Tapentadol, a central-acting analgesic, functions via a dual mechanism. This dual mechanism combines the mu-opioid receptor agonism (MOR), with the norepinephrine reuptake inhibition (NRI). Tapentadol represents the first of its kind in a new class of drugs, called the MOR-NRI agents [Freo et al., 2019].
There are some associated side effects with tapentadol use. In general, side effects brought on by opioids can cause severe problems with patients seeking pain relief [Pergolizzi Jr et al., 2018]. However, tapentadol may lower side effects in the context of chronic pain.
Some side effects, and a brief explanation of how tapentadol can overcome these, is given below:
- Gastrointestinal side effects: tapentadol has been shown (in randomised, double-blind studies) be associated with delayed gastric and small bowel transit time. This was found in comparison to placebo.
- Hormone levels: studies have shown tapentadol to have less effects sex hormone concentrations, in comparison to other pure opioid analgesics (oxytocin and morphine).
- Sleep disorders: tapentadol has been associated with better sleep quality, when administered in a prolonged-release formulation.
Tapentadol and back pain
Several studies have demonstrated the use of tapentadol in lower back pain (LBP). Evidence has shown that tapentadol, based on its dual MOR-NRI action might be a better and effective treatment of chronic lower back pain [Coluzzi et al., 2019].
Tapentadol and cancer pain
Several lines of evidence suggest that tapentadol, in various populations of cancer patients, is well-tolerated and effective in cancer pain patients. Moreover, traditional opioids might not be as effective for cancer pain patients; and tapentadol can provide management of moderate-sever cancer pain in both opioid-naïve and opioid-mature (pre-treated) individuals [Kress et al., 2019].
Tapentadol and abuse potential
Tapentadol is considered an atypical opioid, unlike the main opioids most are familiar with. In this regard, tapentadol is associated with physical and psychologic dependency, in cases of long-term abuse [Pergolizzi Jr et al., 2018]. Statistical studies have shown that non-medical use of tapentadol (immediate release) occurred in less than 1% of patients. Another database study found that the risk of abuse was greater for oxytocin, compared to tapentadol (in those patients given a prescription opioid) [Pergolizzi Jr et al., 2018].
Safety and tolerability
Overall safety and tolerability of Tapentadol has been studied for some time.
In one important study assessing the tolerability and safety of Tapentadol in children and adolescents, researchers administered a single dose of Tapentadol oral solution (adult range dose – 50-100mg) to pediatric patients (2 to 18 years). Result showed good tolerability and safety, with an improvement in post-surgery pain intensity. Researchers noted that Tapentadol might be a new treatment option for pain management in younger cohorts [Muse et al., 2019].
Other research indicates that Tapentadol prolonged release (PR) use for up to two years is well tolerated. Further, patients who switched from traditional opioids to Tapentadol, showed a decrease in adverse events – mainly constipation and nausea [Deeks, 2018].
However, it should be known that prolonged release Tapentadol has been associated with respiratory depression at higher doses, or in patients who are sensitive to opioids that target the mu-opioid receptor (MOR agonists). Moreover, patients considering taking Tapentadol should stay away if they have impaired respiratory function; acute/severe bronchial asthma and/or hypercapnia and/or paralytic ileus [Deeks, 2018].
Tapentadol is currently approved for chronic pain across various countries. In the EU, tapentadol prolonged release (PR) is sold as the brand name Palexia® [Deeks et al., 2018]. Furthermore, in 2008 the FDA approved tapentadol extended release for the management of acute to moderate to severe pain in adults [Miclescu, 2016]. In 2012, the FDA approved tapentadol for use in the treatment of diabetic neuropathy-related pain [Miclescu, 2016].
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