What is the Action Mechanism of Gabapentin ? Is Gabapentin Addictive ?

signs someone is addicted to gabapentin

The chemical structure of gabapentin (Neurontin) is derived by addition of a cyclohexyl group to the backbone of gamma-aminobutyric acid (GABA). Gabapentin prevents seizures in a wide variety of models in animals, including generalized tonic-clonic and partial seizures.

The exact mechanism of action with the GABA receptors is unknown; however, researchers know that gabapentin freely passes the blood-brain barrier and acts on neurotransmitters.

Gabapentin has a cyclohexyl group to the structure of neurotransmitter GABA as a chemical structure. Even though it has a similar structure to GABA, it does not bind to GABA receptors and does not influence the synthesis or uptake of GABA.

Gabapentin works by showing a high affinity for binding sites throughout the brain correspondent to the presence of the voltage-gated calcium channels, especially alpha-2-delta-1, which seems to inhibit the release of excitatory neurotransmitters in the presynaptic area which participate in epileptogenesis.

Even though there is no evidence for direct action at the serotonin, dopamine, benzodiazepine, or histamine receptors, research has shown gabapentin to increase total-blood levels of serotonin in healthy control subjects.

The elimination half-life of gabapentin is 5 to 7 hours, and it takes two days for the body to eliminate gabapentin from its system.

One benefit of gabapentin use is its mild side-effect profile. The most common side effects are fatigue, dizziness, and headache.

Gabapentin has no activity at GABAA or GABAB receptors of GABA uptake carriers of brain. Gabapentin interacts with a high-affinity binding site in brain membranes, which has recently been identified as an auxiliary subunit of voltage-sensitive Ca2+ channels. However, the functional correlate of gabapentin binding is unclear and remains under study.

Gabapentin crosses several lipid membrane barriers via system L amino acid transporters. In vitro, gabapentin modulates the action of the GABA synthetic enzyme, glutamic acid decarboxylase (GAD) and the glutamate synthesizing enzyme, branched-chain amino acid transaminase.

Results with human and rat brain NMR spectroscopy indicate that gabapentin increases GABA synthesis. Gabapentin increases non-synaptic GABA responses from neuronal tissues in vitro. In vitro, gabapentin reduces the release of several mono-amine neurotransmitters.

Gabapentin prevents pain responses in several animal models of hyperalgesia and prevents neuronal death in vitro and in vivo with models of the neurodegenerative disease amyotrophic lateral sclerosis (ALS). Gabapentin is also active in models that detect anxiolytic activity.

Although gabapentin may have several different pharmacological actions, it appears that modulation of GABA synthesis and glutamate synthesis may be important.

Is Gabapentin Addictive ?

Asking about the signs someone is addicted to gabapentin first begs the question: What is gabapentin?

To answer that question requires putting gabapentin in perspective as a pharmaceutical drug that, while providing relief to thousands of people for nerve pain, also has the potential for abuse. It isn’t an opioid, but it has found a niche audience among those who take it recreationally, and for doctors who began to seek alternatives to narcotics as the opioid epidemic reached its apex, it seemed like a safer alternative.

In 2016, gabapentin was the 10th most prescribed drug in the United States, with 64 million prescriptions written that year . That was up from 39 million prescriptions written only four years earlier, in large part because “gabapentin, an anticonvulsant and analgesic for postherpetic neuralgia, has been thought to have no abuse potential despite numerous published reports to the contrary,” according to a 2018 article in the journal Psychology of Addictive Behaviors.

In that particular article, researchers analyzed data from a study of drug users in Kentucky who reported using gabapentin for non-medical purposes. Their findings? “Overall, the sample reported having initiated gabapentin more than 10 years earlier after having it prescribed for a legitimate, though generally off-label, medical indication (e.g., pain, anxiety, opioid detoxification). Participants reported use of gabapentin in combination with buprenorphine, other opioids, cocaine, and caffeine to produce sought-after central nervous system effects (e.g., muscle relaxation, pain reduction, sleep induction, feeling drunk, and feeling ‘high’).”

Gabapentin, such studies reveal, can be problematic. Whether used in conjunction with other drugs or on its own, it can be abused, which makes it a substance of concern. To understand the signs someone is addicted to gabapentin, however, requires some knowledge of what it is, where it comes from, how it works and how it can be addictive.

Comparative Studies

Gabapentin and lamotrigine have been compared in an open, parallel-group, add-on, randomized study in 109 patients with uncontrolled partial epilepsy and learning disabilities. The two drugs were similarly efficacious, with similar incidences of adverse events and serious adverse events. Neither lamotrigine nor gabapentin exacerbated any of the challenging behaviors observed in these patients.

The most common adverse reaction to gabapentin was somnolence, which was mostly reported during the initial titration phase.

In a double-blind comparison of gabapentin and lamotrigine in 309 patients with new-onset partial or generalized seizures, the target doses were gabapentin 1800 mg/day and lamotrigine 150 mg/day.

Severe adverse events were reported in 11% of patients taking gabapentin and 9.3% of patients taking lamotrigine. Two patients had serious adverse events thought to be related to the study drug; one took an overdose of gabapentin and the other had convulsions with lamotrigine. The most frequent treatment-related adverse events in both treatment groups were dizziness, weakness, and headache; 11% of patients taking gabapentin and 15% of those taking lamotrigine withdrew because of adverse events. There was an increase of over 7% in body weight from baseline in 14% of the patients taking gabapentin and 6.6% of those taking lamotrigine. There were benign rashes in 4.4% of those taking gabapentin and 11% of those taking lamotrigine.

The hypothesis that both amitriptyline and gabapentin are more effective in relieving neuropathic pain than diphenhydramine has been tested in a randomized, double-blind, triple crossover, 8-week trial in 38 adults with spinal cord injuries [18]. Maximum daily doses were 2600 mg for gabapentin and 150 mg for amitriptyline.

Amitriptyline was more efficacious in relieving neuropathic pain than diphenhydramine. Withdrawal because of possible adverse reactions occurred five times during gabapentin treatment:

(1) shortness of breath;

(2) dizziness, fatigue, and nausea;

(3) increased spasticity and pain;

(4) fatigue, drowsiness, constipation, and dry mouth; and

(5) severe itching.

The four most frequent adverse events were dry mouth, drowsiness, fatigue, and constipation, which were all more common with amitriptyline.

 

Gabapentin is Used to Treat Seizures and Postherpetic Neuralgia ?

What is gabapentin?

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 it’s used

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.

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.

Nerve pain can be a symptom of many different conditions, including cancer, HIV, diabetes, and shingles. For some, nerve pain is frustrating; for others, nerve pain is devastating and life-changing.

Whether it feels like burning, pinpricks, or sudden shocks of electricity, nerve pain can disrupt your life at home and at work. It can limit your ability to get around. Over time, it can grind you down. Studies show that people with nerve pain have higher rates of sleep problems,anxiety, and depression.Your nervous system is involved in everything your body does, from regulating your breathing to controlling your muscles and sensing heat and cold.

There are three types of nerves in the body:

    1. Autonomic nerves. These nerves control the involuntary or partially voluntary activities of your body, including heart rate, blood pressure, digestion, and temperature regulation.
    2. Motor nerves. These nerves control your movements and actions by passing information from your brain and spinal cord to your muscles.
    3. Sensory nerves. These nerves relay information from your skin and muscles back to your spinal cord and brain. The information is then processed to let you feel pain and other sensations.

Because nerves are essential to all you do, nerve pain and damage can seriously affect your quality of life.

When you have a serious medical condition such as cancer or HIV, dealing with the additional misery of nerve pain can be especially hard. But there is good news. While nerve pain can’t always be cured, it can be treated — and there are a lot of good options available.

Experts believe that 40 million Americans are living with nerve pain. The impact of nerve pain is tremendous. Both the costs to the healthcare system as well as loss of wages and productivity are staggering.

What is Postherpetic Neuralgia ?

Postherpetic neuralgia (post-hur-PET-ik noo-RAL-juh) is the most common complication of shingles. The condition affects nerve fibers and skin, causing burning pain that lasts long after the rash and blisters of shingles disappear.

The chickenpox (herpes zoster) virus causes shingles. The risk of postherpetic neuralgia increases with age, primarily affecting people older than 60. There’s no cure, but treatments can ease symptoms. For most people, postherpetic neuralgia improves over time.

How Are Nerve Pain and Nerve Damage Treated?

In many instances, nerve damage cannot be cured entirely. But there are various treatments that can reduce your symptoms. Because nerve damage is often progressive, it is important to consult with a doctor when you first notice symptoms. That way you can reduce the likelihood of permanent damage.

Often, the first goal of treatment is to address the underlying condition that’s causing your nerve pain or nerve damage. This may mean:

    • Regulating blood sugar levels for people with diabetes
    • Correcting nutritional deficiencies
    • Changing medications when drugs are causing nerve damage
    • Physical therapy or surgery to address compression or trauma to nerves
    • Medications to treat autoimmune conditions

Additionally, your doctor may prescribe medications aimed at minimizing the nerve pain you are feeling. These may include:

    • Pain relievers
    • Tricyclic antidepressants
    • Certain anti-seizure drugs – Gabapentin

Complementary and alternative approaches may also help alleviate your nerve pain and discomfort. These include:

    • Acupuncture
    • Biofeedback
    • Hypnosis
    • Meditation

Dosage for postherpetic neuralgia

Adult dosage (ages 18–64 years)

    • Typical starting dosage: Day 1, 300 mg; day 2, 600 mg (300 mg two times per day, spaced evenly throughout the day); day 3, 900 mg (300 mg, three times per day, spaced evenly throughout the day). Your doctor may further increase your dosage after day 3.
    • Maximum dosage: 1,800 mg per day (600 mg, three times per day, spaced evenly throughout the day)

Child dosage (ages 0–17 years)

Dosage for people younger than 18 years has not been established.

Senior dosage (ages 65 years and older)

Your kidney function may decrease with age. Your body may get rid of this drug more slowly. Your doctor may start you on a lower dose so that too much of this drug does not build up in your body. Too much of the drug in your body can be dangerous. Your doctor may change your dose based on how well your kidneys are working.

Gabapentin in Non-Epilepsy Neuropathic Pain like Postherpetic Neuralgia

The FDA approved gabapentin for the management of postherpetic neuralgia in adults. Recently, gabapentin underwent systemic evaluation in the management of diabetic neuropathy. In 1998, Rowbotham and his research team concluded that in 229 postherpetic neuralgia patients, gabapentin had more significant pain reduction as early as two weeks after initiating the treatment.

Furthermore, other measurements of mood, depression, anger-hostility, fatigue, and physical functioning, were more effectively managed with gabapentin compared to placebo.

During the same time, Backonja reviewed the effect of gabapentin in 165 diabetic neuropathy patients and showed the result that pain reduction in the gabapentin group is greater (as measured with an 11-point Likert scale) in comparison to the placebo group. And the results were significant from 2 weeks of initiation of therapy and stayed significant during the eight weeks of study.

Patients in the treatment group also reported improvement in their quality of life. This medication was well tolerated in 67% of patients who received a maximum daily dosage of 3600 mg.

Treatment for Postherpetic neuralgia

Postherpetic neuralgia is a nerve disease occurs after an attack of herpes zoster infection. Herpes zoster or ‘shingles’ is a viral infection which affects the skin, especially sides of the chest, caused by varicella zoster virus. This is the same virus which causes chicken pox in children.

After an episode of herpes, the virus remains dormant in the nerve tissues of the body. This virus may become active when the immunity of the individual reduces or during convalescence after a major illness, resulting in blisters on the skin, known as shingles. It is accompanied with a rash which disappears without major consequences in about two to four weeks. Around 50% of individuals with shingles go on to develop post herpetic neuralgia (PHN) or after-shingles pain.

The neuralgia begins when the herpetic eruptions begin to heal. The pain appears usually in the affected dermatone or the affected nerve course and results in severe pain in the region which has the same nerve supply. The pain is a drawing, pricking type of intense pain, sometimes accompanied with burning sensation of the skin. The pain lasts from a few weeks to few months, rarely years.

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 Causes

      • Severe rash within three days of shingles infection
      • A study shows that, 65% of patients were women
      • The chances of developing PHN, increases when the shingles occurs in persons over 50 years.
      • The incidence of herpes zoster is up to 15 times higher in HIV-infected patients than in uninfected persons, and as many as 25 percent of patients with Hodgkin’s lymphoma develop herpes zoster.
      • Blacks are one fourth as likely as whites to develop this condition.
      • Site of HZ involvement
        • Lower risk – Jaw, neck, sacral, and lumbar
        • Moderate risk – Thoracic
        • Highest risk – Trigeminal (especially ophthalmic division), brachial plexus.

Signs and symptoms:

    • A pain that continues for 3 months or more, after the healing of shingles, is defined as PHN.
    • PHN pain may be burning, aching, itching and sharp and the pain can be constant or it can come and go
    • The skin which was affected with blisters, may show scarring
    • The involved dermatome may show altered sensations, either hypersensitivity or reduced sensitivity.
    • In rare cases, where if the nerves involved also control muscle movement, the patient might also experience muscle weakness, tremor or paralysis

Postherpetic Neuralgia Treatment:

The conventional treatment is directed at pain control while waiting for the condition to resolve.  Pain therapy may include multiple interventions, such as topical medications, over-the-counter analgesics, tricyclic antidepressants,  anticonvulsants and a number of non medical modalities. Occasionally, narcotics may be required.

When it comes to treating postherpetic neuralgia, you may need to take a combination of medications to effectively manage your pain and other PHN symptoms. No single treatment plan is right for everyone—what medications you take will depend on your PHN symptoms.

While symptoms differ from person to person, for most people, PHN does improve over time. Researchers found that more than half of all patients with PHN stop experiencing pain within one year.1

Fortunately, during that period of intense pain and other symptoms, there are certain medications that you can take to significantly help control postherpetic neuralgia symptoms.

Before trying a prescription medication, your doctor will most likely want you to try an over-the counter (OTC) analgesic (painkiller) medication, such as acetaminophen or non-steroidal anti-inflammatory drugs (NSAIDs). These medications can help relieve pain and other PHN symptoms.

Tylenol is an example of acetaminophen, and Advil is an example of an NSAID you can take to help treat PHN.

Another OTC medication you may want to try for PHN is capsaicin cream. This cream—made from hot chili pepper seeds—is applied to the affected skin, and it can be helpful for reducing PHN-related pain. But this cream can be painful, so talk to your doctor about how much you should apply.

If these medications aren’t strong enough to treat your PHN symptoms, your doctor may suggest some of the prescription medications below to treat your postherpetic neuralgia.

    • Tricyclic antidepressants, such as amitriptyline (Elavil), nortriptyline (Pamelor), and desipramine (Norpramin) are effective at treating postherpetic neuralgia pain. Other classes of antidepressant are also helpful. All classes of antidepressant take a few weeks to start working.
    • Anticonvulsants, developed to control seizures, can help reduce the pain of PHN. These include gabapentin (Neurontin), carbamazepine (Tegretol) and pregabalin (Lyrica). Gabapentin enacarbil (Horizant) and gabapentin (Gralise) are approved by the FDA for the treatment of PHN in adults.
    • Anti-viral drugs valacyclovir and acyclovir are also becoming medications of choice for treating postherpetic neuralgia.
    • Lidocaine Patches for Postherpetic Neuralgia. Lidocaine patches are FDA-approved to treat PHN. The medication in the patch—lidocaine—can penetrate your skin and go to the nerves that are sending the pain signals. A benefit of lidocaine patches is that they don’t numb the skin.
    • Prescription capsaicin patches. These patches contain a very high concentration of the chili pepper extract capsaicin. The capsaicin patch Qutenza is applied in a doctor’s office for one hour every three months.

If you have severe pain and other medications don’t work for you, your doctor may want you to try an opioid.  Tramadol (eg, Ultram) is an example of a relatively weak opioid that can be used to help you manage PHN. Your doctor may have you try a weaker opioid first.  Opioids, such as morphine (MS Contin), oxycodone (OxyContin), and hydrocodone (Vidocin), are also used to treat moderate to severe pain of postherpetic neuralgia.

Homoeopathic Medicine:

Mezereum – For Postherpetic Neuralgia with Intense Burning

Mezereum is rated among the best medicines for postherpetic neuralgia. It is the best-suited prescription when postherpetic neuralgic pains are violent and attended with marked burning.  Mezereum is the most helpful among medicines for postherpetic neuralgia in postherpetic pains located in the face. The pain in the face may get worse while eating.

Warmth brings relief. Mezereum is also helpful during active herpes zoster where eruptions are present. The key symptoms to look out for before prescribing Mezereum during herpes zoster infection are violently itching vesicles with shining red areola and intense burning.

2. Ranunculus Bulbosus – For Pains coming in Paroxysms

Another of the prominently indicated medicines for postherpetic neuralgia is Ranunculus Bulbosus. It is indicated for sharp, shooting, postherpetic neuralgic pains that come in paroxysms.

It is also one of the top listed medicines for intercostal neuralgia following herpetic infection. Ranunculus Bulbosus is also indicated for herpes zoster when the vesicles eruptions are bluish in colour. The eruptions are attended with itching and burning symptoms which worsen on contact.

3. Rhus Tox – One of the best Medicines for Postherpetic Neuralgia

Rhus Tox also figures on the list of highly effective medicines for postherpetic neuralgia. It is one of the best medicines for postherpetic neuralgia where the pains are attended with marked restlessness. The skin is sensitive to cold air in such cases. In herpes zoster, Rhus Tox is the most preferred among medicines when the vesicles are yellowish with itching and stinging.

 

Gabapentin is also Used for Prevention of Fibromyalgia

Fibromyalgia is a muscular condition that affects many people. It refers to muscle fatigue and pain felt across different muscle groups in the body, not just on isolated areas.

Fibromyalgia is a disorder characterized by widespread musculoskeletal pain accompanied by fatigue, sleep, memory and mood issues.

The term fibromyalgia directly means pain that is embedded in the tissues of the muscles, specifically the fibrous tissues.  This very acute pain starts from the ligaments, the tendons, and other such connective muscle tissues that are present all over the muscular system of the body.  Researchers believe that fibromyalgia amplifies painful sensations by affecting the way your brain processes pain signals.

Fibromyalgia Symptoms sometimes begin after a physical trauma, surgery, infection or significant psychological stress. In other cases, symptoms gradually accumulate over time with no single triggering event.

Women are more likely to develop fibromyalgia than are men.  Many people who have fibromyalgia also have tension headaches, temporomandibular joint (TMJ) disorders, irritable bowel syndrome, anxiety and depression.

There are however some controversial theories regarding  Fibromyalgia that propose that this condition is a psychosomatic illness, that is, it is a disorder brought about by psychological factors and not necessarily physical factors. This reasoning is mainly brought about by the strong evidence available that relates Fibromyalgia to major depression.

An in-depth review regarding the association of major depression disorders with Fibromyalgia brought out significant similarities between the two in terms of psychological characteristics and neuroendoctrine abnormalities in the patients.

Researchers believe repeated nerve stimulation causes the brains of people with fibromyalgia to change. This change involves an abnormal increase in levels of certain chemicals in the brain that signal pain (neurotransmitters). In addition, the brain’s pain receptors seem to develop a sort of memory of the pain and become more sensitive, meaning they can overreact to pain signals.

Medications designed to treat epilepsy are often useful in reducing certain types of nerve pain. Gabapentin (Neurontin) is sometimes helpful in reducing fibromyalgia symptoms.  Gabapentin is a medicine used to treat pain caused by nerves that are not working properly.   Gabapentin changes the way that the nerves send messages to the brain. It can be taken in a tablet or a liquid, with or without food.  Doses are usually 1200 mg to 2400 mg each day. At the start of treatment low doses are used to minimise side effects, but the dose is usually increased after a few weeks.

At the reviews of gabapentin for fibromyalgia in drugs.com ,  almost 70% Fibromyalgia Patients think Gabapentin can cure their fiobromyalgia disease.  But almost 20% fiobromyalgia Patients think it doesnot work. ( Rating 1 -2 %),  another 15% patients think it do work but the effect is not that good ( Rating 3 – 5 ).

One of the patient said:

“I have had fibro for 7 years, finally have a doctor that prescribed me Gabapentin. It’s amazing I feel like a normal person again. I sleep through the night, with no pain anymore. My anxiety is gone also, which is awesome. I know everyone is different, but it works for me. I have had little to no side effects yet. First few doses was a bit of an air head other than that no complaints. Being able to function pain free and agitation free is a blessing.”

Another Fiobro patient said:

“I had the best results, in relieving the pain, with gabapentin. I was able to work through the other symptoms. The etodolac helped with the inflammation. I was doing well, until the muscle spasms started, again. I suspect the mould allergies exasperated the symptoms. So, cyclobenzeprine was added. I don’t know what happened, but I was jobless, homeless, and very sick by the time a CVS pharmacist recognized the V.A. had put me on another toxic, prescription drug cocktail. When I brought it to the V.A.s attention, as usual, it was ignored. The medications that help, are the ones the V.A. will not prescribe to veterans like myself. They say speak up, if you do, expect to be classified as mentally ill, violent, aggressive, involuntarily committed”

NatalieW555 Said:
“I was suffering from fibromyalgia pain most of my adult life, I’m 52 by the way, not realizing there was this wonderful medication available to me…I started it about 2 years ago and it really makes a HUGE difference in how my body feels. I take 300 mg 3X daily. I hope it never quits working for me…you should give it a try….It has no side effects on me.”

Member Annabqnm Said:

“Pretty much saved my life. 13 years ago fibromyalgia symptoms (severe pain especially legs and shoulders), started. My father was taking high doses of gabapentin for chronic guillaune barre. He urged me to try it–and it was the first real sleep I had in months! My rheumatologist had me on 1600mg. 3x, gradually lowered to 1600 mg. 2x. Studies at Mayo Clinic and Johns Hopkins show very few (and very mild) side effects, even at high doses. The only problem I have is if I forget to take them. Then I get flu like symptoms. I was able to continue my career (elementary school teacher) with no problems. Retired this year age 66 and very active. BTW my memory seems better than most friends my age.”

But 30% Fibro customers think Gabapentin is not effective for their Fibro disease. I looked the reviews they have wrote, I found most of them are just back pain or leg pain but not Fiobromyalgia. But some Fibro patients do think it has some side effects, especially thought problems such as depression.

One of the Fibro patient said:

“I have “fibromyalgia,” severe muscle pain from a twisted spine/congenitally deformed vertebrae. I was getting better with yoga, but hurt my back/rib muscles overdoing. I developed depression on gabapentin after a few weeks. At first it dulled the pain and made me feel lightheaded, and I had memory problems. Then my anxiety increased and the pain continued, and hit a real low. I spent two weeks in a psych ward until a brilliant psych nurse who believed in treating muscle pain. I am now recovering on a mix of robaxin, a muscle relaxer, a low dose of valium for rib spasms, and prozac and remeron (for sleep) and hope to get off all of them once I can exercise again. Similar reaction to Lyrica four years ago.”

Gabapentin is effective for Fibro. But you need consider whether you can endure the side effects of gabapentin. Please check our website for the Gabapentin Side Effects.

The off-lable use of Gabapentin for migraine

Gabapentin is as an anti-epileptic drug and as an analgesic, particularly for pain of the neuropathic or neurogenic type.  When used for controlling epilepsy, it is usually used in conjunction with another anti-epileptic drug.  But Gabapentin is widely used  to treat nerve pain or neuropathic pain than it is to treat epilepsy.

Gabapentin is also sometimes used to relieve the pain of diabetic neuropathy (numbness or tingling due to nerve damage in people who have diabetes), and to treat and prevent hot flashes (sudden strong feelings of heat and sweating) in women who are being treated for breast cancer or who have experienced menopause (”change of life”, the end of monthly menstrual periods). Talk to your doctor about the risks of using this medication for your condition.

It is also widely used to treat Anxiety and Migraine prevention.

What is gabapentin?

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 it’s 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.

One of Gabapentin “off-label” usage is for migraine prevention and treatment, including migraines with or without aura, vestibular migraines. It can reduce the frequency of headaches, pain intensity, and the use of symptomatic medications. Gabapentin is a good preventive therapy for migraines refractory to standard medications.

The chemical structure of gabapentin is related that of gamma-aminobutyric acid (GABA) which is a neurotransmitter in the brain. The exact mechanism as to how gabapentin controls epilepsy and relieves pain is unknown, but it probably acts like the neurotransmitter GABA.

The effective dose of gabapentin varies greatly. Some persons need only 200-300 mg a day whereas others may need 3000 mg or more a day. It may take several weeks to become effective, so it is important to stay on it for an adequate length of time.

The Efficacy of gabapentin in migraine prophylaxis experiment shows  gabapentin is an effective prophylactic agent for patients with migraine.

In the Clinical trials143 patients evaluated gabapentin for migraine prophylaxis.  After 3 months the patients taking gabapentin had a reduction of the migraine frequency by 1.5 migraines per month (or by 35.7%) compared with a reduction of 0.6 migraines per month for the placebo group. Also, gabapentin reduced the headache frequency by 50% or greater in 45% patients compared with only 16% patients on placebo. The most frequently reported adverse events  were asthenia, dizziness, somnolence, and infection.

In Famous medical websites, migraine patients also review the gabapentin as the migraine prevention medicine. They rate Gabapentin 8.1 stars out of ten stars. It is a high mark and means Gabapentin is a very effective medicine for migraine prevention.

I haven’t been taking this medication for long but it’s helped so much. Neuro started me off on 300mg at night and now I’m at 600mg at night. It doesn’t make me sleepy or drowsy. Before starting gabapentin, I was having migraines just about every day. I started having aphasia and vision changes with my migraines, so I decided to take action. I’ve only been on it for almost 2 weeks but I’ve been migraine free and my triggers are no longer triggers at this point, which is fantastic. I should note it has reduced my appetite but this is not a negative thing.” –  Crystaldreams July 25, 2017

This medication is..interesting. I am 20 with what a few doctors think is Fibro and a chronic pain condition but was Rx’d this med by a psych doctor for tension migraines. While it does NOT really help with migraines, it has been making me awfully sleepy and drowsy, and helping with weird aches and pains throughout my body. It can be used as a mood stabilizer and I can see why- because it makes you so drowsy you can’t do or say anything, especially after taking the evening dose! I’ve been afraid to drive any car since starting this. It makes me more drowsy than my anxiety meds which don’t make me drowsy at all! Doctor is raising the dose because since writing that first part- I have become quite used to the med, where my dose does NOT work  – Chelseabergstresser (taken for 1 to 6 months) May 11, 2017

“I have chronic Migraine called Glutamate Storm. First dose of 100mgs made me sleep 36 hours. Before I got the prescription I never slept more than 5 hours per night and often only got 2 hours of sleep per night. But I did not want to take a prescription every day, so I only took it when my ears were ringing really loud and I was sleep deprived. But then I noticed that my chronic cough was always gone the day after taking Gabapentin. So I started taking it every day for that. When I did, my headache and ear ringing got a lot better. I am now taking 400 mgs per day. I had bad breath at first, but it’s gone. Dr. says it might have detoxed something. I am all for that. Better out than in. This drug has helped me a lot. And I am not pro-pharma.” – Gylm April 26, 2017

Adverse Reactions in Pooled Placebo-Controlled Trials in Postherpetic Neuralgia

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Postherpetic Neuralgia

The most common adverse reactions associated with the use of NEURONTIN in adults, not seen at an equivalent frequency among placebo-treated patients, were dizziness, somnolence, and peripheral edema.

In the 2 controlled trials in postherpetic neuralgia, 16% of the 336 patients who received NEURONTIN and 9% of the 227 patients who received placebo discontinued treatment because of an adverse reaction. The adverse reactions that most frequently led to withdrawal in NEURONTIN-treated patients were dizziness, somnolence, and nausea.

Following table lists adverse reactions that occurred in at least 1% of NEURONTIN-treated patients with postherpetic neuralgia participating in placebo-controlled trials and that were numerically more frequent in the NEURONTIN group than in the placebo group.

TABLE 3. Adverse Reactions in Pooled Placebo-Controlled Trials in Postherpetic Neuralgia
NEURONTIN
N=336
%
Placebo
N=227
%
Reported as blurred vision
Body as a Whole
  Asthenia 6 5
  Infection 5 4
  Accidental injury 3 1
Digestive System
  Diarrhea 6 3
  Dry mouth 5 1
  Constipation 4 2
  Nausea 4 3
  Vomiting 3 2
Metabolic and Nutritional Disorders
  Peripheral edema 8 2
  Weight gain 2 0
  Hyperglycemia 1 0
Nervous System
  Dizziness 28 8
  Somnolence 21 5
  Ataxia 3 0
  Abnormal thinking 3 0
  Abnormal gait 2 0
  Incoordination 2 0
Respiratory System
  Pharyngitis 1 0
Special Senses
  Amblyopia 3 1
  Conjunctivitis 1 0
  Diplopia 1 0
  Otitis media 1 0

Other reactions in more than 1% of patients but equally or more frequent in the placebo group included pain, tremor, neuralgia, back pain, dyspepsia, dyspnea, and flu syndrome.

There were no clinically important differences between men and women in the types and incidence of adverse reactions. Because there were few patients whose race was reported as other than white, there are insufficient data to support a statement regarding the distribution of adverse reactions by race.

 

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 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 Is an Effective Treatment for Alcohol Withdrawal Symptoms?

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 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.

    • A new study reports the nerve pain reliever gabapentin may be helpful in treating people with serious alcohol withdrawal symptoms.
    • Some experts say gabapentin is most effective if used in combination with a benzodiazepine medication.
    • Gabapentin can have serious side effects, including drowsiness and abnormal eye movements.

Gabapentin in Alcohol Withdrawal

For the first time, the DSM-V includes the diagnostic guidelines for alcohol dependency. There are a variety of severe diseases that result from or are influenced by alcohol dependence include stomach ulcers, liver issues, increased risk of heart disease, and neuropathy. Researchers assess that 3.8% of worldwide deaths result from direct or indirect effects of alcohol abuse.

While gabapentin’s mechanism of action is generally understood, it appears to be a logical pharmacologic option for treating issues involving the GABA receptor system. Gabapentin is a safe, readily available, and effective drug for alcohol-use disorder treatment, specifically for the abstinence maintenance phase. A 2014 trial bolstered the evidence base for gabapentin use in the treatment of alcohol use disorder. Results for insomnia and cravings, two symptoms of alcohol use disorder abstinence maintenance, demonstrated significant improvement with gabapentin pharmacotherapy. Gabapentin has also shown a statistical benefit when used as adjunctive therapy to naltrexone (the FDA-approved alcohol use disorder medication). It is also clear that higher doses of gabapentin, 1800 mg per day, seem to have a stronger effect on alcohol-use disorder abstinence maintenance. However, the trials investigating gabapentin as monotherapy have shown mixed results.

For gabapentin, unlike disulfiram and naltrexone, there is no need for hepatic dose adjustments. Gabapentin can also be used in patients whose renal function is below 20 mg/dl (although a dosing adjustment is needed).

In 2007, Melcolm and his team compared gabapentin to lorazepam. They concluded that there were significant reductions in self-reported sleep disturbance and daytime sleepiness in patients undergoing outpatient treatment for alcohol withdrawal.

A double-blind study investigated the use of 1200 mg/ per day gabapentin in alcohol use disorder. Specifically, the researchers found gabapentin to be superior to the benzodiazepine lorazepam in treating outpatients with moderate alcohol withdrawal. This outcome was measured by a lower chance of drinking and a superior, but clinically, similar alcohol withdrawal symptom reduction.

Can a drug used primarily to treat nerve pain and partial seizures be effective in helping ease alcohol withdrawal symptoms?

The anticonvulsant drug gabapentin is used off-label to treat alcohol-related withdrawal, cravings, anxiety, and insomnia. Although it is well tolerated and has demonstrated efficacy for mild alcohol withdrawal and early abstinence, there is concern about its potential for abuse. Gabapentin should be prescribed only as a second-line alternative to standard therapies, and only after screening for opioid or other prescription drug abuse to determine if heightened monitoring is warranted. Clinicians should be aware of gabapentin’s limitations for treating alcohol use disorder and be attentive to emerging data on risks and benefits.

A Trusted Source published this week concluded that gabapentin can relieve alcohol withdrawal symptoms but is most effective for people with a history of more severe symptoms after a few days of abstinence.

Gabapentin is known under brand names such as Neurontin, Gralise, and Horizant.

It was first developed Trusted Source in Japan during the 1970s and approved for use in the United States in 1993.

The drug was originally used as a muscle relaxer and antispasmodic medication. It’s been used off-label for other conditions.

“It has been used for detoxification — alcohol withdrawal — for many years,” said Dr. Raymond F. Anton, the study’s main author and a professor of medicine at the Medical University of South Carolina in Charleston.

“For relapse prevention, other clinical trials have had mixed results. We had published several studies suggesting it would be added to other medications with some success, but it looked like only in those with alcohol withdrawal symptoms prior to treatment,” he said.

“This study proved that gabapentin could work by itself as a relapse prevention medication, but only in this with the higher alcohol withdrawal symptoms, as predicted,” Anton told Healthline.

What the study revealed

Anton’s team looked at 90 people meeting the criteria of serious alcohol use.

Over 16 weeks, 12 of the 44 participants given gabapentin had no heavy drinking days (27 percent) compared with four (9 percent) of those participants given a placebo.

The study found mild to moderate side effects, including dizziness and some fatigue.

“Very few people had significant enough side effects to stop treatment,” Anton said. “It also improved sleep.”

Dr. Meredith Sagan, an addiction psychiatrist at Alo House Recovery Centers in Southern California, says gabapentin is most effective with benzodiazepine medications commonly used for withdrawal.

“Gabapentin cannot necessarily be used safely on its own to support such a detox,” Sagan told Healthline. “It’s always important to consult a medical professional when considering detoxifying from alcohol, as it can be very dangerous due to possible seizure and others risks.”

Individualized treatments

Sagan says the combination of medications and the timeline to take them is specific to each individual.

“Some people may need more or less medication, as well as different types and combinations, depending on their degree of alcohol consumption, in addition to other factors,” she said.

“So, although gabapentin can be a useful adjunct to the benzodiazepine category of medication for alcohol detox, it is not time to say goodbye to ‘benzos’ just yet,” Sagan said.

Benzodiazepines are also used to treat anxiety and seizures as well as to relax muscles. These medications come in many manufactured forms, including Xanax, Klonopin, Librium, Valium, and Ativan.

Participants in the South Carolina study weren’t allowed to take benzodiazepines or opioids.

“For people using gabapentin just for anxiety and not for alcohol withdrawal, gabapentin can be a good non-benzodiazepine alternative,” Sagan said.

“Gabapentin at higher doses can cause an uncomfortable withdrawal when one quits taking it. However, for some people with an addiction history, gabapentin is a safe alternative to benzodiazepines, which over the long term can be physically and psychologically addictive,” she said.

Gabapentin side effects

Common side effects of gabapentin include abnormal eye movements, clumsiness or unsteadiness, constipation, diarrhea, difficulty speaking, drowsiness, dry mouth, nausea, and vomiting.

More serious side effects — which may be more common in people with psychiatric disorders — include anger and violent behavior, increased anxiousness, depression, anxiety or irritability, mania, panic attacks, suicidal thoughts or behavior, and insomnia.

“I was prescribed gabapentin when I was struggling with my severely herniated disc,” Janine McKavish Thalblum, a resident of Dublin, California, told Healthline.

“The side effects were longer than an encyclopedia. With all the pain I was in I was borderline suicidal, so I opted not to take them, as that was one of the side effects. When the pharmacist was reading (them) before handing it over, I literally started to cry,” she explained.

Thalblum did take gabapentin for 2 days before opting out. She says she couldn’t tell if the medication contributed to her “overwhelming sense of wanting to give up.”

Andrea Johnson, a resident of Oakland, California, and her late wife, Julie, both took gabapentin for pain. They had vastly different experiences.

“She had chronic pain from her legs having been shattered in a car crash. Her doctors prescribed gabapentin about 10 years ago under its brand name of Neurontin,” Johnson told Healthline.

“She stopped it after a week because it put her into a constant dream state. She was sort of awake and could do things but without being conscious of what she was doing. When I caught her rolling a cigarette without realizing that she was doing it, I put a stop to the gabapentin and told her doctor why,” Johnson said.

Johnson’s doctor prescribed her gabapentin last year for arthritis in her hips.

“I was concerned about it because of Julie’s experience, but I didn’t get the psych effects that she did,” Johnson said. “By the end of a month, it still wasn’t having an effect on my pain either, so I stopped it.”

Gabapentin and opioids

In recent years, gabapentin has been involved in opioid overdose deaths and been dubbed “an emerging threat” in a national bulletin to law enforcement.

It’s listed as a controlled substance in some states, although officials say it’s usually not the main cause of death and not as dangerous as opioids.

Pfizer, which developed gabapentin, paid $430 million in 2004 under an agreement with government prosecutors over fraudulent claims the company was accused of making about the drug’s uses.

Anton says researchers are still looking at whether gabapentin can be used as an anti-craving drug like naltrexone.

“Right now, it is estimated that only 20 percent of individuals who might benefit from reducing or stopping drinking actually receive treatment,” Anton said.

“And, of those 20 percent, only 20 percent receive any medication-assisted treatment. The standard of care in the U.S. has historically been an AA (Alcohol Anonymous) or 12-step counseling model. While that model has helped many people, many others do not want to partake in it, or haven’t found it useful.

“Medications that can be prescribed by specialized and/or primary care providers can encourage many more people to consider treatment for their alcohol use disorder,” he added.

Gabapentin is a prescription anticonvulsant used to treat epileptic seizures, postherpetic neuralgia, and restless legs syndrome. Postherpetic neuralgia is pain caused by shingles, which can last many months after having the illness.

While the exact mechanism of action of gabapentin is not fully understood, it may work by decreasing excitatory brain signaling. This can prevent seizures and change the way the brain responds to pain signals. This medication can be found as a capsule, tablet, or oral solution.

Alcohol Addiction
Alcohol Addiction

The following 11 questions are designed to help you better understand your relationship to alcohol. They will help you to tell if it resembles abuse or addiction, or is if it closer to average.

1. Do you tend to drink more than you expected to? And for longer periods of time?

2. Do you wish you could drink less, and struggle to cut down your alcohol intake?

3. Does drinking consume much of your time? In other words, do you spend a lot of your time trying to obtain, use, or recover from alcohol hangovers?

4. Do you have very strong cravings or urges to drink? Does it feel like you “need” it to get by?

5. Does drinking cause problems for you at work, in school, or in your family obligations? Does this happen frequently?

6. If drinking does cause these social and interpersonal problems for you, do you continue to drink anyway?

7. Have you given up activities that used to be meaningful for you? For example, have you quit a sport or left friendships because you don’t seem to have the time or energy anymore?

8. Do you use alcohol even when it makes your activity physically dangerous? This could be drinking while driving, using certain prescription drugs, or working with heavy machinery.

9. Do you continue to drink even after discovering that it exacerbates, worsens, or even causes other physical or mental illnesses?

10. Are you developing a tolerance for alcohol? This could show up as a decreased effect after drinking the same quantity of alcohol that you used to use, or having to drink more and more alcohol to achieve the desired level of intoxication.

11. Have you experienced withdrawal symptoms after not drinking any alcohol for a while? These include a racing heart, trouble sleeping, shakiness, sweating, fever, restlessness, nausea, or even auditory or visual hallucinations? Does more alcohol relieve these feelings?

As an Addiction Treatment Medication

The medical research community has made great strides in synthesizing thousands of drugs over the years to treat physical ailments, mental illness, and other health conditions.

Addiction is just one of the many conditions that can be treated with specific medications. And while there are presently only a handful of FDA-approved medications used to manage substance dependence, gabapentin has been considered for off-label use for as an addiction treatment drug.

Different companies, including Parke-Davis, Greenstone, and Teva, manufacture several varieties of the generic drug. Other drugs that have been used to treat the symptoms of addiction withdrawal, for specific substances, include:

    • Clondine
    • Other anticonvulsants, such as Tegretol and Depakote
    • Methadone and buprenorphine
    • Naltrexone

Typical Application

Doses range from 100 mg to 800 mg. The frequency of administration may be based on various factors such as withdrawal symptom severity and withdrawal progress. The drug’s half-life is around 5-7 hours.

Gabapentin has been evaluated for use during medical detox and throughout subsequent treatment modalities to support relapse prevention while clients adjust to their new sober lifestyles.

Treating Substance Abuse

According to Medscape, gabapentin can inflict users with suicidal thoughts and abrupt changes in behavior. For this reason, it should only be used under medical supervision. It can also cause elevated blood pressure, fever, sleep problems, appetite changes, and chest pain.

While it has been used to treat addictions to other substances, gabapentin is most often used to treat alcoholism — an addiction some 16.6 million adults suffered from in 2013, per the National Institute on Alcohol Abuse and Alcoholism.

During withdrawal from alcohol abuse or dependency, clients may experience anxiety, tremors, agitation, and irritability. In order to understand how gabapentin works, there must be a basic understanding of how the brain works first. A balance of excitatory and inhibitory nervous system activity is, in part, mediated by neurotransmitters known as GABA and glutamate. Gabapentin may work by potentiating the inhibitory signaling of GABA and reducing the neural excitation associated with glutamate activity. As a result, signals for pain, agitation, and anxiety are reduced, too.

An American Journal of Psychiatry study showed impressive results during the 16-week treatment of 150 people who were dependent on alcohol, noting better results among those who were treated with both gabapentin and naltrexone than the latter alone. The Journal of Clinical Psychiatry reported on another study in which individuals treated for alcoholism with gabapentin showed a significant reduction in how much they drank and a greater rate of abstinence than those in the placebo group.

Gabapentin may have a similar calming effect on individuals who are detoxing from marijuana and benzodiazepines. Despite claims from fans of the plant-based drug, marijuana is indeed addictive. In 2012, 305,560 people checked into rehab citing cannabis as their primary drug of abuse, per the Substance Abuse and Mental Health Services Administration. One Neuropsychopharmacology study that analyzed the use of gabapentin in the treatment of marijuana addiction and withdrawal noted individuals in the gabapentin treatment group used less marijuana, had fewer withdrawal symptoms, and experienced improvements in cognitive functioning, compared to the placebo group.

While not quite as prevalent as a substance of abuse, benzodiazepines still accounted for 17,019 admissions to treatment in 2012, per SAMHSA. Individuals who have been abusing marijuana or benzodiazepines for a long period of time may have difficulty achieving a state of relaxation without those drugs, and gabapentin can help individuals remain calm while they’re recovering from addiction.

Gabapentin for Fibromyalgia

What Is Gabapentin?

Gabapentin is somewhat commonly prescribed as a fibromyalgia treatment, however, it is not approved by the U.S. Food and Drug Administration (FDA) for this condition.

It’s often prescribed off-label. However, the drug is chemically related to Lyrica (pregabalin), which is approved for fibromyalgia. In fact, Lyrica is sometimes referred to as the “son of Neurontin.”

Gabapentin is classified as an anti-seizure drug. It’s used to treat epilepsy, neuropathy (pain from damaged nerves), restless legs syndrome, and hot flashes. Fibromyalgia pain is similar to neuropathy, but whether this condition involves nerve damage still isn’t clear.

gabapentin mechanism of actions
gabapentin mechanism of actions

How Gabapentin Works

Gabapentin is believed to work by altering the release of glutamate and other neurotransmitters in your brain.1 Neurotransmitters send messages from one brain cell to another. Glutamate is helpful for certain things, like learning new information. That’s because it gets your brain cells stirred up and active.

Though, if you have too much glutamate, your brain cells can become overstimulated. That can make all kinds of things go wrong.

Glutamate also helps transmit pain signals in your brain and nerves. Too much glutamate may play a role in hyperalgesia, which essentially turns up the volume of pain.

To counter the effects of glutamate, you have another neurotransmitter called gamma-aminobutyric acid (GABA).2 It calms your cells and quiets your brain. When GABA and glutamate exist in balance with each other, things go well. (It’s likely out of balance in fibromyalgia, though.)

Some diseases and conditions—including fibromyalgia—may interrupt this balance and let glutamate run amok. Gabapentin is believed to reduce your brain’s release of glutamate so the cells can calm down and your brain can function better.

Gabapentin for Fibromyalgia

Research suggests that people with fibromyalgia have too much glutamate in certain parts of their brain, so gabapentin has long been prescribed for it. But is it effective? Research is mixed.

Gabapentin for Fibromyalgia
Gabapentin for Fibromyalgia

Two reviews of the evidence disagree. One released in 2016 found that gabapentin is an effective fibromyalgia treatment,3 while another, published in 2017,4 reported only low-quality evidence.

A 2014 review of gabapentin for fibromyalgia and neuropathy found that about 35% of study participants saw their pain drop by at least 50% while on the drug.5 It’s important to note, though, that 21% saw similar drops when taking a placebo.

In studies comparing gabapentin with Lyrica (pregabalin) , including one published in The Journal of the American Medical Association, pregabalin appeared to perform better.

An extended-release form of gabapentin showed promise in one small trial published in Pain Practice.3 Researchers say it improved pain, sleep, and quality of life. This was a preliminary trial, though, so more work needs to be done before we’ll know for sure whether it’s safe and effective long term.

New research supported by the National Institutes of Health’s National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS) shows that the anticonvulsant medication gabapentin, which is used for certain types of seizures, can be an effective treatment for the pain and other symptoms associated with the common, often hard-to-treat chronic pain disorder, fibromyalgia.

In the NIAMS-sponsored, randomized, double-blind clinical trial of 150 women (90 percent) and men with the condition, Lesley M. Arnold, M.D., director of the Women’s Health Research Program at the University of Cincinnati College of Medicine, and her colleagues found that those taking gabapentin at dosages of 1,200 to 2,400 mg daily for 12 weeks displayed significantly less pain than those taking placebo. Patients taking gabapentin also reported significantly better sleep and less fatigue. For the majority of participants, the drug was well tolerated. The most common side effects included dizziness and sedation, which were mild to moderate in severity in most cases.

NIAMS Director Stephen I. Katz. M.D., Ph.D., remarked that “While gabapentin does not have Food and Drug Administration approval for fibromyalgia1, I believe this study offers additional insight to physicians considering the drug for their fibromyalgia patients. Fibromyalgia is a debilitating condition for which current treatments are only modestly effective, so a study such as this is potentially good news for people with this common, painful condition.”

Fibromyalgia is a chronic disorder characterized by chronic, widespread muscle pain and tenderness, and is frequently accompanied by fatigue, insomnia, depression, and anxiety. It affects three million to six million Americans, mostly women, and can be disabling.

The precise cause of fibromyalgia in not known, but research suggests it is related to a problem with the central nervous system’s processing of pain. As with some other chronic pain conditions, people with fibromyalgia often develop a heightened response to stimuli, experiencing pain that would not cause problems in other people. Yet, unlike many other pain syndromes, there is no physical evidence of inflammation or central nervous system damage.

Although Gabapentin has little, if any, effect on acute pain, it has shown a robust effect on pain caused by a heightened response to stimuli related to inflammation or nerve injury in animal models of chronic pain syndromes. Researchers have suspected that it might have the same effect in people with Fibromyalgia. The new research, published in the April 2007 edition of Arthritis & Rheumatism, indicates the suspicions were correct.

Although the researchers cannot say with certainty how Gabapentin helps reduce pain, Dr. Arnold says one possible explanation involves the binding of gabapentin to a specific subunit of voltage-gated calcium channels on neurons. “This binding reduces calcium flow into the nerve cell, which reduces the release of some signaling molecules involved in pain processing,” she says.

How gabapentin improves sleep and other symptoms is less clear, and there are probably different mechanisms involved in fibromyalgia symptoms. “Gabapentin improved sleep, which is an added benefit to patients with fibromyalgia who often report unrefreshing or disrupted sleep,” Dr. Arnold says.

What is important is that people with fibromyalgia now have a potential new treatment option for a condition with few effective treatments. “Studies like this give clinicians evidence-based information to guide their treatment of patients,” says Dr. Arnold.

The mission of the National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS), a part of the Department of Health and Human Services’ National Institutes of Health, is to support research into the causes, treatment and prevention of arthritis and musculoskeletal and skin diseases; the training of basic and clinical scientists to carry out this research; and the dissemination of information on research progress in these diseases. For more information about NIAMS, call the information clearinghouse at (301) 495-4484 or (877) 22-NIAMS (free call) or visit the NIAMS website at http://www.niams.nih.gov.

Gabapentin Side Effects

Like all drugs, gabapentin comes with a risk of side effects.5 Some are potentially dangerous, while others are not. If you have any of the following side effects while taking gabapentin, call your healthcare provider immediately:

      • Severe weakness or tiredness
      • Upper stomach pain
      • Chest pain
      • New or worsening cough along with fever
      • Difficulty breathing
      • Severe tingling or numbness
      • Rapid, back-and-forth eye movements
      • Pain or difficulty with urination, or no urination
      • Fever
      • Sore throat
      • Swelling in the face or tongue
      • Burning eyes
      • Rash

Side effects that aren’t cause for immediate concern include:

    • Fatigue
    • Dizziness
    • Headache
    • Falling asleep
    • Weight gain

Children taking gabapentin may experience a different set of side effects. Contact your healthcare provider immediately for the following:

    • Changes in behavior
    • Memory problems
    • Inability to concentrate
    • Restlessness, hostility, or aggression

Gabapentin may interact negatively with other drugs. Be sure your healthcare provider and pharmacist know everything you’re taking.

Is Gabapentin Right for You?

With evidence being weak and mixed, gabapentin has one clear advantage over Lyrica—it’s generic, and therefore much less expensive. Price, however, is far less important than efficacy.

We all react differently to medications. Some people who fail on other drugs, including Lyrica, may find relief from gabapentin. Talk to your healthcare provider about the benefits and drawbacks gabapentin may have for your overall treatment regimen.

Which is better for fibromyalgia gabapentin or amitriptyline?

It depends on your symptoms. Research shows that amitriptyline and pregabalin (a drug similar to gabapentin) are equally effective at relieving pain, fatigue, insomnia, and brain fog. Amitriptyline is better at relieving muscular pain while pregabalin is better at easing neuropathic pain.6 Gabapentin also treats neuropathy.