Pregabalin is a painkiller for the management of epileptic seizures. This drug was invented by Richard Bruce Silverman with the help of Ryszard Andruszkiewicz at the University of Northwestern in the United States. Ryszard Andruszkiewicz is said to have developed a series of molecules for Silverman. In the innovation, they discovered molecules that could be transported to the brain.
The molecule has a specific shape that enables it to activate the enzyme L-glutamic acid decarboxylase. As a result, the molecule is ferried to the brain. The development targeted to increase the production of neurotransmitter gamma-aminobutyric acid (GABA). This is the primary neurotransmitter of the nervous system, and it works by inhibiting brain signals. Suppose these inhibitory effects are raised, then the result could be an effective treatment for convulsive attacks.
In 2004, the United States and the European Union approved this medication. Food and Drug Administration (FDA) approved the drug as an epileptic medication. According to the FDA provision, the drug is to be used as an anticonvulsant and analgesic and sold under Lyrica. During the approval of the extended-release formulation of Lyrica, specific uses of the drug were excluded. This included its therapeutic use for partial onset seizures or as add-on therapy or fibromyalgia.
How does Lyrica work?
The primary mechanism of the pregabalin tablets is still unknown. However, the drug is said to work by penetrating through blood-brain barriers, thereby increasing the levels of GABA. The mode of action is most likely due to events involving a receptor associated with an L-amino acid carrier protein.
Pregabalin is a gabapentinoid, which is a group of GABA derivatives or GABA analogues. These GABA analogues differ from the common psychoactive substance (benzodiazepines). Instead of binding to the GABA receptors, their mechanism of action takes the form of alpha-2-delta subunit of volta gated calcium channels.
However, the action of gabapentinoids cannot be solely attributed to the blocking of calcium channels (Chincholkar, 2018). As it also results from the depression of presynaptic excitory input onto dorsal horn neurons.
It occurs when the component interacts with alpha-2-delta subunits upregulated during injuries. They also control the inhibition of the forward trafficking of thrombospondin mediated processes and alpha-2-delta subunit 1, and the uptake of glutamate by excitory aminoacid transporters, among other mechanisms.
What is pregabalin used for?
FDA approved a diverse use of this medication in comparison with other drugs, and they include:
Neuropathic pain associated with diabetic peripheral neuropathy (DPN): in diabetes, peripheral neuropathy relates to the nerve pain associated with diabetes or excessively high sugar levels. The condition’s symptoms involve a loss of sensation or a feeling of numbness in the hands or feet.
Postherpetic neuralgia (PHN): it refers to the pain that follows infection by shingles or herpes zoster virus. The signs of shingles are blisters or a rash, which disappear, leaving a burning pain of PHN. The pain experienced is due to damage to the skin and nerve fibres.
Fibromyalgia: this is a medical condition that results from a stressful event of emotional or physical pain. Studies suggest that the disease causes widespread pain is amplified due to the brain’s and spinal cord’s interpretation of pain and non-pain signals.
Nerve pain associated with spinal cord injury: this kind of pain causes abnormal communication between the brain and nerves which is interpreted as pain. It can occur from damage to nerves resulting from injuries to the spinal cord.
Adjunctive therapy for treating partial-onset seizures (four and above year olds): Pregabalin is used to treat seizures localised to one area of the brain for persons aged four and above. The condition, also known as partial-onset seizures, occurs from a traumatic brain injury, among other causes.
Other benefits for this therapeutic include treatment of chronic lower back pain. This treatment is, however, unsubstantiated, and it could expose the patient to significant risks. Despite not being approved by the FDA, this off label use has benefited many.
Pregabalin tablets are also used to manage alcohol withdrawal and withdrawal of other narcotics. The evidence on this use is also limited. Again, this is another off the label use that has helped many people.
How do I take pregabalin?
This medication is not just for persons with epilepsy, as it is also used as an analgesic, and the full therapeutic outcome of using this medicine is felt after a few weeks.
For a normal treatment routine, the patient should take pregabalin medicine two or three times a day. Lyrica formulations are entirely for oral intake and are in liquid form, tablets and capsules.
The benefits should be weighed against the risks before the administration of the drug. Check out the medication instructions included in the package for guidance on the use. It is not recommended to take more than the recommended dosage. You should also not use the drug past the recommended period.
You can take the drug before or after meals. If you are using the oral drug solution, always use a marked measuring spoon for accuracy. Avoid using a household spoon as it may give wrong drug quantities.
The number of pregabalin tablets you take depends on the reason for use and how your body responds to the treatment. Important to note is that the amount of tablets you take also depends on the strength of the medicine in terms of the amount of active ingredients.
The use of too much of the active ingredients can lead to some side effects. As you continue overdosing on the medication, you develop a level of dependence and tolerance. However, the potential of abusing this gabapentinoid is lower when compared to other psychotic substances.
For oral solutions, capsules and tablets, the active ingredients come in varying strengths of 25mg to 300mg.
Does Pregabalin Help Anxiety?
Generalised anxiety disorder (GAD) is not easy to diagnose. It, therefore, cannot be treated based on evidence, and for these patients, the feeling of worry and anxiety are often out of proportion. In such cases, pregabalin tablets are used to treat GAD as off-label medication.
According to research findings:
- To manage the symptoms of this disorder, the patient needs to take fixed dosages of 200mg or more per day.
- The advantage of early onset of clinical effects is also supported by substantial evidence.
- The efficacy of pregabalin in clusters of psychological and somatic symptoms of anxiety is also supported by evidence.
- For prevention of the relapse of GAD symptoms, the recommended dose is 450mg a day.
- A recent profile of the side effects of pregabalin on healthy clinical trial patients suggests that the tablets have an advantage in tolerability compared with other psychoactive medications, benzodiazepines. This was of particular significance with a short term use of the drug.
The use of pregabalin for the first-line treatment of GAD is approved by the World Federation of Biological Psychiatry. All in all, pregabalin is not recommended for the treatment of GAD by FDA. However, experts across different regions still recommend its use in the management of GAD.
Never mix pregabalin and alcohol
Pregabalin affects the brain just like alcohol. The consequences of using both substances can be dire, as they cause an effect called a negative synergistic effect.
Additionally, using the two substances together can worsen any underlying medical condition. It is also important to note that the effectiveness of the medicine reduces when the patient uses alcohol.
Taking alcohol while on pregabalin can result in intense depression of the central nervous system which causes:
- Increased dizziness
- Higher levels of drowsiness
- Increase in concentration issues
Other side effects of using alcohol with Lyrica include:
- breathing problems,
- angioedema symptoms which involve swelling of the tongue, eyes and lips.
- Reduced alertness levels
The use of alcohol with medication is a common practice. This is according to substance abuse and Mental health SAMHS. These effects and their severity depend on the action of the drug.
Pragabalin side effects
Medications cause different side effects regardless of their uses. The severity of the side effects also varies and are often just an inconvenience.
The common side effect of using pregabalin involve the gastrointestinal system. The reason for this problem is usually due to the passage of the therapeutic ingredients into the body, and in other cases due to the chemical structure.
Natural ways for reducing these side effects include drinking plenty of water to hydrate the body and flush out the toxins associated with the medications. Exercising helps remove bacteria through the airways or lungs. Aerobic exercise, for instance, is known to reduce these adverse effects. Finally, you should take food in smaller amounts throughout the day.
Common pregabalin side effects
Drowsiness: after taking the medication, you are likely to experience feelings of tiredness and sleepiness during inappropriate times. This feeling can also be accompanied by weakness, fatigue and lack of mental alertness. If you experience these feelings resting would be helpful. You should also avoid engaging in activities that require alertness due to impaired mental cognition.
Blurred vision: this is the lack of sharp eyesight or vision of finer details. Sleep is helpful in recovering from these symptoms. In severe cases, you can use lubricating eye drops.
Dry mouth: this involves a feeling of lack of moisture in the mouth, and it occurs when salivary glands fail to produce sufficient amounts of saliva. Chewing sugarless gum will help you counter these effects. You can also take plenty of caffeine-free fluids or use certain alcohol-free mouthwashes.
Uncommon pregabalin side effects
These are other side effects that occur in one on hundred users of the medicine or one in a thousand population during the drug trials. These include:
Constipation: this refers to difficulties in passing stool and challenges in bowel movement. It is not often a cause to worry unless it persists for over three weeks or you start passing stool with blood. To take care of these symptoms, you should take plenty of water and foods high in fibre.
Muscle spasm: these are involuntary sudden muscle movements occurring in different parts of the body. It might, in some cases involve more than one muscle at a time. Mild exercising and stretching would be helpful in relieving mild muscle spasms. Also, to relieve these symptoms you can apply heat or ice to the affected muscles.
Increased hunger: the problem with frequent feelings of hunger can be addressed by taking foods rich in proteins and reducing high-calorie foods.
Rare side effects of pregabalin include wheezing, low blood sugar and hives. The side effects of using pregabalin can occur on their own or when used alongside other therapeutics such as other painkillers, tranquillizers, antihistamines and diabetes medications. Using these medications together can also worsen the side effects.