Also known as
Horizant, neurontin, bud, bud lite, gabaGamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in your brain, meaning it slows your brain's functions. GABA is known for producing a calming effect., gabby, gabbies, lyrica, nerontin
Classification
Depressant, analgesicpain relieving
Overview
Gabapentin is a prescription medicine used to treat a variety of conditions including epilepsy, neuropathic painpain caused by damage to the nerves. More (pain related to problems with nerve signals) and anxiety disorders.
Some people use gabapentin recreationally and consequently there is an illicit trade in this drug, including through online pharmacies 1.
What does it look like?
Gabapentin comes as white, yellow or orange tablets/capsules. They are normally swallowed, although powder from capsules may be snorted 1.
Source
There has been an increase in the prescribing and use of this drug over the last five years, and with a growing black market of this drug being available without prescriptions through online suppliers 2.
Why take it?
Sought after effects
Undesired effects
- drowsiness,
- sedationthe state of being relaxed or sleepy because of a drug More,
- respiratory depressionslowing the drive and effectiveness of breathing More,
- death 3,
- vomiting,
- nausea,
- flatulenceexcessive wind, also known as 'farts',
- constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More or diarrhoeaWhere you frequently pass watery or loose faeces,
- poor muscle control,
- visual disturbances 2.
How long do its effects last?
Onset of effects
Duration of effects
Pharmacology
Gabapentin modulates the action of glutamate decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in GABAGamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in your brain, meaning it slows your brain's functions. GABA is known for producing a calming effect. biosynthesis. In human and rat studies, gabapentin was found to increase GABAGamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in your brain, meaning it slows your brain's functions. GABA is known for producing a calming effect. biosynthesis, and to increase non-synaptic GABAGamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in your brain, meaning it slows your brain's functions. GABA is known for producing a calming effect. neurotransmission in vitro 6. As the GABAGamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in your brain, meaning it slows your brain's functions. GABA is known for producing a calming effect. system is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of gabapentin on the nervous system.
Gabapentin has also been shown to bind to the α2δ-1 subunit of voltage-gated calcium ion channels which contributes to its analgesicpain relieving effects. It is uncertain how this contributes to gabapentin’s psychoactive effects 4.
Bioavailability
The bioavailability of gabapentin is relatively low and is inversely proportional to the dose. This means that higher doses have lower biovailability than lower doses. The bioavailability of gabapentin is approximately 60%, 47%, 34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day 4.
Half-life
Five to seven hours 7.
Lethal dosage
People who accidentally or intentionally overdose may experience drowsiness, sedationthe state of being relaxed or sleepy because of a drug More, blurred vision, slurred speech, somnolenceis a state of near-sleep, a strong desire for sleep, or sleeping for unusually long periods. More and possibly death (if a very high amount was taken and particularly if combined with alcohol). Serum gabapentin concentrations may be measured to confirm diagnosis 8, 4.
A lethal dose of gabapentin was not identified in mice and rats receiving single oral doses as high as 8000 mg/kg. Signs of acute toxicityThis is when too much of something is taken over a short period of time More in animals included ataxialoss of motor coordination More, laboured breathing, ptosis, sedationthe state of being relaxed or sleepy because of a drug More, hypoactivity, or excitation.
Acute oral overdoses of neurontin up to 49 grams have been reported. In these cases, double vision, slurred speech, drowsiness, lethargy and diarrhoeaWhere you frequently pass watery or loose faeces, were observed. All patients recovered with supportive care 9.
Toxicity
Gabapentin has a low toxicityThis is when too much of something is taken over a short period of time More relative to dose 4. Gabapentin should be used carefully in patients with renal impairment due to possible accumulation and toxicityThis is when too much of something is taken over a short period of time More 9.
Tolerance
Gabapentin is not considered psychologically addictive. However, it is possible to develop a physical dependence on the drug. In fact, people can experience withdrawal symptoms for up to 45 days after they stop taking gabapentin. Although gabapentin does give some people a euphoric ‘high’ which can cause abuse, gabapentin abusers do not present with the kind of compulsive, drug-seeking behaviour or strong cravings associated with other more common depressants such as opioids, alcohol or benzodiazepines.
Tolerancethis is the process by which the receptors in your brain become habituated to the action of a drug. When tolerance is reached, more of the drug is required to achieve the same effect. With benzodiazepines, and probably with many other classes of drugs as well, tolerance is virtually always associated with some degree of physical dependence. If you find that you are experiencing tolerance, this is a clear warning sign that you may have formed a dependence. More will develop to the anxiolyticDrugs that relieve medically-diagnosed anxiety. More effects with prolonged continous usage. After cessation, the tolerancethis is the process by which the receptors in your brain become habituated to the action of a drug. When tolerance is reached, more of the drug is required to achieve the same effect. With benzodiazepines, and probably with many other classes of drugs as well, tolerance is virtually always associated with some degree of physical dependence. If you find that you are experiencing tolerance, this is a clear warning sign that you may have formed a dependence. More returns to baseline in 7 – 14 days. Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction 4.
Mode of use
Gabapentin capsules and tablets are normally swallowed, but there have been reports of the powder from gabapentin capsules being snorted 10.
Effects
Rarely
- hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind,
- suicidal thoughts,
- jaundiceyellowing of your skin or the whites of your eyes 10.
Physical effects
- muscle relaxation,
- physical euphoriaan intense feeling of pleasure and well-being More,
- pain relief,
- perception of decreased weight,
- sedationthe state of being relaxed or sleepy because of a drug More,
- seizure suppression,
- dizziness 4.
Cognitive effects
- cognitive euphoriastate of intense well-being, happiness, and excitement More,
- depersonalisationfeeling detached from yourself, observing yourself and your feelings and thoughts as if they belong to someone else More,
- derealisationan alteration in the perception or experience of the external world so that it seems unreal. More,
- dream potentiationcan be described as a cognitive component which increases the intensity, vividness and frequency of sleeping dream states. This effect also creates higher detail and definition within dreams alongside of an increase in the likelihood of one's dreams becoming lucid. More,
- amnesiainability to remember,
- anxiety suppression,
- decreased libido,
- emotion suppression,
- thought deceleration 4.
Visual effects
- visual disconnection,
- internal hallucinationsbest described as the perception of imagery and scenes which are experienced exclusively within a layer in front of one's open or closed eye vision and not seamlessly within the external environment around oneself. At lower levels, internal hallucinations begin with imagery which does not take up the entirety of one's visual field and is distinctively separate from its background. These can be described as spontaneous moving or still images of scenes, concepts, places, and anything one could imagine. They are manifested in varying levels of detail, ranging from ill-defined and cartoon-like in nature to completely realistic and beyond realism through seemingly impossible, non-euclidean geometric forms. They rarely hold their form for more than a few seconds before fading or shifting into another image. More 4.
Side-effects
- swollen hands and feet,
- headaches,
- abnormal thoughts,
- suicidal thoughts,
- shortness of breath,
- chest pain,
- mouth sores,
- chills,
- nausea,
- coughing,
- tremor,
- cold symptoms 2,
- drowsiness,
- weakness,
- dizziness,
- shaking in one part of the body,
- blurry or doubled vision,
- unsteadiness,
- anxiety,
- difficulty with memory,
- uncontrolled eye movement,
- vomiting,
- heartburn,
- diarrhoeaWhere you frequently pass watery or loose faeces,
- dry mouth,
- constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More,
- increased appetite,
- weight gain,
- back or joint painJoint pain is unpleasant and difficult to deal with, in addition to the other effects of drug abuse on your body. Intravenous drug users in particular are at an increased risk for joint damage. More,
- fever,
- ear pain,
- red, itchy eyes 7.
- dizziness,
- drowsiness,
- dry mouth,
- blurred vision,
- headache,
- diarrhoeaWhere you frequently pass watery or loose faeces,
- oedemathe medical term for fluid retention in the body. Oedema often causes swelling in the feet and ankles. More 11,
- constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More,
- nausea,
- vomiting,
- tremors,
- flatulenceexcessive wind, also known as 'farts',
- increases in blood pressure,
- trouble sleeping,
- weight gain,
- feelings of depression, hostility and anxiety 10.
Overdose
Allergic reaction
- increased seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More,
- fever,
- swollen glands,
- body aches,
- flu-like symptoms,
- skin rash,
- easy bruising or bleeding,
- severe tingling, numbness, pain, or muscle weakness,
- upper stomach pain,
- loss of appetite,
- dark urine,
- jaundiceyellowing of your skin or the whites of your eyes,
- chest pain,
- irregular heart rhythm,
- short of breath,
- confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation,
- nausea and vomiting,
- swelling,
- rapid weight gain,
- change in urination,
- new or worsening cough,
- fever,
- trouble breathing,
- rapid back and forth movement of your eyes,
- severe skin reaction 11.
Risks
Short-term
- drowsiness,
- unsteadiness,
- loss of coordination,
- clumsiness,
- vision disturbances 2.
Long-term
- insomniadifficulty in going to sleep or in getting enough sleep,
- weight gain,
- dependence,
- hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind,
- heart problems – including heart failure,
- depression,
- agitation
- panic attacks 2.
Purity
It’s likely that most of the gabapentin that is available on the black market has been either stolen from a hospital or pharmacy or stolen (possibly bought) from people who have been prescribed gabapentin. They might have also been imported from abroad.
You cannot normally be sure of the purity unless you are certain that the drug you have is a genuine pharmacy medicine 10.
Addiction
Dangerous interactions
Gabapentin significantly potentates the effects of alcohol, benzodiazepines and other GABAgenics which may lead to blackouts 4.
Withdrawal
Harm Reduction
- do not take the drug in higher doses, more frequent doses, or for longer than you were prescribed to do so by a doctor,
- do not stop taking gabapentin suddenly. Unless you are experiencing extreme side-effects caused by the drug, you must talk to your doctor before you stop taking it. Stopping the medication suddenly can lead to ‘withdrawal symptoms such as anxiety, difficulty falling asleep or staying asleep, nausea, pain, and sweating’,
- let your doctor know if you have any history of drug abuse before you start your gabapentin regimen. If you are taking the drug as part of a treatment program for addiction, make sure you attend therapy sessions and discuss your treatment needs with your doctor on a regular basis 12.
Legality
Gabapentin is a prescription only medicines and can only be prescribed following a consultation with a doctor.
In January 2016, the ACMDUK Advisory Council on the Misuse of Drugs. More recommended that gabapentin should be controlled under the Misuse of Drugs Act 1971 as Class C substances 1.
Did you know?
- Like drinking and driving, driving while under the influence of drugs is illegal – with some drugs you can still be unfit to drive the day after using. You can get a heavy fine, be disqualified from driving or even go to prison 10.
Paraphernalia
If the drug is snorted/sniffed – a razor blade will be used to chop it into lines on a hard level surface such as a mirror or a sheet of glass or a tile 2.
Footnotes:
Gabapentin, 2017, http://www.drugwise.org.uk/gabapentin/
Gabapentin, 2015, http://www.dan247.org.uk/Drug_Gabapentin.asp
Advice for prescribers on the risk of the misuse of pregabalin and gabapentin, 2014, https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/385791/PHE-NHS_England_pregabalin_and_gabapentin_advice_Dec_2014.pdf
Gabapentin, 2017, http://psychonautwiki.org/wiki/Gabapentin
Gabapentin, 2017, http://drugs.tripsit.me/gabapentin
Taylor, C. P., Mechanisms of action of gabapentin, Revue Neurologique (Paris), 1997, S39-S45, https://www.ncbi.nlm.nih.gov/pubmed/9686247
Gabapentin: Withdrawal Symptoms, Abuse & Use in Drug & Alcohol Detox, 2017, http://americanaddictioncenters.org/addiction-medications/gabapentin/
Baselt, R. C., Disposition of Toxiccapable of causing injury or death Drugs and Chemicals in Man, 2008, 8th edition, Biomedical Publications, Foster City, CA, ISBN: 978-0-9626523-7-0, 677-678
Highlights Of Prescribing Information, Pfizer, 2014, http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020235s057020882s041021129s039lbl.pdf
Gabapentin, 2015, http://www.talktofrank.com/drug/gabapentin
Horizant: Reviews, Side Effects, Uses, Dosage and Directions, 2017, http://addictionlibrary.org/prescription/horizant-reviews-side-effects-uses-dosage-and-directions.html
Gabapentin abuse, 2016, https://www.addictions.com/gabapentin-abuse/