What is Pregabalin?

Pregabalin (Lyrica) is a painkiller and was identified by the chemist, Richard Bruce Silverman at the Northwestern University (United States of America) for the management of epileptic seizures. With assistance from Ryszard Andruszkiewicz, who was known to develop a series of molecules for Silverman, a molecule was found which could be transported to the brain.

Through its shape, this molecule could activate the enzyme, L-glutamic acid decarboxylase, subsequently to being transported to the brain. The intention of this development was for the increased production of the neurotransmitter, gamma-amino butyric acid (GABA). GABA, being the main neurotransmitter of the nervous system, inhibits brain signals. If the inhibitory effects of this neurotransmitter could be raised, this could be a possible treatment of convulsive attacks.

This medication was approved in the European Union (E.U) and United States (U.S) in 2004. Food and Drug Administration (FDA) approval was for the use of the epileptic medicine to be used as an anticonvulsant and analgesic and marketed this therapeutic as the brand, Lyrica. When the extended-release formulation of Lyrica was approved by the FDA, its therapeutic use for fibromyalgia or partial onset seizures (as an add-on therapy) were excluded.

How Does Lyrica Work?

The primary mechanism of action is yet to be defined but pregabalin tablets are thought to readily penetrate blood-brain barriers and increase the concentration of GABA. The mode of action is most likely modulated through events which involve a receptor associated with an L-amino acid carrier protein.

Pregabalin falls into the class of gabapentinoids. These are derivatives of GABA making them GABA analogues. Unlike the popular class of psychoactive substances, benzodiazepines, these GABA analogues do not bind to GABA receptors. Instead the mechanism of action of these anti-epileptic medicines involves the alpha-2-delta subunit of the voltage gated calcium channels.

The actions of gabapentinoids, however, cannot be solely attributed to the blocking of calcium channels (Chincholkar, 2018). Analgesic action can be attributed to the depression of presynaptic excitory input onto dorsal horn neurons.

This occurs through the interaction with alpha-2-delta subunits which are upregulated following an injury. They regulate the inhibition of forward trafficking of the alpha-2-delta subunit 1 and thrombospondin mediated processes. Gabapentinoids also stimulate the uptake of glutamate by excitory amino acid transporters (EEATs). This is in addition to other mechanisms.

What is Pregabalin Used For?

Compared to other medications, the FDA-approved uses of pregabalin tablets are relatively diverse:

• Neuropathic pain associated with diabetic peripheral neuropathy (DPN): peripheral neuropathy in diabetes relates to the nerve pain associated with chronic levels of high blood sugar and diabetes. The symptoms often present themselves in the hands or feet and often feel like numbness or a loss of sensation.
• Postherpetic neuralgia (PHN): PHN is the lingering pain consequently following an infection by the herpes zoster virus (shingles). Shingles are noticeable through a rash or blisters. After these stages of the infection disappear, PHN remains as a burning pain which is a result of damage to the nerve fibres and skin.
• Fibromyalgia: this medical condition can appear through a stressful or unfortunate event of physical and/or emotional pain. It is characterized through widespread pain which research suggests are amplified by the manner in which the brain and spinal cord interpret pain or non-pain signals.
• Nerve pain (associated with spinal cord injury): abnormal communication between nerves and the brain can be interpreted as pain. This can arise from nerve damage due to an injury of the spinal cord.
• Adjunctive therapy for the treatment of partial onset seizures (4 years or older): for those above the age of 4 years, seizures localised to one area of the brain can be treated with pregabalin. This condition is known as partial onset seizures and can be caused by a traumatic brain injury or other reasons.

Additional benefits of this therapeutic can include the treatment of lower back pain in chronic patients. There is, however, no extensive evidence for this purpose and the risks may also be significant. This is not an FDA-approved use, but an off-label use, which has - nonetheless - benefited many.

Alcohol withdrawal or withdrawal from certain narcotics may also be managed using pregabalin tablets. Again, the evidence related to this use is limited, though many people continue to benefit off-label as per medical surveys.

How do I take Pregabalin?

You do not have to suffer from epilepsy to use pregabalin tablets. It can be used as an analgesic as well. The therapeutic benefits often take a few weeks to come into full effect. The normal treatment routine involves using this medication twice or three times a day.

The formulations of Lyrica are for oral consumption - they come in the form of capsules, tablets or as a liquid solution.

Before using the medication, the benefits should be assessed in relation to the risks. This can be done by following the information on the medication guide, which is included in the packaging. You should not use more than what is recommended, use the medication for longer than cautioned or more often than advised.

It may be administered before or after a meal and oral solution should be measured out using a marked measuring spoon. A standard household spoon may measure out an inaccurate amount of medicine.

Does Pregabalin Help Anxiety?

Generalised anxiety disorder (GAD) is often difficult to recognise or treat in an evidence-based manner. It is the worrying or feelings of anxiety which are often out of proportion to the impacts of the related events.

Pregabalin tablets can be used off-label for the treatment of GAD. Research shows:

• At a 200 mg/day (or more) fixed dosage, there is efficient management of the symptoms of this anxiety disorder
• There is some evidence of the advantage of an early onset of clinical effect
• There is some evidence of efficacy in clusters of somatic and psychological symptoms of anxiety
• A dose of 450 mg/day can effectively prevent the relapse of GAD symptoms
• A current profile of the side effects in healthy clinical trial patients suggests that pregabalin tablets may have an advantage in tolerability over the psychoactive medications, benzodiazepines. This was of special significance when the medication was used in the short-term.

The World Federation of Biological Psychiatry approves of this medication as a first-line treatment of GAD. This pharmaceutical is not approved for this specific intent by the FDA, but continues to be recommended by experts and used by patients across different regions.

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Updated: 27th January 2021
Review Due: January 2022