderate)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dopamine Agents
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs causing inadvertant photosensitivity
- Drugs that are Mainly Renally Excreted
- Gastrointestinal Agents
- Hyperglycemia-Associated Agents
- Ketones
- Moderate Risk QTc-Prolonging Agents
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- NMDA Receptor Antagonists
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Photosensitizing Agents
- Psycholeptics
- Psychotropic Drugs
- QTc Prolonging Agents
- Tranquilizing Agents
- UGT1A9 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as alkyl-phenylketones. These are aromatic compounds containing a ketone substituted by one alkyl group, and a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organic oxygen compounds
- Class
- Organooxygen compounds
- Sub Class
- Carbonyl compounds
- Direct Parent
- Alkyl-phenylketones
- Alternative Parents
- Phenylpiperidines / Phenylbutylamines / Butyrophenones / Aryl alkyl ketones / Benzoyl derivatives / Aralkylamines / Fluorobenzenes / Chlorobenzenes / Aryl chlorides / Aryl fluorides show 9 more
- Substituents
- Alcohol / Alkyl-phenylketone / Amine / Aralkylamine / Aromatic heteromonocyclic compound / Aryl alkyl ketone / Aryl chloride / Aryl fluoride / Aryl halide / Azacycle show 23 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- organofluorine compound, tertiary alcohol, monochlorobenzenes, aromatic ketone, hydroxypiperidine (CHEBI:5613)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- J6292F8L3D
- CAS number
- 52-86-8
- InChI Key
- LNEPOXFFQSENCJ-UHFFFAOYSA-N
- 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
- IUPAC Name
- 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
- SMILES
- OC1(CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1)C1=CC=C(Cl)C=C1
References
- Synthesis Reference
- US3438991
- General References
- Niemegeers CJ, Laduron PM: Pharmacology and biochemistry of haloperidol. Proc R Soc Med. 1976;69 suppl 1:3-8. [Article]
- Gelders YG: Pharmacology, pharmacokinetics and clinical development of haloperidol decanoate. Int Clin Psychopharmacol. 1986 Jul;1 Suppl 1:1-11. [Article]
- Kudo S, Ishizaki T: Pharmacokinetics of haloperidol: an update. Clin Pharmacokinet. 1999 Dec;37(6):435-56. doi: 10.2165/00003088-199937060-00001. [Article]
- Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
- Mumtaz MM, Farooqui MY, Ghanayem BI, Rajaraman S, Frankenberg L, Ahmed AE: Studies on the mechanism of urotoxic effects of N,N'-dimethylaminopropionitrile in rats and mice. 1. Biochemical and morphologic characterization of the injury and its relationship to metabolism. J Toxicol Environ Health. 1991 May;33(1):1-17. doi: 10.1080/15287399109531501. [Article]
- Tardy M, Huhn M, Kissling W, Engel RR, Leucht S: Haloperidol versus low-potency first-generation antipsychotic drugs for schizophrenia. Cochrane Database Syst Rev. 2014 Jul 9;(7):CD009268. doi: 10.1002/14651858.CD009268.pub2. [Article]
- Dold M, Samara MT, Li C, Tardy M, Leucht S: Haloperidol versus first-generation antipsychotics for the treatment of schizophrenia and other psychotic disorders. Cochrane Database Syst Rev. 2015 Jan 16;1:CD009831. doi: 10.1002/14651858.CD009831.pub2. [Article]
- Adams CE, Bergman H, Irving CB, Lawrie S: Haloperidol versus placebo for schizophrenia. Cochrane Database Syst Rev. 2013 Nov 15;(11):CD003082. doi: 10.1002/14651858.CD003082.pub3. [Article]
- Seeman P, Kapur S: Schizophrenia: more dopamine, more D2 receptors. Proc Natl Acad Sci U S A. 2000 Jul 5;97(14):7673-5. [Article]
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Clinical pharmacology of atypical antipsychotics: an update [Link]
- Mechanism of Action of Antipsychotics, Haloperidol and Olanzapine in vitro [Link]
- Haloperidol Overview [Link]
- Haldol Decanoate [Link]
- FDA Approved Drug Products: Haldol (haloperidol) for injection [Link]
- FDA Label - haloperidol [File]
- Health Canada Monograph - haloperidol [File]
- External Links
- Human Metabolome Database
- HMDB0014645
- KEGG Drug
- D00136
- KEGG Compound
- C01814
- PubChem Compound
- 3559
- PubChem Substance
- 46508794
- ChemSpider
- 3438
- BindingDB
- 21398
- 5093
- ChEBI
- 5613
- ChEMBL
- CHEMBL54
- ZINC
- ZINC000000537822
- Therapeutic Targets Database
- DAP000313
- PharmGKB
- PA449841
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- GMJ
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Haloperidol
- PDB Entries
- 6djz / 6luq / 6x10
- FDA label
- Download (169 KB)
- MSDS
- Download (73.2 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Delirium 1 4 Completed Not Available Schizoaffective Disorders / Schizophrenia 1 4 Completed Basic Science Psychosis / Schizophrenia 1 4 Completed Prevention Anxiety / Cognitive Impairment (CI) / Delirium / Depression / Post Traumatic Stress Disorder (PTSD) 1 4 Completed Prevention Delirium 2
Pharmacoeconomics
- Manufacturers
- Ortho mcneil pharmaceutical
- Ortho mcneil pharmaceutical inc
- Duramed pharmaceuticals inc sub barr laboratories inc
- Lederle laboratories div american cyanamid co
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Par pharmaceutical inc
- Purepac pharmaceutical co
- Quantum pharmics ltd
- Roxane laboratories inc
- Royce laboratories inc
- Sandoz inc
- Scs pharmaceuticals
- Vintage pharmaceuticals llc
- Watson laboratories inc
- Zydus pharmaceuticals usa inc
- Ortho mcneil janssen pharmaceutical inc
- App pharmaceuticals llc
- Bedford laboratories div ben venue laboratories inc
- Claris lifesciences ltd
- Hospira inc
- Sandoz canada inc
- Teva parenteral medicines inc
- Alpharma uspd inc
- Morton grove pharmaceuticals inc
- Pharmaceutical assoc inc div beach products
- Silarx pharmaceuticals inc
- Teva pharmaceuticals usa inc
- Teva pharmaceuticals usa
- Ortho mcneil janssen pharmaceuticals inc
- Abraxis pharmaceutical products
- Akorn strides llc
- Gland pharma ltd
- Marsam pharmaceuticals llc
- Smith and nephew solopak div smith and nephew
- Solopak medical products inc
- Solopak laboratories inc
- Actavis mid atlantic llc
- Packagers
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Apotex Inc.
- APP Pharmaceuticals
- APPD
- Bedford Labs
- Ben Venue Laboratories Inc.
- Boca Pharmacal
- Cadila Healthcare Ltd.
- Cardinal Health
- Coupler Enterprises Inc.
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Innoviant Pharmacy Inc.
- Janssen-Ortho Inc.
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Mallinckrodt Inc.
- Mckesson Corp.
- McNeil Laboratories
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Novex Pharma
- Nucare Pharmaceuticals Inc.
- OMJ Pharmaceuticals
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Ortho-McNeil-Janssen Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Association
- Pharmacia Inc.
- Pharmacy Service Center
- Physicians Total Care Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Qualitest
- Ranbaxy Laboratories
- Rebel Distributors Corp.
- Remedy Repack
- Sandhills Packaging Inc.
- Sandoz
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- Silarx Pharmaceuticals
- Southwood Pharmaceuticals
- Superior Pharmeceuticals
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- Vangard Labs Inc.
- Zydus Pharmaceuticals
- Dosage Forms
Form Route Strength Injection, solution Intramuscular Tablet, coated Oral 10 mg Solution Intramuscular; Intravenous 5 mg Injection, solution Solution / drops Oral Solution Intramuscular 50.000 mg Injection, solution Intramuscular 5 MG/ML Solution Oral 200.00 mg Tablet Oral Solution Oral Injection, solution Parenteral Injection Injection Parenteral 50 mg Injection, solution Intramuscular 50 mg/ml Injection, solution Intramuscular; Parenteral 50 MG/ML Solution Parenteral 50.000 mg Injection Parenteral 50 MG/ML Injection, solution Parenteral 50 mg/1ml Injection, solution Parenteral 50 mg/ml Injection Intramuscular 100 mg/1mL Injection Intramuscular 50 mg/1mL Solution Oral 2 MG/ML Liquid Intramuscular 100 mg / mL Liquid Intramuscular 50 mg / mL Injection Intramuscular Injection Intramuscular 5 mg/1mL Injection Intramuscular 5 mg/1 Injection, solution Intramuscular 5 mg/1mL Solution Oral 2 mg/1mL Solution, concentrate Oral 2 mg/1mL Tablet Oral 0.5 MG Tablet Oral 0.5 mg/1 Tablet Oral 1 mg/1 Tablet Oral 10 mg/1 Tablet Oral 2 mg/1 Tablet Oral 20 mg/1 Tablet Oral 5 mg/1 Solution Oral 10 mg Injection Intramuscular 141.04 mg/1mL Injection Intramuscular 250 mg/5mL Injection Intramuscular 500 mg/5mL Injection Intramuscular 70.52 mg/1mL Injection, solution Intramuscular 100 mg/1mL Injection, solution Intramuscular 50 mg/1mL Injection, solution Intramuscular 500 mg/5mL Liquid Intramuscular 5 mg / mL Solution Intramuscular 5 mg / mL Solution Intramuscular 5 mg Solution Parenteral 5 mg Solution Oral 2 mg Tablet Oral 5 mg / tab Tablet Oral 12 MG Tablet Oral 4 MG Injection Parenteral 100 mg Solution Oral 10 mg/mL Solution Oral 2.000 mg Solution Parenteral 5.000 mg Tablet Oral 2 mg Tablet Oral 10 mg Solution 5 mg/1ml Solution / drops Oral 10 ml Solution / drops Oral 20 ml Solution / drops; suspension / drops Tablet, film coated Oral Tablet, film coated Oral 2 MG Injection Intramuscular; Intravenous Injection Intramuscular; Intravenous 5 mg/ml Tablet Oral 1.5 mg Injection Intramuscular 5 mg/ml Injection Intramuscular; Intravenous 10 mg/2ml Injection Intramuscular; Intravenous 5 mg/1ml Injection, solution Intramuscular 150 mg/3ml Solution Intramuscular 50 mg/ml Tablet Oral 0.5 mg / tab Tablet Oral 1 mg / tab Tablet Oral 10 mg / tab Tablet Oral 2 mg / tab Solution Oral 2 mg / mL Tablet Oral .5 mg Solution Intramuscular 100 mg / mL Solution Intramuscular 50 mg / mL Injection, solution 5 mg/ml Injection, solution 5 mg Injection, solution Intramuscular; Parenteral 2 MG/2ML Injection, solution Intramuscular; Parenteral 5 MG/2ML Solution / drops Oral 10 MG/ML Solution / drops Oral 2 MG/ML Solution / drops Oral 30 ML Solution / drops Oral 30 mg Tablet Oral 20 mg Solution Intramuscular 5.000 mg Tablet Oral 5 mg/5mg Tablet Oral 5 mg Solution 50 mg/1ml Solution 2 mg/1ml Tablet Oral 1 mg Tablet, coated Oral 2 mg - Prices
Unit description Cost Unit Haloperidol Decanoate 100 mg/ml Solution 5ml Vial 257.14USD vial Haldol decanoate 100 ampul 107.77USD ml Haldol decanoate 50 ampul 56.53USD ml Haloperidol dec 100 mg/ml vial 29.85USD ml Haloperidol powder 21.42USD g Haloperidol dec 50 mg/ml vial 17.71USD ml Haloperidol La 100 mg/ml 15.42USD ml Haldol 5 mg/ml ampul 13.4USD ml Haloperidol La 50 mg/ml 7.71USD ml Haloperidol 5 mg/ml 4.73USD ml Haloperidol lac 5 mg/ml vial 3.54USD ml Haloperidol 20 mg tablet 2.81USD tablet Haloperidol 10 mg tablet 1.46USD tablet Haloperidol 5 mg tablet 0.8USD tablet Novo-Peridol 20 mg Tablet 0.66USD tablet Haloperidol 2 mg tablet 0.49USD tablet Haloperidol lac 2 mg/ml conc 0.45USD ml Haloperidol 1 mg tablet 0.36USD tablet Haloperidol 0.5 mg tablet 0.25USD tablet Pernox scrub cleanser 0.18USD g Apo-Haloperidol 5 mg Tablet 0.16USD tablet Novo-Peridol 5 mg Tablet 0.16USD tablet Apo-Haloperidol 10 mg Tablet 0.14USD tablet Novo-Peridol 10 mg Tablet 0.14USD tablet Apo-Haloperidol 2 mg Tablet 0.11USD tablet Novo-Peridol 2 mg Tablet 0.11USD tablet Apo-Haloperidol 1 mg Tablet 0.06USD tablet Novo-Peridol 1 mg Tablet 0.06USD tablet Apo-Haloperidol 0.5 mg Tablet 0.04USD tablet Novo-Peridol 0.5 mg Tablet 0.04USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 148 MSDS water solubility 14 mg/L (at 25 °C) https://pubchem.ncbi.nlm.nih.gov/compound/haloperidol logP 4.3 https://pubchem.ncbi.nlm.nih.gov/compound/haloperidol logS -4.43 https://pubchem.ncbi.nlm.nih.gov/compound/haloperidol pKa 8.66 EL TAYAR,N ET AL. (1985) - Predicted Properties
Property Value Source Water Solubility 0.00446 mg/mL ALOGPS logP 3.7 ALOGPS logP 3.66 Chemaxon logS -4.9 ALOGPS pKa (Strongest Acidic) 13.96 Chemaxon pKa (Strongest Basic) 8.05 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 40.54 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 102.59 m3·mol-1 Chemaxon Polarizability 39.15 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9465 Caco-2 permeable + 0.6023 P-glycoprotein substrate Substrate 0.6673 P-glycoprotein inhibitor I Inhibitor 0.8563 P-glycoprotein inhibitor II Inhibitor 0.8137 Renal organic cation transporter Inhibitor 0.6058 CYP450 2C9 substrate Non-substrate 0.8355 CYP450 2D6 substrate Substrate 0.8919 CYP450 3A4 substrate Substrate 0.5796 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9207 CYP450 2D6 inhibitor Inhibitor 0.9197 CYP450 2C19 inhibitor Non-inhibitor 0.9248 CYP450 3A4 inhibitor Inhibitor 0.6899 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7933 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.8769 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.4367 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5 hERG inhibition (predictor II) Inhibitor 0.7474
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 197.9365016 predictedDarkChem Lite v0.1.0 [M-H]- 187.8418187 predictedDarkChem Lite v0.1.0 [M-H]- 200.6782016 predictedDarkChem Lite v0.1.0 [M-H]- 189.38785 predictedDeepCCS 1.0 (2019) [M+H]+ 198.5359016 predictedDarkChem Lite v0.1.0 [M+H]+ 149.6252754 predictedDarkChem Lite v0.1.0 [M+H]+ 201.4162016 predictedDarkChem Lite v0.1.0 [M+H]+ 191.90173 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.7327016 predictedDarkChem Lite v0.1.0 [M+Na]+ 200.58136 predictedDarkChem Lite v0.1.0 [M+Na]+ 200.6852016 predictedDarkChem Lite v0.1.0 [M+Na]+ 199.60866 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Osinski MA, Uchic ME, Seifert T, Shaughnessy TK, Miller LN, Nakane M, Cox BF, Brioni JD, Moreland RB: Dopamine D2, but not D4, receptor agonists are emetogenic in ferrets. Pharmacol Biochem Behav. 2005 May;81(1):211-9. [Article]
- Bustillo J, Barrow R, Paz R, Tang J, Seraji-Bozorgzad N, Moore GJ, Bolognani F, Lauriello J, Perrone-Bizzozero N, Galloway MP: Long-term treatment of rats with haloperidol: lack of an effect on brain N-acetyl aspartate levels. Neuropsychopharmacology. 2006 Apr;31(4):751-6. [Article]
- Ishiwata K, Oda K, Sakata M, Kimura Y, Kawamura K, Oda K, Sasaki T, Naganawa M, Chihara K, Okubo Y, Ishii K: A feasibility study of [11C]SA4503-PET for evaluating sigmal receptor occupancy by neuroleptics: the binding of haloperidol to sigma1 and dopamine D2-like receptors. Ann Nucl Med. 2006 Oct;20(8):569-73. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Naiker DV, Catts SV, Catts VS, Bedi KS, Bryan-Lluka LJ: Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat. Eur J Pharmacol. 2006 Jul 1;540(1-3):87-90. Epub 2006 May 11. [Article]
- Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [Article]
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Seeman P: Dopamine D2 receptors as treatment targets in schizophrenia. Clin Schizophr Relat Psychoses. 2010 Apr;4(1):56-73. doi: 10.3371/CSRP.4.1.5. [Article]
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inverse agonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44224.335 Da
References
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Tuppurainen H, Kuikka JT, Viinamaki H, Husso M, Tiihonen J: Dopamine D2/3 receptor binding potential and occupancy in midbrain and temporal cortex by haloperidol, olanzapine and clozapine. Psychiatry Clin Neurosci. 2009 Aug;63(4):529-37. doi: 10.1111/j.1440-1819.2009.01982.x. Epub 2009 May 22. [Article]
- Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Characterization of aripiprazole partial agonist activity at human dopamine D3 receptors. Eur J Pharmacol. 2008 Nov 12;597(1-3):27-33. doi: 10.1016/j.ejphar.2008.09.008. Epub 2008 Sep 20. [Article]
- Kessler RM, Ansari MS, Riccardi P, Li R, Jayathilake K, Dawant B, Meltzer HY: Occupancy of striatal and extrastriatal dopamine D2/D3 receptors by olanzapine and haloperidol. Neuropsychopharmacology. 2005 Dec;30(12):2283-9. [Article]
- Malmberg, Mikaels, Mohell N: Agonist and inverse agonist activity at the dopamine D3 receptor measured by guanosine 5'--gamma-thio-triphosphate--35S- binding. J Pharmacol Exp Ther. 1998 Apr;285(1):119-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Neuropeptide receptor activity
- Specific Function
- Receptor for melanin-concentrating hormone, coupled to both G proteins that inhibit adenylyl cyclase and G proteins that activate phosphoinositide hydrolysis.
- Gene Name
- MCHR1
- Uniprot ID
- Q99705
- Uniprot Name
- Melanin-concentrating hormone receptor 1
- Molecular Weight
- 45962.185 Da
References
- Theisen FM, Haberhausen M, Firnges MA, Gregory P, Reinders JH, Remschmidt H, Hebebrand J, Antel J: No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. Epub 2006 Sep 19. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Monoamine transmembrane transporter activity
- Specific Function
- Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
- Gene Name
- SLC18A2
- Uniprot ID
- Q05940
- Uniprot Name
- Synaptic vesicular amine transporter
- Molecular Weight
- 55712.075 Da
References
- Gonzalez AM, Walther D, Pazos A, Uhl GR: Synaptic vesicular monoamine transporter expression: distribution and pharmacologic profile. Brain Res Mol Brain Res. 1994 Mar;22(1-4):219-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Opioid receptor activity
- Specific Function
- Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma m...
- Gene Name
- SIGMAR1
- Uniprot ID
- Q99720
- Uniprot Name
- Sigma non-opioid intracellular receptor 1
- Molecular Weight
- 25127.52 Da
References
- Cobos EJ, del Pozo E, Baeyens JM: Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells. J Neurochem. 2007 Aug;102(3):812-25. doi: 10.1111/j.1471-4159.2007.04533.x. Epub 2007 Apr 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Thioesterase binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 48956.275 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Epinephrine binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49565.8 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein homodimerization activity
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR6
- Uniprot ID
- P50406
- Uniprot Name
- 5-hydroxytryptamine receptor 6
- Molecular Weight
- 46953.625 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 Mar;28(3):519-26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. In concert with DAPK1 at extrasynaptic site...
- Gene Name
- GRIN2B
- Uniprot ID
- Q13224
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 2B
- Molecular Weight
- 166365.885 Da
References
- Hattori K, Uchino S, Isosaka T, Maekawa M, Iyo M, Sato T, Kohsaka S, Yagi T, Yuasa S: Fyn is required for haloperidol-induced catalepsy in mice. J Biol Chem. 2006 Mar 17;281(11):7129-35. Epub 2006 Jan 10. [Article]
- Zhuravliova E, Barbakadze T, Natsvlishvili N, Mikeladze DG: Haloperidol induces neurotoxicity by the NMDA receptor downstream signaling pathway, alternative from glutamate excitotoxicity. Neurochem Int. 2007 Jun;50(7-8):976-82. Epub 2006 Nov 7. [Article]
- Gu WH, Yang S, Shi WX, Zhen XC, Jin GZ: Effects of (-)-stepholidine on NMDA receptors: comparison with haloperidol and clozapine. Acta Pharmacol Sin. 2007 Jul;28(7):953-8. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Steinmetz RD, Fava E, Nicotera P, Steinhilber D: A simple cell line based in vitro test system for N-methyl-D-aspartate (NMDA) receptor ligands. J Neurosci Methods. 2002 Jan 15;113(1):99-110. [Article]
- Sinor JD, Du S, Venneti S, Blitzblau RC, Leszkiewicz DN, Rosenberg PA, Aizenman E: NMDA and glutamate evoke excitotoxicity at distinct cellular locations in rat cortical neurons in vitro. J Neurosci. 2000 Dec 1;20(23):8831-7. [Article]
- Gallagher MJ, Huang H, Lynch DR: Modulation of the N-methyl-D-aspartate receptor by haloperidol: NR2B-specific interactions. J Neurochem. 1998 May;70(5):2120-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Cai G, Gurdal H, Smith C, Wang HY, Friedman E: Inverse agonist properties of dopaminergic antagonists at the D(1A) dopamine receptor: uncoupling of the D(1A) dopamine receptor from G(s) protein. Mol Pharmacol. 1999 Nov;56(5):989-96. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Prostaglandin-e2 9-reductase activity
- Specific Function
- NADPH-dependent reductase with broad substrate specificity. Catalyzes the reduction of a wide variety of carbonyl compounds including quinones, prostaglandins, menadione, plus various xenobiotics. ...
- Gene Name
- CBR1
- Uniprot ID
- P16152
- Uniprot Name
- Carbonyl reductase [NADPH] 1
- Molecular Weight
- 30374.73 Da
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1-9
- Molecular Weight
- 59940.495 Da
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Fang J, McKay G, Song J, Remillrd A, Li X, Midha K: In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes. Drug Metab Dispos. 2001 Dec;29(12):1638-43. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Fang J, McKay G, Song J, Remillrd A, Li X, Midha K: In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes. Drug Metab Dispos. 2001 Dec;29(12):1638-43. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Fang J, McKay G, Song J, Remillrd A, Li X, Midha K: In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes. Drug Metab Dispos. 2001 Dec;29(12):1638-43. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Data is limited to in vitro studies.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Tateishi T, Watanabe M, Kumai T, Tanaka M, Moriya H, Yamaguchi S, Satoh T, Kobayashi S: CYP3A is responsible for N-dealkylation of haloperidol and bromperidol and oxidation of their reduced forms by human liver microsomes. Life Sci. 2000 Nov 3;67(24):2913-20. [Article]
- Fang J, McKay G, Song J, Remillrd A, Li X, Midha K: In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes. Drug Metab Dispos. 2001 Dec;29(12):1638-43. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression]. Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. [Article]
- Otani K, Aoshima T: Pharmacogenetics of classical and new antipsychotic drugs. Ther Drug Monit. 2000 Feb;22(1):118-21. [Article]
- Kudo S, Ishizaki T: Pharmacokinetics of haloperidol: an update. Clin Pharmacokinet. 1999 Dec;37(6):435-56. doi: 10.2165/00003088-199937060-00001. [Article]
- Flockhart Table of Drug Interactions [Link]
- Pharm KGB Very Important Pharmacogene: CYP2D6 [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Kalgutkar AS, Taylor TJ, Venkatakrishnan K, Isin EM: Assessment of the contributions of CYP3A4 and CYP3A5 in the metabolism of the antipsychotic agent haloperidol to its potentially neurotoxic pyridinium metabolite and effect of antidepressants on the bioactivation pathway. Drug Metab Dispos. 2003 Mar;31(3):243-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Kalgutkar AS, Taylor TJ, Venkatakrishnan K, Isin EM: Assessment of the contributions of CYP3A4 and CYP3A5 in the metabolism of the antipsychotic agent haloperidol to its potentially neurotoxic pyridinium metabolite and effect of antidepressants on the bioactivation pathway. Drug Metab Dispos. 2003 Mar;31(3):243-9. [Article]
- Kudo S, Ishizaki T: Pharmacokinetics of haloperidol: an update. Clin Pharmacokinet. 1999 Dec;37(6):435-56. doi: 10.2165/00003088-199937060-00001. [Article]
- Fang J, Baker GB, Silverstone PH, Coutts RT: Involvement of CYP3A4 and CYP2D6 in the metabolism of haloperidol. Cell Mol Neurobiol. 1997 Apr;17(2):227-33. [Article]
- Galetin A, Clarke SE, Houston JB: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach. Drug Metab Dispos. 2002 Dec;30(12):1512-22. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Flockhart Table of Drug Interactions [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [Article]
- Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [Article]
- Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 21, 2024 02:38