Pregabalin Anticonvulsant And Analgesic CAS:148553-50-8
Pregabalin is a medication that is readily prescribed across the UK. Due to its anticonvulsant and analgesic properties, it is primarily used to manage symptoms of anxiety and epilepsy. Between 2021 and 2022, 8.4 million prescriptions for pregabalin were dispensed to members of the public in England.Whilst pregabalin is a prescribed – and therefore, for the most part, a controlled drug – it does still carry substantial risk. Concerns surrounding the misuse of pregabalin arose in 2014 following a report from Public Health England, which advises prescribers that whilst the drug has a ‘well-defined role in the management of a number of long-term conditions,’ pregabalin ‘can lead to dependence and may be misused or diverted.’If you or a loved one are prescribed pregabalin, it is important to learn how the substance acts upon the body and the brain. By informing ourselves of the mechanisms of the medicines we take, we can safeguard ourselves from their potential risks.
Why is pregabalin prescribed?
Pregabalin has a range of properties; it acts as an analgesic, an anxiolytic and an anticonvulsant.
●Analgesics are used to manage nerve pain
●Anxiolytics are used to manage anxiety
●Anticonvulsants are used to manage seizures
For this reason, pregabalin is typically prescribed to individuals with an anxiety disorder, a pain condition or a diagnosis of epilepsy.
Pregabalin can be prescribed in capsule, tablet or liquid form. It is usually taken several times a day.
Pregabalin: The chemistry
Pregabalin is a multifaceted substance that acts on the brain in several ways in order to achieve varying effects.
Pregabalin is a GABA analogue (a gamma-aminobutyric acid analogue). Gamma-aminobutyric acid is a neurotransmitter in the brain that sends specific messages. The role of GABA is to help the brain to achieve balance. It does that by ensuring specific neurons aren't becoming overactive.
If we have too much activity in certain areas of the brain, it can lead to feelings of panic and high blood pressure and can even cause seizures. Research has shown that anxiety, pain and symptoms of epilepsy can be managed through the decreasing of GABA levels in the brain. GABA controls these symptoms by calming the neurons in the brain, effectively getting them to stop overworking. Because it acts in this way, GABA is known as an inhibitory neurotransmitter.
Pregabalin is a GABA analogue. This means that it helps to increase the level of GABA in the brain, therefore reducing the activity of nerves in an excited state.
Analgesic effects
To control nerve pain, pregabalin effectively 'blocks' pain messages. It does this by restricting the movement of messages travelling between the brain and the spine.
The brain and the spine comprise one of the body's most complex systems: the central nervous system. The central nervous system is the 'hub' of the body. To and from here, messages are sent and received to allow us to interact and perceive our bodies and the world around us.
These messages are triggered through the release and movement of neurotransmitters (like GABA). It is also how we perceive pain.
By blocking a part of the 'complex circuitry underlying pain,' pregabalin can reduce the intensity and frequency of chronic pain for users.
Anxiolytic effects
Pregabalin works as a treatment for anxiety as it reduces the amount of 'nervous' chemicals the brain releases. One of the neurotransmitters linked with anxiety is glutamate. Glutamate plays an important role in the body, but as it is an excitatory chemical, too much of it can mimic symptoms of panic and high stress.
Pregabalin can work through the binding of 'over-excited presynaptic neurons', reducing the amount of neurotransmitters released. With the level of neurotransmitter activity falling back within a typical level, feelings of anxiety can be reduced.
This means that pregabalin is a common treatment for Generalised Anxiety Disorder (GAD).
Anticonvulsant effects
For seizures, pregabalin aids patients by reducing the electrical activity in the brain to a safer level. Studies found that 'suppression of seizure activity could be demonstrated as early as day 2'; however, the NHS states that it can take several weeks for the drug to start working.
Pregabalin use in addiction treatment
In some circumstances, pregabalin itself is used to help treat addiction, particularly in cases of heroin or alcohol addiction. However, as pregabalin is itself an addictive agent, the decision to do so is made with great caution.
Pregabalin: What are the side effects?
Most substances have side effects. Some side effects are more common than others. With prescribed medications such as pregabalin, you will be provided with an information sheet listing potential side effects. You will also be given the opportunity to speak to your primary clinician about these before beginning the course of medication.
Potential side effects of pregabalin include:
●Nausea and sickness
●Diarrhoea and stomach upset
●Headaches
●Increase in appetite
●Change in blood sugar levels
●Blurred vision
●Swelling in the limbs
●Sexual dysfunction
How Addictive is Pregabalin?
A report by Public Health England urged clinicians to be aware of pregabalin's 'propensity for misuse.'
It is thought that pregabalin's ability to produce euphoria – a common characteristic of addictive substances – plays a role in its misuse. Pregabalin also has a range of other psychological effects, including:
●increased confidence
●increased desire to socialise
●promoting relaxation
●soothing anxiety
Pregabalin, therefore, largely creates positive feelings in users. This is positive in some circumstances, for example, in the treatment of anxiety, but can be dangerous in others. This is because the euphoric and relaxing effects of pregabalin can become addictive.
Polydrug use
Pregabalin can be especially addictive if it is involved in polydrug use. Polydrug use is when an individual uses more than one substance (illicit or otherwise) alongside one another.
Pregabalin's addictive qualities can be heightened if used alongside other substances that work on the central nervous system, including fellow analgesic heroin.
Dosage for pregabalin
Trends in pregabalin misuse suggest that users take anywhere between 200 mg and 5 mg of pregabalin per day. In contrast, prescriptions for pregabalin do not tend to exceed more than 600mg a day (divided into 2 or 3 doses). This suggests that some users could be taking more than five times the suggested upper limit of pregabalin in a single use.
The source
Another potential factor in pregabalin addiction is the mode through which you obtain the substance. If you are accessing pregabalin through a GP or other clinician, your usage will be monitored via check-ups. You will also have limited access to the substance, as you will only be prescribed the amount deemed appropriate by a medical practitioner.
In theory, this suggests that pregabalin use is more controlled when it is prescribed. But that does not mean that people do not develop prescription drug addiction, as we know that is not the case.
An additional protective factor surrounding prescription is that substances accessed through clinical channels adhere to pharmaceutical regulations. When purchasing pregabalin from other sources, it is not possible to identify exactly what is inside the substance you are using.
This adds additional layers of threat for several reasons:
●it is impossible to know the strength of the drug you are using
●is it impossible to know how the drug you are using will interact with other substances
● it is impossible to know if the substance has been 'cut' with something more addictive and/or toxic
This, in turn, heightens the potential overdose risk of pregabalin.
Clinical Data
|
Trade Names |
Lyrica,3-isobutyl GABA, (S)-3-isobutyl-γ-aminobutyric acid |
|
CAS |
148553-50-8 |
|
Molar mass |
159.229 |
|
Formula |
C8H17NO2 |
|
Purity |
Above 98% |
|
Apprarance |
White crystalline powder |
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Signs of pregabalin addiction
It can be difficult to spot an addiction. This is potentially due to misconceptions in the media about what addiction 'looks like.' Culturally, our understanding of addiction may be coloured by stereotypes. These stereotypes are dangerous as they can weaken our knowledge of addiction rather than clarify it.
One of these stereotypes is that addiction is something that happens when someone becomes dependent on an illegal substance. This is not true. It is possible to become addicted to a range of substances; both those that are available illicitly and those that are legally purchased and prescribed.
Pregabalin is an example of this. It may be harder to spot an addiction to prescription medications as individuals experiencing this type of addiction may not necessarily show the typical signs of recreational use. Addiction to prescription medication can, therefore, risk falling under the radar.
Signs of pregabalin addiction can fall into physical, behavioural and psychological categories.
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