Category Archives: Gabapentin

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

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

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.

Buy Authentic US Gabapentin Online COD

the cheapest Gabapentin Online

Gabapentin 800 mg – 180 Tabs $189 free $189 Order
Gabapentin 800 mg – 120 Tabs $179 free $169 Order
Gabapentin 800 mg – 90 Tabs $139 free $139 Order
Gabapentin 600 mg – 180 Tabs $179 free $179 Order
Gabapentin 600 mg – 120 Tabs $169 free $169 Order
Gabapentin 600 mg – 90 Tabs $135 free $135 Order
Gabapentin 400 mg – 180 Tabs $169 free $159 Order
Gabapentin 400 mg – 120 Tabs $138 free $138 Order
Gabapentin 400 mg – 90 Tabs $125 free $125 Order
Gabapentin 300 mg – 180 Tabs $159 free $149 Order
Gabapentin 300 mg – 120 Tabs $138 free $138 Order
Gabapentin 300 mg – 90 Tabs $120 free $120 Order
Gabapentin 100 mg – 180 Tabs $149 free $139 Order
Gabapentin 100 mg – 120 Tabs $128 free $128 Order
Gabapentin 100 mg – 90 Tabs $115 free $115 Order
Generic Fioricet 325/50/40mg – 180 Tabs $239 free $239 Order
Generic Fioricet 325/50/40mg – 120 Tabs $199 free $199 Order
Generic Fioricet 325/50/40mg – 90 Tabs $169 free $169 Order

Welcome to our US licensed online pharmacy – buygabapentin800.com – bringing quality, affordable healthcare from our store to your door.

We are specializing on Pain Medication and we can provide the cheapest fioricet, the cheapest gabapentin online. Once we receive your order, our US licensed pharmacies will fill a prescription for a medication that is FDA approved. If your order was approved, the pharmacy will ship your orders in the same day it is approved or next day.  We only accept form Orders.  We guarantee the cheapest Gabapentin, fioricet, and generic fioricet,  butalbital apap caffeine online.

Order your prescription drugs from buy gabapentin 800mg and benefit from:

    1.  Discreet, no cost medical consultations with US licensed doctors and pharmacists
    1. 100% FDA approved generic and branded prescription drugs sourced in the U.S.
    1.  Free USPS Priority Mail shipping
    1. The security and accountability of a U.S. owned and operated business
    1. All Pharmacies associated are licensed to distribute in the states, you can be 100% sure to receive the same quality medication that you get from your local drug stores.
    1.  Convenient 7 X 24 Access to Online Prescription Order System
    1. Save your Money and time
    1. Privacy Safeguarded Under Physician-Patient Privilege Law
    1. Save your insurance
  1. We accept both COD payment and Credit Card Payment. Credit Card Pharms are only for returned customers. You will get our credit card pharm URL after you have successfully accepted your first COD order.

buygabapentin800.com does not dispense nor prescribe medication directly. It is still a US licensed pharmacy who has the final authorization to approve or deny prescription requests.

Gabapentin (Generic Neurontin ) was developed to treat epilepsy, but it is now used to treat various forms of chronic pain. It works by reducing the number of signals sent through the nerves. If the signals are reduced then the pain will be reduced. Research has shown that Gabapentin can help in treating various types of nerve pain.

Some Research Team performed searches to look for clinical trials where gabapentin was used to treat neuropathic pain or fibromyalgia. They found that 5633 participants had been involved in 37 studies of reasonable quality.  They tested gabapentin against placebo for four weeks or more.  Studies lasting only one or two weeks are unhelpful when pain can last for years.

Neuropathic pain is pain coming from damaged nerves. It differs from pain messages carried along healthy nerves from damaged tissue (a fall, cut, or arthritic knee). Neuropathic pain is treated by different medicines than pain from damagedtissue. Medicines like paracetamol or ibuprofen are not effective in neuropathic pain, while medicines that are sometimes used to treat depression or epilepsy can be very effective in some people with neuropathic pain.  Our understanding of fibromyalgia (a condition of persistent, widespread pain and tenderness, sleep problems, and fatigue) is poor, but fibromyalgia can respond to the same medicines as neuropathic pain.

Gabapentin is helpful for some people with chronic neuropathic pain or fibromyalgia. Gabapentin comes as a capsule, tablet, or solution. You take it by mouth. Gabapentin is available as the brand-name drugs Neurontin, Gralise, and Horizant.  It’s also available as a generic drug.

Order Neurontin Online with Free Prescription

A lot of patients buy Gabapentin (Neurontin) online to prevent migraine and treat nerve pain. When you want to order Neurontin (The Brand Name of Gabapentin ), you can go to our website buygabapentin800mg.com, please complete the health condition form very carefully. We have hired several US licensed doctors to review your health conditions and check whether you are OK to take Neurontin. If all your health conditions are OK to take gabapentin, they will write a free prescription for you to buy Neurontin. Once the doctors approve you to take neurontin, we will send you order to US licensed pharmacies immediately.The US licensed pharmacists will review your order and send you neurontin to your home by COD payment. All the prescription fee is paid by us and it is free for you. If your order is not approved by the doctors, we still need pay them the doctor review fee. so we would like the patients have the history of taking Neurontin.

Please remember that we cannot send you Neurontin if the doctor doesnot approve your prescription. Normally it take longer time for doctors to approve your prescription because they only work in week days and work five hours per day.  We do suggest you refill your Neurontin in our website but not the first time to buy neurontin online in our website. We like to refill gabapentin ( Generic Neurontin ) for you.

DIN (Drug Identification Number)
02084260     Neurontin 100 mg capsule
02084279     Neurontin 300 mg capsule
02084287     Neurontin 400 mg capsule
02239717     Neurontin 600 mg tablet
02239718     Neurontin 800 mg tablet
How long will I have to take Gabapentin for?

This is different for different people. In general, Gabapentin will have to be taken for as long as you are requiring pain relief for nerve pain. Do not stop taking your Gabapentin suddenly if you have been taking it for a while. Your body will be used to the Gabapentin and stopping it suddenly may cause withdrawal symptoms. Reducing the dose slowly as advised by your pain specialist or GP will help stop withdrawal symptoms happening. You may wish to reduce the dose every so often, to check nerve pain is still a problem.

How to take Gabapentin ?

The dose of gabapentin required varies from person to person. To avoid side effects we build up to the dose gradually. The tables in this leaflet show you how this can be done. Some patients can put their dose up faster than others. We call this faster way the FAST TRACK (see table 1).

If you find you are getting side effects with the fast track way of putting your dose up, you can switch to the SLOWER METHOD. ( see table 2).

Other people will need to put their dose up less quickly over a number of weeks. This is THE SLOWER METHOD (see table 2).

As with any medication it is important to check how well it works.  With gabapentin this can be in a few days but for most patients may take 4-8 weeks to assess the full benefit. If you feel you are getting no benefit from this medication please discuss this with your GP or pain specialist.

By Drugs.com, Gabapentin Can be used for a lot of Nerve Pain related health conditions.
including Cough, Hot Flashes, Alcohol Withdrawal, Anxiety 161 reviews, Bipolar Disorder, Trigeminal Neuralgia, Postherpetic Neuralgia, Migraine, Insomnia, Occipital Neuralgia, Peripheral Neuropathy,Vulvodynia, Benign Essential Tremor, Epilepsy, Fibromyalgia, Pain Relief, Diabetic Peripheral Neuropathy , Neuropathic Pain,Reflex Sympathetic Dystrophy Syndrome,Periodic Limb Movement Disorder, Spondylolisthesis, Burning Mouth Syndrome,Pudendal Neuralgia, Small Fiber Neuropathy.

A lot of Patients use Gabapentin (Neurontin) to treat Hot Flashes, Anxiety, Bipolar Disorder, Migraine, Insomnia, Restless Legs Syndrome, Peripheral Neuropathy, Fibromyalgia, Neuropathic Pain. Fe patients use gabapentin to treat Pruritus, Cough, Occipital Neuralgia, Benign Essential Tremor, ement Disorder, Spondylolisthesis, Burning Mouth Syndrome, Pudendal Neuralgia, Small Fiber Neuropathy.

There are totally 1359 reviews on Gabapentin, only eleven reviews are on Epilepsy whereas 1348 reviews are on Gabapentin Off-label usage. The most widely usage of Gabapentin is for Anxiety ( 243 Reviews ), Pain Relief ( 241 Reviews ), Fibromyalgia ( 137 Reviews ), Peripheral Neuropathy (119 reviews ), Bipolar Disorder ( 83 reviews ), Migraine ( 79 reviews), Neuropathic Pain ( 75 reviews ), Hot Flashes (70 reviews ), Restless Legs Syndrome (61 Reviews ) and Insomnia ( 59 reviews). The most effective usage of Gabapentin is for Pruritus and Cough.

Gabapentin is one drug that researchers have studied for preventing migraines. It has a high safety profile and few side effects. This makes it a good option for Migraine prevention.  Results from some clinical trials have shown a modest benefit from the use of gabapentin for migraine prevention.  However, the American Academy of Neurology (AAN), the organization that provides guidance for the use of drugs to prevent migraines, has stated that there is not enough evidence at this time to support the use of gabapentin for migraine prevention. Healthcare professionals can choose to prescribe gabapentin when other prevention therapies have not worked, however.

Gabapentin has been proven to be effective for people who have hard-to-treat depression or other mood disorders. Neurontin is not your traditional anxiety drug. It’s a drug primarily described to those with bipolar disorder, not anxiety. Bipolar disorder is a complicated mental health problem.  Gabapentin was successful in helping with rapid cycling and mixed bipolar states in people who have not received relief from valproate or carbamazepine. It appeared that Gabapentin helped more with anxiety and agitation than the other two drugs. It has also been shown that Gabapentin could aid people with certain types of tardive dyskinesia. That’s why anyone that has been prescribed Neurontin should strongly consider taking it, despite the side effects above and questions about its effectiveness. Bipolar disorder is not something that should be left to chance.

The total number of patients treated with NEURONTIN in controlled clinical trials in patients with postherpetic neuralgia was 336, of which 102 (30%) were 65 to 74 years of age, and 168 (50%) were 75 years of age and older. There was a larger treatment effect in patients 75 years of age and older compared with younger patients who received the same dosage. Since gabapentin is almost exclusively eliminated by renal excretion, the larger treatment effect observed in patients ≥ 75 years may be a consequence of increased gabapentin exposure for a given dose that results from an age-related decrease in renal function. However, other factors cannot be excluded. The types and incidence of adverse reactions were similar across age groups except for peripheral edema and ataxia, which tended to increase in incidence with age.

Clinical studies of NEURONTIN in epilepsy did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and dose should be adjusted based on creatinine clearance values in these patients.

What form(s) does this medication come in?

Capsules

100 mg – Each hard gelatin Coni-Snap capsule, with white opaque body and cap printed with “PD” on one side and “Neurontin/100 mg” on the other, contains gabapentin 100 mg.

300 mg – Each hard gelatin Coni-Snap capsule, with yellow opaque body and cap printed with “PD” on one side and “Neurontin/300 mg” on the other, contains gabapentin 300 mg.

400 mg – Each hard gelatin Coni-Snap capsule, with orange opaque body and cap printed with “PD” on one side and “Neurontin/400 mg” on the other, contains gabapentin 400 mg.

Tablets

600 mg – Each white, elliptical, film-coated tablet with “Neurontin 600” printed on one side contains gabapentin 600 mg.

800 mg –  Each white, elliptical, film-coated tablet with “Neurontin 800” printed on one side contains gabapentin 800 mg.

We do not sell Gabapentin to all patients!

Normally Gabapentin is suitable for all adult and children bigger than six years old. But you are not allowed to order Gabapentin online especially in our online pharmacies if you have any of following health conditions (But you are OK to order in your local street pharmacies):

  1. You are younger than 18 years old;
  2. You have kidney disease;
  3. Alcohol – you are addictive to alcohol, gabapentin may cause alcohol intolerance;
  4. diabetes – Gabapentin may affect blood sugar levels, you must find a local doctor to prescribe you Gabapentin.
  5. kidney disease,liver disease and heart diseases;
  6. a history of depression, mood disorder, drug abuse, or suicidal thoughts or actions;
  7. (for patients with RLS) if you are a day sleeper or work a night shift;
  8. You are breastfeeding mother or you are pregnant;
  9. have thoughts about suicide.
  10. If you are allergy to Gabapentin

Stop immediately if you have any thoughts about suicide. Donot order Gabapentin online if you have suicide thoughts. Please go to your doctor to have you completely checked.

We hope you can refill your Gabapentin online using our online pharmacy. You have already checked by your local doctors and they have prescribed you Gabapentin.  After your first prescription, you can order in our websites. Our doctors and pharmacists will review your health conditions too and it is much easier for you to understand the gabapentin prescription you are taking.

Gabapentin WARNINGS AND PRECAUTIONS

General

Neurontin (gabapentin) is not considered effective in the treatment of absence seizures and should therefore be used with caution in patients who have mixed seizure disorders that include absence seizures.

Discontinuation of Treatment with Neurontin

As with other anticonvulsant agents, abrupt withdrawal is not recommended because of the possibility of increased seizure frequency. There have been post-marketing reports of adverse events such as anxiety, insomnia, nausea, pain and sweating following abrupt discontinuation of treatment. (See ADVERSE REACTIONS, Post-Market Adverse Drug Reactions). When in the judgement of the clinician there is a need for dose reduction, discontinuation or substitution with an alternative medication, this should be done gradually over a minimum of 1 week (a longer period may be needed at the discretion of the prescriber).

Psychomotor Impairment

Patients with uncontrolled epilepsy should not drive or handle potentially dangerous machinery. During clinical trials, the most common adverse reactions observed were somnolence, ataxia, fatigue, and nystagmus. Patients should be advised to refrain from activities requiring mental alertness or physical coordination until they are sure that Neurontin does not affect them adversely.

Central Nervous System Depression

Respiratory Depression

Gabapentin has been associated with central nervous system (CNS) depression including sedation, somnolence, loss of consciousness as well as serious cases of respiratory depression. Patients with compromised respiratory function, respiratory or neurological disease, renal impairment and the elderly are at higher risk of experiencing these severe adverse effects. Concomitant use of CNS depressants with gabapentin is also a contributing factor.

Concomitant Use With Opioids

Concomitant use of opioids with NEURONTIN potentiates the risk of respiratory depression, profound sedation, syncope, and death. Gabapentin concentrations may also increase in patients receiving concomitant opioid (See DRUG INTERACTIONS).

Patients who require concurrent treatment with opioids or other CNS depressants should be observed carefully for signs and symptoms of CNS depression, and the dose of gabapentin or opioid should be reduced accordingly. See also DOSAGE AND ADMINISTRATION, Dosing Considerations.

Carcinogenesis and Mutagenesis

Gabapentin produced an increased incidence of acinar cell adenomas and carcinomas in the pancreas of male rats, but not female rats or in mice, in oncogenic studies with doses of 2000 mg/kg which resulted in plasma concentrations 14 times higher than those occurring in humans at a dose of 2400 mg/day. The relevance of these pancreatic acinar cell tumours in male rats to humans is unknown, particularly since tumours of ductal rather than acinar cell origin are the predominant form of human pancreatic cancer. (See TOXICOLOGY, Carcinogenicity Studies).

Dependence/Tolerance

The abuse and dependence potential of gabapentin has not been evaluated in human studies. Cases of abuse and dependence have been reported in the post-marketing database. These individuals were taking higher than recommended doses of gabapentin for unapproved uses. Most of the individuals described in these reports had a history of polysubstance abuse or used gabapentin to relieve symptoms of withdrawal from other substances. As with any CNS active drug, physicians should carefully evaluate patients for a history of drug abuse and follow such patients closely, observing them for signs of abuse or misuse of Neurontin (e.g. development of tolerance, self-dose escalation, and drug-seeking behavior).

There are rare post-marketing reports of individuals experiencing withdrawal symptoms shortly after discontinuing higher than recommended doses of gabapentin used to treat illnesses for which the drug is not indicated. Such symptoms included agitation, disorientation and confusion after suddenly discontinuing gabapentin that resolved after restarting gabapentin. Most of these individuals had a history of poly-substance abuse or used gabapentin to relieve symptoms of withdrawal from other substances.

Hypersensitivity

Serious Dermatological Reactions

There have been post-marketing reports of Stevens-Johnson syndrome (SJS) and Erythema multiforme (EM) in patients during treatment with gabapentin. Should signs and symptoms suggest SJS or ER, gabapentin should be discontinued immediately. (see Post-Marketing Adverse Drug Reactions)

There have been reports in the post-marketing experience of hypersensitivity including systemic reactions and cases of urticaria and angioedema. (see Post-Marketing Adverse Drug Reactions)

Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)

Severe, life-threatening, systemic hypersensitivity reactions such as Drug rash with eosinophilia and systemic symptoms (DRESS) syndrome have been reported in patients taking antiepileptic drugs including gabapentin.

It is important to note that early manifestations of hypersensitivity, such as fever or lymphadenopathy, may be present even though rash is not evident. If such signs or symptoms are present, the patient should be evaluated immediately. Gabapentin should be discontinued if an alternative etiology for the signs or symptoms cannot be established.

Prior to initiation of treatment with gabapentin, the patient should be instructed that a rash or other signs or symptoms of hypersensitivity such as fever or lymphadenopathy may herald a serious medical event and that the patient should report any such occurrence to a physician immediately.

Anaphylaxis

Gabapentin can cause anaphylaxis. Signs and symptoms in reported cases have included difficulty breathing, swelling of the lips, throat and tongue and hypotension requiring emergency treatment. Patients should be instructed to discontinue gabapentin and seek immediate medical care should they experience signs or symptoms of anaphylaxis.

Neurologic

Gabapentin treatment has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall). There have also been postmarketing reports of agitation, confusion, loss of consciousness and mental impairment. Therefore, patients should be advised to exercise caution until they are familiar with the potential effects of the medication. (See DOSAGE AND ADMINISTRATION, Dosing Considerations and Special Patient Populations).

Psychiatric

Suicidal ideation and behaviour

Suicidal ideation and behaviour have been reported in patients treated with antiepileptic agents in several indications.

All patients treated with antiepileptic drugs, irrespective of indication, should be monitored for signs of suicidal ideation and behaviour and appropriate treatment should be considered. Patients (and caregivers of patients) should be advised to seek medical advice should signs of suicidal ideation or behaviour emerge.

An FDA meta-analysis of randomized placebo controlled trials, in which antiepileptic drugs were used for various indications, has shown a small increased risk of suicidal ideation and behaviour in patients treated with these drugs. The mechanism of this risk is not known.

There were 43,892 patients treated in the placebo controlled clinical trials that were included in the meta-analysis. Approximately 75% of patients in these clinical trials were treated for indications other than epilepsy and, for the majority of non-epilepsy indications the treatment (antiepileptic drug or placebo) was administered as monotherapy. Patients with epilepsy represented approximately 25% of the total number of patients treated in the placebo controlled clinical trials and, for the majority of epilepsy patients, treatment (antiepileptic drug or placebo) was administered as adjunct to other antiepileptic agents (i.e., patients in both treatment arms were being treated with one or more antiepileptic drug). Therefore, the small increased risk of suicidal ideation and behaviour reported from the meta-analysis (0.43% for patients on antiepileptic drugs compared to 0.24% for patients on placebo) is based largely on patients that received monotherapy treatment (antiepileptic drug or placebo) for non-epilepsy indications. The study design does not allow an estimation of the risk of suicidal ideation and behaviour for patients with epilepsy that are taking antiepileptic drugs, due both to this population being the minority in the study, and the drug-placebo comparison in this population being confounded by the presence of adjunct antiepileptic drug treatment in both arms.

Special Populations

Pregnant Women: Based on animal data, gabapentin may cause fetal harm (see TOXICOLOGY – Reproduction Studies). In non-clinical studies in mice, rats and rabbits, gabapentin was developmentally toxic (e.g., increased fetal skeletal and visceral abnormalities, and increased embryofetal mortality) when administered to pregnant animals at doses lower than the maximum recommended human dose (MRHD) of 3600 mg/day on a body surface area (mg/m2) basis.

Teratogenic Potential: Gabapentin crosses the human placental barrier. Although there are no adequate and well-controlled studies in pregnant women, congenital malformations and adverse pregnancy outcomes have been reported with gabapentin use, both from literature and Pregnancy Registries. Since the potential risk for humans is uncertain, gabapentin should only be used during pregnancy if the potential benefit to the mother outweighs the potential risk to the fetus. If women decide to become pregnant while taking NEURONTIN, the use of this product should be carefully re-evaluated.

Pregnancy Registry: Physicians are advised to recommend that pregnant patients taking NEURONTIN enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry. This can be done by calling the toll free number 1-888-233-2334, and must be done by patients themselves. Information on the registry can also be found at the following website: http://www.aedpregnancyregistry.org/.

Nursing Women: Gabapentin is excreted in human milk. There are no controlled studies on the effects of gabapentin on breast-fed infants. Because of the potential for serious adverse reactions in nursing infants, a decision should be made as to whether to discontinue nursing or to discontinue NEURONTIN, taking into account the benefit of the drug to the mother.

Pediatrics: The safety and efficacy in patients under the age of 18 have not been established.

Safety data in 39 patients between the ages of 12 and 18 years included in the double-blind, placebo-controlled trials showed that, at doses of 900 to 1200 mg/day, the incidence of adverse events in this group of patients was similar to that observed in older individuals.

In controlled clinical trials involving patients, 3 to 12 years of age (N=323), psychiatric adverse events such as emotional lability, hostility, hyperkinesia and thought disorder were reported at a higher frequency in patients treated with gabapentin compared to placebo.

Geriatrics: Systematic studies in geriatric patients have not been conducted. Adverse clinical events reported among 59 patients over the age of 65 years treated with Neurontin did not differ from those reported for younger individuals. The small number of individuals evaluated and the limited duration of exposure limits the strength of any conclusions reached about the influence of age, if any, on the kind and incidence of adverse events associated with the use of Neurontin.

As Neurontin is eliminated primarily by renal excretion, dosage adjustment may be required in elderly patients because of declining renal function. (See DOSAGE AND ADMINISTRATION, Dosing Considerations; ACTION AND CLINICAL PHARMACOLOGY, Special Populations and Conditions).

 

Gabapentin Side Effects

Adverse Drug Reaction Overview

Commonly Observed Adverse Events

The most commonly observed adverse events associated with the use of Neurontin (gabapentin) in combination with other antiepileptic drugs, not seen at an equivalent frequency in placebo-treated patients, were somnolence, dizziness, ataxia, fatigue, nystagmus and tremor
(See Table 1).

Adverse Events Leading to Discontinuation of Treatment

Approximately 6.4% of the 543 patients who received Neurontin in the placebo-controlled studies withdrew due to adverse events. In comparison, approximately 4.5% of the 378 placebo-controlled participants withdrew due to adverse events during these studies. The adverse events most commonly associated with withdrawal were somnolence (1.2%), ataxia (0.8%), fatigue, nausea and/or vomiting and dizziness (all at 0.6%).

Clinical Trial Adverse Drug Reactions

Because clinical trials are conducted under very specific conditions the adverse reaction rates observed in the clinical trials may not reflect the rates observed in practice and should not be compared to the rates in the clinical trials of another drug. Adverse drug reaction information from clinical trials is useful for identifying drug-related adverse events and for approximating rates.

Incidence in Controlled Clinical Trials

Adults

Multiple doses of Neurontin were administered to 543 subjects with partial seizures in placebo controlled clinical trials of 12 weeks duration. In these studies, either Neurontin (at doses of 600, 900, 1200 or 1800 mg/day) or placebo was added to the patient’s current antiepileptic drug therapy. Treatment-emergent signs and symptoms that occurred in at least 1% of patients participating in these studies are listed in Table 1.

Table 1
Treatment-Emergent Adverse Event Incidence in Placebo-Controlled Add-On Trials (Events in at Least 1% of Neurontin Patients and Numerically More Frequent than in the Placebo Group)
Neurontina
n= 543 (%)
Placebo
n= 378 (%)
Body as a Whole
Fatigue 11.0 5.0
Weight Increase 2.9 1.6
Back Pain 1.8 0.5
Peripheral Edema 1.7 0.5
Cardiovascular
Vasodilatation 1.1 0.3
Digestive System
Dyspepsia 2.2 0.5
Mouth or Throat Dry 1.7 0.5
Constipation 1.5 0.8
Dental Abnormalities 1.5 0.3
Increased Appetite 1.1 0.8
Hematologic and Lymphatic Systems:
Leukopenia 1.1 0.5
Musculoskeletal
Myalgia 2.0 1.9
Fracture 1.1 0.8
Nervous System
Somnolence 19.3 8.7
Dizziness 17.1 6.9
Ataxia 12.5 5.6
Nystagmus 8.3 4.0
Tremor 6.8 3.2
Nervousness 2.4 1.9
Dysarthria 2.4 0.5
Amnesia 2.2 0.0
Depression 1.8 1.1
Thinking Abnormal 1.7 1.3
Twitching 1.3 0.5
Coordination Abnormal 1.1 0.3
Respiratory System
Rhinitis 4.1 3.7
Pharyngitis 2.8 1.6
Coughing 1.8 1.3
Skin and Appendages
Abrasion 1.3 0.0
Pruritus 1.3 0.5
Urogenital System
Impotence 1.5 1.1
Special Senses
Diplopia 5.9 1.9
Amblyopia 4.2 1.1
Laboratory Deviations
WBC Decreased 1.1 0.5
a
Plus background antiepileptic drug therapy.
Since Neurontin was administered most often in combination with other antiepileptic agents, it was not possible to determine which agent(s) was associated with adverse events.

Dose-Related Treatment Emergent Adverse Events

Among the treatment-emergent adverse events occurring in Neurontin-treated patients, somnolence and ataxia appeared to exhibit a positive dose-response relationship. Patients treated with 1800 mg/day (n=54, from one controlled study) experienced approximately a two-fold increase, as compared to patients on lower doses of 600 to 1200 mg/day (n=489, from several controlled studies), in the incidence of nystagmus (20.4%), tremor (14.8%), rhinitis (13%), peripheral edema (7.4%), coordination abnormal, depression and myalgia (all at 5.6%). Adverse events were usually mild to moderate in intensity, with a median time to resolution of 2 weeks.

Data from long-term, open, uncontrolled studies shows that Neurontin treatment does not result in any new or unusual adverse events.

Other Adverse Events Observed in All Clinical Trials

Adverse events that occurred in at least 1% of the 2074 individuals who participated in all clinical trials, only some of which were placebo-controlled, are described below. During these trials, all adverse events were recorded by the clinical investigators using terminology of their own choosing. To provide a meaningful estimate of the proportion of individuals having adverse events, similar types of events were grouped into a smaller number of standardized categories using modified COSTART dictionary terminology. These categories are used in the listing below. The frequencies presented represent the proportion of the 2074 patients exposed to Neurontin who experienced an event of the type cited on at least one occasion while receiving Neurontin. All reported events are included except those already listed in Table 1, those too general to be informative, and those not reasonably associated with the use of the drug.

Events are further classified within body system categories and enumerated in order of decreasing frequency using the following definitions: frequent adverse events are defined as those occurring in at least 1/100 patients; infrequent adverse events are those occurring in 1/100 to 1/1000 patients; rare events are those occurring in fewer than 1/1000 patients.

Body As A Whole: Frequent: asthenia, malaise, face edema; Infrequent: allergy, generalized edema, weight decrease, chill; Rare: strange feelings, lassitude, alcohol intolerance, hangover effect.

Cardiovascular System: Frequent: hypertension; Infrequent: hypotension, angina pectoris, peripheral vascular disorder, palpitation, tachycardia, migraine, murmur; Rare: atrial fibrillation, heart failure, thrombophlebitis, deep thrombophlebitis, myocardial infarction, cerebrovascular accident, pulmonary thrombosis, ventricular extrasystoles, bradycardia, premature atrial contraction, pericardial rub, heart block, pulmonary embolus, hyperlipidemia, hypercholesterolemia, pericardial effusion, pericarditis.

Digestive System: Frequent: anorexia, flatulence, gingivitis; Infrequent: glossitis, gum hemorrhage, thirst, stomatitis, increased salivation, gastroenteritis, hemorrhoids, bloody stools, fecal incontinence, hepatomegaly; Rare: dysphagia, eructation, pancreatitis, peptic ulcer, colitis, blisters in mouth, tooth discolor, Perleche, salivary gland enlarged, lip hemorrhage, esophagitis, hiatal hernia, hematemesis, proctitis, irritable bowel syndrome, rectal hemorrhage, esophageal spasm.

Endocrine System: Rare: hyperthyroid, hypothyroid, goiter, hypoestrogen, ovarian failure, epididymitis, swollen testicle, cushingoid appearance.

Hematologic and Lymphatic System: Frequent: purpura most often described as bruises resulting from physical trauma; Infrequent: anemia, thrombocytopenia, lymphadenopathy; Rare: WBC count increased, lymphocytosis, non-Hodgkin’s lymphoma, bleeding time increased.

Musculoskeletal System: Frequent: arthralgia; Infrequent: tendinitis, arthritis, joint stiffness, joint swelling, positive Romberg test; Rare: costochondritis, osteoporosis, bursitis, contracture.

Nervous System: Frequent: vertigo, hyperkinesia, paresthesia, decreased or absent reflexes, increased reflexes, anxiety, hostility; Infrequent: CNS tumors, syncope, dreaming abnormal, aphasia, hypesthesia, intracranial hemorrhage, hypotonia, dysesthesia, paresis, dystonia, hemiplegia, facial paralysis, stupor, cerebellar dysfunction, positive Babinski sign, decreased position sense, subdural hematoma, apathy, hallucination, decrease or loss of libido, agitation, paranoia, depersonalization, euphoria, feeling high, doped-up sensation, suicide attempt, psychosis; Rare: choreoathetosis, orofacial dyskinesia, encephalopathy, nerve palsy, personality disorder, increased libido, subdued temperament, apraxia, fine motor control disorder, meningismus, local myoclonus, hyperesthesia, hypokinesia, mania, neurosis, hysteria, antisocial reaction, suicide.

Respiratory System: Frequent: pneumonia; Infrequent: epistaxis, dyspnea, apnea; Rare: mucositis, aspiration pneumonia, hyperventilation, hiccup, laryngitis, nasal obstruction, snoring, bronchospasm, hypoventilation, lung edema.

Dermatological: Infrequent: alopecia, eczema, dry skin, increased sweating, urticaria, hirsutism, seborrhea, cyst, herpes simplex; Rare: herpes zoster, skin discolor, skin papules, photosensitive reaction, leg ulcer, scalp seborrhea, psoriasis, desquamation, maceration, skin nodules, subcutaneous nodule, melanosis, skin necrosis, local swelling.

Urogenital System: Infrequent: hematuria, dysuria, urination frequency, cystitis, urinary retention, urinary incontinence, vaginal hemorrhage, amenorrhea, dysmenorrhea, menorrhagia, breast cancer, unable to climax, ejaculation abnormal; Rare: kidney pain, leukorrhea, pruritus genital, renal stone, acute renal failure, anuria, glycosuria, nephrosis, nocturia, pyuria, urination urgency, vaginal pain, breast pain, testicle pain.

Special Senses: Frequent: abnormal vision; Infrequent: cataract, conjunctivitis, eyes dry, eye pain, visual field defect, photophobia, bilateral or unilateral ptosis, eye hemorrhage, hordeolum, hearing loss, earache, tinnitus, inner ear infection, otitis, taste loss, unusual taste, eye twitching, ear fullness; Rare: eye itching, abnormal accommodation, perforated ear drum, sensitivity to noise, eye focusing problem, watery eyes, retinopathy, glaucoma, iritis, corneal disorders, lacrimal dysfunction, degenerative eye changes, blindness, retinal degeneration, miosis, chorioretinitis, strabismus, eustachian tube dysfunction, labyrinthitis, otitis externa, odd smell.

Post-Market Adverse Drug Reactions

Sudden, unexplained deaths in patients with epilepsy have been reported where a causal relationship to treatment with gabapentin has not been established.

Post-marketing adverse events that have been reported, which may have no causal relationship to gabapentin, are as follows: agitation, anaphylactic reaction, angioedema, blood creatine phosphokinase increased, blood glucose abnormal, drug rash with eosinophilia and systemic symptoms, fall, gynaecomastia, hepatic function abnormal, hepatitis, hepatitis cholestatic, hepatitis fulminant, hyperglycemia, hypoglycemia, hypersensitivity, hyponatremia, jaundice, loss of consciousness, pancreatitis, pulmonary oedema, renal failure acute, rhabdomyolysis, sexual dysfunction (including changes in libido, ejaculation disorders and anorgasmia), Stevens-Johnson syndrome.

Adverse events following the abrupt discontinuation of gabapentin have also been reported during postmarketing experience. The most frequently reported events were anxiety, insomnia, nausea, pain and sweating.

DOSAGE FORMS, COMPOSITION AND PACKAGING

Neurontin (gabapentin) capsules and tablets are supplied as follows:

100-mg capsules:

Hard gelatin CONI-SNAP® capsules with white opaque body and cap printed with “PD” on one side and “Neurontin /100 mg” on the other. -bottles of 100 capsules

300-mg capsules:

Hard gelatin CONI-SNAP® capsules with yellow opaque body and cap printed with “PD” on one side and “Neurontin /300 mg” on the other. -bottles of 100 capsules

400-mg capsules:

Hard gelatin CONI-SNAP® capsules with orange opaque body and cap printed with “PD” on one side and “Neurontin /400 mg” on the other. -bottles of 100 capsules

600 mg tablets:

White, elliptical, biconvex, film-coated tablet with bisecting score on both sides and debossed with “NT” and “16” on one side. -bottles of 100 tablets

800 mg tablets:

White, elliptical biconvex, film-coated tablet with bisecting score on both sides and debossed “NT” and “26” on one side. -bottles of 100 tablets

Capsules contain : gabapentin, lactose, corn starch, and talc, Capsule shells may contain : gelatin, titanium dioxide, silicon dioxide, sodium lauryl sulfate, yellow iron oxide, red iron oxide, and FD&C Blue No. 2.

Tablets contain : gabapentin, poloxamer 407 NF, copolyvidone, corn starch, magnesium stearate, hydroxypropylcellulose, talc and candelilla wax.

ACTION AND CLINICAL PHARMACOLOGY

Mechanism of Action

Neurontin (gabapentin) readily enters the brain and prevents seizures in a number of animal models of epilepsy. Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid), but does not possess affinity for either GABAA or GABAB receptor.

Gabapentin binds with high affinity to the α2-δ (alpha-2-delta) subunit of voltage-gated calcium channels. Broad panel screening suggests it does not bind to other neurotransmitter receptors of the brain and does not interact with sodium channels.

The relevance of the binding activity of gabapentin to the anticonvulsant effects in animal models and in humans remains to be established (See DETAILED PHARMACOLOGY).

Pharmacokinetics

All pharmacological actions following gabapentin administration are due to the activity of the parent compound; gabapentin is not metabolized to a significant extent in humans.

Plasma gabapentin concentrations are dose-proportional at doses of 300 to 400 mg q8h, ranging between 1µg/mL and 10 µg/mL, but are less than dose-proportional above the clinical range (>600 mg q8h). There is no correlation between plasma levels and efficacy.

Gabapentin pharmacokinetics are not affected by repeated administration, and steady state plasma concentrations are predictable from single dose data. Gabapentin steady-state pharmacokinetics are similar for healthy subjects and patients with epilepsy receiving antiepileptic agents.

Absorption: Following oral administration of Neurontin (gabapentin), peak plasma concentrations are observed within 2 to 3 hours. Absolute bioavailability of a 300 mg dose of Neurontin capsules is approximately 59%. At doses of 300 and 400 mg, gabapentin bioavailability is unchanged following multiple dose administration.

Food has no effect on the rate or extent of absorption of gabapentin.

Distribution: Less than 3% of gabapentin is bound to plasma proteins. The apparent volume of distribution of gabapentin after 150 mg intravenous administration is 58+6 L (Mean + SD). In patients with epilepsy, gabapentin concentrations in cerebrospinal fluid are approximately 20% of corresponding steady-state trough plasma concentrations.

Metabolism: Gabapentin is not metabolized to a significant extent in humans. Gabapentin does not induce or inhibit hepatic mixed function oxidase enzymes responsible for drug metabolism and does not interfere with the metabolism of commonly coadministered antiepileptic drugs.

Excretion: Gabapentin is eliminated solely by renal excretion as unchanged drug, and can be removed from plasma by hemodialysis. Gabapentin elimination rate constant, plasma clearance and renal clearance are directly proportional to creatinine clearance. The elimination half-life of gabapentin is independent of dose and averages 5 to 7 hours in subjects with normal renal function.

Table 3 summarizes the mean steady-state pharmacokinetic parameters of Neurontin capsules.

Table 3. Summary of Neurontin (gabapentin) Mean Steady-State Pharmacokinetic Parameters in Adults Following Q8H Administration
Pharmacokinetic Parameter 300 mg (N = 7) 400 mg (N = 11)
Cmax (µg/mL)

tmax (hr)

T½(hr)

AUC(0-∞) (µg·hr/mL)

AE%1

4.02

2.7

5.2

24.8

NA

5.50

2.1

6.1

33.3

63.6

1
Amount excreted in urine (% of dose)
NA = Not available