Tapentadol

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Ilona Steigerwald - One of the best experts on this subject based on the ideXlab platform.

  • effectiveness of Tapentadol prolonged release pr compared with oxycodone naloxone pr for the management of severe chronic low back pain with a neuropathic component a randomized controlled open label phase 3b 4 study
    Pain Practice, 2016
    Co-Authors: Ralf Baron, Dietmar Falke, E Martinmola, Matthias Muller, Rudolf Likar, Francisco J Blanco, Lieven Kennes, Ilona Steigerwald
    Abstract:

    Objective To evaluate the effectiveness of Tapentadol prolonged release (PR) vs. oxycodone/naloxone PR in non–opioid-pretreated patients with severe chronic low back pain with a neuropathic pain component. Methods Eligible patients (average pain intensity [numerical rating scale-3 (NRS-3)] ≥6; painDETECT positive/unclear) were randomized to twice-daily Tapentadol PR 50 mg or oxycodone/naloxone PR 10 mg/5 mg. After a 21-day titration (maximum twice-daily doses: Tapentadol PR 250 mg, or oxycodone/naloxone PR 40 mg/20 mg plus oxycodone PR 10 mg), target doses were continued for 9 weeks. The primary effectiveness endpoint was the change in NRS-3 from baseline to final evaluation; the exact repeated confidence interval (RCI) for Tapentadol PR minus oxycodone/naloxone PR was used to establish noninferiority (upper limit <1.3) and superiority (confirmatory analyses). Results For the primary effectiveness endpoint, Tapentadol PR was noninferior to oxycodone/naloxone PR (97.5% RCI: [−1.820, −0.184]; P < 0.001). This exact RCI also yielded evidence of superiority for Tapentadol PR vs. oxycodone/naloxone PR (significantly greater reduction in pain intensity; P = 0.003). Improvements (baseline to final evaluation) in painDETECT and Neuropathic Pain Symptom Inventory scores were significantly greater with Tapentadol PR vs. oxycodone/naloxone PR (all P ≤ 0.005). Conclusions The study was formally shown to be positive and demonstrated, in the primary effectiveness endpoint, the noninferiority for Tapentadol PR vs. oxycodone/naloxone PR. The effectiveness of Tapentadol PR was superior to that of oxycodone/naloxone PR by means of clinical relevance and statistical significance (confirmatory evidence of superiority). Tapentadol PR was associated with significantly greater improvements in neuropathic pain-related symptoms and global health status than oxycodone/naloxone PR and with a significantly better gastrointestinal tolerability profile. Tapentadol PR may be considered a first-line option for managing severe chronic low back pain with a neuropathic pain component.

  • tolerability safety and quality of life with Tapentadol prolonged release pr compared with oxycodone naloxone pr in patients with severe chronic low back pain with a neuropathic component a randomized controlled open label phase 3b 4 trial
    Pain Practice, 2016
    Co-Authors: Ralf Baron, Dietmar Falke, Matthias Muller, Lieven Kennes, Janpeter Jansen, Andreas Binder, Manuel Pombosuarez, Ilona Steigerwald
    Abstract:

    Objective To evaluate tolerability, safety, and quality-of-life outcomes in non-opioid-pretreated patients with severe chronic low back pain with a neuropathic component receiving Tapentadol PR vs. oxycodone/naloxone PR. Methods Eligible patients (average pain intensity [numerical rating scale] ≥ 6; painDETECT positive/unclear ratings) were randomized to twice-daily Tapentadol PR 50 mg or oxycodone/naloxone PR 10 mg/5 mg. After a 21-day titration (maximum twice-daily doses: Tapentadol PR 250 mg, or oxycodone/naloxone PR 40 mg/20 mg plus oxycodone PR 10 mg), target doses were continued for 9 weeks. Change in the Patient Assessment of Constipation Symptoms (PAC-SYM) total score from baseline to final evaluation was a primary endpoint. Results For the primary tolerability-related endpoint, the 97.5% exact repeated confidence interval for Tapentadol PR minus oxycodone/naloxone PR for the PAC-SYM total score was [−0.259, 0.121], showing noninferiority (upper limit < 0.7). Incidences of constipation and vomiting were significantly lower with Tapentadol PR than oxycodone/naloxone PR (P ≤ 0.045). Confirmatory superiority based on formal noninferiority was shown for the primary effectiveness endpoint (change from baseline to final evaluation in pain intensity) for Tapentadol PR vs. oxycodone/naloxone PR (presented separately). Improvements in the Short Form-12 physical component summary and EuroQol-5 Dimension health status index and health state assessment were significantly greater with Tapentadol PR vs. oxycodone/naloxone PR (P ≤ 0.024). Conclusions Tapentadol PR had a minimal impact on bowel function (noninferior to oxycodone/naloxone PR) and, along with superior effectiveness (presented separately), was associated with significantly lower incidences of constipation and vomiting and significant improvements in quality-of-life measures vs. oxycodone/naloxone PR.

  • effectiveness and safety of Tapentadol prolonged release pr versus a combination of Tapentadol pr and pregabalin for the management of severe chronic low back pain with a neuropathic component a randomized double blind phase 3b study
    Pain Practice, 2015
    Co-Authors: Ralf Baron, Dietmar Falke, E Martinmola, Matthias Muller, Cecile Dubois, Ilona Steigerwald
    Abstract:

    Objective To evaluate the effectiveness and tolerability of Tapentadol PR monotherapy versus Tapentadol PR/pregabalin combination therapy for severe, chronic low back pain with a neuropathic component. Methods Eligible patients had painDETECT “unclear” or “positive” ratings and average pain intensity ≥ 6 (11-point NRS-3 [average 3-day pain intensity]) at baseline. Patients were titrated to Tapentadol PR 300 mg/day over 3 weeks. Patients with ≥ 1-point decrease in pain intensity and average pain intensity ≥ 4 were randomized to Tapentadol PR (500 mg/day) or Tapentadol PR (300 mg/day)/pregabalin (300 mg/day) during an 8-week comparative period. Results In the per-protocol population (n = 288), the effectiveness of Tapentadol PR was clinically and statistically comparable to Tapentadol PR/pregabalin based on the change in pain intensity from randomization to final evaluation (LOCF; LSMD [95% CI], −0.066 [−0.57, 0.43]; P < 0.0001 for noninferiority). Neuropathic pain and quality-of-life measures improved significantly in both groups. Tolerability was good in both groups, in line with prior trials in the high dose range of 500 mg/day for Tapentadol PR monotherapy, and favorable compared with historical combination trials of strong opioids and anticonvulsants for combination therapy. The incidence of the composite of dizziness and/or somnolence was significantly lower with Tapentadol PR (16.9%) than Tapentadol PR/pregabalin (27.0%; P = 0.0302). Conclusions Tapentadol PR 500 mg is associated with comparable improvements in pain intensity and quality-of-life measures to Tapentadol PR 300 mg/pregabalin 300 mg, with improved central nervous system tolerability, suggesting that Tapentadol PR monotherapy may offer a favorable treatment option for severe low back pain with a neuropathic component.

  • Practical considerations for the use of Tapentadol prolonged release for the management of severe chronic pain.
    Clinical therapeutics, 2014
    Co-Authors: Manuel J. Sánchez Del Águila, Michael Schenk, Kai-uwe Kern, Tanja Drost, Ilona Steigerwald
    Abstract:

    Abstract Purpose Chronic pain is often challenging to address appropriately. Although patients with severe chronic pain may respond to treatment with an opioid analgesic, opioids are often associated with adverse effects that may lead patients to disrupt or discontinue therapy. In addition, opioid analgesics alone may not be effective for all types of chronic pain, including neuropathic pain. Tapentadol prolonged release (PR), a centrally acting analgesic with 2 mechanisms of action (μ-opioid receptor agonism and noradrenaline reuptake inhibition), provides strong and reliable analgesia across a range of indications, including nociceptive, neuropathic, and mixed types of chronic pain, and is associated with an improved tolerability profile relative to classic opioid analgesics. The purpose of this article was to review the recent literature on different aspects related to the clinical use of Tapentadol PR. Methods A review was conducted of the current literature and relevant unpublished data on initiation and titration of Tapentadol PR, switching from classic strong opioids, risk of withdrawal after discontinuation, long-term treatment, coadministration with other medications, and risk of abuse and diversion. Findings Tapentadol PR may provide clinically meaningful benefits over classic opioid analgesics, including ease of initiating and titrating Tapentadol PR treatment in opioid-naive and opioid-experienced patients, low risk of withdrawal after cessation of Tapentadol PR therapy, a favorable pharmacokinetic profile (allowing for coadministration with other medications) of Tapentadol PR, and low potential for Tapentadol PR abuse. Implications The broad analgesic efficacy of Tapentadol PR may simplify chronic pain management by allowing for the treatment of different types of pain with a single analgesic. In addition, Tapentadol is associated with a low risk of pharmacokinetic interactions, which permits its use in patients taking multiple medications. Furthermore, the favorable tolerability profile of Tapentadol PR may result in improved patient compliance and allow for easy titration and rotation from previous strong opioids.

  • Driving Ability in Patients with Severe Chronic Low Back or Osteoarthritis Knee Pain on Stable Treatment with Tapentadol Prolonged Release: A Multicenter, Open-label, Phase 3b Trial
    Pain and Therapy, 2014
    Co-Authors: Rainer Sabatowski, Rüdiger Scharnagel, Anne Gyllensvärd, Ilona Steigerwald
    Abstract:

    Introduction Strong centrally acting analgesics, including Tapentadol prolonged release (PR), have demonstrated efficacy for the management of non-malignant, chronic pain. Maintaining patient independence, including the ability to drive safely, is a key goal of long-term analgesic therapy. This multicenter, open-label, phase 3b trial evaluated the effects of Tapentadol PR on driving ability. Methods This study included patients who had completed previous Tapentadol PR trials for severe low back or osteoarthritis pain. After at least 6 weeks of dose stability, patients continued taking Tapentadol PR (50–250 mg twice daily) and could take supplemental immediate-release Tapentadol 50 mg, except on the day before or day of the driving test (before the test). Pain intensity was assessed using an 11-point numerical rating scale. The Vienna Test System-Traffic Plus was used to assess cognitive and psychomotor function. The key surrogate parameter for driving ability was a global judgment based on 6 battery tests. Results Thirty-eight patients enrolled and completed the trial, and 35 patients completed all 6 tests. Pain scores remained unchanged from enrollment to final visit [mean (standard deviation) change, –0.2 (1.0)]. Approximately two-thirds [65.7% (23/35)] of patients were classified as fit to drive based on the global judgment of driving-specific ability [34.3% (12/35) not fit to drive]. Total daily Tapentadol PR dose (>200 vs. ≤200 mg/day) did not affect global judgment of driving ability ( P  = 0.4885). Two adverse events (considered unrelated to study drug) were reported. Conclusion Results suggest that most patients receiving a stable dose of Tapentadol PR for severe, chronic pain would be able to drive, consistent with earlier studies evaluating stable treatment with strong opioids. Study design limitations and needs for individual patient assessment must be considered in clinical practice.

Ralf Baron - One of the best experts on this subject based on the ideXlab platform.

  • A Novel Algorithm to Identify Predictors of Treatment Response: Tapentadol Monotherapy or Tapentadol/Pregabalin Combination Therapy in Chronic Low Back Pain?
    Frontiers in neurology, 2019
    Co-Authors: Jan Carl Otto, Julia Forstenpointner, Juliane Sachau, Philipp Hüllemann, Martin Hukauf, Thomas Keller, Janne Gierthmühlen, Ralf Baron
    Abstract:

    Purpose: High dose monotherapies or drug combinations are used to achieve sufficient analgesia for the treatment of severe chronic low back pain, before invasive therapy options are considered. In order to demonstrate an alternative for an empirical treatment approach, the authors' primary aim was to present an algorithm for the objective identification of treatment predictors. Additionally, the study identified baseline-characteristics in chronic low back pain patients prior to Tapentadol PR treatment, as well as scrutinized those patients, either benefitting from a medium/high dose Tapentadol PR monotherapy or a combination therapy (medium dose Tapentadol PR + pregabalin). Patients and Methods: The statistical approach included data of a previously published randomized, double blind, phase 3b study which compared the effectiveness and safety of Tapentadol PR vs. a combination of Tapentadol PR and pregabalin. In total, 46 clinical parameters were included in the statistical prediction models which were applied separately either to 50 patients who already responded well during the titration period (i.e., medium dose Tapentadol PR) or to 261 patients with in the comparative treatment period [i.e., monotherapy (high dose Tapentadol PR) or combination therapy (medium dose Tapentadol PR/pregabalin)]. Results: The first statistical model identified three co-variables (NRS-3, PDQ, SQ) with predictive effects on patients responding well ("optimal responders") to a medium dose Tapentadol PR titration. Those patients presented low baseline pain intensity scores, good sleep quality and high painDETECT scores. The second statistical model identified eight co-variables (PDQ, numbness, SF-12 MCS, SF-12 PCS, VAS, HADS-A, HADS-D, SQ) with predictive effects on patients responding to high dose Tapentadol PR monotherapy vs. a combination therapy (Tapentadol PR + pregabalin). The high dose Tapentadol PR responders indicated high painDETECT scores, little numbness and a good mental health status. Whereas, the combination therapy (Tapentadol PR + pregabalin) responders were characterized by severe sleep disturbances and little anxiety. Conclusion: The statistical analysis characterized chronic low back pain patients and identified factors contributing to a treatment response. Thus, this retrospective statistical algorithm represents an elegant method, which may contribute to future strategies toward a more individualized and improved mechanism based pain therapy.

  • Tapentadol prolonged release for chronic pain a review of clinical trials and 5 years of routine clinical practice data
    Pain Practice, 2017
    Co-Authors: Ralf Baron, Kai-uwe Kern, L H J Eberhart, Stefan Regner, Roman Rolke, Christian Simanski, Thomas R Tolle
    Abstract:

    Tapentadol prolonged release (PR) for the treatment of moderate to severe chronic pain combines 2 modes of action. These are μ-opioid receptor agonism and noradrenaline reuptake inhibition in a single molecule that allow higher analgesic potency through modulation of different pharmacological targets within the pain transmitting systems. At the same time, this can also serve as a clue for modulation of different pain-generating mechanisms according to nociceptive, neuropathic, or mixed pain conditions. Tapentadol PR has now been on the market for 5 years, with over 4.6 million people treated worldwide. A panel of pain specialists convened in Germany to review the clinical program and to discuss the role of Tapentadol PR in the management of chronic pain. The clinical study program demonstrated effective and generally well-tolerated treatment for up to 2 years in a broad range of chronic pain conditions, including those with neuropathic pain components. This was confirmed in routine clinical practice observations. Head-to-head studies with World Health Organization (WHO) III opioids such as oxycodone controlled release and oxycodone/naloxone PR showed at least comparable pain relief in the treatment of moderate-to-severe musculoskeletal pain. Rotation from poorly tolerated WHO III opioids to Tapentadol PR provided effective pain relief and better symptom control for musculoskeletal pain compared to previous medication. Functionality, health status and quality of life also improved under Tapentadol PR treatment. The gastrointestinal tolerability profile was more favorable compared to other tested WHO III opioids. Tapentadol PR has a good safety profile and no evidence of acquired tolerance from the long-term data so far collected. Overall, Tapentadol PR represents an effective and generally well-tolerated alternative to "classical" opioidergic drugs.

  • effectiveness of Tapentadol prolonged release pr compared with oxycodone naloxone pr for the management of severe chronic low back pain with a neuropathic component a randomized controlled open label phase 3b 4 study
    Pain Practice, 2016
    Co-Authors: Ralf Baron, Dietmar Falke, E Martinmola, Matthias Muller, Rudolf Likar, Francisco J Blanco, Lieven Kennes, Ilona Steigerwald
    Abstract:

    Objective To evaluate the effectiveness of Tapentadol prolonged release (PR) vs. oxycodone/naloxone PR in non–opioid-pretreated patients with severe chronic low back pain with a neuropathic pain component. Methods Eligible patients (average pain intensity [numerical rating scale-3 (NRS-3)] ≥6; painDETECT positive/unclear) were randomized to twice-daily Tapentadol PR 50 mg or oxycodone/naloxone PR 10 mg/5 mg. After a 21-day titration (maximum twice-daily doses: Tapentadol PR 250 mg, or oxycodone/naloxone PR 40 mg/20 mg plus oxycodone PR 10 mg), target doses were continued for 9 weeks. The primary effectiveness endpoint was the change in NRS-3 from baseline to final evaluation; the exact repeated confidence interval (RCI) for Tapentadol PR minus oxycodone/naloxone PR was used to establish noninferiority (upper limit <1.3) and superiority (confirmatory analyses). Results For the primary effectiveness endpoint, Tapentadol PR was noninferior to oxycodone/naloxone PR (97.5% RCI: [−1.820, −0.184]; P < 0.001). This exact RCI also yielded evidence of superiority for Tapentadol PR vs. oxycodone/naloxone PR (significantly greater reduction in pain intensity; P = 0.003). Improvements (baseline to final evaluation) in painDETECT and Neuropathic Pain Symptom Inventory scores were significantly greater with Tapentadol PR vs. oxycodone/naloxone PR (all P ≤ 0.005). Conclusions The study was formally shown to be positive and demonstrated, in the primary effectiveness endpoint, the noninferiority for Tapentadol PR vs. oxycodone/naloxone PR. The effectiveness of Tapentadol PR was superior to that of oxycodone/naloxone PR by means of clinical relevance and statistical significance (confirmatory evidence of superiority). Tapentadol PR was associated with significantly greater improvements in neuropathic pain-related symptoms and global health status than oxycodone/naloxone PR and with a significantly better gastrointestinal tolerability profile. Tapentadol PR may be considered a first-line option for managing severe chronic low back pain with a neuropathic pain component.

  • tolerability safety and quality of life with Tapentadol prolonged release pr compared with oxycodone naloxone pr in patients with severe chronic low back pain with a neuropathic component a randomized controlled open label phase 3b 4 trial
    Pain Practice, 2016
    Co-Authors: Ralf Baron, Dietmar Falke, Matthias Muller, Lieven Kennes, Janpeter Jansen, Andreas Binder, Manuel Pombosuarez, Ilona Steigerwald
    Abstract:

    Objective To evaluate tolerability, safety, and quality-of-life outcomes in non-opioid-pretreated patients with severe chronic low back pain with a neuropathic component receiving Tapentadol PR vs. oxycodone/naloxone PR. Methods Eligible patients (average pain intensity [numerical rating scale] ≥ 6; painDETECT positive/unclear ratings) were randomized to twice-daily Tapentadol PR 50 mg or oxycodone/naloxone PR 10 mg/5 mg. After a 21-day titration (maximum twice-daily doses: Tapentadol PR 250 mg, or oxycodone/naloxone PR 40 mg/20 mg plus oxycodone PR 10 mg), target doses were continued for 9 weeks. Change in the Patient Assessment of Constipation Symptoms (PAC-SYM) total score from baseline to final evaluation was a primary endpoint. Results For the primary tolerability-related endpoint, the 97.5% exact repeated confidence interval for Tapentadol PR minus oxycodone/naloxone PR for the PAC-SYM total score was [−0.259, 0.121], showing noninferiority (upper limit < 0.7). Incidences of constipation and vomiting were significantly lower with Tapentadol PR than oxycodone/naloxone PR (P ≤ 0.045). Confirmatory superiority based on formal noninferiority was shown for the primary effectiveness endpoint (change from baseline to final evaluation in pain intensity) for Tapentadol PR vs. oxycodone/naloxone PR (presented separately). Improvements in the Short Form-12 physical component summary and EuroQol-5 Dimension health status index and health state assessment were significantly greater with Tapentadol PR vs. oxycodone/naloxone PR (P ≤ 0.024). Conclusions Tapentadol PR had a minimal impact on bowel function (noninferior to oxycodone/naloxone PR) and, along with superior effectiveness (presented separately), was associated with significantly lower incidences of constipation and vomiting and significant improvements in quality-of-life measures vs. oxycodone/naloxone PR.

  • effectiveness and safety of Tapentadol prolonged release pr versus a combination of Tapentadol pr and pregabalin for the management of severe chronic low back pain with a neuropathic component a randomized double blind phase 3b study
    Pain Practice, 2015
    Co-Authors: Ralf Baron, Dietmar Falke, E Martinmola, Matthias Muller, Cecile Dubois, Ilona Steigerwald
    Abstract:

    Objective To evaluate the effectiveness and tolerability of Tapentadol PR monotherapy versus Tapentadol PR/pregabalin combination therapy for severe, chronic low back pain with a neuropathic component. Methods Eligible patients had painDETECT “unclear” or “positive” ratings and average pain intensity ≥ 6 (11-point NRS-3 [average 3-day pain intensity]) at baseline. Patients were titrated to Tapentadol PR 300 mg/day over 3 weeks. Patients with ≥ 1-point decrease in pain intensity and average pain intensity ≥ 4 were randomized to Tapentadol PR (500 mg/day) or Tapentadol PR (300 mg/day)/pregabalin (300 mg/day) during an 8-week comparative period. Results In the per-protocol population (n = 288), the effectiveness of Tapentadol PR was clinically and statistically comparable to Tapentadol PR/pregabalin based on the change in pain intensity from randomization to final evaluation (LOCF; LSMD [95% CI], −0.066 [−0.57, 0.43]; P < 0.0001 for noninferiority). Neuropathic pain and quality-of-life measures improved significantly in both groups. Tolerability was good in both groups, in line with prior trials in the high dose range of 500 mg/day for Tapentadol PR monotherapy, and favorable compared with historical combination trials of strong opioids and anticonvulsants for combination therapy. The incidence of the composite of dizziness and/or somnolence was significantly lower with Tapentadol PR (16.9%) than Tapentadol PR/pregabalin (27.0%; P = 0.0302). Conclusions Tapentadol PR 500 mg is associated with comparable improvements in pain intensity and quality-of-life measures to Tapentadol PR 300 mg/pregabalin 300 mg, with improved central nervous system tolerability, suggesting that Tapentadol PR monotherapy may offer a favorable treatment option for severe low back pain with a neuropathic component.

Christine Rauschkolb - One of the best experts on this subject based on the ideXlab platform.

  • long term safety and efficacy of Tapentadol extended release following up to 2 years of treatment in patients with moderate to severe chronic pain results of an open label extension trial
    Clinical Therapeutics, 2015
    Co-Authors: Robert Buynak, Christine Rauschkolb, Stephen A Rappaport, Kevin Rod, Pierre Arsenault, Fabian Heisig, M. Etropolski
    Abstract:

    Abstract Purpose Tapentadol extended release (ER) has demonstrated efficacy and safety for the management of moderate to severe, chronic pain in adults. This study evaluated the long-term safety and tolerability of Tapentadol ER in patients with chronic osteoarthritis or low back pain. Methods Patients were enrolled in this 1-year, open-label extension study after completing one of two 15-week, placebo-controlled studies of Tapentadol ER and oxycodone controlled release (CR) for osteoarthritis knee pain (NCT00421928) or low back pain (NCT00449176), a 7-week crossover study between Tapentadol immediate release and Tapentadol ER for low back pain (NCT00594516), or a 1-year safety study of Tapentadol ER and oxycodone CR for osteoarthritis or low back pain (NCT00361504). After titrating the drug to an optimal dose, patients received Tapentadol ER (100–250 mg BID) for up to 1 year (after finishing treatment in the preceding studies); patients who were previously treated with Tapentadol ER in the 1-year safety study received Tapentadol ER continuously for up to 2 years in total. Findings Of the 1,154 patients in the safety population, 82.7% were aged >65 years and 57.9% were female; 50.1% had mild baseline pain intensity. Mean (SD) pain intensity scores (11-point numerical rating scale) were 3.9 (2.38) at baseline (end of preceding study) and 3.7 (2.42) at end point, indicating that pain relief was maintained during the extension study. Improvements in measures of quality of life (eg, EuroQol-5 Dimension and the 36-item Short Form Health Survey [SF-36]) health status questionnaires) achieved during the preceding studies were maintained during the open-label extension study. Tapentadol ER was associated with a safety and tolerability profile comparable to that observed in the preceding studies. The most common treatment-emergent adverse events (incidence ≥10%; n=1154) were headache (13.1%), nausea (11.8%), and constipation (11.1%). Similar efficacy and tolerability results were shown for patients who received up to 2 years of Tapentadol ER treatment. Implications Pain relief and improvements in quality of life achieved during the preceding studies were maintained throughout this extension study, during which Tapentadol ER was well tolerated for the long-term treatment of chronic osteoarthritis or low back pain over up to 2 years of treatment. (ClinicalTrials.gov identifier: NCT00487435.)

  • Comparable efficacy and superior gastrointestinal tolerability (nausea, vomiting, constipation) of Tapentadol compared with oxycodone hydrochloride
    Advances in Therapy, 2011
    Co-Authors: Mila Etropolski, Kathleen Kelly, Akiko Okamoto, Christine Rauschkolb
    Abstract:

    Introduction Two randomized, double-blind, placebo-controlled studies in acute and chronic pain treatment, powered to assess noninferiority of the efficacy of Tapentadol immediate release (IR) (50 mg, 75 mg) versus oxycodone hydrochloride (HCl) IR (10 mg), established comparable efficacy of Tapentadol IR with oxycodone HCl IR, and suggested Tapentadol IR’s improved gastrointestinal tolerability. The impact of these equianalgesic doses of Tapentadol and oxycodone HCl on bowel function and gastrointestinal tolerability was then directly assessed in the current study, using a validated bowel function diary to comprehensively assess opioid-induced constipation symptoms and outcomes.

  • long term safety and tolerability of Tapentadol extended release for the management of chronic low back pain or osteoarthritis pain
    Pain Practice, 2010
    Co-Authors: James E Wild, Mila Etropolski, Bernd Lange, Brigitte Kuperwasser, A Steup, Thomas Haufel, Stefan Grond, Jane S Gilbert, Bettyanne Mccann, Christine Rauschkolb
    Abstract:

    Background:  Tapentadol is a novel, centrally acting analgesic with 2 mechanisms of action: µ-opioid receptor agonism and norepinephrine reuptake inhibition. This randomized, open-label phase 3 study (ClinicalTrials.gov Identifier: NCT00361504) assessed the long-term safety and tolerability of Tapentadol extended release (ER) in patients with chronic knee or hip osteoarthritis pain or low back pain. Methods:  Patients were randomized 4:1 to receive controlled, adjustable, oral, twice-daily doses of Tapentadol ER (100 to 250 mg) or oxycodone HCl controlled release (CR; 20 to 50 mg) for up to 1 year. Efficacy evaluations included assessments at each study visit of average pain intensity (11-point numerical rating scale) over the preceding 24 hours. Treatment-emergent adverse events (TEAEs) and discontinuations were monitored throughout the study. Results:  A total of 1,117 patients received at least 1 dose of study drug. Mean (standard error) pain intensity scores in the Tapentadol ER and oxycodone CR groups, respectively, were 7.6 (0.05) and 7.6 (0.11) at baseline and decreased to 4.4 (0.09) and 4.5 (0.17) at endpoint. The overall incidence of TEAEs was 85.7% in the Tapentadol ER group and 90.6% in the oxycodone CR group. In the Tapentadol ER and oxycodone CR groups, respectively, TEAEs led to discontinuation in 22.1% and 36.8% of patients; gastrointestinal TEAEs led to discontinuation in 8.6% and 21.5% of patients. Conclusion:  Tapentadol ER (100 to 250 mg bid) was associated with better gastrointestinal tolerability than oxycodone HCl CR (20 to 50 mg bid) and provided sustainable relief of moderate to severe chronic knee or hip osteoarthritis or low back pain for up to 1 year.

  • Dose conversion between Tapentadol immediate and extended release for low back pain.
    Pain physician, 2010
    Co-Authors: Mila Etropolski, Akiko Okamoto, Douglas Y. Shapiro, Christine Rauschkolb
    Abstract:

    Background Tapentadol, a novel, centrally acting analgesic with 2 mechanisms of action (mu-opioid receptor agonism and norepinephrine reuptake inhibition), has been developed in an immediate-release (IR) and an extended-release (ER) formulation. Determination of the safety and equianalgesic ratios for conversion between formulations is important for physicians with patients taking Tapentadol IR who may want to switch to Tapentadol ER, or vice versa, for any reason. Objectives To test whether the total daily dose (TDD) of Tapentadol IR may be directly converted into a comparable TDD of Tapentadol ER, and vice versa, with equivalent efficacy and comparable safety. Study design Randomized, double-blind, 2-period (2 weeks each) crossover study. Setting Study centers (N = 13) in the United States. Methods Patients with moderate to severe chronic low back pain received Tapentadol IR 50, 75, or 100 mg every 4 or 6 hours (maximum TDD, 500 mg) during the 3-week open-label period to identify an optimal, stable dose of Tapentadol IR for each patient. Patients were then randomized in a 1:1 ratio to receive, during the first 2-week double-blind period, either the optimal dose of Tapentadol IR identified during the open-label period or a TDD of Tapentadol ER (100, 150, 200, or 250 mg bid) that was as close as possible to the TDD of Tapentadol IR from the open-label period. During a subsequent, 2-week double-blind period, patients received whichever formulation was not received during the first double-blind period. The primary endpoint was the mean average daily pain intensity (on an 11-point numerical rating scale) during the last 3 days of each double-blind treatment period. If the 95% confidence intervals (CIs) of the least squares mean difference between formulations were within the range of -2 to 2, the formulations were considered equivalent. Results Of the 88 patients who were randomized, 72 completed both double-blind treatments, and 60 were included in the per-protocol analysis. The mean (standard deviation [SD]) pain intensity score decreased from 7.3 (1.19) pre-treatment to 4.2 (2.13) after 3 weeks of open-label treatment with Tapentadol IR and remained constant throughout double-blind treatment (3.9 or 4.0 each week) for both formulations. The mean (SD) of the average pain intensity scores over the last 3 days of double-blind treatment was 3.9 (2.17) with Tapentadol IR and 4.0 (2.29) with Tapentadol ER, for an estimated difference of 0.1 (95% CI, -0.09 to 0.28). For both Tapentadol IR and Tapentadol ER, the median TDD administered was 300.0 mg, and acetaminophen was used by 39.5% and 45.2% of patients, respectively. The incidence of treatment-emergent adverse events during double-blind treatment was similar between the Tapentadol IR and Tapentadol ER groups. Limitations Use of rescue medication theoretically could have influenced pain measurements, but in practice, pain measurements did not differ between treatments. Conclusions Approximately equivalent TDDs of Tapentadol IR and Tapentadol ER provided equivalent analgesic efficacy for the relief of moderate to severe chronic low back pain and were similarly well tolerated, allowing for direct conversion between the 2 formulations. Clinical trial registration NCT00594516.

  • tolerability of Tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days a randomized double blind study
    Current Medical Research and Opinion, 2009
    Co-Authors: Martin Hale, A. Okamoto, David Upmalis, Claudia Lange, Christine Rauschkolb
    Abstract:

    ABSTRACTObjective: Tapentadol is a novel, centrally acting analgesic with two mechanisms of action, μ-opioid receptor agonism and norepinephrine reuptake inhibition, in a single molecule. This phase III, randomized, double-blind, active-controlled study evaluated the tolerability of Tapentadol immediate release (IR) and oxycodone IR for low back pain or osteoarthritis pain (hip or knee), using flexible dosing over 90 days.Methods: Patients (N = 878) were randomly assigned (4:1 ratio) to receive Tapentadol IR (50 or 100 mg, q4-6h, p.o.) or oxycodone IR (10 or 15 mg, q4-6h, p.o.). Tapentadol IR was evaluated for tolerability over 90 days, tolerability relative to oxycodone IR, withdrawal symptoms, and pain intensity. This study was not placebo-controlled, which limited efficacy evaluations.Results: In total, 849 intent-to-treat patients received Tapentadol IR (n = 679) or oxycodone IR (n = 170), and among these, 391 patients (57.6%) in the Tapentadol IR group and 86 patients (50.6%) in the oxycodone IR grou...

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  • First evaluation of Tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to
    Journal of pain research, 2019
    Co-Authors: Julia C. Finkel, Jutta Goldberg, Ronald Rosenburg, Jay Ariyawansa, Tao Sun, Rachel Ochs-ross, Peter Zannikos, Liping Zhang, M. Etropolski
    Abstract:

    Background This is the first clinical trial in the global pediatric clinical development program for the use of the analgesic Tapentadol in children and adolescents. Patients and methods This multicenter, open-label clinical trial investigated pharmacokinetics, safety and tolerability, and efficacy of Tapentadol and its major metabolite Tapentadol-O-glucuronide after administration of a single dose of Tapentadol oral solution (OS) in pediatric patients aged 6 to

  • Quantifying the Exposure of Tapentadol Extended Release in Japanese Patients with Cancer Pain and Bridging Tapentadol Pharmacokinetics Across Populations Using a Modeling Approach.
    Clinical drug investigation, 2016
    Co-Authors: Liping Zhang, Peter Zannikos, M. Etropolski, Xiaoyu Yan, Sayori Nobe, Partha Nandy
    Abstract:

    Background and Objectives Tapentadol extended release (ER) is approved for the management of chronic and acute pain in adults. There has been no report of Tapentadol ER pharmacokinetics in subjects with cancer pain. This analysis investigated Tapentadol ER pharmacokinetics in Japanese patients with cancer pain and bridged it with the pharmacokinetics in Japanese healthy subjects and Caucasian patients with cancer pain.

  • long term safety and efficacy of Tapentadol extended release following up to 2 years of treatment in patients with moderate to severe chronic pain results of an open label extension trial
    Clinical Therapeutics, 2015
    Co-Authors: Robert Buynak, Christine Rauschkolb, Stephen A Rappaport, Kevin Rod, Pierre Arsenault, Fabian Heisig, M. Etropolski
    Abstract:

    Abstract Purpose Tapentadol extended release (ER) has demonstrated efficacy and safety for the management of moderate to severe, chronic pain in adults. This study evaluated the long-term safety and tolerability of Tapentadol ER in patients with chronic osteoarthritis or low back pain. Methods Patients were enrolled in this 1-year, open-label extension study after completing one of two 15-week, placebo-controlled studies of Tapentadol ER and oxycodone controlled release (CR) for osteoarthritis knee pain (NCT00421928) or low back pain (NCT00449176), a 7-week crossover study between Tapentadol immediate release and Tapentadol ER for low back pain (NCT00594516), or a 1-year safety study of Tapentadol ER and oxycodone CR for osteoarthritis or low back pain (NCT00361504). After titrating the drug to an optimal dose, patients received Tapentadol ER (100–250 mg BID) for up to 1 year (after finishing treatment in the preceding studies); patients who were previously treated with Tapentadol ER in the 1-year safety study received Tapentadol ER continuously for up to 2 years in total. Findings Of the 1,154 patients in the safety population, 82.7% were aged >65 years and 57.9% were female; 50.1% had mild baseline pain intensity. Mean (SD) pain intensity scores (11-point numerical rating scale) were 3.9 (2.38) at baseline (end of preceding study) and 3.7 (2.42) at end point, indicating that pain relief was maintained during the extension study. Improvements in measures of quality of life (eg, EuroQol-5 Dimension and the 36-item Short Form Health Survey [SF-36]) health status questionnaires) achieved during the preceding studies were maintained during the open-label extension study. Tapentadol ER was associated with a safety and tolerability profile comparable to that observed in the preceding studies. The most common treatment-emergent adverse events (incidence ≥10%; n=1154) were headache (13.1%), nausea (11.8%), and constipation (11.1%). Similar efficacy and tolerability results were shown for patients who received up to 2 years of Tapentadol ER treatment. Implications Pain relief and improvements in quality of life achieved during the preceding studies were maintained throughout this extension study, during which Tapentadol ER was well tolerated for the long-term treatment of chronic osteoarthritis or low back pain over up to 2 years of treatment. (ClinicalTrials.gov identifier: NCT00487435.)

  • Pharmacokinetic evaluation of Tapentadol extended-release tablets in healthy subjects.
    Journal of opioid management, 2013
    Co-Authors: Peter Zannikos, Johan W. Smit, Vera Hillewaert, Hans-jürgen Stahlberg, Birger Wenge, M. Etropolski
    Abstract:

    Objective: To evaluate serum pharmacokinetics of Tapentadol administered to healthy subjects as extended-release (ER) tablets. Design: Seven single-dose studies (five randomized, crossover, bioequivalence studies; a study in Japanese men; and a randomized, crossover, effects-of-food study) and one repeated-dose study. Setting: Clinical research settings in the United States and The Netherlands. Patients or participants: Healthy males and females were enrolled into seven studies; one study enrolled only Japanese males. Interventions: In the bioequivalence studies, subjects first received one polyethylene oxide- or hypromellose-based Tapentadol ER tablet (50, 100, 150, 200, or 250 mg; one dose per study), then (after washout) the other formulation (matching dose). In all other studies, subjects received polyethylene oxide-based Tapentadol ER tablets. In the repeated-dose study, subjects received one 250 mg tablet, then (after washout) one 250 mg tablet every 12 hours (five doses). In the food-effect study, subjects received one 250 mg tablet within 30 minutes after a high-fat meal or after 10 hours of fasting. In the study in Japanese men, subjects received one 100 mg tablet. Main outcome measures: Maximum Tapentadol concentrations (C max ) were typically observed 5 hours after dosing. Mean terminal half-life values ranged from 4.4 to 5.9 hours. Tapentadol C max and AUC values increased proportionally following single ER (polyethylene oxide-based tablets) doses of 50 to 250 mg. Trough Tapentadol concentrations increased during repeat dosing until reaching steady-state by the third dose. Serum C max and area under the concentration-time curve (AUC) values at steady state were 1.6 and 1.9 times higher relative to singledose administration. Coadministration of the 250 mg dose with a high-fat meal increased C max and AUC values by an average of < 17 percent. Conclusions: The pharmacokinetics of Tapentadol ER are consistent after repeated and single-dose administration. Tapentadol ER may be administered without regard to food intake. No clinically significant differences were observed in the pharmacokinetics of Tapentadol between Japanese and Caucasian subjects.

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  • assessment of Tapentadol api abuse liability with the researched abuse diversion and addiction related surveillance system
    The Journal of Pain, 2017
    Co-Authors: Suzanne K Vosburg, Richard C Dart, Steven P Kurtz, Geoffrey S Severtson, Theodore J Cicero, Mark Parrino, Jody L Green
    Abstract:

    Abstract Tapentadol, a Schedule II opioid with a combination of µ-opioid activity and norepinephrine reuptake inhibition, is used for the management of moderate to severe acute and chronic pain. Its dual mechanism of action is thought to reduce opioid-related side effects that can complicate pain management. Since approval, Tapentadol has been tracked across multiple outcomes suggesting abuse liability, and a pattern of relatively low, although not absent, abuse liability has been found. This retrospective cohort study further details the abuse liability of Tapentadol as an active pharmaceutical ingredient (API) when immediate-release as well as extended-release formulations were on the market together (fourth quarter of 2011 to second quarter of 2016). Tapentadol (API) was compared with tramadol, hydrocodone, morphine, oxycodone, hydromorphone, and oxymorphone across Poison Center, Drug Diversion, and Treatment Center Programs Combined data streams from the Researched Abuse, Diversion and Addiction-Related Surveillance system. Findings suggest the public health burden related to Tapentadol to date is low, but present. Event rates of abuse per population-level denominators were significantly lower than all other opioids examined. However, when adjusted for drug availability, event rates of abuse were lower than most Schedule II opioids studied, but were not the lowest. Disentangling these 2 sets of findings further by examining various opioid formulations, such as extended-release and the role of abuse-deterrent formulations, is warranted. Perspective This article presents the results from an examination of Tapentadol API across the Researched Abuse, Diversion and Addiction-Related Surveillance System: a broad and carefully designed postmarketing mosaic. Data to date from Poison Center, Drug Diversion, and Treatment Centers combined suggest a low, but present public health burden related to Tapentadol.

  • diversion and illicit sale of extended release Tapentadol in the united states
    Pain Medicine, 2016
    Co-Authors: Richard C Dart, Hilary L Surratt, Marieclaire Le Lait, Yami Stivers, Vikhyat S Bebarta, Clark C Freifeld, John S Brownstein, John J Burke, Steven P Kurtz
    Abstract:

    Objective .  Prescription opioid analgesics are commonly prescribed for moderate to severe pain. An unintended consequence of prescribing opioid analgesics is the abuse and diversion of these medications. Tapentadol ER is a recently approved centrally acting analgesic with synergistic mechanisms of action: μ-opioid receptor agonism and inhibition of norepinephrine reuptake. We assessed the amount of diversion and related cost of obtaining Tapentadol IR (Nucynta®) and Tapentadol ER (Nucynta ER®) as well as other Schedule II opioid medications in street transactions in the United States using the Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS®) System. Methods .  The Drug Diversion Program measures the number of cases opened by 260 drug diversion investigators in 49 states. StreetRxTM uses a crowd-sourcing Website to collect the prices paid for licit or illicit drugs. Results .  The population-based rates of diversion were 0.003 (Tapentadol IR), 0.001 (Tapentadol ER), and 1.495 (other Schedule II opioid tablets) reports per 100,000 population. The Tapentadol ER rate was lower than the other Schedule II opioid tablets ( P < 0.001) and Tapentadol IR ( P = 0.004). Diversion rates based on drug availability were 0.03 (Tapentadol IR), 0.016 (Tapentadol ER), and 0.172 (other Schedule II opioid tablets) per 1,000 prescriptions dispensed. The median street price per milligram was $0.18 (Tapentadol IR), $0.10 (Tapentadol ER), and $1.00 (other Schedule II opioid tablets). Discussion .  Our results indicate that Tapentadol ER is rarely sold illicitly in the United States. When sold illicitly, Tapentadol ER costs less than other Schedule II opioid products.

  • Diversion and Illicit Sale of Extended Release Tapentadol in the United States
    Pain medicine (Malden Mass.), 2015
    Co-Authors: Richard C Dart, Hilary L Surratt, Marieclaire Le Lait, Yami Stivers, Vikhyat S Bebarta, Clark C Freifeld, John S Brownstein, John J Burke, Steven P Kurtz, Nabarun Dasgupta
    Abstract:

    Objective .  Prescription opioid analgesics are commonly prescribed for moderate to severe pain. An unintended consequence of prescribing opioid analgesics is the abuse and diversion of these medications. Tapentadol ER is a recently approved centrally acting analgesic with synergistic mechanisms of action: μ-opioid receptor agonism and inhibition of norepinephrine reuptake. We assessed the amount of diversion and related cost of obtaining Tapentadol IR (Nucynta®) and Tapentadol ER (Nucynta ER®) as well as other Schedule II opioid medications in street transactions in the United States using the Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS®) System. Methods .  The Drug Diversion Program measures the number of cases opened by 260 drug diversion investigators in 49 states. StreetRxTM uses a crowd-sourcing Website to collect the prices paid for licit or illicit drugs. Results .  The population-based rates of diversion were 0.003 (Tapentadol IR), 0.001 (Tapentadol ER), and 1.495 (other Schedule II opioid tablets) reports per 100,000 population. The Tapentadol ER rate was lower than the other Schedule II opioid tablets ( P

  • Nonmedical use of Tapentadol immediate release by college students.
    The Clinical journal of pain, 2014
    Co-Authors: Richard C Dart, Becki Bucher Bartelson, Edgar H. Adams
    Abstract:

    OBJECTIVES Prescription opioid analgesics play an important role in managing moderate to severe pain. An unintended consequence of the availability of these drugs is nonmedical use. We report rates and methods of nonmedical use of the analgesic Tapentadol immediate release (IR) and other commonly prescribed opioid analgesics among US college students following the launch of Tapentadol IR in June 2009. MATERIALS AND METHODS The Researched Abuse, Diversion and Addiction-Related Surveillance System College Survey Program collects data from approximately 2000 self-identified college students throughout the United States during fall, spring, and summer terms using a web-based questionnaire. Responses from July 2009 through September 2011 were analyzed for the rate of nonmedical use of Tapentadol IR. RESULTS Nonmedical use of prescription opioids was reported by 1626 of 13,514 respondents (12.0%); Tapentadol IR use was reported by 101 respondents (0.7%). The rate of nonmedical Tapentadol IR use per 100,000 population was highest in 4Q2009 (0.013 per 100,000 population) and decreased over the subsequent 2 years to 0.004 per 100,000 population. Similarly, the rate per 1000 unique recipients of dispensed drug (URDD) was highest in 4Q2009 (0.66 per 1000 URDD) and decreased to 0.06 per 1000 URDD. The primary route of administration endorsed for nonmedical Tapentadol IR use was intact swallow (49.5%), chewed and swallowed (41.6%), followed by inhalation (20.8). DISCUSSION Since its launch, rates of nonmedical Tapentadol IR use by college students have been low and have decreased over time. The initial levels of reported nonmedical use may represent a brief period of experimentation after introduction.

  • Assessment of the abuse of Tapentadol immediate release: The first 24 months
    Journal of opioid management, 2012
    Co-Authors: Richard C Dart
    Abstract:

    Objective: Prescription opioid analgesics play an important role in the management of moderate to severe pain. An unintended consequence of prescribing opioid analgesics is the abuse and diversion of these medications. The authors estimated abuse and diversion rates for Tapentadol immediate release (IR) compared with oxycodone, hydrocodone, and tramadol during the first 24 months of Tapentadol IR availability. Methods: The Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS®) System measures rates of prescription opioid abuse and diversion throughout the United States. Quarterly data from the Poison Center, Drug Diversion, Opioid Treatment, and Survey of Key Informants’ Patients (SKIP) programs were plotted to visually compare the rates of Tapentadol IR abuse and diversion with those of other opioid analgesics from July 2009 through June 2011 using both cases per 100,000 population and per 1,000 unique recipients of dispensed drug (URDD) as denominators. Trends in abuse and diversion rates over time were determined using a linear regression model of rate versus time. Results: During the 24 months following its introduction, Tapentadol IR had very low population-based rates of abuse and diversion that were similar to rates for tramadol and lower than rates for oxycodone and hydrocodone. Rates of Tapentadol IR abuse and diversion based on URDD were variable by program due to changes in market share and had not stabilized as of June 2011. Conclusions: Rates of Tapentadol IR abuse and diversion have been low during the first 24 months after its launch. Continued monitoring of trends in these data is warranted. Keywords: Tapentadol, opioid, abuse, diversion, RADARS DOI:10.5055/jom.2012.0139

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