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Gabapentinoids

Gabapentinoids

What are gabapentinoids?

  • Two drugs were originally shown to be effective in treating seizures.
    • The drugs are gabapentin and pregabalin.
  • It was later discovered that these drugs were helpful for treating some types of chronic pain.
  • These drugs are approved in the US for treatment of neuropathic pain and fibromyalgia.
    • They 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.
    • This receptor is the alpha-2-delta calcium channel receptor.
  • The drug reduces the excitability of the nervous system when it binds to these receptors.
  • Hyperexcitability of the nervous system is thought to contribute to many types of pain.
  • The excitability-reducing effects of these drugs can occur in several areas of the nervous system:
    • nerves, spinal cord, brain.

What are the names of some gabapentinoids?

  • Gabapentin (Neurontin)
  • Pregabalin (Lyrica)

Risks

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 like opioids.
  • 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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