Haloperidol

Haloperidol

Haloperidol (Haldol)

Mechanism of action

Antipsychotic (butyrophenone derivative; first generation).

Non-selective blockade of dopaminergic Dreceptors in the brain. 

Some alpha-adrenoreceptor and muscarinic receptor blockade.

Highly potent with very high extrapyramidal toxicity and low sedative action.

Very low hypotensive effect.

Indications and dose

Contraindications

Parkinson’s disease
Severe CNS depression

Dementia with Lewy bodies

Long QTc

Side-effects

Extrapyramidal symptoms, parkinsonism

Involuntary body movements

Neuroleptic malignant syndrome

Amenorrhea, galactorrhea, impotence, hyperprolactinemia

QT interval prolongation

Constipation

Dry mouth

Drowsiness

Oculogyric crisis

Postural hypotension

Precautions

Additive effect with other sedative drugs, alpha-adrenoreceptor blockers, anticholinergics.

Pharmacokinetics

Onset of action: peak in 30 minutes

Duration of action: mean 2 hours

Bioavailability: Oral: 60-70%

Distribution: 90% protein bound

Metabolism: Hepatic

Half-life of elimination: 14-26 hours

Excretion: Urine

Directions for administration

Lactate for intravenous or intramuscular administration.

Decanoate only for intramuscular administration - must not be administered intravenously.

Medicinal forms

Tablet - 1.5 mg tablets

Intravenous - 1 vial = 5mg in 1 ml

Injection oil (decanoate)

Injection solution (lactate)

Drops - 2mg in 1 ml

References

  1. https://www.uptodate.com/contents/haloperidol-drug-information?search=haloperidol&source=panel_search_result&selectedTitle=1~148&usage_type=panel&kp_tab=drug_general&display_rank=1#F178529 
  2. https://bnf.nice.org.uk/drugs/haloperidol/ 
  3. https://litfl.com/pharm-101-haloperidol/