Tb. Vree et al., REGIONAL METABOLISM OF ARTICAINE IN 10 PATIENTS UNDERGOING INTRAVENOUS REGIONAL ANESTHESIA DURING DAY-CASE SURGERY, British journal of clinical pharmacology, 44(1), 1997, pp. 29-34
Aims To study the pharmacokinetics of articaine and its metabolite art
icainic acid, in patients undergoing intravenous regional anaesthesia.
Methods Ten patients (three male, seven female, ASA class 1-2), sched
uled for surgery of the hand or forearm were included in the study. Ar
ticaine (40 mi, 0.5% solution (200 mg) was injected over 30 s. In tota
l fifteen arterial blood samples were taken; one before injection and
then at 10 min intervals, starting 10 min after completion of injectio
n, until the tourniquet was released; thereafter blood samples were dr
awn at intervals of 1, 5, 10, 15, 20, 25, 30, 45, 60, 75 and 90 min. T
he tourniquet was released 30 min after completing the injection. Resu
lts During tourniquet application and regional analgesia of 30 min dur
ation, 55% of articaine was hydrolysed by plasma (20%) and tissue (35%
) esterase activity to the metabolite articainic acid. After releasing
the tourniquet, articaine and its metabolite appeared in the blood; a
rticaine was rapidly eliminated with a t(1/2z) Of approximately 60 min
. The plasma concentration of the metabolite articainic acid was the s
um of the amount formed during IVRA (55%) and the amount formed after
tourniquet release (45%). Conclusions Articaine is a safe agent for in
travenous regional anaesthesia (IVRA) with rapid onset of good surgica
l anaesthesia. During tourniquet application and regional analgesia, 5
5% of the administered dose is already hydrolysed, thus reducing the c
hance of side effects after tourniquet release.