Gabapentin for Restless Leg Syndrome

Where is Gabapentin used?

Gabapentin is an oral medication mainly used to help control certain types of seizures in people who have epilepsy. This can also be used to relieve the pain of postherpetic neuralgia which has a stabbing pain that may last for months or years after an attack of shingles. This medication is in the class of anticonvulsants that lessens abnormal excitement in the brain. Gabapentin eases the pain of postherpetic neuralgia by altering the way the body senses pain.

How does Gabapentin work?

Gabapentin works in the nervous system and brain. The drug appears to affect the build-up of electrical signals in the nerve cells. It also affects the activity of neurotransmitters in the nervous system and brain, mainly glutamate and GABA. GABA is a neurotransmitter that helps keep the nerve activity in the brain stable. Glutamate excites more nerve cells that are thought to play a key role in causing epileptic seizures and transmitting pain signals to the brain. This medication seems to and decrease glutamate levels and increase GABA, which helps keep the nerve activity in the brain more balanced.

Possible Side Effects of Gabapentin

  • Vertigo
  • Drowsiness
  • Dizziness
  • Sleepiness
  • Swelling of the extremities
  • Tired feeling or weakness
  • Headache
  • Diarrhea
  • Nausea
  • Loss of balance or coordination
  • Constipation
  • Blurred vision
  • Dry mouth
  • Back pain

Gabapentin for Restless Leg Syndrome

The Food and Drug Administration (FDA) has already approved Gabapentinin 2011 as the first non-dopaminergic agent for the treatment of the symptoms of Restless Leg Syndrome (RLS). Even though this medication is a pro-drug, its pharmacokinetics differs. Absorption of Gabapentinis more anticipated and inter-patient variability in bioavailability is lower than that of Gabapentin.

Studies have established the advantage of Gabapentincompared to placebo. Contrasts to currently existing treatments for Restless Leg Syndrome are insufficient however clinical trials demonstrate comparable progress in the symptoms of the condition to the dopamine agonists Pramipexole and Ropinirole. These are usually measured primary treatments for daily symptoms of RLS. Gabapentin was well tolerated in clinical trials. The role of the medication in Restless Leg Syndrome treatment remains unclear, even though it will likely be used as a substitute for refractory Restless Leg Syndrome when other treatments have failed. Moreover, Gabapentinmay be recommended for patients with daily symptoms of the condition that are less intense or are accompanying by pain as an alternative to dopamine agonists.

How does Gabapentin work for Restless Legs Syndrome?

How Gabapentin works in Restless Legs Syndrome is unknown. Regardless of structural similarity to GABA, this drug does not interact directly with GABA receptors. Instead, it binds with high affinity to a certain subunit of voltage-activated calcium channels. It is vague how this binding of Gabapentin is linked to its therapeutic effects. Nonetheless, it is thought that these binding fallouts in the inhibition of calcium entry over a high voltage of calcium channels. In turn, it leads to the normalization of the release of neurotransmitters.

Gabapentin is immersed by low-capacity solute transporters that are limited to one zone of the small intestine. As a result, the concentration of the drug could be saturated at higher a dosage which possibly causes unpredictable or sub-therapeutic levels of the drug. Due to the variability in the pharmacokinetics of Gabapentin, there can be pronounced changes in serum levels between individuals.

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