pregabalin

pregabalin. It is a medication primarily used to treat neuropathic pain, fibromyalgia, generalized anxiety disorder, and as an adjunct therapy for partial-onset seizures. Marketed under the brand name Lyrica among others, it is classified as a gabapentinoid and is a controlled substance in many jurisdictions due to its potential for misuse. Its development was a significant milestone for the pharmaceutical company Pfizer.

Medical uses

Pregabalin is approved by regulatory bodies like the U.S. Food and Drug Administration and the European Medicines Agency for several conditions. Its primary indications include diabetic neuropathy, postherpetic neuralgia, and neuropathic pain associated with spinal cord injury. It is also a first-line treatment for fibromyalgia, as established in clinical trials, and is used for generalized anxiety disorder in many countries outside the United States. As an antiepileptic drug, it is indicated for partial-onset seizures in combination with other medications like levetiracetam or lamotrigine.

Adverse effects

Common adverse effects include dizziness, somnolence, peripheral edema, and weight gain. More serious risks involve angioedema, respiratory depression, especially when combined with opioids like oxycodone, and potential for suicidal ideation, a warning issued by the FDA for many anticonvulsants. Abrupt discontinuation can lead to a withdrawal syndrome with symptoms including insomnia, headache, and nausea. Its misuse potential has led to scheduling by the Drug Enforcement Administration.

Pharmacology

Pregabalin acts by binding to the α2δ subunit of voltage-gated calcium channels in the central nervous system, particularly in regions like the cerebral cortex and spinal cord. This binding inhibits the release of several neurotransmitters, including glutamate, noradrenaline, and substance P. Unlike many psychoactive drugs, it is not metabolized in the liver and does not bind to GABA receptors. It exhibits high bioavailability and is excreted largely unchanged by the kidneys.

Society and culture

The drug has been the subject of significant legal and regulatory scrutiny. Pfizer faced litigation, including a settlement with the U.S. Department of Justice regarding marketing practices. Its non-medical use and associated harms have been reported in regions like the United Kingdom and Scotland, influencing its classification as a Class C drug under the Misuse of Drugs Act 1971. The high cost of Lyrica has also sparked debates within healthcare systems like the National Health Service.

History

Pregabalin was discovered by medicinal chemists at Pfizer and was developed as a successor to gabapentin. It received its first approval from the European Commission in 2004, followed by FDA approval in the United States later that year. Key clinical trials demonstrating its efficacy were conducted at institutions like the University of Michigan and published in journals such as Neurology. Its patents have expired in many markets, leading to the availability of generic drug versions.

Category:Drugs