Folia Pharmacol. Jpn.133 1 2 Chiroscience UCB S RR-..% AA C IC C/A A/ A R- II/ III II/III Chiroscience UCB S 1 - E-mail: koji_taya@maruishi-pharm.co.jp Author: Koji Taya, Satoshi Shimizu Title: Levobupivacaine hydrochloride injection(popscaine ): Pharmacological characteristics and clinical study result.
.%.% S RR - 1. 1 In vitro % O % CO.. Krebs ml/min.. Hz R- 1 M % Levobupivacaine... Bupivacaine... R-bupivacaine... Ropivacaine... n levobupivacaine M Krebs mv %..%R-..%..%..% R-... R- In vitro in vivo In vivo -....%...%. ml L tail-flick cm %MPEpercent of maximum possible effect %MPE Tail-flick / % %MPE AUC %MPE Time tail-flick %MPET%MPE %
%MPE AUC%MPET..%.%...%.%...%.%... pka Whiteside pka pka pka mm mg in vitro Brüu TTX Na 2 AUC of %MPE %MPET Levobupivacaine Bupivacaine......... Ropivacaine......... -..%. ml levobupivacaine /ropivacainebupivacaine% 3 AUC of %MPE %MPET Levobupivacaine Bupivacaine......... Ropivacaine......... -..% L levobupivacaine /ropivacainebupivacaine%
4 pka % Lidocaine. Mepivacaine. Bupivacaine.. Levobupivacaine.. Ropivacaine. 21 20 6*P 005 **P 001***P 0001..%..%.%.%.% Kanai Kanai AUC %MPET.%.%.% Bader 3 9 10 P 005 11
550 % A A C A/A C/A Levobupivacaine..... Bupivacaine..... R-bupivacaine..... Ropivacaine..... C A Oda TTX TTX IC.M TTX IC.M TTX TTX TTX Bader Oda R Oda in vivo in vitro Uta Uta 450 AA C IC IC C/A A/A R- A C M M A.% A
C.%.% A/A. C/A. R- M A C A Na Na Na Novakovic Na Na v.. Nax Na Na Na 2. mg/kg/.%. mg/kg. mg/kg. mg/kg Huang mg mg mg mg 3 Valenzuela hkv. Ltk- 6 mg s mg Levobupivacaine. na na Bupivacaine * * ** ** SDna: *P.**P.levobupivacaine P.levobupivacaine
ms M R- M..%..% Valenzuela M R- M..%..% Vanhoutte V max APDV max.% R-.% APD.% R-.% Graf R- % % M R- Mazoit RRS QRS R- R 7 2 mg/kg.-. mg/kg mg/kg CNS cardiovascular collapsecc Morishima CC/CNS....... mg/kg. mg/kg. mg/kg 2. 1 II.% ml III.%.% Th.....
8 2.. kg a.% Levobupivacaine Bupivacaine Ropivacaine mg/kg... s b... s s s s s s s s s s f f s s s f f f s f f f s f f d d d ab sfd... Bromage scale Bromage scale............ Bromage scale III III III.%.% II.% ml/h III.%.%.. mg.%.. mg.%.% VAS Visual Analog Scale Bromage Scale.%.% 2 II/III.%/ III.%.%/
QOL.. ;.. p. -.,,.. ;. p. -. Albright GA. Anesthesiology. ;:-............. Whiteside JB, et al. Br J Anesthesia. ;():-.. Levobupivacaine in vitro.. Bräu ME, et al. Eur J Aanesthesiol. ;:-. Kanai Y, et al. Reg Anesth Pain Med. ;():-. Bader AM, et al. Anesth Analg. ;:-.,. Pain Clinic. ; Spring Suppl:S-S. Oda A, et al. Aneth Analg. ;:-. Uta D, et al. th Annual Meeting of Society for Neuroscience Washington DC, USA.. Program No.... Levobupivacaine has more inhibitory effects on action potentials in A and C fibers than the racemic mixture or R(+)enantiomer in adult rat DRG neurons.. Novakovic SD, et al. Trends Neurosci. ;:-.,.. ;():-.. Comparative acute systemic toxicity of intravenously administered Levobupivacaine, Bupivacaine and Ropivacaine in the dog.. Huang YF, et al. Anesth Analg. ;:-. Valenzuela C, et al. Biophys J. ;:-. Valenzuela C, et al. Circulation. ;():-. Vanhoutte F, et al. Br J Pharmacol. ;:-. Graf BM, et al. Anesthesiology. ;:-. Mazoit JX, et al. Anesth Analg. ;:-. Morishima HO, et al. Anesthesiology. ;:-.. Treatment of acute systemic toxicity after the rapid in travenous injection of Levobupivacaine, Bupivacaine and Ropivacaine in the conscious dog..,.. ;(Suppl):-.. A Randomized, Multicentre, Double Blind, Parallel Group Study to evaluate the dose response, safety & kinetics of ml of.% &.% Levobupivacaine (S-Enantiomer) with ml of.% Bupivacaine (Racemic Mixture) in patients undergoing Elective Surgery under Epidural Anaesthesia... Double Blind Randomized Controlled Trial of.% Levobupivacaine compared to.% Bupivacaine for Epidural Anaesthsia in Patients undergoing Major Elective Abdominal Surgery... A Double-Blind Randomized Controlled Trial of.% Levobupivacaine Compared to.% Bupivacaine for Extradural Anaesthsia in Patients Undergoing Elective Caesarean Section... Double-Blind, Randomized, Controlled Trial of.% Levobupivacaine Compared to.% Bupivacaine for Epidural Anesthesia in Patients Undergoing Elective Cesarean Section..,.. ;(Suppl):-.