Pharmacology for Anaesthesia and Intensive Care

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11 Muscle relaxants and anticholinesterases

Rocuronium
This aminosteroidal drug was developed from vecuronium and is structurally differ-
ent at only four positions. Its main advantage is its rapid onset (intubating conditions
within 60–90 seconds), which in turn is due to its low potency.
Amuscle relaxant with a low potency must be given at a higher dose to achieve
aclinically significant effect. A higher number of molecules result in a greater con-
centration gradient from the plasma to the NMJ so that diffusion is faster and onset
time is reduced.

Presentation and uses
Rocuronium is prepared as a colourless solution containing 50 mg in 5 ml. At
0.6 mg.kg−^1 intubating conditions are reached within 100–120 seconds, although
this may be reduced to 60 seconds with higher doses (0.9–1.2 mg.kg−^1 ). Its duration
of action is similar to that of vecuronium.

Other effects
Cardiovascular – like vecuronium it has minimal cardiovascular effects, although
at high doses when used to facilitate a more rapid tracheal intubation, it may cause
an increase in heart rate.

Kinetics
Rocuronium is mainly excreted unchanged in the bile and to a lesser extent in the
urine, although some de-acetylated metabolites may be produced. Its duration of
action may be prolonged in hepatic and renal failure.

Pancuronium
Pancuronium is a bisquaternary aminosteroidal compound.

Presentation and uses
Pancuronium is presented as a colourless solution containing 4 mg in 2 ml and
should be stored at 4◦C. At 0.1 mg.kg−^1 intubating conditions are reached within
90–150 seconds. Its duration of action is about 45 minutes.

Other effects
Cardiovascular – pancuronium causes a tachycardia by blocking cardiac mus-
carinic receptors. It may also have indirect sympathomimetic actions by preventing
the uptake of noradrenaline at post-ganglionic nerve endings.

Kinetics
Between 10% and 40% is plasma protein bound, and in keeping with other drugs in
its class pancuronium has a low volume of distribution. About 35% is metabolized in
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