Core pharmacology

Class Group

Non-Depolarizing
Aminosteroid

Legacy Cicm Level

Level 2

Introduction

Aminosteroid

Indications Uses

to facilitate intubation and controlled ventilation

Chemical Pharmaceutics

Bisquaternary

Presentation

Clear, colourless solution, 2mg/mL as pancuronium bromide

Mechanism of action

ND-NMB acts as competitive antagonist →
competes with ACh for nAChR binding → blocks cholinergic transmission → muscle
relaxation (> 70% post-synaptic nAChR occupancy required to result in block)
ND-NMB also inhibits pre-synaptic ACh receptors →prevents enhancement of ACh
release → fade with repeated stimulation

Onset Peak Duration

Intubate @ 90 – 150s

Duration 85mins

Adverse Effects Toxicity

HISTAMINE RELEASE
- None
EFFECT ON ANS
- Can be vagolytic ( Cardiac M2 AChR block →↑HR)
OTHER
- Anaphylaxis

Distribution

Doesn’t cross BBB

Protein binding

PB 20 – 60%

Volume of distribution

VD 0.27L/kg

Metabolism

10-20% hepatic deacetylation to
multiple metab:
3-hydroxy derivative → 50% potency of panc.
Delayed Total clearance & sign prolonged durn of axn in ren/hep failure

Excretion

Renal: 60-80%
Liver: 10%

Clearance

Pl cl 2ml/kg/min

Half-life

El t1/2: 130mins

Special Points

Duration prolonged by:
- ↓K ↓Ca ↑Mg
- ↑pH ↑PaCO2
- ↓temp ↓protein Dehydration

Reversible with sugammadex

Route And Dose

ED95 0.07 mg/kg
Int 0.1 mg/kg

Inf -