
TaP -ASH -100 TAPENTADOL HYDROCHORIDE TABLET
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Tapentadol is a centrally acting, multime-chanistic analgesic with a combination of l-opioid agonist activity and norepinephrine reuptake inhibition(NRI) that is used to treat moderate to severe acute andchronic pain.1-5 The FDA approved the immediate-release formulation (Nucynta ER) of tapentadol in December 2008, and the FDA approved the extended-release (ER) formulation (Nucynta ER) in August 2011.6 Tapentadol is a new analgesic that acts as both an agonist of the -opioid receptor (MOR) and a norepinephrine reuptake inhibitor in a single molecule (NRI). Its analgesic benefits start right away, at roughly 30 m for both acute and chronic nociceptive and neuropathic pain.7 Surprisingly, NRI blockers can suppress this last component of tapentadol activity.8 Furthermore, an opioid antagonist like naloxone does not reduce the efficacy of tapentadol, indicating that this molecule has a dual mode of action.9, 10 Tapentadol is not a prodrug, and its therapeutic benefits are not dependent on metabolism. It's a powerful opioid with no known active metabolites, and none of them contribute to its analgesic properties.11, 12 Tapentadol is metabolised via glucuronidation to tapentadol-O-glucuronide, which then conjugates with glucuronic acid to create glucuronides. It is poorly processed by cytochrome P3A4 (CYP3A4) and cytochrome P2D6, which are found throughout the human body.11, 12 Tapentadol is a prescription pain reliever that is taken by mouth, and its metabolites are eliminated in the urine. Between 1.25 and 1.5 hours after intake, the maximal serum concentration is recorded, and the half-life is four hours.11, 12 Because tapentadol is not considerably metabolised by the CYP450 system and does not activate or inhibit CYP enzymes, medication interactions are unlikely.11, 12
Uses:
Tapentadol is a drug that is used to treat musculoskeletal pain as well as neuropathic pain caused by diabetic peripheral neuropathy.13 In cases of opioid-related gastrointestinal (GI) intolerance, nausea, vomiting, or itching, tapentadol may be used instead of other opioid pain medications. Tapentadol, like tramadol, another dual-acting analgesic, delivers multimodal opioid and non-opioid analgesic effects.13
When compared to equal analgesic doses of conventional opioids, tapentadol has less side effects, which could be due to the fact that the analgesic pathways for this molecule are only partially mediated by opioid agonist mechanisms.14
Tapentadol's use could broaden the pharmaceutical toolkit against NP, which is notoriously difficult to treat with other analgesics or co-analgesics such antidepressants or anticonvulsants.15-20
It is used to treat moderate to severe chronic pain as well as neuropathic pain in adults with diabetic peripheral neuropathy (DPN). It is not, however, intended for use as an analgesic for acute pain or minor pain that is not expected to last for a long time. It's also not indicated for postoperative pain unless the patient is already on long-term opioid medication before surgery.21
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