Haloperidol

Chemical

Butyrophenone antipsychotic → first gen antipsychotic

Use

  1. Delirium & agitation in ICU
  2. Schizophrenia
  3. N&V

Presentation

Tablets, syrup solution (5mg/mL)

Dose

1 – 15mg (divided doses)

Route

PO/IV/IM

Onset

IM → 30 mins

PO → 60 mins

CMAX → 6hrs

MoA (mechanism)

  1. Central dopaminergic blockade
  2. Post synaptic GABA antagonism

PD

CNS

  • ↓motor activity
  • Anxiolysis
  • ↑seizure threshold
  • Indifference to external environment

CVS – ↓BP (some α1 antagonism)

GI – antiemesis (powerful) by ↑vomiting threshold @ CTZ

PK

A

OBA 60%

D

90% PPB

VD 9 – 20L/kg

M

Liver glucuronidation then reduction

(some) active metabolites

E

Metabolites via urine

15% faeces

t ½ B 10 – 45hrs

Adverse Effects

  • Hypotension
  • Abnormal LFTs
  • GI & haematopoietic disturbances
  • EXTRAPYRAMIDAL → NMS