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What are gabapentinoids?

Two drugs, gabapentin and pregabalin, that were originally shown to be effective in treating seizures, were subsequently shown to be helpful for treating some types of chronic pain. These drugs are approved in the US for treatment of neuropathic pain and fibromyalgia, but are more widely used to treat other types of chronic pain, and even acute pain (for example, in the period following surgery).

These drugs are available by prescription only.

How do gabapentinoids work?

Gabapentinoids are known to bind to a specific receptor in the body, the alpha-2-delta calcium channel receptor. When the drug binds to these receptors, it reduces the excitability of the nervous system. Hyperexcitability of the nervous system is thought to contribute to many types of pain. The excitability-reducing effects of these drugs may occur in several areas of the nervous system (e.g. nerves, spinal cord, brain).

What are the names of some gabapentinoids?

  • Gabapentin (Neurontin)
  • Pregabalin (Lyrica)


Some short-term side effects of these drugs include: - drowsiness - dizziness - swelling of hands and feet - trouble concentrating - increased appetite - weight gain - dry mouth - blurred vision

Less common side effects include: - A severe allergic reaction. Stop taking this medicine and seek emergency medical help if you have hives or blisters on your skin, trouble breathing, or swelling in your face, mouth, or throat. - Some people have thoughts about suicide while taking these drugs. Stay alert to changes in your mood or symptoms. Report any new or worsening symptoms to your doctor. - People can become addicted to these drugs. They are not as addictive as many other classes of drugs such as opioids but these drugs should not be used (or used with caution) in individuals who have a history of addiction to other substances or other substance use issues.

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