API: Gabapentin

What Is Gabapentin and How Does It Work?

Gabapentin is a manufactured structural analog of the neurotransmitter gamma aminobutyric acid (GABA), and has anticonvulsant (anti-seizure) and analgesic properties. Although the mechanism of action is not known for this drug, gabapentin is known to interact with the cortical neurons of calcium channels, thereby increasing the synaptic concentration of GABA and enhancing GABA response elsewhere. Gabapentin is widely used to treat pain, especially neuropathic pain and in the treatment of epilepsy.

For more information, including a MSDS sheet, please see PNA’s Gabapentin page.

Approved Indications1

  • Epilepsy: Gabapentin is used in conjunction with other medications to prevent and manage focal, partial, and mixed epileptic seizures.
  • Postherpetic Neuralgia: Gabapentin used to relieve nerve pain following shingles (a painful rash caused by herpes zoster infection).
  • Other conditions: Gabapentin may also be used to treat other neuropathic pain, such as numbness and tingling from diabetic or peripheral neuropathy, and pain associated with trigeminal neuralgia. The drug may also be helpful in the treatment of restless legs syndrome, hot flashes, and for certain anxiety disorders.

Side Effects and Drug Interactions

Common side effects in patients taking gabapentin include:

  • Drowsiness
  • Dizziness or loss of coordination
  • Fatigue
  • Blurred or double vision
  • Unusual eye movements
  • Tremors

Patients who suffer from severity of these common side effects should contact their pharmacist or physician right away. Patients who experience swelling of the limbs, swollen glands, jaundice, dark urine, changes in the amount of urination, chest pain, or thoughts of suicide should inform their physician immediately.

Gabapentin has a known Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), which is also known as multiorgan hypersensitivity.2 DRESS can present in many ways but typically starts with a fever, rash, and/or lymphadenopathy, with the involvement of other organ systems. Eosinophilia is often present. Other symptoms that can occur include hepatitis, nephritis, hematological abnormalities, myocarditis, myositis, or symptoms that resemble an acute viral infection. Patients with these symptoms should contact their physician immediately.

Patients who are allergic or hypersensitive to gabapentin should not take this drug. Patients who are taking acetaminophen/propoxyphene, buprenorphine (with or without naloxone), levomethadyl acetate, or sodium oxybate should consult their physicians before taking this medication.3

Latest News and Research

Gabapentin was initially investigated as part of a drug discovery program to treat central nervous system disorders diseases such epilepsy, spasticity and multiple sclerosis.4 At the time, GABA was recently discovered to be an inhibitory neurotransmitter, with only a few known agonists (such as baclofen). As scientists studied how to increase oral bioavailability of GABA, gabapentin was developed. In line with the program’s mission to find drugs to treat central nervous system disorders, gabapentin has mostly been used to treat epilepsy and neuropathic pain. However, studies have indicated that gabapentin may have broader applications.

A clinical trial studying the effects of gabapentin on alcohol dependency has shown that the drug may help reduce alcohol dependence in patients while improving mood and sleep patterns.5 Gabapentin may also be effective in treating bipolar disorder in patients who don’t respond to other treatments, and shows effectiveness in stabilizing moods and combating depression.6 The drug also shows promise for managing fibromyalgia pain with no significant side effects.7

Buying Guide

PNA is a recommended bulk supplier of Gabapentin and other APIs. You can learn more about Gabapentin here.

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Resources

Show 7 footnotes

  1. “Neurontin,” 2016, http://www.rxlist.com/neurontin-drug/consumer-uses.htm
  2. “Gabapentin,” December 1, 2015, http://www.drugs.com/pro/gabapentin.html
  3. “Gabapentin Drug Interactions,” 2016, http://www.drugs.com/drug-interactions/gabapentin-index.html?filter=3&generic_only=
  4. “Calcium Channel a2–d Ligands: Gabapentin and Pregabalin,” 2007, http://isites.harvard.edu/fs/docs/icb.topic882884.files/Gabapentin%20case%20history.pdf
  5. “Clinical Trial Indicates Gabapentin Is Safe and Effective for Treating Alcohol Dependence,” November 11, 2013, https://www.scripps.edu/newsandviews/e_20131111/mason.html
  6. “Gabapentin in the Treatment of Bipolar Disorder, 2012, http://jdc.jefferson.edu/cgi/viewcontent.cgi?article=1405&context=jeffjpsychiatry
  7. “Gabapentin in the treatment of fibromyalgia: a randomized, double-blind, placebo-controlled, multicenter trial,” April 2007, http://www.fmcpaware.org/medications/80-research/276-research-article-gabapentin