Gabapentin For Restless Legs Syndrome

What is Gabapentin?

Gabapentin is an anti-epileptic drug, also called an anticonvulsant. It affects chemicals and nerves in the body that are involved in the cause of seizures and some types of pain.

Gabapentin is used together with other medicines to treat partial seizures in adults and children at least 3 years old.

Gabapentin is also used to treat neuropathic pain (nerve pain) caused by herpes virus or shingles (herpes zoster) in adults.

Use only the brand and form of gabapentin your doctor has prescribed. Check your medicine each time you get a refill to make sure you receive the correct form.

The Gralise brand of gabapentin is indicated for the management of neuropathic pain only. It is not used for epilepsy.

Horizant is used to treat nerve pain and restless legs syndrome (RLS).

The Neurontin brand is used to treat seizures in adults and children who are at least 3 years old, in addition to neuropathic pain.

Gabapentin for Restless Legs Syndrome

Compared to placebo, gabapentin was associated with reduced symptoms on all rating scales. In addition, sleep studies showed a significantly reduced periodic leg movements during sleep (PLMS) index and improved sleep architecture (increased total sleep time, sleep efficiency, and slow wave sleep, and decreased stage 1 sleep). Patients whose symptoms included pain benefited most from gabapentin. The mean effective dosage at the end of the 6-week treatment period was 1,855 mg, although therapeutic effects were already observed at the end of week 4 (1,391 mg).

Gabapentin improves sensory and motor symptoms in RLS and also improves sleep architecture and PLMS.

I have suffered with RLS for pretty much my entire life, I’m 55 now. Discovered gabapentin reading blog posts.

I have tried all the other meds. My RLS was getting so bad I was having a lot of episodes during the day and not just at night, but worse at night. I could not sit still to even look at a newspaper or magazine. There were time I actually thought I was going to go completely insane.

Most night I didn’t sleep more than an hour or two.

Even then I was not getting a good deep sleep. When I asked my GP about gabapentin, he had no problem prescribing it for me. He even followed recommendation for the dosage.

I take 100mg in the morning and at lunch. Before bedtime I take 200 mg.. All I can say is that this has been a godsend for me.

One of Gabapentin off-label use is to treat Restless Legs Syndrome. 76% patients think Gabapentin is good for RLS. A lot of doctors also recommend its off-label usage for RLS.

Joge siad: “I have had RLS and insomnia since around age nine. I was 1st prescribed gabapentin after herniating a disc three years ago. Didn’t notice any effect on my RLS, but I was so drugged up, I wouldn’t have. I was prescribed it again as a sleep aid two months ago.

I have been taking lorazepam for sleep for years, and wasn’t thrilled about taking 2mg of a benzo every night. It works great for sleep, but I feel hung over the next day — can’t seem to clear the fog. I ran out of gabapentin and noticed, holy cow, my legs are driving me crazy.

Only then did it occur to me – – I hadn’t had any RLS symptoms since I started taking it. I thought I had made a major discovery. LOL. This is the only drug that has ever touched my RLS.”

Gabapentin Side Effects

What is gabapentin?

Gabapentin is an anti-epileptic drug, also called an anticonvulsant. It affects chemicals and nerves in the body that are involved in the cause of seizures and some types of pain.

Gabapentin is used together with other medicines to treat partial seizures in adults and children at least 3 years old.

Gabapentin is also used to treat neuropathic pain (nerve pain) caused by herpes virus or shingles (herpes zoster) in adults.

Use only the brand and form of gabapentin your doctor has prescribed. Check your medicine each time you get a refill to make sure you receive the correct form.

The Gralise brand of gabapentin is indicated for the management of neuropathic pain only. It is not used for epilepsy.

Horizant is used to treat nerve pain and restless legs syndrome (RLS).

The Neurontin brand is used to treat seizures in adults and children who are at least 3 years old, in addition to neuropathic pain.

What is Gabapentin side effects ?

Gabapentin may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

drowsiness
tiredness or weakness
dizziness
headache
uncontrollable shaking of a part of your body
double or blurred vision
unsteadiness
anxiety
memory problems
strange or unusual thoughts
unwanted eye movements
nausea
vomiting
heartburn
diarrhea
dry mouth
constipation
increased appetite
weight gain
swelling of the hands, feet, ankles, or lower legs
back or joint pain
fever
runny nose, sneezing, cough, sore throat, or flu-like symptoms
ear pain
red, itchy eyes (sometimes with swelling or discharge)

Some side effects may be serious. If you experience any of the following symptoms, call your doctor immediately:

rash
itching
swelling of the face, throat, tongue, lips, or eyes
hoarseness
difficulty swallowing or breathing
seizures

Gabapentin may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

Call your doctor at once if you have:

increased seizures;
fever, swollen glands, body aches, flu symptoms;
skin rash, easy bruising or bleeding, severe tingling, numbness, pain, muscle weakness;
upper stomach pain, loss of appetite, dark urine, jaundice (yellowing of the skin or eyes);
chest pain, irregular heart rhythm, feeling short of breath;
confusion, nausea and vomiting, swelling, rapid weight gain, urinating less than usual or not at all;
new or worsening cough, fever, trouble breathing;
rapid back and forth movement of your eyes; or
severe skin reaction — fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Some side effects are more likely in children taking gabapentin. Contact your doctor if the child taking this medication has any of the following side effects:

changes in behavior;
memory problems;
trouble concentrating; or
acting restless, hostile, or aggressive.

Common gabapentin side effects may include:

dizziness, drowsiness;
dry mouth, blurred vision;
headache;
diarrhea; or
swelling in your hands or feet.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Can You Overdose On Gabapentin?

Compared with some drugs, such as opioids, gabapentin appears to be relatively non-lethal in overdose situations, meaning the morbidity associated with a toxic dose is low. However, the primary danger of gabapentin overdose appears when individuals use gabapentin in conjunction with other drugs, such as alcohol or opioids.

Mixing substances with central nervous system depressant effects can easily result in an amplification of certain side effects and can lead to significant issues, including overdose. For instance, individuals using gabapentin in conjunction with alcohol are subject to intensified depressant side effects such as sedation and dizziness. Alcohol itself may also cause a more rapid release of the contents of certain extended-release tablet formulations of the drug, potentially putting the user at greater risk of gabapentin overdose.

Alcohol isn’t the only danger for those using gabapentin. Among those on a prescription opioid regimen, being concurrently prescribed gabapentin is associated with a substantially increased risk of opioid-related death.

an overdose of gabapentin may result in the following symptoms:

Dizziness.
Drowsiness.
Double vision.
Slurred speech
Diarrhea.
Nausea.
Vomiting.
Loss of control of bodily movements (ataxia).
Low blood pressure.
Rapid heart rate.
Labored breathing.
Coma (in patients with kidney failure).

Gabapentin overdoses are often medically managed without significant complications. Nonetheless, any type of drug overdose can be very serious, and some individuals may experience more severe reactions in the setting of a gabapentin overdose. For instance, children, elderly individuals, and those with impaired renal function may be at a much higher risk of complications from a toxic dose of gabapentin than healthy adults.

The concurrent ingestion of other substances may also result in a more dire medical situation and, as mentioned, could increase the likelihood of overdose death. Individuals who overdose on a combination of gabapentin and another drug with depressant effects (e.g., alcohol, benzodiazepines, opioids, etc.) are at serious risk of significant adverse effects, and these individuals may require immediate medical attention.

Gabapentin may cause respiratory depression when used alone or with other substances. Combining the drug with other respiratory depressing substances may be deadly.

Unfortunately, it is all too common for gabapentin to be prescribed to individuals who also use opioids, the combination of which can result in profound respiratory depression (especially when these drugs are misused in larger-than-recommended doses).

Because of the very real risk of dangerously slowed breathing and, ultimately, respiratory arrest, those who abuse gabapentin to intensify an opioid high may risk death with each use.

Depending on the severity of any resultant oxygen deprivation and the length of time that it persists, consequences may include:

Seizures.
Permanent brain damage.
Coma.
Death.

Gabapentin Dosage

Usual Adult Dose of Gabapentin for Epilepsy:

Initial dose: 300 mg orally on day one, 300 mg orally twice a day on day two, then 300 mg orally 3 times a day on day three.
Maintenance dose: 900 to 1800 mg orally in 3 divided doses. If necessary, the dose may be increased using 300 mg or 400 mg capsules three times a day up to 1800 mg/day. Dosages up to 2400 mg/day have been well tolerated in long-term clinical studies. Doses of 3600 mg/day have also been administered to a small number of patients for a relatively short duration, and have been well tolerated. The maximum time between doses in the three times a day schedule should not exceed 12 hours.

The safety and effectiveness of gabapentin available under the trade name Gralise (R) or Horizant (R) in patients with epilepsy has not been studied.

Usual Adult Dose for Postherpetic Neuralgia:

Initial dose: 300 mg orally on day one, 300 mg orally twice a day on day two, then 300 mg orally 3 times a day on day three.

The dose may be titrated up as needed for pain relief to a daily dose of 1800 mg.
Maintenance dose: 900 to 1800 mg orally in 3 divided doses.
Efficacy was demonstrated in clinical studies over a range of 1800 mg/day to 3600 mg/day. However, no additional benefit was demonstrated from the use of doses over 1800 mg/day.

Gabapentin available under the trade name Gralise (R):
Maintenance dose: Gralise (R) should be titrated to 1800 mg orally once daily with the evening meal.
Recommended titration schedule:

Day 1: 300 mg orally with the evening meal
Day 2: 600 mg orally with the evening meal
Days 3 through 6: 900 mg orally with the evening meal
Days 7 through 10: 1200 mg orally with the evening meal
Days 11 through 14: 1500 mg orally with the evening meal
Day 15: 1800 mg orally with the evening meal

Gralise (R) is not interchangeable with other gabapentin products because of differing pharmacokinetic profiles that affect the frequency of administration.
Gabapentin enacarbil extended release tablets available under the trade name Horizant (R):
The recommended dosage is 600 mg orally twice daily. Therapy should be initiated at a dose of 600 mg orally in the morning for 3 days of therapy, then increased to 600 mg twice daily (1,200 mg/day) on day four.

Gabapentin enacarbil extended release tablets available under the trade name Horizant (R) and gabapentin are not interchangeable.

Usual Adult Dose for Restless Legs Syndrome:

Gabapentin enacarbil available under the trade name Horizant (R):
600 mg orally once daily with food at about 5 PM

Usual Pediatric Dose for Epilepsy:

Less than 3 years: Effectiveness has not been established.

Greater than or equal to 3 and less than 12 years:
Starting Dose: ranges from 10 to 15 mg/kg/day in 3 divided doses.
Effective Dose: reached by upward titration over a period of approximately 3 days. The effective dose of gabapentin in patients 5 years of age and older is 25 to 35 mg/kg/day and given in divided doses (three times a day). The effective dose in pediatric patients ages 3 and 4 years is 40 mg/kg/day and given in divided doses (three times a day). Gabapentin may be administered as the oral solution, capsule, or tablet, or using combinations of these formulations. Dosages up to 50 mg/kg/day have been well tolerated in a long term clinical study. The maximum time interval between doses should not exceed 12 hours.
Greater than 2 years:
Initial dose: 300 mg orally on day one, 300 mg orally twice a day on day two, then 300 mg orally 3 times a day on day three.
Maintenance dose: 900 to 1800 mg orally in 3 divided doses. If necessary, the dose may be increased using 300 mg or 400 mg capsules three times a day up to 1800 mg/day. Dosages up to 2400 mg/day have been well tolerated in long term clinical studies. Doses of 3600 mg/day have also been administered to a small number of patients for a relatively short duration, and have been well tolerated. The maximum time between doses in the three times a day schedule should not exceed 12 hours.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage forms (capsules, liquid, and tablets):
- For epilepsy:
  - Adults and teenagers 12 years of age and older—At first, 300 milligrams (mg) 3 times per day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 1800 mg per day.
  - Children 3 to 12 years of age—Dose is based on body weight and must be determined by your doctor. The starting dose is 10 to 15 milligrams (mg) per kilogram (kg) of body weight per day and divided in 3 doses. Your doctor may adjust your dose as needed.
  - Children younger than 3 years of age—Use and dose must be determined by your doctor.
- For postherpetic neuralgia:
  - Adults— At first, 300 milligrams (mg) as a single dose in the evening. Your doctor may adjust your dose as needed. However, the dose is usually not more than 1800 mg per day.
  - Children—Use and dose must be determined by your doctor.
For oral dosage form (extended-release tablets):
- For postherpetic neuralgia:
  - Adults— At first, 600 milligrams (mg) in the morning. Then, your doctor will increase your dose to 600 mg 2 times per day.
  - Children—Use and dose must be determined by your doctor.
- For restless legs syndrome:
  - Adults—600 milligrams (mg) as a single dose at about 5 PM.
  - Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Horizant® extended-release tablets: If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule.

the Mechanism of Action of Gabapentin

Gabapentin is an anti-epileptic medication, also called an anticonvulsant. It affects chemicals and nerves in the body that are involved in the cause of seizures and some types of pain.

Gabapentin is used in adults to treat nerve pain caused by herpes virus or shingles (herpes zoster).

Mechanism Action of Gabapentin

The Horizant brand is also used to treat restless legs syndrome (RLS).

The Neurontin brand is also used to treat seizures in adults and children who are at least 3 years old.

Use only the brand and form of gabapentin that your doctor has prescribed. Check your medicine each time you get a refill at the pharmacy, to make sure you have received the correct form of this medication.

Gabapentin is also used to treat certain types of long-lasting pain caused by damage to nerves. This type of pain, called neuropathic pain, can be caused by a number of different diseases, such as diabetes (where it is called diabetic neuropathy) andshingles (where it is called postherpetic neuralgia).

Gabapentin interacts with voltage-sensitive calcium channels in cortical neurons. Gabapentin increases the synaptic concentration of GABA, enhances GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine neurotransmitters.

One of the mechanisms implicated in this effect of gabapentin is the reduction of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in the CA1 area of the hippocampus. This is mediated through its binding to presynaptic NMDA receptors.

Other studies have shown that the antihyperalgesic and antiallodynic effects of gabapentin are mediated by the descending noradrenergic system, resulting in the activation of spinal alpha-2 adrenergic receptors. Gabapentin has also been shown to bind and activate the adenosine A1 receptor.

The mechanism by which gabapentin exerts its analgesic action is unknown, but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli).

In particular, gabapentin prevents pain-related responses in several models of neuropathic pain in rats or mice (e.g., spinal nerve ligation models, streptozocin-induced diabetes model, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase offormalin test). Gabapentin did not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase, acetic acid abdominal constriction test, footpad heat irradiation test). The relevance of these models to human pain is not known.

The mechanism by which gabapentin exerts its anticonvulsant action is unknown, but in animal test systems designed to detect anticonvulsant activity, gabapentin prevents seizures as do other marketed anticonvulsants. Gabapentin exhibits antiseizure activity in mice and rats in both the maximal electroshock and pentylenetetrazole seizure models and other preclinical models (e.g., strains with genetic epilepsy, etc.). The relevance of these models to human epilepsy is not known.

Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. Gabapentin was tested in radioligand binding assays at concentrations up to 100 μM and did not exhibit affinity for a number of other common receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine, alpha 1, alpha 2, or beta adrenergic, adenosine A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, serotonin S1 or S2, opiate mu, delta or kappa, cannabinoid 1, voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem, or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A 20-alpha-benzoate. Furthermore, gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin.

In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain tissue has been identified as an auxiliary subunit of voltage-activated calcium channels. However, functional correlates of gabapentin binding, if any, remain to be elucidated.

Gabapentin Reviews for Restless Legs Syndrome

What is gabapentin?

Gabapentin (brand names: Neurontin®, Aclonium®, Equipax®, Gantin®, Gabarone®, Gralise®, Neurostil®, Progresse®) is an anti-seizure and pain medication that is used with other medications to treat seizures and is also used to treat chronic pain, primarily nerve pain. It has also been used in cats to treat fear and anxiety associated with veterinary visits.

Gabapentin reviews for restless legs syndrome

Restless legs syndrome (RLS), also known as Willis-Ekbom disease, is a movement disorder characterized by unpleasant sensations and involuntary leg movements during sleep.

This condition may leave you kicking your legs as you fall asleep. The continued nighttime movements can prevent you from getting restorative sleep—making you sleepy during the day. There are many medical issues that can cause RLS, and it can also be idiopathic (without a known cause).

If you meet the diagnostic criteria for RLS, you can be treated with medications. Lifestyle strategies —like not smoking—can help diminish the symptoms of RLS too.

There are no cures for primary restless legs syndrome, or RLS, although various treatments often can help relieve symptoms. Treatment for secondary restless legs syndrome (RLS caused by another medical problem) involves treating the underlying cause.

The First Step in Treating Restless Legs Syndrome

The first line of defense against restless legs syndrome is to avoid substances or foods that may be causing or worsening the problem. Stay away from alcohol, caffeine, and nicotine. This may help relieve your symptoms. In addition, review all medications you are taking with your doctor to determine if any of these drugs could be causing the problem.

Any underlying medical conditions, such as anemia, diabetes, nutritional deficiencies, kidney disease, thyroid disease, varicose veins, or Parkinson’s disease, should be treated. Dietary supplements to correct vitamin or mineral deficiency may be recommended. For some people, these treatments are all that is needed to relieve RLS symptoms.

You may also benefit from physical therapy and self-care treatments, such as stretching, taking hot or cold baths, whirlpool baths, applying hot or cold packs to the affected area, limb massage, or vibratory or electrical stimulation of the feet and toes before bedtime. Exercise and relaxation techniques also may be helpful.

Gabapentin Medications for Restless Legs Syndrome

Daily medication is usually recommended only for people who have symptoms of restless legs syndrome at least three nights a week, or as determined by your doctor. Keep in mind that drugs used to treat primary RLS do not cure the condition, but only relieve symptoms. People whose RLS symptoms occur sporadically may be prescribed medication to take only when they have symptoms.

The prescription drug gabapentin (sold under the trade name Neurontin or Horizant) is a commonly used medication that can help treat the symptoms of restless legs syndrome (RLS).

Uses

Gabapentin can be used to treat the symptoms of restless legs syndrome (RLS).1 It may be especially helpful if the symptoms are perceived as less intense yet painful. In individuals with a history of peripheral neuropathy or chronic pain, it may be of added benefit. Furthermore, gabapentin may be helpful to treat RLS in the context of other neurological disorders such as Parkinson’s disease or dementia.

How It Works

Gabapentin is a medication that has been used to treat seizures. It is similar in structure to GABA, which is present in nerve cells, but it does not interact with the same receptors.

It is not known how gabapentin works to improve the symptoms of RLS.

Who Should Not Use It

Gabapentin is a relatively safe drug that can be used by most people. There are a few situations where caution may be indicated. For example, if you have impaired kidney function, are elderly, or have depression you may want to be cautious.3 If these situations apply to you, you may want to speak to your physician before taking gabapentin.

Safety Warnings

It will be important to monitor for signs of depression, unusual behavior changes, and thoughts of suicide.5

Other medications that can be used to treat RLS

The following medications are the most widely prescribed to treat RLS. They may be given alone or, in certain cases, in combination. Your doctor will prescribe the best treatment plan for you.

Dopamine agonists: These are most often the first medicines used to treat RLS. These drugs, including pramipexole (Mirapex), rotigotine (Neupro), and ropinirole (Requip), act like the neurotransmitter dopamine in the brain. Side effects include daytime sleepiness, nausea, and lightheadedness.
Dopaminergic agents: These drugs, including Sinemet — a combination of levodopa and carbidopa — increase the level of dopamine in the brain and may improve leg sensations in RLS. However, they may cause a worsening of symptoms for some people after daily use. Side effects can also include nausea, vomiting, hallucinations, and involuntary movements (dyskinesias).
Benzodiazepines: Benzodiazepines, such as alprazolam (Xanax), clonazepam (Klonopin), and temazepam (Restoril), are sedatives. They do not so much relieve symptoms as help you sleep through the symptoms.
Opiates: These drugs are most often used to treat pain, but they can also relieve RLS symptoms. Because opiates are very addictive, they are usually used only when other drugs don’t work. Hydrocodone (Vicodin, Norco) is one example.
Anticonvulsants: These agents, such as gabapentin (Neurontin) and gabapentin enacarbil (Horizant), may help relieve the symptoms of RLS as well as any chronic pain or nerve pain.
Alpha2 agonists: These agents stimulate alpha2 receptors in the brain stem. This activates nerve cells (neurons) that “turn down” the part of the nervous system that controls muscle involuntary movements and sensations. The drug clonidine (Catapres) is an example.