氟比洛芬酯注射液对老年癌性疼痛的疗效分析

目的观察氟比洛芬酯脂微球注射液对老年癌性疼痛的疗效和毒副反应。方法对20例未用阿片类药物的老年患者出现癌性疼痛给予氟比洛芬酯脂微球注射液50～100mg/d静脉推注,应用1周以上,评价其疗效以及不良反应。结果氟比洛芬酯脂微球注射液治疗癌性疼痛的有效率（CR＋PR）为70%,生活舒适感得到不同程度的改善,不良反应发生率低,程度轻,未见消化道出血、便秘、尿潴留、嗜睡、返酸、恶心呕吐及呼吸抑制等。结论氟比洛芬酯脂微球注射液治疗老年癌性疼痛效果较理想,不良反应少。     

氟比洛芬酯脂微球载体制剂与注射用酮洛芬对照治疗术后及癌性疼痛

目的:观察氟比洛芬酯与酮洛芬对照治疗术后及癌性疼痛患者的有效性.方法:日本36家医院共入选腹部术后患者224例,癌性疼痛患者163例,随机分为氟比洛芬酯组192例与酮洛芬组195例,分别用氟比洛芬酯与酮洛芬安慰剂和酮洛芬与氟比洛芬酯安慰剂.氟比洛芬酯及其安慰剂5mL静脉内注射,酮洛芬及其安慰剂每瓶用2.5mL溶液溶解臀部肌内注射.结果:可评价病例氟比洛芬酯组对术后疼痛111例患者改善率为73.9%,高于酮洛芬组(n=109)的66.1%,但2组差异无显著性(P>0.05);药效持续时间氟比洛芬酯组比酮洛芬组延长(P<0.05).氟比洛芬酯组癌性疼痛(n=77)改善率为77%,高于酮洛芬组(n=81)的59.3% (P>0.05),药效持续时间氟比洛芬酯组比酮洛芬组延长(P<0.05).结论:在治疗术后疼痛和癌性疼痛时,氟比洛芬酯的疗效与酮洛芬相近,但镇痛时间明显延长.     

氟比洛芬酯对手术致痛大鼠行为学的影响

目的观察氟比洛芬酯对手术致痛大鼠行为学的影响。 方法将48只SD大鼠随机分为6组。对照1（D1）组大鼠单纯吸入异氟醚麻醉,不进行手术,其余5组（D2、K1～K4组）以异氟醚吸入使大鼠麻醉,按BRENNAN 法手术,建立大鼠手术切口疼痛模型。20 min后经尾静脉给药。D1组、D2组大鼠给予0.9%氯化钠注射液,K1～K4组分别给予氟比洛芬酯注射液2,4,8,16 mg·kg 1。待大鼠手术清醒及每组给药后1 h,进行累积疼痛评分,观察给药后反应。结果氟比洛芬酯可剂量依赖性地降低切口疼痛模型大鼠的累积疼痛评分(P＜0.05)。 结论氟比洛芬酯可抑制外科手术的疼痛反应,并呈一定的剂量依赖性。     

氟比洛芬酯脂微球载体注射液治疗中度术后疼痛的Ⅱ期临床试验

目的:考察氟比洛芬酯脂微球载体注射液对中度术后疼痛患者的止痛效果及安全性.方法:采用多中心随机双盲对照试验设计.试验药和对照药分别为氟比洛芬酯脂微球载体注射液和安慰剂.选骨科、普通外科和妇科术后中度疼痛(疼痛强度4～6)的受试者197例,试验组99例,对照组98例.试验组与对照组均单次给药,缓慢静脉注射1支(5mL).用药前及用药后6h内评价疼痛强度(PI)、疼痛强度差(PID)、疼痛缓解率(PAR)和有效率.结果:试验组单次用药后6h的PI,PID和PAR分别为1.3,4.1,98.0%,显效率为89.9%;对照组则分别为3.3,1.7,43.9%,25.5%,2组比较差异有显著性(P<0.01),氟比洛芬酯脂微球载体的镇痛效果明显优于安慰剂.结论:氟比洛芬酯脂微球载体注射液是安全有效的中等强度靶向镇痛药.     

氟比洛芬酯注射液的药理作用探讨

氟比洛芬酯注射液是氟比洛芬酯微球制剂中的一种,适应症通常为术后或者癌症的镇痛,可有效缓解患者的疼痛程度,临床为为患者选择注射的方式给药可显著减轻药物对人体产生的副作用。本次研究中笔者重点探讨氟比洛芬酯注射液的药理作用,同时概述其在临床上的具体运用。     

帕瑞昔布钠与氟比洛芬酯用于骨折术后镇痛效果的评估

目的 评估帕瑞昔布钠和氟比洛芬酯在骨折术后的临床镇痛效果.方法 选择2019年10月至2020年6月安庆市第二人民医院骨折术后病人,分为氟比洛芬酯组和帕瑞昔布钠组.氟比洛芬酯组采用50 mg氟比洛芬酯注射液,帕瑞昔布钠组采用40 mg帕瑞昔布钠注射液,均静脉滴注,一日1～2次.采用视觉模拟评分法(VAS)对病人进行疼痛评分,比较两组病人术后VSA评分、不良反应发生及药物治疗费用.结果 氟比洛芬酯组45例,帕瑞昔布钠组55例.氟比洛芬酯组镇痛药物治疗(3.80±1.28)d,较帕瑞昔布钠组(4.56±2.04)d明显缩短(P=0.026).治疗12 h氟比洛芬酯组VAS评分(4.20±0.73)分,明显低于帕瑞昔布钠组的(5.75±1.31)分(P<0.05).两组不良反应发生率差异无统计学意义(P>0.05).氟比洛芬酯组镇痛药物总费用(360.44±152.88)元,较帕瑞昔布钠组的(502.38±234.77)元明显降低(P=0.001).结论 氟比洛芬酯可有效缓解骨折术后病人疼痛,降低病人治疗费用,优于帕瑞昔布钠.     

氟比洛芬酯用于小儿唇腭裂修补术镇痛效果观察

术后疼痛是机体受到手术伤害刺激后的生理、心理和行为上的一系列反应,小儿唇腭裂患者术后疼痛可引起应激反应导致小儿生理和心理发生变化,对心身、家庭及社会带来负面影响[1].传统的术后镇痛治疗常以阿片类药物为主,如杜冷丁、吗啡及芬太尼等,但大量使用阿片类药物会引起许多围术期副作用.氟比洛芬酯(Flurbiprofen)是临床上广泛使用的非甾体抗炎药,具有抗炎、止痛及解热作用.氟比洛芬酯微球载体注射液,采用微球载体技术,使药物具有靶向性,起效时间短,持续时间长,静脉注药可以避免消化道局部刺激、呼吸抑制等副作用[2,3].本研究观察了氟比洛芬酯微球载体注射液用于小儿唇腭裂手术患者术后镇痛的效果及安全性.     

利多卡因和氟比洛芬酯联用治疗异丙酚注射痛的疗效观察

目的 评估利多卡因和氟比洛芬酯联用治疗异丙酚注射痛的疗效观察.方法 将100例年龄22 ～69 a的患者(男55例,女45例)随机分成4组:安慰剂组(生理盐水);利多卡因40 mg组;氟比洛芬酯50 mg组:利多卡因-氟比洛芬酯联用组(n=25),静脉阻塞2min,然后手背静脉注射0.5 mg/kg的异丙酚.结果 异丙酚注射痛在安慰剂组、利多卡因组、氟比洛芬酯组、联用组分别为88％、32％ 、40％和8％.结论 利多卡因40 mg和氟比洛芬酯注射液50 mg联合治疗有效地降低了异丙酚注射痛.     

氟比洛芬酯注射液用于腹腔镜手术的术后镇痛作用

目的:观察患者应用氟比洛芬酯注射液对腹腔镜下手术的预先镇痛作用和术后疼痛的镇痛效果。方法:普通外科和妇科行腹腔镜手术的患者120例,随机分为三组,每组各40例:A(术前给药组)、B(术后给药组)和C(对照组)。A组于麻醉诱导后、手术开始前缓慢静脉注射氟比洛芬酯注射液50 mg,B组于术终缓慢静脉注射氟比洛芬酯注射液50 mg,C组不给药。采用视觉模拟量表(VAS)评价静息时疼痛强度。结果:三组VAS评分差异显著,分别为(1．3±1．1),(2．1±1．7)和(3．8±2．1)分,从小到大依次为A相似文献   

氟比洛芬酯复合异丙酚用于烧伤换药镇痛的效果观察

目的 评价氟比洛芬酯复合异丙酚用于烧伤换药的镇痛效果.方法 将50例Ⅱ0烧伤病人随机分成观察组和对照组.观察组先缓慢静脉注射氟比洛芬酯50mg,10min后静脉注射异丙酚2.5mg/kg,对照组静脉注射异丙酚2.5mg/kg.结果 两组患者麻醉前的疼痛评分无统计学差异（P〉0.05）,换药后,观察组的VAS评分显著低于对照组（P〈0.01）.结论 氟比洛芬酯复合异丙酚可有效的缓解烧伤换药的创面疼痛.     

Extended-release formulations of tramadol in the treatment of chronic pain

Introduction: Tramadol is a centrally acting analgesic available throughout the world. Its dual opioid and non-opioid mechanisms of action, favorable efficacy and safety clinical profiles and non-controlled regulatory status in most markets contribute to its widespread use. A drawback of the immediate-release formulation of tramadol (four-times-a-day dosing) might be addressed by an extended-release formulation. Extended-release formulations also can offer advantages in the management of chronic pain: convenience, reduced pill burden (possibly leading to improved compliance) and the attenuation of peaks and troughs in serum concentration (possibly leading to reduced adverse effects).

Areas covered: The authors review tramadol's mechanisms of action and the clinical literature regarding the use of tramadol extended-release formulations for the management of conditions involving chronic pain, such as neuropathic pain syndromes, osteoarthritis and cancer pain.

Expert opinion: Based on the literature cited, extended-release formulations of tramadol seem to offer a rational and important addition to the analgesic armamentarium. As is true for all such options, the benefits and risks must be assessed for each patient.     

羟考酮临床治疗研究进展

羟考酮（oxycodone）是由蒂巴因（thebaine）改造合成的阿片类中枢神经镇痛药。近几年,随着新的羟考酮剂型的开发,该药物在急性疼痛以及慢性疼痛的控制中均广泛使用,并且出现与少量阿片类药物拮抗剂联用镇痛的方式。本文综述羟考酮的基本药理学性质以及临床应用进展。     

Evaluation of intravenous parecoxib for the relief of acute post-surgical pain

Parecoxib is a prodrug of valdecoxib, which is a potent and selective inhibitor of COX-2. Intravenous preparation of parecoxib is in Phase III clinical trials for the management of acute and severe post-surgical pain. It is the only COX-2 inhibitor that is available in a parenteral formulation. Clinical results compare parecoxib with ketorolac, a NSAID, which is the only non-narcotic analgesic available in parenteral formulation that can be administered for the relief of moderate to severe acute pain. Pharmacokinetic studies have shown that parecoxib is converted to valdecoxib within a short time following administration by im. or iv. injection. In clinical trials, parecoxib compares favourably with ketorolac and produces less gastric or duodenal ulcers, the predominant adverse effect, than ketorolac. Parecoxib, thus, fulfils some of the desirable characteristics of an ideal non-narcotic analgesic for severe post-surgical pain and has application in other acutely painful conditions. Parecoxib is expected to be filed for approval before the end of 2000 and is expected to be introduced in the market in 2001. It has favourable prospects for a fair share of the post-surgical pain relief market which is valued at approximately US$ 1 billion for the year 2000.     

The treatment of depression with different formulations of venlafaxine: a comparative analysis

Venlafaxine is the first of a group of antidepressants that show dual reuptake inhibition of serotonin and noradrenaline (SNRIs). Originally marketed in an immediate release (IR) formulation a microencapsulated, extended release (XR) formulation is now available. Significant differences exist between these two formulations with respect to pharmacokinetic parameters which have an impact on clinical use. The XR has lower maximum plasma concentrations (Cmax) and achieves these at a later time (higher Tmax). The longer apparent elimination half-life of the drug after single XR doses suggests that it is suitable for once daily dosing compared with the twice daily dosing regimen required by the IR formulation. With respect to antidepressant efficacy the XR formulation is equivalent to other marketed antidepressants and to the IR formulation. Consistent with its pharmacokinetic properties the use of the XR formulation is associated with less nausea and dizziness at the initiation of therapy. While in clinical usage XR might be expected to increase compliance with medication and to reduce discontinuation syndromes there are few comparative studies for which this has been evaluated. The XR formulation of venlafaxine is no worse than the IR form with respect to tolerability and offers some benefits to patients in terms of ease of use. On the other hand there does not appear to be any increase in the efficacy of the active agent.     

New formulations of existing antidepressants: advantages in the management of depression

For nearly 50 years, antidepressant drugs have been the first-line treatment for various forms of depression. Despite their widespread use, these medications have significant shortcomings, in particular problems of patient compliance due to adverse effects. The introduction of new formulations of existing antidepressant medications may provide patients with benefits in terms of convenience of use. As a consequence, improvements in compliance may lead to better antidepressant efficiency.An orally disintegrating formulation of mirtazapine (mirtazapine SolTab), a once-weekly formulation of fluoxetine, an enantiomer-specific formulation of citalopram (escitalopram), an extended-release formulation of venlafaxine (venlafaxine XR), a controlled-release formulation of paroxetine (paroxetine CR) and intravenous formulations of some of the newer antidepressants have all been evaluated in limited clinical trials. In this article, a review of the pharmacokinetics and clinical evaluations of these formulations is presented.While there do not appear to be major clinical advantages for the new formulations in terms of antidepressant efficacy, none of them is less efficacious than their older counterpart. Indeed, some of the new formulations are more acceptable to patients (fluoxetine once-weekly, paroxetine CR), others have pharmacokinetic advantages (venlafaxine XR, paroxetine CR), while others may have a faster onset of effect (mirtazapine SolTab, intravenous formulations). Further evaluation of some formulations is still required (mirtazapine SolTab, fluoxetine once-weekly), while others (venlafaxine XR, escitalopram) are finding widespread acceptance in clinical practice.     

Ketamine for chronic pain: risks and benefits

The anaesthetic ketamine is used to treat various chronic pain syndromes, especially those that have a neuropathic component. Low dose ketamine produces strong analgesia in neuropathic pain states, presumably by inhibition of the N-methyl-D-aspartate receptor although other mechanisms are possibly involved, including enhancement of descending inhibition and anti-inflammatory effects at central sites. Current data on short term infusions indicate that ketamine produces potent analgesia during administration only, while three studies on the effect of prolonged infusion (4–14 days) show long-term analgesic effects up to 3 months following infusion. The side effects of ketamine noted in clinical studies include psychedelic symptoms (hallucinations, memory defects, panic attacks), nausea/vomiting, somnolence, cardiovascular stimulation and, in a minority of patients, hepatoxicity. The recreational use of ketamine is increasing and comes with a variety of additional risks ranging from bladder and renal complications to persistent psychotypical behaviour and memory defects. Blind extrapolation of these risks to clinical patients is difficult because of the variable, high and recurrent exposure to the drug in ketamine abusers and the high frequency of abuse of other illicit substances in this population. In clinical settings, ketamine is well tolerated, especially when benzodiazepines are used to tame the psychotropic side effects. Irrespective, close monitoring of patients receiving ketamine is mandatory, particularly aimed at CNS, haemodynamic, renal and hepatic symptoms as well as abuse. Further research is required to assess whether the benefits outweigh the risks and costs. Until definite proof is obtained ketamine administration should be restricted to patients with therapy-resistant severe neuropathic pain.     

临床药师参与癌痛伴肾功能不全患者止痛方案的实践与经验

目的 探讨临床药师在止痛治疗中的作用,促进镇痛药更加规范的使用。方法 临床药师通过参与癌痛伴肾功能不全患者止痛方案的制定,从药物的选择、给药剂量以及不良反应预计等方面,提出药学观点。结果 医师采用了临床药师的建议,首日使用盐酸吗啡片进行快速滴定,次日起使用羟考酮缓释片控制背景疼痛,小剂量盐酸吗啡片控制爆发痛,在疼痛控制稳定后,改用芬太尼贴剂以减轻肾功能损害。结论 临床药师参与到重度癌痛患者的治疗方案制定中,能提高患者用药安全性、合理性,提高临床治疗效果。     

Clinical benefits versus shortcomings of diltiazem once-daily in the chronotherapy of cardiovascular diseases

Background: The introduction of chronotherapy (that is improving a drugs therapeutic efficacy by paralleling the drugs plasma levels to circadian rhythms) has recently become a focus of interest. Objective: This article addresses the efficacy and potential shortcomings of chronotherapy, and focuses on one specific type of chronotherapy: a novel long-acting diltiazem formulation, DTZ-LA. Methods: We reviewed the literature to assess the clinical benefits and shortcomings associated with DTZ-LA in the management of hypertension and angina. Results/conclusions: The clinical benefits of DTZ-LA outweigh its disadvantages when surrogate outcomes are evaluated, but it still remains to be determined whether chronotherapy benefits hard clinical outcomes. Nonetheless, chronotherapy has the potential to address the cardiovascular triggers that peak in the early morning hours when the preponderance of cardiovascular events occur, as well as providing better target organ protection compared with non-chronotherapeutic therapy.     

A “mix‐and‐use” approach for formulation of human clinical doses of 177Lu‐DOTMP at hospital radiopharmacy for management of pain arising from skeletal metastases

Use of bone‐seeking radiopharmaceuticals is an established modality in the palliative care of pain due to skeletal metastases. ¹⁷⁷Lu‐DOTMP is a promising radiopharmaceutical for this application owing to the ideally suited decay properties of ¹⁷⁷Lu and excellent thermodynamic stability and kinetic rigidity of the macrocyclic complex. The aim of the present study is to develop a robust and easily adaptable protocol for formulation of clinical doses of ¹⁷⁷Lu‐DOTMP at hospital radiopharmacy. After extensive radiochemical studies, an optimized strategy for formulation of clinical doses of ¹⁷⁷Lu‐DOTMP was developed, which involves simple mixing of approximately 3.7 GBq of ¹⁷⁷Lu activity as ¹⁷⁷LuCl₃ solution to an aqueous solution containing 5 mg of DOTMP and 8 mg of NaHCO₃. The proposed protocol yielded ¹⁷⁷Lu‐DOTMP with >98% radiochemical purity, and the resultant formulation showed excellent in vitro stability and desired pharmacokinetic properties in animal model. Preliminary clinical investigations in 5 patients showed specific skeletal accumulation with preferential localization in the osteoblastic lesion sites and almost no uptake in soft tissue or any other major nontarget organ. The developed “mix‐and‐use” strategy would be useful for large number of nuclear medicine centers having access to ¹⁷⁷Lu activity and would thereby accelerate the clinical translation of ¹⁷⁷Lu‐DOTMP.     

Hydromorphone-OROS formulation

Importance to the field: Hydromorphone is a semi-synthetic opioid approved in the USA for the treatment and relief of moderate to severe pain and postoperative pain. However, the compound is short-acting, and there is no extended-release formulation clinically available. A previous hydromorphone extended-release formulation that successfully came to market was subsequently withdrawn on account of safety concerns. Clinical need supports the presence of an extended-release formulation of hydromorphone.

Areas covered in this review: Medline articles showing from a search of ‘hydromorphone and OROS’ were included in the review. In addition, searches were done relating to published data regarding regulatory affairs dealing with this specific topic. Physicians prescribing information for hydromorphone was also reviewed.

What the reader will gain: The reader will gain an increased understanding of the use of an extended-release formulation of hydromorphone using the OROS technology and will appreciate that this technology has safety advantages compared with previous extended-release formulations of hydromorphone.

Take home message: Hydromorphone-OROS is an effective agent for the long-acting control of pain and a welcome addition to other available opioid formulations.