Corticosteroid agents in renal disease

Corticosteroid agents have a major role in the treatment of several renal disorders which have an immune basis. They remain the treatment of choice for minimal-change glomerulonephritis, inducing remission in over 90% of patients. The role of corticosteroid therapy in patients with membranous glomerulonephritis remains controversial, although an extensive controlled trial indicated benefit from a two-month course of alternate-day therapy. Intravenously-administered methylprednisolone has been shown to benefit rapidly progressive crescentic glomerulonephritis; the benefit is probably comparable to that which is obtained with immunosuppression and plasma exchange. Corticosteroid therapy has improved dramatically the prognosis of glomerulonephritis that is associated with systemic lupus erythematosus and the various forms of vasculitis (excluding Wegener's granulomatosis), although the concomitant use of immunosuppressive therapy in these disorders reduces the required doses of corticosteroid drugs. For the last 20 years prednisolone and azathioprine have been standard therapy to prevent renal allograft rejection. However, corticosteroid agents are used currently in much lower doses or have been replaced by cyclosporin A.     

Essential hypertension--investigations and management

When one is faced with the problem of essential hypertension it is prudent to pay attention to lifestyle factors, especially alcohol, smoking and obesity. Modification of salt intake in the diet is a simple measure. Drug therapy will need to be long-term therapy and ease of treatment is important, which means that drugs given once a day or at most twice a day should be used. Diuretics and beta-blockers are inexpensive and well proven but have many side-effects. Newer agents may have fewer side-effects but are more expensive. The choice will be an individual one.     

具有抗肿瘤免疫治疗作用的铂类药物研究进展

经典铂类药物是一类潜在的免疫调节剂,通过诱导免疫原性细胞死亡(ICD)来参与肿瘤免疫调节。因而可将铂类药物分子与免疫治疗药物分子或其药效团进行拼合或融合,提高协同抗肿瘤疗效。铂(Ⅱ)药物是临床化疗最常见药物,由于其副作用和耐药性等缺点,使其临床应用受限。铂(Ⅳ)配合物具有动力学惰性和优于铂(Ⅱ)配合物的药理作用机制受到广泛关注和研究。本文旨在总结近年来发表的具有免疫调节功能的抗肿瘤铂配合物,通过化疗协同免疫疗法提高抗肿瘤疗效,为具有免疫功能的铂类药物的进一步研发和未来临床应用提供依据。

     

What has happened to the new antidepressant drugs?

Depression is a widespread and serious disease for which a multiplicity of antidepressant drugs is available for treatment. Although these agents are numerous, there is little to distinguish among them except for their different side-effects. This article reviews the antidepressant drugs that currently are available in Australia, the antidepressant drugs that are used in other countries and some antidepressant drugs that are likely to become available internationally in the next few years.     

载阿霉素靶向制剂治疗肝癌研究现状

药物缺乏选择性是目前肿瘤化疗的主要问题,为提高药物疗效,减少不良反应,人们开始对靶向载药制剂进行探索。靶向药物制剂最突出的优点是靶向性明显,能在靶位保持有效药物浓度和时间。近些年越来越多的靶向制剂用于肝癌的靶向治疗。现对抗肿瘤药物阿霉素靶向制剂治疗肝癌的研究现状进行综述,并指出其治疗前景及存在的若干问题。     

短程化疗期间抗结核药物副作用观察

目的 探讨短程化疗期间抗结核药物的副作用。方法 对2002—2003年在我结核门诊确诊并应用抗结核药物治疗的142例患者进行回顾性分析。结果 短程化疗期间使用抗结核药物共有35例(24．6％)发生副作用。其中肝损害及胃肠道症状发生率较高，多发生在抗结核治疗2周内。轻者不需要改变治疗方案而加用保肝等治疗，重者需停用抗结核药物并加用保肝等治疗，35例患者副作用均得到不同程度的缓解，并最终完成化疗。结论 掌握抗结核药物副作用产生的种类、频率、时间和防治对策，不仅能够及时、有效的判断是何药物引起的副作用。并调整抗结核治疗方案等，确保抗结核治疗顺利完成，而且还可及时发现、处理这些严重副作用，挽救患者生命。     

全反式维甲酸治疗急性甲幼粒细胞白血病中的致命性副作用

用全反式维甲酸（ＡＴＲＡ）治疗８２便急性早幼粒细胞白血病（ＡＰＬ）,其中３５例（４２．７％）出现白细胞增多症,２２例（２６．８％）出现致命性副作用。后者包括维甲酸综合征１５例,颅内出血７例。提示：在ＡＴＲＡ治疗ＡＰＬ过程中,白细胞增多是致命性副作用发生的重要危险因素;ＡＴＲＡ与小剂量三尖杉酯碱相结合,可降低因白细胞增多导致颅内出血的发生率;肾上腺皮质激素显著降低维甲酸综合征的死亡率。     

Medical therapy for systemic lupus erythematosus

The many clinical manifestations of systemic lupus erythematosus (SLE) result in the involvement of many specialties of medicine in its treatment. An understanding of the indications, potential side-effects, and toxicity monitoring required of common agents used as medical therapy in SLE disease management is important for all providers who care for lupus patients. Pharmacological therapy is based on the type and severity of clinical manifestation and involves four primary classes of drugs: non-steroidal antiinflammatory drugs, antimalarials, corticosteroids, and immunosuppressives/cytoxics.     

奥马珠单抗在嗜酸细胞性肉芽肿性多血管炎中应用的研究进展

嗜酸细胞性肉芽肿性多血管炎(eosinophilia granulomatosis polyangiitis,EGPA)是一种临床少见但可累及全身多系统的自身免疫性疾病。当前诱导EGPA缓解和预防复发的药物主要是糖皮质激素和免疫抑制剂,患者在治疗过程中常出现复发和皮质类固醇依赖相关的问题,因此亟需新的治疗方法。奥马珠单抗(omalizumab,OMA)是一种人源化抗IgE单克隆抗体,在我国于2017年8月获批用于中重度变应性哮喘的治疗,已有超过3万例哮喘患者接受治疗,应用前景广阔。近年来OMA在EGPA中的应用研究日益增多,本文对近年来国内外使用OMA治疗EGPA的临床研究包括潜在药理机制、临床获益及不良反应等进行综述,为奥马珠单抗的相关临床治疗研究提供参考。     

凝血因子Ⅹa抑制剂专利技术分析

抗凝血药物被广泛用于血栓栓塞性疾病的预防和治疗。近年来,凝血因子Ⅹa抑制剂成为新型抗凝血药物的研发热点,但目前上市的抗凝药物仍存在长期使用会增加出血风险等不良反应。本文通过文献检索,对凝血因子Ⅹa抑制剂相关专利申请状况进行了分析,以百时美施贵宝公司和广东东阳光药业有限公司作为该领域重点企业代表,对其专利申请发展路线进行梳理,总结凝血因子Ⅹa抑制剂化合物的改造位点和研发方向,以期能够为国内研发机构和相关企业对凝血因子Ⅹa的新药研发、专利保护以及知识产权布局提供有益的参考和建议。     

Should we treat herpes zoster with corticosteroid agents?

Herpes zoster is a common disease which is frequently followed by severe long-term pain--post-herpetic neuralgia. The arrival of new antiviral agents, not yet widely available, may lead to the neglect of the older, effective and inexpensive method of treatment with systemic corticosteroid agents. Evidence for the value of corticosteroid therapy is strong, while published data discouraging its use is weak. Consequently, the administration of these agents should be the standard treatment for painful acute zoster.     

糖尿病性黄斑水肿的药物治疗现状

糖尿病性黄斑水肿及增殖型糖尿病性视网膜病变是导致糖尿病性视网膜病变患者视功能损害的两大主要原因,其中糖尿病性黄斑水肿是非增殖型糖尿病病变视功能损害的主要原因。目前糖尿病性黄斑水肿的治疗包括眼底激光、药物及玻璃体手术。血管内皮生长因子及炎症因素在糖尿病性黄斑水肿发生发展过程中均起非常重要作用,且炎症因子及血管内皮生长因子相互刺激分泌,促进糖尿病性黄斑水肿的形成,因此药物主要包括抗血管内皮生长因子药物及皮质类固醇类药物。近年来,随着对抗血管内皮生长因子药物及皮质类固醇类药物治疗研究的不断深入,现就糖尿病性黄斑水肿的药物治疗现状作一综述。     

Vasodilator drugs in the treatment of hypertension

Vasodilator drugs counteract the major haemodynamic abnormality of hypertension, namely, arteriolar constriction. As a group, they tend to cause tachycardia and fluid retention, but these side-effects are variable within the group. Vasodilator drugs are effective in the treatment of the whole range of hypertensive diseases, from severe refractory hypertension to mild hypertension. With increasing recognition of the necessity of treatment in mild asymptomatic hypertension, those vasodilator drugs which can be used on their own, such as prazosin and calcium antagonists, are attractive as initial therapy, because they do not have adverse effects on the levels of atherogenic lipids and other risk factors for vascular disease. The major current use of vasodilator drugs in combination with a thiazide and a beta-adrenoreceptor-blocking drug is in the treatment of moderate-to-severe hypertension.     

小儿重症肌无力综合治疗及非特异性预防

本文对37例重症肌无力患儿采用短期、间歇激素疗法,小剂量抗胆硷脂酶药物,人血丙种球蛋白以及辅助药物等综合治疗措施取得了满意结果,而且副作用少。症状痊愈后以人血丙种球旦白作非特异性免疫预防,随访2年无复发。通过临床观察发现综合治疗能减少各种药物的用量,缩短治疗时间,最大限度地发挥药物的药理作用。以人血丙种球蛋白作非特异性免疫预防能调节患儿的体液和细胞免疫功能,抑制自身免疫抗体产生。从而消除诱发因素。     

鼓室内注射甲泼尼龙治疗难治性突发性感音神经性聋的疗效观察

目的观察鼓室内注射甲泼尼龙对难治性突发性耳聋的治疗效果,探索常规治疗无效的突发性聋的挽救治疗手段。方法对47例（47耳）常规治疗无效的突聋患者经鼓膜穿刺向鼓室内注入甲泼尼龙混悬液约0．5m1（20邛喀）,使药液进入圆窗龛1）．L／3d,共4次。在治疗开始前和治疗结束后3d,分别测试受治疗耳的纯音听阈,比较语言频率纯音听阈均值（era）,下降15dB HL以上为有效。结果47例经治患者14例有效,33例无效,有效率为29．8％。治疗前PTA为（67．59±16．57）dBHL,治疗后为（53．65±18．75）dBHL,治疗后比治疗前明显降低（P=0．000）。治疗时间短、不伴有眩晕的患者治疗效果好;听力下降的程度和听力下降的类型以及是否伴有耳呜、糖尿病对治疗效果无明显影响。结论鼓室内注射甲泼尼龙可作为常规治疗无效的突聋患者的挽救治疗手段,亦可作为避免全身大剂量使用激素的副作用的常规治疗手段之一。     

Drug interactions with oral contraceptive preparations

Oral contraceptives (OCs) should be used with additional caution in combination with other drugs in certain disease states. This discussion focuses on only those interactions which are due to identifiable pharmacokinetic processes. Pharmacological interactions between OCs and other compounds may be of 2 kinds: drugs may impair the effectiveness of the OCs to cause breakthrough bleeding or to allow pregnancy to occur; and OCs may interfere with the metabolism of other componds. In general, interactions of the 1st kind are due to interference with the absorption, metabolism, or excretion of estrogens, and interactions of the 2nd kind are due to competition for metabolic pathways. It is difficult to obtain estimates of the frequency of interactions, but it seems likely that, as low-dose preparations become more widely used, interactions of the 1st type will become more common and those of the 2nd type less common. Although it is probably only those women with low plasma hormone concentrations who are at risk that other drugs may interfere with contraceptive efficacy, and women with high plasma concentrations of estrogen who are at risk of side-effects and that OCs may interfere with other drugs, there is no way of detecting women in either category. Consequently, it is safer for the present to assuume that all women who take OCs might be at risk of some form of interaction. Significant drug interactions in which contraceptive efficacy is reduced are more likely to occur in the early part of the cycle when circulating hormone concentrations are of critical importance. It is well known that infective diarrhea can induce OC failure by increasing gastrointestinal motility and reducing hormone absorption. Thus, any drug which reduces gut transit time and causes diarrhea is potentially likely to reduce circulating concentrations of OCs. The sulphation of ethinl-estradiol in the gastrointestinal wall has been shown to be a site of interaction for the enhancement of the activity of OCs. Ascorbic acid also undergoes sulphate conjugation in the gut wall and acts as a competitive inhibitor for sulphation of estrogens. The most clinically significant group of interactions occurs with other drugs that are metabolized by the same hepatic microsomal pathways as is estrogen. Most of the anticonvulsant drugs are inducers of microsomal enzymes. Rifampicin is known to be a potent inducer of hepatic microsomal enzymes and has been shown to increase the rate of metabolism of both estrogeens and progestogens. A recent report has suggested that the antifugal drug griseofulvin may cause a clinically important interaction with OCs. There are numerous well documented clinical reports of women who have taken OCs without missing a dose who have become pregnant while taking a variety of antibiotic agents such as ampicllin and tetracycline. Estrogens are inhibitors of hepatic microsomal enzymes. In this way they may show the metabolsim of other drugs, thus increasing their plasma and tissue concentrations and increasing the risk of side-effects. These interactions might be expected to become less common as the concentration of estrogen in OCS decreases.     

共价修饰类药物的研究进展

共价修饰类药物通过共价键与靶标结合而发挥其药理作用,由于其可能带来脱靶效应及不良反应,长期以来在药物设计领域尽可能被避免。随着对已上市的重磅级共价药物结合模式的深入研究,越来越多共价修饰类药物重新得到研发人员的重视,寻找高选择性、低不良反应的共价修饰类药物已成为目前研究的热点。本文对一些共价修饰类药物进行分类,对其与靶标结合的模式以及近年来共价修饰类药物设计的新策略进行综述,为共价药物的合理药物设计提供参考。     

Anti-epileptic drugs

As a sizeable population is affected by epilepsy, so its effective management is a matter of concern. Newer anti-epileptic drugs are now in use, aimed at controls of seizure with fewer side-effects over and above the conventional anti-epileptic drugs. The anti-epileptic drugs can be divided in two groups--conventional anti-epileptic drugs and newer anti-epileptic drugs. The drugs which fall in the first group are--phenytoin, phenobaibitone, valproic acid, carbamazepine, ethosuximide and clonazepam. The second group of drugs are--lamotrigine, clobazam, oxcarbazepine, topiramate and gabapentin. The pharmacology of the drugs are described in a nutshell in this article.     

系统性红斑狼疮血液学异常及治疗后的变化

目的:探讨系统性红斑狼疮(SLE)病人血液学异常改变及临床特征。方法:对62例SLE患者血液学资料及应用糖皮质激素、免疫抑制剂治疗的效果进行回顾性分析。结果:血象异常者为53例,占82.5%,以二系以上减少为主,46例进行了骨髓象检查,发现骨髓增生活跃或明显活跃40例,增生减低6例,表现为增生性贫血或特发性血小板减少性骨髓象,47例诊断后做Coombs试验,9例阳性,血细胞减少者,用糖皮质激素及免疫抑制剂治疗,血象均有升高。结论:血液系统是SLE易损器官,SLE病人血液学异常较常见,其特点是血液学改变多样性,缺乏特异性,以二系以上减少常见,骨髓象表现增生活跃为主,对糖皮质激素及免疫抑制治疗有效。     

Primary glaucomas: current concepts and management

Glaucoma is a leading cause of blindness. Delay in diagnosis of open angle glaucoma (OAG) results from lack of symptoms. In angle closure glaucoma (ACG) there is often neglect of symptoms. Creating awareness about the disease and screening the high risk groups would reduce the burden of irreversible blindness due to glaucoma. Adequate therapy in the form of drops, lasers and surgery is available. Close interaction with the physician is important as many topical antiglaucoma medications have adverse systemic side-effects and many drugs used for systemic diseases raise the intra-ocular pressure (IOP). All drugs currently available for glaucoma lower IOP but new drugs for neuroprotection may change the future management strategies. While drugs and surgery are the mainstay for OAG, laser iridotomy is the definitive treatment for ACG.