Tapentadol is a centrally acting opioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008.
The immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy.
Tapentadol is used for the treatment of moderate to severe pain for both acute (following injury, surgery, etc.) and chronic musculoskeletal pain. It is also specifically indicated for controlling the pain of diabetic neuropathy when around-the-clock opioid medication is required.
Tapentadol is a centrally-acting synthetic analgesic that is 18 times less potent than morphine in binding mu-opioid receptors. It also increases norepinephrine concentrations in the brains of rats via inhibition of norepinephrine reuptake.
Selective mu-opioid antagonists like naloxone can block analgesia from tapentadol. It also has not effect on the QT interval.
Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition.
Tapentadol is a μ opioid receptor agonist and a noradrenaline (norepinephrine) reuptake inhibitor. These opioidergic and noradrenergic activities are believed to account for the analgesic effects of the drug. Tapentadol is also a weak serotonin reuptake inhibitor; however, this weak serotonergic activity is not thought to be relevant with regard to the drug’s analgesic activity.
Metabolism: 97% of the dose is metabolized mostly via conjugation with glucuronic acid to produce glucuronides. Tapentadol is also metabolized into N-desmethyl tapentadol (13%) by CYP2C9 and CYP 2C19. CYP2D6 is involved in the formation of the metabolite, hydroxy tapentadol (2%). All metabolites are inactive.
Absorption: Bioavailability, immediate release in 1.5 hours; Bioavailability, extended release in 5.0 hours; Tapentadol accumulates following multiple repeat doses.
Route of elimination: Tapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug.
Half life: Elimination half-life, IV: 4 hours.
All medicines may cause side effects, but many people have no, or minor, side effects. Some medical conditions may interact with Tapentadol.
Tell your doctor or pharmacist if you have any medical conditions.
The most common reasons for discontinuation due to adverse events were dizziness, nausea, vomiting, somnolence, and headache.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.
