TY - JOUR
T1 - Effect of penbutolol on lidocaine kinetics
AU - Ochs, H. R.
AU - Skanderra, D.
AU - Abernethy, D. R.
AU - Greenblatt, D. J.
N1 - Copyright:
Copyright 2004 Elsevier B.V., All rights reserved.
PY - 1983
Y1 - 1983
N2 - The effect of penbutolol (Betapressin®), a stereospecific β-adrenergic antagonist, on the pharmacokinetics of a single dose of intravenous lidocaine was evaluated in seven healthy volunteers. Subjects received a single 100-mg lidocaine intravenous dose of lidocaine hydrochloride, one in the control state and a second time during coadministration of penbutolol, 60 mg daily. Lidocaine volume of distribution was significantly increased during penbutolol treatment (4.9 vs 3.4 l/kg, p<0.005), resulting in a significant prolongation of elimination half-life (2.5 vs 2.0 h, p<0.025). The mechanism of the distributional shift is not established, but may result from a change in the pattern of peripheral blood flow and therefore the profile of tissue uptake of lidocaine. Total metabolic clearance of lidocaine, however, was not significantly altered by penbutolol (23.0 vs 19.4 ml/min/kg). The present study of healthy volunteers suggests that penbutolol increases lidocaine volume of distribution. If the finding also applied to patients, a higher loading dose of lidocaine might be necessary.
AB - The effect of penbutolol (Betapressin®), a stereospecific β-adrenergic antagonist, on the pharmacokinetics of a single dose of intravenous lidocaine was evaluated in seven healthy volunteers. Subjects received a single 100-mg lidocaine intravenous dose of lidocaine hydrochloride, one in the control state and a second time during coadministration of penbutolol, 60 mg daily. Lidocaine volume of distribution was significantly increased during penbutolol treatment (4.9 vs 3.4 l/kg, p<0.005), resulting in a significant prolongation of elimination half-life (2.5 vs 2.0 h, p<0.025). The mechanism of the distributional shift is not established, but may result from a change in the pattern of peripheral blood flow and therefore the profile of tissue uptake of lidocaine. Total metabolic clearance of lidocaine, however, was not significantly altered by penbutolol (23.0 vs 19.4 ml/min/kg). The present study of healthy volunteers suggests that penbutolol increases lidocaine volume of distribution. If the finding also applied to patients, a higher loading dose of lidocaine might be necessary.
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M3 - Article
C2 - 6686773
AN - SCOPUS:0021070213
SN - 0004-4172
VL - 33
SP - 1680
EP - 1681
JO - Arzneimittel-Forschung/Drug Research
JF - Arzneimittel-Forschung/Drug Research
IS - 12
ER -