Kaeding C C, Hill J A, Katz J, Benson L
Department of Orthopaedic Surgery, Northwestern University Medical School, Chicago IL.
Arthroscopy. 1990;6(1):33-9. doi: 10.1016/0749-8063(90)90094-t.
Bupivacaine (Marcaine) pharmacokinetics were determined in 11 patients receiving the drug intraarticularly after arthroscopic procedures performed on the knee with patients under general anesthesia. Forty milliliters of 0.25% bupivacaine (100 mg) were given as a bolus into the intraarticular space of the knee of each patient. The thigh tourniquet was released 2-3 min after injection and blood samples were obtained 5, 10, 15, 20, 30, 60, 120, 180, 250, and 300 min after tourniquet release. Pharmacokinetic parameters obtained were (mean +/- SD): Vd beta 206 +/- 88 L; Cle 0.816 +/- 0.378 L/min; t 1/2 beta 189 +/- 84 min; ka 9.92 +/- 6.79 x 10/min; Cpmax 0.48 +/- 0.20 micrograms/ml; and tmax 43.4 +/- 23.1 min. Correlations between higher peak plasma concentrations and longer tourniquet times (p = 0.02) and shorter intervals from injection to tourniquet deflation (p = 0.03) were found using multiple linear regression. Our results indicate that injections of 100 mg of bupivacaine intraarticularly after knee arthroscopy will produce peak blood levels within the 1st h after surgery and that these levels will be well below those noted to produce toxic reactions. Peak levels can be minimized with shorter tourniquet inflation times and with longer injection to tourniquet release intervals. Ninety healthy adult outpatient knee arthroscopy patients also were studied to evaluate the effectiveness of bupivacaine in relieving postoperative knee discomfort when injected immediately postoperatively. The subjects were randomized into four groups: (a) intraarticular injection of saline, (b) intraarticular injection of bupivacaine, (c) subcutaneous injection of bupivacaine at the portal sites, and (d) both intraarticular and subcutaneous injection of bupivacaine.(ABSTRACT TRUNCATED AT 250 WORDS)
在11例接受膝关节关节镜手术且处于全身麻醉状态的患者中,测定了布比卡因(耐乐品)的药代动力学。给每位患者的膝关节关节腔内一次性推注40毫升0.25%布比卡因(100毫克)。注射后2 - 3分钟松开大腿止血带,并在松开止血带后5、10、15、20、30、60、120、180、250和300分钟采集血样。获得的药代动力学参数为(平均值±标准差):β相分布容积206±88升;清除率0.816±0.378升/分钟;β相半衰期189±84分钟;吸收速率常数9.92±6.79×10/分钟;血药浓度峰值0.48±0.20微克/毫升;达峰时间43.4±23.1分钟。使用多元线性回归发现,较高的血浆浓度峰值与较长的止血带使用时间(p = 0.02)以及注射至止血带放气的间隔时间较短(p = 0.03)之间存在相关性。我们的结果表明,膝关节镜检查后关节腔内注射100毫克布比卡因会在术后1小时内产生血药峰值水平,且这些水平远低于产生毒性反应的水平。通过缩短止血带充气时间和延长注射至止血带松开的间隔时间,可使峰值水平降至最低。还对90例健康成年门诊膝关节镜手术患者进行了研究,以评估术后立即注射布比卡因缓解术后膝关节不适的效果。受试者被随机分为四组:(a)关节腔内注射生理盐水;(b)关节腔内注射布比卡因;(c)在切口部位皮下注射布比卡因;(d)关节腔内和皮下均注射布比卡因。(摘要截取自250字)