tapentadol and Acute-Pain

Tapentadol (TAP) immediate release (IR) is a newer opioid option for acute pain. The aim of this systematic review was to examine the efficacy and safety of TAP IR compared with other opioids for acute pain.. A systematic literature search as conducted using the Cochrane Library, Embase, International Pharmaceutical Abstracts, MEDLINE, PubMed, and Web of Science. The search included all randomized controlled trials and observational studies examining TAP IR versus other orally administered IR opioids for acute pain. The protocol for this study was registered on PROSPERO (CRD42018110267).. Thirteen studies and 1 abstract were included in the systematic review (n=12,814 patients). Of these, 5 studies and 1 abstract were included in the qualitative review (n=9108 patients). Eight randomized controlled trials (n=3706 patients) comparing 50 to 100 mg TAP IR versus 5 to 15 mg oxycodone IR were included in the meta-analysis. The lowest dose of TAP IR (ie, 50 mg) was associated with less pain control compared with oxycodone IR (standardized mean difference=0.25, 95% confidence interval: 0.06-0.44, P<0.01). However, there were no significant differences at higher doses (ie, 75, 100 mg, or when a titration strategy was used). In the qualitative analysis, pain control with TAP IR was also similar to morphine IR and tramadol IR. TAP IR was less likely to have gastrointestinal adverse effects such as nausea and constipation compared with other opioids.. TAP IR is as effective as other opioids at higher doses for acute pain and is associated with fewer gastrointestinal adverse effects. On the basis of these findings, TAP IR can be considered as a first-line opioid for acute pain.

Topics: Acute Pain; Analgesics, Opioid; Humans; Observational Studies as Topic; Oxycodone; Randomized Controlled Trials as Topic; Tapentadol

Tapentadol is a newly approved novel analgesic drug with a dual mode of action: a mu-opioid agonist and an inhibitor of norepinephrine reuptake (MOR-NRI). Preclinical evidence supports a synergistic interaction between these two effects. It is the first opioid agonist to exhibit predominant norepinephrine reuptake inhibition with minimal serotonin effects. It is FDA approved for use in the US for moderate to severe pain in adults, available in the immediate release form for acute pain and as an extended-release formulation for chronic pain when continuous analgesia is required. Tapentadol has demonstrated reduced treatment-emergent opioid-related gastrointestinal adverse effects compared with pure opioid agonists. The synergistic mu-opioid and alpha(2)-adrenergic effects suggest the potential for particular utility in neuropathic pain states or other pain states associated with hyperalgesia.

Topics: Acute Pain; Adrenergic Uptake Inhibitors; Analgesics, Opioid; Chronic Pain; Humans; Phenols; Receptors, Opioid, mu; Tapentadol

Tapentadol may allow greater pain relief with reduced "opioid load" compared to oxycodone. Its use has not been studied in the obstetric population. The objective of this study was to compare the efficacy and side effect profile of tapentadol with oxycodone in patients who received spinal anesthesia for elective cesarean section. The trial was registered with EU Clinical Trials Register with CT number 2016-001621-33.. This was a multicenter, randomized controlled trial. Randomized patients (n = 68) received either 50 mg tapentadol or oxycodone 10 mg 12 hourly postoperatively. The primary endpoint was the sum of pain intensity difference over the first 48 hours of treatment (SPID. There was no significant difference in the primary endpoint of SPID. Tapentadol did not provide superior pain control or improved tolerability compared to oxycodone post cesarean section. Results should be interpreted however with consideration of administration of intrathecal opioids to all patients in this study and debate over the optimal dose of tapentadol for acute pain.

Topics: Acute Pain; Adult; Analgesics, Opioid; Cesarean Section; Double-Blind Method; Female; Humans; Oxycodone; Pain Management; Pregnancy; Single-Blind Method; Tapentadol

The Short-form McGill Pain Questionnaire (SF-MPQ-2) assesses the major symptoms of both neuropathic and nonneuropathic pain and can be used in studies of epidemiology, natural history, pathophysiologic mechanisms, and treatment response. Previous research has demonstrated its reliability, validity, and responsiveness in diverse samples of patients with chronic pain. However, the SF-MPQ-2 has not been evaluated for use in patients with acute pain. Data were examined from a double-blind, randomized clinical trial of immediate-release tapentadol versus immediate-release oxycodone in patients with acute low back and associated radicular leg pain (N = 666). Analyses of internal consistency, convergent validity, and confirmatory factor structure were conducted using baseline data, and analyses of responsiveness were conducted using baseline and endpoint data. The SF-MPQ-2 total score and its 4 subscale scores (continuous pain, intermittent pain, predominantly neuropathic pain, and affective descriptors) generally showed good psychometric properties and 1) were internally consistent, 2) displayed good convergent validity, 3) fit the a priori factor structure, and 4) were highly responsive to analgesic treatment. These data extend previous evidence of the reliability, validity, and responsiveness of the SF-MPQ-2 in patients with chronic pain to those with acute low back and associated radicular leg pain.. Considered together with the results of other recent studies, the data suggest that the SF-MPQ-2 can provide a valid, responsive, and efficient assessment of both neuropathic and nonneuropathic pain qualities for clinical trials and other clinical research examining patients with various acute and chronic pain conditions.

Topics: Acute Pain; Analgesics, Opioid; Double-Blind Method; Factor Analysis, Statistical; Female; Humans; Leg; Low Back Pain; Male; Middle Aged; Neuralgia; Oxycodone; Pain Measurement; Phenols; Psychometrics; Reproducibility of Results; Surveys and Questionnaires; Tapentadol

To evaluate the efficacy and safety of tapentadol immediate-release (IR) for treating acute pain following orthopedic bunionectomy surgery in a Taiwanese population.. This was a phase 3, randomized, double-blind, placebo-controlled, parallel-group bridging study in which Taiwanese patients (N = 60) with moderate-to-severe pain following bunionectomy were randomized (1:1:1) to receive tapentadol IR 50 or 75 mg or placebo orally every 4-6 hours over a 72 hour period. The primary endpoint was the sum of pain intensity difference over 48 hours (SPID48), analyzed using analysis of variance.. Out of 60 patients randomized (mainly women [96.7%]; median age 44 years), 41 (68.3%) completed the treatment. Mean SPID48 values were significantly higher for tapentadol IR (p ≤ 0.006: 50 mg, p ≤ 0.004: 75 mg) compared with placebo. Between-group differences in LS means of SPID48 (vs. placebo) were tapentadol IR 50 mg: 105.6 (95% CI: 32.0; 179.2); tapentadol IR 75 mg: 126.6 (95% CI: 49.5; 203.7). Secondary endpoints including SPID at 12, 24, and 72 hours, time to first use of rescue medication, cumulative distribution of responder rates, total pain relief and sum of total pain relief and sum of pain intensity difference at 12, 24, 48, and 72 hours, and patient global impression of change showed numerically better results supporting that tapentadol IR (50 and 75 mg) was more efficacious than placebo in relieving acute pain. The most frequent treatment emergent adverse events reported in ≥ 10% patients in either group were dizziness, nausea, and vomiting. A limitation of this study may possibly include more controlled patient monitoring through 4-6 hour dosing intervals, which reflects optimal conditions and thus may not approximate real-world clinical practice. However, all treatment groups would be equally affected by such bias of frequent monitoring, if any, since it was a randomized and double-blind study.. Tapentadol IR treatment significantly relieved acute postoperative pain and was well tolerated in a Taiwanese population. ClinicalTrials.gov identifier: NCT01813890.

Topics: Acute Pain; Adult; Analgesics, Opioid; Double-Blind Method; Female; Humans; Longitudinal Studies; Male; Middle Aged; Nausea; Orthopedic Procedures; Pain Measurement; Pain, Postoperative; Phenols; Taiwan; Tapentadol; Vomiting

To broaden the ethnic groups in which tapentadol IR is evaluated for treating acute postoperative pain to include Asians.. In this phase 3, multicenter, double-blind, randomized study, 352 Korean adults with moderate-to-severe pain following hallux valgus surgery received tapentadol IR 50 or 75 mg or placebo orally every 4-6 hours for 72 hours. Patients requesting other (rescue) analgesics during this period were discontinued for lack of efficacy. The primary endpoint, sum of pain intensity difference (SPID) over 48 hours, was evaluated based on the difference between tapentadol IR and placebo in least squares (LS) mean change from baseline using analysis of covariance (ANCOVA). Secondary endpoints included the time to first rescue medication use and the distribution of responder rates.. A treatment effect, favoring tapentadol IR, was observed for SPID48 (p < 0.001 for both doses vs. placebo, ANCOVA). The between-group difference (vs. placebo) in LS means of SPID48 was 76.4 (95% CI: 51.0, 101.7) for tapentadol IR 50 mg and 90.6 (95% CI: 65.1, 116.1) for tapentadol IR 75 mg. Time to first rescue medication use was delayed for tapentadol IR (p < 0.001 for both doses vs. placebo; log-rank test). The distribution of responders at 12, 24, 48, and 72 hours favored tapentadol IR (p ≤ 0.001 for both doses vs. placebo; Cochran-Mantel-Haenszel test). Dizziness, nausea, and vomiting were each reported in ≥ 10% tapentadol-treated patients and at an incidence ≥ 2-fold higher vs. placebo. The study findings may be limited by study drug dosing every 4 to 6 hours and frequent monitoring during treatment, neither of which mimic pain treatment in clinical practice. However, any potential bias based on this systematic monitoring of patients would be mitigated by the randomized, double-blind nature of the study, with all treatment groups similarly affected by such biases, if any.. Tapentadol IR reduced acute pain intensity, significantly more than placebo, after orthopedic surgery in Korean patients.. NCT01516008.

Topics: Acute Pain; Adult; Aged; Aged, 80 and over; Analgesics, Opioid; Asian People; Double-Blind Method; Female; Hallux Valgus; Humans; Male; Middle Aged; Orthopedic Procedures; Pain Measurement; Pain, Postoperative; Phenols; Republic of Korea; Tapentadol; Young Adult

Tapentadol exhibits a synergistic dual effect effect (MOR / NRI) -agonist effect on noradrena-line reuptake inhibition (NRI). Tapentadol is effective on pain with neuropathic characteristics, therefore we decided to use it in an experimental model of acute orofacial pain.. The Orofacial Stimulation Test, developed by Ugo Basile, measures hypersensitivity to thermal or mechanical stimulation of the trigeminal area. In the experiment, rats had to voluntarily contact a thermal or mechanical stimulator with their unshaved vibrissal pad in order to access a food reward. Twenty adult laboratory rats (average weight 345 grams) were tested. Intraperitoneal tapentadol was used in doses of 1 mg/kg and 2 mg/kg.. The results of the pilot study indicate that intraperitoneal administration of tapentadol (2 mg/kg) increased mechanical anti-nociception in rats.

Topics: Acute Pain; Analgesics, Opioid; Animals; Central Amygdaloid Nucleus; Dose-Response Relationship, Drug; Facial Pain; Naloxone; Pain Measurement; Pilot Projects; Rats; Tapentadol; Yohimbine

Topics: Acute Pain; Adult; Chronic Pain; Drug Tolerance; Early Medical Intervention; Humans; Male; Morphine; Morphine Derivatives; Neural Inhibition; Oligopeptides; Opioid-Related Disorders; Pain Management; Peptides, Cyclic; Phenols; Receptors, Opioid, mu; Spinal Cord Stimulation; Tapentadol; Tramadol; Young Adult

Even though pain is a complex process involving many different mediators, enzymes, receptors and ion channels, pain medications usually address only individual targets. Nucynta, which addresses multiple pain targets, was the first new centrally acting analgesic to be approved by the FDA in 2008.. Pharmacology: Tapentadol is a centrally acting opioid with two mechanisms of action, including agonism at the μ-opioid receptor (MOR) and inhibition of norepinephrine reuptake (NRI), producing analgesia individually and via a combination of both acts synergistically at the spinal and supraspinal levels. The pharmacokinetics of both forms of tapentadol (immediate release-IR and extended release-ER) is relatively predictable and stable in healthy individuals. Clinical efficacy: Tapentadol IR was studied in clinical trials involving patients mainly with postoperative pain, but also in patients suffering from acute low back pain and osteoarthritis-related pain. Tapentadol ER was approved for management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate.. Although future improved, well-designed prospective, randomized double-blind controlled studies are needed to determine both the relative efficacy of tapentadol and its safety, we believe that tapentadol has the potential to become a uniquely suited opioid medication in the multi-modal management of moderate-to-severe acute and chronic pain conditions.

Topics: Acute Pain; Analgesics, Opioid; Animals; Chronic Pain; Humans; Phenols; Receptors, Opioid, mu; Severity of Illness Index; Tapentadol

The standard opioids for relieving moderate to severe pain are: codeine as a step 2 analgesic and morphine for step 3. Tapentadol is an opioid similar to tramadol. An immediate-release form has been authorised in France for moderate to severe acute pain in adults and a sustained-release form for severe chronic pain in adults. It has been evaluated in comparative trials in several types of acute pain: pain following orthopaedic or gynaecological surgery or tooth extraction, and joint pain. These trials were principally designed to show its analgesic effect versus placebo.They did not establish the equianalgesic dose ratios of tapentadol to codeine, morphine or oxycodone. In chronic pain, one trial compared sustained-release tapentadol versus sustained-release morphine, but only unconvincing preliminary results are available.The results of other trials versus sustained-release oxycodone are unconvincing, because half of the patients were lost to follow-up. The known adverse effects of tapentadolare mainly those associated with all opioids, including neuropsychiatric disorders and addiction. Aggression and serotonin syndrome are possible reactions that require further investigation. Gastrointestinal disorders appeared less common with tapentadol than with oxycodone, but the data could well be biased due to the use of a relative overdose of oxycodone in the trials. In practice, the evaluation of tapentadol was not designed to show whether this drug represents a therapeutic advance. Its analgesic efficacy remains unclear, and it provokes the adverse effects common to all opioids.

Topics: Acute Pain; Adult; Analgesics, Opioid; Chronic Pain; Delayed-Action Preparations; Drug Approval; France; Humans; Phenols; Severity of Illness Index; Tapentadol

Tapentadol (Palexia - Grünenthal) is a recently introduced strong analgesic with µ-agonistic opioid and additional noradrenaline reuptake inhibition properties. The summary of product characteristics (SPC) states that it is indicated for the relief of moderate to severe acute pain in adults, which can be adequately managed only with opioid analgesics.1 Here we review the place of tapentadol in the treatment of patients with moderate to severe acute pain.

Topics: Acute Pain; Analgesics, Opioid; Delayed-Action Preparations; Drug Approval; Drug Costs; Humans; Phenols; Practice Guidelines as Topic; Randomized Controlled Trials as Topic; Receptors, Opioid, mu; Tapentadol