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pharmacotherapy Update: Risperidone in the Treatment of schizophrenia 药物治疗最新进展:利培酮治疗精神分裂症
Pub Date : 2009-09-07 DOI: 10.4137/CMT.S1123
M. Raja
The paper is a review of the clinical use of risperidone, an antipsychotic introduced in the treatment of schizophrenia in 1994. Randomized controlled trials, naturalistic studies and extensive clinical experience have definitively shown strong efficacy and effectiveness of risperidone in the treatment of schizophrenia and other psychotic disorders. On the basis of available evidence, no other antipsychotic drug has shown superior clinical effectiveness in the treatment of psychotic disorders, with the significant exception of clozapine. The wide use of risperidone in the last 15 years has confirmed a favorable safety index. Some features of risperidone render it uniquely useful in the management of psychotic disorders, including a very wide range of dosage, availability in liquid and long-term injectable forms. Finally, the drug is currently available in generic form, at lower cost. However, risperidone presents major limitations. A substantial number of patients with psychotic symptoms do not respond to risperidone, whatever its dose. Most of these patients will need clozapine. For some risperidone treated patients, extrapyramidal side effects remain a serious concern. Weight gain, metabolic syndrome, and hyperprolactinemia related side effects are frequent and may be severe, unacceptable, and even dangerous in some patients.
本文综述了利培酮的临床应用,利培酮是一种1994年引入治疗精神分裂症的抗精神病药物。随机对照试验、自然主义研究和广泛的临床经验明确表明利培酮在治疗精神分裂症和其他精神障碍方面具有很强的疗效和有效性。根据现有证据,除氯氮平外,没有其他抗精神病药物在治疗精神障碍方面表现出更好的临床疗效。近15年来利培酮的广泛应用证实了其良好的安全性指标。利培酮的一些特点使其在精神疾病的治疗中具有独特的作用,包括剂量范围很广,可获得液体和长期注射形式。最后,该药物目前以较低成本的仿制药形式提供。然而,利培酮有很大的局限性。相当数量的有精神病症状的患者对利培酮没有反应,无论其剂量如何。大多数患者需要氯氮平。对于一些利培酮治疗的患者,锥体外系副作用仍然是一个严重的问题。体重增加,代谢综合征和高泌乳素血症相关的副作用是常见的,可能严重的,不可接受的,甚至在一些患者中是危险的。
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引用次数: 4
Palonosetron Hydrochloride in the Treatment of Chemotherapy-Induced Nausea and Vomiting 盐酸帕洛诺司琼治疗化疗引起的恶心呕吐
Pub Date : 2009-09-03 DOI: 10.4137/CMT.S2179
Quan-wang Li, J. Roddy, Michael Berger
Chemotherapy-induced nausea and vomiting (CINV) is among the most unpleasant and stressful aspects of chemotherapy. Poorly controlled nausea and vomiting may have negative impacts on clinical treatment and quality of life. Clinical trials aimed at the prevention of CINV have focused on both acute and delayed phases of CINV. The use of first generation serotonin subtype 3 serotonin (5-HT3) receptor antagonists has significantly improved symptom control in acute CINV. However, they are less effective in controlling delayed CINV. Palonosetron is a second generation 5-HT3 receptor antagonist with high potency, selectivity, prolonged half-life, and a unique allosteric binding mechanism. Previous trials which compared palonosetron to other first generation 5-HT3 antagonists had used the prevention of delayed CINV as a secondary end point. Recent data have demonstrated palonosetron, when used with a corticosteroid, was superior to granisetron in the prevention of delayed CINV as a primary end point. This article will review recently published literature focusing on mechanism of action, metabolism, pharmacokinetics, clinical efficacy, and safety of palonosetron in the treatment of CINV, specifically delayed CINV.
化疗引起的恶心和呕吐(CINV)是化疗中最令人不快和紧张的方面之一。恶心和呕吐控制不佳可能对临床治疗和生活质量产生负面影响。旨在预防CINV的临床试验主要集中在CINV的急性期和延迟期。第一代血清素亚型3血清素(5-HT3)受体拮抗剂的使用显著改善了急性CINV的症状控制。然而,它们在控制迟发性CINV方面效果较差。帕洛诺司琼是第二代5-HT3受体拮抗剂,具有高效、选择性、长半衰期和独特的变构结合机制。先前比较帕洛诺司琼与其他第一代5-HT3拮抗剂的试验将预防迟发性CINV作为次要终点。最近的数据表明,当帕洛诺司琼与皮质类固醇一起使用时,作为主要终点,帕洛诺司琼在预防迟发性CINV方面优于格拉司琼。本文将对帕洛诺司琼治疗CINV,特别是迟发性CINV的作用机制、代谢、药代动力学、临床疗效和安全性进行综述。
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引用次数: 2
A Review of Raltegravir and its Use in HIV-1 Infection 雷替格拉韦及其在HIV-1感染中的应用综述
Pub Date : 2009-09-03 DOI: 10.4137/CMT.S1985
C. Boesecke, L. Gelgor
Raltegravir is the first antiretroviral drug in the class of integrase inhibitors approved for the treatment of human immunodeficiency virus type 1 (HIV-1) in combination with other antiretroviral agents in treatment-experienced adults with evidence of ongoing viral replication and resistance to multiple antiretroviral drugs. Since raltegravir has a different mechanism of action to the currently licensed antiretroviral agents, it is a welcome addition in the treatment of HIV-1. Results from clinical studies to date indicate that raltegravir exhibits potent antiviral activity particularly against HIV-1 strains which exhibit resistance to other classes of antiretroviral drugs. It is well tolerated and has a favorable safety profile. Long-term follow-up data on its resistance profile and on potential interactions with other antiretroviral as well as concomitant medications will ultimately define its future role in the treatment of HIV-1 infection. This review briefly describes the mechanism of action of raltegravir and its pharmacokinetic profile, summarizes efficacy and safety data from recent clinical trials and implications for the use in treatment-naive as well as treatment-experienced patients, depicts raltegravir’s emerging resistance profile, and highlights potential drug-drug interactions.
雷替格拉韦是整合酶抑制剂类别中首个被批准用于治疗人类免疫缺陷病毒1型(HIV-1)的抗逆转录病毒药物,该药物与其他抗逆转录病毒药物联合用于有治疗经验的成年人,这些成年人有证据表明病毒持续复制和对多种抗逆转录病毒药物有耐药性。由于雷替韦韦的作用机制与目前已获许可的抗逆转录病毒药物不同,因此它是HIV-1治疗中一个受欢迎的补充。迄今为止的临床研究结果表明,雷替格拉韦具有强大的抗病毒活性,特别是对对其他抗逆转录病毒药物具有耐药性的HIV-1毒株。它具有良好的耐受性和良好的安全性。关于其耐药情况和与其他抗逆转录病毒药物以及伴随药物的潜在相互作用的长期随访数据将最终确定其在治疗HIV-1感染中的未来作用。本文简要介绍了雷替格拉韦的作用机制及其药代动力学特征,总结了近期临床试验的疗效和安全性数据,以及在初次治疗和有治疗经验的患者中使用的意义,描述了雷替格拉韦的新耐药性特征,并强调了潜在的药物-药物相互作用。
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引用次数: 3
A Re-assessment of the Safety and Efficacy of Interleukin-2 for the Treatment of Renal Cell Carcinoma 白介素-2治疗肾细胞癌安全性和有效性的再评价
Pub Date : 2009-08-31 DOI: 10.4137/CMT.S2037
A. Jarkowski, M. Wong
Interleukin-2 (IL-2) can provide long term durable remissions for patients with advanced or metastatic renal cell carcinoma. The perceived morbidity and the difficulties in delivering this treatment hampered its widespread use in these patients. This review aims to place IL-2 in the modern milieu by reviewing the pharmacology, efficacy and toxicity of this drug. These will be contrasted and compared with the new targeted-agents. The methodology of providing high dose IL-2 treatment, follow-up care and its impact on patient quality of life will be discussed. Importantly, the ability of these agents to provide durable, complete remissions for RCC patients will be placed in context. The goal is to provide the perspective and framework for the reader to balance the important attributes of each of these drugs during the clinical decision making process.
白介素-2 (IL-2)可以为晚期或转移性肾细胞癌患者提供长期持久的缓解。该病的发病率和提供这种治疗的困难阻碍了其在这些患者中的广泛应用。本文旨在通过对IL-2的药理、疗效和毒性的综述,将其置于现代环境中。这些将与新的靶向药物进行对比和比较。本文将讨论提供高剂量IL-2治疗的方法、随访护理及其对患者生活质量的影响。重要的是,这些药物为RCC患者提供持久、完全缓解的能力将被置于背景中。目的是为读者在临床决策过程中平衡每种药物的重要属性提供视角和框架。
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引用次数: 2
Reduction in Risk of Myocardial Infarction, Stroke, and Death from Cardiovascular Causes. Focus on Rampiril 降低心肌梗死、中风和心血管疾病死亡的风险。重点服用Rampiril
Pub Date : 2009-08-31 DOI: 10.4137/CMT.S2095
M. Khazaei, A. Sharifi, S. Golbidi, I. Laher
Several clinical studies demonstrate a beneficial role of angiotensin-converting enzyme (ACE) inhibitors in patients with myocardial infarction, hypertension and diabetes mellitus. This review focuses on the effects of ramipril, a weak inhibitor of ACE that is rapidly hydrolyzed to ramiprilat, an active metabolite. The Heart Outcome Prevention Evaluation (HOPE) study evaluated the effects of ramipril in patients with a high risk for cardiovascular events without pre-existing left ventricular dysfunction or heart failure. In this review, we summarized the effects of ramipril on myocardial infarction, death, diabetes mellitus, and stroke.
一些临床研究表明血管紧张素转换酶(ACE)抑制剂在心肌梗死、高血压和糖尿病患者中的有益作用。这篇综述的重点是雷米普利的作用,雷米普利是一种ACE的弱抑制剂,可以迅速水解成雷米普利特,一种活性代谢物。心脏结局预防评估(HOPE)研究评估了雷米普利在没有左心室功能障碍或心力衰竭的高危心血管事件患者中的作用。在这篇综述中,我们总结了雷米普利对心肌梗死、死亡、糖尿病和中风的影响。
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引用次数: 0
cardiotoxicity of Oral Methadone as an Analgesic— recommendations for safe Use 口服美沙酮作为镇痛药的心脏毒性——安全使用的建议
Pub Date : 2009-08-31 DOI: 10.4137/CMT.S3041
D. Guay
Once used only as third-line therapy in the management of chronic pain states, methadone is now being used as first- and second-line therapy. Most risks and the stigma associated with methadone use have been known for years. Only over the past decade or so have the unique pharmacokinetic-pharmacodynamic properties and methods for conversion from other opioids to methadone been established. Pertinent English-language literature was obtained from MEDLINE/PUBMED and EMBASE searches (1966–June 2009). This paper provides an overview of the cardiotoxicity of oral methadone, with an emphasis on its use as an analgesic. Cardiotoxicity during its use in the maintenance of opioid addiction has also been reviewed due to the wealth of epidemiologic, risk factor, and correlative analytic data contained therein. A series of recommendations are provided to improve the cardiac safety profile of oral methadone used for analgesia. In addition, there is a discussion of settings and patient types which may impact upon these recommendations.
美沙酮曾经仅作为治疗慢性疼痛状态的三线治疗,现在已被用作一线和二线治疗。与使用美沙酮相关的大多数风险和耻辱感多年来一直为人所知。仅在过去十年左右,才建立了从其他阿片类药物转化为美沙酮的独特药代动力学-药效学性质和方法。相关英文文献从MEDLINE/PUBMED和EMBASE检索(1966 - 2009年6月)中获得。本文概述了口服美沙酮的心脏毒性,重点介绍了其作为镇痛药的用途。由于其中包含了大量的流行病学、危险因素和相关分析数据,因此对阿片类药物成瘾维持过程中的心脏毒性也进行了综述。本文提出了一系列建议,以改善口服美沙酮用于镇痛的心脏安全性。此外,还讨论了可能影响这些建议的环境和患者类型。
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引用次数: 5
exudative Age-Related Macular Degeneration: current Therapies and potential Treatments 渗出性年龄相关性黄斑变性:目前的治疗方法和潜在的治疗方法
Pub Date : 2009-08-27 DOI: 10.4137/CMT.S2225
P. Quiram, Yahui Song
Strategies for preventing vision loss in patients with neovascular age-related macular degeneration (ARMD) have evolved over the past decade. Whereas earlier treatments were based on thermal destruction of choroidal neovascularization (CNV), new therapies rely on targeted pharmacologic approaches to reduce the harmful effects of CNV treatment. For the first time in the history of neovascular ARMD treatment, anti-VEGF therapies have consistently improved visual acuity in a subset of patients. Clinical trials continue to investigate the optimal dosing strategies and combination therapies to better refine the treatment of this chronic and debilitating disease.
在过去的十年中,预防新生血管性年龄相关性黄斑变性(ARMD)患者视力丧失的策略已经发生了变化。早期的治疗是基于脉络膜新生血管(CNV)的热破坏,而新的治疗方法依赖于靶向药物方法来减少脉络膜新生血管治疗的有害影响。在新血管性ARMD治疗史上,抗vegf疗法首次持续改善了一部分患者的视力。临床试验继续研究最佳剂量策略和联合疗法,以更好地改善这种慢性和衰弱性疾病的治疗。
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引用次数: 0
Safety and Efficacy of Doxycycline 多西环素的安全性和有效性
Pub Date : 2009-08-27 DOI: 10.4137/CMT.S2860
P. Leggat
Doxycycline has remained one of the most commonly used and inexpensive of the broad-spectrum antibiotic drugs currently in use. It has a variety of applications to common respiratory and genitourinary tract infections, but also amongst atypical infections, such as malaria, rickettsial infections, leptospirosis, brucellosis and some of the bioterrorist agents, including anthrax. It is known that the tetracycline class of antibiotics does have a range of side-effects, such as photosensitivity and gastrointestinal side effects, and noteworthy contraindications, especially amongst pregnant women and young children.
强力霉素仍然是目前使用的最常用和最便宜的广谱抗生素药物之一。它有多种应用于常见的呼吸道和泌尿生殖道感染,但也适用于非典型感染,如疟疾、立克次体感染、钩端螺旋体病、布鲁氏菌病和一些生物恐怖剂,包括炭疽。众所周知,四环素类抗生素确实有一系列副作用,如光敏性和胃肠道副作用,以及值得注意的禁忌症,特别是孕妇和幼儿。
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引用次数: 5
Safety and Efficacy of Eplerenone in the Management of Essential Hypertension 依普利酮治疗原发性高血压的安全性和有效性
Pub Date : 2009-08-25 DOI: 10.4137/CMT.S2211
F. McManus, J. Connell
Suppression of the Renin-Angiotensin-Aldosterone system (RAAS) is an established intervention in the management of cardiovascular disease. Large, randomized controlled trials have provided a sound evidence base for the use of mineralocorticoid receptor antagonists to block the end product of the RAAS in the treatment of heart failure. However, the place for mineralocorticoid blockade in the treatment of hypertension is less well defined and lacking a strong evidence base. The main indication for the use of this strategy in hypertension is as a third line agent in the treatment of refractory hypertension. The most widely used mineralocorticoid receptor antagonist, spironolactone, is associated with dose related sexual side effects, limiting its use in clinical practice. Eplerenone, the selective mineralocorticoid receptor antagonist, is a promising cardiovascular drug licensed for the treatment of heart failure in Europe and heart failure and hypertension in the USA. It effectively blocks the mineralocorticoid receptor without the unpleasant sexual side effect profile of spironolactone. We review the use of eplerenone, a selective mineralocorticoid receptor antagonist in the treatment of hypertension; discuss its mechanism of action, safety profile as well as its current place in therapy.
抑制肾素-血管紧张素-醛固酮系统(RAAS)是心血管疾病管理的既定干预措施。大型随机对照试验为使用矿皮质激素受体拮抗剂阻断RAAS治疗心力衰竭的最终产物提供了可靠的证据基础。然而,矿皮质激素阻断在高血压治疗中的地位尚不明确,缺乏强有力的证据基础。在高血压中使用这种策略的主要适应症是作为治疗难治性高血压的三线药物。最广泛使用的矿物皮质激素受体拮抗剂螺内酯与剂量相关的性副作用有关,限制了其在临床实践中的应用。Eplerenone是一种选择性矿皮质激素受体拮抗剂,是一种很有前途的心血管药物,在欧洲被批准用于治疗心力衰竭和美国的心力衰竭和高血压。它有效地阻断了矿物皮质激素受体,而没有螺内酯令人不快的性副作用。我们回顾了选择性矿皮质激素受体拮抗剂eplerenone在高血压治疗中的应用;讨论其作用机制、安全性以及目前在治疗中的地位。
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引用次数: 1
Antipsychotic Drug Treatment for Patients with Schizophrenia: Theoretical Background, Clinical Considerations and Patient Preferences 精神分裂症患者的抗精神病药物治疗:理论背景、临床考虑和患者偏好
Pub Date : 2009-08-17 DOI: 10.4137/CMT.S2175
R. Nielsen, J. Nielsen
The cornerstone in treatment of psychosis is antipsychotic drugs. Treatment options have increased over the years; newer antipsychotic drugs with a proposed increased efficacy regarding negative and cognitive symptoms, but also a shift in side-effects from neurological side-effects to metabolic side-effects have arisen as the new challenge. The basis of successful pharmacological treatment is a fundamental understanding of the mechanisms of action, the desired effects and side-effects of antipsychotic drugs, a good relationship with the patient and a thorough monitoring of the patient before and during treatment. The clinically relevant aspects of antipsychotic drug treatment are reviewed; mechanism of antipsychotic drug action, clinical considerations in treatment, switching antipsychotic drugs, polypharmacy, safety and patient preference.
治疗精神病的基石是抗精神病药物。多年来,治疗方案有所增加;新的抗精神病药物对阴性症状和认知症状的疗效有所提高,但副作用也从神经系统副作用转变为代谢副作用,这是新的挑战。成功的药物治疗的基础是对抗精神病药物的作用机制、预期效果和副作用的基本理解,与患者的良好关系以及在治疗前和治疗期间对患者的彻底监测。综述了抗精神病药物治疗的临床相关方面;抗精神病药物的作用机制,治疗中的临床考虑,抗精神病药物的转换,多种药物,安全性和患者偏好。
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引用次数: 9
期刊
Clinical Medicine and Therapeutics
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