Tapentadol

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Tapentadol

Tapentadol (pronounced: ta-PEN-ta-dol) is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the mu-opioid receptor and as a norepinephrine reuptake inhibitor.

Etymology

The name "Tapentadol" is derived from its chemical structure, which is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol.

Usage

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.

Mechanism of Action

Tapentadol acts in two ways. It binds to the mu-opioid receptor on nerves (the same mechanism that is responsible for the effect of opioids), and it also inhibits the reuptake of norepinephrine by the nerves. This dual mode of action is thought to reduce pain signals in the brain.

Related Terms

  • Opioid: A class of drugs that include the illegal drug heroin, synthetic opioids such as fentanyl, and pain relievers available legally by prescription, such as oxycodone (OxyContin®), hydrocodone (Vicodin®), codeine, morphine, and many others.
  • Mu-opioid receptor: A class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. They are also referred to as μ opioid receptors.
  • Norepinephrine: A neurotransmitter, norepinephrine also acts as a stress hormone. Some areas of the brain, like the locus coeruleus, have neurons that primarily release this hormone.
  • Diabetic neuropathy: A type of nerve damage that can occur if you have diabetes. High blood sugar (glucose) can injure nerves throughout your body. Diabetic neuropathy most often damages nerves in your legs and feet.

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