Background: Intramuscular rocuronium, in doses of 1,000 mu g/kg in inf
ants and 1,800 mu g/kg in children, produces complete twitch depressio
n in 5-6 min. To determine the rare and extent of absorption of rocuro
nium after intramuscular administration, blood was sampled at Various
intervals after rocuronium administration by both intramuscular and in
travenous routes to determine plasma concentrations (Cp) of rocuronium
. Methods: Twenty-nine pediatric patients ages 3 months to 5 yr were a
nesthetized with N2O and halothane. The trachea a as intubated, ventil
ation was controlled, and adductor pollicis twitch tension was measure
d. When anesthetic conditions were stable, rocuronium (1,000 mu g/kg f
or infants and 1,800 mu g/kg for children) was injected either intramu
scularly (in the deltoid muscle) or intravenously. Four venous plasma
samples were obtained from each child 2-240 min after rocuronium admin
istration. A mixed-effects population pharmacokinetic analysis was app
lied to these values to determine bioavailability, absorption rate con
stant, and time to peak Cp with intramuscular administration. Results:
With intramuscular administration, rocuronium's bioavailability avera
ged 82.6% and its absorption rate constant was 0.105 min(-1). Simulati
on indicated that Cp peaked 13 min after rocuronium was given intramus
cularly, and that 30 min after intramuscular administration, less than
4% of the administered dose remained to be absorbed from the intramus
cular depot. Conclusions: After rocuronium is administered into the de
ltoid muscle, plasma concentrations peak at 13 min, and approximately
80% of the administered drug is absorbed systemically.