Tapentadol

As mentioned, tapentadol (Fig. 1) is a centrally acting analgesic that binds to several receptors, and also inhibits norepinephrine (NE) reuptake. This combination effect of tapentadol has been proposed to improve the therapeutic potential of opioid analgesics [Miclescu, 2016]. Moreover, tapentadol has a half-life of around 4 hours and is excreted in the urine and stool.

The main differences between tapentadol and other traditional opioids is that these traditional types – namely, morphine and oxycodone – carry out their analgesic effects through the m-opioid receptor (MOR) agonism [Polati et al., 2019]. In contrast, tapentadol works differently as it produces an analgesic effect in individuals from two separate mechanisms [Polati et al., 2019] (Fig. 2). Once taken, tapentadol is excreted via the kidneys.