Gabapentin: what is it, the effect of the drug, consequences

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Attention! The material contains information about substances, the use of which can cause serious harm to your health!

Pharmacy addicts are confident that the drugs sold at the pharmacy are less dangerous than drugs. In addition, they have a more favorable price, and it is possible to purchase without a prescription (for example, through friends or just like that, if the pharmacist practices this). All this makes pharmacy drug addiction accessible to teenagers and young people. This problem also includes the use of gabapentin, a pharmacological drug for epilepsy.

  • Gabapentin as a drug
  • What is gabapentin?
  • Composition of gabapentin
  • Photo of the drug: what it looks like
  • Effect of gabapentin
  • Duration of action of gabapentin
  • Signs of Gabapentin Use
  • Combination with other substances
  • Gabapentin and Lyrica
  • Gabapentin and coffee
  • Gabapentin and alcohol
  • Gabapentin and phenibut
  • Consequences of using gabapentin
  • Quick addiction from the drug effect
  • The effect of gabapentin on the body
  • Gabapentin addiction
  • Overdose
  • Gabapentin poisoning: first aid
  • Withdrawal
  • Treatment of Gabapentin Addiction

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Review

Unlike other neurotransmitters such as serotonin and dopamine, GABA (gamma-aminobutyric acid) does not seem to get the popularity it deserves. GABA is one of the most involved inhibitors

in our central nervous system. This means that GABA prevents certain neurotransmitters from being effective, or at least completely effective.

Thus, GABA helps you relax or stop being afraid and ensures that you get a good night's sleep. Unfortunately, we live in a stressful world, but increasing the levels of GABA in your brain may be one of the solutions to getting rid of sleep problems.

Signs of Gabapentin Use

You can suspect a drug addict using gabapentin based on the following signs:

  • uncertain, shaky gait;
  • confused speech;
  • impaired coordination of movements, balance;
  • excessive sociability;
  • depression;
  • insomnia combined with drowsiness;
  • outbursts of aggression without reason;
  • rave;
  • hallucinations.

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GABA neurotransmitter

First of all, what is a neurotransmitter? It is a chemical in our brain that transmits information from one neuron (nerve cell) to another.

To send information, a neuron releases neurotransmitters into the space between itself and another neuron. This space is called a synapse. Neurotransmitters then attach to the receptors of the next neuron, transmitting their part of the information. The signal is called an action potential

fires and passes through the neuron, maintaining a chain reaction.

However, when GABA enters a synapse, it sends information to the nerve cell that it should not

activate an action potential
.
For example, if we are very stressed because we are about to give a public speech, our body produces adrenaline. However, it also produces GABA, which prevents excessive adrenaline. Because GABA suppresses adrenaline, we can calm down and get up on stage.

In this example, GABA has attached itself to our neurons, telling them to ignore the message from adrenaline. This does not mean that the adrenaline has now completely stopped - it still has its effect, but to a lesser extent. GABA ensures that our neurons do not become overworked or overexcited.

By suppressing wakefulness-promoting neurotransmitters and reducing muscle tension, GABA prepares our body to fall asleep. In addition to sleep, GABA promotes mental health, immune health, and overall relaxation. Increased levels of GABA make us feel happy.

GABA receptors and their functions

Each neuron has receptors to which neurotransmitters attach. There are receptors for each type of neurotransmitter. GABA has two - GABA (A) and GABA (B).

GABA(A) receptors are responsible for your sleep, sedation and relaxation. Alcohol in small amounts can help you relax because it mimics GABA and binds to your GABA(A) receptors. This may explain why some people prefer a nightcap just before bed, but don't forget that alcohol before bed can interfere with your brain's deep sleep and REM stages of sleep.

GABA (B) receptors also help relax both the mind and muscles, but they do not affect the brain as strongly as GABA (A) receptors.

Our intestines also have GABA receptors, although there are not as many of them as in the brain. A study showed how the food we eat and gut bacteria can affect our mood. The more good bacteria you take in, the more GABA is released into your brain. This is one way that a healthy diet can lead to healthy sleep.

Benefits of GABA for sleep

For approximately half a century, drugs that activate GABA have been used to improve sleep. These drugs are known as barbiturates (aspirin, amobarbital, butabarbital and many others). In contrast, drugs that act as GABA suppressors promote wakefulness and REM sleep while suppressing deep sleep, which is important for its restorative purpose.

High GABA levels can:

  • Reduce sleep latency. This means it will take less time to fall asleep if your brain has plenty of the neurotransmitter GABA.
  • A study conducted in Japan found that eating foods rich in GABA can improve sleep and longer NREM (non-rapid eye movement) sleep.
  • Induce deep sleep. The same group of authors found a correlation between high GABA levels and more time people spent in deep sleep, one of the NREM stages. More time in this restorative sleep leads to an improved immune system, improved memory, reduced inflammation, reduced risk of Alzheimer's disease and better learning.
  • Keep your dreams pleasant. Many benzodiazepines work by blocking GABA receptors. People taking these drugs report having nightmares more often.

GABA, sleep paralysis and other sleep disorders

A learn published in the Journal of Neuroscience

provided plausible evidence that disruptions of both GABA (A and B) receptors and glycine receptors are closely associated with sleep paralysis in mice.

They found that REM sleep atonia is associated with these three types of receptors in the brain. It is known that paralysis of the REM muscles is a normal phenomenon during sleep, but a nervous disorder in this system can lead to problems. After blocking the GABA(A), GABA(B) and glycine receptors, they were able to reverse REM sleep paralysis.

Following this discovery, more research is needed into other sleep disorders associated with REM, such as REM behavior disorder (RBD), cataplexy, and narcolepsy. Now that we know that GABA plays a role in REM sleep, it may inspire further research into GABA and REM.

Another study published in the Journal of Sleep Research

reported that patients suffering from obstructive sleep apnea (OSA) have low levels of GABA and high levels of glutamate.
Glutamate is a neurotransmitter that plays a role in learning and memory. However, it can overexcite the nerve cell and damage or even kill it. Thus, glutamate has both good and bad sides, and when it causes cell damage, it is called an excitotoxin.
When GABA levels are low, nerve cells are not protected from overexcitation. This means that due to high levels of glutamate and low levels of GABA, patients with OSA live and work under high stress and may experience anxiety, restlessness and an inability to concentrate.

Combination with other substances

Often, polydrug addicts, in order to reduce the symptoms of “withdrawal” or, on the contrary, enhance the narcotic effects of drugs, take different drugs at the same time. For example, it could be Amphetamine, Baclofen, Habana (aka Lyrica), ethyl alcohol and others. All combinations, without exception, increase the side effects of drugs, and some options end in coma or death.

Gabapentin and Lyrica

Gabapentin and Lyrica (Pregabalin, or Gabana) have almost similar properties in terms of both GABA and effects on the body. Both drugs are used in pharmacological practice for epilepsy.

However, there are also differences between them. For example, Gabapentin is absorbed only in the small intestine, partially, entering the bloodstream slowly and unevenly. Lyrica is absorbed completely, quickly, and penetrates the mucous membrane not only of the small intestine, but also beyond. The combined use of drugs leads to the receipt of the drug effect at different times, and also provokes an increase in the adverse reactions of both drugs.

Gabapentin and coffee

Scientific studies have not found an interaction between gabapentin and caffeine. The combined use of both substances has not been studied.

Gabapentin and alcohol

However, the body's reaction to the combination of gabapentin with ethyl alcohol has been studied quite well. These two substances are absolutely incompatible with each other. Their simultaneous use threatens with the following consequences:

  • confusion;
  • pain throughout the body;
  • irritability, hostility;
  • dryness of the oral mucosa;
  • loss of coordination of movements;
  • bruising (increased fragility of blood vessels);
  • swelling of the face, limbs;
  • convulsive muscle contraction.

Alcohol greatly increases the side effects of gabapentin, which can lead to coma and death.

Gabapentin and phenibut

Phenibut is a nootropic pharmacological agent, a stimulator of metabolism in the central nervous system. This is an antidepressant not prohibited in sports, which is used to treat anxiety, sleep disorders, restlessness, and irritability. According to reviews, it enhances the effect of gabapentin. At the same time, the likelihood of developing adverse reactions of both drugs increases.

Symptoms and consequences of low GABA

Scientists have found that insomniacs have significantly lower levels of GABA than those who don't have trouble falling asleep. Low GABA levels are also associated with waking up earlier.

Depression, anxiety, and panic are symptoms of insufficient GABA levels and can be alleviated with supplements and foods that increase GABA.

GABA appears to be linked to substance addiction—using alcohol and drugs that promote GABA increases your chances of becoming addicted. Patients who are trying to quit substance abuse are often prescribed GABA-promoting drugs, which, although they help with the money transfer, are themselves addictive.

Gabapentin addiction

The rapid development of dependence on gabapentin is explained by the rapid emergence of body resistance to a certain dosage of the drug. The desired effect is not achieved, and the withdrawal syndrome makes itself felt fully, which forces the drug addict to increase the dosage.

Overdose

As with any drug, using too much gabapentin can lead to an overdose. The reaction depends on the dose, and it will be individual for everyone: the gastrointestinal tract will react more strongly in some, the heart and blood vessels in others, and others may fall into a coma. In general terms, the symptoms of an overdose are as follows:

  • depressed state, drowsiness;
  • speech problems;
  • double vision;
  • breathing problems;
  • vomiting and/or diarrhea.

If the dose is very large, death is possible, especially in combination with alcoholic beverages.

Gabapentin poisoning: first aid

In case of overdose, first of all, it is necessary to keep vital functions under control. You should definitely call an ambulance. Primary measures include gastric lavage and taking sorbent medications. There are no antidotes for gabapentin. Treatment is mainly symptomatic, but if necessary, hemodialysis can be performed in a hospital setting. In some cases, resuscitation measures may be required.

Withdrawal

Drug withdrawal, or withdrawal syndrome, can occur even in people who take gabapentin for therapeutic purposes, not to mention pharmaceutical drug addicts. Withdrawal syndrome is characterized by such phenomena as: changes in blood pressure and body temperature, severe pain in joints, muscles, and head. A depressive state reaches its peak, irritability and aggressiveness arise, sleep is disturbed, and appetite disappears.

This condition may last up to 10 days after stopping the drug. Moreover, in a more or less mild version, these manifestations will persist for another 1-1.5 months.

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How to Increase GABA Naturally?

We know that alcohol and some legal (and illegal) drugs can increase GABA, but the downside is that they disrupt the sensitivity of our neurons and lead to an imbalance in our body's natural production of GABA. This further leads to addiction.

Some scientists argue that GABA from the blood cannot enter the brain due to the blood-brain barrier.

It is a natural defense mechanism that protects our brain from harmful chemicals. There are a number of studies to support this claim, but some scientists insist that small amounts of GABA can nevertheless reach the brain.

There was evidence that GABA from the bloodstream, when taken along with L-arginine, can cross the blood-brain barrier and greatly increase GABA levels in the brain. This is due to nitric oxide, which is produced after consuming L-arginine.

There are many natural ways to safely increase GABA levels in our brains, whether through food or physical activity. Here are two lists of natural ways to get this precious neurotransmitter.

Foods that promote the development of GABA:

  • Fermented foods. Foods containing lactobacilli are rich in GABA. Some of them are kefir, yogurt, kimchi (Asian-style sauerkraut), sauerkraut, miso and tempeh. Since you already have GABA receptors in your gut, you may feel better soon after eating some of this food.
  • Foods high in glutamine. Your body uses glutamine to make GABA, so you'll benefit from the following animal foods—beef, chicken, and eggs—as well as plants such as red cabbage, beets, and beans.
  • Foods high in flavonoids. Tea, cocoa, and fruits such as apples, pears, citruses, and berries are rich in flavonoids, which can improve GABA function in your brain.
  • magnesium products rich in zinc and vitamin B6. Spinach, almonds, cashews and vegetables are high in magnesium, while fish, potatoes, carrots, peas and seeds are rich in B6. Zinc is found in meat, dairy products, seeds, legumes and nuts.

Activities to promote GABA:

  • Exercise. Daily exercise helps increase GABA levels. However, you should exercise regularly to see improvement. Exercise can help with most sleep problems and is part of good sleep hygiene.
  • Meditation and breathing exercises. By learning to relax, you allow your body to balance all of your neurotransmitters, including GABA.

GABA isn't the only natural sleep aid. There are many more foods, supplements, and habits that can help you get a good night's sleep. If you choose foods or supplements that promote GABA, be sure to take L-arginine with you.

How to take GABA

This is the jar I have with GABA.

Gamma-aminobutyric acid should be taken along with vitamin B6.

Why?

Because vitamin B6, according to recent research, is the limiting cofactor of gamma-aminobutyric acid.

The synthesis of gamma-aminobutyric acid is SENSITIVE TO VITAMIN B6 LEVEL.

If you take GABA separately from vitamin B6, you may experience:

  • Sleep disturbance.
  • Nervousness.
  • Increased risk of cardiovascular dysfunction.

There are studies that suggest that the maximum effect of GABA in terms of growth hormone production is observed if you take gamma-aminobutyric acid AFTER TRAINING.

In general, there are also studies that GABA is effective both at rest and after training, but it is not at all difficult to adhere to this recommendation, so I advise taking this neurotransmitter AFTER TRAINING.

The next recommendation concerns the blood-brain barrier, which inhibits the penetration of this substance to the pituitary gland.

In this regard, a number of scientists recommend taking GABA in dosages of 2-4 grams to feel the effect.

Reception: It is better to take GABA AFTER TRAINING, 2-4 grams per serving.

If you want better sleep, take 500-1000 mg of GABA before bed.

Attention! Increase your dosage very carefully. Start with about 500-1000 mg per day and gradually increase it to 2-4 grams.

The fact is that the substance can lead to mild side effects:

  • My face is burning.
  • Pulse and breathing increase.

These side effects can only appear if you immediately start with equine dosages of more than 4 grams per day.

The side effects go away over time (the body gets used to GABA).

GABA Supplements – Are They Worth It?

You can buy GABA supplements over the counter, but there is a lot of speculation about whether they can be used by our bodies or not.

There are two main types of GABA supplements - PharmaGABA and synthetic GABA supplement (phenibut). PharmaGABA is GABA obtained from nature, that is, from the lactobacilli that produce it. Phenibut is a synthetically modified GABA, or more precisely, beta-phenyl-GABA.

Although naturally derived supplements seem to produce better effects, the exact effect of any GABA supplements is not yet entirely clear to researchers. Much work needs to be done to come to clear conclusions about GABA intake and its actual effects.

If you decide to take GABA supplements, make sure you are familiar with their side effects and possible risks. Consult your doctor before making any important decisions.

My feelings from taking GABA

About 2 months ago, I received a package in the mail with a bunch of different additives, which I decided to test, thereby adding to the supply of useful articles on my blog.

I noticed that you really like it when I write about my feelings on any supplement, and publish the results of various experiments. This was the case, for example, when I used yohimbine hydrochloride or clenbuterol for weight loss.

I took your wishes into account, and now I will do similar experiments more often.

I purchased GABA from Now Foods. One capsule contains 500 mg of GABA and 2 mg of VITAMIN B6 (which is necessary when taking this supplement, remember?).

Here we kill two birds with one stone. We drank GABA and forgot about it.

So I started taking GABA 1.5 months ago.

I started taking it with a dosage of 500 mg per day. No side effects were noticed.

Then, in the second week, I increased the dosage to 1000 mg per day.

And after another week, up to 2 grams per day.

Now I take GABA at a dosage of 3 grams per day. I’m not in a hurry to increase the dosage yet, from the point of view of economy.

What I felt from taking this supplement:

  1. I lost about 5 kg of fat mass.
  2. I gained 1 kg of muscle mass.
  3. Periodic insomnia has disappeared (I used to have problems sleeping, especially after the weekend, before getting up early for work).
  4. I began to tolerate stress more calmly.

I measured fat loss and muscle gain using body bioimpedance analysis.

I did this for the first time (initially not to try the effect of GABA, the analysis simply coincided with taking this supplement).

In general, I was very pleased with the effect that during fat loss (catabolism), I somehow gained muscle mass. This, in theory, cannot be, but, as we said, GABA increases the level of growth hormone by 4-6 times. This could have played such a role.

Although, this may just be a measurement error. Anything is possible.

There really was periodic insomnia. I was afraid to use sleeping pills because it was addictive, but GABA itself solved the problem. I am very happy about it.

It so happened that for a long time I worked as a section manager at my plant for the production of nuclear and petrochemical equipment.

The stress was incredible. Dozens of tasks had to be completed daily and constantly planned. Closing salaries, reporting to directors, dismissals and constant debates with the working staff, all this was very exhausting.

GABA was good for relieving stress. For some it’s alcohol, friends, for others it’s healthy supplements and sports. Actually, everyone has their own choice.

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In general, there are a number of very interesting studies about GABA that show many positive properties.

For example, I looked at a study that tested combining GABA with whey protein. This neurotransmitter significantly increased protein synthesis (i.e. the protein worked much BETTER).

All these things convinced me to use this supplement. Due to it, you can get a positive synergistic effect with other supplements.

Too much GABA is bad

While there are ways to improve your GABA levels, if you overdo it, you can get results that are the exact opposite of what you are trying to achieve. This event is called a paradoxical reaction

. There are a number of physiological and psychological side effects from excessive use of GABA. Some of them are paradoxical, and some are not.

  • Anxiety. Attempting to treat anxiety with excessive consumption of this amino acid may make it worse. You may have panic attacks and a general worsening mood.
  • Insomnia. The inability to relax is associated with the inability to sleep. If you struggle with insomnia, try small doses of GABA.
  • Unusual skin sensations and redness. The effects of GABA on your nervous system can cause tingling and crawling sensations in your skin. Redness may also appear with or without these sensations. These skin problems should go away quickly.
  • Dyspnea. The inability to inhale completely may be due to the inhibitory nature of GABA. For example, the role of adrenaline is to increase breathing during brisk walking or due to stress, however, because GABA suppresses it, a person may feel the need to breathe faster but experience an inability to do so, resulting in shortness of breath.

Consequences of using gabapentin

The drug not only has a lot of side effects. In the case of recreational use, it causes a stable addiction, gradually depresses the nervous system, leading to the death of neurons, and provokes respiratory arrest.

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Quick addiction from the drug effect

Drug addiction to gabapentin develops very quickly. Among its signs are the following:

  • loss of interest in what is happening around, in loved ones, in oneself;
  • irresistible craving to use the drug;
  • loss of ability to control the use of the drug;
  • development of withdrawal syndrome, withdrawal symptoms;
  • the emergence of resistance to the usual dose, the need to increase it;
  • using a substance even when you feel very unwell.

The effect of gabapentin on the body

Long-term and excessive recreational use of the drug in violation of the instructions poisons the body, destroys the central nervous system, and reduces immunity. Among the most obvious consequences of using the drug as a drug are the following conditions and pathologies:

  • disruption of the digestive system, abdominal pain, nausea to vomiting, stool disorders;
  • the development of numerous infectious diseases due to low immunity;
  • inflammatory processes in the lungs and nasopharynx;
  • urinary tract infections, cystitis, pyelonephritis and so on;
  • pathological changes in the central nervous system: impaired coordination of movements, depressive states;
  • changes in the cardiovascular system - tachycardia, dizziness, noise or ringing in the ears;
  • skin damage in the form of rashes, constant itching;
  • swelling of soft tissues, face, limbs.

The addict constantly feels pain in the joints and/or muscles. The state of weakness and malaise is combined with drowsiness and irritability at the same time. Depression can lead to thoughts of suicide.

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