Pregabalin: What Is It and What's It Used For?

Pregabalin is an antiepileptic drug that's also used to treat neuropathic pain caused by multiple diseases. Do you want to know what it's used for and how it works? Here we'll explain it to you.
Pregabalin: What Is It and What's It Used For?

Last update: 21 April, 2023

Antiepileptic drugs have been shown to be effective in treating a type of chronic pain called neuropathic pain. Drugs such as pregabalin are used throughout the world to improve both the physical and psychological components of this condition.

Neuropathic pain is a special type of pain that can occur as a result of damage to peripheral nerves or the central nervous system. It’s characterized by having an atypical presentation that lasts over time and doesn’t respond to traditional analgesics.

Various studies have shown that the most common forms of chronic pain are low back pain and neck pain. This condition is associated with the appearance of anxiety, sleep, and mood disorders. In this way, the importance of compounds capable of treating all aspects of the disease is highlighted.

What is pregabalin?

Pregabalin is a synthetic analog of gamma-aminobutyric acid (GABA), which means it has an effect similar to that of the acid in the body. GABA is a chemical substance that synthesizes the body and allows the transmission of signals from one neuron to another, thus making it being the inhibitory neurotransmitter par excellence.

The drug will inhibit the release of various neurotransmitters, thus managing to improve the clinical condition. In addition, pregabalin is a lipophilic compound, that is, it has an affinity for lipids, which facilitates its entry into the cell.

The form of administration is oral, which can vary between slow-release capsules, tablets, and solutions. The dosage is also very varied and goes from 25 milligrams to 300 milligrams of active principle.

Epileptic seizure in woman.
Pregabalin was first developed for epilepsy.

What is this drug used for?

This compound was created to be used to treat certain types of epilepsy in adults. Its greatest efficacy is in the context of treatments of partial seizures with or without secondary generalization. However, it must be used in conjunction with other medications.

Currently, pregabalin is the first-line treatment for neuropathic pain, both central and peripheral. Since 2004, the Food and Drugs Administration (FDA) has approved its use for diabetic neuropathy and postherpetic neuralgia.

The efficacy of the compound is demonstrated by studies that have revealed that pain reduces its intensity by 30% in 5 out of 10 patients with postherpetic neuralgia. In turn, the same analysis reveals that 3 out of 10 patients with the same pathology noted a decrease in pain equivalent to 50%.

On the other hand, pregabalin is also used in the treatment of generalized anxiety disorder (GAD). The psychiatric pathology in question is characterized by the presence of anxiety attacks and prolonged worry, difficult to control.

Mechanism of action of pregabalin

The drug has a mechanism of action similar to that of gabapentin. Both bind to the alpha-2-delta subunit of the type 1 receptor for voltage-gated calcium channels. The drugs exert their action on these channels by decreasing the entry of calcium to the nerve terminals.

By doing so, the release of vesicles with multiple neurotransmitters, such as glutamate, norepinephrine, and substance P, is prevented. The decrease in them is what causes the analgesic action.

In this sense, pregabalin decreases neuronal excitability, especially in areas of the brain with a large number of synapses. Despite having a similar mechanism of action, pregabalin’s binding to the receptor is up to 6 times greater than that of gabapentin.

How should you take this medicine?

The intake of this compound should be carried out under strict medical supervision. It should start with an approximate dose of 150 milligrams per day divided into 3 doses, which can be increased gradually according to the patient’s requirements.

The maximum recommended dose is 300 milligrams daily in all patients to avoid kidney disease. However, in certain cases, it’ll be necessary to administer 600 milligrams. In the case of slow-release tablets, a daily intake should be taken after dinner.

Discontinuation of pregabalin treatment shouldn’t be done immediately. This is in order to prevent an increase in the frequency of seizures in patients with epilepsy. In this sense, it’s recommended to gradually reduce the doses for at least a week.

Possible side effects of pregabalin

The consumption of this drug is safe in most cases, although it may produce some side effects that aren’t usually disabling. Studies have shown that the most frequent adverse reactions are dizziness and somnolence, with an incidence of 29% and 22% respectively.

According to the internal package insert, the following side effects may affect up to 1 in 10 people:

  • Increased appetite
  • Headaches
  • Changes in mood and attention
  • Dry mouth
  • Decreased libido
  • Muscle pains
Pregabalin for chronic hand pain.
Chronic pain is difficult to treat, which is why pregabalin stands out as a therapeutic option.

Warnings and contraindications of pregabalin

The only existing absolute contraindication regarding the intake of pregabalin is the presence of allergies to the active principle or to any of its components. In this case, it will be necessary to consult with the specialist and look for a new medication that doesn’t hold these risks.

On the other hand, there are medical conditions that can influence the action of the drug, which should be reported to the doctor before taking them. In this sense, the following stand out:

  • Pre-existing heart or kidney disease
  • Consumption of other medications: oxycodone or lorazepam
  • Gastrointestinal problems: such as constipation
  • History of alcoholism or abuse of other psychoactive substances
  • Pregnancy or lactation

Activities that require great concentration or effort, such as driving a car, shouldn’t be performed after taking pregabalin. This is because the state of consciousness could be altered, which increases the probability of having an accident.

An effective treatment for chronic pain

Pregabalin is one of the few drugs available with proven efficacy in the treatment of chronic pain. It mimics the function of GABA in the brain, depressing the nervous system. In this way, it has an analgesic effect and controls seizures.

This drug is capable of altering the state of consciousness and cause drowsiness, so its consumption should only be carried out under medical prescription and the corresponding indications must be followed.

  • Derry S, Bell R, Straube S, Wiffen PJ, Aldington D, Moore R. Pregabalin for neuropathic pain in adults. Cochrane Database of Systematic Reviews. 2019, Issue 1. Art. No.: CD007076.
  • Bansal A, Tewari A, Garg S, Gupta A. Eficacia analgésica y efectos adversos de la pregabalina.  Journal of Anaesthesiology Clinical Pharmacology 25(3):321-326.
  • Saldaña M, Navarro A, Rejas J et al. La pregabalina es un tratamiento eficaz de la lumbalgia y la cervicalgia. Rheumatol Int. 2010;30(8):1005-15.
  • González-Escalada J. Pregabalina en el tratamiento del dolor neuropático periférico. Rev. Soc. Esp. Dolor. 2005;12( 3 ): 169-180.
  • López-Trigo J, Sancho Rieger J. Pregabalina. Un nuevo tratamiento para el dolor neuropático. Neurología. 2006;21(2): 96-103.
  • Agencia Española de Medicamentos y Productos Sanitarios. Prospecto: información para el usuario. Pregabalina Aristo 75 mg cápsulas duras EFG. Documento online disponible en:

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