Pregabalin, also marketed as Lyrica, is an antiepileptic used to treat neuropathic pain in disorders such as diabetic neuropathy and postherpetic neuralgia.
Currently, neuropathic pain is one of the great challenges of health facilities, due to its resistance to the usual analgesic treatments and the disrecognise associated with causal pathologies.
So, let’s see what pregabalin is, what it’s used for, how it works, and what its side effects may be.
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 calm brain activity.
Although pregabalin is an antiphylactic drug, it is also classified as a neuromodulatory drug and comes from gabapentin, with a specific indication of peripheral neuropathic pain.
It is a drug with a linear pharmacokinetics, which does not vary only individually, does not join plasma proteins, is not metabolized in the kidneys and is excreted in the urine, characteristics that cause it to have little interaction with other drugs.
The analgesic effects of pregabalin begin to develop in the first few days of treatment and continue in the long term.
Pregabalin, according to its data sheet, is indicated for the treatment of:
Treatment with pregabalin has been shown to be effective compared to placebo, thanks to an independent dose, as it controls pain, improves sleep and improves many parameters of the quality of life of patients with neuropathic pain.
It is particularly useful in the treatment of diabetic neuropathy and postherpetic neuralgia.
Pregabalin is a link of an auxiliary subunit of voltage-dependent calcium channels in the central nervous system, although its exact mechanism of action is unknown.
Its analgesic effect is due to its ability to bind to this protein subunit, with greater affinity than gabapentin, another antipiletic used for chronic neuropathic pain and fibromyalgia in adults, so its pharmacological profiles are similar.
By joining this subunit, it modulates the entry of calcium ions through voltage-dependent channels and therefore decreases the release of exquisite neurotransmitters such as glutamate, norepinephrine and substance P.
This results in a decrease in neuronal excitability in different areas of the nervous system, especially those related to pathologies such as 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 their absorption, so it cannot develop gabaergic actions.
The most common side effects of pregabalin treatment are
Despite this list of possible side effects, it should be noted that most of them are transient and well tolerated by patients. Discontinuation rates are minimal.
Withdrawal symptoms have been observed in some patients after discontinuation of pregabalin treatment, so it is recommended to reduce the dose gradually to avoid possible complications.