Patient considerations in the use of tapentadol for moderate to severe pain

Abstract

Poorly controlled acute and chronic pain can increase morbidity, impair quality of life and prolong disability. Over 80 percent of post surgical patients report moderate to severe uncontrolled postoperative pain. Over-reliance on potent opioid agonists can lead to several opioid related side effects such as gastrointestinal intolerability, respiratory depression and cognitive impairment. A recently approved dual acting central analgesic tapentadol may offer improved tolerability over traditional opioid agonists while having multimodal opioid and nonopioid analgesic benefits. Tapentadol, classified by the US Food and Drug Administration as a class 2 opioid, is currently marketed in the United States as immediate release (IR) NUCYNTA® for moderate to severe acute pain in tablets of 50 mg, 75 mg, and 100 mg, and as extended release (ER) NUCYNTA ER® for the treatment of chronic moderate to severe pain in tablets of 50 mg, 100 mg, 150 mg, 200 mg, and 250 mg. Tapentadol is a low affinity mu opioid receptor agonist and a norepinephrine reuptake inhibitor. Tapentadol has no active metabolites and this property makes it useful in patients with hepatic and renal failure. Clinical trials with tapentadol IR showed that there was improved gastrointestinal tolerability and similar pain relief as compared to oxycodone IR. Tapentadol ER allows for twice daily dosing. Clinical trials showed that tapentadol ER could effectively relieve moderate to severe chronic pain and was associated with significantly fewer gastrointestinal adverse effects as compared to oxycodone controlled release. Tapentadol ER is indicated and has Food and Drug Administration approval for the treatment of chronic painful diabetic neuropathy. The most common side effects of tapentadol are nausea (30%), vomiting (18%), dizziness (24%), and somnolence (15%). Tapentadol, due to its potential synergistic effects on norepinephrine levels, is contraindicated in patients who have taken monoamine oxidase inhibitors within the last 14 days. Caution has to be exercised with the use of tapentadol IR and tapentadol ER in the presence of other central nervous system depressants such as neuroleptics, opioids, illicit drugs, muscle relaxants, sedatives, and anxiolytics.

Role of preemptive tapentadol in reduction of postoperative analgesic requirements after laparoscopic cholecystectomy

“…Furthermore, the lower affinity of tapentadol for μ-opioid receptors could have resulted in better gastrointestinal tolerability in this group. [71011] Besides this, no ST-segment changes were observed in any of the patients, and vital parameters remained stable for the period of observation. This underscores the good tolerability profile of preemptive tapentadol, although we acknowledge that our study was not powered to access this secondary outcome.…”

“…Its selective norepinephrine reuptake inhibition and alpha-2-adrenoceptor agonism inhibits the pain transmission through dorsal horn neurons, by modulating spinal interneurons, and descending inhibitory fibers from periaqueductal gray matter and rostral ventromedial medulla. [1011] Several advantages over tramadol include its action as a single enantiomer, with a time-dependent parallel change in opioid and monoaminergic receptor dynamics, potentiating its analgesic activity under minimal adverse effects. Though, lack of action on CYP450 receptors could negatively affect its analgesic activity.…”

“…The analgesic efficacy of tapentadol has been investigated over a dose range of 50–200 mg.[781011] Kleinert et al showed that single oral dose of tapentadol 75 mg or higher efficiently reduces moderate-to-severe postoperative dental pain in a dose-related fashion and are well-tolerated relative to morphine. [7] However, a recent report of cardiovascular abnormalities after intake of tapentadol (100 mg, single dose) raised the need for a dose-response study to evaluate the safety and efficacy profile of tapentadol.…”

“…[15] While the usual initiating dose of tapentadol is reported as 50–75 mg, higher doses are currently considered for patients having opioid tolerance or severe pain. [10] As the severity of postoperative pain is lower in patients operated by laparoscopic technique, we preferred a dose of 75 mg tapentadol as a preemptive analgesic, to minimize any side effects. After oral administration, tapentadol is absorbed rapidly and completely with a peak plasma concentration achieved within 1.25–1.5 h, and an elimination half-life of about 4.5 h.[1617] We chose to administer the studied drug an hour before the scheduled surgery, to envelop the time point of maximal pain stimulus for the period of the surgical procedure.…”

Pharmacotherapeutic Management of Neuropathic Pain in End-Stage Renal Disease

“…Tapentadol represents one of the most promising opioids for the treatment of neuropathic pain in ESRD. Categorized in the same chemical class as tramadol, tapentadol offers increased affinity to the mu-opioid receptor (18 times less than morphine) as well as inhibition of NE reuptake [56]. Tapentadol is a full opioid agonist, whereas tramadol is a partial opioid agonist.…”