What is Gabapentin?

Gabapentin is a γ-aminobutyric acid analog (GABA receptor agonist) that is used as an anticonvulsant and analgesic (such as postherpetic neuralgia, fibromyalgia, and neuropathic pain). In addition, Gabapentin is used off-label to treat symptoms such as mood disorders, mild alcohol withdrawal, alcohol use disorder, migraine, chronic pain, and postoperative pain management. However, Gabapentin is not a federally controlled substance under the Controlled Substances Act, and the nationwide opioid abuse crisis has led to an increase in the use of non-opioid drugs (including gabapentinoids) for pain management. This has led to an increase in adverse events associated with these drugs.

Side Effects

Common side effects of Gabapentin include feeling tired and dizzy. It may cause vision changes, clumsiness, unsteadiness, dizziness, drowsiness, or difficulty thinking. Gabapentin abuse has also been reported to produce anxiety effects and euphoria similar to opioid abuse. It can cause respiratory depression, especially when used in combination with other central nervous system depressants. Long-term use can cause physical dependence and a withdrawal syndrome characterized by sweating, anxiety, confusion, and, rarely, seizures. It may also cause breathing problems in people using opioid pain relievers and in patients with chronic obstructive pulmonary disease (COPD). There is evidence that other gabapentinoids, such as pregabalin, may have similar risks.

Rates of gabapentin and pregabalin exposure reported to U.S. poison centers increased by more than 230% from 2012 to 2019 and then stabilized from 2019 to 2022. The observed rate trends were driven primarily by gabapentin exposures and suspected suicides. While most exposures were associated with mild or no effects, 22% of individuals experienced serious medical consequences, including 96 deaths.

High doses of gabapentin were associated with a two-fold increase in adverse effects, including drowsiness, tremor, ataxia, and nystagmus. Exposure to moderate-dose (adjusted OR 1.56) and high-dose gabapentin (adjusted OR 1.58) was associated with a 60% increased risk of opioid-related death compared with opioid use alone.

In summary, although Gabapentin is a good drug for pain management, its side effect of suicidal tendencies should also raise concerns.

References:

[1] Gabapentin Extended-Release - Depomed: Gabapentin ER, Gabapentin Gastric Retention, Gabapentin GR.[J]. Drugs in Research & Development, 2007, 8 5: 317-320. DOI:10.2165/00126839-200708050-00005.

[2] EMILY J R CARTER. Gabapentin and pregabalin exposures reported to United States poison centers, 2012-2022.[J]. Injury Epidemiology, 2024, 11 1: 59. DOI:10.1186/s40621-024-00547-9.