COMPARISON OF THE EFFECTS AND DISPOSITION KINETICS OF LIDOCAINE AND (+ -)PRILOCAINE IN PATIENTS UNDERGOING AXILLARY BRACHIAL-PLEXUS BLOCK DURING DAY-CASE SURGERY/
Mam. Simon et al., COMPARISON OF THE EFFECTS AND DISPOSITION KINETICS OF LIDOCAINE AND (+ -)PRILOCAINE IN PATIENTS UNDERGOING AXILLARY BRACHIAL-PLEXUS BLOCK DURING DAY-CASE SURGERY/, Clinical drug investigation, 16(3), 1998, pp. 241-250
Objective: The aim of this investigation was to compare the clinical e
ffects and pharmacokinetics of lidocaine and prilocaine in two groups
of 15 patients undergoing axillary brachial plexus anaesthesia. Method
s: The study had a randomised design. Patients were allocated to one o
f the two groups of 15. Each group received either lidocaine (600mg =
2.56 mmol/L + 5 mg/L adrenaline) or prilocaine (600mg = 2.72 mmol/L 5 mg/L adrenaline), injected over a period of 30 seconds. Onset of the
surgical analgesia was defined as the period from the end of the inje
ction of the local anaesthetic to the loss of pinprick sensation in th
e distribution of all three nerves. Results: The mean onset time of su
rgical analgesia of both lidocaine and prilocaine was 10 minutes. Lido
caine was biexponentially eliminated with a rapid elimination phase ha
lf-life (t1/2 alpha) of 9.95 +/- 14.3 minutes and a terminal eliminati
on phase half-life (t1/2 beta) of 2.86 +/- 1.55 hours. Lidocaine was m
etabolised to MEGX (monoethylglycylxylidide); time to reach maximum pl
asma concentration (t(max)) 2.3 +/- 0.8 hours; maximum plasma concentr
ation (C-max) 0.32 +/- 0.13 mg/L; t1/2 beta 2.4 +/- 2.4 hours. Lidocai
ne total body clearance was 67.8 +/- 28.8 L/h. Prilocaine was rapidly
and biexponentially eliminated with a t1/2 alpha of 9.4 +/- 18.4 minut
es and a t1/2 beta of 2.12 +/- 1.28 hours. The total body clearance of
prilocaine (150 +/- 53 L/h) was higher than that of lidocaine (p = 0.
0255). Both compounds demonstrated a comparable volume of distribution
(Vd), while the volume of distribution at steady-state (V-ss) and the
volume of distribution in the second compartment (V-beta) values of p
rilocaine were a factor of 1.6 higher than those of lidocaine (p < 0.0
01). Both compounds showed a comparable t1/2 alpha (p > 0.8) and a com
parable t1/2 beta (p = 0.26). Conclusion: Following axillary administr
ation, lidocaine and prilocaine demonstrated similar pharmacokinetic b
ehaviour and could therefore be used as the clinical preference for th
is regional anaesthesia technique.