Core pharmacology

Class Group

Non-Depolarizing
Aminosteroid

Legacy Cicm Level

Level 2

Introduction

Aminosteroid

Indications Uses

to facilitate intubation and controlled ventilation

Chemical Pharmaceutics

Monoquaternary

Presentation

Lyophilised powder with citrate & mannitol buffer, dil in water, stable for 24hrs

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 – 120s

Duration 35mins

Adverse Effects Toxicity

HISTAMINE RELEASE
- None
EFFECT ON ANS
- Minimal
OTHER
- Anaphylaxis

Critical illness myopathy

Distribution

Doesn’t cross BBB

Protein binding

PB 10%

Volume of distribution

VD 0.23L/kg

Metabolism

30-40% hepatic deacetylation to
3-desacetyl-vecuronium → 80% potency of vec with NMB effects,
↓ clearance & ↑duration of action→Accumulates
in renal failure

Excretion

Renal: 40% (metab)
Liver: 10-20% (metab)

Clearance

Pl cl 3-5ml/kg/min

Half-life

El t1/2: 50-110mins

Special Points

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

Reversible with sugammadex

Route And Dose

ED95 0.05 mg/kg
Int 0.1 mg/kg

Inf 1 mcg/kg/min