The Benefits and Side Effects of Treatment with Pregabalin

September 8, 2019
Have you ever heard of pregabalin? In this article, we'll tell you all about it and how it works.

Treatment with pregabalin has proven to be effective in controlling neuropathic pain and improving a patient’s quality of life. In this article, we describe its effects in detail.

Pregabalin, also marketed as Lyrica, is an antiepileptic medication used for the treatment of neuropathic pain in disorders caused by disorders such as diabetic neuropathy or post-herpetic neuralgia.

Currently, neuropathic pain is one of the great medical challenges. This is due to its resistance to common analgesic treatments, and our lack of knowledge about its causative pathologies.

What’s pregabalin?

Pregabalin is an analog of gamma-aminobutyric acid or GABA. GABA is the main inhibitory neurotransmitter in our central nervous system and its function is to slow down brain activity. Although pregabalin is an antiepileptic drug, scientists also classify it within the area of neuromodulatory drugs. It arose from gabapentin and was specifically indicated for peripheral neuropathic pain.

It’s a drug with linear pharmacokinetics, which doesn’t vary just individually. It doesn’t bind to plasma proteins, isn’t metabolized in the kidneys, and our bodies excrete it through urine. These characteristics mean that it has few interactions with other drugs.

The analgesic properties of pregabalin begin to take effect in the first days of treatment and remain long term.

Some white and red capsules.

Treatment with pregabalin

Pregabalin is used for the treatment of:

  • Neuropathic pain. Doctors recommend pregabalin for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy. Doctors prescribe pregabalin in the combined treatment of partial seizures, with or without secondary generalization, in adults.
  • Generalized anxiety disorder. Pregabalin is also used in the treatment of generalized anxiety disorder (GAD) in adults.

Pregabalin treatment has been shown to be effective in placebo-controlled studies, in a dose-dependent manner. This is because it controls pain, improves sleep, and improves the quality of life of patients with neuropathic pain in many different ways. It’s especially useful in the treatment of diabetic neuropathy or post-herpetic neuralgia.

  • Diabetic neuropathy. This is a nervous system disorder caused by diabetes.
  • Post-herpetic neuropathy. This a persistent neuropathic pain, located in the dermatome, where an acute case of shingles has previously occurred. We know that it lasts more than three months after the skin lesions have disappeared.

How does it work?

Pregabalin is a ligand of an auxiliary subunit of the voltage-dependent calcium channels in the central nervous system. However, scientists don’t understand exactly how it works and interacts.

Its analgesic effect is due to its ability to bind to this protein subunit better than gabapentin – another antiepileptic used for chronic neuropathic pain and fibromyalgia in adults. Therefore, their pharmacological profiles are similar.

By joining this subunit, it modulates how the calcium ion enters the voltage-dependent channels and, as a result, decreases the release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P.

This decreases neuronal excitability in the different areas of the nervous system. This is especially the case in those related to pathologies with neuropathic pain, epilepsy, or anxiety. Although it’s an analog of gamma-aminobutyric acid (GABA), it doesn’t interact with the GABA-A or B receptors, nor does it affect its reuptake. Because of that, it can’t develop gamma-aminobutyric actions.

A woman with back pain.

Side effects

The most frequent adverse reactions in treatment with pregabalin are:

  • Dizziness
  • Drowsiness
  • Headaches
  • Nasopharyngitis
  • Increased appetite
  • Weight gain
  • Euphoric mood
  • Confusion
  • Irritability
  • Disorientation
  • Insomnia
  • Decreased libido
  • Erectile dysfunction
  • Blurry vision
  • Diplopia
  • Vertigo
  • Gastrointestinal disorders
  • Muscle cramps
  • Back pain and limb pain

Despite this list of possible side effects, we should point out that most of them are transient and well tolerated by patients. Treatment abandonment rates are minimal. In some patients, withdrawal symptoms have been observed after discontinuing pregabalin treatment. For this reason, doctors recommend that patients decrease the dosage little by little in order to avoid possible complications.

  • Agencia Española de Medicamentos y Productos sanitarios (20187). Ficha técnica. Lyrica. [Online] Disponible en: https://cima.aemps.es/cima/pdfs/ft/04279003/FT_04279003.pdf
  • González-Escalada, J. R. (2005). Pregabalina en el tratamiento del dolor neuropático periférico. Revista de la Sociedad Española del Dolor12(3), 169-180.
  • López-Trigo, J., & Sancho Rieger, J. (2006). Pregabalina. Un nuevo tratamiento para el dolor neuropático. Neurología21(2), 96-103.