Synthesis of a new hydroxyethylene dipeptide isostere Phe ψ[CH2CH(OH)]Phe as HIV-1 protease inhibitor

A new type of pseudodipeptide isostere exampled by Phe ψ[CH2CH(OH)]Phe was synthesized from phenylalanine. The H]V protease inhibitory activity (IC50) of Noa-His-Pheψ[CH2CH(OH)]Phe-Ile-Amp was 0. 8 pmol·L-1.     

愈肾汤治疗小儿急性肾炎

笔者自1985～1990年以来,应用愈肾汤治疗小儿急性肾炎100例,结果:痊愈(症状消失,小便化验正常,随访1年无复发)64例,好转(症状改善,小便化验有少量红、白细胞)28例,无效8例。总有效率92%。     

Effects of Volatile Anesthetics on Glutamate Transporter, Excitatory Amino Acid Transporter Type 3: The Role of Protein Kinase C

Background: Glutamate transporters play an important role in maintaining extracellular glutamate homeostasis. The authors studied the effects of volatile anesthetics on one type of glutamate transporters, excitatory amino acid transporter type 3 (EAAT3), and the role of protein kinase C in mediating these effects.

Methods: Excitatory amino acid transporter type 3 was expressed in Xenopus oocytes by injection of EAAT3 mRNA. Using two-electrode voltage clamp, membrane currents were recorded before, during, and after application of l-glutamate. Responses were quantified by integrating the current trace and are reported as microcoulombs. Data are mean +/- SEM.

Results: l-Glutamate-induced responses were increased gradually with the increased concentrations of isoflurane, a volatile anesthetic. At 0.52 and 0.70 mm isoflurane, the inward current was significantly increased compared with control. Isoflurane (0.70 mm) significantly increased Vmax (maximum velocity) (3.6 +/- 0.4 to 5.1 +/- 0.4 [mu]C;P < 0.05) but not Km (Michoelis-Menten Constant) (55.4 +/- 17.0 vs. 61.7 +/- 13.6 [mu]m;P > 0.05) of EAAT3 for glutamate compared with control. Treatment of the oocytes with phorbol-12-myrisate-13-acetate, a protein kinase C activator, caused a significant increase in transporter current (1.7 +/- 0.2 to 2.5 +/- 0.2 [mu]C;P < 0.05). Responses in the presence of the combination of phorbol-12-myrisate-13-acetate and volatile anesthetics (isoflurane, halothane, or sevoflurane) were not greater than those when volatile anesthetic was present alone. Oocytes pretreated with any of the three protein kinase C inhibitors alone (chelerythrine, staurosporine, or calphostin C) did not affect basal transporter current. Although chelerythrine did not change the anesthetic effects on the activity of EAAT3, staurosporine or calphostin C abolished the anesthetic-induced increase of EAAT3 activity.     

带血管隔肌瓣翻转术治疗贲门失驰缓症

贲门失弛缓症是吞咽时食管体部无蠕动,贲门括约肌弛缓不良。本病的治疗方法甚多,1898年Russel氏首先用气囊扩张治疗。1915年Heity改用泵囊扩张。1913年Heller设计将食管肌层纵行切开直至粘膜膨出,取得较好的效果。本文报道用带有血管的膈肌瓣翻转术治疗     

Oxygenation of Liver Transplants as a Predictor of Success

ＯｘｙｇｅｎａｔｉｏｎｏｆＬｉｖｅｒＴｒａｎｓｐｌａｎｔｓａｓａＰｒｅｄｉｃｔｏｒｏｆＳｕｃｃｅｓｓＹＥＱｉｆａ（ＤｅｐａｒｔｍｅｎｔｏｆＳｕｒｇｅｒｙ，ＴｏｎｇｊｉＨｏｓｐｉｔａｌ，ＴｏｎｇｊｉＭｅｄｉｃａｌＵｎｉｖｅｒｓｉｔｙ，Ｗｕｈａｎ４３００...     

大剂量鲁米那钠加安定静脉滴入治疗新生儿破伤风

近年来新生儿破伤风有增加趋势,死亡率高,我院子1985年起,试用大剂量鲁米那钠加安定静脉滴入,治疗住院病儿52例,疗效满意,现报告如下: 临床资料治疗组52例,男36例,女16例,平均发病日龄9.19天。对照组123例,男91例,女32例,平均发病日龄9.75天。诊断标准参照教科书。痉挛强度用计分法:单纯牙关紧闭为1分,牙关紧闭+角弓反张+刺激性痉挛为2分,频繁自发性痉挛为3分,持久而严重的自发性痉挛+紫绀或呼吸暂停为4分。     

FDA审查Pfizer改变Norvasc标签的要求

美国FDA的心血管肾脏药物咨询委员会将在4月5日审查Pfizer公司请求修改Norvasc（amlodipine besylate，氨氯地平）（Ⅰ）的商标资料，其中包括具有里程碑意义的2002年ALLHAT研究中减少冠心病发作危险的结果。这项降压降脂预防心脏病发作试验共有42000多名高危的高血压病人参加。     

Beneficial Effects of Short-term Vasopressin Infusion during Severe Septic Shock

Background: Septic shock is associated with vasopressin deficiency and a hypersensitivity to its exogenous administration. The goal of the current study was to determine whether short-term vasopressin infusion in patients experiencing severe septic shock has a vasopressor sparing effect while maintaining hemodynamic stability and adequate end-organ perfusion.

Methods: Patients experiencing septic shock that required high-dose vasopressor support were randomized to a double-blinded 4-h infusion of either norepinephrine (n = 11) or vasopressin (n = 13), and open-label vasopressors were titrated to maintain blood pressure. To assess end-organ perfusion, urine output and creatinine clearance, gastric mucosal carbon dioxide tension, and electrocardiogram ST segment position were measured.

Results: Patients randomized to norepinephrine went from a median prestudy norepinephrine infusion of 20.0 [mu]g/min to a blinded infusion of 17.0 [mu]g/min at 4 h, whereas those randomized to vasopressin went from a median prestudy norepinephrine infusion of 25.0 [mu]g/min to 5.3 [mu]g/min at 4 h (P < 0.001). Mean arterial pressure and cardiac index were maintained in both groups. Urine output did not change in the norepinephrine group (median, 25 to 15 ml/h) but increased substantially in the vasopressin group (median, 32.5 to 65 ml/h;P < 0.05). Similarly, creatinine clearance did not change in the norepinephrine group but increased by 75% in the vasopressin group (P < 0.05). Gastric mucosal carbon dioxide tension and electrocardiogram ST segments did not change significantly in either group.     

福建省室内蜚蠊调查研究

对福建省室内蜚蠊的调查结果,已发现四科、五属、十五种(已定的九种,未定的六1种).并就蜚蠊的种群分布,季节消长、活动规律、生态习性和蜚蠊与疾病关系以及诱捕、杀灭方法等进行了较系统的研究为进一步研究、防制蜚蠊提供科学依据。     

医院门诊药房与医院分离的理性探讨

介绍了医药分业的定义、国外医药分业的目的和少数医院无门诊药房的原因。指出门诊药房从医院分离出去弊大于利,认为门诊药房从医院分离,难以达到预期目的,反而有损于医疗卫生事业的公益性;医药分离削弱、甚至取消了医院对医师不当处方和合理药物治疗等医疗行为的行政和技术监管与干预;医药分离不适合我国的国情,不符合我国卫生体制改革的精神,不利于医疗质量的提高,不利于病人安全、有效、经济用药,不利于调动医院广大药学技术人员的积极性,不利于医院药物治疗管理自动化的实现与信息的传递。建议医药结合的模式必须加强;保留门诊药房,加大监督力度;建立药品配送中心,完善社会化物流机制;加速非处方药药品的发展;在条件成熟后实施处方调剂费;高薪养廉,较大幅度提高医师职业的收入;解决当前医疗体系中分配不合理问题,适当提高挂号、手术、诊疗等收费标准,降低药品收入在医院总收入中所占的比例。