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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Drugs minimally effective for neuropsychiatric symptoms of dementia
From Journal of Family Practice, 5/1/05 by K.M. Sink

Sink KM, Holden KF, Yaffe K. Pharmacological treatment of neuropsychiatric symptoms of dementia. A review of the evidence. JAMA 2005; 293:596-608.

* Clinical Question

How useful are the various pharmacologic agents in the management of neuropsychiatric symptoms of dementia?

* Bottom Line

Pharmacologic agents are minimally, if at all, effective in managing the neuropsychiatric symptoms of dementia. The atypical antipsychotics olanzapine (Zyprexa) and risperidone (Risperdal) are the most effective, but these agents may increase the risk of stroke. The decision to use any of these drugs must be made on the basis of individual circumstances. (LOE=1a-)

Study Design Systematic review

Setting Various (guideline)

Synopsis

Every week it seems as if somebody publishes Neuropsychiatric symptoms of dementia--such as agitation, aggression, delusions, hallucinations, and wandering--increase caregiver stress and lead to an increased risk of hospitalization and nursing home placement. To evaluate the value of various pharmacologic agents in treating these symptoms, the investigators systematically reviewed the English-language literature using Medline, the Cochrane Database of Systematic Reviews, and a manual search of relevant bibliographies. They included only doubleblind placebo-controlled randomized trials or meta-analyses of drug trials of patients with dementia that used measured outcomes, including neuropsychiatric symptoms.

Two authors independently evaluated the quality of each trial and a third served as the final arbitrator when consensus was not reached. From an initial 78 articles reviewed, only 25 randomized controlled trials and 4 meta-analyses met the inclusion criteria. The investigators do not discuss the possibility of publication bias but report informally on the homogeneity of the results.

The atypical antipsychotics, including olanzapine and risperidone, showed modest benefit in reducing agitation/aggression, hallucinations, and delusions. However, the atypical antipsychotics may increase the risk of stroke. There is no clear evidence that typical antipsychotics, such as haloperidol (Haldol), thioridazine (Mellaril), thiothixene (Navane), and chlorpromazine (Thorazine) were useful for treating any neuropsychiatric symptoms. Haloperidol may be slightly useful for reducing aggression, but the adverse effects may outweigh the benefits.

There is no evidence that 1 typical antipsychotic is more efficacious than any other. Trials investigating the use of serotonergic antidepressants reported no efficacy for treating neuro-psychiatric symptoms other than depression, with the exception of i industry-sponsored trial of citalopram (Celexa), which reported a 10-point reduction (out of 168 points) in agitation compared with placebo.

Mood stabilizers (eg, valproate [Depakote] and carbamazepine [Tegretol]) were ineffective.

The available evidence on cholinesterase inhibitors (eg, galantamine [Reminyl], donepezil [Aricept], rivastigmine [Exelon]) shows a small benefit (summary estimate of 1.72-point improvement vs placebo on a scale of 0 to 120). Most of the statistically significant difference was driven by 2 studies on a drug never approved for use by the Food and Drug Administration in the United States because of toxicities.

Memantine (Namenda) may be of some benefit, but the evidence is mixed and unlikely to be clinically significant.

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