金锁匙口服液药效学及毒性研究

通过对金锁匙口服液的药效学及毒性的研究表明：本品能明显抑制吗啡依赖性小白鼠停药后的跳跃反应，协同戊巴比妥钠催眠作用，提高小鼠热板法痛阈值，抑制醋酸引起的小鼠扭体反应，提示金锁匙口服液对吗啡类成瘾患者有一定的治疗作用，毒理研究表明；本品服用无药物依赖性、安全、无毒。     

Favorable effects of epidural analgesia on hemodynamics,oxygenation and metabolic variables in the immediate post-anesthetic period

Fourteen adult patients undergoing elective major abdominal surgery were divided into two groups. One group received epidural and general anesthesia (epidural group), and 20 ml of 0.125% bupivacaine and 2 mg of morphine were administered epidurally about 30 min before the end of the operation for post-anesthetic analgesia. The other group (control group) received general anesthesia alone with nitrous oxide, oxygen and enfiurane. Flow-directed pulmonary arterial and radial arterial catheters were inserted preoperatively, and hemodynamic, respiratory, neuroendocrine and metabolic variables were measured serially. The data were compared during anesthesia and the immediate post-anesthetic recovery period. In the control group, the plasma epinephrine level in the post-anesthetic recovery period increased about four times over the anesthetic period. Oxygen consumption was increased and mixed venous oxygen saturation was decreased significantly. There was a close linear correlation between oxygen consumption (Y) and plasma epinephrine (X) level: Y = 285.7X + 90.5 (P < 0.01, r = 0.72). On the other hand, plasma epinephrine, oxygen consumption and mixed venous oxygen saturation did not change significantly in the epidural group in the post-anesthetic recovery period. There was also a close linear correlation between oxygen consumption (Y) and oxygen delivery (X): Y = 0.22X -32.0 (P < 0.01, r = 0.89). We conclude that the surgical stress and anesthetic reversal may seriously influence neuroendocrine responses and subsequently increase plasma epinephrine. Tissue oxygenation and metabolic imbalance may occur due to the rapid increase of epinephrine in the postanesthetic recovery period. Epidural analgesia at this period may play a more important role and have a more favorable effect on the tissue metabolism.     

Analgesic dose-response relation in cervical epidural block

The relationship between the age and the spread of analgesia from different epidural anesthetic doses was examined by studying analgesic dose responses in cervical epidural analgesia. Two different anesthetic doses (5ml or 10ml) of 2% mepivacaine were injected into the cervical epidural space at a constant pressure (80mmHg) using an intravenous apparatus, and the spread of analgesia to pinprick was assessed. The significant correlation was found between the patients age and the number of spinal segments blocked (5ml:r = 0.8498, P < 0.01, 10ml:r = 0.5988, P < 0.01). The inverse linear relationship was found between the patients age and the segmental dose requirement (5ml:r = –0.6754, P < 0.01, 10ml:r = –0.5784, P < 0.01). Patients under 39 years of age showed a direct relationship between the dose injected and the number of spinal segments blocked, enabling prediction of the number of segments blocked with a given dose of local anesthetic. Doubling the epidural dose approximately doubled the number of spinal segments blocked. The analgesic dose-response relation in patients over 60 years of age differed from that in patients under 39 years of age and doubling the epidural dose did not double the number of spinal segments blocked. Progressively more extensive analgesia was obtained from a given dose of local anesthetic with advancing age. It was difficult to limit the extent of analgesia by injecting a smaller dose of local anaesthetic in the elderly.(Hirabayashi Y, Matsuda I, Inoue S et al.: Analgesic dose-response relation in cervical epidural block. J Anesth 2: 22–27, 1988)     

硬膜外镇痛联合应用乙酰氨基酚在剖宫产术后的镇痛效果

目的：比较对乙酰氨基酚联合自控硬膜外镇痛的多模式术后镇痛与单纯自控硬膜外镇痛用于剖宫产产妇术后镇痛效果。方法：200名行剖宫产的产妇随机分为实验组（S组）和对照组（C组）,S组产妇在术前15min静脉注射对乙酰氨基酚1g,C组产妇在术前15min静脉注射安慰剂（生理盐水）。两组产妇均采用腰硬联合麻醉方案,缝合切口时启动自控硬膜外镇痛泵。术前、术后即刻、术后1天、术后2天观察疼痛强度和血清IL-6、IL -10水平;记录新生儿出生Apgar评分、术后阿片类药物使用量及术后不良反应、产妇满意度和对母乳喂养的影响程度。结果：术后1天疼痛评分S组显著低于C组。术后即刻、术后1天S组IL-6表达水平低于C组,而该时点S组IL-10表达水平高于C组（P＜0.05）。两组间不良反应、新生儿出生Apgar评分、产妇满意度和母乳喂养情况无统计学差异（P＞0.05）。结论：剖宫产术前静脉注射对乙酰氨基酚联合自控硬膜外镇痛比单独应用自控硬膜外镇痛能够为产妇提供更好的术后疼痛管理。     

Effects of epidural bupivacaine and epidural morphine on bowel function and pain after hysterectomy

A comparison was made of the effects of continuous epidural analgesia with bupivacaine and intermittent epidural morphine on bowel function after abdominal hysterectomy. The duration of postoperative ileus was assessed as the time from the end of operation to the first postoperative passage of flatus and feces. Twenty-two patients were randomly allocated to two equal groups. An "epidural morphine" group received general anesthesia and epidural morphine for postoperative pain relief, and an "epidural bupivacaine" group was given combined general anesthesia and epidural anesthesia with 0.5% bupivacaine intraoperatively and epidural analgesia with 0.25% bupivacaine postoperatively. Epidural morphine or bupivacaine was given for 42 h postoperatively. Pain intensity (visual analog scale) was low in both groups, but lower (P less than 0.05) in the epidural bupivacaine group. The time to first passage of flatus was 22 +/- 16 h in the epidural bupivacaine group and 56 +/- 22 h in the epidural morphine group (P less than 0.001). The time to first postoperative passage of feces was shorter (P less than 0.05) in the former than in the latter 57 +/- 44 h vs 92 +/- 22 h). The patients of the epidural bupivacaine group started intake of oral fluids earlier (P less than 0.01) and to a greater extent (P less than 0.05) than those in the epidural morphine group. It is concluded that the duration of postoperative ileus after hysterectomy is shorter when epidural bupivacaine is given for postoperative pain relief than when this is achieved by epidural morphine.     

Computerized axial tomo-epidurographic and radiographic documentation of unilateral epidural analgesia

A 23-year-old primigravid patient who received epidural analgesia for pain of labour presented with persistent, apparently irremediable, unilateral analgesia. Computerized axial tomo-epidurography demonstrated absence of circumferential spread due to lateral placement of the catheter. Transforaminal escape of contrast medium into the paravertebral area had occurred and anterior and posterior midline partitioning of the epidural space was obvious. All the usual measures to promote contralateral analgesia, except re-insertion of the catheter, had been tried without success.     

Epidural compression from metastatic tumor with resultant paralysis

To determine the value of the usually given urgent palliative radiotherapy in paraplegic patients with epidural compression from metastatic tumor, 20 consecutive cases treated between 1981 and 1986 were retrospectively analyzed. Bronchogenic and prostatic carcinoma were the more common extraspinal sources of metastasis. Epidural metastasis involved the thoracic spine in most cases. The onset of neurological symptomatology was frequently within two weeks prior to hospitalization. The majority of the subjects received at least 3000 cGy given in 10 to 15 fractions. Symptomatic (pain relief) response rate was 78 (7/9) percent. The observed period of survival averaged 2.5 months after treatment. This study reaffirmed the little chance for recovery of lost limb(s) motor function. None of the patients (most of whom were paraplegic from two to 90 days pre-irradiation) became ambulatory including the two in whom irradiation was administered within 24 hours from the onset of paraplegia.     

Changes in the antinociceptive effect of mesencephalic stimulation produced by analgesics and tranquilizers

Chronic experiments on cats showed that analgesics, in subanalgesic doses, not only exhibit an antinociceptive effect when accompanied by subthreshold stimulation of the mesencephalon, but also potentiate the analgesic action of central stimulation. Tranquilizers only facilitate the development of an analgesic effect during subthreshold mesencephalic stimulation. The possible reasons for differences in the action of these substances are discussed.Department of Pharmacology, I. P. Pavlov First Leningrad Medical Institute. (Presented by Academician of the Academy of Medical Sciences of the USSR S. V. Anichkov.) Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 85, No. 1, pp. 36–41, January, 1978.     

激活AMPA受体抑制大鼠骶髓后连合核神经元NMDA反应──制霉菌素穿孔法膜片钳研究

在急性分离的大鼠骶髓后连合核神经元上，采用制霉菌素穿孔法膜片钳技术，研究ＡＭＰＡ受体和ＮＭＤＡ受体的相互作用．结果显示，激活ＡＭＰＡ受体可逆性地抑制ＮＭＤＡ反应，该效应依赖于细胞外钙离子．而且，通过ＡＭＰＡ受体通道内流的钙离子单独即足以抑制ＮＭＤＡ受体介导的反应．本结果证明，钙离子可透性ＡＭＰＡ受体可能参与了脊髓伤害性信息的调控．该过程可能与针刺镇痛的机制有关．