Pain control and functional recovery as therapeutic goals in patients with chronic musculoskeletal pain: two experiences with tapentadol hydrochloride.

OBJECTIVE: This study aimed to evaluate pain control, functioning, and quality of life (QoL) recovery in patients with chronic low back pain (cLBP) or post-traumatic osteoarthritis (OA) pain in the ankle/foot area, treated with tapentadol prolonged release and unresponsive to other treatments. PATIENTS AND METHODS: Two observational retrospective studies were conducted using clinical practice datasets of patients with chronic pain in cLBP and OA foot/ankle at different time points (total follow-up=60-90 days). The studies assessed pain intensity by the Numerical Rating Scale (NRS) pain scale (patients were classified as responder in case of ≥30% pain reduction), QoL by the 5-level EQ-5D (EQ-5D-5L) questionnaire, patient satisfaction by the 7-point Patients' Global Impression of Change (PGIC) scale; cLBP health status by the Roland Morris Disability Questionnaire (RMDQ); foot and ankle functional status by European Foot and Ankle Society (EFAS) score; and treatment-related AEs. RESULTS: For the cLBP setting, 37 patients were enrolled, of which 86.50% were classified as responders (n=32; CI: 75.5% ÷ 97.5%). For the foot/ankle OA pain setting, 21 patients were enrolled. Pain assessment at final follow-up was available only for 11 patients, of which 72.73% (n=8; CI: 39.0% ÷ 94.0%) were classified as responders. Statistically significant improvements were seen in the RMDQ, EQ-5D-5L, and PGIC scores in cLBP. Improvements in the EFAS, EQ-5D-5L, and PGIC scores were seen in OA as well. The incidence of treatment-related adverse reactions was low in both studies. CONCLUSIONS: In the study population, tapentadol prolonged release was effective and well tolerated in treating cLBP and post-traumatic foot/ankle OA chronic pain when used in a multimodal manner. The reduction in pain was accompanied by clinically relevant improvements in patients' functionality and QoL.

Tapentadol dependence through intravenous injection ('shooting') of crushed tablets associated with cutaneous pseudoallergic reactions.

Tapentadol is a synthetic opioid analgesic with a low risk of abuse and diversion. The rising trend of abuse of tapentadol is largely attributable to its intrinsic pharmacological profile and easy availability due to poor regulatory control. We report a case of intravenous injection of crushed tapentadol tablets that presented with cutaneous adverse drug reactions. Cutaneous adverse reactions are common in injection drug abuse, and clinical examination is a must to inspect the injection sites. Stringent regulatory measures are required to restrict the increasing abuse of tapentadol in India.

Tapentadol in Cancer Patients with Neuropathic Pain: A Comparison of Methadone, Oxycodone, Fentanyl, and Hydromorphone.

Tapentadol has µ-opioid receptor stimulating and noradrenaline reuptake inhibiting properties, and should be effective for neuropathic pain (NP). However, the efficacy of tapentadol for NP in cancer patients is unclear. Ashiya Municipal Hospital (Hyogo, Japan) enrolled five groups of Japanese cancer patients between January 1, 2013, and December 31, 2019. Patients with NP were administered tapentadol (n = 29), methadone (n = 32), oxycodone (n = 20), fentanyl (n = 26), or hydromorphone (n = 20). The primary endpoint was the difference in the verbal rating scale (VRS) scores between days 0 and 7. The secondary endpoint was the tolerability of each opioid. Before administering opioids among the five groups, there was no significant difference in the VRS score (p = 0.99). The mean reduction in the VRS score on day 7 was significantly greater in the tapentadol group than in the oxycodone group (p = 0.0024) and was larger than that of the methadone, fentanyl, and hydromorphone groups. Regarding safety, the discontinuation rate in the tapentadol group was the lowest of all groups (tapentadol vs. methadone vs. oxycodone vs. fentanyl vs. hydromorphone, 0.0% vs. 6.3% vs. 5.0% vs. 3.8% vs. 10.0%, respectively). This study suggests that tapentadol could be efficacious for cancer patients with NP, and a preferred option in cases that require immediate dose adjustment or for those at high risk for adverse effects. However, the pain intensity was evaluated without pain assessment scales specific to NP. Thus, we think that it is desirable to validate our findings using assessment scales, such as the painDETECT questionnaire in future.

The effects of tapentadol and oxycodone on central processing of tonic pain.

OBJECTIVE: The present study investigated differences between opioids to experimental tonic pain in healthy men. METHODS: Twenty-one males participated in this cross-over-trial. Interventions twice daily were oxycodone (10 mg), tapentadol (50 mg) and placebo for 14 days. Tonic pain was induced on day 1, 4 and 14 by immersing the hand in 2 °C water for 120 s. Electroencephalography was recorded during test pain at baseline and after 14 days. Spectral analysis and source localization were investigated in predefined frequency bands. RESULTS: A decreased perception of pain on day 4 persisted throughout the 14 days compared to baseline (p < 0.006). Oxycodone decreased the electroencephalography spectral power in the delta and theta bands and increased power in the alpha1, alpha2 and beta1 bands (p < 0.03). Tapentadol increased spectral power in the alpha1 band (p < 0.001). Source localization revealed that oxycodone decreased activity of the temporal and limbic region in the delta band, and frontal lobe in the alpha2 and beta1 bands, whereas tapentadol decreased alpha1 band activity in the temporal lobe compared to placebo. CONCLUSION: Oxycodone and tapentadol reduced pain perception and changed the central processing of tonic pain. SIGNIFICANCE: Different mechanisms of action were involved, where oxycodone affected cortical structures more than tapentadol.

Tapentadol results in less deterioration of gastrointestinal function and symptoms than standard opioid therapy in healthy male volunteers.

BACKGROUND: Tapentadol is a combined opioid agonist and norepinephrine reuptake inhibitor with fewer gastrointestinal side effects at equianalgesic doses compared with classical strong opioids. Previous studies on tapentadol have included multi-morbid patients in whom confounders exclude detailed assessment of the mechanistic effects and strict comparison with other opioids or placebo. This study aimed at investigating the effects of tapentadol and oxycodone on gastrointestinal motility and gastrointestinal side effects. METHODS: 21 healthy males participated in a randomized, double-blind, placebo-controlled, crossover study. Tapentadol (50 mg twice daily), oxycodone (10 mg twice daily), or placebo tablets were administered for 14 days. Segmental gastrointestinal transit times and colonic motility parameters were measured with electromagnetic capsules. Gastrointestinal side effects were assessed using questionnaires. KEY RESULTS: During dosing with tapentadol, gastrointestinal side effects and motility parameters were on placebo level. Compared with tapentadol, oxycodone increased whole gut transit time by 17.9 hours (p = .015) and rectosigmoid transit time by 6.5 hours (p = .005). Compared with tapentadol, oxycodone also reduced long, fast antegrade colonic movements (p = .001). In comparison with placebo, oxycodone prolonged whole gut transit time by 31.6 hours, (p < .001). Moreover, less long, fast antegrade colonic movements (p = .002) were observed during oxycodone. For oxycodone only, slow colonic movements were associated with gastrointestinal side effects. CONCLUSIONS & INFERENCES: In this mechanistic study, tapentadol caused significantly less colonic dysmotility and gastrointestinal side effects as compared with oxycodone in equianalgesic doses.

Efectividad analgésica del tapentadol en el dolor neuropático secundario al síndrome postlaminectomía / Analgesic effectiveness of tapentadol in neuropathic pain secondary to post-laminectomy syndrome

Objetivo: El objetivo del presente estudio es evaluar la eficacia y seguridad de tapentadol de liberación a 100 o 200 mg vía oral cada 24 horas, de acción prolongada, para el tratamiento del síndrome postlaminectomía (SPL) en una serie de pacientes con dolor neuropático en tratamiento analgésico inefectivo. Material y métodos: Se realizó un estudio unicéntrico, longitudinal, prospectivo y observacional, en el que se reclutaron 30 pacientes a la clínica de dolor de un centro de referencia de tercer nivel que sufrían de SPL y que cumplían con todos los criterios de inclusión; a quienes se les aplicó el cuestionario Brief Pain Inventory en su versión en español y el test de Lanss antes y después de iniciar tratamiento con tapentadol, y se aplicó una t de Student para comparar la efectividad global del tratamiento del dolor neuropático. Resultado: Se analizaron datos de 30 pacientes, de los cuales 19 fueron mujeres (63,3 %) y 11 hombres (36,6 %) con diagnóstico de SPL confirmado y con características de dolor de tipo neuropático, quienes fueron divididos en dos grupos: el primer grupo de 13 pacientes (43,3 %) recibió tapentadol a 100 mg vía oral cada 24 horas y el segundo de 17 pacientes (56,6 %) recibió 200 mg vía oral cada 24 horas por cuatro semanas. Se les dio un seguimiento de 4 semanas y se encontró una disminución estadísticamente significativa (valor de p = 0,05) del dolor neuropático en la consulta subsecuente de la clínica del SPL.(AU)

Objective: The objective of this study is to eva­luate the efficacy and safety of long-acting tapentadol 100 or 200 mg orally every 24 hours for the treatment of Postlaminectomy Syndrome (SPL) in a series of patients with pain neuropathic in ineffective analgesic treatment. Material and methods: A single-center, longitudinal, prospective and observational study was conducted, in which 30 patients were recruited to the pain clinic of a third-level reference center who suffered from SPL and who met all the inclusion criteria; To whom the Brief Pain Inventory questionnaire in its Spanish version and the Lanss Test were applied before and after starting treatment with tapentadol and a student's t was applied to compare the overall effectiveness of the treatment of neuropathic pain. Results: Data from 30 patients were analyzed, of which 19 were women (63.3 %) and 11 were men (36.6 %) with a diagnosis of confirmed SPL and the presentation of neuropathic pain, who were divided into two groups. The first group of 13 patients (43.3 %) received tapentadol at 100 mg orally every 24 hours, and the second group of 17 patients (56.6 %) received 200 mg orally every 24 hours for four weeks. They were followed up for 4 weeks and statistically significant improvement (p value = 0.05) was found in the SPL clinic.(AU)

Tapentadol, Buprenorphine, and Levorphanol for the Treatment of Neuropathic Pain: a Systematic Review.

PURPOSE OF REVIEW: The objective of this systematic review is to present the available evidence for the utilization of the atypical opioids tapentadol, buprenorphine, and levorphanol for the treatment of neuropathic pain. RECENT FINDINGS: In total, 1619 articles were retrieved of which 10 studies were included. Of 5 included studies pertaining to tapentadol, 4 studies show tapentadol monotherapy to be effective for the treatment of diabetic peripheral neuropathy or chronic, radiating low back pain. Of the 3 studies included for buprenorphine, only one was a randomized controlled trial found not to have a statistically significant reduction in pain with TD buprenorphine likely due to very high withdrawal rates during the trial. Only 2 case reports were included from the available literature for levorphanol providing low-quality anecdotal evidence. The role of tapentadol, buprenorphine, and levorphanol for neuropathic pain conditions requires robust research including randomized controlled trials to evaluate their efficacy and safety.

Sublingual delivery of chondroitin sulfate conjugated tapentadol loaded nanovesicles for the treatment of osteoarthritis.

Recent treatment approaches of osteoarthritis (OA) face a number of obstacles due to the progressive multitude of pain generators, nociceptive mechanisms, first pass mechanism, less efficacy and compromised safety. The present study was aimed to bring a novel approach for the effective management of OA, by developing sublingual targeted nanovesicles (NVs) bearing tapentadol HCl (TAP), surface modified with chondroitin sulfate (CS). Optimized nontargeted nanovesicle formulation (MB-NV) was developed by an ultrasound method, characterized as spherical in shape, nanometric in size (around 150 nm) with narrow size distribution (polydispersity index <0.5), and good entrapment efficiency (around 50%). MB-NV conjugated with CS which was confirmed by IR and 1H NMR spectroscopy. C-MB-NV showed improved pharmacokinetics parameters i.e. increased t1/2 (9.7 h), AUC (159.725 µg/mL*h), and MRT (14.99 h) of TAP than nontargeted formulation and plain drug soln. C-MB-NV in in vitro release studies proved sustained drug release pattern for more than 24 h following Higuchi model kinetics with Fickian diffusion (n ≤ 0.5).Targeted nanovesicles exhibited an improved bioavailability and enhanced analgesic activity in a disease-induced Wistar rat model which indicated the superior targeting potential of C-MB-NV exploiting CD44 receptors as mediators, overexpressed at the affected joints in the OA model. It could be a propitious approach to accustomed therapies for methodical and efficient management in advanced OA therapy.

Quality of life and functional outcomes with tapentadol prolonged release in chronic musculoskeletal pain: post hoc analysis.

Aims: To investigate quality of life (QOL) and functionality changes in chronic pain during tapentadol prolonged release (PR) treatment. Patients & methods: Post hoc analysis of data from three Phase III trials in patients with osteoarthritis knee pain or low back pain. QOL and functionality changes were assessed by SF-36 scores. Results: All SF-36 subdomain scores improved progressively to week 3 of tapentadol titration and were sustained during 12-week maintenance treatment. Improvements in SF-36 scores were similar between tapentadol dose groups (e.g., 200 to <300 mg vs ≥500 mg), with no greater effect from higher doses. QOL and functionality improvements were consistently greater with tapentadol PR than oxycodone controlled release. Conclusion: Tapentadol PR provides consistent, clinically relevant improvements in QOL and functionality in chronic pain.

Antinociception and less gastric injury with the dexketoprofen-tapentadol combination in mice.

The purpose of this study was to evaluate the antinociceptive interaction between dexketoprofen and tapentadol in three different dose ratios, as well as the ulcerogenic activity of this combination. Dose-response curves were carried out for dexketoprofen, tapentadol, and dexketoprofen-tapentadol combinations in the acetic acid-induced writhing test in mice. On the other hand, the gastric damage of all treatments was assessed after the surgical extraction of the stomachs. Intraperitoneal administration of dexketoprofen and tapentadol induced a dose-dependent antinociceptive effect, reaching a maximal effect of about 58% and 99%, respectively. Isobolographic analysis and the interaction index showed that the three proportions produced an analgesic potentiation (synergistic interaction). Interestingly, the 1:1 and 1:3 ratios of the drugs combination produced minor gastric injury in comparison with the 3:1 proportion. Our data suggest that all proportions of the dexketoprofen-tapentadol combination produced a synergistic interaction in the acetic acid-induced visceral pain model in mice with a low incidence of gastric injury.

Tapentadol abuse and dependence in India.

BACKGROUND: Tapentadol is a synthetic opioid analgesic available in India since 2011. International evidence suggests a low risk of abuse and diversion. Our study aims to question this perception in Indian context. METHOD: We report the trend and profile of Tapentadol abuse cases that were treated at a tertiary level addiction treatment centre in southern India. We also describe the ease of repurposing oral tablets of Tapentadol into an injection. At the national level, we have examined the temporal and spatial trends of online interest in Tapentadol and compared it with a non-opioid drug Ilaprazole and an opioid drug Tramadol using Google Trends. We have used the National Drug Use Survey 2019 to illustrate the regional data. RESULTS: 23 cases of Tapentadol abuse sought treatment between 01/01/2011 and 30/08/2019. In last one year, the number of cases has more than doubled. A majority (N = 19, 83 %) of cases had intravenous Tapentadol abuse, needle sharing and 60 % were diagnosed with Hepatitis C. Tapentadol is attracting new users (N = 13, 56.5 %) as well as replacing other opioids (N = 10, 43.5 %) amongst drug users. Tapentadol has received more online interest than Ilaprazole. Temporal and spatial trends of online interest in Tapentadol parallel Tramadol. States with high prevalence of opioid users have shown high online interest in both opioid drugs. CONCLUSION: Tapentadol is being widely abused, and urgent regulatory measures are required.

Tapentadol prolonged release for severe chronic osteoarthritis pain in the elderly: improvements in daily functioning and quality of life.

Background: Chronic osteoarthritis (OA) pain leads to severe impairments in physical functioning and quality of life. Patients & methods: Data of patients with severe chronic knee and/or hip OA pain were extracted from the database of a prospective, noninterventional trial to assess the benefits of tapentadol prolonged release (PR) in elderly patients (>65 years of age; n = 1162) compared with younger patients (≤65 years of age; n = 498). Results: Tapentadol PR treatment (up to 3 months) significantly reduced pain intensity and pain-related restrictions on daily functioning and significantly improved physical and mental quality of life in both patient groups. The incidence of adverse drug reactions was low. Conclusion: Tapentadol PR is a useful strong analgesic to improve pain intensity, physical functioning and quality of life in elderly OA patients.

Tapentadol prolonged release for managing moderate to severe chronic neck pain with or without a neuropathic component.

Background: Despite the high prevalence of neck pain, few studies have addressed the pharmacological treatment of this condition.Purpose: We evaluated the effectiveness of tapentadol prolonged-release (PR) in patients with or without a neuropathic pain component, with a focus on functional movements, disability and Quality of Life (QoL).Study design/setting: Observational, retrospective study.Patient sample: Ninety-four adult patients with severe neck pain not responsive to opioid step III treatment.Outcome measures: The primary endpoint was a ≥ 30% improvement of pain intensity at 4 weeks (W4). Several secondary outcomes were evaluated, including neck disability index (NDI), range of motion (ROM), and QoL.Methods: Patients received tapentadol PR at the starting dose of 100 mg/day. Dose titration was allowed in 50 mg increments, up to 500 mg daily.Results: At W4, the primary endpoint of ≥30% improvement of pain was reported in 70% (n = 35; 95% confidence interval [CI]: 55-82%) of patients with a neuropathic pain component and in 69% (n = 20; 95% CI: 49-85%) of those without a neuropathic component. The percentage of patients reporting a neuropathic pain component significantly decreased from baseline (64.2%) to W4 (27.8%). NDI significantly improved in both groups at W12. ROM significantly improved in all three planes of motion (p < .01), with no difference between the two groups. Interference of pain with sleep and QoL also improved.Conclusions: The reduction in pain provided by tapentadol is associated with functional recovery, which may in turn be linked to an improvement in QoL.

Concomitant use of benzodiazepines in chronic pain patients adherent to extended-release tapentadol or oxycodone treatment-A retrospective claims analysis.

OBJECTIVE: To compare concomitant benzodiazepine (BZDs) use among chronic pain patients adherent to extended-release tapentadol (TapER) or oxycodone (OxnER) and estimate the number of lives potentially saved by switching pa-tients to the less BZD coprescribed treatment. DESIGN: Retrospective database study. SETTING: Patients were identified using the IBM MarketScan® Commercial Database. The opioid overdose death esti-mates were obtained from the US national mortality register and were used to estimate the number of lives potentially saved by switching patients to the opioid treatment with lower rates of BZD coprescribing. PATIENTS, PARTICIPANTS: The authors identified 30,213 chronic pain patients between October 2012 and March 2016. Af-ter propensity score matching, N = 2,355 and N = 6,761 patients were adherent (proportion of days covered ≥80 percent) to TapER and OxnER, respectively. INTERVENTIONS: TapER versus OxnER, during the 180-day treatment. MAIN OUTCOME MEASURE(S): Proportions of BZD coprescribing, BZD dosing patterns in matched patients, and the esti-mated number of lives potentially saved by the opioid treatment switch. RESULTS: TapER patients were less coprescribed BZDs during the treatment period (38.9 percent versus 49.2 percent, OR = 0.659, p < 0.001), and had fewer days of BZD supply per patient (mean: 49.6 versus 70.2 days, p < 0.001) with similar BZD average daily dose. Due to less frequent coprescribing of BZDs with TapER, it is estimated that ~800 deaths may have been avoided in the U.S. as a result of switching patients from OxnER to TapER. CONCLUSIONS: Among treatment-adherent patients, TapER patients had fewer BZD coprescriptions than OxnER pa-tients had. Moreover, when BZDs were coprescribed, those BZD prescriptions were for shorter periods of time. Pro-spective studies are warranted to explore rates and consequences of BZD coprescribing among opioids.

Efficacy and tolerability of tapentadol prolonged release during rehabilitation: a prospective, observational study.

OBJECTIVE: The treatment of chronic pain frequently combines pharmacologic and non-pharmacological options, and analgesia after surgery is of major importance. Tapentadol is both µ-opioid receptor agonist (with a 40% agonism on these receptors) and noradrenaline reuptake inhibitor, with similar analgesic efficacy to strong opioids, but fewer adverse effects. For these reasons, tapentadol may represent a valuable first choice option in the treatment of chronic, neuropathic, and mixed pain. PATIENTS AND METHODS: The primary endpoint of the present study was the proportion of responder patients, with ≥30% reduction in pain intensity during loading on the NRS; several additional endpoints were also evaluated. RESULTS: Twenty-five adult patients were enrolled, with a rate of response to treatment of 100%. Moreover, pain reduction was as high as 50% in 23/25 patients (92%). The average NRS at rest at V0 was 7.2 ± 1.0, whereas the average NRS at loading was 7.7 ± 0.9; this score significantly decreased at all visits. The score of the Roland-Morris questionnaire, a score of disability, improved significantly throughout the study (p<0.0001), as well as the Barthel Index (p<0.0005), and the neuropathic component of pain, which was significantly reduced during the study, from 88% at V0 to 12% at V3. Sleep quality improved throughout the study, and the treatment was rated as good (91% of patients) or optimal (9%). CONCLUSIONS: Our findings show that tapentadol PR may contribute to improve patients' quality of life, especially during rehabilitation after back surgery, when tapentadol PR treatment is effective and well tolerated.

Efficacy of tapentadol prolonged release for pre- and post-operative low back pain: a prospective observational study.

OBJECTIVE: Low back pain (LBP) is a highly prevalent chronic pain condition with a neuropathic component of pain that limits the benefits of classical opioids. Tapentadol is an innovative drug for the treatment of chronic severe pain, with a dual mechanism of action combining µ-opioid receptors agonism and noradrenaline re-uptake inhibition (NRI). Its efficacy is equal to that of strong opioids, with a better tolerability profile and a consequently lower risk of treatment discontinuation. The aim of this study was to evaluate the analgesic efficacy and tolerability of tapentadol prolonged release (PR) vs. other analgesics in patients with moderate-to-severe neuropathic low back pain, before and after back surgery. PATIENTS AND METHODS: The primary endpoints of the study were the rate of response to treatment, measured as ≥30% reduction in pain intensity on the Numeric Rating Scale (NRS), and tapentadol PR efficacy for pain relief. The secondary endpoints were the improvements of the neuropathic component of pain and of sleep quality. RESULTS: A total of 40 patients were enrolled in the study, receiving either tapentadol PR (n=21, 52.5%) or other analgesics (n=19, 47.5%), both before and after surgery. The rate of response to treatment was statistically in favor of tapentadol PR (p<0.01). The reduction in pain intensity was statistically significant in the group treated with tapentadol PR, both before and after surgery (p<0.01), with a complete resolution of pain 90 days after surgery. The quality of sleep after surgery improved more in patients treated with tapentadol PR than in the comparator group (p<0.01), with 100% of the patients reporting a "good" sleep quality 2 months after surgery. CONCLUSIONS: Tapentadol PR was well tolerated by all patients, and its efficacy for pain relief was also confirmed in our small group of "real-life" patients with chronic, severe low back pain. Overall, the tolerability of this treatment may help to improve patients' quality of life, which is frequently compromised because of pain and its related comorbidities.

Tapentadol prolonged release and the long-term management of chronic musculoskeletal pain in the elderly - focus on anxiety, depression, cognitive status and life quality: the TaPE study.

OBJECTIVE: The use of long-term opioids for the management of chronic musculoskeletal pain is a hot topic in the scientific community, especially when it concerns the elderly. This paper aimed at assessing the efficacy and tolerability of tapentadol prolonged release (PR), a molecule with a unique mechanism of action combining µ-opioid-receptor (MOR) agonism and noradrenaline reuptake inhibition (NRI), administered to patients aged ≥80 years with chronic persistent pain. The effect of this molecule on anxiety, depression, cognitive status, and overall quality of life were investigated. PATIENTS AND METHODS: This was a spontaneous, observational, open-label, prospective study, in 80 older patients aged ≥80 years, naïve to strong opioids, presenting moderate-to-severe chronic pain from different etiologies. Tapentadol PR was initially prescribed at the dose of 25-50 mg/day and increased gradually in case of insufficient analgesia. Pain intensity was assessed by a 10-point Numeric Rating Scale (NRS). Other endpoints were as follows: DN4 questionnaire for the evaluation of the neuropathic component of pain, SF12, HADS, and MMSE questionnaires to evaluate the quality of life, anxiety, and cognitive impairment, respectively. Safety evaluations were also performed through the assessment of the frequency and severity of adverse events. RESULTS: At T45, NRS score reduction was achieved in 86.0% of patients. On average, pain decreased by 55% from a mean of 8.2 to a mean of 3.6. At T90, tapentadol PR did not affect the psychophysical and cognitive abilities of older patients. CONCLUSIONS: The benefits with tapentadol PR in controlling pain have improved the quality of life of our patients, also showing a favorable effect on their cognitive performance.

Tapentadol prolonged release in the treatment of musculoskeletal pain: an innovative pharmacological option.

Musculoskeletal pain, encompassing back and osteoarthritis (OA) pain, represents the most frequent source of chronic pain in western countries, and it is particularly frequent in older adults. Remarkably, back and OA pain present, in most cases, both a nociceptive and a neuropathic component of pain. Treatment selection should, therefore, properly consider the ability of a drug to act on both components, reducing the possibility of plastic changes in the central nervous system, and consequently promoting physical rehabilitation. The pharmacological profile of tapentadol, combining synergistically µ-opioid receptor (MOR) agonist and norepinephrine reuptake inhibition (NRI) in one single molecule with a concomitant reduction in the burden of adverse events, is unique, to date, and makes this drug particularly suitable for the treatment of back pain and OA-associated pain, especially when a neuropathic component is present. Tapentadol is an innovative dual-acting analgesic molecule, which combines two mechanisms of action, namely MOR agonism and NRI. This narrative review will briefly discuss the pharmacological action of tapentadol and its rationale for use in back pain and OA.

Tapentadol prolonged release in association with analgesic radiofrequency for the treatment of chronic lumbar radicular pain: an observational, prospective study.

OBJECTIVE: Chronic pain is frequently irreversible, representing a major health problem. A survey has shown that 19% of European adults experience chronic pain which is not adequately managed. Innovative interventional techniques for the treatment of chronic pain have been developed, as a further step beyond the three-layer WHO analgesic ladder. Among these techniques, continuous and pulsed radiofrequency (RF) are very effective in the management of radicular pain syndrome. Usually, these techniques are associated with a pharmacologic approach with a wide-spectrum analgesic. Tapentadol has a double mechanism of action, as a µ-opioid receptor agonism (MOR) and noradrenaline reuptake inhibitor (NRI), contributing synergistically to its analgesic efficacy on both nociceptive and neuropathic pain. PATIENTS AND METHODS: We aimed to test the efficacy of tapentadol prolonged release (PR) combined with pulsed RF in improving neuropathic symptoms and disability in 50 patients with moderate-to-severe chronic pain due to lumbar radiculopathy. RESULTS: The responders to treatment, showing at least a 30% reduction in pain intensity on the Numerical Rating Scale (NRS), were 38 (76%). Both average NRS at rest and during loading were statistically significantly reduced compared with baseline (p<0.0001). Other parameters investigated (sleep quality, neuropathic symptoms, the degree of disability) were all statistically better with tapentadol PR. Patients requiring RF intervention dropped dramatically from 98% at baseline to 10% at the end of the study (p<0.01). Adverse events were reported in 14 patients (28%), four of which required therapy discontinuation. However, patients' satisfaction and overall tolerability of tapentadol PR treatment were high. CONCLUSIONS: Tapentadol PR is effective in reducing pain intensity at rest and during loading, with a favorable safety and tolerability profile. Moreover, the use of tapentadol PR decreases the degree and severity of disability, as well as the intensity of neuropathic symptoms.

Tapentadol prolonged release for pain control in a frail obese patient: a case report.

We present the case of a 59-year-old woman with third-grade obesity and severe comorbidities including osteoporosis, dyslipidemia, diabetes mellitus, hypertension, night eating following bariatric biliary-intestinal bypass surgery, severe fibromyalgia, poly-arthrosis, lumbar disc herniation in L5S1, sleep disorders and sleep apnea syndrome, and emotional disorders with anxiety and depression, who suffered from chronic pain unresponsive to a combination of multiple analgesics. After a period of metabolic and nutritional rehabilitation, analgesic treatment with tapentadol prolonged release (PR) was started and gradually increased to a daily dose of 300 mg with optimal pain control and a marked improvement in the quality of life and autonomy. Therapy suspension was followed by rebound pain with a worsening in functional capacity, and thus, the patient requested a new rehabilitation treatment, with new benefits. Analgesia is of paramount importance in fragile patients who are undergoing a rehabilitation period, in order to improve compliance with the rehabilitation protocols and increase the success of behavioral therapy. Tapentadol PR can be an effective analgesic therapy for pain control in several settings. Its peculiar tolerability profile improves the acceptability of tapentadol, even in patients with multiple previous analgesic treatments.