&lt;p&gt;Tapentadol in the treatment of osteoarthritis: pharmacological rationale and clinical evidence&lt;/p&gt;

Osteoarthritis comprises several joint disorders characterized by articular cartilage degeneration and persistent pain, causing disability and economic burden. The incidence of osteoarthritis is rapidly increasing worldwide due to aging and obesity trends. Basic and clinical research on osteoarthritis has been carried out for decades, but many questions remain unanswered. The exact role of subchondral bone during the initiation and progression osteoarthritis remains unclear. Accumulating evidence shows that subchondral bone lesions, including bone marrow edema and angiogenesis, develop earlier than cartilage degeneration. Clinical interventions targeting subchondral bone have shown therapeutic potential, while others targeting cartilage have yielded disappointing results. Abnormal subchondral bone remodeling, angiogenesis and sensory nerve innervation contribute directly or indirectly to cartilage destruction and pain. This review is about bone-cartilage crosstalk, the subchondral microenvironment and the critical role of both in osteoarthritis progression. It also provides an update on the pathogenesis of and interventions for osteoarthritis and future research targeting subchondral bone.

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“…Tapentadol, an analgesic molecule that acts via both mechanisms, has been proven to be helpful against neuropathic pain in knee OA. 177 …”

Section: Subchondral Bone Microenvironment and Oa Painmentioning

confidence: 99%

Subchondral bone microenvironment in osteoarthritis and pain

et al. 2021

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“…Tapentadol has been extensively evaluated in chronic pain conditions, such as back pain, OA, cancer pain, and specifically in neuropathic pain. A detailed presentation of all clinical experiences with tapentadol in these settings goes beyond the aims of the present paper but can be found in a series of recently published reviews [15,[55][56][57]. A paper highlighting the positive impact of tapentadol on QoL has also been recently published [58].…”

Section: Clinical Rationale For the Use Of Tapentadol In Chronic Painmentioning

confidence: 99%

“…In most cases, the waiting period prior to surgery is characterized by persisting moderate-severe pain, with a limitation in the ability to perform daily activities and an increased risk of post-surgical pain. Control of pain is also important postoperatively, since pain is associated with longer hospitalization, modest compliance with the rehabilitation program, delayed return to daily activities and increased risk of postoperative complications [55]. On these bases, a molecule able to act both on the nociceptive and the neuropathic components of pain may be considered in the treatment of OA pain.…”

Section: Osteoarthritismentioning

confidence: 99%

Modulation of sensitization processes in the management of pain and the importance of descending pathways: a role for tapentadol?

Caraci

Coluzzi

Marinangeli

et al. 2020

Current Medical Research and Opinion

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This paper presents and discusses recent evidence on the pathophysiological mechanisms of pain. The role of tapentadol-an analgesic molecule characterized by an innovative mechanism of action (i.e., µ-opioid receptor [MOR] agonism and inhibition of noradrenaline [NA] reuptake [NRI])-in the modulation of pain, and the most recent pharmacological evidence on this molecule (e.g., the µ-load concept) are also presented and commented upon. Methods Narrative review. Results Solid evidence has highlighted the importance of central sensitization in the transition from acute to chronic pain. In particular, the noradrenergic system holds a major role in limiting central sensitization and the progression to chronic pain. Therefore, pharmacological modulation of the noradrenergic system appears to be a well-grounded strategy for the control of chronic pain. Tapentadol is characterized by a to-date-unique mechanism of action, since it acts both as a MOR agonist and as an inhibitor of NA reuptake. The synergistic interaction of these two mechanisms allows a strong analgesic effect by acting on both ascending and descending pathways. Of note, the reduced µ-load of tapentadol has two important consequences: first, it limits the risk of opioidrelated adverse events, as well as the risk of dependence; second, the NA component becomes predominant at least in some types of pain with consequent specific clinical efficacy in the treatment of neuropathic and chronic pain. Conclusions According to these characteristics, tapentadol appears suitable in the treatment of chronic pain conditions characterized by both a nociceptive and a neuropathic component, such as osteoarthritis or back pain.

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“…)-3-(dimethylamino)-1-ethyl-2-methyl]-propylphenol hydrochloride (TAP), the first US FDA-approved centrally acting analgesic for the treatment of moderate to severe acute pain 1,2 .…”

Section: Introduction: Tapentadol 3-[(1r2rmentioning

confidence: 99%

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2020

IJPSR

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The objective was to develop and validate an easy, economical, fast, reliable, reproducible, precise and accurate reversed-phase high-performance liquid chromatography (RP-HPLC) method for the estimation of tapentadol hydrochloride (TAP, a mu opioid-receptor agonist, and noradrenaline reuptake inhibitor) in the bulk and pharmaceutical dosage form. The chromatographic separation was achieved by using the HPLC system equipped with a C-18(2) column (250 × 4.6 mm, Particle size 5µm) at wavelength 217 nm. The mobile phase consisting of Potassium phosphate buffer: Acetonitrile (50:50 v/v) was used in isocratic mode. The flow rate was fixed at 1.0 mL/min with a continuous run up to 5 min, while the retention time was located near about 2.5 min. In the concentration range of 60-160 µgmL-1 , the detector response was found linear with linear regressed equation Y=22791X+120122. In the assay of TAP, 99.65% of the drug was recovered. This method proved a satisfactory validation for all the parameters such as accuracy, linearity, specificity, precision, range, ruggedness, robustness, reproducibility, and peak purity assessment as per ICH guidelines. The results of the study evidenced that it is useful for the routine determination of tapentadol in the bulk and pharmaceutical dosage forms like a tablet.

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<p>Tapentadol in the treatment of osteoarthritis: pharmacological rationale and clinical evidence</p>

Cited by 8 publications

References 38 publications

Subchondral bone microenvironment in osteoarthritis and pain

Subchondral bone microenvironment in osteoarthritis and pain

Modulation of sensitization processes in the management of pain and the importance of descending pathways: a role for tapentadol?

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