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Summary
General Info

PubChem

PubChem Compound 11495267

Name:	Haloperidol
PubChem Compound ID:	11495267
Description:	A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
Molecular formula:	C₂₁H₂₄Cl₂FNO₂
Molecular weight:	412.325 g/mol

DrugBank

Identification

Name:	Haloperidol
Name (isomeric):	DB00502
Drug Type:	small molecule
Description:	A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
Brand:	Eukystol, Brotopon, Serenase, Pms Haloperidol, Pekuces, Sernas, Serenelfi, Haldol La, Haldol Solutab, Sigaperidol, Mixidol, Haldol, Peridol, Halidol, Aloperidolo, Apo-Haloperidol, Lealgin Compositum, Haloperidol Decanoate, Halopoidol, Vesalium, Halosten, Keselan, Einalon S, Aloperidol, Aloperidon, Peluces, Novo-Peridol, Haloperidol Lactate, Pernox, Aloperidin, Halol, Sernel, Uliolind, Dozic, Galoperidol, Halopidol, Ulcolind, Haldol Decanoate, Bioperidolo, Linton, Haloperido, Serenace, Dozix, ALDO, Haloperidol Intensol, Halojust, Halopal
Category:	Antidyskinetics, Anti-Dyskinesia Agents, Antiemetics, Dopamine Antagonists, Antipsychotic Agents, Antipsychotics, Butyrophenones
CAS number:	52-86-8

Pharmacology

Indication:	For the management of psychotic disorders (eg. schizophrenia) and delirium, as well as to control tics and vocal utterances of Tourette's syndrome (Gilles de la Tourette's syndrome). Also used for the treatment of severe behavioural problems in children with disrubtive behaviour disorder or ADHD (attention-deficit hyperactivity disorder). Haloperidol has been used in the prevention and control of severe nausea and vomiting.
Pharmacology:	Haloperidol is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Haloperidol principal pharmacological effects are similar to those of piperazine-derivative phenothiazines. The drug has action at all levels of the central nervous system-primarily at subcortical levels-as well as on m... show more » Haloperidol is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Haloperidol principal pharmacological effects are similar to those of piperazine-derivative phenothiazines. The drug has action at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Haloperidol has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity. show less «
Mechanism of Action:	The precise mechanism whereby the therapeutic effects of haloperidol are produced is not known, but the drug appears to depress the CNS at the subcortical level of the brain, midbrain, and brain stem reticular formation. Haloperidol seems to inhibit the ascending reticular activating system of the brain stem (possibly through the caudate nucleus), ... show more » The precise mechanism whereby the therapeutic effects of haloperidol are produced is not known, but the drug appears to depress the CNS at the subcortical level of the brain, midbrain, and brain stem reticular formation. Haloperidol seems to inhibit the ascending reticular activating system of the brain stem (possibly through the caudate nucleus), thereby interrupting the impulse between the diencephalon and the cortex. The drug may antagonize the actions of glutamic acid within the extrapyramidal system, and inhibitions of catecholamine receptors may also contribute to haloperidol's mechanism of action. Haloperidol may also inhibit the reuptake of various neurotransmitters in the midbrain, and appears to have a strong central antidopaminergic and weak central anticholinergic activity. The drug produces catalepsy and inhibits spontaneous motor activity and conditioned avoidance behaviours in animals. The exact mechanism of antiemetic action of haloperidol has also not been fully determined, but the drug has been shown to directly affect the chemoreceptor trigger zone (CTZ) through the blocking of dopamine receptors in the CTZ. show less «
Absorption:	Oral-60%
Protein binding:	92%
Biotransformation:	Hepatic
Half Life:	3 weeks
Toxicity:	LD₅₀=165 mg/kg (rats, oral)
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take with food to reduce irritation, limit caffeine intake. Avoid alcohol.

Drug interaction:

Lithium	Possible extrapyramidal effects and neurotoxicity with this combination
Tolterodine	Haloperidol may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Tamoxifen	Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
Guanethidine	Haloperidol may decrease the effect of guanethidine.
Carbamazepine	Carbamazepine may decrease the serum concentration of haloperidol by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of haloperidol if carbamazepine is initiated, discontinued or dose changed.

Lithium	Possible extrapyramidal effects and neurotoxicity with this combination
Tolterodine	Haloperidol may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Tamoxifen	Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
Guanethidine	Haloperidol may decrease the effect of guanethidine.
Carbamazepine	Carbamazepine may decrease the serum concentration of haloperidol by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of haloperidol if carbamazepine is initiated, discontinued or dose changed.
Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Methyldopa	Methyldopa increases haloperidol effect or risk of psychosis
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Anisotropine Methylbromide	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Ketoconazole	Ketoconazole may increase the effect and toxicity of haloperidol.
Glycopyrrolate	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Tridihexethyl	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Propranolol	Increased effect of both drugs
Thioridazine	Increased risk of cardiotoxicity and arrhythmias
Ethopropazine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Atomoxetine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Fluconazole	Fluconazole may increase the effect and toxicity of haloperidol.
Mepenzolate	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Itraconazole	Itraconazole may increase the effect and toxicity of haloperidol.
Benztropine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Artemether	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Trimethobenzamide	Trimethobenzamide and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Toremifene	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
Clozapine	Clozapine, a moderate CYP2D6 inhibitor, may increase the serum concentration of haloperidol by decreasing its metabolism. Additive CNS despresant and anticholinergic effects may also occur. Monitor for changes in the therapeutic and adverse effects of haloperidol if clozapine is initiated, discontinued or dose changed. Also monitor for increased CNS depressant and anticholinergic effects during concomitant therapy.
Homatropine Methylbromide	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Haloperidol, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
Trazodone	The CYP3A4 inhibitor, Haloperidol, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. The CYP2D6 inhibitor, Trazodone, may increase the efficacy of Haloperidol by decreasing Haloperidol metabolism and clearance. Monitor for changes in Trazodone and Haloperidol efficacy/toxicity if either agent is initiated, discontinued or dose changed.
Rifabutin	The rifamycin decreases the effect of haloperidol
Rifampin	The rifamycin decreases the effect of haloperidol
Hyoscyamine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Oxyphencyclimine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Trihexyphenidyl	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Zuclopenthixol	Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Dicyclomine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Methantheline	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Scopolamine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Mesoridazine	Increased risk of cardiotoxicity and arrhythmias
Tamsulosin	Haloperidol, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Haloperidol is initiated, discontinued, or dose changed.
Procyclidine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Biperiden	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Terbinafine	Terbinafine may reduce the metabolism and clearance of Haloperidol. Consider alternate therapy or monitor for therapeutic/adverse effects of Haloperidol if Terbinafine is initiated, discontinued or dose changed.
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Tramadol	Haloperidol may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Haloperidol may decrease the effect of Tramadol by decreasing active metabolite production.
Telithromycin	Telithromycin may reduce clearance of Haloperidol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Haloperidol if Telithromycin is initiated, discontinued or dose changed.
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Triprolidine	Triprolidine and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Isopropamide	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Clidinium	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Orphenadrine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Trospium	Trospium and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trimipramine	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Voriconazole	Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of haloperidol by decreasing its metabolism. Additive QTc prolongation may also occur. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of haloperidol if voriconazole is initiated, discontinued or dose changed.
Atropine	The anticholinergic increases the risk of psychosis and tardive dyskinesia
Propantheline	The anticholinergic increases the risk of psychosis and tardive dyskinesia