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.
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.
Compared to other medications, the FDA-approved uses of pregabalin tablets are relatively diverse:
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.
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.
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:
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.
Check out the following link for more information about painkillers - or read more in the blogs below!
Updated: 27th January 2021
Review Due: January 2022
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