Pharmacopeia

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Field ROCURONIUM
Neuromuscular · Neuromuscular · Level 1
CISATRACURIUM
Neuromuscular · Neuromuscular · Level 1
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

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

Distribution

Doesn’t cross BBB

—
Protein binding

PB 10%

PB 15%

Volume of distribution

VD 0.2L/kg

VD 0.15L/kg

Metabolism

<5% Metabolism Hep

77% Hofmann degradation →
laudanosine and quat.
monoacrylates
Minimal ester hydrolysis
Inactive metabolites

Excretion

Renal: 30-40%
Liver: 60%

Ren: 10-30% (laud.)
Liver: (laudanosine)

Clearance

Pl cl: 3ml/kg/min

Pl cl 4-5ml/kg/min

Half-life

El t1/2: 90mins

El t1/2: 25mins

Adverse Effects Toxicity

HISTAMINE RELEASE
- None
EFFECT ON ANS
- Can be vagolytic (↑HR)
OTHER
- Anaphylaxis
- Pain on injection

HISTAMINE RELEASE
- None
VAGOLYSIS
- None
OTHER
- Anaphylaxis

Chemical Pharmaceutics

Monoquaternary

Bisquaternary. 1 of 10 stereoisomers. In atrac (15% wt, 50% pot)

Class Group

Non-Depolarizing
Aminosteroid

Non-Depolarizing
Isoquinolone

Indications Uses

1. to facilitate tracheal intubation during routine and modified rapid
sequence induction
2. for controlled ventilation.

to facilitate intubation and controlled ventilation

Introduction

Aminosteroid

Benzylisoquinolinium ester

Legacy Cicm Level

Level 1

Level 1

Onset Peak Duration

Int @ 100 – 120s
RSI @ 60s
Duration 35mins

Intubate @ 3 – 5min

Duration 45mins

Presentation

Clear, colourless solution, 10mg/mL rocuronium bromide

Clear, 10mg in 5mL as cisatracurium besylate, stored at 4°C.

Route And Dose

ED95 0.3 mg/kg
Int 0.6 mg/kg
RSI 0.9 ~ 1.2 mg/kg
Inf 9 – 12 mcg/kg/min

ED95 0.05 mg/kg
Int 0.15 mg/kg

Inf 1 – 2 mcg/kg/min

Special Points

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

Reversible with sugammadex

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