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Saturday, December 6, 2014

Pregabalin Mechanism Of Action And Side Effects

What is pregabalin ?


Pregabalin (INN) or (S) -3-aminomethyl-5-methyl-hexanoic acid is a γ-amino acid which is related to the neurotransmitter γ-aminobutyric acid (GABA). It is a GABA-agonist with an anti-convulsant activity. In addition, the agent is also indicated for the treatment of generalized anxiety disorder and of neuropathic pain. Pregabalin is the active ingredient in the drug Lyrica from Pfizer. This is available in capsules with 75 to 300 mg of pregabalin, or as an oral solution containing 20 mg / mL of pregabalin.

History


Pregabalin was developed at Northwestern University in Evanston (Illinois) by Professor Richard Bruce Silverman and employees, with the support of the Warner-Lambert Company. Warner-Lambert was acquired in 2000 by Pfizer. Pfizer has pregabalin marketed with the brand name Lyrica.

In the European Union Lyrica is allowed since July 6, 2004.

In the United States, Lyrica by the Food and Drug Administration for the first time admitted on 30 December 2004. In 2007, Lyrica was approved for the treatment of fibromyalgia.

Indications


-Neuropathic pain caused by nerve damage in both the central and peripheral nervous systems, including caused by diabetes, shingles or spinal cord injury;
-Generalized anxiety disorder;
-Epilepsy: as adjunctive treatment as other antiepileptic drugs are not enough.

Pregabalin mechanism of action


The chemical structure of pregabalin is similar to that of gamma-aminobutyric acid (GABA), but the effect of the agent is not similar to that of GABA. Pregabalin is neither an antagonist nor an agonist of GABA receptors. Pregabalin binds in the central nervous system to an auxiliary subunit of voltage dependent calcium channels. As a result, it reduces the neuronal sensitivity. It also reduces the release of various neurotransmitters including substance P, glutamate and noradrenaline. The exact mechanism of action of pregabalin is not yet clear.

Pregabalin side effects


The most commonly reported side effects are dizziness and drowsiness. When using Lyrica may blurred vision, double vision or loss of vision occur. Increased appetite, weight gain, and erectile dysfunction may also occur. A list of possible side effects can be found in the leaflet.

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