Dexibuprofen: pharmacology, therapeutic uses and safety

Dexibuprofen is the single pharmacologically effective enantiomer of rac-ibuprofen. Racibuprofen and dexibuprofen differ in their physico-chemical properties, in terms of their pharmacological properties and their metabolic profiles. Several clinical trials and post-marketing surveillance studies were performed to broaden the findings on dexibuprofen. In the last 5 years 4836 patients have been exposed to dexibuprofen in clinical trials and PMS trials. Only in 3.7% of patients adverse drug reactions have been reported and 3 serious adverse drug reactions (0.06%) were observed. In the dose ratio of 1 : 0.5 (rac-ibuprofen vs. dexibuprofen) at least equivalent efficacy was proven in acute mild to severe somatic and visceral pain models. Dexibuprofen has proven at least comparable efficacy to diclofenac, naproxen and celecoxib and has shown a favourable tolerability. The results suggest that dexibuprofen processed in a special crystal form is a safe and effective treatment for different pain conditions.     

Evaluation of the efficacy and dose-response relationship of dexibuprofen (S(+)-ibuprofen) in patients with osteoarthritis of the hip and comparison with racemic ibuprofen using the WOMAC osteoarthritis index

OBJECTIVE: Treatment with non-steroidal anti-inflammatory drugs is the most common pharmacological therapy of rheumatic diseases. For the symptomatic treatment of painful disorders a dose-response relationship of the NSAID should be a basic requirement, which is difficult to be proven in studies because rheumatic diseases are heterogenous in terms of clinical involvement. The aim of this double-blind randomized trial was to compare the isolated active enantiomer dexibuprofen (S(+)-ibuprofen) with the double dose of racemic ibuprofen and to show a dose-response relationship of dexibuprofen in painful osteoarthritis of the hip. METHODS: 178 patients were randomly assigned to dexibuprofen 600/1,200 mg or racemic ibuprofen 2,400 mg daily. The primary endpoint was the improvement of the WOMAC osteoarthritis index after 15 days of therapy. The analysis was by intention to treat. RESULTS: The evaluation of the WOMAC OA index showed statistically significant equivalence of dexibuprofen 400 mg t.i.d. compared with racemic ibuprofen 800 mg t.i.d. by a Mann-Whitney statistic of 0.578 and the corresponding lower bound of the 95% confidence interval of 0.498. The test for superiority of dexibuprofen was borderline significant with p = 0.055. Dexibuprofen 400 mg t.i.d. and dexibuprofen 200 mg t.i.d. showed a statistically significant dose-response relationship in improving the WOMAC OA index (p = 0.023). Patients suffered from adverse drug reactions, mainly gastrointestinal disorders, 13.34% on dexibuprofen 200 mg, 15.25% on dexibuprofen 400 mg and 16.94% on racemic ibuprofen 800 mg. CONCLUSIONS: The active enantiomer dexibuprofen (S(+)-ibuprofen) proved to be an effective non-steroidal anti-inflammatory drug with a significant dose-response relationship in patients with painful osteoarthritis of the hip. Compared with racemic ibuprofen half of the daily dose of dexibuprofen shows at least equivalent efficacy. In contrast to pharmacokinetic data, the additional administration of R(-)-ibuprofen in form of racemate does not contribute to the clinical efficacy of racemic ibuprofen.     

右布洛芬片与布洛芬片治疗类风湿关节炎比较

目的:评估右布洛芬治疗类风湿关节炎的疗效和安全性。方法: 81例类风湿关节炎病人随机分为试验组和对照组,试验组给予右布洛芬 0. 4 ~0. 6g,po,bid,对照组给予布洛芬 0. 4 ~0. 6g,po,bid,疗程 4wk。结果:试验组总改善率为 ( 52±s17) %,总有效率为 80 %,对照组总改善率为(38±13) %,总有效率为 58 % (P<0. 01,P<0. 05);不良反应发生率试验组为 11 %,对照组为 14 % (P>0. 05)。结论:右布洛芬疗效优于布洛芬,不良反应未增加,用药安全。     

The effects and safety of dexibuprofen compared with ibuprofen in febrile children caused by upper respiratory tract infection

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT

• The analgesic and anti-inflammatory efficacy of dexibuprofen compared with ibuprofen in adults with osteoarthritis, rheumatoid arthritis and dental pain.

WHAT THIS STUDY ADDS

• Dexibuprofen is as effective and tolerable as ibuprofen, and a dose of 5 mg kg⁻¹ of dexibuprofen would be sufficient to control fever caused by upper respiratory tract infection in children.

AIM

To evaluate the antipyretic efficacy and tolerability of dexibuprofen compared with ibuprofen in children with fever caused by upper respiratory tract infection (URTI).

METHODS

The study population consisted of children aged 6 months to 14 years. At the time of visit to the hospital, the children had fever; the cause of fever was determined to be URTI by a paediatrician based on history taking and physical examination. The study was a multicentre, randomized, double-blind, controlled parallel group, comparative, Phase 3 clinical trial, conducted at three hospitals. By using a computer-based random assignment program, the subjects were allocated to the following three groups: 5 mg kg⁻¹ dexibuprofen group, 7 mg kg⁻¹ dexibuprofen group, and 10 mg kg⁻¹ ibuprofen group.

RESULTS

In the clinical trial of the antipyretic action of dexibuprofen in patients with fever caused by URTI, there was no statistically significant difference in maximal decrease of temperature and mean time to become apyrexial among the 5 mg kg⁻¹ dexibuprofen, 7 mg kg⁻¹ dexibuprofen and 10 mg kg⁻¹ ibuprofen groups (P > 0.05). There also was no significant difference in adverse drug reaction (P > 0.05).

CONCLUSIONS

Dexibuprofen is as effective and tolerable as ibuprofen. A dose of 5 mg kg⁻¹ and 7 mg kg⁻¹ dexibuprofen in place of 10 mg kg⁻¹ ibuprofen would be sufficient to control fever caused by URTI in children.     

Comparison of the efficacy and tolerability of dexibuprofen and celecoxib in the treatment of osteoarthritis of the hip

CONTEXT: Osteoarthritis (OA) is often treated with nonsteroidal anti-inflammatory drugs (NSAIDs) or selective inhibitors of cyclooxygenase-2 (COX-2). OBJECTIVE: This clinical trial aimed to assess directly the relative therapeutic efficacy of the isolated active enantiomer of ibuprofen, named dexibuprofen (S(+)-ibuprofen) in a special crystal form, and the selective COX-2 inhibitor celecoxib in adults with OA of the hip. Moreover, the hypothesis that the tolerability/safety profile of dexibuprofen is comparable to celecoxib is to be tested. METHODS: The investigation was a randomized, parallel-group, double-blind, active controlled clinical trial, conducted from January 2001 to February 2002 in 4 rehabilitation centers in Austria. 148 inpatients were randomly assigned to dexibuprofen 800 mg or celecoxib 200 mg daily. The primary criterion was the improvement in the Western Ontario and' McMasters osteoarthritis index (WOMAC OA index) after 15 days of therapy. RESULTS: Evaluation of the WOMAC OA index proved that dexibuprofen 400 mg b.i.d. is not inferior to celecoxib 100 mg b.i.d. with the Mann-Whitney estimator equal to 0.5129 and the corresponding lower boundary of the 95% confidence interval equal to 0.4409. The overall incidence of adverse drug reactions was 12.16% in the dexibuprofen group and 13.51% in the celecoxib group. 8.1% of patients on dexibuprofen and 9.5% on celecoxib suffered from gastrointestinal disorders. CONCLUSION: In the presented clinical trial dexibuprofen has at least equal efficacy and a comparable safety/tolerability profile as celecoxib in adult patients suffering from osteoarthritis of the hip.     

Meta-analysis of smooth muscle relaxants in the treatment of irritable bowel syndrome

Aim: To assess the efficacy of smooth muscle relaxants in the treatment of patients with irritable bowel syndrome, a meta-analysis of 26 selected double-blind randomized trials vs. placebo was performed. Methods: Five end-points were assessed: global assessment, abdominal pain, constipation, abdominal distension and the absence of adverse reactions. Analyses were performed according to the intention-to-treat method. For each end-point, the drug efficacy was assessed by the Der Simonian and Peto methods. When a significant difference was observed, sensitivity analyses were performed by successive stratifications according to the type of drug, the treatment duration, the prevalence of constipated patients, the trial design and the methodological quality. Results: All myorelaxants analysed were significantly better than placebo for the improvement of global assessment (62% improvement rate vs. 35% on placebo, that is 27% improvement rate, P < 0.01) and for pain improvement (64% improvement rate vs. 45% on placebo, that is 19% improvement rate, P < 0.01). No significant differences were observed for constipation and abdominal distension. The percentage of patients with adverse reactions was significantly higher in patients receiving myorelaxants than placebo (6% mean difference, P < 0.01). Conclusion: According to this overview five drugs have proved their clinical efficacy in patients with irritable bowel syndrome, without significant adverse reactions: cimetropium bromide, pinaverium bromide, trimebutine. octilium bromide and mebeverine.     

S(+)-ibuprofen (dexibuprofen) — Excellent tolerance has not to be combined with poor clinical efficacy

S(+)-ibuprofen (dexibuprofen) is an NSAID offering a lot of advantages in the treatment of rheumatism and pain. A randomized double-blind, parallel group study in 110 patients showed equivalence in efficacy of 900 mg dexibuprofen (Seractil 300 mg, Gebro Fieberbrunn, Austria) vs. 150 mg diclofenac sodium. Regarding tolerance there was a trend to superiority of dexibuprofen. Therefore dexibuprofen can be characterized as an effective and very tolerable drug against inflammation and pain.     

右旋布洛芬凝胶的抗炎镇痛作用

目的 考察右旋布洛芬凝胶的抗炎、镇痛作用。方法 以角叉菜胶致大鼠足跖肿胀、二甲苯致小鼠耳廓肿胀、大鼠辐射热刺激及小鼠醋酸扭体法，观察右旋布洛芬凝胶的局部抗炎、镇痛作用。结果 2.5%、4.0%右旋布洛芬凝胶局部涂药能显著抑制角叉菜胶所致大鼠足跖肿胀及二甲苯所致小鼠耳廓肿胀，并能明显提高大鼠对光热刺激的痛阈，减少小鼠醋酸刺激的扭体次数。结论 2.5%右旋布洛芬凝胶局部外用具有显著的抗炎、镇痛活性。     

Modification of pepsinogen I levels and their correlation with gastrointestinal injury after administration of dexibuprofen, ibuprofen or diclofenac: a randomized, open-label, controlled clinical trial

OBJECTIVE: To assess the effect of a 2-week treatment with dexibuprofen, in comparison with ibuprofen and diclofenac, on pepsinogen plasma concentrations and gastrointestinal mucosa, as well as the correlation of these changes with gastrointestinal mucosal injury. METHODS: 60 patients with rheumatologic disease in chronic therapy with NSAID, were included. After a 7-day run-in period patients were randomly assigned to receive a 14-day treatment with dexibuprofen (Group A; Day 1 - 3 = 400 mg t.i.d; Day 4 - 14 = 400 mg b.i.d.), ibuprofen (Group B; Day 1 - 3 = 800 mg t.i.d; Day 4 -14 = 800 mg b.i.d.) or diclofenac (Group C; Day 1 - 3 = 50 mg t.i.d; Day 4 - 14 = 50 mg b.i.d.). Upper gastrointestinal endoscopy (Day 15), capsule-endoscopy (Day 16, 7 patients of each group) and determination of pepsinogen plasma concentrations were performed (basal and Day 15). A semiquantitative scale was designed for the assessment of the gastrointestinal mucosa. RESULTS: No differences in plasma pepsinogen were found between treatment groups or gastrointestinal injury grades or between basal and post-therapy determinations. Dexibuprofen showed gastroduodenal mucosal injury in fewer patients (42.1%) than was the case with ibuprofen (5%; p = 0.003) and diclofenac (30%; p = N.S.). Dexibuprofen administration was also associated with more patients having no intestinal mucosal damage (42.86% vs. 28.7% in the diclofenac group and 14.29% in the ibuprofen group; p = 0.0175). The rate of clinical adverse events was similar in Groups A, B and C (28%, 38% and 34%). CONCLUSIONS: Dexibuprofen showed a lower rate of gastroduodenal and intestinal mucosal injury. This effect was not mediated by modifications of plasma pepsinogen levels.     

Buprenorphine 5, 10 and 20 μg/h transdermal patch: a review of its use in the management of chronic non-malignant pain

This article reviews the pharmacology, therapeutic efficacy and tolerability profile of the 7-day lower-dose (5, 10 and 20?μg/h) buprenorphine transdermal patch (BuTrans?, Norspan?) in the management of chronic non-malignant pain, with a focus on European labelling for the drug. Buprenorphine is a semi-synthetic opioid analgesic that acts primarily as a partial agonist at the mu opioid receptor. The transdermal formulation provides continuous delivery of buprenorphine, resulting in relatively consistent plasma drug concentrations throughout the 7-day dosing interval. The analgesic efficacy of transdermal buprenorphine in patients with osteoarthritis of the hip and/or knee has been demonstrated in several randomized controlled trials, which have shown the formulation to be equivalent to sublingual buprenorphine, noninferior to prolonged-release tramadol tablets, noninferior to codeine plus paracetamol (acetaminophen) combination tablets (when transdermal buprenorphine was used together with regularly scheduled oral paracetamol) and generally superior to a matching transdermal placebo patch. Transdermal buprenorphine was significantly more effective than placebo in reducing chronic low back pain of at least moderate severity in two randomized, double-blind, crossover trials. Other clinical trials, including a randomized, double-blind, maintenance-of-analgesia study, have also demonstrated the analgesic efficacy of transdermal buprenorphine in patients with chronic non-malignant pain of various causes. In general, serious adverse events with transdermal buprenorphine are similar to those for other opioid analgesics. Transdermal buprenorphine has a ceiling effect for respiratory depression, and the main risk is when it is combined with other CNS depressants. The most frequently reported adverse events with transdermal buprenorphine are headache, dizziness, somnolence, constipation, dry mouth, nausea, vomiting, pruritus, erythema, application site pruritus and application site reactions. Transdermal buprenorphine was better tolerated than sublingual buprenorphine in a 7-week, randomized, double-blind trial in patients with osteoarthritis pain. Nevertheless, as with other opioids, persistence with transdermal buprenorphine therapy is difficult for many patients because of adverse events or other reasons. Thus, transdermal buprenorphine has generally demonstrated good efficacy and tolerability in clinical trials in chronic non-malignant pain, providing effective background analgesia as part of pain management strategies for patients with osteoarthritis, low back pain and other persistent pain syndromes of at least moderate severity. It also has favourable pharmacodynamic and pharmacokinetic properties, which have beneficial clinical implications, most notably the convenience of once-weekly administration and no need for dosage adjustments in the elderly or those with compromised renal function, making it an opioid of choice in these patients, and a useful therapeutic option overall in the management of chronic non-malignant pain.     

回访调查羟考酮治疗晚期癌痛的不良反应率及护理体会

目的观察出院患者口服羟考酮治疗癌痛的不良反应发生率及与其满意度。方法对出院后在家口服羟考酮治疗晚期癌症疼痛的的患者进行每周一次电话回访,调查癌痛治疗不良反应率及对止痛效果的满意度,并提供相关的护理宣教。结果对80例患者共901次电话回访,疼痛治疗中主要不良反应表现为便秘(13.7%)、恶心呕吐(1.2%)、头晕(0.3%)及排尿不畅(0.2%);98.3%患者对止痛效果满意。结论羟考酮治疗中、重度晚期癌痛满意度高,不良反应可耐受,是目前控制中重度癌痛的理想药物之一,疼痛护士对患者良好的健康教育的可减轻患者对不良反应的恐惧感,对提高其服药的依从性有重要的作用。     

中西医结合治疗消化性溃疡的临床研究

目的探讨中西医结合治疗消化性溃疡的临床疗效和用药安全性。方法回顾性分析2010年5月~2012年5月本院接诊的消化性溃疡患者58例的临床治疗资料,58例患者分为2组,观察组采用中西医结合治疗,对照组采用口服西药治疗,对比两组患者临床疗效及药物不良反应发生率。结果观察组29例患者中,显效21例,有效7例,无效1例,总有效率达96.55%,明显高于对照组的总有效率79.56%（显效14例,有效9例,无效6例）,P〈0.05;对照组1例出现恶心,1例出现轻度皮疹,而观察组1例出现腹痛,经适当处理后均好转。对照组的不良反应发生率为6.90%,高于观察组发生率3.45%,P〈0.05。结论中西医结合治疗消化性溃疡疗效比单纯西药联合治疗效果更为显著,值得推广应用于临床。     

氨酚羟考酮片与盐酸羟考酮缓释片在晚期癌痛治疗的药物经济学分析

目的:评价氨酚羟考酮片与盐酸羟考酮缓释片治疗晚期癌痛患者镇痛的成本-效果,为临床合理用药提供指导。方法:选取晚期癌痛患者148例,其中氨酚羟考酮组73例,羟考酮缓释片组75例,比较用药4周后的镇痛疗效、不良反应及治疗成本,并进行成本-效果分析。结果:氨酚羟考酮组和羟考酮缓释片组镇痛治疗总有效率分别为86.3%,和90.7%,2组间疗效差异无统计学意义(P>0.05),成本/效果比(C/E)分别为16.3和26.3,氨酚羟考酮组的不良反应发生率较羟考酮缓释片组低。结论:氨酚羟考酮片和盐酸羟考酮缓释片用于治疗晚期癌痛患者镇痛疗效相当,氨酚羟考酮片治疗成本较低,是晚期癌痛患者镇痛治疗的较佳方案。     

Treatment-resistant depression: no panacea, many uncertainties. Adverse effects are a major factor in treatment choice

At least 50% of patients with depression do not enter remission after several weeks of antidepressant therapy. To determine the treatment options and their respective risk-benefit balances in this setting, we reviewed the literature using the standard Prescrire methodology. Clinical trials and epidemiological studies show that depression should only be considered drug-resistant after at least 6 weeks of therapy. After assessing residual symptoms and their impact on the patient's quality of life, a search should be made for factors responsible for the persistence of depression, such as the patient's environment, a psychiatric or somatic disorder, and drug intake or addiction. Increasing the dose of the first-line antidepressant is only based on weak evidence. Trials comparing continuing the first-line antidepressant versus switching to another pharmacological class have yielded conflicting results. A switch may benefit some patients, but the elimination half-life of the discontinued drug must be taken into account to limit the risk of interactions during the transition. Combining two antidepressants mainly increases the risk of adverse effects, without a tangible clinical benefit. Two meta-analyses suggest that adding a so-called atypical neuroleptic to ongoing antidepressant therapy leads to 1 extra remission per 7 to 10 treated patients, but also to treatment cessation due to adverse effects in 8% to 9% of cases. Older neuroleptics have not been properly evaluated in this setting. Comparative trials suggest that lithium may have a certain antidepressant effect in this setting, but there is no firm evidence that adding lithium increases the chances of remission. Lithium has a narrow therapeutic margin and overdose can be fatal; the blood lithium concentration must therefore be monitored. Adding an antiepileptic or a psychostimulant is more harmful than beneficial. Adding a thyroid hormone, a benzodiazepine, buspirone or pindolol has no proven antidepressive effect. Four trials, each including fewer than 20 patients, have assessed the efficacy of psychotherapy in patients with treatment-resistant depression. Two of them provided positive results. Electroconvulsive therapy is probably effective for some patients with refractory depression but it necessitates general anaesthesia and carries a risk of memory disorders. Vagal nerve electrostimulation has no proven efficacy. Transcranial magnetic stimulation seems to have some efficacy and few adverse effects, but its optimal modalities remain to be determined. In practice, when the patient and doctor decide to attempt second-line therapy for treatment-resistant depression, adverse effects must be taken into account in the choice of drug(s). Maintaining a good quality relationship between patient and doctor may be more important than attempting to obtain remission "at any cost".     

Ortho Evra,a new contraceptive patch

Ortho Evra is the first transdermal patch approved for the prevention of pregnancy. Comparative trials have shown that Ortho Evra has efficacy similar to the oral contraceptives Mercilon (not available in the United States) and Triphasil for the prevention of pregnancy when used as directed. Adverse effects with Ortho Evra are similar to those reported with combined oral contraceptives, with the exceptions of mild-to-moderate application-site reactions and an increased frequency of breast symptoms. The most commonly reported adverse reactions were breast symptoms, headache, application-site reactions, nausea and vomiting, dysmenorrhea, and abdominal pain. Approximately 5% of study subjects had at least one patch that did not stay attached to their skin, and about 2% of women withdrew from clinical trials due to irritation from the patch. In clinical studies, the patch appeared to be less effective in women weighing more than 90 kg than in women with lower body weights. More research is needed on the relationship between body weight and contraceptive patch efficacy. In two clinical trials, compliance was greater with the patch than with oral contraceptives. Whether this will result in reduced pregnancy rates in general use is unknown. Additional studies are warranted to determine if the patch offers any significant efficacy or safety advantages over current methods of hormonal contraception.     

丙戊酸钠血药浓度与抗癫痫疗效及不良反应关系研究

目的：研究丙戊酸钠血药浓度与其抗癫痫疗效及不良反应的关系,为临床合理应用抗癫痫药丙戊酸钠提供参考,同时也为制订个体化给药方案提供依据。方法：采用回顾性分析方法,查阅我院2010—-2012年服用丙戊酸钠的癫痫患者的病历,收集整理资料,对丙戊酸钠血药浓度、抗癫痫疗效和各个系统出现的不良反应进行统计和分析。结果：研究共收集114例患者监测结果,丙戊酸钠血药浓度在正常范围内的（50—100μg/ml）有72例,其中显效和有效的有50例（占69．44％）,疗效不足或疗效差与无效的有22例（占30．56％）;丙戊酸钠血药浓度〈50μg／ml的有35例,其中显效和有效的有21例（占60．00％）,疗效不足或疗效差与无效的有14例（占40．00％）;丙戊酸钠血药浓度〉100μg／ml的有7例。服用丙戊酸钠,出现肝功能异常者4例、肾功能异常者2例、血液系统异常者4例、消化系统不良反应者3例、神经系统不良反应者5例及皮肤不良反应者3例。结论：丙戊酸钠血药浓度在有效浓度范围内有较好的疗效,但存在个体差异。丙戊酸钠在有效浓度范围内,出现了血液系统、消化系统等不良反应,因此在临床上使用时应监测其血药浓度和不良反应。     

降钙素治疗骨质疏松性疼痛的疗效观察

目的:观察降钙素治疗骨质疏松患者疼痛症状的疗效。方法:将121例患者随机分为试验组和对照组,分别给予降钙素和一般钙剂治疗,12周后观察疼痛缓解效果、骨密度(BMD)和生化指标变化及不良反应。结果:试验组疼痛缓解有效率为93.0%,对照组为35.7%,差异有统计学意义(P<0.05)。试验组BMD较对照组明显升高(P<0.05)。2组患者生化指标在治疗前、后均无显著性差异(P>0.05)。试验组患者在治疗过程中部分患者出现面色潮红、食欲减退、头晕等不良反应,继续用药2周不良反应消失。结论:降钙素是治疗骨质疏松性疼痛的有效药物,可能会出现部分轻微不良反应,可自行消失。     

吗啡控释片治疗癌性疼痛的疗效和安全性评价

目的：通过Meta分析,评估吗啡控释片直肠给药在癌性疼痛治疗中的临床应用价值。方法：检索中国生物医学文献库（CBMdisc）、中国期刊全文数据库、维普数据库（VIP）等国内数据库已发表的相关文献,收集国内有关吗啡控释片直肠给药治疗癌性疼痛的临床随机、对照试验（randomized controlled trials,RCT）,由2位评价者分别按检索策略收集并纳入标准入选资料,分析指标为疼痛缓解率和不良反应发生率。结果：8个研究共598例患者纳入分析,吗啡控释片直肠给药和口服给药的疼痛缓解率分别是83.69%和87.97%（P=0.09）;在不良反应方面,吗啡控释片直肠给药导致便秘的发生率降低了15%（P〈0.000 1）,消化道反应的发生率降低了21%（P〈0.000 1）,嗜睡头晕的发生率降低了9%（P=0.001）。结论：吗啡控释片直肠给药和口服给药治疗中重度癌性疼痛的效果相近,但直肠给药不良反应的发生率可能较低,临床医生应根据患者个体情况合理选用。     

Review of lidocaine patch 5% studies in the treatment of postherpetic neuralgia

Postherpetic neuralgia (PHN) is a chronic pain syndrome that disproportionately affects the elderly; its incidence is anticipated to increase as the population ages. PHN presents as pain (continuous burning or intense paroxysmal), most often with tactile allodynia, which may be severe and disabling, resulting in poor quality of life and depression. Traditional treatments have included tricyclic antidepressants, anticonvulsants and opioids; however, adverse systemic effects associated with these agents have led to the development of a newer and potentially safer agent, the topical lidocaine patch 5% (Lidoderm), a targeted peripheral analgesic.This article reviews the clinical pharmacology of the lidocaine patch 5% for the treatment of PHN and summarises data from clinical trials of its safety, tolerability and efficacy. The Medline search terms "lidocaine" and "patch" were used to search for English-language articles on the pharmacokinetics of the lidocaine patch 5% and its clinical use for the treatment of PHN. Additional published studies not identified by the database search but performed by the authors or their colleagues were also included in the review.The systemic absorption of lidocaine from the patch was minimal in healthy adults when four patches were applied for up to 24 hours/day, and lidocaine absorption was even lower among PHN patients than healthy adults at the currently recommended dose. Vehicle-controlled and open-label trials found the lidocaine patch 5%, either alone or in combination with other agents, to be effective in the treatment of PHN. Most adverse events were at patch application sites; no clinically significant systemic adverse effects were noted, including when used long term or in an elderly population.In patients with PHN, the lidocaine patch 5% has demonstrated relief of pain and tactile allodynia with a minimal risk of systemic adverse effects or drug-drug interactions. Because of its proven efficacy and safety profile, the lidocaine patch 5% has been recommended as a first-line therapy for the treatment of the neuropathic pain of PHN.