What Is Gabapentin?
Gabapentin is a prescription-only drug in the United Kingdom. It was initially formulated to emulate the neurotransmitter gamma-aminobutyric acid (GABA) as a treatment for spasticity. The drug is most widely used to treat epilepsy as it has profound anticonvulsant effects. Gabapentin can also be used in the treatment of nerve pain caused by diseases such as diabetes, shingles or an accident or injury. On rare occasions, it can also be used in the treatment of migraine headaches.
The medication is taken on a long-term basis to treat partial epileptic seizures. Partial seizures are also known as focal seizures and only affect one part of a person’s brain, meaning the sufferer doesn’t lose consciousness. It can also be highly effective at treating chronic pain, particularly of the neuropathic type. Gabapentin is thought to prevent certain signals, such as nerve pain, from reaching the brain. (1)
It is a well-regarded drug for treating epilepsy and neuropathic pain because it has minimal side effects and doesn’t interact negatively with other epilepsy medications. Certain antacids and orlistat, a drug used to treat obesity, can prevent gabapentin from working. Advice should also be sought before combining gabapentin with strong painkillers, antidepressants, antipsychotics and mefloquine. (2) This medication should never be stopped suddenly.
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Available Forms of Gabapentin
- Capsules (100 milligram, 300 milligram or 400 milligram): This form of the medication is indicated for use as conjunctive therapy or monotherapy in the treatment of focal epileptic seizures in adults and children. Capsules are also used to treat peripheral neuropathic pain such as post-herpetic neuralgia and painful diabetic neuropathy in adults.
- Tablets (600 milligram or 800 milligram): Tablets are indicated for use as conjunctive therapy or monotherapy in the treatment of focal epileptic seizures in adults and children. Capsules are also used to treat peripheral neuropathic pain such as post-herpetic neuralgia and painful diabetic neuropathy in adults.
- Oral Solution (50 milligram): The oral solution is indicated for use as conjunctive therapy or monotherapy in the treatment of focal epileptic seizures in adults and children. Capsules are also used to treat peripheral neuropathic pain such as post-herpetic neuralgia and painful diabetic neuropathy in adults. (3)
Medical Uses of Gabapentin
Gabapentin was initially manufactured in 1974 as a muscle relaxant with the potential to treat epilepsy. Benzodiazepines had been showing some positive effects in patients with epilepsy. Scientists attempted to isolate the cause of this and concluded it was the impact they have on the neurotransmitter GABA. They concluded that people with epilepsy have a deficiency of the neurotransmitter.
It was quickly discovered that GABA itself is not able to cross the blood-brain barrier. Gerhard Satzinger initiated a project that aimed to create drug molecules that would target the neurotransmitter. Satzinger and his lab synthesised gabapentin, which incorporates a lipophilic cyclohexane ring that allows GABA to pass from the blood into the brain. The drug was first marketed in the United States in 1993.
The drug was seen as having a strong safety profile and seemingly had few side effects. Tests had shown its effectiveness at treating pain that opioids and paracetamol had been ineffective for, and by 2001, 83% of the brand-name Neurontin prescriptions were not related to epilepsy. While the drug is only approved for two uses in the United Kingdom, it has several other off-label uses that some doctors may prescribe it for.
The drug can be effective at treating generalised anxiety disorder, bipolar disorder, restless leg syndrome, migraine, drug and alcohol dependence, ADHD, premenstrual syndrome and more. Doctors are usually reluctant to prescribe the drug for this reason because it emerged that there is a high potential for abuse. The drug can induce feelings of euphoria, intense relaxation and calmness, especially in those who do not follow dosage instructions. (4)
Legal Status (UK)
Gabapentin has been reclassified as a Class C, schedule 3 controlled drug in the United Kingdom as of April 2019. (5) Up until this point, it was legal to possess and distribute the drug. The reclassification is due to the rising number of deaths related to gabapentin and the similar drug, pregablin. (6) Data shows that there were 32 gabapentin- and pregablin-related deaths in 2013, rising to 127 in 2017. The prescription rate also rose by 72% in England in the last five years. (7)
The reclassification is intended to prevent people from stockpiling prescriptions and to make getting repeat prescriptions more difficult. The maximum penalties for drug possession, selling, sharing and manufacture are dictated by whether a substance is deemed Class A, B or C. Class C drugs carry up to two years and/or an unlimited fine for possession and up to 14 years and/or an unlimited fine for selling or sharing. (8)
Controlled drugs are also put into five categories that set out strict guidelines on how they are bought, sold, produced and prescribed. These controls are in place to prevent misuse, minimise harm and prevent illegal production and distribution. Gabapentin has recently been made a schedule 3 controlled substance. Prescriptions are only valid for 28 days, and specific information must be given on the label about the name, form, strength, dose and quantity by the prescribing doctor. (9)
Routes of Administration
All forms of gabapentin are intended to be taken orally. Some users have reported that chewing or crushing and snorting the substance leads to a high similar to that brought on by stimulant drugs. Using a drug in any way other than how it was prescribed by the doctor is considered substance abuse. This includes taking more than advised, taking the drug for longer than advised, sharing the drug, snorting or chewing the drug and exaggerating symptoms in order to obtain a prescription.
Pharmacological Actions of Gabapentin
The medication does not block the uptake of GABA and doesn’t exert any direct GABAergic action. It has been shown to slightly decrease levels of serotonin, norepinephrine and dopamine, but this is not thought to be clinically significant. It is postulated that the drug causes an increase in the activity of glutamic acid decarboxylase, which produces GABA.
One of the leading theories as to why gabapentin acts as a painkiller is that it inhibits calcium channels in the brain. This leads to analgesia due to the role calcium plays in chronic neuropathic pain. GABA is the brain’s main inhibitory neurotransmitter, which means it dulls or stops certain signals from being passed from the body to the brain. It has been theorised that people who suffer from epilepsy have a GABA deficiency. (1)
Chemical formula – C9H17NO2
https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?cid=3446&t=s
Gabapentin is a bitter, off-white crystalline solid that is soluble in water. It is a synthetic analogue of the neurotransmitter GABA, which has anticonvulsant activity. Its antiepileptic effect occurs through decreased levels of central nervous system disorganised electrical activity. (10)
Gabapentin Brand and Other Names
The generic name for the medication is gabapentin, and it was originally produced as a brand of the company Pfizer under the brand name Neurontin. It is also sold in the United Kingdom as Lecomig tablets, and various companies produce the drug in its generic form. Pregabalin is a gabapentinoid, meaning it has similar properties to gabapentin. Some street names for the drug include:
- Gabbies
- Johnnies
- Morontin
Gabapentin Addiction and How it Develops
This drug is a highly effective treatment for sufferers of epilepsy and neuropathic pain associated with diseases such as HIV and diabetes. The actions that cause the relief for these types of symptoms are what gives the drug its potential for abuse. Using psychoactive drugs can get an individual’s brain used to chemicals bypassing its reward system.
When this occurs, the drug causes neurotransmitters to become imbalanced through its active mechanism of binding to a receptor and replicating the effects of GABA. Addiction is also caused by the effects drugs can have on a person’s reward centre, especially if they have previously been diagnosed with a substance dependence disorder. Maintaining the correct balance of neurotransmitters is imperative to an individual’s mental health. (11)
An influx of neurotransmitters such as GABA can cause relaxation, euphoria and a sense of well-being. When gabapentin is used in higher doses, it brings on these sensations. This may lead an individual to take more of the drug to continue to experience that physical and psychological response. Discontinuing the medication can lead to severe withdrawal symptoms that may stop the person from being able to discontinue use.
Why Is Gabapentin Addictive and How Addictive Is It?
Research has shown that gabapentin is a prevalent drug of abuse. While its effects vary according to various factors, it can create a euphoric high, improved sociability, a sense of calm and zombie-like states. The rise in prescriptions for the drug since around 2002 is not thought to be proportionate to the rise in cases of epilepsy and neuropathic pain. The drug is sold for £1 per 300-milligram tablet and, due to its status as a non-controlled substance until April 2019, currently widely available. (12)
It is thought that gabapentin is being used as an opiate substitute or drug to help people who take other substances to manage withdrawal symptoms in between doses of heroin, cocaine or alcohol. When combined with these drugs and taken in high quantities, the medication can be extremely dangerous. It is a central nervous system depressant, like opiates and alcohol, so combining the two can cause seizures, coma and death. (13)
If the drug is taken according to the instructions of a doctor, there shouldn’t be any problems. Any person using the drug must be aware that stopping immediately can be very dangerous. Never cease taking the drug without medical supervision.
Causes & Risk Factors of Gabapentin Addiction
It is thought that the most significant risk factor for developing an addiction to gabapentin is the concurrent use of opiates. In a 2018 study, significantly more people who were concomitantly prescribed opiates were found to be inclined to become heavy users of gabapentin. Risk factors for people who had been taking gabapentin without opioids were bipolar disorder, insomnia and euphoria.
Risk factors of people who were prescribed opiates and gabapentin were markedly different. The most prevalent was a history of substance abuse, followed by altered mental status. It has been concluded that there is a compounded risk when an individual is prescribed opiates and gabapentin at the same time. This is especially true when the person has a history of substance abuse. (14)
Other risk factors for addiction include stress, quality of home life, the age at which the first addictive substance is taken, genetics and whether family members used drugs when an individual was a child. (15) If someone is worried about their use of gabapentin or is aware that a loved one is displaying signs of addiction, they must seek urgent medical assistance. The withdrawal process can be made easier in a clinical detoxification centre through medication, therapy and exercise.
Common Drug Combinations with Gabapentin
Recreational drug users combine the drug with cannabis, baclofen, alcohol, SSRIs, LSD and amphetamines, among others.
Co-Occurring Disorders
When a co-occurring disorder such as another substance abuse disorder or a mental health problem is present, it is important that this is identified and all problems are addressed by medical professionals. A common dual diagnosis is alcoholism and substance abuse disorder. People also sometimes have co-occurring mental health disorders that may have been present prior to the addiction and may have been a causing factor, or they may have been caused as a result of drug use.
Signs, Symptoms and Effects of Gabapentin Addiction
- Drowsiness
- Weakness
- Dizziness
- Headache
- Shaking in one part of the body
- Blurry or double vision
- Unsteadiness
- Anxiety
- Difficulty with memory
- Strange or unusual thoughts
- Uncontrolled eye movement
- Nausea and vomiting
- Heartburn
- Diarrhoea
- Dry mouth
- Constipation
- Increased appetite and weight gain
- Swelling in the extremities
- Back or joint pain
- Fever
- Ear pain
- Red, itchy eyes
The Dangers of Gabapentin Addiction
- Double vision
- Slurred speech
- Drowsiness
- Diarrhoea
- Damage to the heart, liver and kidneys
Impact of Long-Term Gabapentin Abuse on the Brain
Over time, the brain becomes accustomed to the imbalances caused by the impact gabapentin has on neurotransmitters. If it is taken away, the body has a violent reaction and causes withdrawal symptoms and cravings. It can take several months or more for the brain to fully return to normal after gabapentin abuse.
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Gabapentin Overdose Explained
Unlike opiates, there is no antidote for gabapentin. One of the most prolific ways the drug is being used is in combination with other drugs, especially opiates. It is thought that the drug potentiates the effects of substances such as heroin and methadone because both drugs depress the central nervous system. (17) While gabapentin is marketed as having a safe side effect profile, it has been indicated in suicides and as a drug of abuse with rising frequency. (18)
The side effects of taking gabapentin are usually mild if taken at the recommended dose, and these effects often subside after several weeks of use. Weakness, tiredness, drowsiness, dizziness and diarrhoea are the most commonly occurring side effects. It would take a significant amount of the drug to overdose; however, when taken in combination with other drugs, the amount necessary to overdose becomes markedly lower.
The symptoms of a gabapentin overdose are characteristic of the dulled responses of the central nervous system. This means that the signals the brain sends to nerve centres in the body are weakened or stopped entirely. Some symptoms of gabapentin overdose include:
- Drooping eyelids
- Sluggishness
- Muscle weakness
- Lethargy
- Diarrhoea
Teen Gabapentin Abuse
This type of drug is particularly worrying in terms of its appeal to young people. It has only very recently become a controlled substance, which means those who have already illicitly used the drug rarely regard the change. The drug is extremely cheap, and it has been legal for anyone to supply it. This means that there is a backlog of stock on the black market that needs to be depleted before a change in availability is likely to be seen in reality.
One of the main causing factors in the development of addiction is a young age. People who take their first psychoactive substance at a younger age are more likely to develop substance dependence. There is a particularly worrying risk posed to young people by the use of gabapentinoids: an increase in suicide. (19)
This type of drug can easily be hidden, as the way it is packaged makes it look no different from any other harmless medication. Young people can easily deceive their families into thinking there is no problem because there is no smell, paraphernalia or pronounced physical effects associated with gabapentin.
Signs and Symptoms of Withdrawal
It is very important that someone who is using gabapentin for epilepsy doesn’t stop taking their medication unless advised by a doctor. Any person who is concerned that they are addicted to the substance or is aware they have been taking more than the recommended dose must seek medical help as soon as possible. Even using the drug for longer than advised is considered abuse, and help should be sought to taper off the drug. Stopping immediately can be dangerous.
If an individual has obtained gabapentin for non-medical reasons or from non-medical sources, they must seek help immediately. The drug can cause serious side effects when abused and has a profound impact on neurotransmitters in the brain. Taking a lot of this medication causes the brain to become reliant upon the way it interacts with chemicals within the body. Stopping the medication can cause physical and psychological side effects, as well as cravings.
The symptoms of gabapentin withdrawal are thought to replicate those present in alcohol or benzodiazepine drug withdrawal due to the similar mechanism of action. (20) Gabapentin withdrawal is most likely in clients who use other illicit substances such as alcohol or opiates. (21) Some common withdrawal symptoms include:
- Anxiety
- Depression
- Insomnia
- Muscle pain
- Nightmares
- Headaches
- Dizziness
- Fatigue
- Sweating
- Shaking
- Diarrhoea
Gabapentin Detox Process
Gabapentin cessation must be tapered over a minimum of one week. (22) Detox would involve the patient giving their full medical history to a clinic and undergoing a pre-assessment. This is the point when they could ask questions and find out anything they would need to know about the details of the process. This is also the first point the medical staff at the clinic have to assess the client and begin the process of devising an individual plan to suit their unique needs.
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Overcoming Gabapentin Addiction
Gabapentin works in the same area of the brain as alcohol and benzodiazepines. It is a drug that has seriously addictive potential, especially for people who are predisposed to its effects or have previously suffered from a substance abuse disorder.
The potency of the drug shouldn’t be underestimated, and anyone who takes the drug to achieve a high should seek help immediately.
Understanding the severity of the problem is an important step in learning how to overcome addiction and find new coping mechanisms. One of the most valuable parts of finding a suitable rehabilitation clinic is having the input of a full clinical team on which therapy is best and then taking part in treatment. If a person goes into therapy with a positive attitude and a desire to change, the chances of recovery are high.
Inpatient and Outpatient treatment
Inpatient treatment involves a stay in hospital or a residential clinic. During this time, the individual has the chance to change their environment completely, which can be useful in facilitating the change necessary to overcome addiction. The person also has 24/7 access to care, and the home-like setting necessitates a close bond between the staff and the residents. Residential care also offers a space away from home, where the service user may have access to a supply.
Outpatient care usually has all the same resources and follows the same programme as an inpatient treatment programme. The main difference is that the service user goes home during the evenings and sometimes at weekends. Outpatient treatment can be particularly useful for people who have caught the addiction early and are addressing it before it has had a significant impact on their brain.
Gabapentin Addiction Treatment Medications
The type of medication used for gabapentin addiction is usually a tapering dose of the substance itself. The dose should be lowered over the course of at least a week to prevent a sudden imbalance in an individual’s neurochemistry. In some cases, benzodiazepines such as diazepam may be used. This is because both types of drug affect the same neurotransmitter, albeit in different ways. Diazepam can give relief to the withdrawal symptoms and help with insomnia.
It is a common misconception that medications are abundantly given to people in detox or rehab. This is not true; medication can help to minimise the discomfort of withdrawal symptoms and promote recovery. The doses that are given during treatment are gradually lowered until the client is no longer reliant on any substance. The only case where further medication may be given would be in the case of concurrent opiate addiction or a mental health disorder.
Therapy for Gabapentin Addiction
Traditional 12-step programmes
This type of therapy has been proven to be one of the most effective long-term ways to treat alcoholism. (23) The programme encourages people to share their feelings in a group setting, surrender to a higher power and follow the 12 steps to the best of their abilities. New recruits are encouraged to not feel intimidated by the rules and focus on other aspects of the treatment in the beginning.
Family therapy
Family therapy can be particularly useful for adolescents and young people who are struggling with addiction. This type of treatment looks at mental health problems and addresses how they impact the wider life of the individual. Sometimes, our environment has a bigger impact on us than we realise. Certain behaviours that have been normalised within a family may be causing some problems, and a therapist may be the only person who can notice and help.
Research has shown that treatment that incorporates family therapy is more effective than treatment that doesn’t. How well a family functions can make a significant impact on whether the addiction is maintained or help to create an environment conducive to abstinence. (24)
Behaviour modification
Behaviour modification has its roots in classical theory. This is where rewards are offered in return for abstinence or good behaviour. It can be very effective when used in conjunction with other forms of therapy, as it teaches the individual to gain satisfaction from a positive action as opposed to the negative action of drug-taking.
Other Kinds of Intervention
The level of intervention necessary depends on the individual. For people who have not been using gabapentin for a long period of time or whose doses have not escalated to dangerous levels, a trip to the GP may be all that it is in order. They can help the person to taper off the drug and offer guidance and advice. If the drug has been in the person’s system for longer than a month, detox and rehabilitation should be considered.
There are non-medical forms of intervention that incorporate mindfulness techniques and encourage a healthy lifestyle. While someone who chooses this kind of detox may experience more uncomfortable withdrawal symptoms, it can be a positive route to recovery. Methods include meditation, yoga, therapy and regular exercise.
Gabapentin Addiction Facts and Statistics
- Gabapentinoids were responsible for or contributed to the deaths of 367 people in Scotland in 2018, up 52% from the previous year. (25)
- Gabapentin became available as a generic drug in 2004.
- In 2002, 1.2% of people used gabapentin; this figure was 3.9% in 2015. There has been no significant rise in epilepsy or neuropathic pain (the two uses the drug is approved for) to explain this sharp increase. (26)
- Recent figures have shown that prescription rates for substances such as morphine, gabapentin and oxycodone have risen by 100%. (27)
Ready to Get Help for Your Addiction?
Admitting that there is a problem is widely dubbed as the first step towards recovery. The importance of this cannot be stressed enough. A person who has a positive, genuine attitude towards their recovery is much more likely to go through with quitting and maintain abstinence. If you feel like you are ready to make the effort to change, it is time to seek medical help.
Get Help Today
The real risks of gabapentin are only beginning to be understood. The seeming innocuousness of the substance should not put anyone off seeking treatment. The side effects, withdrawal symptoms and cravings are completely real, and medical attention is usually required to quit. Call UKAT on 0800 511 8111 to discuss how a bespoke treatment programme can help you to overcome addiction and change your life.
Sources
(2) https://www.nhs.uk/medicines/gabapentin/
(3) https://www.medicines.org.uk/emc/search?q=gabapentin
(4) https://www.chemistryworld.com/podcasts/gabapentin/1017577.article
(5) https://www.england.nhs.uk/wp-content/uploads/2019/03/pregabalin-and-gabapentin-guidance-v1.pdf
(6) https://www.gov.uk/government/news/pregabalin-and-gabapentin-to-be-controlled-as-class-c-drugs
(7) https://www.bbc.co.uk/news/uk-england-leeds-47737707
(8) https://www.gov.uk/penalties-drug-possession-dealing
(9) https://www.nhs.uk/common-health-questions/medicines/what-is-a-controlled-medicine-drug/
(10) https://pubchem.ncbi.nlm.nih.gov/compound/Gabapentin#section=3D-Conformer
(11) https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2442440/
(12) https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3404313/
(13) https://www.statnews.com/2017/07/06/gabapentin-becomes-target-of-opioid-abuse/
(14) https://www.empr.com/home/news/certain-factors-may-increase-the-likelihood-of-gabapentin-overuse/
(15) https://www.medicalnewstoday.com/articles/323467.php
(16) https://www.ncbi.nlm.nih.gov/pubmed/11882775
(17) https://www.healthline.com/health-news/gabapentin-latest-pain-medication-in-opioid-overdoses#1
(18) https://onlinelibrary.wiley.com/doi/full/10.1111/j.1556-4029.2011.01798.x
(20) https://www.ncbi.nlm.nih.gov/pubmed/15898970
(21) https://www.verywellmind.com/gabapentin-withdrawal-symptoms-timeline-and-treatment-4176217
(22) https://www.sps.nhs.uk/wp-content/uploads/2016/08/M-Protocol_for_Mgmt_of_pregab-gaba_Sussex.pdf
(23) https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2746426/
(24) https://www.ncbi.nlm.nih.gov/books/NBK64269/
(25) https://www.dailyrecord.co.uk/news/scottish-news/cheap-street-pills-help-turn-18326014
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