吡喹酮致药疹三例

吡喹酮是近年来治疗吸虫、绦虫的新型药物,该药疗效高、疗程短、毒副作用轻。近几年我们用该药治了近2000例华支睾吸虫病,有3例发生了药疹。现报告如下。例1 魏某,男,54岁。1987—06来诊,40天前曾食用过生鱼,华支睾虫成虫抗原皮内试验(+),嗜酸粒细胞计数1.9×10~9/L,便检发现华支睾吸虫卵,诊断为急性华支睾吸虫病。应用吡喹酮治疗,总剂量为150mg/kg,一次5片(每片200mg)3次/d,3天疗法,服用3次后两下肢发痒,有微热(37.4℃),全身出现散在性红色皮疹,以小腿部位为多。停药1天后皮疹消     

吡喹酮、六氯对二甲苯及两药联合应用治疗华枝睾吸虫病的临床观察

应用吡喹酮、六氯对二甲苯及两药较小剂量联合疗法治疗华枝睾吸虫病94例,发现吡喹酮80mg/kg、120mg/kg二日疗法,六氯对二甲苯500mg/kg五日疗法以及两药较小剂量的联合疗法疗效都较满意,远期阴转率85％以上。哟喹酮60mg/kg二日疗法疗效较差,远期阴转率仅58.33％。副作用以单独应用六氯对二甲苯组比较明显;联合疗法组的尿检异常发生率较高,达48.3％。认为对轻度华枝睾吸虫病感染患者,应用吡喹酮总剂量80mg/kg二日疗法比较恰当,六氯对二甲苯只能作为次选药物。     

吡喹酮对大鼠体内不同发育时期华支睾吸虫的实验治疗

近年来国内外应用吡喹酮治疗华支睾吸虫病取得了显著疗效。为进一步探讨该药对体内不同发育时期华支睾吸虫的作用及其作用机理,本文进行了实验研究。实验动物为体重200～330g的♀性大鼠。随机分为对照组和治疗组,每鼠经口接种30个华支睾吸虫囊蚴。所用吡喹酮系南京制药厂供给,每片含吡喹酮200mg。治疗时将药加     

以EPG选择吡喹酮治疗华支睾吸虫病剂量的观察

以EPG选择吡喹酮治疗华支睾吸虫病的剂量，并与以体重选择吡喹酮剂量的疗效相比较，结果显示，二者疗效相同，而前者应用剂量小，尤以轻，中度感染更为明显，我们认为，以EPG推算虫荷，以量化的虫荷指标计算吡喹酮剂量，符合吡喹酮药物代谢动力学及杀虫特点，符合大剂量，短疗程，毒性小的用药原则，具有合理性及可行性，因此量化的虫荷指标与较精确的药物剂量是治疗的关键。     

吡喹酮治疗动物华支睾吸虫病和肺吸虫病的实验观察

吡喹酮(Praziquantel)对人、畜体内大多数绦虫的成虫和幼虫均有驱杀作用,对治疗人体的三种血吸虫病亦有效。Davis又引述吡喹酮对动物华支睾吸虫病和肺吸虫病有效。     

647例华支睾吸虫病患者的病例特征及其对不同驱虫药物的疗效比较

目的:比较华支睾吸虫病患者的病例特征及其对不同驱虫药物的疗效。方法:选取2014年9月—2017年9月期间收治的华支睾吸虫病患者734例次病历资料,分析其病例特征即患者的性别、年龄和住院情况,以及其并发症的发生情况,以及不同驱虫药物的用药合理性、不良反应的发生率以及治疗后虫卵转阴率差异。结果:734例次华支睾吸虫病住院患者的确诊病历涉及647例(以40～69岁中老年人为主),其中男性占72.49%(469/647)高于女性为27.51%(178/647);有39.78%患者采用驱虫药物阿苯达唑片或吡喹酮片治疗,驱虫药物的用药合理率为80.14%,用药后粪检虫卵复检率为27.05%。结论:对华支睾吸虫感染,首先应从预防开始对其加深华支睾吸虫病的认识,临床药师应为临床提供专业的用药指导,从而确保华支睾吸虫病的有效治疗。     

5例重度感染华支睾吸虫患者的误诊分析

自1997年来，我教研室陆续发现5例重度感染华支睾吸虫的患者，其感染虫体的数量均约在500条以上。最高的1例患者体内感染了9974条华支睾吸虫，是目前国内外文献中活体计数最高者[1]。这5例患者均因被误诊而行胆囊切除术，并在术中或术后进行T型管引流时发现虫体。现将5例重度感染华支睾吸虫患者的误诊病例报道如下。1临床资料5例华支睾吸虫患者，男3例，女2例。年龄31~45岁。5例附表5例重度感染华支睾吸虫患者的一般情况2驱虫方法与结果术后用吡喹酮(Praziquantel)治疗，剂量16.6mg/kg,tid，3d一疗程。自服药当日起，从T型管收集引流虫体…     

吡喹酮衍生物治疗日本血吸虫病的实验研究

吡喹酮衍生物′S77078、S78015、S79046和21542对小鼠血吸虫均有明显的杀死作用。S78015、S79046和21542的剂量为200～400mg/kg/d,疗程2天,对病鼠的减虫率分别为22.5～53.9%、27.6%和32.8～66.9%;S77078 200～600mg/kg/d,疗程1～2天的减虫率为60.1～97.3%,与吡喹酮的83.6～95.6%的相近似。当S77078每天总剂量为30～60mg/Kg、疗程1～2天,对病兔和病犬的减虫率分别为18.3～40.8%和53.7～80.4%,均较吡喹酮的30～60mg/kg×1天的97.1～97.3%和89.7～98.5%的为低。     

单次口服三苯双脒与不同剂量吡喹酮治疗华支睾吸虫的疗效及安全性研究

目的 探讨单次口服三苯双脒与不同剂量吡喹酮治疗华支睾吸虫的疗效性及安全性。方法 回顾性分析2020年1月1日～2021年6月31日共收治100例罹患华支睾吸虫病患者的资料,根据患者所使用药物的不同分为三苯双脒组(A组)、吡喹酮25 mg/kg组(B组)、吡喹酮50 mg/kg(C组),其中A组、B组分别有33例患者,C组有34例患者,分析各组华支睾吸虫虫卵阴转率,轻度感染、中度感染、重度感染虫卵阴转率,不良反应发生率,合并其他肠道寄生线虫的阴转情况。结果 A组虫卵阴转率为93.94%,B组虫卵阴转率为66.67%,C组虫卵阴转率为88.24%,A组与C组虫卵阴转率明显高于B组,差异具有统计学意义(P <0.05);A组、C组患者轻度感染、中度感染阴转率明显高于B组,A组重度感染阴转率明显高于B组、C组,差异具有统计学意义(P <0.05);A组不良反应发生率为24.24%,明显低于B组、C组的48.48%、67.65%,差异具有统计学意义(P <0.05);A组、B组、C组患者均有合并感染其他肠道寄生线虫情况,治疗后,A组、C组肠道寄生线虫阴转情况优于B组(χ     

吡喹酮治疗囊虫病61例

吡喹酮治疗猪囊尾蚴病61例,采用总剂量120mg-140mg/kg。全疗程不超过6d。治程中药物反应轻微,仅个别出现颅内高压症;治后0.5-1yr,有效率67％。     

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.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.