Tapentadol is an opioid used to manage severe pain that has not responded to non-opioid medications, and for which opioid analgesic therapy is appropriate. Tapentadol is a centrally-acting synthetic analgesic with a dual mechanism of action.
- Mechanism
- Curator reviewed · 5 references
Tapentadol is a centrally-acting synthetic analgesic. Although their clinical relevance is unclear, tapentadol is believed to have two main mechanisms of action. Tapentadol is a selective mu-opioid receptor (MOR) agonist: it binds to MOR with an affinity greater than or equal to ten-fold affinity compared to delta- and kappa-opioid receptors. Tapentadol also inhibits noradrenaline reuptake, thereby increasing noradrenaline levels and activating alpha-2 receptors to promote analgesia. Tapentadol is a weak serotonin reuptake inhibitor; however, this action does not contribute to its analgesic effect.
- Primary indication
- Tapentadol is indicated for the management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.Curator reviewed · 4 structured indications
- Formula / weight
- C14H23NO · 221.3385 g/mol (avg)
- First approval
- Canada, 2010 · United States, 2009
- Also known as
- 3-[(1R,2R)-3-(Dimethylamino)-1-ethyl-2-methylpropyl]phenol · PHENOL, 3-((1R,2R)-3-(DIMETHYLAMINO)-1-ETHYL-2-METHYLPROPYL)-
- Code names
- BN-200 · CG-5503 · CG5503 IR · R331333
- Brand names
Resolves to
KWTWDQCKEHXFFR-SMDDNHRTSA-NSMILESCC[C@H]([C@@H](C)CN(C)C)C1=CC(O)=CC=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Tapentadol, and which of those have an active Phase 3 trial?
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