Pregabalin, What Is It And What Is It Used For?

Pregabalin has been shown to be effective in treating neuropathic pain by improving patients’ quality of life. In this article we describe in detail its effects and its mechanism of action.
Pregabalin, what is it and what is it used for?

The pregabalin , marketed under the name Lyrica, is an antiepileptic drug used to treat neuropathic pain in disorders such as diabetic neuropathy or postherpetic neuralgia.

Currently, neuropathic pain still represents a major challenge for pain units. This is due to the strong resistance to common analgesic treatments and the poor knowledge of the causative pathogens.

So let’s find out what pregabalin is, why it is used, how it works and what its side effects may be.

What is pregabalin?

Pregabalin is an analogue of gamma-aminobutyric acid or GABA. GABA is the main inhibitory neurotransmitter of the central nervous system and its function is to slow down brain activity. Although pregabalin is an antiepileptic drug, it is also classified within neuromodulatory drugs. It originated from gabapentin, with a specific indication for peripheral neuropathic pain.

It is a drug with linear pharmacokinetics, which barely varies from individual to individual. It does not bind to plasma proteins, is not metabolised in the kidneys or excreted in the urine. Precisely for these reasons it has very few characteristics in common with other similar drugs.

Pregabalin pills

What is pregabalin used for?

Pregabalin is used to treat:

  • Neuropathic pain: This drug is suitable for treating peripheral and central neuropathic pain in adults.
  • Epilepsy : Pregabalin is indicated in the combined treatment of partial seizures with or without secondary generalization in adults.
  • Generalized Anxiety Disorder: It is also used to treat generalized anxiety disorder, or GAD, in adults.
  • Pregabalin treatment has been shown to be effective in placebo, with a dose-dependent mechanism, as it controls pain and improves sleep, along with many other quality of life parameters for patients with neuropathic pain. It is particularly useful in the treatment of diabetic neuropathy or postherpetic neuralgia.
  • Diabetic Neuropathy: It is one of the disorders of the nervous system caused by diabetes.
  • Postherpetic neuralgia: this is a persistent neuropathic pain, localized in the dermatome in which an acute case of herpes zoster has previously occurred. We know it lasts more than three months after the dermal lesions disappear.

Mechanism of action

Pregabalin is highly bound to a unitary subunit of voltage-gated calcium channels in the central nervous system, however its mechanism of action is not precisely known. Its analgesic effect is linked to the ability to join this protein subunit, with greater affinity than gabapentin, another antiepileptic used for chronic neuropathic pain and fibromyalgia in adults. The two pharmacological profiles are therefore similar.

By joining this subunit, it modulates the entry of the calcium ion through voltage-gated channels and, therefore, reduces the release of excitatory neurotransmitters such as glutamate, noradrenaline and substance P.

This involves the reduction of neuronal excitability of different areas of the nervous system, in particular those related to pathologies of neuropathic pain, epilepsy or anxiety. Although it is an analogue of gamma-aminobutyric acid, or GABA, it does not interact with GABA-A or B receptors, and does not affect its reuptake. Therefore it cannot develop GABA actions.

Woman with sore neck

Side effects

Among the most frequent undesirable reactions in treatment with pregabalin are :

  • Nausea.
  • Drowsiness.
  • Headache.
  • Nasopharyngitis.
  • Increased appetite.
  • Euphoric state of mind.
  • Confusion.
  • Irritability.
  • Disorientation.
  • Insomnia.
  • Weight gain.
  • Drop in libido.
  • Erectile dysfunction.
  • Blurred view.
  • Diplopia.
  • Vertigo.
  • Gastrointestinal disorders.
  • Muscle cramps.
  • Pain in the back or extremities.

Regardless of the list of possible side effects, it should be noted that most of these are transient and well tolerated by patients. The cases of abandonment of the treatment are in fact minimal. Withdrawal symptoms have been observed in some patients after discontinuation of pregabalin treatment. It is therefore advisable to reduce the doses little by little to avoid possible complications.

Related Articles

Leave a Reply

Your email address will not be published. Required fields are marked *

Back to top button