Gabapentin Overdose and Toxicity

What Is Gabapentin?

Gabapentin is a pharmaceutical medication originally intended for use in the treatment of seizures.

However, gabapentin is most commonly prescribed for conditions other than seizures and epilepsy, such as pain syndromes. Since gabapentin is not an opioid, in theory, it has lower abuse potential and is more readily prescribed for pain than more addictive medications. Gabapentin can also be used to treat:

      • Nerve pain, such as from a shingles outbreak
      • Treating alcohol or cocaine withdrawal
      • Restless legs syndrome
      • Diabetic neuropathy
      • Fibromyalgia
      • Hot flashes

How Does Gabapentin Work?

Gabapentin is a calming chemical that has a similar chemical structure to Gamma-aminobutyric acid (GABA), which is a brain chemical that calms the nervous system. However, gabapentin does not bind to the body’s GABA receptors. Instead, gabapentin affects the body’s calcium channels to reduce seizures and nerve pain.

gabapentin mechanism of actions
gabapentin mechanism of actions

How Addictive is Gabapentin?

Gabapentin is thought to be less addictive than opioid medications for pain relief. Overall, gabapentin is not considered a highly addictive drug. Many cases of gabapentin abuse occur in people who already have addictions to opioids and other drugs.

In response to increased abuse of gabapentin, some states are classifying gabapentin as a Schedule V controlled substance. While gabapentin appears to have low abuse potential, it is often used in conjunction with other, more addictive, drugs.

It’s possible to fatally overdose on gabapentin. Reports of gabapentin being abused alone, and with opioids, prompted the FDA to release a warning statement (in December 2019) about the fatal risk of respiratory depression. Signs of overdose include:

      • Ataxia (decreased muscle coordination)
      • Diarrhea
      • Drooping eyelid
      • Drowsiness and lethargy
      • Double vision
      • Excitation
      • Hypoactivity
      • Labored breathing
      • Marked sedation
      • Slurred speech

If you suspect an overdose, you need immediate medical treatment. The only way to remove the drug is through kidney dialysis in the emergency room.

Gabapentin Addiction Statistics

A study published in 2013 conducted in Kentucky showed that among 503 participants reporting illegal drug use, 15% reported using gabapentin to “get high” in the previous six months.

That percentage was a 165% increase from the year prior. A national assessment found that nearly a quarter of patients with co-prescriptions of opioids and gabapentin had three or more prescriptions exceeding established dosage thresholds.

In comparison, in patients prescribed just opioids or just gabapentin, the figures were 8% and 3% respectively.

Can You Overdose on Gabapentin?

Despite the well-known withdrawal side effects, it’s difficult to overdose on gabapentin. Studies have shown that even at very high levels of ingestion, people have only suffered mild to moderate physical and mental side effects that are rarely life-threatening. So far, there have been only two peer-reviewed case reports of death  from gabapentin toxicity (related to gabapentin overdose). Despite this low statistic, gabapentin abuse as a suicide attempt has risen over the years.

While this means gabapentin is a relatively safe drug, it still should not be ingested in large amounts. However, people taking gabapentin should be aware that it does have particularly unpleasant withdrawal symptoms, even after taking it for a relatively short amount of time and at low doses.

Symptoms of Gabapentin Overdose

Most side effects of a gabapentin overdose will be related to an overall deceleration of the body’s systems. Drowsiness, muscle weakness, lethargy and drooping eyelids can be expected. Other gabapentin overdose symptoms include diarrhea and sedation. These symptoms arise because gabapentin is formulated to slow down misfirings in the brain that cause seizures.

Those who use gabapentin should be aware that stopping gabapentin abruptly can actually increase the chance of experiencing seizure activity. Suddenly removing the anti-seizure effect can cause a rebound, raising the risk of seizures. Gabapentin is a powerful drug that must be tapered slowly to avoid some of its more severe withdrawal side effects.

Is Gabapentin Considered as Controlled Substance ?

Gabapentin is not currently a controlled substance at the federal level, but certain states have made gabapentin a controlled substance at the state level. This includes Kentucky, Michigan, Tennessee, Virginia and West Virginia.

Does Gabapentin have any warnings when taking the drug?

The FDA has issued several warnings for gabapentin. These include certain side effects like Drug Reaction with Eosinophilia and Systemic Symptoms, or DRESS, and allergic reactions like anaphylaxis or angioedema, a swelling of the lips or face. The drug should be stopped immediately if any of those side effects are suspected. Other side effects that need to be monitored include impaired motor skills, drowsiness, dizziness, mental status changes, slowed breathing and a possible increase in suicide risk.

How is Gabapentin taken?

Gabapentin is taken by mouth. There are various dosage forms of the medication, including capsules, oral solutions and tablets. The drug comes in both immediate-release (IR) and extended-release (ER) formulations.

Does Gabapentin have other names?

Gabapentin may be sold under different brand names, including Neurontin and Gralise.

What ingredients are in Gabapentin?

Gabapentin is part of its own drug class, called gabapentinoids. Typical dosages range from 100 milligrams to 800 milligrams of the drug. Some inactive ingredients in the gabapentin tablets or capsules include:

Gabapentin is not currently a controlled substance at the federal level, but certain states have made gabapentin a controlled substance at the state level. This includes Kentucky, Michigan, Tennessee, Virginia and West Virginia.

Does Gabapentin have any warnings when taking the drug?

The FDA has issued several warnings for gabapentin. These include certain side effects like Drug Reaction with Eosinophilia and Systemic Symptoms, or DRESS, and allergic reactions like anaphylaxis or angioedema, a swelling of the lips or face. The drug should be stopped immediately if any of those side effects are suspected.

Other side effects that need to be monitored include impaired motor skills, drowsiness, dizziness, mental status changes, slowed breathing and a possible increase in suicide risk.

How is Gabapentin taken?

Gabapentin is taken by mouth. There are various dosage forms of the medication, including capsules, oral solutions and tablets. The drug comes in both immediate-release (IR) and extended-release (ER) formulations.

Does Gabapentin have other names?

Gabapentin may be sold under different brand names, including Neurontin and Gralise.

What ingredients are in Gabapentin?

Gabapentin is part of its own drug class, called gabapentinoids. Typical dosages range from 100 milligrams to 800 milligrams of the drug. Some inactive ingredients in the gabapentin tablets or capsules include:

        • Lactose
        • Talc
        • Cornstarch
        • Gelatin
        • Colors such as FD&C blue no. 2, yellow iron oxide
        • Titanium dioxide
        • Poloxamer 407
        • Magnesium stearate
        • Copovidone, cornstarch
        • Candelilla wax
        • Hydroxypropyl cellulose

 

Gabapentin Dosage for Partial Seizures

Gabapentin is used to treat epilepsy. It’s also taken for nerve pain. Nerve pain can be caused by different illnesses, including diabetes and shingles, or it can happen after an injury.

Occasionally, gabapentin is used to treat migraine headaches.

Gabapentin is available on prescription. It comes as capsules, tablets, and a liquid that you drink.

A doctor will need to sign your prescription by hand, and you’ll need to collect your medicine within 28 days. You’ll need to show the pharmacist proof of your identity.

How gabapentin works ?

In epilepsy, it’s thought that gabapentin stops seizures by reducing the abnormal electrical activity in the brain.

With nerve pain and migraine, it’s thought to interfere with pain messages travelling through the brain and down the spine to block pain.

Gabapentin dosage for partial seizures

Gabapentin is FDA-approved as adjunctive therapy for partial seizures in adults and children 3 years of age or older.

  • Standard gabapentin dosage for adults: 300 to 600 mg taken three times per day by mouth.
  • Maximum gabapentin dosage for adults: 3600 mg daily in three divided doses.
  • Renally impaired patients (kidney disease)—dose amount and dose frequency adjustment:
    1. Creatinine clearance of 30-59 ml/min: 200 to 700 mg twice per day
    2. Creatinine clearance of 16-29 ml/min: 200 to 700 mg once per day
    3. Creatinine clearance of 15 ml/min or less: 100 to 300 mg once per day decreased proportionately (1/15 per whole number value) for each decrease in creatinine clearance
    4. Hemodialysis: dose is dependent on estimated creatinine clearance; a supplemental dose of 125 to 350 mg is given after dialysis

Gabapentin Dosage for Children

Gabapentin is used to help control partial seizures (convulsions) in the treatment of epilepsy. This medicine cannot cure epilepsy and will only work to control seizures for as long as you continue to take it.

Gabapentin is also used to manage a condition called postherpetic neuralgia, which is pain that occurs after shingles.

Gabapentin works in the brain to prevent seizures and relieve pain for certain conditions in the nervous system. It is not used for routine pain caused by minor injuries or arthritis. Gabapentin is an anticonvulsant.

This medicine is available only with your doctor’s prescription.

This product is available in the following dosage forms:

      • Capsule
      • Tablet
      • Tablet, Extended Release, 24 HR
      • Solution
      • Suspension

Gabapentin Dosage for Children

Please remember that you are not allowed to buy Gabapentin Online if you are 19 years old and under. Please find a local doctor to prescribe you Gabapentin prescription and buy it in a local Gabapentin pharmacy.

Gabapentin is FDA-approved as a secondary treatment for partial seizures in children 3 years or older with epilepsy. The use of gabapentin in children for any other medical condition is not FDA-approved. Dosing will be determined by both the child’s age and weight.

Gabapentin dosage by age for children older than 3 years
Age (yr) Recommended dosage
3-4 yrs 40 mg per kg (18.2 mg/lb) of body weight divided into three doses Maximum: 50 mg per kg (22.7 mg/lb) of body weight daily
5-11 yrs 20-35 mg per kg (9.1-15.9 mg/lb) of body weight divided into three doses Maximum: 50 mg per kg (22.7 mg/lb) of body weight daily
12 yrs or older 300-600 mg taken three times per day Maximum: 3600 mg per day

Gabapentin Dosage for Adults

Gabapentin is a prescription drug. It comes as an oral capsule, an immediate-release oral tablet, an extended-release oral tablet, and an oral solution.

Gabapentin oral capsule is available as the brand-name drug Neurontin. It’s also available as a generic drug. Generic drugs usually cost less than the brand-name version. In some cases, the brand-name drug and the generic version may be available in different forms and strengths.

Why Gabapentin is Used

Gabapentin oral capsule is used to treat the following conditions:

    • Seizures: Gabapentin is used to treat partial (focal) seizures. It’s taken together with other seizure medications in adults and in children 3 years of age and older who have epilepsy.
    • Postherpetic neuralgia: This is pain from nerve damage caused by shingles, a painful rash that affects adults. Shingles appears after infection with the varicella zoster virus. This virus occurs in people who have had chicken pox.

Gabapentin may be used as part of a combination therapy. This means you may need to take it with other drugs.

Gabapentin Dosage for Adults

For adults, the gabapentin dosage can vary widely depending on the condition being treated. Upon starting treatment with gabapentin, the starting dose may be 100 to 300 mg per day and steadily increase until an effective dose is reached. The maximum dosage will depend on the condition being treated.

    • Standard gabapentin dosage for adults: 300-600 mg taken three times per day.
    • Maximum gabapentin dosage for adults: 1200 mg taken three times per day for a maximum daily dose of 3600 mg.

Gabapentin Dosage Chart for Adult

Indication Age Standard dosage Maximum dosage
Partial seizures
12 years and older 300-600 mg three times per day 3600 mg per day
5-11 years 25-35 mg/kg (11.4-15.9 mg/lb) per day divided into three daily doses 50 mg/kg (22.7 mg/lb) per day
3-4 years 40 mg/kg (18.2 mg/lb) per day divided into three daily doses 50 mg/kg (22.7 mg/lb) per day
Postherpetic neuralgia 18 years and older 300 mg on day 1, 300 mg twice daily on day 2, then 300 mg three times daily on day 3; dosage may be further increased after day 3 to 600 mg three times per day 1800 mg per day
Diabetic peripheral neuropathy 18 years and older 300-1200 mg three times per day (off-label) 3600 mg per day
Fibromyalgia 18 years and older 600 mg twice daily and 1200 mg at bedtime (off-label) 2400 mg per day
Alcohol dependence 18 years and older 300-600 mg three times per day (off-label) 1800 mg per day

Gabapentin Can be Used to Treat Anxiety and Depression

Gabapentin is an anticonvulsive medication which first discovered in the 1970s in Japan.

Its original use was as a muscle relaxer and anti-spasmodic medication, but later, it was discovered the potential of the medication as anticonvulsive medication and as an adjunct to stronger anticonvulsants.

Gabapentin
Gabapentin

Gabapentin is an anticonvulsant medication that got FDA approval for partial seizure therapy in 1993. Currently, gabapentin has FDA approval for:

    • Postherpetic neuralgia
    • Adjunctive therapy in the treatment of partial seizures with or without secondary generalization in patients over the age of 12 years old with epilepsy, and the pediatric population, 3 to 12 year-olds with a partial seizure
    • Moderate to severe restless leg syndrome (RLS) moderate to severe

It also has off-label use for neuropathic pain, fibromyalgia, bipolar disorder, postmenopausal hot flashes, essential tremors, anxiety, resistant depressant and mood disorders, irritable bowel syndrome (IBS), alcohol withdrawal, postoperative analgesia, nausea and vomiting, migraine prophylaxis, headache, interstitial cystitis, painful diabetic neuropathy, social phobia, generalized tonic-clonic seizures, pruritus (itching), insomnia, post-traumatic stress disorder (PTSD), and refractory chronic cough.

In one placebo-controlled, retrospective study that investigated the effects of gabapentin on about 700 patients with refractory partial seizure disorder, there was an improvement in overall well-being in patients. The effect prompted a controlled investigation of the drug in primary psychiatric conditions.

An important benefit of gabapentin is that there is no interaction with valproate, lithium, and carbamazepine. Also, gabapentin has minor side effects.

Gabapentin in the Treatment of Anxiety and Depression

Gabapentin is rarely prescribed for patients with only anxiety disorder but is commonly prescribed for patients with bipolar disorder to reduce anxiety levels. Clinicians can also use it for patients who have anxiety and depression. Since anxiety is a coping skill, there is no drug to treat anxiety, but the medications used for this purpose make it possible to live at the moment, giving patients a chance to undergo anxiety treatment with non-pharmaceuticals. Even though the studies show that gabapentin is ineffective in the treatment of bipolar disorder, a case-control study with 60 patients in an acute phase of mania had a significant reduction in symptoms of anxiety with lithium and 900 mg of gabapentin. In another study with 21, mixed-state patients refractory to mood stabilizers received gabapentin (up to 2000 mg per day) for eight weeks, and patients with depressive symptoms had significant improvement in their CGI-BP (Clinical Global Impression-Bipolar) scores.

A meta-analysis of 7 trials pointed to gabapentin’s greater efficacy versus placebo in generalized anxiety disorder (GAD), although the effect size was approximately 0.35 for mental anxiety symptoms. A study of 153 patients who responded to the initial treatment of 450 mg per day for maintenance treatment of social anxiety disorder.

There are no clinical studies on the effectiveness of gabapentin as monotherapy or adjunctive therapy in major depressive disorders. However, there are case reviews that show some patients with depression who are refractory to standard antidepressants but showed therapeutic improvement when using gabapentin as adjunctive therapy.

In a randomized, double-blind study, with 130 patients that had under eye surgery, a one-time dose of 600 mg gabapentin significantly reduced the perioperative anxiety compared to a placebo. However, there was no significant difference compared to melatonin.