微量皮质类固醇联合抗病毒药物治疗单纯疱疹病毒性角膜炎

目的观察微量皮质类固醇与抗病毒药物合用对单纯疱疹病毒性角膜炎（ＨＳＫ）的疗效。方法将１６０例ＨＳＫ患者随机分为治疗组和对照组,治疗组用５ｇ·Ｌ－１可的松、１ｇ·Ｌ－１无环鸟苷（ＡＣＶ）和２５ｇ·Ｌ－１三氮唑核苷（ＲＢＶ）３种眼液,对照组用１ｇ·Ｌ－１ＡＣＶ和２５ｇ·Ｌ－１ＲＢＶ２种眼液交替滴眼治疗。结果治疗组治愈率、有效率明显高于对照组（Ｐ＜０．０１）,治愈时间明显短于对照组（Ｐ＜０．０１）,随访１４～２４ｍｏ复发率明显低于对照组（Ｐ＜０．０１）。结论在临床上用微量皮质类固醇联合足量有效的抗病毒药物,对上皮型和实质层型ＨＳＫ都能促进其痊愈过程,并可降低复发率。     

Inhibition of cardiac inward-rectifier K current by terodiline

The antispasmodic agent terodiline has cardiotoxic effects that include QT lengthening. To determine whether inhibition of inwardly-rectifying K⁺ current (I_K1) might be a factor in the cardiotoxicity, we measured I_K1 in guinea pig ventricular myocytes. Terodiline reduced outward I_K1 with an IC₅₀ of 7 μM; maximal reduction was 60% with 100–300 μM concentration. Inhibition was independent of current direction, and persisted after removal of the drug. Terodiline (3–5 μM) lengthened action potentials in guinea pig papillary muscles by ca. 10%, primarily by slowing phase 3 repolarization; higher concentrations abbreviated the plateau and markedly slowed late repolarization. Terodiline washout provoked an extra lengthening, consistent with persistent inhibition of I_K1 and rapid recovery of net inward plateau current. The results suggest that inhibition of I_K1 is a likely factor in the cardiotoxicity of the drug.     

Synthesis of 2′,3′-dideoxyisoguanosine from guanosine

2,3'-Dideoxyisoguanosine was synthesized from guanosine via intermediate 6-[(4-methylphenyl)thio]-2-oxo-9-(2',3',5'-tri-O-acetyl-beta-D-ribofuran osyl)-2,3-dihydropurine (4). The 2-oxo, 6-amino and 5'-hydroxy triprotected isoguanosine derivative was utilized to reduce high polarity and promote poor solubility of intermediates. The protecting groups for oxo and 6-amino were easily removed in reduction of olefin in ribose without additional reaction steps. 2',3'-Vicinal diol in ribose sugar moiety was transformed to olefin with Bu3SnH by radical reaction via bisxanthate. Removing 5'-O-TBDMS protecting group gave final product, 2',3'-dideoxyisoguanosine (12) in a 10% overall yield.     

Haemodynamic study as guideline for the use of beta blockers in acute theophylline poisoning

It has been proposed that -blocker therapy reverses metabolic and cardiovascular disorders in acute theophylline poisoning. We present a case of acute theophylline overdose treated with esmolol under haemodynamic control. Haemodynamic monitoring was useful in determining the appropriate duration of administration of esmolol and in deciding on treatment with fluids.     

The cardiotonic bipyridine AWD 122-60 inhibits adenosine triphosphate-sensitive potassium channels of mouse skeletal muscle

Summary The inhibition of ATP-sensitive potassium channels in mouse skeletal muscle by the cardiotonic bipyridine AWD 122-60 was investigated with the patch-clamp technique. In excised patches of the inside-out configuration, internally applied AWD 122-60 (10^–6–10^–3 mol/1) reversibly reduced the open-probability of single ATP-sensitive potassium channels. The agent shortened the periods of channel activity but did not affect the channel conductance. At positive membrane potentials channel inhibition by AWD 122-60 was more pronounced than at negative potentials, the drug concentrations producing 50% channel inhibition were 11 mol/l at + 40 mV and 29 mol/l at –40 mV. The Hill coefficients of the concentration-response curves were in the range between 0.5 and 0.6 for both potentials. milrinone (10^–4 mol/I), had no effects on ATP-sensitive potassium channels in skeletal muscle. potassium channels in heart muscle by AWD 122-60 are discussed. Send offprint requests to B. Neumcke at the above address     

Subacute sclerosing panencephalitis: brain stem involvement in a peculiar pattern

The most common pattern in subacute sclerosing panencephalitis, is in the cerebral hemisphere white matter on T2-weighted images with or without atrophy. Brain-stem lesions are rare. We report brain-stem involvement in two children with subacute sclerosing panencephalitis. A peculiar pattern, with involvement of the pons with extension to both middle cerebellar peduncles and substantia nigra but sparing the pontine tegmentum, is suggested. Received: 10 January 2000/Accepted: 18 April 2000     

白血病化疗药物研究

白血病是一类血液系统的恶性肿瘤，发病机制复杂，涉及到染色体易位、融合基因及融合蛋白的形成、基因拷贝数的改变、癌基因的活化、抑癌基因的失活等。针对不同白血病，从药物作用的分子机制分类综述国内外抗白血病药物的发展及治疗现状。     

2000年～2002年重庆市18家医院抗糖尿病药物应用分析

目的 :对2000年～2002年重庆市18家医院抗糖尿病药物的用药现状和趋势做出客观评估。方法 :调查重庆市18家医院2000年～2002年应用抗糖尿病药物的主要品种、金额等 ,分析临床用药情况。结果 :抗糖尿病药物金额2000年、2001年、2002年分别为498、643、649万元 ,年平均增长率为15 03 %。胰岛素注射液占据38 56 %的市场份额 ,其中混合胰岛素注射液占整个胰岛素注射液59 02 %的市场份额。结论 :抗糖尿病药物是一类很有发展潜力的药物 ,混合胰岛素和新型口服抗糖尿病药物的用量将不断增加。     

盐酸布替萘芬合成工艺改进

盐酸布替萘芬 ( butenafine hydrochloride,1 ) ,化学名为 N- [[4- ( 1 ,1 -二甲基乙基 )苯基 ]甲基 ]- N -甲基 - 1 -萘甲胺盐酸盐 ,系由日本科研株式会社研发的新型苄胺类广谱抗真菌药 [1] ,于 1 992年在日本首次上市 ,商品名 Mentax。本品能选择性抑制真菌角鲨烯环氧化酶 ,阻碍麦角甾醇的生物合成 ,从而导致真菌细胞死亡 ,具有疗效高、见效快、复发率低、副作用小等特点 [2 ]。1的合成以由 N -甲基 - 1 -萘甲胺盐酸盐 ( 2 )与对叔丁基卤苄反应的路线具有原料易得、操作简单等优点。多以 2与对叔丁基氯苄 ( 3)或对叔丁基溴苄在干燥 DMF…     

帕珠沙星合成中的Hofmann重排反应

将帕珠沙星的合成关键中间体(3S)—9—氟—10—(1—氨甲酰基环丙基)—3—甲基—7—氧代—2，3—二氢—7H—吡啶[1，2，3—de]—1，4—苯并嚼嗪—6—羧酸溶于甲醇钠／甲醇溶液中，于—40℃加溴进行Hofmann重排得到帕珠沙星。收率69％。