PHARMACOKINETICS OF ROPIVACAINE AND BUPIVACAINE FOR BILATERAL INTERCOSTAL BLOCKADE IN HEALTHY MALE-VOLUNTEERS

被引:64
作者
KOPACZ, DJ [1 ]
EMANUELSSON, BM [1 ]
THOMPSON, GE [1 ]
CARPENTER, RL [1 ]
STEPHENSON, CA [1 ]
机构
[1] ASTRA PAIN CONTROL AB,DEPT CLIN PHARMACOL,SODERTALJE,SWEDEN
关键词
ANESTHETIC TECHNIQUES; INTERCOSTAL NERVE BLOCK; ANESTHETICS; LOCAL; BUPIVACAINE; ROPIVACAINE; PHARMACOKINETICS; LOCAL ANESTHETICS;
D O I
10.1097/00000542-199411000-00007
中图分类号
R614 [麻醉学];
学科分类号
100217 ;
摘要
Background: Intercostal blockade produces the highest serum local anesthetic concentrations of all regional anesthetic techniques. The purpose of this study was to determine the pharmacokinetic properties of ropivacaine and bupivacaine after bilateral intercostal blockade. Methods: The pharmacokinetics of ropivacaine (n = 7) and bupivacaine (n = 7) were determined in adult human volunteers from venous samples drawn over 24 h after bilateral intercostal blockade of T5-T11 with 140 mg of either drug (0.25% plain solutions, 56 ml). Sensory (pinprick, temperature, and touch) and motor blockade (RAM-test and integrated electromyography) were assessed every 2 h. Results: There was no significant difference between the maximum plasma concentrations (C-max) obtained for either drug (ropivacaine 1.1 +/- 0.4 mu g/ml, bupivacaine 0.9 +/- 0.2 mu g/ml, P = 0.39), and there were no toxic signs observed in the obtained plasma concentration ranges. Plasma concentrations tended to peak (t(max)) earlier with ropivacaine (21 +/- 9 versus 30 +/- 8 min, P = 0.09). The terminal half-life (t(1/2 beta)) of ropivacaine (2.3 +/- 0.8 h) was significantly less than that for bupivacaine (4.6 +/- 2.6 h, P = 0.04). Sensory blockade measured by pinprick was of shorter duration with ropivacaine (6.0 +/- 2.5 h versus bupivacaine 10.0 +/- 3.0 h; P < 0.001). Likewise, motor blockade was less intense and of shorter duration for ropivacaine by RAM-test (P = 0.02). Conclusions: The results of this pharmacokinetic study indicate that 0.25% ropivacaine and 0.25% bupivacaine (56 ml, 140 mg) produce peak plasma levels less than those considered toxic when used in bilateral intercostal blockade. Studies of ropivacaine for intercostal blockade in surgical patients are necessary before the optimum concentration for efficacy and anesthetic/analgesic duration is identified.
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页码:1139 / 1148
页数:10
相关论文
共 29 条
[1]   TOXICOLOGICAL AND LOCAL ANESTHETIC EFFECTS OF OPTICALLY ACTIVE ISOMERS OF 2 LOCAL ANESTHETIC COMPOUNDS [J].
ABERG, G .
ACTA PHARMACOLOGICA ET TOXICOLOGICA, 1972, 31 (04) :273-&
[2]  
ARTHUR GR, 1988, ANESTH ANALG, V67, P1053
[3]  
BADER AM, 1989, ANESTH ANALG, V68, P724
[4]   CAPILLARY GAS-CHROMATOGRAPHIC METHOD FOR THE SIMULTANEOUS DETERMINATION OF LOCAL-ANESTHETICS IN PLASMA SAMPLES [J].
BJORK, M ;
PETTERSSON, KJ ;
OSTERLOF, G .
JOURNAL OF CHROMATOGRAPHY-BIOMEDICAL APPLICATIONS, 1990, 533 :229-234
[5]  
BRIDENBAUGH PO, 1975, BRIT J ANAESTH, V47, P306
[6]  
CHAMBERLAIN DP, 1987, ANESTH ANALG, V66, P57
[7]  
CONCEPCION M, 1990, ANESTH ANALG, V70, P80
[8]   THE EFFECT OF 0.5-PERCENT ROPIVACAINE ON EPIDURAL BLOOD-FLOW [J].
DAHL, JB ;
SIMONSEN, L ;
MOGENSEN, T ;
HENRIKSEN, JH ;
KEHLET, H .
ACTA ANAESTHESIOLOGICA SCANDINAVICA, 1990, 34 (04) :308-310
[9]  
DENSON D, 1984, CLIN PHARMACOL THER, V35, P155
[10]   SYSTEMIC FENTANYL ENHANCES THE SPREAD OF SPINAL ANALGESIA PRODUCED BY LIGNOCAINE [J].
FASSOULAKI, A ;
SARANTOPOULOS, C ;
CHONDRELI, S .
BRITISH JOURNAL OF ANAESTHESIA, 1991, 67 (04) :437-439