Effect of prolonged-release tapentadol in the management of moderate-to-severe chronic pain in elderly patients. Case reports / Efeito do tapentadol de liberação prolongada no manejo da dor crônica de moderada a intensa em pacientes idosos. Relato de casos

ABSTRACT BACKGROUND AND OBJECTIVES: Prolonged-release (PR) tapentadol has demonstrated efficacy, safety, and good tolerability for the management of moderate to severe chronic pain in patients over 65 years of age. The objective of this study was to describe three clinical cases in which tapentadol PR was used as treatment of moderate to severe chronic pain in individuals aged 75 to 83 years old. CASE REPORT: Two female patients (75 and 83 years old) and one male patient (78 years old) with chronic osteoarticular pain or low back pain of moderate to severe intensities and with functional limitation, who had undergone previous unsuccessful treatments and were functionally limited, underwent treatment with tapentadol PR. Tapentadol PR was associated with considerable improvement of pain in all three patients, leading to greater independence in performing daily activities. In addition, the use of tapentadol PR did not cause any significant adverse effects. CONCLUSION: Treatment with tapentadol PR seems to be effective and tolerable in the management of moderate to severe chronic pain in senior patients.

RESUMO JUSTIFICATIVA E OBJETIVOS: O tapentadol de liberação prolongada (LP) demonstrou eficácia, segurança e boa tolerabilidade para o tratamento de dor crônica moderada a grave em pacientes com mais de 65 anos de idade. O objetivo deste estudo foi descrever três casos clínicos em que o tapentadol de liberação prolongada foi usado como tratamento para dor crônica de moderada a grave em indivíduos de 75 a 83 anos de idade. RELATO DOS CASOS: Dois pacientes do sexo feminino (75 e 83 anos de idade) e um paciente do sexo masculino (78 anos de idade) com dor osteoarticular crônica ou dor lombar de intensidade moderada a intensa e com limitação funcional, que haviam sido submetidos a tratamentos anteriores sem sucesso e estavam limitados funcionalmente, foram submetidos a tratamento com tapentadol LP. O tapentadol LP foi associado a uma melhora considerável da dor em todos os três pacientes, levando a uma maior independência na realização das atividades diárias. Além disso, o uso do tapentadol LP não causou nenhum efeito adverso significativo. CONCLUSÃO: O tratamento com tapentadol parece ser eficaz e tolerável no tratamento da dor crônica moderada a grave em pacientes idosos.

Tapentadol extended-release as a therapeutic strategy for pain control in cases of osteoarthritis. Case reports / Tapentadol de liberação prolongada como estratégia terapêutica para o controle da dor em casos de osteoartrite. Relato de casos

ABSTRACT BACKGROUND AND OBJECTIVES: Osteoarthritis affects many individuals worldwide and is caused by multiple factors that lead to joint wear and tear, inflammation and, consequently, chronic pain that is difficult to treat. It is predominant in seniors, but not restricted to older age groups. Pain reduction is prioritized when facing crises, so that rehabilitation work and postural corrections can be applied later. The present study aimed to evaluate the analgesic potential of tapentadol extended-release (ER) in three patients with osteoarthritis who had undergone numerous previous treatments and had a history of moderate to severe chronic pain. CASE REPORTS: Three women, aged 49, 75 and 86 years old, diagnosed with osteoarthritis, with complaints of severe pain and who had undergone numerous therapies including drug use, without significant pain control were included in the study. The use of tapentadol ER was recommended and adjusted to each patient according to the intensity of pain. All of them responded satisfactorily and returned to their daily activities. One of them presented nausea after two days of tapentadol use, which was controlled with an antiemetic drug only during the two days of nausea CONCLUSION: Tapentadol ER was effective in controlling pain from osteoarthritis in the three cases evaluated, without serious adverse effects. The period and dosage of tapentadol ER must be in accordance with the clinical evolution of each patient.

RESUMO JUSTIFICATIVA E OBJETIVOS: A osteoartrite afeta muitos indivíduos em todo o mundo, é causada por múltiplos fatores que conduzem ao desgaste articular, a inflamações e, consequentemente, a dores crônicas de difícil tratamento. É predominante em idosos, mas não restrita às faixas etárias mais elevadas. A diminuição da dor é priorizada diante das crises, para que trabalhos de reabilitação e correções posturais possam ser aplicados posteriormente. O presente estudo teve por objetivo avaliar o potencial analgésico do tapentadol de liberação prolongada (LP) em três pacientes com osteoartrite que já haviam passado por inúmeros tratamentos prévios, com histórico de dor crônica de moderada a intensa. RELATO DOS CASOS: Três pacientes do sexo feminino, com idades de 49, 75 e 86 anos, diagnosticadas com osteoartrite, com queixas de dor intensa e que haviam passado por inúmeras terapias e uso de fármacos, sem controle significativo da dor. O uso do tapentadol LP foi recomendado e ajustado a cada paciente conforme a intensidade da dor e todas elas apresentaram resposta satisfatória e retomaram suas atividades diárias. Uma delas apresentou náusea após dois dias de uso do fármaco, que foi controlada com um fármaco antiemético somente durante dois dias de enjoo. CONCLUSÃO: O tapentadol LP foi efetivo para controlar as dores decorrentes da osteoartrite nos três casos avaliados, sem efeitos adversos graves. O período e a dose do tapentadol LP deve considerar a evolução clínica de cada paciente.

Experiencia en la práctica clínica real de la efectividad y la tolerabi- lidad de tapentadol de liberación prolongada para el tratamiento de dolor crónico postraumático producido por accidentes de trabajo / Real-world clinical practice experience of the effectiveness and tolerability of pro- longed-release tapentadol for the treatment of chronic post-traumatic pain caused by occupational accidents

Se llevó a cabo un estudio observacional para analizar si tapentadol de liberación prolongada (LP) puede considerarse un tratamiento de primera línea para pacientes con dolor crónico postraumático (DCPT). Métodos: Se presenta una serie de casos de la práctica clínica real de pacientes con DCPT producido por accidentes de trabajo. Antes de ingresar al estudio, todos los pacientes recibían tramadol, que se interrumpió cuando se inició la administración de tapentadol LP. Las evaluaciones de dolor incluyeron una escala de valoración numérica, el cuestionario DN4 y la escala de Impresión Global de Cambio del Paciente (PGIC, Patients' Global Impression of Change). Se recuperaron y registraron los eventos adversos. Resultados: 94 pacientes participaron en el estudio y 77 (82 %) completaron todas las visitas predefinidas. Cerca de la mitad de los pacientes informaron dolor crónico que tenía una duración de al menos 3 años; se observó un componente neuropático en el 87 % de los pacientes. El puntaje de dolor se redujo en 1,5 puntos luego del primer mes de tratamiento con tapentadol LP y en 2,48 puntos luego de 4 meses (p<0,05). También se asoció la administración de tapentadol LP con una reducción del 28,9 % de la dosis concomitante de pregabalina (p<0,01). De acuerdo con el cuestionario PGIC, el 74 % y el 77,9 % de los pacientes informó mejoría luego de uno y cuatro meses de tratamiento, respectivamente. El perfil de seguridad fue consistente con los datos actuales sobre tapentadol LP. Conclusión: El dolor osteomuscular crónico es una enfermedad prevalente que se caracteriza por tener resultados terapéuticos deficientes y se asocia a una mayor discapacidad y una mala calidad de vida. En este estudio de la práctica clínica real en pacientes que trabajan y que cuentan con un componente de dolor neuropático elevado, se observó que tapentadol LP produce efectos beneficiosos en términos del control del DCPT, y se obtuvieron índices altos de eficacia y seguridad.

An observational study was carried out to analyze whether prolonged-release (PR) tapentadol may be considered a first-line treatment for patients with chronic post-traumatic pain (PTD). Methods: A case series of cases of patients with PTFE caused by work accidents in a real clinical practice setting is described. Before entering the study, all patients were receiving tramadol, which was discontinued when PR tapentadol was started. Pain assessments included a numerical rating scale, the DN4 questionnaire, and the Patients' Global Impression of Change (PGIC) scale. Adverse events were retrieved and described. Results: 94 patients participated in the study and 77 (82%) completed all the predefined visits. About half of the patients reported chronic pain that lasted for at least 3 years. A neuropathic component was reported in 87% of patients. The pain score was reduced by 1.5 points after the first month of treatment with PR tapentadol and by 2.48 points after 4 months (p < 0.05). Administration of PR tapentadol was also associated with a concomitant reduction of pregabalin dose of 28.9% (p < 0.01). According to the PGIC questionnaire, 74% and 77.9% of patients reported improvement after one and four months of treatment, respectively. The safety profile was consistent with current data on PR tapentadol. Conclusion: Chronic musculoskeletal pain is a prevalent disease characterized by poor therapeutic results and associated with increased disability and poor quality of life. In our study in a real clinical practice setting with patients with a high neuropathic pain component, PR tapentadol produced beneficial effects in terms of DCPT control, and high efficacy and safety rates were obtained. Keywords: tapentadol, chronic pain, pain caused by work accidents, chronic post-traumatic pain, evidence from real clinical practice.

Development and validation of stability indicating LC-MS/MS Technique for the quantification of tapentadol in biological matrices: Application to bioavailability study in healthy rabbits

An Liquid chromatography tandem mass spectrometry (LC-MS/MS) technique is one of the best analytical methods for thequantification of drugs in biological samples. A stability-indicating analytical technique was developed for the quantitationof tapentadolin biological matrices as tapentadol with short runtime. Developed technique also suitable for bioavailabilitystudies in healthy rabbits. Separation of tapentadol and tapentadol-d3 were achieved from plasma sample with solid-phaseextraction and elution was processed with Luna-C18 (5 μ, 100 mm × 4.6 mm) stationary column with movable phase ratiocomprising 2-mM ammonium acetate buffer (pH-3.6) and acetonitrile in the proportion of 10:90 % V/V. Quantitationwas processed by processing the transitions of tapentadol and tapentadol-d3 at m/z 222.2 → 177.1 and 228.2 → 183.1,respectively, in positive ionization mode. Linearity was performed over the concentration range of 0.121 to 35.637 mg/ml(R2 > 0.99) without matrix effect (2.74%). The inter- and intra-day precision findings were within 8.62% and 11.38%,respectively. Stability data showed that the tapentadol was stable when it exposed to different stability conditions. Thistechnique was effectively applied to bioavailability studies of tapentadol in healthy rabbits

Safety and Efficacy of Tapentadol in Osteoarthritis: A Prospective Observational Study

Osteoarthritis (OA) is the most common type of arthritis. Its high prevalence, especially in the elderly, and the high rate of disability related to disease make it a leading cause of impaired mobility in the elderly. To evaluate the efficacy, safety and tolerability of tapentadol in OA of knee joint in Indian population this study was undertaken. Methods: A prospective observational study involving patients of 40 years and above suffering from moderate to severe pain due to OA of knee joints attending the orthopaedics OPD of the National Medical College were recruited according to inclusion and exclusion criteria. Pain intensity was measured by 10 point VAS score on baseline and 2 follow up visits at 1st and 2nd week. Patients were given 50 -100 mg twice daily oral tapentadol tablets. ADRs were noted and data analysis done. Results: Total of 84 with baseline mean VAS score was 4.7 (SD 0.62). Significant reductions from baseline were noted at 1 week and 2 weeks follow up visits. At first follow up visit i.e on week 1 the mean pain intensity score was 2.48 (SD 1.45) whereas in 2nd follow up visit on week 2 it was 1.7 (SD 1.39). The change in pain intensity score were statistically significant (p<0.0001) for both the situations. Adverse drug events were mostly non serious. Commonly presented ADRs were diarrhoea, nausea, dizziness, constipation and hyperhidrosis. The incidence were around 6%. Conclusion: This observational study of pain relief in patients suffering from moderate to severe pain due to OA had been treated with tapentadol showed significant clinical improvement with few adverse effects. There are limitations due to small sample size and non-comparative design.

Meta-analysis of Efficacy and Safety of Tapentadol Immediate-release Preparation for Relie ving Moderate and Severe Acute Pain after Brachiocephalic Arteritis / 中国药房

OBJECTIVE： To systematically evaluate the efficacy and safety of Tapentadol immediate-release preparation （Tap IR） for relieving severe acute pain after brachiocephalic arteritis， and to provide evidence-based reference for rational drug use. METHODS： Retrieved from PubMed， Medline， Cochrane library， CNKI， VIP， Wanfang database and American clinical trial database， randomized controlled trials （RCTs） about Tap IR （trial group） versus Oxycodone immediate-release preparation or placebo for relieving severe acute pain after brachiocephalic arteritis were collected. After literature screening， data extraction and literature quality evaluation with modified Jadad scale， Meta-analysis was conducted by using RevMan 5.3 software. RESULTS： A total of 6 RCTs were included， involving 2 378 patients. Results of Meta-analysis showed that 48 h total pain relief value （TOTPAR48） of trial group was significantly higher than control group [MD＝35.60，95％CI（27.31， 43.88）， P＜0.000 01]. Results of sub-group analysis showed that TOTPAR48 of trial group using Tap IR 50 mg [MD＝28.68， 95％CI （18.18， 39.17），P＜0.00 001]， 75 mg [MD＝39.97， 95％CI （34.21， 45.73）， P＜0.000 01] and 100 mg[MD＝38.50， 95％CI（1.46， 75.54），P＝0.04] were significantly higher than control group； TOTPAR48 of patients who received Tap IR 75 mg were significantly higher than patients who received Tap IR 50 mg [MD＝9.04，95％ CI（4.31， 13.77），P＝0.000 2]. There was no statistical significance in the utilization rate of rescue medicine （URM） between 2 groups [RR＝1.23，95％ CI（0.84， 1.80），P＝0.29]. Subgroup analysis showed that URM in patients who received Tap IR 75 mg was significantly lower than those receiving Tap IR 50 mg [RR＝0.62，95％CI（0.41， 0.94），P＝0.02]. The total difference of 48 h pain intensity （SPID48） in trial group was significantly lower than control group [MD＝－18.96，95％CI（－37.28，－0.64），P＝0.04]. Subgroup analysis showed that SPID48 in patients who received Tap IR 75 mg was significantly higher than those receiving Tap IR 50 mg [MD＝21.66，95％CI（8.93， 34.39），P＝0.000 9]. There was no statistical significance in the total change of pain impression （PGIC） between 2 groups [RR＝0.95，95％CI（0.88， 1.03），P＝0.23]. Subgroup analysis showed that PGIC in patients who received Tap IR 75 mg was significantly higher than those receiving Tap IR 50 mg [RR＝1.07，95％CI（1.01， 1.13），P＝0.02] but significantly lower than those receiving Tap IR 100 mg [RR＝0.86，95％CI（0.77， 0.97），P＝0.01]. The incidence of nausea， vomiting， constipation， dizziness and headache in trial group were significantly lower than control group （P＜0.05）. CONCLUSIONS： Tap IR shows good therapeutic efficacy and safety for severe acute pain after brachiocephalic arteritis， and the efficacy of Tap IR might be better when the dose of Tap IR is 75 mg.

A Case of Serotonin Syndrome Caused by Combination Therapy with Tapentadol and a Selective Serotonin Reuptake Inhibitor

Tapentadol was developed from tramadol by reducing its inhibitory effects on serotonin reuptake. In the present study, tapentadol was administered to a 49-year-old female esophageal cancer patient receiving a selective serotonin reuptake inhibitor (SSRI). On the day of administration, akathisia, nausea, dizziness, and insomnia developed. On the following day, she was diagnosed with serotonin syndrome, accompanied by fever, perspiration, myoclonic jerks mainly affecting the upper limbs, tremor of the extremities, and tachycardia. The diagnosis was made using three criteria. The symptoms disappeared immediately after discontinuation of tapentadol administration and initiation of benzodiazepine treatment. In Japan, tapentadol is an opioid analgesic for cancer pain management. If it is combined with an antidepressant, follow-up care is needed in consideration of serotonin syndrome.

Tapentadol: what every doctor needs to know about this new drug / Tapentadol: o que todo médico precisa saber sobre esse novo fármaco

ABSTRACT BACKGROUND AND OBJECTIVES: Acute and chronic pain is a major problem with repercussion in our society, causing impairment in the quality of life of patients as well as socioeconomic losses, due to work absenteeism. This review aims to analyze the use of tapentadol, an analgesic not yet available in Brazil, with a dual mechanism of action, in the treatment of acute and chronic pain syndromes. CONTENTS: A review about this new drug was made on the Pubmed database using the keywords "tapentadol" and "opioids," evaluating its pharmacological and clinical aspects comparing with other current drugs in pain treatment, as well as its indications and contraindications in the management of patients with pain disorders. CONCLUSION: Tapentadol has been shown to be effective in the treatment of acute and chronic pain, with potency equivalent to the opioids currently used. In addition, it developed less tolerance, less adverse effects and better therapeutic response in chronic neuropathic pain when compared to pure µ-opioid receptors agonists.

RESUMO JUSTIFICATIVA E OBJETIVOS: A dor aguda e crônica consiste em um problema de grande repercussão em qualquer sociedade atual, causando degradação na qualidade de vida dos próprios pacientes e comprometimento socioeconômico pelo absenteísmo laboral. O objetivo deste estudo foi analisar o uso do tapentadol, um analgésico ainda não disponível no Brasil e com duplo mecanismo de ação, no tratamento das síndromes dolorosas agudas e crônicas. CONTEÚDO: Foi realizada uma pesquisa na base de dados Pubmed utilizando os descritores "tapentadol" e "opioides" para revisão da literatura mundial sobre esse novo fármaco, avaliando as características farmacológicas e aspectos clínicos do seu uso na realidade atual, em comparação com os fármacos já existentes no mercado, assim como suas indicações e contraindicações no manuseio do paciente com dor. CONCLUSÃO: O tapentadol se mostrou eficaz no tratamento de dores agudas e crônicas, com potência equiparável aos opioides já comercializados. Além disso, desenvolveu menos tolerância, menos efeitos adversos e melhor resposta terapêutica na dor crônica neuropática quando comparado com agonistas receptores opioides tipo µ puros.

Emerging horizons in anaesthetic practice: a pharmacological update

Anesthesiologists are in search for new drugs possessing properties like rapid onset of action, minimal residual effects, better hemodynamic stability, organ independent metabolism and cost effective. Structural alterations of the currently available compounds or newer formulations of the older ones or newer anaesthetic drug delivery system will be an useful alternative to newer discovery by reducing the cost and time. Tapentadol is a centrally acting µ opioid receptor (MOR) agonist with selective norepinephrine reuptake inhibition, approved by US FDA for treating moderate to severe acute pain in adults more than 18 years of age. Sugammadex, a novel selective relaxant binding agent to reverse steroidal neuromuscular blockers is recently approved by the European Union. Gantacurium, a rapid and ultra short acting non depolarizing neuromuscular blocker, inactivated rapidly by the adduction of non essential amino acid cysteine to the gantacurium molecule is in clinical trials. Remimazolam is a new drug in clinical trials that has a rapid onset of action like midazolam and is metabolized by non specific tissue esterases like remifentanil and expected to have a promising future. Liposomal Bupivacaine is approved by FDA in October 2011 that uses bupivacaine in liposomal vesicles to extend the duration of analgesia upto 72 hours and reduces the opioid use in the post operative period. Methoxy carbonyl carboetomidate is in clinical trials that combines the advantages of MOC etomidate and carboetomidate. Hence anaesthesiology is marching towards a bright pathway with new soft drugs coming up making not only anaesthesiology soft but also pharmacology.

Comparison of Analgesic Efficacy of Tramadol and Tapentadol in Impacted Mandibular Third Molar Surgery: A Randomized, Double Blind Clinical Study.

Introduction: The chronological age of eruption of third molars is between 18 and 24 years with wide variation in the eruption time. The eruption failure being very common makes the extraction of impacted third molars one of the most frequent surgical procedures in the maxillofacial region. Materials and Methods: A study was conducted on one hundred patients who visited the Department of Oral and Maxillofacial Surgery, Subbiah institute of Dental Sciences for the removal of impacted mandibular third molars to compare the analgesic efficacy of tramadol and tapentadol in patients undergoing surgical extraction of impacted mandibular molars. Patients were divided into two equal groups, group A and group B. Patients were randomly assigned in either treatment groups with an assigned code. Both patient and investigator were not aware of the drug code. Group A patients received 50mg tramadol and group B patients received 50mg tapentadol orally immediately after surgery and 12 hours after surgery. Results: VAS score of group A was 6.22±0.65 and group B was 5.92±0.97 at the end of 2 hours. VAS score of group A was 6.18±1.08 and group B was 5.76±1.25 at the end of 8 hours. VAS score of group A was 6.36±0.96 and group B was 6.46±1.2 at the end of 12 hours. VAS score of group A was 6.2±1.2 and group B was 6.2±1.47 at the end of 24 hours. VAS scores, statistically were found to be in significant between two groups. All patients had moderate pain at the end of 2 hours, 92% of group A and 96% of group B patients had moderate pain at the end of 8 hours. Mild pain was noted in most patients around 24 hours according to the categorical pain scale. Conclusion: A study was conducted to compare the analgesic efficacy of tramadol and tapentadol on patients undergoing third molar surgeries. The results of the statistical analysis suggested that Tramadol and Tapentadol are effective in managing postoperative pain and neither of the drugs mentioned above were superior to other.

A simple method for quantification of tapentadol in dog plasma by liquid chromatography-tandem mass spectrometry and evaluation of the effects of conjugated metabolites on tapentadol / 药学学报

Tapentadol is a novel drug of opioid pain reliever, which is extensively metabolized primarily through conjugation. Tapentadol glucuronide and tapentadol sulfate are major drug-related metabolites in circulation. The objectives of this study were to develop a simple and rapid method to determine tapentadol and evaluate the effects of conjugated metabolites on tapentadol quantification using liquid chromatography with tandem mass spectrometry in dog plasma. The analyte and tramadol (IS) were extracted from plasma by protein precipitation with methanol, and chromatographied on a XDB C18 (50 mm×4.6 mm, 1.8 μm) column using a mobile phase of methanol and 5 mmol·L-1 ammonium acetate (0.01% ammonia). Mass spectrometric detection was performed using the m/z 222→121 transition for tapentadol and the m/z 264→58 transition for the internal standard tramadol, the m/z 398→m/z 121 transition for glucuronides conjugate and the m/z 302→m/z 222 transition for sulfate conjugate. Conjugated metabolites could undergo in-source conversion to generate an ion that interfered the quantification of tapentadol. Chromatographic separation was achieved to elimination interferences due to in-source conversion of the conjugated metabolites. The standard curves were demonstrated to be linear in the range of 0.100 to 20.0 ng·mL-1 for tapentadol. The intra-and inter-day precisions were within 5.1%, and accuracy ranged from -3.2% to 0. This method was successfully applied to the pharmacokinetics of tapentadol hydrochloride sustained release tablets in Beagle dogs.

A Multicenter, Open-label Study of Tapentadol Extended-release Tablets in Opioid-naïve and Opioid-switching Subjects with Moderate to Severe Cancer Pain

The present multicenter, open-label study evaluated the efficacy and safety of tapentadol ER administered at 50 mg/day to 500 mg/day in opioid-naive and opioid-switching subjects with moderate to severe cancer pain. For opioid-naive subjects, the initial dose was tapentadol ER 50 mg/day. For opioid-switching subjects, the initial dose was determined depending on previously used opioid and was dose-adjusted for each subject. The study design consists of two parts of titration period and maintenance period to which a patient who achieves dose adjustment can proceed. The percentage of subjects achieving dose adjustment in the titration period was 93.3% for opioid-naive subjects and 80.6% for opioid-switching subjects. The percentage of subjects who maintained adequate analgesia throughout the maintenance period (primary endpoint) was 89.7% for opioid-naive subjects and 92.9% for opioid-switching subjects. The most frequent adverse events were were nausea, vomiting, somnolence, and constipation, all of which were commonly reported with the use of opioids. These findings showed that tapentadol ER was well tolerated in the dose range of 50 mg/day to 500 mg/day.

Tapenatadol Induced Hyperactive Delirium: Report of One Case Successfully Managed with Opioid-switching

Introduction: This report describes a case of hyperactive delirium induced by tapenatadol whose symptoms were successfully managed with opioid-switching to oxycodon. Case: A 67-year-old female, who had been treated with chemotherapy for malignant thymoma, had to stop chemotherapy because of her carcinomatous pericarditis. Tapentadol 200 mg per day was administrated for her unbearable chest wall tumor invasion-related somatic pain. After a while, insomnia, visual hallucination, thought disturbance, and attention disturbance were appeared. We diagnosed as hyperactive delirium. Because her somatic pain was favorably controlled by tapentadol, we additionally administered quetiapine 50 mg per day instead of replacing tapentadol. Unfortunately, quetiapine was not effective for the delirium. We therefore switched opioids from tapentadol to oxycodon. The delirium was remitted soon after the switching without relapsing of the pain. Conclusion: Tapentadaol reportedly induce hyperactive delirium via its noradrenaline reuptake inhibitory action. This case suggests that switching tapenatadol to other opioid could be an effective option for opioid induced delirium.

8-week Safety Profile of Tapentadol Extended Release Tablets Switched from Other Opioids for Well-controlled, Moderate to Severe, Chronic Malignant Tumor-related Pain: Constipation, Nausea, Vomiting and Somnolence

It was previously reported the safety and efficacy of oral tapentadol ER switched from other opioids for 8 weeks in subjects with moderate to severe cancer pain, who received opioid analgesics prior to study participation. All treatment emergent adverse events were evaluated in previous safety analysis. In this report, the incidence and timing of opioid specific adverse events related to tapentadol administration were analyzed and compared with those of morphine SR as a reference. Fifty subjects each was randomized to the tapentadol ER group and the morphine SR group. The incidences of major adverse events that are considered related to treatment in the tapentadol ER group and the morphine SR group were nausea (8.0%, 14.0%), vomiting (2.0%, 24.0%), constipation (8.0%, 20.0%), and somnolence (8.0%, 18.0%), the incidences of these events were lower in the tapentadol ER group. These results suggest that tapentadol ER is a orally opioid which has well safety profiles, and is a new option of cancer pain therapy.

Retrospective Analysis Based on Clinical Experience of Tapentadol in Cancer Pain Management

Objective: To examine the clinical significance of an opioid, tapentadol, for cancer pain relief including its analgesic effects and indications based on our clinical experience. Methods: We retrospectively studied 31 patients receiving tapentadol in our hospital. Results: In 19 successfully treated patients, the numerical rating scale (NRS) scores showed a significant decrease in pain, and the doses at the start and completion of administration were 73.7±25.6 mg (morphine equivalent dose: 30 mg or less) and 125±49.3 mg, respectively. Six successfully treated patients showed improvement of gastrointestinal symptoms. The results of the comparison between successfully and unsuccessfully treated patients suggested titration to be difficult in patients with mixture of somatic pain and neuropathic pain. Conclusion: Based on our clinical experience, we consider tapentadol to be easy to use during the introductory period after treatment with non-opioids or low-dose opioids.

Method Development for Quantification of Donor-Acceptor Complexes of Alverine Citrate and Tapentadol by Visible Spectrophotometry.

In this present work two colorimetric methods were developed based on donor-acceptor complexes of alverine citrate (ALV) and tapentadol (TAP) with cobalt thiocyanate. These methods were developed on Perkin Elmer LAMBDA 25 UV–VIS spectrophotometer with 1cm quartz cells. The colored species formed are the coordination complexes of the drugs (electron donor) and the central metal atom of cobalt thiocyanate (electron acceptor) which is extractable into nitrobenzene from aqueous solution. The reaction conditions were optimized and validated to achieve maximum colour intensity. The colored complexes show maximum absorbance measured at 625 nm for both ALV and TAP. The absorbances were found to increase linearly with an increase in concentration which was corroborated by the calculated regression coefficients (0.9998-0.9999). Linearity was obeyed in the range of 100-600 μg/ml for both ALV and TAP, respectively. The molar absorptivity, sandell’s sensitivity, LOD, LOQ and other validation parameters have been evaluated extensively as per ICH guidelines and all the parameters were found within the acceptance criteria for both methods. The proposed methods were proven to be more accurate, simple, precise and rapid by statistical validation of recovery studies and could be suitable for regular analysis.

Comparison of tapentadol with tramadol for analgesia after cardiac surgery.

Background: Tapentadol is a relatively new analgesic. We decided to compare it with tramadol for their various effects after cardiac surgery. Setting: A study in a tertiary care hospital. Materials and Methods: Sixty adults undergoing cardiac surgery were divided into 2 groups of 30 each by computerized random allotment (Group X = tapentadol 50 mg oral and Group Y = tramadol 100 mg oral). Informed Consent and Institutional Ethics Committee approval were obtained. The patients were given either drug X or drug Y after extubation in this single blinded study, wherein the data collectors and analyzers were blinded to the study. All patients received oral paracetamol qds and either drug X or drug Y tds. The pain score was noted on a Visual Analog Scale before each drug dose, 3 h later and on coughing. Heart rate, respiratory rate, and blood pressure were recorded before the drug dose and 3 h later. Postoperative nausea or vomiting (PONV), temperature, and modified Glasgow Coma Scale readings were recorded. The above readings were obtained for 6 doses (up to 48 h after extubation). Statistics: t‑test, Pearson Chi‑square test, Fisher exact test, and Mantel–Haenszel test were used for statistics. Results: Tapentadol group patients had significantly better analgesia 3 h after the drug and “on coughing” than tramadol group. The difference in their effects on blood creatinine levels, temperature, hemodynamics, oxygen saturation, and respiratory rate were not clinically significant. Tapentadol produced lesser drowsiness and lesser vomiting than tramadol. Conclusions: Tapentadol, due to its norepinephrine reuptake inhibition properties, in addition to mu agonist, is a better analgesic than tramadol and has lesser PONV.

Pain management of malignant psoas syndrome with tapentadol and lumbar plexus blockade：A case report

Malignant psoas syndrome（MPS）is one of challenging cancer pain states, which is often refractory to conventional analgesic therapy. We report a case of a 67 years-old female patient suffering from left MPS caused by lumbar paravertebral malignant lymphoma. Tapentadol, a dual action analgesic, has relatively low affinity to mu-opioid receptor and provoke noradrenergic reuptake inhibition simultaneously. Neuropathic component is predominant in MPS. Tapentadol is reported to be a drug of choice for the treatment of neuropathic pain. Psoas compartment blockade is a choice of interventions to relieve severe thigh pain caused by a lesion of lumbar plexus which exists in a compartment between psoas and quadratus lumborum muscles. Pain and numbness in the affected left thigh region of the patient were well managed by opioid switching from oxycodone to tapentadol and supplemental psoas compartment blocks with a local anesthetic and dexamethasone. The activity of daily life and quality of life of the patient were dramatically improved. Tapentadol with psoas compartment blockade may be efficacious for the management of MPS.

A comparative study of oral tapentadol with thoracic epidural analgesia versus intravenous tramadol and paracetamol combination for postoperative analgesia in off pump CABG.

Background: Accurate management of post operative pain is quite impossible with single drug therapy approach. For this, our aim was to combine use of tapentadol tablet orally along with thoracic epidural in comparison with intravenous combined use of tramadol, paracetamol and diclofenac for postoperative analgesia in case CABG patients. Methods: 60 patients of CABG (Coronary Artery Bypass Surgery) randomly and equally divided into two groups. Group TTE (Tab. Tapentadol -Thoracic Epidural, n=30) were given oral Tablet Tapentadol through NG (Nasogastric) tube at the time of shifting the patient from Operation Theatre to postoperative ward along with Tramadol through Thoracic epidural catheter. In Group TPD (Tramadol -Paracetamol -Diclofenac, n=30) were given Inj. Tramadol, Inj. Paracetamol IV at time of shifting of patient. If pain score is too high (>4) then additional analgesia were given with Diclofenac only if preoperative renal and hepatic profile were normal. Patients were monitored for duration of rescue analgesia, total no. of doses of analgesics in first 72 hours, total consumption of analgesics and response to physiotherapy. Results: Duration of need of rescue analgesia was significantly longer in TTE group (p<0.05) while total no. of rescue doses were significantly more in group TPD (p<0.001). We also observed that patients of TTE group were recovered earlier, response to chest physiotherapy was significantly better and thus reduces their total length of ICU stay (p<0.05). Conclusions: Our study concludes that Tapentadol with Thoracic epidural is very much effective as a multimodal analgesia approach in controlling acute postoperative pain after CABG. Tapentadol is quite a newer drug so its usefulness for other patients and different surgeries is still to be debated.

Evaluation of analgesic effect of tapentadol, a central novel analgesic versus tramadol, a widely used opioid analgesic in treatment of low back pain: a randomized controlled trial.

Background: The objective of the study was to compare efficacy and tolerability (safety) of tapentadol with tramadol in the treatment of low back pain. Methods: The study was a prospective, randomized, single blinded, total 102 patients are recruited for study in which 44 patients are prescribed (50mgtwice daily) tapentadol and 58 patients prescribed (50mg twice daily) tramadol for 4 weeks. Follow-up was done on days 7, 14, 28 and 4 week after stoppage of treatment. Assessment of improvement were performed by Indian Health Assessment Questionnaire Disability Index (Indian HAQDI), Visual Analogue Scale (VAS), Numerical Rating Scale (NRS) and measurement of Pain Relief Rate (PRR). Adverse events were recorded. Results: Scores in Indian HAQDI, VAS and NRS improved significantly in both groups in the last visit but more so with tapentadol. PRR was reasonably higher with tapentadol [27(n=44)61.36%] patients experiencing significant to complete pain relief at the end of the study, compared to tramadol [25(n=58) 43.10%]. Adverse effects was less in tapentadol group [15(n=44)34.09%] versus 33(n=58)56.89%], p<0.05]. Conclusion: Tapentadol has better sustained efficacy and tolerability than tramadol in low back pain.