琥珀胆碱诱发吸气延长效应及机制

用63只麻醉、制动、切断双侧迷走神经、人工呼吸的家兔,以偏神经放电作为呼吸观测指标,观察股动脉注射射琥珀胆碱（Sch）诱发的肌梭传入活动对呼吸的影响。结果发现23只吸气延长,表现为吸气时程（Ti）明显延长,呼气时程（Te）有缩短趋势,Ti／Te比值增加;肌注布比卡因破坏肌梭后,同剂量Sch则便吸气延长效应明显减弱。提示股动脉注射Sch诱发的肌梭传入活动对呼吸运动具有明显的吸气增强作用。     

布比卡因注射致大鼠脊髓损伤模型的制作

目的建立动物模型观察脊髓损伤后的病理生理改变,寻找可直接判断脊髓损伤程度的方法 ,优选出治疗脊髓损伤的最佳方案。方法暴露大鼠L2-3脊髓后,于脊髓内注射0.5%布比卡因,评价大鼠行为学改变及脊髓形态学改变。观察并记录大鼠后肢行为学改变及脊髓神经元和周围组织的病理改变,评估脊髓损伤程度。结果与生理盐水注射组(对照组)相比,布比卡因注射组(观察组)大鼠脊髓损伤,表现为术后大鼠BBB评分降低,与对照组比较差异有统计学意义,病理HE染色可见脊髓神经元出现空泡变性及液化坏死。结论应用腰麻针进行大鼠脊髓穿刺并注射布比卡因的大鼠动物模型,具有稳定可控的脊髓损伤效果。     

0.375%左旋布比卡因与罗哌卡因用于肌间沟臂丛神经阻滞果及术后镇痛的临床观察

目的 观察罗哌卡因和左旋布比卡因用于肌间沟臂丛神经阻滞的阻滞效果以及术后镇痛时间.方法 选择行上肢手术的病人40例,随机分为两组,每组20例,分别用0.375%左旋布比卡因和0.375%罗哌卡因25ml行臂丛神经阻滞,术中行阻滞满意程度评价,术后行VAS评分,并记录感觉、运动阻滞恢复时间.结果 两组术中阻滞满意度相同,同时左旋布比卡因组感觉和运动恢复时间长于罗哌卡因组(P＜0.01).结论 两组术中阻滞满意度相同.和罗哌卡因相比,左旋布比卡因可提供更为满意的术后镇痛.     

相同浓度的左旋布比卡因与罗哌卡因用于颈丛阻滞的比较

布比卡因用于颈丛阻滞对心血管系统的影响较大，出现声嘶或呼吸困难后恢复较慢，而罗哌卡因及左旋布比卡因对心脏毒性作用明显低于布比卡因，左旋布比卡因对心脏的抑制作用只有布比卡因的1／3。本研究观察相同浓度剂量的0．5％左旋布比卡因与0．5％罗哌卡因用于颈丛阻滞的临床效果及对心血管系统的影响，报告如下。     

舒芬太尼和左旋布比卡因用于下腹部外科术后自控镇痛的效果研究

目的比较舒芬太尼和左旋布比卡因配伍以及哌替啶和异丙嗪配伍术后镇痛的效果。方法100例手术患者分成两组，Ⅰ组（50例）舒芬太尼100μg＋0．125％左旋布比卡因100ml利用微量泵进行术后自控镇痛（PCA）2ml／h，患者疼痛时可自行或由家属控制给药2ml；Ⅱ组（50例）哌替啶50mg和异丙嗪25mg配伍肌内注射进行术后镇痛，疼痛时即肌内注射1次，下次肌内注射用药时间一般不少于6h。结果使用舒芬太尼和左旋布比卡因配伍进行术后自控镇痛以及使用哌替啶和异丙嗪配伍肌内注射术后镇痛，两种方法镇痛效果差异有显著统计学意义。相比之下，前者具有操作简单、见效快、镇痛效果稳定可控、无成瘾性等优点。结论舒芬太尼和左旋布比卡因配伍术后自控镇痛法优于哌替啶和异丙嗪配伍术后肌内注射镇痛。     

比较不同比重布比卡因腰麻应用于产科麻醉的临床效果

目的比较不同比重布比卡因腰麻应用于产科麻醉的临床效果。方法选取我院2009年8月至2011年8月收治的剖宫产手术患者90例,按照随机分配的方法,将其分为A、B、C三组,A组给予1.5mL布比卡因加1mL注射用水,B组给予1.5mL布比卡因加10%葡萄糖1mL,C组给予1.5mL布比卡因加0.9%生理盐水1mL,观察三组的麻醉效果、起效时间、循环指标、血流动力学、肌松效果、麻醉平面、麻醉消退时间。结果三组效果的起效时间、肌松效果、麻醉满意度均无显著差异;麻醉平面相比,A组0.05)。结论针对产科麻醉有利于麻醉平面的调节与扩展,可取得较好的临床效果,且无明显的不良反应增加,值得临床推广应用。     

左旋布比卡因腰硬联合阻滞在剖宫产手术的应用

目的探讨0.75%左旋布比卡因用于蛛网膜下腔阻滞的临床效果和安全性。方法选择ASAⅠ-Ⅱ级的60例剖宫产患者,随机分成两组：A组腰麻用0.75%左旋布比卡因7.5mg,容量为1.5mL;B组腰麻用量为0.75%布比卡因,剂量及容量与A组相同。胎儿取出后硬膜外导管注入1%利多卡因5mL。必要时可续注1%利多卡因5mL。术中测BP、HR、SPO2、RR变化。注意观察不良反应的发生,观察胎儿取出时情况。结果两组最高阻滞平面及达到时间,持续时间、肌松效果、胎儿Apgar评分均无显著意义。结论 0.75%左旋布比卡因用于腰硬联合麻醉下剖宫产手术是安全有效的,其结果与0.75%布比卡因相比差异无显著性。     

0．375％左旋布比卡因与罗哌卡因用于肌间沟臂丛神经阻滞效果及术后镇痛的临床观察

目的观察罗哌卡因和左旋布比卡因用于肌间沟臂丛神经阻滞的阻滞效果以及术后镇痛时间。方法选择行上肢手术的病人40例，随机分为两组，每组20例。分别用0．375％左旋布比卡因和0．375％罗哌卡因25ml行臂丛神经阻滞，术中行阻滞满意程度评价．术后行VAS评分，并记录感觉、运动阻滞恢复时间。结果两组术中阻滞满意度相同，同时左旋布比卡因组感觉和运动恢复时间长于罗哌卡因组（P〈0．01）。结论两组术中阻滞满意度相同。和罗哌卡因相比，左旋布比卡因可提供更为满意的术后镇痛。     

不同浓度布比卡因复合芬太尼用于术后镇痛效果比较

目的 比较不同浓度布比卡因复合芬太尼用于妇产科手术后硬膜外镇痛的效果及下肢运动阻滞的影响,以推荐合适的布比卡因浓度,供临床参考应用。方法 择期妇产科手术病人60例。按术后硬膜外用药不同随机分为3组,每组20例.A组术后硬膜外用0.1％布比卡因,B组为0.15％布比卡因,C组为0.2％布比卡因。3组均加入芬太尼0.2mg,总药液量为100ml,记录3组患者术后(36小时内)主诉手术部位疼痛程度及下肢运动阻滞的程度,进行统计学处理。结果①B、C两组在术后36小时内不同时段疼痛评分明显低于A组,有显著性差异(P<0.01),B组与C组疼痛评分无组间差异(P>0.05)。②各组镇痛期间下肢运动阻滞程度:C组与A组比较有显著性差异(P<0.05)。结论 0.15％布比卡因复合芬太尼硬膜外应用可获得良好的术后镇痛效果,同时对下肢运动阻滞较轻。     

小儿患者左旋布比卡因臂丛神经阻滞的药代动力学

目的:研究左旋布比卡因用于小儿患者臂丛神经阻滞的药代动力学特性。方法:9例行择期上肢手术小儿患者,分别予0.375%左旋布比卡因(0.4 mL/kg)行肌间沟入路臂丛神经阻滞。于注药后10、20、30、45、60、90、120、180、240、360、480和720 min测定左旋布比卡因血药浓度,3P97软件计算药代动力学参数。结果:左旋布比卡因血药浓度-时间数据符合二房室开放模型,主要药代动力学参数消除半衰期(t1/2β)、达峰时间(Tmax)和峰值浓度(Cmax)分别为(4.77±0.52)、(0.28±0.14)h和(1.02±0.22)mg/L。结论:0.375%左旋布比卡因可安全用于小儿臂丛神经阻滞,其临床药代动力学符合二房室开放模型。     

Myotoxic activity of the crude venom and the principal neurotoxin, taipoxin, of the Australian taipan, Oxyuranus scutellatus.

1 The crude venom of the Australian taipan. Oxyuranus scutellatus and its principal neurotoxin, taipoxin, were injected into the anterolateral aspect of one hind limb of the rat. 2 The effects of the venom and toxin on the morphology and physiology on the underlying soleus muscles were examined. 3 Both the crude venom and the toxin caused necrosis and degeneration of the muscle. Damage to the peripheral muscle fibres could be seen at the light microscopic level as early as 3 h after injection of the toxic compounds. 4 The necrotic response was accompanied by an infiltration of phagocytic cells and an extensive oedema. The wet weight of the damaged muscles was almost doubled by 6 h. 5 In individual muscle fibres, necrosis was associated with the disruption of the plasma membrane and the disorganization of the myofibrils. The basal lamina of the muscle fibres was left intact. 6 Denervated mammalian muscles and innervated avian muscles were also destroyed by tiapoxin, but immature avian muscle growing in tissue culture was resistant. 7 Of the 3 subunits of taipoxin, only the basic alpha-taipoxin was itself myotoxic. However, its potency was enhanced by the presence of the acid gamma subunit. The role of the neutral beta-subunit is unclear. 8 The period of necrosis and degeneration lasted for approximately 48 h, after which the muscle fibres began to regenerate. Regeneration took place within the surviving basal lamina, with the formation of myotubes by three days, and small, immature muscle fibres by five days. Regeneration was virtually complete by 21 days.     

Differential vulnerability of 3 rapidly conducting somatosensory pathways in the dog with vitamin B6 neuropathy

In anesthetized dogs with chronically implanted cortical electrodes somatic sensory-evoked potentials (SEPs) were produced by electrical stimulation at neural, muscular or cutaneous sites of the contralateral hind leg. Stimulation of the tibial nerve at the calcaneus or of the short flexor muscles of the hind paw caused SEPs having characteristics following activation of rapidly conducting afferents from muscle spindles. Stimulation of the glabrous skin of the central pad resulted in SEPs arriving after a more protracted latency evidently related to activation of afferents from Merkel cells, Krause and Pacinian corpuscles known to be located at these sites. Stimulation of the hairy skin from the dorsal surface of the hindpaw produced a further type of SEP presumably resulting from activation of afferents from receptors of tylotrich hair follicles. Vitamin B6-induced neuropathy involves the selective degeneration of the largest neurons in the spinal ganglia and of associated long peripheral and central neurites performing rapid impulse transmission. In the course of vitamin B6 neuropathy the relatively slow impulse transmission following stimulation of the central pad was more severely impaired than the faster one after activation of afferents from muscle spindles or receptors from hair follicles. This allows us to conclude that in the dog afferents from the glabrous skin of the central pad conduct centrally via the dorsal columns, susceptible to vitamin B6 intoxication, while muscle and hair receptor afferents ascend in the dorsal spinocerebellar and spinocervical tract, respectively, which are vitamin B6 resistant.     

Pharmacological studies on schizandra fruits. III. Effects of wuweizisu C, a lignan component of schizandra fruits, on experimental liver injuries in rats

The effects of wuweizisu C, a lignan component of schizandra fruits, on liver injuries induced by carbon tetrachloride (CCl4), d-galactosamine and dl-ethionine were investigated by means of serum-biochemical and histopathological examinations in rats. Pretreatment or combined administration of wuweizisu C dose-dependently reduced the elevation of serum transaminase activity and histological changes such as fatty degeneration, cell necrosis, inflammatory cell infiltration, etc., which were caused by the single administration of 1 ml/kg, p.o., or the repeated administration of 0.2 ml/kg, s.c., daily for 4 days of CCl4, respectively. The effects of wuweizisu C on the liver injuries induced by a low dose (200 mg/kg, i.p.) and a high dose (400 mg/kg, i.p.) of d-galactosamine were compared with those of uridine. Wuweizisu C significantly lowered the rise of serum transaminase activity after the administration of a low dose of d-galactosamine in the serum-biochemical analysis. A tendency was also shown to inhibit cell necrosis and inflammatory cell infiltration caused by both doses of d-galactosamine in the histopathological examination. On the other hand, uridine markedly repaired the serum-biochemical and histopathological changes after the administrations of both doses of d-galactosamine. Also wuweizisu C cured the liver injury by the repeated administration of 150 mg/kg, i.p., daily for 4 days of d-galactosamine. After the repeated administration of 250 mg/kg, s.c., daily for 4 days of ethionine, liver cell atrophy, diffuse fatty degeneration and decrease of serum triglyceride were observed, but not cell necrosis. Wuweizisu C dose-dependently inhibited fatty degeneration and decrease of serum triglyceride. These findings suggest that wuweizisu C can be protective and/or therapeutic on hepatocellular phenomena such as cell necrosis, fatty degeneration, inflammatory cell infiltration, etc., in human hepatitis.     

Absorption of Bupivacaine after Administration of a Lozenge as Topical Treatment for Pain from Oral Mucositis

The aim was to investigate systemic exposure after administration of a novel bupivacaine lozenge in healthy individuals with normal mucosa and in head and neck cancer (HNC) patients with oral mucositis. A lozenge containing 5, 10, 25 and 50 mg bupivacaine, respectively, was administered as single dose to 10 healthy individuals, and a lozenge containing 25 mg bupivacaine was administered as single dose to 10 HNC patients with oral mucositis and as multiple doses to five patients with HNC. Blood samples were collected for 6 hr from the healthy individuals and 3 hr from the patients with HNC, respectively, after administration. The plasma concentration–time profiles of bupivacaine were fitted to pharmacokinetic models using nonlinear mixed‐effects modelling, evaluating demographics and health status as covariates. The population pharmacokinetics (PK) of bupivacaine lozenge was best described by a two‐compartment distribution model with absorption transit compartments. All the observed plasma concentrations were well below the bupivacaine concentrations (2000–2250 ng/ml) which have caused toxic symptoms. The PK model suggested that relative bioavailability was two times higher in HNC patients with oral mucositis grade 1–2 and three times higher in HNC patients with oral mucositis grade 3–4 than in the healthy individuals. Simulations showed that the plasma concentrations would be below the toxic limit after repeated dosing every second hour with 25 mg bupivacaine for five days. The 25‐mg bupivacaine lozenges were safe without systemic toxic levels of bupivacaine or risk of side effects. Based on PK simulations of repeated doses of 25 mg every two hours for 16 hr a day, the lozenges can be administered with minimum risk of exceeding the toxic limit.     

布比卡因复合舒芬太尼用于剖宫产术腰麻布比卡因的最低有效剂量研究

目的采用序贯法测定布比卡因复合舒芬太尼腰麻用于剖宫产术布比卡因的最低有效剂量。方法30例单胎和妊娠足月行剖宫产术患者,于L3～4蛛网膜下腔穿刺成功后,给予舒芬太尼5．0ug复合布比卡因腰麻,第一个病人给予布比卡因7．5mg,每次剂量调整0．5mg。成功：麻醉诱导10min内改良Bromage运动阻滞评分为3级,阻滞60min内麻醉平面维持在T6水平,下一个病人的布比卡因用量减少0．5mg;反之为失败,下一个病人的布比卡因用量则增加0．5mg。结果布比卡因的半数有效剂量为5．12mg,95％可信区间（4．33～6．05）mg。结论采用序贯法测定布比卡因复合舒芬太尼腰麻用于剖宫产术布比卡因的最低有效剂量是5．12mg。     

FURTHER OBSERVATIONS ON THE PATHOLOGICAL RESPONSES OF RAT SKELETAL MUSCLE TO TOXINS ISOLATED FROM THE VENOM OF THE AUSTRALIAN TIGER SNAKE, NOTECHIS SCUTATUS SCUTATUS

1. Some aspects of the response of mammalian skeletal muscle following the injection of purified toxins from the venom of the Australian tiger snake, Notechis scutatus scutatus, are described. 2. The toxins used were notexin, notechis II-5, notechis II-1 and a modified form of notexin (PBP-notexin). They were injected into the dorso-lateral aspect of one hind limb so that the soleus muscle would be exposed to the toxins. 3. Within 1 h after the injection of notexin, the soleus muscles were oedematous and by 3–6 h, polymorphonuclear leucocytes had entered the interstitial spaces. The invasion of necrotic muscle fibres was extensive by this time. Muscle spindles appeared relatively unaffected by the toxin. 4. The muscle regenerated via myoblasts at 2–3 days to myotubes at 3–5 days, immature muscle fibres at 7–14 days and fully differentiated muscle fibres by 21–28 days. Even after 6 months, however, the nuclei of many muscle fibres remained in a central position. 5. A second component of Australian tiger snake venom was also found to be myotoxic. It was slightly less potent than notexin, but caused qualitatively similar damage to that caused by notexin. It was identified as notechis II-5. A third fraction, notechis II-l, was found to be inactive. 6. Notexin could be neutralized by incubation with tiger snake antivenene; the simultaneous injection of antivenene with notexin did not afford complete protection against muscle damage.     

Neurotoxicology of vincristine in the cat

Cats were given vincristine sulfate (50 g/kg i.v. every 4 days) and studied after 7–29 injections when neurological deficits became evident. The conduction velocity spectrum of individual afferent nerves from soleus muscles was shifted toward slower velocities. Relatively few functional muscle spindles or other proprioceptors which responded to muscle stretch were encountered. Those primary endings of soleus muscle spindles which did respond were significantly reduced in dynamic but not length sensitivity. Length sensitivity of secondary endings was unchanged. Thresholds of secondary but not primary endings were elevated. The average conduction velocity of soleus motor axons was reduced 30% but no deficit was detected in motor nerve terminal function. Indirectly-elicited contractile tension of the soleus muscles of the neuropathic cats was not significantly lower than that in untreated animals. Amplitudes of spinal monosynaptic reflexes were unaffected. These data indicate, that in the cat, neurological impairment results partly from dysfunction in muscle spindles and peripheral nerves.     

Muscular irritation study of gadobenate dimeglumine formulation (E7155) in rabbits

To examine the local muscular irritation potency of gadobenate dimeglumine formulation (E7155), E7155 was injected into the right vastus lateralis muscle of male Kbl:JW rabbits, and saline as the negative control was injected into the left muscle. Half of the animals were subjected to necropsy at 2 or 14 days after administration. The muscles were examined macroscopically and histopathologically. Also, 0.425 w/v% and 1.7 w/v% acetic acid solutions were used as a positive control. In macroscopic observation, hemorrhage with white or brown coloration was seen in the muscles treated with E7155 at 2 days after administration, and white coloration was seen in one case at 14 days after administration. In histopathological examination, slight or moderate hemorrhage, edema, cellular infiltration, degeneration of muscle fibers and necrosis of muscle fibers were seen in the muscles treated with E7155 at 2 days after administration, and very slight to slight cellular infiltration, degeneration of muscle fibers, fibrosis, calcification of muscle fibers and foreign body giant cells were seen in the muscles treated with E7155 at 14 days after administration. The changes in the muscle caused by E7155 were definitely less than those caused by the 1.7 w/v% acetic acid solution at both 2 and 14 days, and slightly less and definitely less than those caused by the 0.425 w/v% acetic acid solution at 2 days and 14 days after administration, respectively. The changes caused by E7155 were more severe than those caused by saline. It was concluded that the local muscular irritation potency of E7155 could be classified at Grade 2.     

Depression of muscle spindle activity—a new type of pharmacological action?

The effect of 2,4-di(diethylamino)-6-(2-phenylacetylhydrazino)-1,3,5-triazine (Ciba 28882-Ba) injected intravenously on the activity of de-efferented muscle spindles of the tibialis anterior and extensor digitorum longus muscles of anaesthetized cats, and on γ-motoneurones of decerebrate cats, was investigated. The drug depressed both the static activity of muscle spindles and the spontaneous activity of γ-motoneurones. In contrast, the response of muscle spindles to rapid stretch was not affected. The effect of 28882-Ba on the activity of the muscle spindles resembled that of progressive unloading or shortening of the muscle. 28882-Ba antagonized excitation of the muscle spindle by suxamethonium. The effect of 28882-Ba on the response of the γ-motoneurones to various driving stimuli was not predictable.     

The effects of dimethothiazine on muscle spindle activity in the decerebrate cat

1. The effects of dimethothiazine have been studied on the response of afferent fibres from primary and secondary endings of muscle spindles in the soleus muscle of the decerebrate cat during stretching of the muscle under controlled conditions.2. Dimethothiazine in doses of 1 to 4 mg/kg intravenously reduced the discharge frequency of primary and secondary endings. Higher doses of dimethothiazine had little further significant effect on the discharge frequency.3. The discharge frequency recorded from de-efferented muscle spindles in soleus of the decerebrate cat were similar to the discharge frequencies obtained in preparations with intact ventral roots which had received a high dose of dimethothiazine.4. Dimethothiazine had little significant effect on the discharge frequency of afferent fibres from muscle spindles in the soleus muscle of decerebrate preparations where the ventral roots were cut.5. These effects of dimethothiazine on muscle spindle activity were not related to any changes in blood pressure of the decerebrate cat.6. Dimethothiazine appears to reduce the effects of both the dynamic and static fusimotor fibres on the spindle.7. The doses of dimethothiazine which effect spindle discharge frequency are similar to those required to reduce decerebrate rigidity.