Gabapentin is a drug used to treat partial seizures, pain from nerve damage, and some movement disorders. However, it’s been increasingly used off-label and many people misuse or abuse it. Read this post to learn about the conventional and not-so-conventional uses of gabapentin.
- Mechanism of Action
- Uses and Positive Effects of Gabapentin
- 1) Gabapentin Reduces Seizures in Drug-Resistant Partial Epilepsy
- 2) Gabapentin For Pain
- 3) Gabapentin Treats Essential Tremor and Restless Leg Syndrome
- 4) Gabapentin For Anxiety
- 5) Gabapentin Treats Migraines
- 5) Gabapentin For Sleep
- 6) Gabapentin May Help Extreme Hiccupping
- 7) Gabapentin May Treat Addiction
- Gabapentin Dosage
- Gabapentin and Neurontin Side Effects
- Gabapentin and Neurontin High
- Gabapentin Withdrawal
- Is Gabapentin a Narcotic?
- Is Gabapentin Addictive?
- Gabapentin Drug Interactions
- Gabapentin and Alcohol
- SNPs that Affect Gabapentin Metabolism
- Pregabalin: A More Efficient Gabapentin
- Gabapentin for Dogs
- User Reviews
Gabapentin is an anticonvulsant and antiepileptic drug usually prescribed under the brand name Neurontin. It is used to treat partial seizures, neuropathic pain, and essential tremors. However, it has several “off-label” uses with mixed results. The full mechanism is not yet known.
Mechanism of Action
The mechanisms are not fully understood, but it is known that gabapentin increases GABA in the brain in both rodent and human brains [R].
Gabapentin binds to calcium ion channels in the brain and spine, which decreases neurotransmitters like glutamate, calcitonin gene-related peptide (CGRP), and substance P. This reduces abnormal brain activity that causes seizures, tremors, and pain [R, R, R].
Uses and Positive Effects of Gabapentin
1) Gabapentin Reduces Seizures in Drug-Resistant Partial Epilepsy
Many epileptic patients suffer from drug-resistant epilepsy and require additional intervention to control their seizures [R].
Gabapentin is primarily used as an add-on medication for partial epilepsy, also known as focal epilepsy. In focal epilepsy, the seizures start on one side of the brain, while in generalized epilepsy seizures start on both sides [R, R, R].
Gabapentin can reduce the frequency of both drug-resistant secondarily generalized partial seizures and complex partial seizures [R].
A meta-analysis of 1206 patients with drug-resistant partial epilepsy showed that gabapentin significantly reduced seizure frequency [R].
2) Gabapentin For Pain
Neuropathic pain is any pain due to nerve damage. Gabapentin reduces neuropathic pain caused by shingles (postherpetic neuralgia) and diabetes (peripheral diabetic neuropathy) [R].
Specifically, gabapentin reduces pain caused by increased sensitivity to already painful stimuli (hyperalgesia) and pain due to normally painless stimuli (allodynia), by binding to calcium channels [R].
A meta-analysis of 5914 patients found that 30-40% of them (on a normal daily dose of gabapentin – 1800-3600 mg) experienced “worthwhile” pain reduction by at least 50%. “Worthwhile” pain reduction is associated with improved:
- Sleep disturbances
- Quality of life
- Quality of work
- Quality of function
However, not everyone will experience this level of improvement and may find that the side effects (dizziness, sleepiness, swelling of limbs, and gait disturbance) outweigh the benefits [R].
A study of 351 patients (DB-PCT) focused on patients with at least two of the following:
- Pain due to normally painless stimuli (allodynia)
- Burning pain
- Shooting pain
- Increased sensitivity to pain (hyperalgesia)
Overall, gabapentin significantly improved their neuropathic pain and quality of life [R].
Similarly, there is some evidence that gabapentin treats sciatica, which is pain that spreads from the back to below the knee. It has multiple causes (i.e. herniated disk, tumors, infections, pregnancy, etc.). Two case studies showed that gabapentin significantly improved pain, and one patient was permanently cured [R].
Gabapentin Treats Pain and Impaired Walking due to Multiple Sclerosis
Multiple sclerosis is a common autoimmune disease of the brain. Four out of five multiple sclerosis patients suffer from spasticity, which involves contraction of the muscles that can impair walking and cause pain [R].
Gabapentin Treats Pain in Cancer Patients
Gabapentin, in combination with opioids (morphine), improves neuropathic cancer pain, leading to more daily activity, better sleep, improved mood, and enhanced quality of life. Importantly, when gabapentin and morphine are used together, they can be taken at lower doses [R].
Gabapentin May Treat Fibromyalgia
Gabapentin may also be used to treat pain due to fibromyalgia, which affects approximately 2% of the population [R].
Fibromyalgia is pain that lasts more than three months [R].
A study of 150 patients (DB-PCT) found that gabapentin significantly improved pain and sleep. Notably, half of the patients experienced at least 30% reduction in their pain [R].
3) Gabapentin Treats Essential Tremor and Restless Leg Syndrome
Essential tremor is a movement disorder that causes tremors when trying to continue a particular action [R].
Gabapentin significantly improved tremors in a study of 16 patients (DB-PCT) who were not taking other tremor medications [R].
Gabapentin may improve tremor through binding and inhibiting calcium-ion channels (alpha-2 delta subunit) leading to a reduction in tremors [R].
Restless Leg Syndrome
Restless leg syndrome is a brain disorder that also results in involuntary movements. A study of end-stage kidney failure patients found that gabapentin could be used (usually 200–300 mg/3 times a week) to treat this syndrome in combination with dialysis [R].
According to a small trial with 8 patients, regular use of gabapentin can:
4) Gabapentin For Anxiety
Several small studies have shown that gabapentin improves anxiety.
A study of 50 female patients with moderate-to-high anxiety (DB-PCT) found that taking 1,200 mg of gabapentin before a surgery significantly reduced anxiety and pain catastrophizing, which is when patients are severely fixated and worried about experiencing or anticipating pain [R].
Social anxiety causes people to fear and avoid social situations. A small study of 8 patients with social anxiety disorder found that gabapentin (1800 mg/day) reduces anxiety similarly to other anxiety medications like selective serotonin reuptake inhibitors (SSRIs) and benzodiazepines [R].
Finally, gabapentin also reduces anxiety and improves sleep in patients with both an anxiety-related disorder (i.e., panic disorder, alcohol dependence, obsessive-compulsive disorder, generalized anxiety, or drug dependency) and schizophrenia, schizoaffective or bipolar disorder [R].
Similar cases of patients with anxiety-related disorders showed various improvements such as better sleep as well as the reduction of the following:
- Depression symptoms
- Use of alcohol as self-medication
- Avoidance of fears (phobic avoidance)
- Anxiety related to anticipation (anticipatory anxiety) [R]
5) Gabapentin Treats Migraines
Gabapentin is also used to treat chronic migraines. A study of 143 patients (DB-PCT) found that gabapentin helps treat chronic migraines, and almost half of patients taking 2400 mg/day had their migraine frequency cut in half [R].
Another study of 63 patients (DB-PCT) showed similar results while taking 1200 mg/day [R].
In rats, gabapentin reduces the release of calcitonin gene-related peptide (CGRP) and substance P in the spinal cord, which is associated with inflammation and pain [R].
5) Gabapentin For Sleep
Hot flashes are a common side effect in breast cancer survivors and menopause and can negatively impact sleep quality.
A study of 58 breast cancer survivors with chronic daily hot flashes found that a daily dose of gabapentin (900 mg) improves the duration and quality of their sleep [R].
Gabapentin also improves hot flashes due to menopause [R].
6) Gabapentin May Help Extreme Hiccupping
A case study of a patient with essential tremor who suffered from chronic refractory hiccup for over 50 years found that giving her gabapentin as an add-on daily medication (3 x 300 mg/day) improved her hiccups. When she stopped taking gabapentin, the hiccups returned [R].
Due to the lack of large-scale studies and because most patients were treated for other health issues, it is hard to conclude how effective gabapentin is as a primary medication [R].
7) Gabapentin May Treat Addiction
For opioid addiction, a study of 27 patients showed that taking high doses of gabapentin (1600 mg) in combination with methadone can reduce some opioid withdrawal symptoms such as coldness, twisting (yawing), diarrhea, mood deterioration (dysphoria), and muscle tension [R].
A similar study of 60 patients (DB-PCT) showed similar opioid withdrawal symptom relief, but only at 300 mg. Importantly, gabapentin also lowered the amount of methadone that the patients used [R].
The typical adult dosage (>12 years) is between 900-3600 mg/day, depending on individual response [R].
In all cases, patients start at lower doses and titrate up to a full dose.
Oral doses are normally taken three times per day due to the short half-life of the drug [R].
Adults (over 12 years): Effective dose is 900-1800 mg/day (maximum 2400 mg/day)
- Titration: Start at 300 mg/day (1 x 300 mg), then titrate up to 600 mg/day (2 x 300 mg) and finally to 900 mg/day (3 x 300 mg). Increase dose as needed.
- Maximum dose: 2400 mg (3 x 800 mg/day)
Children (3-4 years): 40 mg/kg/day (divided into three doses)
Children (5-12 years): 25–35 mg/kg/day (divided into three doses) [R].
Adults (over 12 years): Effective dose is 900-1800 mg/day [R].
- Day 1: 300mg (1 x 300 mg/day)
- Day 2: 600 mg (2 x 300 mg/day)
- Day 3: 900 mg (3 x 300 mg/day)
- Increase as needed
Note: People with kidney problems take lower doses in guidance with their doctor [R].
100 mg capsules are the lowest dose available. It may be used for those who require lower doses (i.e., children and people with kidney problems) or in combination with other capsules and tablets to create a higher dose.
300 mg capsules are used as the initial dose for the treatment of epilepsy and postherpetic neuralgia in adults. Patients start at 1 x 300 mg/day and increase by 300 mg increments until an effective dose is reached [R].
800 mg tablets are the highest dose available. In the treatment of epilepsy, the maximum recommended dose is 2400 mg/day (3 x 800 mg/day) [R].
Interestingly, in India, over 80% of doctors only prescribe 100 mg-300 mg of gabapentin per day for the treatment of neuropathic pain [R].
Gabapentin is hardly metabolized, so gabapentin overdose is rare. However, in people with kidney problems, toxicity is possible and symptoms may include: dizziness, confusion, lack of energy (lethargy), twitching (myoclonus), poor coordination or unsteady gait (ataxia), and shaking (tremulousness). Peritoneal dialysis effectively treats toxicity [R].
Gabapentin and Neurontin Side Effects
Most users reported the following side effects, but they are usually mild:
- Sleepiness [R, R].
- Dizziness [R, R].
- Poor coordination or unsteady gait (ataxia) [R].
- Weakness/Fatigue [R, R].
- Nausea [R].
- Weight gain [R].
- Infections [R].
- Swelling (edema) [R].
- Memory loss [R].
- Diarrhea [R].
Gabapentin passes through the kidneys and is released from the body with the urine. Gabapentin poses a risk for patients with kidney problems. However, it can be used with guidance from a doctor and in conjunction with dialysis, which will remove the gabapentin from the body [R].
Gabapentin and Neurontin High
Some users report a “high” when taking gabapentin alone or in combination with other drugs. Self-described effects include:
- Euphoria (like a weaker opioid high)
- Marijuana-like high
- Becoming more social
- Effects similar to amphetamine
Gabapentin (1500 mg-12,000 mg) may cause euphoria alone or when combined with:
Gabapentin (600-4800 mg) may cause sedation alone or when combined with:
- Buprenorphine/naloxone [R].
Withdrawal symptoms can appear in the window of 12 hours to a week after stopping the medication. Most occur within a 48-hour window [R].
Symptoms usually include agitation, confusion or disorientation. However, they may also consist of sweating, gastrointestinal problems, tremor, irregular heartbeat, high blood pressure, sleep problems, restlessness, immobility (catatonia), and seizures. Gabapentin use during pregnancy may cause withdrawal in newborns [R].
Therefore, patients should slowly taper off of the medication with doctor supervision [R].
Is Gabapentin a Narcotic?
In the US, gabapentin is not officially a narcotic. The FDA defines a narcotic as any of the following:
- Opium/Opiates and their derivatives (e.g. heroin and morphine)
- Poppy straw
- Coca leaves and extracts with their derivatives intact (cocaine and ecgonine)
- Cocaine and its derivatives, salts, and/or isomers
- Ecgonine and its derivatives, salts, and/or isomers
- Any combination of the above [R].
Informally, however, the definition is broader and may refer to any addictive, controlled, or illegal painkiller that affects mood and behavior.
Medically, it has the same meaning as opioid medications but often gives a negative connotation [R].
Importantly, gabapentin is often used in combination with, or instead of, opioids, which are narcotics [R].
Is Gabapentin Addictive?
People experiment with doses 3-20 times higher than the recommended dose [R].
According to one study, around 50% of the people misuse the prescribed medication through self-medication, recreational use, or self-harm. Some people combine it with opioids, benzodiazepines, alcohol, or heroin [R, R].
Opioid addicts/abusers are the most at risk. About 1 in 5 opioid abusers abuse gabapentin [R].
Importantly, combining gabapentin with opioids can increase the chances of overdose and death due to respiratory problems. This may be due to gabapentin reversing the person’s accumulated drug tolerance or due to its effect on breathing [R, R].
Gabapentin May Increase Alcohol Dependence in Social Drinkers
Despite some medical interest in using gabapentin to help with alcohol addiction, there may be a risk of dependence. A study found that gabapentin (60 mg/kg) increased rats’ dependence on alcohol. There is interest in determining whether Gabapentin poses the same risk to humans, i.e., social drinkers [R].
Gabapentin Has Controversial Effects on Depression and Suicide
An analysis of 131,178 psychiatric and nonpsychiatric patients found that gabapentin decreased the risk of suicides among psychiatric patients and did not affect non-psychiatric patients at all [R].
However, another analysis of 297,620 patients found that gabapentin significantly increased the risk of suicide or suicide attempts [R].
Gabapentin Drug Interactions
- Antacids – Antacids (magnesium oxide or aluminum) decrease the effect of gabapentin on the body [R, R]. Take gabapentin at least two hours apart from antacids [R].
- Opiates [R] – There is a risk of drug abuse among opioid addicts. Gabapentin may affect breathing, increasing the risk of opioid overdose and death [R, R].
Gabapentin and Alcohol
- In addition to the risk of abuse, gabapentin may increase the effects of alcohol, including impairing coordination dexterity function [R]. People recreationally combine gabapentin with alcohol [R, R].
- Gabapentin may increase the effects of alcohol, including impairing coordination dexterity function [R].
- Gabapentin may help treat alcohol addiction [R], but there may also be a risk of dependence. Gabapentin (60 mg/kg) increased rats’ dependence on alcohol, which might pose a risk to social drinkers [R].
SNPs that Affect Gabapentin Metabolism
Proper kidney function is critical for removing gabapentin from the body. OCTN1 is responsible for transporting gabapentin in the intestine and kidney. The OCTN1-L503F polymorphism decreases the transport gabapentin in the kidney [R].
Pregabalin: A More Efficient Gabapentin
Pregabalin is a drug in the same class as gabapentin (gabapentinoids), with a similar mechanism of binding to calcium channels [R].
Pregabalin is absorbed much more quickly than gabapentin.
Dosages for pregabalin are much lower than gabapentin, ranging from 75-600 mg/day.
Gabapentin and pregabalin are absorbed in the small intestine, but pregabalin is also absorbed by the colon [R].
Pregabalin is taken two or three times a day while gabapentin is usually taken three times a day. Additionally, pregabalin differs from gabapentin in that its absorption into the body is independent of the dose. However, gabapentin is dose-dependent, meaning that as the dose increases, the proportion of gabapentin absorbed by the body is reduced [R].
Neither drug is significantly broken down by the body (metabolized), so both are released through urine [R].
Similar to gabapentin, it is used to treat anxiety disorder, fibromyalgia and also has a similar risk for side effects, drug abuse and withdrawal [R].
Gabapentin for Dogs
Gabapentin is used in both dogs and cats to treat chronic pain, particularly neuropathic. However, the current evidence for its use in dogs is low.
Several studies found that gabapentin was not better than placebo in relieving pain after surgical procedures in dogs. However, none of these studies used the previously suggested dosing (10–20 mg/kg every 8 hours) [R].
Gabapentin was effectively reduced postoperative pain in dogs only in combination with morphine, reducing the amount of morphine required [R].
Gabapentin was effective in treating epilepsy in dogs, which was not responsive to other treatments, with few minor side effects [R].
One woman found gabapentin helpful for peripheral neuropathy. However, she has blurry vision in the mornings and also feels pain whenever she misses a dose.
Another woman began taking gabapentin for her hot flashes when other medications and acupuncture stopped working. She only takes it as needed.
A user who has struggled for over 20 years with alcoholism found that gabapentin helped with the alcohol withdrawal.
One person taking gabapentin for epilepsy mentioned he is now experiencing erectile dysfunction.
One person using gabapentin in combination with Tegretol has had no seizures for 15 years.
However, another individual who experienced seizures and was an alcoholic saw no improvement with gabapentin.
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