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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].
Mechanism and Pharmacokinetics
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.
Some of the more well-described opioids include:
In terms of manufacturing, oxycodone and buprenorphine are considered semi-synthetic opioids. Whereas the others mentioned in the above list are classed as synthetic opioids [Franchi et al., 2019]. Tapentadol is also considered a synthetic opioid, with less opioid-related side effects [Franchi et al., 2019].”
| Strength: | 100MG, 50MG |
|---|---|
| Quantity of Tablets: | 30, 60, 90 |
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