How Does Pregabalin Work?

In the human body Pregabalin works to resolve pain by targeting neurons. Pregabalin binds to P/Q-type voltage gated calcium channels in the central nervous system. P/Q-type voltage gated calcium channels are responsible for mediating certain kinds of neuronal activity. Pregabalin’s binding to these channels decreases neuron excitability and eases pain signals from traveling through the nervous system.

The Difference Between Gabapentin, Carbamazepine & Pregabalin

The mechanism of action for Pregabalin is still under investigation, but it has been shown that Pregabalin has better efficacy than other antiepileptic drugs such as Gabapentin and Carbamazepine (Tegretol). With Pregabalin there was less drug resistance over time, higher rates of remission, and Pregabalin also resulted in lower rates of suicide compared to the other drugs. Pregabalin is a newer drug that is being used as a first line treatment for neuropathic pain, but there has been some challenges with Pregabalin due to the fact that it can cause dry mouth and/or somnolence.

In addition Pregabalin level checks have shown Pregabalin levels increased from off label use for Fibromyalgia, so Pregabalin may not be as effective over time if used beyond its FDA approved uses. On the bright side Pregabalin’s effect on P/Q-type voltage gated calcium channels appears to be more specific than Carbamazepine’s effect on voltage gated sodium channels, so Pregabalin is showing more promising results than Carbamazepine in specific kinds of pain.

Is Pregabalin Safe?

So far Pregabalin has been given to over 5 million people and there have been no significant adverse reactions so Pregabalin’s long term effects on the body are still under investigation. Pregabalin has proven effective at treating neuropathic and peripheral forms of pain and some studies show that Pregabalin can help treat Complex Regional Pain Syndrome (CRPS). Pregabalin also shows promise as a treatment for Fibromyalgia.

What is the recommended dosage for Pregabalin?

Pregabalin is typically given in doses of 300-600 milligrams depending on what the drug is being used for. Pregabalin’s side effects are usually mild to moderate, especially when Pregabalin is taken with food.

Pregabalin was developed by the pharmaceutical company Pfizer and Pregabalin went on sale in 2005 under the brand name Lyrica. Pregabalin has been prescribed to treat conditions such as Fibromyalgia, CRPS, Neuropathic pain caused by Diabetes or damage to nerves due to chemotherapy treatment, Epilepsy seizures, and restless leg syndrome. Pregabalin can be used off label for other forms of pain not listed here.

How Long Does Pregabalin Take to Work?

In most cases Pregabalin takes about 1 week before its effects are noticeable, but depending on Pregabalin dosage timing of doses may affect how long it takes Pregabalin to work. Pregabalin is taken by mouth and the time Pregabalin stays in a person’s system can be anywhere from 12-36 hours.

How does Pregabalin interact with other medications?

Pregabalin may react with prescription and over-the-counter medicines because it is filtered through the liver. Pregabalin’s level in the bloodstream can be altered by P-glycoprotein inhibitors which can affect Pregabalin. P-glycoprotein inhibitors are used to improve P-glycoprotein substrate delivery across biological membranes and P-glycoprotein substrates include Pregabalin as well as many other medicines such as Azole antifungals, calcium channel blockers, P/Q-type calcium channel blockers like Pregabalin, chemotherapeutic agents, contraceptives, HIV protease inhibitors and others.

Pregabalin may also interact with other First Seizure medications due to its effects on GABA receptors. Some first seizure medications work by inhibiting or stimulating GABA (gamma aminobutyric acid) receptors in the brain which Pregabalin does, so Pregabalin can affect first seizure medications by reducing their effects. Pregabalin may also reduce levels of other medications that are changed by P-glycoprotein which could be dangerous for people who are being treated with P-glycoprotein inhibitors.

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