Alfentanil (R 39 209) — a particularly short-acting intravenous narcotic analgesic in rats

Alfentanil, N-{1-[2-(4-ethyl-4,5-dihydro-5-oxo-1H-tetrazol-l-yl)ethyl]-4-(methoxymethyl)-4-piperidinyl}-N-phenyl propanamide monohydrochloride monohydrate, is a chemically novel, potent, extremely short-acting and safe intravenous morphine-like agent in laboratory animals. As an analgesic in rats, alfentanil is 137 times as potent as pethidine (tail withdrawal reaction test: i.v. ED50 is 6.04 mg/kg for pethidine and 0.044 mg/kg for alfentanil). The safety margin in rats is 1,080 (LD50: 47.5 mg/kg i.v.). Alfentanil reaches its peak effect within 2 min after injection, and its duration of action is very short: at two times its lowest ED50 the drug has a duration of action of 10 min. This duration is 30–35 min for pethidine and fentanyl, and 120 min for morphine. The narcotic antagonist naloxone produces an immediate and complete reversal of all morphine-like effects of alfentanil. In dogs, alfentanil is a potent antiemetic (ED50: 0.032 mg/kg i.v.) with a safety margin of over 850 (LD50: > 20 mg/kg i.v.).     

盐酸阿芬太尼在手术病人中的药代动力学研究

本文进行了两组不同剂量的阿芬太尼在14例手术病人中药代动力学研究。7例一次性iv 80μg·kg~(-1)阿芬太尼,另7例一次性iv 40μg·kg~(-1)。用RIA方法测定0-8 h阿芬太尼的血浆浓度和0-48 h尿中的回收率。研究表明:阿芬太尼在两组病人体内的药代动力学过程均为3室模型。阿芬太尼的初级消除很快,给药后30 min内90％的原型药被消除。病人血浆浓度未发现2次上升现象。二者药-时曲线接近平行,说明阿芬太尼的代谢过程为1级消除。两组阿芬太尼的药代动力学数据经t检验无显著差异(P>0.05)。阿芬太尼的快、慢分布相和消除相的半衰期t_(1/2)π,t_(1/2)α和t_(1/2)β分别为0.71 min±s 0.37 min,11.66 min±s 3.46 min和86.12 min±s 19.15 min;平均总体和中心室的分布容积Vd、Vc分别为34.22L±s 8.27L和4.23L±s 1.72L;平均总体清除率Cl为0.29 L·min~(-1)±s 0.08L·min~(-1)。另外,k_(12)/k_(21)为1.5,k_(13)/k_(31)为3.5,k_(10)大于k_(31)。用药后48 h以内,40μg·kg~(-1)组和80μg·kg~(-1)组的病人尿中排出的原形阿芬太尼分别占总给药量的0.68％±s 0.72％和0.66％±s 0.54％。其肾清除率分别为0.0016 L·min~(-1)±s 0.0011 L·min~(-1)和0.0021 L·min~(-1)±s 0.0015 L·min~(-1)。     

Alfentanil hydrochloride: a new short-acting narcotic analgesic for surgical procedures

The chemistry, pharmacology, pharmacokinetics, clinical use, adverse effects, dosage, and administration of the short-acting synthetic narcotic analgesic alfentanil hydrochloride are reviewed. Alfentanil is a tertiary amine with an ionization constant of 6.5, resulting in approximately 10% ionization at physiologic pH. When compared with fentanyl, alfentanil has a faster onset and one third the duration of action, one fourth to one tenth the potency, less lipid solubility, greater protein binding, and a much greater unionized fraction at physiologic pH. Alfentanil is approximately 20-40 times less potent than sufentanil on a weight basis, but it has a faster onset and shorter duration of action. After i.v. injection, alfentanil is distributed in the body according to a two- or three-compartment model. When given to young and middle-aged patients for various surgical procedures, alfentanil has an elimination half-life of 70-99 minutes independent of the dose or route of administration. Clinical studies comparing alfentanil with fentanyl in short surgical procedures are reported; alfentanil produces earlier peak analgesic effect, faster recovery of consciousness, and a more pronounced narcotic effect without increased adverse effects. When alfentanil was given in high doses for anesthesia induction, chest-wall rigidity occurred frequently. Like fentanyl, alfentanil was found to produce a high incidence of nausea and vomiting. It was more effective when administered by infusion than by bolus. Alfentanil is useful for supplementation of analgesia for outpatient surgical procedures, as an infusion for maintenance of anesthesia during surgery, and perhaps as an induction agent.     

妇科腔镜手术后氟比洛芬酯静脉镇痛的临床观察

目的观察妇科腔镜手术后患者氟比洛芬酯自控静脉镇痛（PCIA）的效果与不良反应。方法选择ASAⅠ～Ⅱ级妇科腔镜手术后行PCIA患者60例,随机均分为两组。芬太尼组术后PCIA予芬太尼500ug＋昂丹司琼8mg;氟芬组术后PCIA予氟比洛芬酯100mg＋芬太尼250Pg＋昂丹司琼8mg,手术结束前10min静脉予氟比洛芬酯50mg为负荷剂量。两组PCIA均以昂丹司琼作为止吐药,均用生理盐水稀释至100ml。两组PCIA泵的设置相同：维持量2ml／h,单次负荷剂量0．5ml,锁定时间15min。观察两组术后48h的镇痛评分（VAS）、镇静评分（SS）及不良反应发生率。结果两组术后镇痛及镇静评分差异无显著性（P〉0．05）,氟芬组药物不良反应发生率低于芬太尼组。结论氟比洛芬酯用于妇科腔镜手术后PCIA,镇痛效果与单纯芬太尼相似,但不良反应明显减少,提高了镇痛质量。     

氟比洛芬酯芬太尼用于腰椎管狭窄镇痛研究

目的研究氟比洛芬酯复合小剂量芬太尼与单纯芬太尼和单纯氟比洛芬酯用予椎管狭窄扩大成形椎弓钉内固定手术后静脉镇痛的临床效应。方法腰椎管狭窄手术的患者45例,随机分为3组,泵内药物：A组,芬太尼1mg＋格拉司琼3mg＋0．9％NaCl共100ml;B组,氟比洛芬酯200mg＋格拉司琼3mg＋0．9％NaCl共100ml;C组,氟比洛芬酯100mg＋芬太尼0．5mg＋格拉司琼3mg＋0．9％NaCl共100ml。参数设定：A组负荷量为泵内药物5ml,B、C组负荷量为氟比洛芬酯50mg（5ml）,持续输注为各组泵内药物2ml／h,PCA2ml,锁定30min.观察24b内的镇痛评分（VAS）,PCA使用次数及不良反应的发生情况。结果术后24h时A,B和C组的VAS,3组间差异无显著性（P〉0．05）。24h内的PCA按压次数C组显著少于A和B组（P〈0．05）。B,C组不良反应的发生率显著低于A组（P〈0．05）：镇痛期间无异常出血等并发症发生。结论氟比洛芬酯复合小剂量芬太尼用于腰椎管狭窄手术后静脉镇痛效果良好,可明显减少芬太尼和氟比洛芬酯的用量及不良反应的发生率。     

Cognitive and EEG recovery following bolus intravenous administration of anesthetic agents

Bolus intravenous (IV) administration of commonly used IV anesthetic agents such as fentanyl and the fentanyl analogues, alfentanil, remifentanil, and sufentanil, etomidate and propofol, produced anesthesia in rats as measured by the loss of righting (LOR) with calculated ED₁₅₀ doses of 0.06, 0.09, 0.037, 0.007, 2.51 and 6.12 mg/kg, respectively. Animals trained in an eight arm radial maze (RAM) were assessed for cognitive recovery, as measured by response efficiency (percentage of correct arm entries within 10 min), immediately, 15 min and 30 min following IV administration of the calculated ED₁₅₀ dose of each of these agents, and the subsequent return of righting (ROR). Animals administered fentanyl or sufentanil were unable to successfully complete the maze throughout the testing periods. Animals receiving remifentanil showed cognitive recovery within the first testing interval (immediately following the return of righting), while animals receiving alfentanil, etomidate or propofol showed recovery at the 15-min testing interval following ROR. In a separate experiment, bolus IV administration of the ED₁₅₀ dose of these agents was evaluated in an acute rat EEG model. Following ROR, return to baseline EEG levels occurred at 0.30, 2.88, 5.06, 16.25, 31.29 and 43.98 min for remifentanil, propofol, alfentanil, etomidate, fentanyl and sufentanil, respectively. These data show that the return to efficient cognitive functioning corresponds to the return to normal baseline EEG waveforms.     

利多卡因用于老年患者术后镇痛的临床观察

目的：观察利多卡因复合芬太尼静脉输注用于老年患者术后镇痛的效果及不良反应。方法：择期老年手术患者40例,ASAⅡ～Ⅲ级。其中男25例,女15例,年龄66～79岁,食道癌和肺切除10例,腹腔镜胆囊切除12例,乳腺癌根治4例,前列腺切除11例,肾切除3例。将40例患者随机分为A、B两组,每组20例。两组患者术后镇痛均使用一次性恒速输注泵（速度4mL/h,容量200mL）。A组镇痛泵的配方为利多卡因50mg/kg＋芬太尼10μg/kg＋昂丹司琼0.2mg/kg＋生理盐水共200mL;B组镇痛泵的配方的为芬太尼20μg/kg＋昂丹司琼0.2mg/kg＋生理盐水共200mL。A、B两组患者分别在手术结束前10min给予利多卡因1mg/kg和芬太尼1μg/kg并随后接镇痛泵。两组患者的麻醉诱导和维持均相同。记录术后2、4、8、12、24h疼痛视觉模拟评分（VAS评分）,镇静评分、不良反应。结果：两组患者镇痛效果均较满意,各时间点VAS评分组间比较无显著差异（P〉0.05）。B组的恶心、呕吐、过度镇静、呼吸抑制和心动过缓等不良反应的发生率明显多于A组（P〈0.05或P〈0.01）。结论：芬太尼复合利多卡因静脉持续输注用于老年患者术后镇痛效果满意,不良反应较少。     

苯磺酸瑞马唑仑联合阿芬太尼用于无痛胃肠镜患者的双盲对照研究

目的:研究分析苯磺酸瑞马唑仑联合阿芬太尼在无痛胃肠镜麻醉中的应用价值。方法:选取在青海省人民医院行无痛胃肠镜的患者200例,按1∶1比例随机分为2组,即注射用苯磺酸瑞马唑仑组(A组)和丙泊酚组(S组)。A组:静脉注射阿芬太尼7μg·kg^-1,随后静脉注射苯磺酸瑞马唑仑7mg待患者意识消失后开始进镜。S组:静脉注射舒芬太尼0.1μg·kg^-1,随后静脉注射丙泊酚1.5mg·kg^-1;待患者意识消失后开始进镜。观察2组有效性指标(起效时间、苏醒时间、离室时间),比较2组术前术中及术后血流动力学指标(如心率、平均动脉压),血氧饱和度,MOAA/S评分等,以及术后不良反应、医患双方满意度。结果:A组苏醒时间及离室时间均短于S组(P均＜0.05),两者起效时间差异无统计学意义(P＞0.05)。A组在给药后1,3,5,10,15,20,25,30min、结束时平均动脉压、心率、血氧饱和度均高于S组(P＜0.05)。在MOAA/S评分方面A组在给药1min时低于S组,而给药30min及检查结束时高于S组(P＜0.05)。A组在术中低氧血症、低血压、呛咳及术后恶心、呕吐、头晕、注射痛发生率与S组比较较低(P均＜0.05)。并且A组操作医生满意度及术后患者满意度均高于S组(P均＜0.05)。结论:苯磺酸瑞马唑仑联合阿芬太尼在无痛胃肠镜应用中具有血流动力学稳定,对呼吸影响小、苏醒快、无注射痛等优点,不良反应发生率与丙泊酚相比明显较低。     

地佐辛与芬太尼术后静脉自控镇痛对老年胃肠道肿瘤患者免疫功能的影响

目的研究地佐辛与芬太尼术后静脉自控镇痛（PCIA）对胃肠道肿瘤患者免疫功能的影响。方法将80例肿瘤手术患者按数字表法分为地佐辛组与芬太尼组,每组各40例患者。芬太尼组采用芬太尼0．8mg＋生理盐水稀释到100ml镇痛方案;地佐辛组采用镇痛泵使用前先静脉注射5mg负荷量的地佐辛,然后采用地佐辛20mg＋生理盐水稀释到100ml的镇痛方案．手术前、手术后24小时、48小时、72小时测定患者外周血T淋巴细胞亚群（CD3^＋、CD4＋,CD4＋／CD8＋）。结果两组患者的一般资料无统计学差异．两组术后24小时CD3^＋、CD4＋,CD4＋／CD8^＋均较手术前降低,差异有显著性（P〈0．05）,两组术后24小时CD3＋、CD4^＋相比地佐辛组更高,差异有显著性（P〈0．05）,48小时后两组均升高,而芬太尼组仍低于手术前水平,地佐辛组则恢复接近正常水平,两组相比地佐辛组高于芬太尼组,差异有显著性（P〈0．05）,72小时后两组均恢复至术前水平。结论地佐辛术后静脉自控镇痛对患者免疫功能抑制较轻,术后患者免疫功能恢复较快,对机体的免疫功能有较好的保护作用,值得老年胃肠道肿瘤患者临床广泛推广应用。     

Comparative analgesic efficacy and tolerability of ketorolac tromethamine and glafenine in patients with post-operative pain

Summary

In a randomized, single-dose, double-blind, parallel comparative trial of analgesic efficacy, 96 adult patients received either 10?mg ketorolac tromethamine or 400?mg glafenine orally the morning after surgery if they requested pain relief medication. Each patient provided a baseline pain assessment and then received the assigned medication. Patients assessed pain intensity and pain relief and reported any adverse events in interviews held 30 minutes after drug administration and then hourly for 6 hours. The demographic characteristics, baseline pain intensity, and surgical categories of the 47 patients who received ketorolac tromethamine and the 49 who received glafenine were similar. Both drugs provided prompt, sustained pain relief throughout the 6-hour observation period, and there were no statistically significant differences between the two groups in any of the efficacy measures analyzed. The global assessment recorded by patients suggested a slight clinical advantage for ketorolac tromethamine (32.6% of ‘excellent’ responses) as compared to glafenine (12.5% ‘excellent’). The differences in overall response were statistically significant (p = 0.017). Fourteen (30%) patients who received ketorolac tromethamine and 17 (35%) who received glafenine reported adverse experiences that began or seemed to worsen after administration of the study drugs. The most prominent were drowsiness and sleeping, both of which are common in post-surgical patients.     

等效剂量阿芬太尼与芬太尼在全麻诱导时诱发咳嗽的对比研究

目的：比较等效剂量阿芬太尼与芬太尼对患者咳嗽的影响。方法：50例全麻手术患者,随机分为阿芬太尼组、芬太尼组,每组25例,两组患者分别在5S内静脉注射阿芬太尼8gg／kg、芬太尼2μg／kg,观察给药后2min内两组患者的咳嗽起始时间、咳嗽发生率以及严重程度,并记录给药前（T1）和给药后2rain（T2）两个时点的心率（HR）、平均动脉压（MAP）变化。结果：阿芬太尼组患者咳嗽的起始时间明显早于芬太尼组,阿芬太尼组咳嗽的发生率显著低于芬太尼组（P〈0．05）。与T1时相比,T2时芬太尼组和阿芬太尼组的HR和MAP均显著下降（P〈0．05）,且阿芬太尼组HR和MAP下降程度显著低于芬太尼组（P〈0．05）。结论：与等效剂量芬太尼相比,阿芬太尼诱发咳嗽的发生率较低,循环更为平稳。     

高乌甲素治疗56例胆道术后病人疼痛的临床疗效分析

目的：观察高乌甲素在胆道手术后的镇痛效果。方法：选择本院2007年1月至2008年1月择期行胆道手术患者56例,随机分为高乌甲素组和芬太尼组,分别在手术后给予高乌甲素和芬太尼进行术后镇痛。结果：胆道手术术后48h内高乌甲素组和芬太尼组的临床治疗效果没有显著的统计学差异（P〉0.05）,且高乌甲素组比芬太尼组在恶心、呕吐、嗜睡、皮肤瘙痒等副反应上要小得多（P〈0.01）。结论：应用高乌甲素对胆道手术术后镇痛有良好效果,与芬太尼的镇痛效果相当,但高乌甲素副作用要小得多,术后患者的接受度更佳,适宜临床推广使用。     

氯诺昔康复合芬太尼用于心血管手术后患者自控静脉镇痛的临床研究

目的探讨氯诺昔康复合芬太尼用于心血管手术后患者自控静脉镇痛的有效性、可行性和安全性.方法选择18～66岁,体重46～67kg,ASAⅡ～Ⅲ,择期行心脏手术患者120例,其中男63例,女57例。随机分为芬太尼(F)组40例,氯诺昔康(L)组40例,氯诺昔康复合芬太尼(LF)组40例。在麻醉清醒,拔出气管导管后合作,安静时感疼痛,视觉模拟评分(VAS)≥3分,开始实施患者静脉自控镇痛.F组:芬太尼1.0mg以生理盐水稀释成100mL,负荷剂量芬太尼50μg,L组:氯诺昔康40mg以生理盐水稀释成100mL,负荷剂量氯诺昔康8mg;LF组:氯诺昔康40mg复合芬太尼0.5mg以生理盐水稀释成100mL,负荷剂量氯诺昔康8mg,然后三组均以2mL/h的镇痛液维持镇痛.观察镇痛起效时间,记录镇痛前、镇痛10min、12、24、48h、撤泵时的有效按压和实际按压次数之比,药物消耗量,安静和咳嗽时VAS、镇静评分、血流动力学参数、镇痛期不良反应(恶心、呕吐、头晕、瘙痒等)。结果镇痛期,组间同时点的有效按压/实际按压值比较,L组比LF组、F组、低(P<0.05).组间同时点药物消耗量比较,L组比LF组、F组高(P<0.05).血流动力学参数比较,三组间差异无显著意义.镇痛期,安静时痛组间VAS比较,10min时L组高于LF组、F组(P<0.05).咳嗽时VAS在10min、12、24h时L组均高于LF组、F组(P<0.05).镇静评分比较。10min时L组小于LF组、F组(P<0.05),其他时间点组间比较,F组均大于LF组、L组(P<0.05).常见不良反应中,恶心率比较,组间差异无显著意叉,但恶心程度比较,F组评分明显高于LF组,L组(P<0.05),LF组和L组之间比较,无显著性差异.呕吐率、头晕发生率及其他不良反应三组间差异无显著意义.结论氯诺昔康复合芬太尼静脉镇痛效果满意、不良反应少,安全可靠,适合心血管手术后静脉镇痛。     

地佐辛和氟比洛芬酯联合术后自控静脉镇痛研究

目的 比较地佐辛、芬太尼、氟比洛芬酯联合地佐辛应用于术后患者静脉自控镇痛(PCIA)的有效性和安全性.方法 选择240例行择期手术,ASA分级Ⅰ～Ⅲ级,年龄18～65岁的患者.随机分为3组:地佐辛组(D组)、氟比洛芬酯+地佐辛组(FD组)、芬太尼组(F组)、每组各80例.术后行PCIA,地佐辛组(D组):负荷量地佐辛5 mg,镇痛泵为地佐辛1.0 mg/kg+昂丹司琼8 mg+0.9%氯化钠注射液;氟比洛芬酯+地佐辛组(FD组):负荷量氟比洛芬酯25 mg+地佐辛2.5 mg,镇痛泵为氟比洛芬酯1 mg/kg+地佐辛0.8 mg/kg+昂丹司琼8 mg+0.9%氯化钠注射液;芬太尼组(F组):负荷量芬太尼1 μg /kg,镇痛泵为芬太尼15 μg /kg+昂丹司琼8 mg+0.9%氯化钠注射液;容量均为100 ml.镇痛泵参数设定均为持续输注量2 ml/h,PCA量0.5 ml,锁定时间15 min.采用疼痛视觉模拟评分(VAS评分)和Ramsy镇静评级评估患者48 h内的疼痛程度和镇静情况,同时记录不良反应发生情况,并于术后4、12、24、48 h时采集外周静脉血测定血浆皮质醇浓度.结果 3组患者均获得良好的镇痛效果,各组在同时点的疼痛视觉模拟评分(VAS)无显著差异(P>0.05),各组在同时点的Ramsy镇静评级无显著差异(P>0.05),各组在同时点的血浆皮质醇无显著差异(P>0.05).各组均存在不良反应,但芬太尼组不良反应发生率显著高于其他两组(P<0.05);氟比洛芬酯-地佐辛组的不良反应发生率显著低于其他两组(P<0.05).结论 地佐辛与氟比洛芬酯联合用于术后PCIA能达到满意的镇痛效果,同时可减少不良反应,是一种可行、安全、有效的镇痛方法.     

肛门手术后硬膜外自控镇痛的药物选择

目的比较不同浓度舒芬太尼及芬太尼复合低浓度布比卡因用于肛门手术术后自控镇痛的效果及不良反应。方法选择择期肛门手术病例80例分为A、B、C、D4组,每组病例20例,其中A组PCEA配方为芬太尼0．5mg（5mg/L）、布比卡因75mg（0．75g／L）及格拉斯琼3mg,B组为芬太尼1mg（10mg／L）、布比卡因75mg（0．75g／L）及格拉斯琼3mg,C组为舒芬太尼50μg（0．5mg／L）、布比卡因75mg（0．75g/L）及格拉斯琼3mg,D组为芬太尼100μg（1mg/L）、布比卡因75mg（0．75g／L）及格拉斯琼3mg,均配成100ml。观察各组患者术后不同时段VAS评分、镇痛药用量、PCA按压次数、恶心、皮肤瘙痒、呼吸抑制发生率。结果VAS评分：B、D组静息状态下术后4、16h均低于A、C组,术后24hA组明显高于其他三组;镇痛药用量：B、D组静息状态下术后4、16、24h镇痛药用量均高于A、C组;实际PCA按压次数：B、D组静息状态下术后4、16、24、48h均高于A、C组;B组患者镇痛期间不良反应如恶心、皮肤瘙痒、呼吸抑制发生率明显高于其他组。术后镇痛满意度：D组明显高于其他三组。结论1mg／L舒芬太尼复合布比卡因应用于肛门手术PCEA镇痛效果较好,不良反应发生率低。     

瑞芬太尼静脉自控镇痛与罗哌卡因复合芬太尼硬膜外自控镇痛在分娩镇痛中的比较

目的：比较瑞芬太尼静脉与罗哌卡因复合芬太尼硬膜外自控分娩镇痛的有效性和安全性。方法选择产前检查适于阴道分娩、接受分娩镇痛初产妇60例,ASA玉～Ⅱ级,单胎足月妊娠,随机分为两组（n=30）：静脉瑞芬太尼自控组（A组）,硬膜外罗哌卡因复合芬太尼自控组（B组）。 A组瑞芬太尼以生理盐水稀释到50μg/ml,开始时以0.15μg/kg剂量给予,逐步以0.15μg/kg的剂量增加,每15min调整输注速度,锁定时间为2min,瑞芬太尼以2ml/min的速度通过PCA泵维持。B组以0.2％罗哌卡因复合芬太尼2μg/ml负荷量10ml,当VAS≥20mm时,自控给药4ml/次,锁定时间为15min。连续监测呼吸循环状况,记录产妇的生命体征、胎心率（FHR）、产程时间、分娩方式、催产素用量、新生儿Apgar评分、脐静脉血气分析及母体和新生儿副作用。结果产妇在30~240min分娩期间,VAS评分为无明显差异;分娩方式和催产素使用情况、产妇分娩期恶心呕吐等副作用及胎儿娩出后1min、5min、10min Apgar评分无明显差异（P＆gt;0.05）。镇痛后1h和第二产程结束时A组产妇血氧饱和度较B组降低（P＆lt;0.05）,产妇镇静评定A组较B组安静率更高,而B组产妇头晕率更高（P＆lt;0.05）。结论瑞芬太尼静脉和罗哌卡因复合芬太尼硬膜外自控给药都能安全有效地应用于分娩镇痛,但静脉给予瑞芬太尼产妇镇静深度更高,血氧下降较硬膜外镇痛发生率高。     

Negative inotropic effects of tumour necrosis factor-alpha and interleukin-1beta are ameliorated by alfentanil in rat ventricular myocytes

BACKGROUND AND PURPOSE: Serum levels of tumour necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta) increase during an inflammatory response and have been reported to induce a negative inotropic effect on the myocardium. Alfentanil, an opioid analgesic often used in the critical care of patients with sepsis, has been shown to enhance ventricular contractility. This study characterised the effects of TNF-alpha and IL-1beta on contraction and the Ca(2+) transient and investigated whether depressed ventricular function was ameliorated by alfentanil. EXPERIMENTAL APPROACH: Isolated rat ventricular myocytes were loaded with fura-2 and electrically stimulated at 1 Hz. Contraction and Ca(2+) transients were measured after 60, 120 and 180 min incubations in TNF-alpha (0.05 ng ml(-1)) and IL-1beta (2 ng ml(-1)). The effects of 10 microM alfentanil on contractility and Ca(2+) transients of TNF-alpha and IL-1beta treated cells were determined.Key results:After 180 min of TNF-alpha and IL-1beta treatment, the amplitude of contraction, the Ca(2+) transient and sarcoplasmic reticulum (SR) Ca(2+) content were significantly reduced. Alfentanil significantly increased contraction of TNF-alpha and IL-1beta treated cells via a small increase in the Ca(2+) transient and a larger increase in myofilament Ca(2+) sensitivity, effects that were not blocked by 10 microM naloxone, a broad spectrum opioid receptor antagonist. CONCLUSIONS AND IMPLICATIONS:TNF-alpha and IL-1beta induce a significant negative inotropic effect on ventricular myocytes in a time dependent manner through disruption of SR Ca(2+) handling and the Ca(2+) transient. This negative inotropic effect was ameliorated by alfentanil, but this response may not be mediated via opioid receptors.     

氟比洛芬复合芬太尼用于术后镇痛的疗效及安全性的研究

目的评价与芬太尼合用进行中等手术病人围术期镇痛的效果及安全性。方法192例病人随机分为4组，常规采用静吸复合麻醉，根据手术时间对术中芬太尼总量进行控制，术后采用静脉镇痛。氟比洛芬按照以下方案给予，除A组外，其余3组均于手术结束前给予氟比洛芬50mg。A组：术后芬太尼1mg＋生理盐水100ml；B组：术后芬太尼1mg＋生理盐水100ml；C组：术后100mg氟比洛芬＋芬太尼0．5mg＋生理盐水至100ml；D组；术后150mg氟比洛芬＋芬太尼0．5mg＋生理盐水至100ml。术后随访24h，记录生命体征、镇痛情况及其不良反应。结果整个研究共完成病例191例，4组手术病人一般情况无显著差别，术后24h内生命体征基本平稳。结果术后0h，VAS（视觉模拟疼痛评分）B、C、C〈VASA，术后4，8h，VASCD〈VASA，术后24h，VASC〈VAS10。D组病人呕吐的发生率显著高于其它3组。结论氟比洛芬复合芬太尼用于中等手术病人围术期镇痛具有确切的疗效，不良反应发生率较低，可以安全用于临床。     

家庭病房晚期癌患者皮下与硬膜外自控镇痛的效果比较

目的比较患者皮下自控镇痛(PCSA)与硬膜外自控镇痛(PCEA)在家庭病房晚期癌痛治疗中的疗效及安全性。方法32例患者随机分为二组,每组各16例。PCSA组:为100ml液体中含芬太尼30μg、氟哌啶5mg、玻璃酸酶500U,PCSA泵注前先经肌肉注射芬太尼1μg/kg、氟哌利多0.05mg/kg、PCA每次0.5ml,背景输注量2ml/h,锁定时间15min。PCEA组:为100ml液体中含0.75%布比卡因25ml、芬太尼500μg、氟哌利多5mg,置管后注入负荷剂量5ml,PCA每次0.5ml,PCEA2ml/h,锁定时间15min。观察患者第1、3、7天的心率、血压、呼吸频率、VAS、镇静评分及镇痛期间的其它不良反应。结果首日PCEA镇痛效果优于PCSA,其它时间段两种镇痛方法的总体满意度无明显差异。腹胀、尿潴留及穿刺部位炎症不良反应发生率PCEA组明显高于PCSA组(P<0.05),头晕、嗜睡则以PCSA为著。结论PCEA组患者镇痛效果确切,PCSA不良反应少,安全、经济、管理方便。     

布托啡诺复合芬太尼在口腔颌面部手术术后镇痛中的应用

目的观察静脉酒石酸布托啡诺复合芬太尼在口腔颌面部手术术后镇痛的临床效果及不良反应。方法ASAⅠ～Ⅱ级75例择期行口腔颌面部手术病人,随机分成三组,每组25例。A组：单独的酒石酸布托啡诺8mg加生理盐水共120ml;B组：单独的枸橼芬太尼0．8mg加生理盐水共120ml;C组：枸橼酸芬太尼0．4mg与酒石酸布托啡诺4mg加生理盐水共120ml;术毕给予负荷剂量4ml后连接镇痛泵进行自控镇痛（PCIA）,术后分别记录6h、24h、48h三个时段的视觉模拟评分（VAS）并观察各种不良反应的发生情况。结果B组与C组VAS评分显著低于A组（P〈0．05）,A组与C组不良反应发生率明显少于B组（P〈0．05）。结论枸橼酸芬太尼0．4mg与酒石酸布托啡诺4mg加生理盐水共120ml（C组）镇痛效果确切,不良反应较少,是口腔颌面部手术术后静脉镇痛治疗的良好选择之一。