Image:Haloperidol_decanoate_chemical_structure.png

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Haldol

Haloperidol (sold as Aloperidin®, Bioperidolo®, Brotopon®, Dozic®, Einalon S®, Eukystol®, Haldol®, Halosten®, Keselan®, Linton®, Peluces®, Serenace®, Serenase®, Sigaperidol®) is a conventional butyrophenone antipsychotic drug. It was developed in 1957 by the Belgian company Janssen Pharmaceutica and submitted to first clinical trials in Belgium in the same year. After being rejected by U.S. company Searle due to side effects, it was later marketed in the U.S. more...

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Chemistry

Haloperidol is an odourless white to yellow crystalline powder. Its chemical name is 4--4'-fluorobutyrophenone and its empirical formula is C₂₁H₂₃ClFNO₂

Pharmacology

Haloperidol is a neuroleptic, a butyrophenon. Due to its strong central antidopaminergic action, it is classified as a highly potent neuroleptic. It is approximately 50 times more potent than chlorpromazine on a weight basis (50mg chlorpromazine are equivalent to 1mg haloperidol). Haloperidol possesses a strong activity against delusions and hallucinations, most likely due to an effective dopaminergic receptor blockage in the mesocortex and the limbic system of the brain. Too, it blocks the dopaminergic action in the nigrostriatal pathways, which is the probable reason for the high frequency of extrapyramidal-motoric side-effects (dystonias, akathisia, pseudoparkinsonism). It has minor antihistaminic and anticholinergic properties, therefore cardiovascular and anticholinergic side-effects such as hypotension, dry mouth, constipation, etc., are seen quite infrequently, compared to less potent neuroleptics such as chlorpromazine. Haloperidol also has sedative properties and displays a strong action against psychomotor agitation, due to a specific action in the limbic system. It therefore is an effective treatment for mania and states of agitation. Additionally, it can be given as an adjuvant in the therapy of severe chronic pain.

The peripheral antidopaminergic effects of haloperidol account for its strong antiemetic activity. There, it acts at the CTZ (Chemical Trigger Zone). Haloperidol is useful to treat severe forms of nausea/emesis such as those resulting from chemotherapy. The peripheral effects lead also to a relaxation of the gastric sphincter muscle and an increased release of the hormone prolactin, with the possible emergence of breast enlargement and secretion of milk (lactation) in both sexes.

Pharmacokinetics

Oral dosing

Haloperidol is well absorbed after oral dosing. There is a first pass metabolism leading to a reduced oral biovailability of the drug (60 to 70%). Peak plasma-levels are observed after 3 to 6 hours.

I.m. injections

The drug is well and rapidly absorbed and has a high bioavailability. Plasma-levels reach their maximum within 20 minutes after injection.

I.v. injections

The bioavailability is 100% and the very rapid onset of action is seen within about ten minutes. The duration of action is 3 to 6 hours. If haloperidol is given as slow i.v.-infusion, the onset of action is retarded, but the duration prolonged compared to i.v.-injection.

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Antipsychotic use and cardiac events
From American Family Physician, 11/15/05 by Karl E. Miller

Patients treated with some antipsychotic medications have been shown to be at increased risk for ventricular arrhythmias, cardiac arrest, and sudden death. This includes patients with schizophrenia who are treated with thioridazine (Mellaril), haloperidol (Haldol), and other conventional antipsychotics (see accompanying table). This increased risk has been attributed to the QT-prolonging properties of conventional antipsychotics. The newer atypical antipsychotics may be more effective in the treatment of negative symptoms in schizophrenia, and they may have a lower risk of extrapyramidal side effects and tardive dyskinesia compared with conventional antipsychotics. Because of this improved side effect profile, the use of atypical antipsychotics has increased. The effects of atypical antipsychotics on cardiac events and sudden death has not been established. Liperoti and associates performed a case-control study to compare the effects of conventional and atypical antipsychotics on the risk of hospitalization for ventricular arrhythmias or cardiac arrest among older patients.

The authors collected data from the Systematic Assessment of Geriatric Drug Use via Epidemiology database for patients at Medicaid- and Medicare-certified nursing homes in six states. This information is linked to the Medicare inpatient claim files. Patients were included in the study if they had a primary diagnosis of cardiac arrest or ventricular arrhythmia. A control group consisting of residents in the same facilities was selected from the database.

A total of 649 patients had used antipsychotic medication within seven days of admission, and 2,962 patients were included in the control group. The use of conventional antipsychotics was associated with an increased risk of hospitalizations for cardiac arrest or ventricular arrhythmias (odds ratio [OR], 1.86; 95% confidence interval [CI], 1.27 to 2.74). The use of atypical antipsychotics was not associated with an increased risk for hospitalization. Patients with cardiac disease who took conventional antipsychotics were at increased risk of hospitalizations for ventricular arrhythmias compared with the control group (OR, 3.27; 95% CI, 1.95 to 5.47). The synergy index for this data was 1.19, indicating that there was no interaction between conventional antipsychotic use and preexisting cardiac disease.

The authors conclude that the use of conventional antipsychotic medications is associated with an increased risk of hospitalizations for cardiac arrest and ventricular arrhythmias, and that atypical antipsychotics are not associated with increased risk. They add that the use of conventional antipsychotics should be avoided, if possible, in patients with cardiac disease.

KARL E. MILLER, M.D. Liperoti R, et al. Conventional and atypical antipsychotics and the risk of hospitalization for ventricular arrhythmias or cardiac arrest. Arch Intern Med March 28, 2005;165:696-701.

Antipsychotic Medications

Atypical

Clozapine (Clozaril) Olanzapine (Zyprexa) Quetiapine (Seroquel) Risperidone (Risperdal)

Conventional

Chlorpromazine (Thorazine) Chlorprothixene (Taractan) Fluphenazine (Prolixin) Haloperidol (Haldol) Loxapine (Loxitane) Molindone (Moban) Perphenazine (Trilafon) Promazine * Thioridazine (Mellaril) Thiothixene (Navane) Trifluoperazine (Stelazine)

*--Not available in the United States.

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