Core pharmacology

Class Group

Anti-emetic

Dopamine Antagonist

Legacy Cicm Level

Level 3

Introduction

Butyrophenone D2-antagonist

Indications Uses

1. Central and peripheral D2
2. Post-synaptic GABA antagonism
3. Other effects:
- Inhibition of 5-HT3
- Anti-H1 effects

Mechanism of action

1. Central and peripheral D2
2. Post-synaptic GABA antagonism
3. Other effects:
- Inhibition of 5-HT3
Anti-H1 effects

Physiological effects

CVS- cardiostable. Alpha1 antagonism may lead to hypotension if hypovolaemic

CNS- neurolepsis

Adverse Effects Toxicity

1. NMS
2. EPS
3. Sedation
4. Hyperprolactinaemia
QTc prolongation

Protein binding

90% PB

Volume of distribution

Vd 1.5-2.5L/kg

Metabolism

Extensive hepatic

Excretion

75% renal (1% unchanged)