Gabapentin For Pain

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.

How it works?

Gabapentin belongs to a class of drugs called anticonvulsants. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

It’s not fully understood how gabapentin works. For postherpetic neuralgia, it seems to prevent the increase in sensitivity to pain that occurs. For seizures, it may alter the effect of calcium (low levels of calcium may cause seizures).

Gabapentin is off label used for treatment of nerve pain not all kinds of pains. 65% patients think it is effective for pain but as high as 35% think it doesnot work.

bubba smith Reviewed it very good for nerve pain:

“I have severe spine damage. t7 t8 and disc in between basically gone, nerve pain unbelievable. I tried lyrica in large dose and no relief.

Then one doctor said some meds don’t work on some but do on others you just have to get the correct one. So I tried gabapentin and to me it was a life saver, within 3 days the pain was gone or close to gone. 1800 mgs a day ( 6x300mg) plus 40 mg of oxyneo (4x10mg) which is oxycodone time release formula.

The pain specialist say maybe more dose needed but I can’t function properly. That is my minimum dose even drop 1 pill out of them amounts I can feel the difference in pain.

The side effects to me are , tiredness, constipation, memory, blurred vision, moody, seems heat and humid days if outside I get really disoriented so I stay inside”

But a Anonymous guy reviewed it not good for Knee Pain:

“My Husband was given this medication due to suffering long term knee pain. He took it for approx 6 weeks max and had to stop.

The most awful side effects you can imagine for the whole time blighted him. Maybe he was just unlucky and this med didn’t suit him but it’s Cons certainly outweighed its Pros in his case.

Weight gain Excess gas Dizzyness Nausea Vomiting Diarrhoea Headaches…… Not a good one for him at all. UK Based.”

Because I am a recovering alcoholic it is crucial for me to find non-narcotic treatment for the persevering pain of my chronic pancreatitis.

I was feeling a bit hopeless with the repeated prescriptions of pain meds (which of course offer only temporary relief, and for me a danger of over-use), until my GI prescribed me Gabapentin.

This med has been incredibly successful in mitigating my pain, while also giving me huge energy (I’m a consistent runner so this factor is welcomed), and allowing me to move forward with my sobriety.

I give it four stars, though I realize like anything, it’s not for everyone. That said, good luck to you all with finding what works.

Gabapentin is Widely Used for Pain Relief

Gabapentin is approved to treat the type of nerve pain (neuralgia) that results from nerve damage. Gabapentin is used to treat neuralgia caused by a herpes zoster viral infection, also known as shingles. This pain is called post-herpetic neuralgia (PHN), and it can be severe and chronic. Gabapentin is also used to treat pain from diabetic neuropathy, which happens when nerves in the feet damaged by diabetes cause chronic burning pain.

The exact way that gabapentin works to relieve pain is not known. It may change the way the body senses and reacts to pain. Gabapentin is used to manage long-term (chronic) pain, not to be taken for pain as needed. Chronic pain can interfere with sleep and work, and lead to depression.

Studies show that pain relief may start within one week and reach a maximum effect in about 4 weeks. It can take this long because gabapentin is usually started at a low dose and gradually increased over time until it works.

For treating neuralgia, gabapentin is often started at 300 mg per day and gradually raised by 300 mg per day. One 2017 review of 37 studies found that pain relief usually occurs at a dose of 1,200 mg or more.

The same review compared gabapentin to an inactive medicine (placebo) in almost 6,000 adults with chronic pain from PHN or diabetic neuropathy. Study participants were given either gabapentin or a placebo for 4 to at least 12 weeks. The results showed that 30-40% of people taking gabapentin were able to reduce their pain by half or more, compared to 10-20% of people taking the placebo.

Although some people may get significant relief, others may have side effects without relief of pain. More than half of people taking gabapentin did not get significant relief and had side effects from the drug.

According to the review, about 60% of people taking gabapentin had side effects, including:

Dizziness
Sleepiness
Water retention (edema)
Clumsiness while walking (ataxia)

It does not typically make pain worse: In trials comparing gabapentin side effects to placebo side effects, only 1% of people reported increased pain, and this was the same for gabapentin and placebo.

Once you find the dose that relieves neuralgia for you, it is important not to stop taking it suddenly. Stopping suddenly can lead to withdrawal symptoms such as:

Anxiety
Insomnia
Nausea
Pain
Sweating

What Diseases is Gabapentin Used For ? Is Gabapentin Suitable for Children under 6 Years of Age ?

Gabapentin is not suitable for children under 6 years of age but, if it has been prescribed for a child who is older than this, check the label carefully to make sure you are giving the correct dose.
Gabapentin is FDA approved as an anti-convulsant for the treatment of Epilepsy and seizures resulting from other disorders. It is used to treat neuralgia and neuropathy, both of which are syptoms of many different diseases; such as, diabetic neuropathy or Shingles related neuralgia, among other disorders like fibromyalgia, as well as, physical trauma.

Dr.s also prescribe it for general anxiety and panic disorders, instead of more addicting benzodiazepines. and very recently it has been tried as a treatment for major depression and mood disorders.
It can help potentiate the efficacy of analgesic drugs, mostly opiate/opioid medications. It also helps mitigate the unpleasant side effects of withdrawal from opiates during titration and cessation of those drugs. It can treat Restless Leg Syndrome (RLS).
It is not a controlled substance in the United States, and has a very low abuse potential, because it’s efficacy is dose dependent, with limited bioavailability and therefore, the higher the dose the less effective it is. It’s a gabapentinoid and it’s molecular structure is similar to that of GABA , making it a GABA analog, and it works by inhibiting Voltage-dependent Calcium channels (VDCC), it often is thought of as a GABA agonist, like benzodiazepines, but that is incorrect.
Take gabapentin exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.
The Horizant brand of gabapentin should not be taken during the day. For best results, take Horizant with food at about 5:00 in the evening.
Both Gralise and Horizant should be taken with food. Neurontin can be taken with or without food.
If you break a Neurontin tablet and take one half of it, take the other half at your next dose. Any tablet that has been broken should be used as soon as possible or within a few days.
Measure liquid medicine with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.
If your doctor changes your brand, strength, or type of gabapentin, your dosage needs may change. Ask your pharmacist if you have any questions about the new brand you receive at the pharmacy.
Do not stop using gabapentin suddenly, even if you feel fine. Stopping suddenly may cause increased seizures. Follow your doctor’s instructions about tapering your dose.
Wear a medical alert tag or carry an ID card stating that you take gabapentin. Any medical care provider who treats you should know that you take seizure medication.
This medication can cause you to have a false positive urine protein screening test. If you provide a urine sample for testing, tell the laboratory staff that you are taking gabapentin.
Store at room temperature away from light and moisture.

How to take gabapentin

Before starting this treatment, read the manufacturer’s printed information leaflet from inside the pack. The leaflet will give you more information about gabapentin and any possible side-effects from taking it.
Take gabapentin exactly as your doctor has told you to. You will be advised to take a small dose when you first start taking gabapentin and then to increase your doses over a few days as your body gets used to it. Your doctor or pharmacist will explain this to you and your dose will also be on the label of your pack.
Gabapentin is not suitable for children under 6 years of age but, if it has been prescribed for a child who is older than this, check the label carefully to make sure you are giving the correct dose.
You can take gabapentin before or after meals. Swallow the tablets/capsules with a drink of water.
Once you are taking a regular amount of gabapentin, try to take your doses at the same times each day. This will help you to avoid missing any of your doses.
If you do forget to take a dose, take it as soon as you remember, but do not take two doses together to make up for a forgotten dose.
If you need to take an antacid or indigestion remedy, do not take it during the two hours before and the two hours after you take gabapentin. This is because they interfere with the way gabapentin works.

Store the liquid medicine in the refrigerator. Do not freeze.

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.

Is Gabapentin an Opiate?

Gabapentin is a drug that is sold under numerous brand names (most commonly, Neurontin), and there are numerous generic forms of the drug.

Gabapentin is formally listed as an anticonvulsant drug, meaning that it is designed to control seizures. It is also used for the control of certain types of pain, for anxiety control in certain types of mental health disorders, for the treatment of withdrawal symptoms, and for numerous other applications.
Gabapentin was designed to be a synthetic analog of the neurotransmitter GABA, or gamma-aminobutyric acid. GABA is the primary inhibitory neurotransmitter in the brain and spinal cord. Neurotransmitters are chemical substances that are released by the neurons in the brain and spinal cord when they are activated, and they allow neurons to communicate with each other and to produce different types of behaviors. Inhibitory neurotransmitters like GABA slow the activity of other neurons, allowing for different types of control and communication between neurons in the brain and spinal cord.

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.

How Gabapentin Works ?

Gabapentin belongs to a class of drugs called anticonvulsants. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

It’s not fully understood how gabapentin works. For postherpetic neuralgia, it seems to prevent the increase in sensitivity to pain that occurs. For seizures, it may alter the effect of calcium (low levels of calcium may cause seizures).

What Are Opiates?

Opiate drugs are either developed from substances that come from the Asian poppy plant (from opium), or they are synthetically manufactured chemical substances that resemble various aspects of substances found in opium. The primary use of opiate drugs is for pain control, although there are some other uses, such as to control coughing or diarrhea.
Opiate drugs are significant drugs of abuse and have received much attention in the media as drugs of abuse. Some of the more common and well-known opiate drugs include the illicit drug heroin and prescription medications like morphine, Vicodin (a combination of the over-the-counter pain reliever acetaminophen and the opiate drug hydrocodone), OxyContin (the opiate drug oxycodone), and many others.

Major Differences and Similarities between Opiates and Gabapentin

prescription bottles and white pills Both drugs have different mechanisms of action. Gabapentin’s mechanism of action is not fully understood. Even though it was designed to be a synthetic form of the neurotransmitter GABA, it does not attach to the GABA receptors. Instead, it appears to affect the electrical activity within the neuron, and this may result in an inhibitory or slowing response that may lead to an increase in the levels of GABA in the brain and spinal cord.
Opiate drugs attached to specific receptor sites in the brain that are naturally designed to affect the subjective experience of pain and stress, and they are designed for endorphins and other neurotransmitters known as enkephalins. These neurotransmitters are often collectively referred to as endogenous opiates and the receptor sites as opioid receptors. Thus, both drugs are chemically different with different mechanisms of action.
Both drugs require prescriptions from a physician in order to use legally; however, gabapentin is not listed as a controlled substance by the United States Drug Enforcement Administration (DEA), whereas all opiate drugs are controlled substances. The DEA now requires close monitoring of opiates, and people must get a new prescription from their physician in order to continue using the drug once they have run out of it, whereas this does not apply to gabapentin. Thus, the level of control placed on these drugs is entirely different.
Both gabapentin and opiate drugs appear to slow the functioning of the neurons in the brain and spinal cord (the central nervous system), but as mentioned above, they do so by different mechanisms of action. Thus, both drugs can be used to treat issues with the subjective experience of pain as a result of specific types of signals in the brain. By slowing down the singling process in the brain, both drugs can affect or decrease this subjective experience of pain.
Both gabapentin and opiate drugs can be drugs of abuse; however, gabapentin has a much lower potential for abuse than opiate drugs. Gabapentin does not appear to produce euphoria to the extent that opiate drugs do. Research studies looking at the abuse of gabapentin suggest that it is most commonly abused in conjunction with other drugs of abuse, whereas opiate drugs are primary drugs of abuse.
Chronic use of either gabapentin or opiate drugs can lead to physical dependence (tolerance and withdrawal), but the potential for physical dependence on gabapentin is much lower than it is for the opiate drugs. Moreover, the withdrawal syndrome that occurs with opiate drugs is far more severe than the withdrawal syndrome that occurs with gabapentin.
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The Bottom Line
While gabapentin and opiate drugs share some minor similarities, they are very different drugs. Gabapentin is not an opiate drug and not considered to be a dangerous drug of abuse like most opiate drugs.