酮咯酸氨丁三醇对舒芬太尼用于老年病人术后镇痛的节俭作用

目的 评价酮咯酸氨丁三醇对舒芬太尼用于老年妇科手术病人术后镇痛效果的影响.方法 择期妇科开腹手术病人60例,ASA分级Ⅱ或Ⅲ级,年龄≥65岁,体重指数18～24 kg/m2,采用随机数字表法,将病人随机分为2组(n=30):舒芬太尼组(S组)和酮咯酸氨丁三醇混合舒芬太尼组(T组).采用静吸复合全身麻醉下,术后采用静脉病人自控镇痛,T组镇痛药为酮咯酸氨丁三醇和舒芬太尼,负荷剂量酮咯酸氨丁三醇30 mg(手术结束前15 min时静脉注射),酮咯酸氨丁三醇180 mg混合舒芬太尼100μg稀释至100 ml,背景输注速率1.5 ml/h,PCA剂量1.6 ml,锁定时间20 min;S组镇痛药物为舒芬太尼,负荷剂量5μg(手术结束前15 min时静脉注射),舒芬太尼100μg稀释至100 ml,背景输注速率1.5 ml/h,PCA剂量1.6 ml,锁定时间20 min.术后48 h内维持临床有效镇痛(静态和动态VAS评分在3分以下),记录术后48 h舒芬太尼用量和不良反应的发生情况.结果 与S组比较,T组术后48 h舒芬太尼用量减少,不良反应发生率降低(P＜0.05).结论 酮咯酸氨丁三醇可减少舒芬太尼用于老年妇科手术病人术后镇痛的用量,产生显著的节俭作用,提高镇痛的安全性.     

酮咯酸氨丁三醇穴位注射治疗肾绞痛的疗效观察

目的：观察酮咯酸氨丁三醇穴位注射治疗肾绞痛的疗效。方法将176例肾绞痛患者随机分为治疗组和对照组,每组88例,均使用酮咯酸氨丁三醇30 mg,对照组采用肌肉注射,治疗组采用穴位注射（双侧三阴交和肾腧穴）,对比2组疗效（包括总有效率、止痛起效时间、疼痛完全缓解时间）。结果治疗组疗效优于对照组,差异具有统计学意义（P＜0.05）。结论将酮咯酸氨丁三醇用药途径由肌肉注射改为穴位注射后,可显著提高疗效,值得临床推广。     

Anti-hyperalgesic and anti-inflammatory effects of Ketorolac Tromethamine gel using pulsed ultrasound in inflamed rats

The aim of this study was to determine if a Ketorolac Tromethamine (KT) gel solution could be administered in vivo via phonophoretic transdermal delivery using pulsed ultrasound by examining its anti-hyperalgesic and anti-inflammatory effects in a rat carrageenen inflammation model. 1% carrageenan was injected into the plantar surface of the right hindpaw of a rat, and anti-hyperalgesic and anti-inflammatory effects of KT via phonophoretic transdermal delivery were examined. The changes in the mechanical and thermal hyperalgesia, nociceptive flexor reflex (NFR), as well as the swelling changes were determined. According to the anti-hyperagesia and anti-inflammation tests, which were used to determine the change in the pain thresh-old, NFR and swelling showed that the group given the phonophoretic transdermal delivery of KT exhibited significantly more noticeable anti-hyperalgesic and anti-inflammatory effects than those treated with the simple application of a KT gel. The transdermal application of KT gel using phonophoresis had significant anti-hyperalgesic and anti-inflammatory effects. These findings suggest that the transdermal administration of a KT gel using phonophoresis using pulsed ultrasound might be useful for treating acute inflammation and pain.     

Iontophoretic transport kinetics of ketorolac in vitro and in vivo: Demonstrating local enhanced topical drug delivery to muscle

The objective of the study was to investigate the iontophoretic delivery kinetics of ketorolac (KT), a highly potent NSAID and peripherally-acting analgesic that is currently indicated to treat moderate to severe acute pain. It was envisaged that, depending on the amounts delivered, transdermal iontophoretic administration might have two distinct therapeutic applications: (i) more effective and faster local therapy with shorter onset times (e.g. to treat trauma-related pain/inflammation in muscle) or (ii) a non-parenteral, gastrointestinal tract sparing approach for systemic pain relief. The first part of the study investigated the effect of experimental conditions on KT iontophoresis using porcine and human skin in vitro. These results demonstrated that KT electrotransport was linearly dependent on current density – from 0.1875 to 0.5 mA/cm² – (r² > 0.99) and drug concentration – from 5 to 20 mg/ml (r² > 0.99). Iontophoretic permeation of KT from a 2% hydroxymethyl cellulose gel was comparable to that from an aqueous solution with equivalent drug loading (584.59 ± 114.67 and 462.05 ± 66.56 μg/cm², respectively). Cumulative permeation (462.05 ± 66.56 and 416.28 ± 95.71 μg/cm²) and steady state flux (106.72 ± 11.70 and 94.28 ± 15.47 μg/cm² h), across porcine and human skin, were statistically equivalent confirming the validity of the model. Based on the results in vitro, it was decided to focus on topical rather than systemic applications of KT iontophoresis in vivo. Subsequent experiments, in male Wistar rats, investigated the local enhancement of KT delivery to muscle by iontophoresis. Drug biodistribution was assessed in skin, in the biceps femoris muscle beneath the site of iontophoresis (‘treated muscle’; TM), in the contralateral muscle (‘non-treated muscle’; NTM) and in plasma (P). Passive topical delivery and oral administration served as negative and positive controls, respectively. Iontophoretic administration for 30 min was superior to passive topical delivery for 1 h and resulted in statistically significant increases in KT levels in the skin (91.04 ± 15.48 vs. 20.16 ± 8.58 μg/cm²), in the biceps femoris at the treatment site (TM; 6.74 ± 3.80 vs. <LOQ), in the contralateral site (NTM; 1.26 ± 0.54 vs. <LOQ) and in plasma (P; 8.58 ± 2.37 μg/ml vs. <LOD). In addition to increasing bioavailability, iontophoretic administration of KT showed clear selectivity for local delivery to the biceps femoris at the treatment site – the TM:NTM ratio was 5.26 ± 1.45, and the TM:P and NTM:P ratios were 0.75 ± 0.32 and 0.14 ± 0.04, respectively. Furthermore, the post-iontophoretic concentration of KT in the ‘treated’ biceps femoris muscle and the muscle:plasma ratio were also superior to those following oral administration of a 4 mg/kg dose (6.74 ± 3.80 vs. 0.62 ± 0.14 μg/g and 0.75 ± 0.32 vs. 0.14 ± 0.03, respectively). In conclusion, the results demonstrate that iontophoresis of ketorolac enables local enhanced topical delivery to subjacent muscle; this may have clinical application in the treatment of localised inflammation and pain.     

酮咯酸氨丁三醇对烧伤患者镇痛效应及麻醉深度的影响

目的探讨酮咯酸氨丁三醇对烧伤患者镇痛效应及麻醉深度的影响。方法将50例美国麻醉医师协会（ASA）I～Ⅱ级择期行烧伤植皮手术患者随机分为2组,每组25例。实验组静脉推注酮咯酸氨丁三醇30mg,对照组输注生理盐水,记录不同时点的脑电双频指数（BIS）、平均动脉压（MAP）及心率（HR）。术中以异丙酚和瑞芬太尼靶控输注（TCI）维持麻醉,调节异丙酚血浆靶控浓度（Ct）,维持BIS稳定。结果麻醉剂诱导后,2组患者的HR及MAP均无显著性改变,但BIS均显著下降;给予药物后,实验组BIS继续下降。HR显著下降,MAP略有下降,而对照组上述指标均无明显变化。分别给予酮咯酸氨丁三醇和生理盐水后,实验组患者HR、MAP和BIS均显著低于对照组,差异有统计学意义;实验组异丙酚用量及苏醒期间咽喉疼痛、烦躁发生率均显著低于对照组,差异有统计学意义,而2组麻醉时间、呼吸恢复时间、睁眼时间及拔管时间比较,差异无统计学意义。结论酮咯酸氨丁三醇在不影响患者术后苏醒状态的情况下可产生明显镇痛效应,减少术中TCI异丙酚用量及不良反应的发生。     

酮咯酸氨丁三醇联合利多卡因用于妇科小手术镇痛效果观察

目的观察酮咯酸氨丁三醇联合利多卡因用于妇科小手术患者术中镇痛疗效和安全性。方法 87例择期行妇科麻醉手术的患者,随机分为观察组(44例)和对照组(43例),观察2组术后镇痛效果及不良反应。结果 2组患者手术时间、术中出血量比较无明显差异,观察组镇痛效果明显高于对照组。结论酮咯酸氨丁三醇联合利多卡因用于妇科急诊小手术镇痛效果好,值得推广。     

酮咯酸氨丁三醇在甲状腺手术术后镇痛的应用

目的研究单次静脉应用酮咯酸氨丁三醇对甲状腺手术术后镇痛的效果及不良影响。方法选择择期行甲状腺次全切除手术的患者60例,随机分成三组：A组手术结束前10min静脉推注生理盐水5mL,B组静脉推注酮咯酸氨丁三醇30mg,C组静脉推注芬太尼0．05mg。观察并记录三组患者VAS评分和Ramsay镇静评分、围术期副作用,记录引流量。结果使用酮咯酸氨丁三醇组与芬太尼组能明显减轻患者疼痛,且与对照组相比24h引流量无差异,副作用少。结论使用酮咯酸氨丁三醇能减轻术后疼痛,且不良反应少,可安全用于甲状腺手术术后止痛。     

酮咯酸复合曲马多超前镇痛对术后舒芬太尼静脉镇痛效果的影响

目的探讨酮咯酸复合曲马多用于妇科手术超前镇痛对术后舒芬太尼PCA效果的影响。方法择期于全麻下行妇科手术患者90例,随机分为3组,每组30例。实验组(T组)静注酮咯酸0.5 mg/kg复合曲马多2 mg/kg,侧管滴入;T1组静脉注入0.5 mg/kg酮咯酸,侧管滴入;对照组(N组)侧管滴入生理盐水5 mL。术毕三组均给予患者自控静脉镇痛泵术后镇痛(PCIA),镇痛药配方为舒芬太尼2μg/kg,稀释至100 mL,首次量为5mL,背景剂量2 mL/h,追加量0.5 mL,锁定时间15 min。记录术后1、4、6、12、24 h内的镇痛评分(VAS)、镇静评分(Ramsay)、患者自控镇痛泵的次数、不良反应及术后镇痛满意度。结果 T组和T1组患者术后1、4 h的VAS评分显著低于对照组(P<0.05),而T组1、4 h的Ramsay镇静评分高于T1组和N组(P<0.05)。T组及T1组术后24 h内PCA按压次数显著低于N组(P<0.05),各组患者在PCA期间不良反应发生率差异无统计学意义(P>0.05)。T组及T1组患者术后镇痛满意度高于N组(P<0.05)。结论酮咯酸复合曲马多用于妇科手术患者的超前镇痛,可明显减少舒芬太尼的用量,提高镇痛镇静质量。     

HPLC法检测酮咯酸氨丁三醇注射液中的有关物质

目的:建立一种测定酮咯酸氨丁三醇注射液有关物质的高效液相色谱法.方法:采用Alltima-C18(250 mm ×4.6 mm,5 μm)色谱柱,以0.02 mol·L-1磷酸二氢铵溶液(用磷酸调pH至3.0)-乙腈(65:35)为流动相;流速1.2 ml·min -1;柱温40℃;检测波长为313 nm;进样量为20 μl.结果:酮咯酸氨丁三醇峰与各杂质峰均能良好的分离.3批样品有关物质分别为0.15%、0.13%、0.12%,均符合规定.结论:本方法简便、灵敏、专属性好,可用于酮咯酸氨丁三醇注射液有关物质的检查.     

酮咯酸氨丁三醇联合盐酸哌替啶治疗肾绞痛的临床观察

目的:观察酮咯酸氨丁三醇联合盐酸哌替啶治疗肾绞痛的临床疗效。方法:将我院2008年5月-2010年5月收治的中、重度疼痛的肾绞痛患者120例随机均分为3组,均采取肌肉注射药物进行镇痛治疗。其中,Ⅰ组应用酮咯酸氨丁三醇60mg;Ⅱ组应用盐酸哌替啶100mg;Ⅲ组应用酮咯酸氨丁三醇30mg+盐酸哌替啶50mg。记录用药前以及用药后3h内(0、0.5、1、1.5、2、2.5、3h)的疼痛强度、疼痛强度差、疼痛缓解度以判断镇痛效果,并观察各组治疗中的不良反应情况。结果:用药后,3组均在0.5h起效,在中度疼痛的镇痛方面,Ⅲ组在用药3h内的所有观察点均优于Ⅰ、Ⅱ组(P<0.05),在2h时差异最为显著(P<0.01);在重度疼痛的镇痛方面,Ⅲ组在用药1.5、2、2.5、3h时效果优于Ⅰ、Ⅱ组(P<0.05);Ⅲ组的中度以上疼痛缓解程度除0.5h外,其余各点与Ⅰ、Ⅱ组比较,差异均有统计学意义(P<0.05)。Ⅲ组不良反应的发生率小于其他2组(P<0.05)。结论:酮咯酸氨丁三醇联合盐酸哌替啶治疗肾绞痛效果显著,同时可减少盐酸哌替啶的使用量,并可延长镇痛时间,且安全性较好。