Pregabalin, what is it and what is it used for?

Treatment with pregabalin has demonstrated effectiveness in controlling neuropathic pain and improving patients’ quality of life. In this article we describe in detail its effects and mechanism of action.

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

At the moment, Neuropathic pain is one of the great challenges of pain units. This is due to its resistance to common analgesic treatments and the lack of knowledge associated with the causing pathologies. Let’s see, then, what pregabalin is, what it is used for, how it works and what its side effects may be.

What is pregabalin?

Pregabalin It 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 It is classified within neuromodulatory drugs. It arose from gabapentin, with a specific indication for peripheral neuropathic pain.

It is a drug with linear pharmacokinetics, which hardly varies individually. It is not bound to plasma proteins, is not metabolized in the kidney and is excreted in the urine. These characteristics mean that it has few interactions with other drugs..

The analgesic effects of pregabalin begin to appear in the first days of treatment and are maintained in the long term.

What is pregabalin used for?

Pregabalin, according to its technical data sheet, is indicated for the treatment of:

Neuropathic pain: Pregabalin is indicated for the treatment of 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: Pregabalin is also indicated in the treatment of generalized anxiety disorder or GAD in adults.

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Treatment with pregabalin has demonstrated efficacy compared to placebo, in a dose-dependent manner, because it controls pain, improves sleep and improves many of the quality of life parameters of patients with neuropathic pain. It is especially useful in the treatment of diabetic neuropathy or post-herpetic neuralgia:

Diabetic neuropathy: It is one of the nervous system disorders caused by diabetes.Post-herpetic neuropathy: It is a persistent neuropathic pain, located in the dermatome where an acute case of herpes zoster has previously occurred. We know that it lasts more than three months after the dermal lesions have disappeared.

Mechanism of action

Pregabalin is a ligand for an auxiliary subunit of voltage-gated calcium channels in the central nervous system, although its mechanism of action is not exactly known. Yesu analgesic effect to its ability to bind to this protein subunit, with greater affinity than gabapentin, another antiepileptic used for chronic neuropathic pain and fibromyalgia in adults. Therefore, their pharmacological profiles are similar.

By binding to this subunit, it modulates the entry of calcium ion through voltage-gated channels and, therefore, decreases the release of excitatory neurotransmitters such as glutamate, norepinephrine and substance P.

This translates into a decreased neuronal excitability of different areas of the nervous system; specifically, those related to pathologies with 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, nor does it affect its reuptake. Therefore, cannot develop GABAergic actions.

Side effects

The Most frequent adverse reactions in treatment with pregabalin They are, for example:

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Dizziness.Drowsiness.Headache.Nasopharyngitis.Increased appetite.Weight gain.Eauphoric mood.Confusion.Irritability. Disorientation. Insomnia.Decreased libido.Erectile dysfunction. Blurred vision. Diplopia.Vertigo.Gastrointestinal disorders.Muscle cramps.Back pain and pain in extremities.

Despite this list of possible side effects, it is worth saying that most of them are transient and well tolerated by patients. Treatment abandonment rates are minimal. Withdrawal symptoms have been observed in some patients after discontinuation of pregabalin treatment. For this, It is recommended to reduce the dose little by little to avoid possible complications.