Print ISSN 2319-2003 | Online ISSN 2279-0780 doi: http://dx.doi.org/10.18203/2319-2003.ijbcp20150359 IJBCP International Journal of Basic & Clinical Pharmacology www.ijbcp.com International Journal of Basic & Clinical Pharmacology | July-August 2015 | Vol 4 | Issue 4 Page 601 Review Article A review of the drug pregabalin N. Manjushree*, Ananya Chakraborty, K. Shashidhar, Srinivas Narayanaswamy INTRODUCTION Pregabalin (PGB) is a well-recognized central nervous system depressant. It is a structural analog of gamma- aminobutyric acid. It is a non-opioid drug and is a α2-δ ligand that modulates the activity of voltage-gated calcium channels. It was introduced by US Food and Drug Administration (FDA) in December 2004. It was first discovered for the treatment of neuropathic pain associated with diabetic peripheral neuropathy and post-herpetic neuralgia (PHN). In June 2005, the drug was approved for the treatment of partial onset seizures with or without secondary generalization in adults as an adjunctive drug. Currently, FDA is considering the approval of PGB as an adjunctive therapy in adults with generalized anxiety disorder (GAD) or social anxiety disorder (SAD), spinal cord injury, and fbromyalgia. In the European Union, PGB is indicated for peripheral and central neuropathic pain, epilepsy, and GAD. 1 Previous studies have shown that PGB can be used with safety and an acceptable effcacy in treatment of childhood refractory partial seizures. 2 Preclinical studies of PGB in animal models of neuropathic pain have shown its effectiveness in treating symptoms such as allodynia and hyperalgesia. Clinical studies in different age groups and in different types of neuropathic pain have projected it as the most effective agent either as monotherapy or in combination regimens. This is based on the cost effectiveness, tolerability and overall improvement in neuropathic pain scores. 3 Also, PGB is well-tolerated and relieves painful symptoms of distal symmetrical polyneuropathy (DPN) with minimal risk of dependence or impact on patient’s diabetes control. PGB has consistently proved itself as an effective treatment for DPN and PHN in its extensive clinical trial programs. It is among the agents recommended by the American Academy of Neurology as a Group 1 treatment for PHN. European Federation of Neurological Societies have considered the drug as a frst-line treatment for painful polyneuropathy. 4 MECHANISM OF ACTION PGB is an antagonist of voltage-gated calcium channels. It crosses the blood brain barrier and binds potently to ABSTRACT Pregabalin (PGB) is a well-established anticonvulsant and analgesic agent. The stydy reviewed the mechanism of action, pharmacokinetics, adverse drug reactions, contraindications, and various uses of PGB. Literature search was done to identify the relevant studies. PGB is an antagonist of voltage-gated calcium channels and specifcally binds to α2-δ subunit to produce antiepileptic and analgesic activity. It has less protein binding activity and lacks hepatic metabolism. It is unlikely to cause pharmacokinetic drug-drug interactions. It has a wide safety margin and does not require serum drug monitoring. The above-mentioned favorable pharmacological benefts of PGB makes it a frst-line or adjunctive therapy in various conditions like diabetic peripheral neuropathy, post-herpetic neuralgia, in partial seizures and generalized anxiety disorders. Keywords: Pregabalin, Neuropathic pain, Partial seizures, Effcacy, Safety Department of Pharmacology, Vydehi Institute of Medical Sciences and Research Centre, Bengaluru, Karnataka, India Received: 02 July 2015 Accepted: 18 July 2015 *Correspondence to: Dr. N. Manjushree, Email: manjubmch@gmail. com Copyright: © the author(s), publisher and licensee Medip Academy. This is an open- access article distributed under the terms of the Creative Commons Attribution Non- Commercial License, which permits unrestricted non- commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.