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What Is Gabapentin?  Definition, Usage, Side Effects, Addiction

Gabapentin

Gabapentin is primarily prescribed for neuropathic pain, seizures, and conditions like postherpetic neuralgia. Marketed under the brand name Neurontin, gabapentin is prescribed for nerve pain, seizures, and chronic conditions. While intended for therapeutic use, excessive consumption or misuse sparks dependency, making it difficult to control usage despite negative physical, emotional, or social consequences.

The medical uses of gabapentin are for managing epilepsy, postherpetic neuralgia, diabetic neuropathy, fibromyalgia, restless leg syndrome, and certain anxiety disorders. It is also prescribed for chronic pain and neurological conditions due to its effect on nerve activity. Research indicates a higher risk of abuse among individuals with prior substance use disorders involving alcohol, cocaine, or opioids.

A review of 18 case reports and studies documented addiction at daily doses exceeding 3,000 mg (600–8,000 mg/day). Misuse rates were 1.1% in the general population and 22% among individuals in drug treatment programs. Withdrawal symptoms typically emerge within 12 hours to seven days after discontinuation, as reported by Mersfelder & Nichols 2015 in “Gabapentin: Abuse, Dependence, and Withdrawal.”

The main side effects of gabapentin addiction include fatigue, dizziness, oversedation, nausea, muscle weakness, respiratory depression, cognitive impairment, and withdrawal seizures. In pregnant individuals, it increases the risk of preterm delivery and low birth weight. Short-term effects, such as sedation and dizziness, lower quality of life, while long-term abuse breeds cognitive decline and organ damage. Severe cases necessitate professional intervention to prevent irreversible health consequences.

Gabapentinoid use such as gabapentin rose globally by an average of +17.2% annually, rising from 4.17 to 18.26 defined daily doses per ten thousand inhabitants per day (DDD/TID) between 2008 and 2018, with high-income countries consuming 39.92 DDD/TID in 2018, over six times more than the 6.11 DDD/TID in lower-middle-income countries, as shown in a longitudinal study by Chan et al. 2023 in “Gabapentinoid Consumption in 65 Countries and Regions from 2008 to 2018: A Longitudinal Trend Study.”

Gabapentin addiction requires responsible prescribing, patient education, alternative treatment options, and monitoring for misuse. Addressing co-occurring mental health disorders is critical, as highlighted by Smith et al. 2018 in “A Qualitative Analysis of Gabapentin Misuse and Diversion Among People Who Use Drugs in Appalachian Kentucky.” Healthcare providers assist in mitigating risks through careful patient monitoring and individualized treatment plans.

What Is Gabapentin?

Gabapentin is a prescription medication classified as an anticonvulsant that alters nerve signaling in the central nervous system. As of September 2022, several states have reclassified gabapentin as a Schedule C-V controlled substance. According to Drugs.com, these states include Michigan, Kentucky, North Dakota, Tennessee, Virginia, West Virginia, and Alabama.

As an anticonvulsant, gabapentin is commonly prescribed for epilepsy and specific pain conditions. It is also used off-label to manage alcohol withdrawal symptoms, reduce cravings, and alleviate anxiety and insomnia. Its broad applications have contributed to increased usage, raising concerns about potential abuse and dependency.

Between 2012 and 2022, U.S. poison centers reported 124,161 cases of gabapentin and pregabalin exposures, with gabapentin accounting for 85.9% of cases. Most cases involved females (59.4%), single-substance exposures (62.9%), and incidents occurring at home (97.2%). Suspected suicides made up 45.2% of cases, and while 61.4% resulted in minor or no effects, 22.1% led to serious outcomes, including 96 deaths. Exposure rates surged by 236.1% from 2012 to 2019 before stabilizing. These findings underscore the need for suicide prevention strategies and discussions on rescheduling gabapentin as a federally controlled substance, as highlighted by Carter et al. 2024 in “Gabapentin and Pregabalin Exposures Reported to United States Poison Centers, 2012–2022.”

How Does Gabapentin Work?

Gabapentin works by regulating nerve cell activity in the brain and spinal cord by modifying how signals for pain and seizures are transmitted. While its exact mechanism remains incompletely understood, gabapentin interacts with calcium channels in nerve cells, reducing the release of excitatory neurotransmitters that contribute to excessive nerve activity. Despite its name suggesting a link to Gamma-Aminobutyric Acid (GABA), gabapentin does not directly target GABA receptors. Instead, it influences nerve cell communication, stabilizing neural activity and alleviating pain and seizures.

How Does Gabapentin Work

The widespread misuse of gabapentin and its involvement in overdose deaths highlight its major impact. According to an analysis by the CDC using data from the State Unintentional Drug Overdose Reporting System (SUDORS) across 23 states and the District of Columbia, gabapentin was detected in 9.7% of 58,362 toxicology reports from overdose deaths in 2019–2020. Notably, in 52.3% of cases where gabapentin was found, it was identified as a contributing cause of death. Most fatalities occurred among non-Hispanic White individuals (83.2%), primarily aged 35–54 (52.2%), with nearly equal gender distribution between men (49.7%) and women (50.3%). These findings emphasize the necessity for enhanced monitoring and education regarding gabapentin use.

Is Gabapentin a Controlled Substance?

No, Gabapentin is not a federally controlled substance, but some U.S. states classify it as a Schedule V drug due to concerns over misuse and dependency. While the Drug Enforcement Administration (DEA) does not regulate Gabapentin at the federal level, reports highlight its increasing misuse, especially when combined with opioids. As a result, states like Kentucky, Michigan, and Tennessee have placed restrictions on its distribution and require prescription monitoring. These regulations aim to reduce illicit use while ensuring that patients who need Gabapentin for nerve pain or epilepsy continue to have access under medical supervision.

What Is Gabapentin Used For?

Gabapentin is used to manage seizures and neuropathic pain, but it also has several off-label applications. Originally developed as an anticonvulsant, Gabapentin helps control epilepsy by stabilizing nerve activity. The drug is prescribed for nerve pain conditions, such as postherpetic neuralgia and diabetic neuropathy. Additionally, Gabapentin is used to treat anxiety disorders, improve sleep quality, and assist in substance withdrawal management. Its ability to modulate nerve signaling makes it effective for various neurological and pain-related conditions.

What Is Gabapentin Used For

Common conditions that Gabapentin is used for are given below:

  • Seizures – Used as an adjunctive therapy for epilepsy, Gabapentin helps control partial seizures by stabilizing electrical activity in the brain. Gabapentin is prescribed alongside other antiepileptic drugs to enhance seizure management.
  • Neuropathic pain – Effective for conditions like diabetic neuropathy and postherpetic neuralgia, Gabapentin minimizes abnormal nerve signaling that causes chronic pain. Gabapentin is prescribed when first-line pain relievers fail to provide relief.
  • Anxiety – Gabapentin is used off-label for generalized anxiety disorder and social anxiety, helping to regulate nerve activity linked to excessive worry and tension.  The Anxiety and Depression Association of America (2022) notes that nearly 20% of adults experience these symptoms
  • each year, spotlighting the widespread impact of these conditions Gabapentin is considered when standard anxiolytics are ineffective or unsuitable.
  • Sleep disturbances – Helps improve sleep quality by reducing nerve excitability, making it useful for insomnia and restless leg syndrome (RLS). Gabapentin is particularly beneficial for individuals who struggle with sleep due to chronic pain or neurological conditions.
  • Drug dependence – Used in managing withdrawal from alcohol, opioids, and benzodiazepines, Gabapentin cuts cravings and withdrawal symptoms by affecting the brain’s neurotransmitter balance. Gabapentin is sometimes included in medication-assisted treatment (MAT) programs. Gabapentin addiction affects 1.1% of the general population and 22% of individuals in drug treatment centers. Between January 2011 and December 2020, California reported 24 to 49 cases per 100,000 individuals aged 15 or older, according to the Drug Enforcement Administration’s Diversion Control Division in “NFLIS-Drug Special Report: Gabapentin and Pregabalin Reported in NFLIS, 2011–2020.”
  • Migraines – Sometimes prescribed as a preventive treatment, Gabapentin diminishes the frequency and severity of migraines by stabilizing nerve activity and dampening pain pathways in the brain.
  • Fibromyalgia – Helps manage widespread chronic pain by affecting nerve function and reducing pain sensitivity. Gabapentin is chosen when other pain medications fail to provide adequate relief.
  • Restless Leg Syndrome (RLS) – Reduces uncomfortable sensations in the legs by altering nerve activity, prompting boosted sleep and reduced nighttime discomfort. Gabapentin is especially useful for individuals with moderate to severe RLS symptoms.
  • Hot flashes – Used off-label to alleviate menopausal hot flashes by stabilizing nerve activity that influences body temperature regulation. Gabapentin is an alternative for those who cannot take hormone therapy.

What Are the Side Effects of Gabapentin?

The side effects of Gabapentin are dizziness, drowsiness, and nausea, which lessen over time as the body adjusts, mood changes, breathing difficulties, severe allergic reactions, requiring medical attention, dependence, withdrawal symptoms, or cognitive impairment.

What Are the Side Effects of Gabapentin

Gabapentin’s increasing prevalence has raised concerns about its potential for misuse. Prescriptions in the United States surged from 39 million in 2012 to 64 million in 2016, making it the 10th most prescribed medication that year, according to Lanham S. & Riley B. 2022 in “Gabapentin Presents High Potential for Misuse.” This sharp rise underscores growing worries about both the short-term and long-term effects of gabapentin addiction.

The side effects of Gabapentin are given below:

  • Nausea – A feeling of sickness or discomfort in the stomach, sometimes leading to vomiting. Gabapentin affects the central nervous system, which interferes with digestion and causes stomach irritation, especially in the early stages of treatment. Taking it with food does cut nausea.
  • Headaches – Persistent or throbbing pain in the head, occurring in the first weeks of use. Gabapentin alters nerve activity, which generates changes in blood flow and neurotransmitter levels, triggering headaches in some users. Staying hydrated and adjusting dosage under medical supervision helps.
  • Diarrhea – Loose or watery stools that are accompanied by stomach cramps. Gabapentin influences the nervous system, which also regulates digestion, eliciting gastrointestinal issues. This side effect gets better as the body adjusts to the medication.
  • Mood changes – Increased irritability, anxiety, or depressive symptoms, especially in individuals with mental health conditions. Gabapentin affects gamma-aminobutyric acid (GABA) levels in the brain, which regulate mood, potentially leading to emotional instability or heightened distress in sensitive individuals.
  • Swollen arms and legs – Fluid retention causing puffiness, particularly in the hands, feet, or ankles. Gabapentin modifies sodium and fluid balance in the body, leading to peripheral edema. This swelling is more pronounced in those with pre-existing kidney conditions.
  • Blurred vision – Difficulty focusing or seeing clearly, temporary but requiring caution when driving or operating machinery. Gabapentin impacts nerve signals, including those involved in vision, which induces temporary visual disturbances or double vision.
  • Dry mouth – A lack of saliva production, leading to discomfort, difficulty swallowing, or an increased risk of cavities. Gabapentin affects nervous system function, sometimes reducing saliva secretion, which elicits persistent dry mouth and oral health issues.
  • Difficulty getting an erection – Sexual dysfunction, including reduced libido or erectile difficulties in men. Gabapentin affects neurotransmitters and nerve signaling involved in sexual response, potentially leading to decreased blood flow and arousal issues.
  • Memory problems – Difficulty recalling information, short-term memory loss, or trouble concentrating. Gabapentin alters brain function by influencing GABA activity, which brings about cognitive fog, difficulty processing information, or confusion.
  • Fatigue – Persistent tiredness, lack of energy, or feeling excessively sleepy during the day. Gabapentin depresses central nervous system activity, slowing down brain function and leading to excessive drowsiness or lethargy.
  • Dizziness – A spinning sensation or unsteadiness, increasing the risk of falls. Gabapentin affects balance and coordination by interfering with nerve signals in the brain, making users more prone to lightheadedness or vertigo.
  • Tremors – Involuntary shaking of hands, fingers, or other parts of the body. Gabapentin influences nerve excitability, which sometimes results in unintended muscle movements or trembling, particularly in higher doses.
  • Weight gain – Increased appetite and metabolic changes leading to gradual weight gain. Gabapentin alters metabolism and hunger signals, causing an increase in caloric intake and fluid retention, contributing to gradual weight gain over time.
  • Breathing difficulties – Shortness of breath or slowed breathing, particularly when combined with opioids or sedatives. Gabapentin depresses the nervous system, which affects respiratory function, especially in individuals with pre-existing lung conditions or those taking other depressants.
  • Severe allergic reactions – Rash, itching, swelling, or anaphylaxis requiring immediate medical attention. Gabapentin triggers hypersensitivity reactions in some individuals, potentially leading to life-threatening symptoms such as difficulty breathing or widespread swelling.

Does Gabapentin Cause Weight Gain?

Yes, gabapentin causes weight gain, though it is considered an uncommon side effect. DeToledo et al. 1997 examined body weight changes in 44 patients on high-dose gabapentin (GPN) therapy for ≥12 months. Of these, 10 patients gained >10% of their baseline weight, 15 gained 5–10%, 16 had no change, and 3 lost 5–10%. Weight gain began around months 2–3 and stabilized by months 6–9, despite unchanged GPN doses. This effect occurred with GPN monotherapy and combination therapy with other antiepileptic drugs, as detailed in “Changes in Body Weight with Chronic, High-Dose Gabapentin Therapy.”

Does Gabapentin Make You Sleepy?

Yes, gabapentin does make you sleepy. Clinical data has shown that approximately 19% of patients older than 12 years of age reported somnolence when taking gabapentin, compared to 9% in the placebo group, as per data provided by the FDA (2017).

Does Gabapentin Make You Sleepy

This sedative effect is attributed to gabapentin’s influence on the central nervous system, which slows neural activity and sets up feelings of sleepiness. Patients are advised to exercise caution when engaging in activities that require alertness, such as driving or operating heavy machinery until they understand how gabapentin affects them.

Is Gabapentin Addictive?

Yes, gabapentin is addictive, particularly when misused or taken in higher doses than prescribed. While initially considered to have a low potential for abuse, recent reports indicate that some individuals misuse gabapentin to enhance the effects of other substances, such as opioids, or to achieve a euphoric high. This misuse precipitates physical dependence and withdrawal symptoms upon cessation.

The U.S. Food and Drug Administration (FDA) approved gabapentin for treating seizures and shingles-related pain. However, its widespread off-label use for nerve pain and other conditions led to a rise in prescriptions, doubling from approximately 13 to 27 per 1,000 insured individuals between 2009 and 2016. By 2019, gabapentin had become the seventh most prescribed medication in the U.S., as reported by Kuehn B. 2022 in “Gabapentin Increasingly Implicated in Overdose Deaths.”

What Are the Withdrawal Symptoms of Gabapentin?

The withdrawal symptoms of gabapentin are anxiety, insomnia, rapid heartbeat, sweating, nausea, headaches, irritability, and tremors. These effects arise as the body, having adapted to gabapentin’s regulation of nerve activity, struggles to restore balance once the drug is discontinued. Symptoms typically emerge within 12 to 24 hours after the last dose, peak in intensity between 48 and 72 hours, and persist for several days.

What Are the Withdrawal Symptoms of Gabapentin

A survey established that individuals taking daily doses ranging from 400 mg to 8,000 mg for at least three weeks experienced withdrawal symptoms upon cessation. Higher doses, linked to substance misuse, accelerate tolerance, heighten dependence, and intensify withdrawal severity. The drug’s manufacturer has also documented withdrawal cases in individuals who discontinued high off-label doses of gabapentin, as noted by Drugs.com in “Is Gabapentin Addictive?”.

How Long Does Gabapentin Stay in Your System?

Gabapentin has an average half-life of 6 to 8 hours, meaning it takes this duration for half of the drug to be eliminated from the body, as revealed by Siao et al. 2010 in “Pharmacokinetics of Gabapentin in Cats.” Complete elimination occurs within 48 hours, but detection varies depending on the biological sample tested. In blood, gabapentin remains detectable for up to two days, while in urine, it is identified for one to three days due to renal excretion.

Saliva tests detect gabapentin for up to 48 hours, whereas hair tests provide the longest detection window, with traces potentially remaining for up to 90 days. In humans, gabapentin is excreted unchanged through renal clearance and does not interact with plasma proteins.

Can You Overdose on Gabapentin?

Yes, you can overdose on gabapentin, particularly when taken in excessive doses exceeding 49 grams, as provided by the FDA Approved Labeling Text (2011), or combined with other central nervous system depressants like opioids or alcohol. Gabapentin overdose ensues because the drug affects neurotransmitter activity, hatching severe nervous system depression and toxicity. High doses overwhelm the body’s ability to eliminate the drug, increasing the risk of life-threatening complications. Symptoms of a gabapentin overdose are extreme drowsiness, dizziness, confusion, slurred speech, double vision, loss of coordination, respiratory depression, and unconsciousness.

Can You Take Gabapentin While Pregnant?

Yes, you can take gabapentin while pregnant but its safety remains uncertain. There are clinical extrapolations that suggest potential risks, including fetal malformations and low birth weight, others indicate minimal harm. The U.S. Food and Drug Administration (FDA) classifies gabapentin as a Category C drug, meaning animal experiments have shown adverse effects on fetal development, but adequate human studies are lacking. Pregnant individuals must only take gabapentin if the latent benefits outweigh the risks, certainly when treating severe conditions like epilepsy or chronic neuropathic pain.

Maternal gabapentin use, particularly in the later stages of pregnancy, has been connected to a higher risk of preterm birth (delivery before 37 weeks) and small for gestational age (SGA) infants, defined as newborns weighing less than 5 pounds, 8 ounces (2,500 grams) at birth. A study by Fujii et al. 2013 in “Pregnancy Outcomes Following Gabapentin Use” analyzed 223 pregnancies and found that among 61 infants exposed to gabapentin until delivery, 38% (23 cases) necessitated admission to the neonatal intensive care unit (NICU) or special care nursery for treatment or observation. In contrast, only 2.9% (6 of 201) of unexposed live births needed NICU care, underscoring the potential neonatal risks associated with gabapentin use during pregnancy.

Can You Drive While Taking Gabapentin?

No, you cannot drive while taking gabapentin, especially when starting the medication or adjusting the dose. Gabapentin affects the central nervous system, causing drowsiness, dizziness, blurred vision, and impaired coordination, all of which considerably trim reaction times and jack up the risk of accidents. Patients are advised to assess how gabapentin affects them before driving or operating heavy machinery, as the severity of side effects varies among individuals.

In controlled epilepsy trials involving patients over 12 years old taking NEURONTIN at doses up to 1,800 mg daily, somnolence, dizziness, and ataxia occurred at higher rates compared to placebo. Somnolence was reported in 19% of gabapentin users versus 9% in the placebo group, dizziness in 17% versus 7%, and ataxia in 13% versus 6%. These side effects were among the most common reasons for discontinuation, with 1.2% stopping due to somnolence, 0.8% due to ataxia, and 0.6% due to fatigue, as reported by the U.S. FDA (2017).

How Does Gabapentin Interact with Alcohol?

Gabapentin interacts with alcohol by augmenting central nervous system depression, causing elevated drowsiness, dizziness, impeded coordination, and cognitive dysfunction. This combination heightens the risk of respiratory depression, which is life-threatening at high doses. Additionally, concurrent use worsens mood instability and contributes to substance dependence.

A randomized, placebo-controlled, double-blind clinical trial involving 150 patients, conducted by researchers at The Scripps Research Institute (TSRI), confirmed that gabapentin is both safe and effective in treating alcohol dependence. Barbara J. Mason, co-director of the Pearson Center for Alcoholism and Addiction Research at TSRI, stated that gabapentin’s effect on reducing alcohol consumption is comparable to or even greater than FDA-approved treatments. Additionally, gabapentin is the only medication shown to bolster sleep and mood in individuals cutting or quitting alcohol, making it a promising option for primary care settings.

How Does Gabapentin Interact with Other Medications?

Gabapentin interacts with other medications in ways that adjust its effectiveness or raise the risk of adverse effects. Nearly 90% of drug overdose deaths in which gabapentin was detected also involved an opioid, with an increasing presence of illicitly manufactured fentanyl, as highlighted by the Centers for Disease Control and Prevention (2022) in “Notes from the Field: Trends in Gabapentin Detection and Involvement in Drug Overdose Deaths — 23 States and the District of Columbia, 2019–2020. Common medications Gabapentin interacts with are given below:

  • Opioids: Combining gabapentin with opioids, such as morphine or oxycodone, intensifies sedation and respiratory depression, mounting the risk of overdose. ” Concurrent use of gabapentin with opioids increases the risk of fatal opioid overdose by 49%, as determined by Gomes et al. 2017 in “Gabapentin, Opioids, and the Risk of Opioid-related Death: A Population-based Nested Case-control Study.”
  • Antidepressants: Gabapentin amplifies the effects of antidepressants, particularly SSRIs and SNRIs, thus magnifying dizziness, drowsiness, and coordination issues.
  • Antacids: Aluminum- and magnesium-based antacids interfere with gabapentin absorption, reducing its effectiveness if taken within two hours of gabapentin administration.

Can You Take Gabapentin on an Empty Stomach?

Yes, you can take gabapentin on an empty stomach. The medication’s absorption is not relevantly affected by food, though taking it with a meal does assist in diminishing potential gastrointestinal discomfort. Certain formulations, such as gabapentin enacarbil, are taken with food to crank up absorption. Always follow the prescribing instructions to ensure optimal effectiveness.

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