Zink Wolfgang, Graf Bernhard M
Department of Anesthesiology, University of Heidelberg, Heidelberg, Germany.
Drug Saf. 2004;27(14):1093-114. doi: 10.2165/00002018-200427140-00003.
Ropivacaine is a long-acting amide-type local anaesthetic, released for clinical use in 1996. In comparison with bupivacaine, ropivacaine is equally effective for subcutaneous infiltration, epidural and peripheral nerve block for surgery, obstetric procedures and postoperative analgesia. Nevertheless, ropivacaine differs from bupivacaine in several aspects: firstly, it is marketed as a pure S(-)-enantiomer and not as a racemate, and secondly, its lipid solubility is markedly lower. These features have been suggested to significantly improve the safety profile of ropivacaine, and indeed, numerous studies have shown that ropivacaine has less cardiovascular and CNS toxicity than racemic bupivacaine in healthy volunteers. Extensive clinical data have demonstrated that epidural 0.2% ropivacaine is nearly identical to 0.2% bupivacaine with regard to onset, quality and duration of sensory blockade for initiation and maintenance of labour analgesia. Ropivacaine also provides effective pain relief after abdominal or orthopaedic surgery, especially when given in conjunction with opioids or other adjuvants. Nevertheless, epidurally administered ropivacaine causes significantly less motor blockade at low concentrations. Whether the greater degree of blockade of nerve fibres involved in pain transmission (Adelta- and C-fibres) than of those controlling motor function (Aalpha- and Abeta-fibres) is due to a lower relative potency compared with bupivacaine or whether other physicochemical properties or stereoselectivity are involved, is still a matter of intense debate. Recommended epidural doses for postoperative or labour pain are 20-40 mg as bolus with 20-30 mg as top-up dose, with an interval of >or=30 minutes. Alternatively, 0.2% ropivacaine can be given as continuous epidural infusion at a rate of 6-14 mL/h (lumbar route) or 4-10 mL/h (thoracic route). Preoperative or postoperative subcutaneous wound infiltration, during cholecystectomy or inguinal hernia repair, with ropivacaine 100-175 mg has been shown to be more effective than placebo and as effective as bupivacaine in reducing wound pain, whereby the vasoconstrictive potency of ropivacaine may be involved. Similar results were found in peripheral blockades on upper and lower limbs. Ropivacaine shows an identical efficacy and potency to that of bupivacaine, with similar analgesic duration over hours using single shot or continuous catheter techniques. In summary, ropivacaine, a newer long-acting local anaesthetic, has an efficacy generally similar to that of the same dose of bupivacaine with regard to postoperative pain relief, but causes less motor blockade and stronger vasoconstriction at low concentrations. Despite a significantly better safety profile of the pure S(-)-isomer of ropivacaine, the increased cost of ropivacaine may presently limit its clinical utility in postoperative pain therapy.
罗哌卡因是一种长效酰胺类局部麻醉药,于1996年获准用于临床。与布比卡因相比,罗哌卡因在手术、产科手术及术后镇痛的皮下浸润、硬膜外阻滞和周围神经阻滞方面同样有效。然而,罗哌卡因在几个方面与布比卡因不同:首先,它作为纯S(-)-对映体上市,而非消旋体;其次,其脂溶性明显较低。这些特性被认为可显著改善罗哌卡因的安全性,事实上,大量研究表明,在健康志愿者中,罗哌卡因的心血管和中枢神经系统毒性比消旋布比卡因小。大量临床数据表明,在分娩镇痛的启动和维持方面,硬膜外注射0.2%罗哌卡因在感觉阻滞的起效、质量和持续时间上与0.2%布比卡因几乎相同。罗哌卡因在腹部或骨科手术后也能有效缓解疼痛,尤其是与阿片类药物或其他佐剂联合使用时。然而,低浓度硬膜外给予罗哌卡因引起的运动阻滞明显较少。与布比卡因相比,罗哌卡因对参与疼痛传导的神经纤维(Aδ纤维和C纤维)的阻滞程度大于对控制运动功能的神经纤维(Aα和Aβ纤维),这是由于其相对效能较低,还是涉及其他物理化学性质或立体选择性,仍存在激烈争论。术后或分娩疼痛的推荐硬膜外剂量为推注20 - 40mg,追加剂量为20 - 30mg,间隔≥30分钟。或者,0.2%罗哌卡因可通过硬膜外持续输注给药,速率为6 - 14mL/h(腰椎途径)或4 - 10mL/h(胸椎途径)。术前或术后皮下伤口浸润,在胆囊切除术或腹股沟疝修补术中,使用100 - 175mg罗哌卡因已被证明在减轻伤口疼痛方面比安慰剂更有效,且与布比卡因效果相同,这可能与罗哌卡因的血管收缩效能有关。在上下肢周围阻滞中也发现了类似结果。罗哌卡因与布比卡因具有相同的疗效和效能,单次注射或连续导管技术的镇痛持续时间相似,可达数小时。总之,罗哌卡因作为一种新型长效局部麻醉药,在术后疼痛缓解方面,其疗效通常与相同剂量的布比卡因相似,但在低浓度时引起的运动阻滞较少,血管收缩作用较强。尽管罗哌卡因的纯S(-)-异构体安全性明显更好,但目前罗哌卡因成本的增加可能会限制其在术后疼痛治疗中的临床应用。