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Pharmacology of Opioids
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
In contrast to tramadol, tapentadol has been classified as a controlled drug in the same category as conventional opioids in many countries. Data from the Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS®) System Poison Center Program in the United States (corrected for amounts dispensed) show that both tapentadol and tramadol have the lowest rates for intentional abuse and diversion compared with morphine, oxycodone, hydromorphone, and oxymorphone (Schug et al, 2020).
Anaesthesia and pain relief
Published in Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie, Bailey & Love's Short Practice of Surgery, 2018
Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie
Paracetamol and the non-steroidal anti-inflammatory drugs (NSAIDs) are the mainstay of musculoskeletal pain treatment. The tricyclic antidepressant drugs and anticonvulsant agents are often useful for the pain of nerve injury, although side effects can prove troublesome and reduce compliance. Both pregabalin and gabapentin reduce spontaneous neuronal activity by their action on the alpha-2-delta subunit of calcium channels, and are now used for managing neuropathic chronic pain. In more severe and debilitating non-malignant chronic pain, opioid analgesic drugs are used in slow release oral preparations of morphine and oxycodone, and transcutaneous patches delivering fentanyl and buprenorphine. Tapentadol with its dual action on opioid and noradrenaline selective reuptake inhibition pathways may provide relief in patients with pain of both neuropathic and nociceptive elements. Combinations of drugs often prove useful to achieve the optimum of efficacy with minimal side effects.
Development of palliative medicine in the United Kingdom and Ireland
Published in Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita, Textbook of Palliative Medicine and Supportive Care, 2015
Tapentadol is an opioid agonist and a norepinephrine reuptake inhibitor [194]. Tapentadol binds to mu, kappa, and delta opioid receptors. One hundred milligrams is equivalent to 20mg of oxycodone and 30mg of morphine (with some individual patient differences). The type of pain influences equivalence [195-197]. Tapentadol has been compared with morphine when treating neuropathic pain. In another randomized trial following bunionectomy, tapentadol 100mg was equivalent to oxycodone 15mg, and had less side effects (i.e., reduced constipation) [198].
The state-of-the-art pharmacotherapeutic options for the treatment of chronic non-cancer pain
Published in Expert Opinion on Pharmacotherapy, 2022
Ryan S. D’Souza, Brendan Langford, Rachel E. Wilson, Yeng F. Her, Justin Schappell, Jennifer S. Eller, Timothy C. Evans, Jonathan M. Hagedorn
Another unique class of agents includes those that exert its effects on the mu-opioid receptor but are not considered opioid medications. These include both tramadol and the recently approved medication known as tapentadol. In addition to mu-opioid agonism, these agents also lead to analgesia via inhibition of norepinephrine (tapentadol and tramadol) and serotonin reuptake (tramadol only) [30,31]. Tramadol may be efficacious in relieving pain in diabetic neuropathy [30], osteoarthritis [32], and neuropathic pain syndromes [33]. A Cochrane-based systematic review revealed that analgesia from tapentadol may be superior in chronic musculoskeletal pain compared to placebo and oxycodone [34]. Recently, tapentadol also received FDA approval for treatment of painful diabetic neuropathy [31,35]. Notable side effects with tramadol and tapentadol include constipation, nausea, vomiting, dizziness, and somnolence [34]. There is also a risk for serotonin syndrome, especially with concomitant use of SSRIs and MAOIs [34].
Cost-effectiveness of tapentadol immediate release versus oxycodone immediate release for acute post-operative pain after major hip surgeries
Published in Current Medical Research and Opinion, 2022
Xinyi Wang, Jonathan Penm, Asad E. Patanwala
Tapentadol is a newer synthetic opioid available for the management of acute pain. It is considered to be a strong centrally-acting opioid that mediates its effect by μ-opioid receptor agonist activity and noradrenaline reuptake inhibition4. This dual mechanism of action targets both nociceptive and neuropathic components of post-operative pain. A recent systemic review and meta-analysis, which included 14 randomised controlled trials compared tapentadol immediate-release (IR) to other opioids for acute pain2. The results showed that tapentadol had similar efficacy on pain control but was associated with fewer GI ADEs compared to traditional opioids such as oxycodone. However, tapentadol IR has a higher drug cost compared to traditional opioids. Also, tapentadol IR is not subsidised by the Australian Pharmaceutical Benefit Schedule (PBS)5. Thus, it is unlikely to be available on most hospital formularies in Australia. This limits its use for post-operative pain.
Postoperative pain: a review of emerging therapeutic options
Published in Expert Review of Neurotherapeutics, 2021
Abhishek K Gupta, Shayla Mena, Zhaosheng Jin, Tong J Gan, Sergio Bergese
In a phase III trial on postoperative pain after elective arthroscopic shoulder surgery, tapentadol 50 to 100 mg were comparable to oxycodone 5 to 10 mg in analgesic efficacy [115]. In hip arthroplasty, patients treated with tapentadol and ketoprofen were found to have less pain at rest and with movement when compared to patients treated with oxycodone and ketoprofen. These patients were also found to have less nausea, vomiting, itching, and constipation [116]. Finally, preoperative administration of tapentadol demonstrated a reduction in acute postoperative pain and perioperative analgesic requirements in laparoscopic cholecystectomy patients without increasing Ramsay sedation scores [117]. While other studies are underway, current literature suggests tapentadol may be efficacious and associated with less adverse events than conventional opioids. The data on tapentadol is notably very limited, and the risk of addiction has not been explored.