Description

Simple

A medication used to treat certain mental disorders and behavioral issues related to them, including agitation and an irritable mood.

Clinical

An antipsychotic agent used to treat schizophrenia and other psychoses, as well as symptoms of agitation, irritability, and delirium.

Overview

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... Read more

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 combat... Read more

Pharmacodynamic

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 limi... Read more

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... Read more

Absorption

Haloperidol is a highly lipophilic compound and is extensively metabolized in humans, which may cause a large interindividual variability in its pharmacokinetics.[ Read more

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.[ Read more

Volume of distribution

The apparent volume of distribution was found to range from 9.5-21.7 L/kg.[3] This high volu... Read more

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).[ Read more

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.[ Read more

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 a... Read more

Toxicity

Acute oral toxicity (LD50): 71 mg/kg in rats [MSDS].

Adverse Effects

Contraindications

  • Regions: Canada
  • Patient Conditions:
      • Name: Severely depressed states
      • Drugbank Id: DBCOND0107871
  • Regions: Canada
  • Patient Conditions:
      • Name: Basal Ganglia Lesions
      • Drugbank Id: DBCOND0032094
  • Regions: Canada
  • Patient Conditions:
      • Name: Children
      • Drugbank Id: DBCOND0032515
  • Route:
    • Intramuscular
    • Oral
  • Dose Form:
    • Injection
  • Regions: US
  • Patient Conditions:
      • Name: Severe toxic central nervous system depression
      • Drugbank Id: DBCOND0107801
  • Route:
    • Intramuscular
    • Oral
  • Dose Form:
    • Injection
  • Regions: US
  • Patient Conditions:
      • Name: Comatose states
      • Drugbank Id: DBCOND0107802
  • Route:
    • Intramuscular
    • Oral
  • Dose Form:
    • Injection
  • Regions: US
  • Patient Conditions:
      • Name: Parkinson’s disease
      • Drugbank Id: DBCOND0104397

Food Interactions

  • Avoid alcohol. Alcohol may potential hypotension and CNS adverse effects.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of Haloperidol can be increased when it is combined with (R)-warfarin.
(S)-Warfarin
The serum concentration of Haloperidol can be increased when it is combined with (S)-Warfarin.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Haloperidol can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Haloperidol.
2,5-Dimethoxy-4-ethylamphetamine
The therapeutic efficacy of 2,5-Dimethoxy-4-ethylamphetamine can be decreased when used in combination with Haloperidol.
2,5-Dimethoxy-4-ethylthioamphetamine
The therapeutic efficacy of 2,5-Dimethoxy-4-ethylthioamphetamine can be decreased when used in combination with Haloperidol.
3,5-diiodothyropropionic acid
The serum concentration of Haloperidol can be increased when it is combined with 3,5-diiodothyropropionic acid.
3,5-Dinitrocatechol
The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Haloperidol.
4-Bromo-2,5-dimethoxyamphetamine
The therapeutic efficacy of 4-Bromo-2,5-dimethoxyamphetamine can be decreased when used in combination with Haloperidol.
4-hydroxycoumarin
The serum concentration of Haloperidol can be increased when it is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The risk or severity of CNS depression can be increased when Haloperidol is combined with 4-Methoxyamphetamine.
5-androstenedione
The serum concentration of Haloperidol can be increased when it is combined with 5-androstenedione.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of CNS depression can be increased when Haloperidol is combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The serum concentration of Haloperidol can be increased when it is combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The serum concentration of Haloperidol can be increased when it is combined with 6-O-benzylguanine.
7-ethyl-10-hydroxycamptothecin
The serum concentration of Haloperidol can be increased when it is combined with 7-ethyl-10-hydroxycamptothecin.
7-Nitroindazole
The risk or severity of CNS depression can be increased when Haloperidol is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of CNS depression can be increased when Haloperidol is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Haloperidol.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Haloperidol.
17 References
  1. 1 . Niemegeers CJ, Laduron PM: Pharmacology and biochemistry of haloperidol. Proc R Soc Med. 1976;69 suppl 1:3-8.PubMed: 14331
  2. 2 . Gelders YG: Pharmacology, pharmacokinetics and clinical development of haloperidol decanoate. Int Clin Psychopharmacol. 1986 Jul;1 Suppl 1:1-11.PubMed: 3559159
  3. 3 . Kudo S, Ishizaki T: Pharmacokinetics of haloperidol: an update. Clin Pharmacokinet. 1999 Dec;37(6):435-56. doi: 10.2165/00003088-199937060-00001.PubMed: 10628896
  4. 4 . Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38.PubMed: 11873706
  5. 5 . 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.PubMed: 2033640
  6. 6 . 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.PubMed: 25007358
  7. 7 . 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.PubMed: 25592299
  8. 8 . 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.PubMed: 24242360
  9. 9 . Seeman P, Kapur S: Schizophrenia: more dopamine, more D2 receptors. Proc Natl Acad Sci U S A. 2000 Jul 5;97(14):7673-5.PubMed: 10884398
  10. 10 . 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.PubMed: 12629531
  11. 11 . Clinical pharmacology of atypical antipsychotics: an update Link
  12. 12 . Mechanism of Action of Antipsychotics, Haloperidol and Olanzapine in vitro Link
  13. 13 . Haloperidol Overview Link
  14. 14 . Haldol Decanoate Link
  15. 15 . FDA Approved Drug Products: Haldol (haloperidol) for injection Link
  16. 16 . FDA Label - haloperidol File
  17. 17 . Health Canada Monograph - haloperidol File