静脉注射三磷酸腺苷治疗阵发性室上性心动速的临床观察及护理

目的观察三磷酸腺苷（ATP）治疗阵发性室上性心动过速（PSVT）的疗效及护理要点。方法进行心电监护,结合心理护理,给予ATP0.25mg/kg直接弹丸式静脉注射,注射同时观察心率、血压变化及患者的不良反应。结果转复率91.4%。出现的不良反应停注后自行消失。结论严格规范应用ATP治疗PSVT,疗效显著,为复率首选。     

不同剂量三磷酸腺苷治疗阵发性室上性心动过速的疗效观察

阵发性室上性心动过速(PSVT)为临床上常见的快速性心率失常,起病突然,持续时间长,发作时相当顽固,难以控制,严重时可危及生命,需紧急处理[1].静脉注射三磷酸腺苷(ATP)是终止PSVT的有效药物,但其不良反应随剂量增大而增加,最佳有效剂量和安全性仍存在争议,使其应用受到限制.本研究探讨静脉注射ATP终止PSVT的最佳有效剂量及安全性,为临床合理使用ATP提供依据.     

三磷酸腺苷治疗阵发性室上性心动过速的疗效观察

目的 观察三磷酸腺苷(ATP)治疗阵发性室上性心动过速(PSVT)疗效及安全性.方法 选择我院2010年1月-2012年12月收治的PSVT患者78例,给予ATP静脉注射,记录ATP的剂量及起效时间、转复率及不良反应.结果 10mg时转复率为80.7%(63/78),当ATP剂量增加为15mg时,又有7例转复成功,当剂量增加为最大量20mg时,共有75例(96.1%)转复成功.45例(57.7%)患者注射ATP原液后出现胸闷,38例(48.7%)患者出现头晕症状,8例(10.2%)患者出现呼吸困难,5例(6.4%)患者出现室性逸博.结论 ATP治疗PSVT具有起效快,操作简单,转复率高,不良反应持续时间短,安全性高.     

三磷酸腺苷不同注射方式终止阵发性室上性心动过速比较研究

目的通过观察静脉注射三磷酸腺苷（ATP）40 mg与弹丸注射ATP 20 mg比较,明确静脉注射大剂量ATP在终止PSVT中的安全性和有效性。方法 PSVT患者46例,随机分为弹丸注射组与静脉注射组,每组23例,分别给予弹丸注射ATP 20 mg与静脉注射40 mg。结果 2组转复成功率分别为87.0%和95.7%,静脉注射组高于弹丸注射组,但差异无统计学意义（P〉0.05）;弹丸注射组不良反应发生率明显多于静脉注射组（P〈0.01）,分别为60.9%和8.7%。结论静脉注射ATP 40 mg与弹丸注射ATP20 mg有效性相当,安全性明显高于弹丸注射。     

不同剂量的三磷酸腺苷对转复阵发性室上性心动过速的疗效观察

目的:探讨不同剂量的三磷酸腺苷(ATP)对转复阵发性室上性心动过速(PSVT)的疗效。方法:将120例PVST患者随机分为4组,分别以不同剂量的ATP(第一组:0.1mg/kg,第二组:0.2mg/kg,第三组:0.3mg/kg,第四组:0.4mg/kg),快速静脉推注,未转复者,3分钟后重复同样剂量再给药1次,观察每组患者的转复时间、有效率、不良反应及转复时伴发的心律失常。结果:0.1mg/kg组的转复时间、有效率与其他3组比较有统计学差异(P<0.05)。0.4mg/kg组伴发严重缓慢心律失常较高。结论:以剂量为0.2～0.3mg/kg的ATP治疗PSVT是安全有效的,且严重心律失常发生率较低。     

盐酸关附甲素用于终止阵发性室上性心动过速52例

目的观察盐酸关附甲素用于终止阵发性室上性心动过速（PSVT）的疗效及安全性。方法采用随机开放对照多中心试验,选取自发或经食管起搏心房诱发的PSVT患者50例,均持续15rain以上,采用盐酸关附甲素按4mg／kg的剂量于5min内静脉注射完毕,转复为窦性心律则终止注射,若第1剂治疗无效则补充注射第2剂,观察临床疗效。结果转复率为76．92％,无严重不良事件发生。结论该研究所采用的盐酸关附甲素的剂量可有效转复PSVT,且在所使用的剂量下无严重不良反应发生。     

小剂量三磷酸腺苷静脉注射终止阵发性室上性心动过速的临床观察

目的观察静脉注射小剂量三磷酸腺苷（ATP）对阵发性室上性心动过速（PSVT）的终止作用。方法对12例PSVT患者肘静脉快速弹丸式注射ATP5～10mg,给药前1—7min持续进行心电监护,观察起效时间、心率、心律、血压和不良反应。结果静脉快速注射小剂量ATP后,12例患者中10次PSVT得到终止,仅3例次患者发现轻微的不良反应,但均在2min内消失。结论静脉快速注射小剂量ATP能安全有效地终止PSVT。     

两种药物治疗小儿阵发性室上性心动过速比较

目的比较三磷腺苷（ATP）与盐酸普罗帕酮治疗儿童阵发性室上性心动过速（ PSVT）的疗效与安全性。方法回顾性分析1992年1月～2009 年 6 月使用ATP与盐酸普罗帕酮复律PSVT患儿85例的临床资料。所有患儿均给予吸氧等一般治疗,在心电监护下使用抗心律失常药物。使用ATP者,每次0.1～0.2 mg&#8226;kg 1,于3 s内快速静脉注射,无效者重复给药1次,注药5 s内复律为有效,第一次用药后5 min无效加至0.2～0.3 mg&#8226;kg 1,重复1次,2次使用均无效停用;使用盐酸普罗帕酮者每次1～2 mg&#8226;kg 1,稀释后缓慢静脉注射,转为窦性心律后停止,若首次静脉注射未转复,每隔15 min重复1或2次,3次未复律者视为无效。患者治疗前后均行血压及心电监测。结果应用ATP治疗45例,有效38例,有效率84.4%;应用盐酸普罗帕酮治疗40例,有效33例,有效率82.5%。结论ATP与盐酸普罗帕酮终止小儿PSVT疗效差异无显著性,但ATP复律时间短,不良反应较少。     

不同方式的三磷酸腺苷注射对终止阵发性室上性心动过速的临床研究

目的观察不同的三磷酸腺苷注射方式对阵发性室上性心动过速的终止作用。方法将26例阵发性室上性心动过速（PSVT）患者随机分为两组,即静脉注射组和弹丸注射组,每组13人;分别给予静脉注射ATP40mg与弹丸注射ATP20mg。结果两组转复成功率分别为92．31％（12／13）和84。62％（11／13）,但差异无显著性（P〉0．05）;静脉注射组的不良反应发生率明显少于弹丸注射组,分别为7．69％（1／13）和53．85％（7／13）,差异具有极显著性（P〈0．01）。结论静脉注射ATP40mg与弹丸注射ATP20mg对于PSVT治疗成功率无明显差异,但静脉注射ATP40mg的安全性优于弹丸注射ATP20mg。     

三磷酸苷和异搏定静注治疗阵发性室上速比较

目的:比较三磷酸腺苷(ATP)和异搏定静脉注射治疗阵发性室上性心动过速(PSVT)的异同。方法:给34例PSVT患者静脉注射ATP104次,给30例此类患者静注异搏定98次。分别观察两者终止急性发作的有效率,终止发作时间及对血流动力学的影响。结果:ATP与异搏定相比,终止急性发作有效率分别为98%与82.5%。终止发作时间相应为36.8±12.3秒与5.4±1.8分。对血流动力学影响都表现为血压降低。结论:两者静注治疗PSVT,ATP有效率高(P＜0.05),终止发作时间短(P＜0.01),对血流动力学影响都表现为血压降低。     

普罗帕酮和胺碘酮治疗阵发性室上性心动过速疗效与安全性比较

目的 比较普罗帕酮和胺碘酮静脉用于急诊转复阵发性室上性心动过速的疗效及不良反应.方法 将急诊阵发性室上性心动过速患者86例完全随机分成普罗帕酮组(44例)和胺碘酮组(42例),普罗帕酮组给予普罗帕酮70 mg静脉注射(5 min注完),若无效,20min后重复1次;胺碘酮组给予胺碘酮5～7 mg/kg加入100 ml 5%葡萄糖或0.9%氯化钠注射液中静脉滴注,30 min滴完,继之以1 mg/min的速度持续静脉滴注.观察2组的治疗效果和不良反应发生情况.结果 普罗帕酮组和胺碘酮组转复有效率分别为93.2%(41/44)和88.1%(37/42)(P＞0.05);平均转复时间普罗帕酮组[(12.4±7.8)min]明显短于胺碘酮组[(30.7±10.3)min](P＜0.01);不良反应发生率普罗帕酮组为[29.5%(13/44)]明显高于胺碘酮组[11.9%(5/42)](P＜0.05).结论 普罗帕酮和胺碘酮用于急诊转复阵发性室上性心动过速,疗效基本相同,但普罗帕酮起效快,更适用于无器质性心脏疾患者,胺碘酮用于有器质性心脏疾患者较普罗帕酮相对安全.     

三磷酸腺苷与阿托品合用治疗室上性心动过速的疗效

目的：探讨三磷酸腺苷与阿托品合用在治疗室上性心动过速（PSVT）中的疗效。方法：将三磷酸腺苷（ATP）20mg加阿托品1mg快速静注,并与单用ATP20mg快速静注作为对照,无效可重给药。结果：有效率ATP与阿托品合用组为85％,单用ATP组为73％,而缓慢性心律失常的发生率前者较后者低。结论：ATP与阿托品合用治疗PSVT,方法简单、快速有效。     

Adenosine. An evaluation of its use in cardiac diagnostic procedures, and in the treatment of paroxysmal supraventricular tachycardia.

Adenosine (adenine riboside), administered either as the free base or as the 5'-triphosphate (ATP) by rapid intravenous bolus, depresses atrioventricular (AV) nodal conduction, resulting in transient AV block. Adenosine is the active agent and ATP is rapidly converted to adenosine after exogenous administration. By blocking the anterograde AV nodal limb of a re-entrant circuit, adenosine 6 to 12 mg (or ATP 10 to 20 mg) converts almost all episodes of paroxysmal supraventricular tachycardia (PSVT) involving the AV node within 30 seconds of administration. This is at least equivalent in efficacy to verapamil in adults, and superior to lanatoside C in children, with a considerably more rapid onset of action. Furthermore, if a dose of adenosine is ineffective, the exceptionally short plasma half-life of the adenyl nucleosides (less than 10 sec) allows rapid upward dosage titration until PSVT is terminated. Because the induced conduction block primarily affects the AV node, adenosine is a useful diagnostic tool in patients with broad or narrow QRS complex tachycardia; it terminates arrhythmias dependent on the AV node, unmasks other supraventricular mechanisms during transient AV block, but almost always has no effect on ventricular tachycardia. Noncardiac adverse effects, i.e. flushing, dyspnoea and chest pain, may occur during acute arrhythmia termination or diagnosis with adenosine, and arrhythmias may develop; however, these effects are usually transient (lasting less than 1 minute). Adenosine has also been used to induce coronary vasodilation in patients undergoing thallium-201 single photon emission computed tomography (201Tl SPECT), 2-dimensional echocardiography or positron emission tomography to evaluate suspected coronary artery disease. Intravenous infusion of adenosine 140 micrograms/kg/min for 6 minutes was generally associated with only mild adverse effects. These usually resolved within 1 to 2 minutes of discontinuing adenosine, although occasionally patients required aminophylline and/or nitroglycerin (glyceryl trinitrate). Diagnoses based on the results of scintigraphy were of a sensitivity, specificity and predictive accuracy comparable to those achieved with exercise- or dipyridamole-201Tl SPECT. Adenosine is therefore particularly suitable for the diagnosis of tachycardias and the acute management of PSVT involving the AV node in all age groups, without the risks of cardiac arrest and hypotension associated with verapamil. Furthermore, intravenous adenosine infusion may be used to induce coronary vasodilation in patients unable to perform exercise stress tests for 201Tl scintigraphy, and is well tolerated.     

Safety evaluation of micronomicin. I. Subacute and chronic toxicity in dogs

Micronomicin (MCR) is a new aminoglycoside antibiotic produced by Micromonospora sagamiensis var. nonreducans which was isolated from soil collected at Sagamihara by Nara et al. The purified antibiotic showed a close similarity to gentamicin C complex in physical and chemical properties. The antibacterial activity of MCR is broad-spectrum and almost equal to that of gentamicin C complex. MCR exhibits particularly high activity against Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia, etc. and high activity against some Pseudomonas aeruginosa strains resistant to gentamicin C1a. Toxicological studies of MCR in dogs were carried out by intravenous injection for safety evaluation. 1. Study on subacute toxicity: Beagle dogs were injected intravenously with MCR at the dose levels of 4, 10, 25, 63 mg/kg and 100 mg/kg for 30 days. 2. Study on chronic toxicity: Beagle dogs were injected intravenously with MCR at the dose levels of 1.6, 4 mg/kg and 10 mg/kg for 180 days. The results of the studies are as follows: 1. In the subacute toxicity study, animals died at the dose level of 100g/kg (3 out of 6 animals). Main changes observed were renal disorders and ataxia which showed a close similarity to those seen during intramuscular toxicity studies in dogs. The renal histological disorders occurred at the dose levels of 10 mg/kg and over, but they were slight at the dose levels of 10 mg/kg and 25 mg/kg. Ataxia was observed at the dose levels of 63 mg/kg and over, but its grade was slight at the dose level of 63 mg/kg. 2. In the chronic toxicity study, animals did not die at any dose. Renal disorders occurred; they were almost similar to those observed in the subacute toxicity study and were slight at the dose level of 10 mg/kg. Ataxia was not observed at any dose. 3. The maximum safety dose was equal to in the subacute toxicity and chronic toxicity study (4 mg/kg). Therefore, cumulative toxicity by intravenous injection seemed very slight.     

Biological evaluation of N-octyl-O-sulfate chitosan as a new nano-carrier of intravenous drugs

An amphiphilic chitosan derivate, N-octyl-O-sulfate chitosan (NOSC) was prepared by octylation of amino group at C-2 position and sulfonylation at C-6 position. Micelle formed by NOSC has great capability in solubilization of water-insoluble drug paclitaxel. Enormous attention was attracted by the potential application of NOSC as a new drug delivery system. Tritium labeled NOSC (³H NOSC) was injected by tail vein at dose of 13.44 mg/kg in mice; kidney retained the maximum amount of NOSC all the time even after 24 h following the injection. Pharmacokinetic parameters (the area under the plasma concentration–time curve, maximum plasma concentration, apparent plasma half-life of distribution phase and elimination phase, mean residence time, apparent volume of distribution, total body clearance) were obtained by fluorometric method in rats. The results showed a linear pharmacokinetics proceeding of FITC-NOSC in vivo. 75.4 ± 11.6% ³H NOSC of dose was excreted in urine over a 7-day period, urinary excretion was the predominant way of excretion of NOSC compared with bilary or fecal pathway. A series of safety studies consisted of acute toxicity study, intravenous stimulation study, injection anaphylaxis study, hemolysis study and cell viability assay were performed to warrant the biocompatibility of the NOSC as intravenous materials. The LD₅₀ value of NOSC administrated by i.v. and i.p. were calculated as 102.59 and 130.53 mg/kg, respectively. No intravenous stimulation, injection anaphylaxis, hemolysis and cytotoxicity were observed in the safety studies. The tissue distribution, pharmacokinetics, excretion and safety study were persuasive for the potential application of NOSC as a new drug carrier.     

Protective effects of a PAF receptor antagonist and a neutrophil elastase inhibitor on multiple organ failure induced by cerulein plus lipopolysaccharide in rats

The inhibitory effects of YM264, a selective platelet activating factor (PAF) receptor antagonist, and 2-(3-methylsulfonylamino-2-oxo-6-phenyl-1,2-dihydro-1-pyridyl)-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide (compound 1), a neutrophil elastase inhibitor, on mortality, and pancreatic, hepatic, renal and pulmonary dysfunction were evaluated in a rat model of multiple organ failure (MOF) accompanying acute pancreatitis. MOF was produced by intraperitoneal injection of lipopolysaccharide (LPS, 30 mg/kg) in rats with cerulein-induced pancreatitis. LPS dose-dependently increased the mortality in rats with or without pancreatitis. The threshold dose which produced death in rats without pancreatitis was 30 mg/kg. This same dose evoked death in more than 40% of rats with pancreatitis. Time-course changes in serum enzyme and organ myeloperoxidase (MPO) levels were first examined in rats with induced MOF, and the results were compared with those in rats treated with only LPS or cerulein. Pancreatic weight, and serum amylase and lipase levels significantly increased in rats with cerulein-induced pancreatitis despite the presence or absence of LPS, but recovery of these pancreatic dysfunctions was slower in the group given LPS. However, serum GOT, GPT, BUN and creatinine levels were significantly elevated only in MOF rats. In the MOF rats, the MPO level in the lung was significantly elevated and arterial oxygen pressure was decreased, indicating that infiltration of neutrophils into the lung might be involved in pulmonary dysfunction. However, the MPO levels in the pancreas and kidney in the MOF rats were not remarkably different from those in normal rats. The inhibitory effects of YM264 and compound 1 on mortality and organ dysfunction were examined in this MOF model. The 24-h survival rate for rats prophylactically and therapeutically treated with an intravenous infusion of YM264 at 0.1 mg/kg h was significantly higher than that of controls. The 24-h survival rate for rats treated prophylactically by intravenous infusion of 2 mg/kg h of compound 1 was significantly higher than that of control, whereas a beneficial dose of compound 1 was 5 mg/kg h in therapeutically treated rats. Prophylactic treatment with YM264 (0.1 mg/kg h) and compound 1 (2 mg/kg h) ameliorated organ dysfunction in rats with MOF. In conclusion, pancreatic, hepatic, renal and pulmonary dysfunctions are observed in this rat MOF model. The PAF receptor antagonist and neutrophil elastase inhibitor reduce the mortality rate in rats with MOF due to their inhibitory effects on organ dysfunction, indicating that PAF and neutrophil elastase may play important roles in the development of MOF. These results in the present model are largely consistent with those in patients with MOF, indicating that this model is suited for MOF in humans and may be used as a model to test new therapeutic approaches. Received: 22 December 1997 / Accepted: 6 April 1998     

曲马朵对大鼠吗啡辨别行为的影响(英文)

AIM: To study the potential of the psychological dependence of tramadol. METHODS: Rats were trained to discriminate 4.0 mg/kg morphine, and to discriminate 0.5 mg/kg methamphetamine (MA) from saline under a fixed-ratio (FR10) schedule of reinforcement. After they acquired the discrimination, different doses of tramadol were used to substitute for training dose of morphine and MA. Naltrexone was injected concomitantly with tramadol. RESULTS: Tramadol fully substituted morphine at a dose of 32 mg/kg or higher. The ED50 value of the discriminative effects of tramadol was 20.94 mg/kg, higher than that of morphine (2.04 mg/kg, P < 0.01). MA failed to generalize to tramadol at the doses tested. Naltrexone antagonized the discriminative response of tramadol. CONCLUSION: Tramadol can substitute for morphine in morphine discriminative rats. The discriminative stimulus effects of tramadol are mediated by a mu opioid mechanism.     

Comparison of the effects of methamphetamine, bupropion, and methylphenidate on the self-administration of methamphetamine by rhesus monkeys

The effectiveness of methadone as a treatment for opioid abuse and nicotine preparations as treatments for tobacco smoking has led to an interest in developing a similar strategy for treating psychostimulant abuse. The current study investigated the effects of three such potential therapies on intravenous methamphetamine self-administration (1 - 30 μg/kg/injection) in rhesus monkeys. When given as a presession intramuscular injection, a high dose of methamphetamine (1.0 mg/kg) decreased intravenous methamphetamine self-administration but did not affect responding for a food reinforcer during the same sessions. However, the dose of intramuscular methamphetamine required to reduce intravenous methamphetamine self-administration exceeded the cumulative amount taken during a typical self-administration session, and pretreatment with a low dose of methamphetamine (0.3 mg/kg) actually increased self-administration in some monkeys at the lower self-administration dose. Like pretreatment with methamphetamine, pretreatment with bupropion (3.2 mg/kg) decreased methamphetamine self-administration but did not affect responding for food. Pretreatment with methylphenidate (0.56 mg/kg) did not significantly alter methamphetamine self-administration. These results suggest that some agonist-like agents can decrease methamphetamine self-administration. Although the most robust effects occurred with a high dose of methamphetamine, safety and abuse liability considerations suggest that bupropion should also be considered for further evaluation as a methamphetamine addiction treatment.     

Pharmacokinetics, pharmacodynamics, tolerability and safety of single doses of bivalirudin in healthy chinese subjects

The objectives of the present study were to assess pharmacokinetics, pharmacodynamics, tolerability and safety of intravenous administration of bivalirudin, a direct thrombin inhibitor, in healthy Chinese subjects. 48 subjects were equally divided into 4 groups (0.5 mg/kg, 0.75 mg/kg, 1.05 mg/kg intravenous bolus, and 0.75 mg/kg intravenous bolus followed by an infusion of 1.75 mg/kg per hour for 4 h) by a randomized, single-blind and placebo-controlled (bivalirudin groups: n=9/group; placebo groups: n=3/group) design. The safety observations showed that bivalirudin was well tolerated in the studied dose range, all adverse events were mild in severity. The half-life of bivalirudin was approximately 0.57 h (34 min), exposure increased in a dose-dependent manner. In group receiving a 0.75 mg/kg intravenous bolus followed by 1.75 mg/kg per hour infusion for 4 h, bivalirudin concentrations remained at 5000-5500 μg/l within the 4 h infusion period, which was similar to the reported data of Caucasian patients and can provide the desired anticoagulant effects. There was a strong correlation between bivalirudin concentration and anticoagulant effect. A Sigmoid model was used to fit the pharmacodynamic parameters activated clotting time (ACT), activated partial thromboplastin time (APTT) and prothrombin time (PT) and bivalirudin concentrations. The findings of this study suggest that the same dosing regimens of bivalirudin may be administered to Chinese and Caucasian patients. Ongoing and future studies in large populations may add further information.