抗青光眼药物的应用

用于抗青光眼的药物种类繁多,目的在于降低眼压及缓解瞳孔阻滞。1肾上腺素能神经制剂1．1拟肾上腺素能神经制剂1．1．1 1％-2％肾上腺素(Epinephrine),直接兴奋肾上腺素能β受体,局部应用可增加房水引流,减少血流及超滤过功能,导致房水生成减少,从而降低眼压。降压作用可持续数周或     

常用抗青光眼药物的药理及临床应用

综述抗青光眼药物的药理作用及临床应用.根据其化学结构和药理性质,临床上常用的抗青光眼药物主要分为7类:拟副交感神经药、拟肾上腺素药、抗肾上腺素药、碳酸酐酶抑制剂、高渗脱水剂、前列腺素类降眼压药和复合制剂.目前抗青光眼的治疗主要是降低眼压,同时增加眼血流量及保护视神经.     

α2-肾上腺素能受体激动剂酒石酸溴莫尼定的临床应用

α2-肾上腺素能受体激动剂酒石酸溴莫尼定(Brmonidine BMN)对α2-受体具有高度选择性,降眼压效果确实而持久,是一类安全有效的抗青光眼药物,可应用于原发性开角型青光眼及高眼压患者的治疗,尤其适用于β-受体阻滞剂使用禁忌证的患者,有望成为治疗青光眼的首选药物.     

曲伏前列素滴眼液对原发性开角型青光眼患者的眼压 疗效及不良反应的影响

<正>青光眼是临床上较为常见的眼科疾病,其临床表现以视野缺损及视神经萎缩为主,是一种不可逆的致盲疾病,据统计,原发性开角型青光眼大约占所有青光眼的70%,全球范围内约有450万人因此失明,故临床对其治疗尤为重视[1,2]。该疾病主要病理特征为眼压增高,目前治疗仍以降低眼压为主,常用药物马来酸噻吗洛尔属于β受体阻断剂,对β1、β2受体均有阻断作用,从而产生降低眼压的疗效[3]。目前曲伏前列     

抗青光眼药物的研究进展

近年来，一些新型抗青光眼药物被用于眼科临床，例如，α2-肾上腺素能受体激动剂溴莫尼定、局部碳酸酐酶抑制剂多佐胺和布林佐胺、前列腺素拟似剂等。本文对该类药物对青光眼和高眼压症患者增加眼部血流量、视神经保护和控制24h眼压的效果进行了文献综述，旨在促进抗青光眼药物的临床应用。     

巩膜瓣可拆除缝线在小梁切除术中的应用

小梁切除术是目前抗青光眼的主要术式 ,适用于各种类型的青光眼[2 ] ,在临床上已被广泛应用。但基本的小梁切除术在临床上还存在诸如术后早期低眼压、浅前房、低眼压性黄斑病变、术后后期滤过泡瘢痕化而致失败等问题 ,因此逐渐趋向于用若干新技术联合组成的复合式小梁切除术[1] 。巩膜瓣可拆除缝线技术是现代复合式小梁切除术中重要的新技术之一。笔者将该技术应用于临床 ,在防止小梁切除术后低眼压、浅前房的发生以及促进功能性滤过泡的形成方面取得了初步成效 ,现总结如下。1　资料与方法1 1　临床资料　本组病例为我科 1999年 6月至2 0 0…     

比马前列素滴眼液的药理和临床应用

比马前列素是合成的前列酰胺F2α衍生物，通过增加小梁网通道和葡萄膜巩膜通道的房水流出而降低眼内压（IOP），被认为是目前降眼压作用最强的局部抗青光眼药物。主要用于开角型青光眼（POAG）或高眼压症（OHT）的患者，全身不良反应较少。现主要综述该药的药理作用、药动学及临床应用。     

原发性闭角型青光眼持续高眼压状态下的手术治疗

目的探讨原发性闭角型青光眼持续高眼压下施行小梁切除术的手术要点及治疗效果。方法:对21例22眼急性闭角型青光眼持续高眼压状态患者,术前、术中用多种方法使眼压逐渐下降后,进行小梁切除术。结果:术后6～12mo,22眼中有17眼术后不用抗青光眼药物,眼压能控制在21mmHg(1mmHg=0.133kPa)以下,4眼加用降眼压药物眼压控制正常;19眼视力有所提高,无严重并发症。结论:对于应用药物治疗不能有效控制眼压的青光眼患者,应当机立断进行手术治疗。只要完善术前准备,术中精心操作,术后精心护理,高眼压下小梁切除术是必要、安全、有效的。     

大麻素WIN55 212-2对牛眼小梁细胞内钙离子及组织型转谷氨酰胺酶表达的影响

<正>青光眼主要与病理性眼压升高有关。眼压升高的重要发病机制是小梁细胞形态和功能发生改变以及细胞外基质增多致房水流出阻力增加。研究表明小梁细胞有平滑肌样功能,而钙离子使小梁细胞收缩,增加房水流出阻力[1]。组织型     

闭角型青光眼合并白内障高眼压下行超声乳化人工晶体植入联合小梁切除术的疗效观察

目的探讨闭角型青光眼合并白内障患者在持续高眼压状态下行白内障超声乳化人工晶体植入联合小梁切除术的方法、治疗时机及疗效。方法对经多种降眼压药物联合应用治疗后仍不能降低眼压在40mmHg以下的闭角型青光眼合并白内障32例（32眼）在高眼压下行白内障超声乳化人工晶体植入联合小梁切除术,并观察其疗效。结果术后随访6个月,所有患者术后视力均有不同程度提高,眼压情况均比术前用降眼压药物的情况下明显下降,眼底、视野无进行性损害。结论闭角型青光眼合并白内障在经积极药物治疗无效时行白内障超声乳化人工晶体植入联合小梁切除术是安全、有效的。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.     

直肠癌下切缘病理组织学分析

目的探讨直肠癌逆向浸润与下切缘的安全距离的关系。方法对36例直肠癌Miles手术和Dixon手术后标本的肿瘤下缘1.0cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查,观察直肠癌逆向浸润或转移的距离。结果36例直肠癌标本距癌肿下缘1.0 cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查均为阴性,结论直肠癌远恻逆向浸润或转移未见超过1.0cm,因此认为保肛手术时切除肿瘤远侧肠管(包括系膜)2.0cm是安全的。