What is Pregabalin?
Complete information about this important anticonvulsant medication
Overview
Pregabalin is a prescription medication belonging to the class of drugs known as anticonvulsants or antiepileptic drugs (AEDs). It was first approved by the FDA in December 2004 and is marketed under the brand name Lyrica, among others. Pregabalin is structurally similar to the neurotransmitter GABA (gamma-aminobutyric acid) but works through a different mechanism.
Quick Facts
- Generic Name: Pregabalin
- Brand Names: Lyrica, Lyrica CR
- Drug Class: Anticonvulsant, Neuropathic Pain Agent
- Chemical Formula: C₈H₁₇NO₂
- Controlled Substance: Schedule V
How Pregabalin Works
Pregabalin works by binding to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system. This binding reduces the release of several neurotransmitters, including:
- Glutamate
- Norepinephrine
- Substance P
- Calcitonin gene-related peptide (CGRP)
By reducing the release of these excitatory neurotransmitters, pregabalin helps to calm overactive nerve signals that can cause pain, seizures, and anxiety.
Pharmacokinetics
Absorption
Rapidly absorbed after oral administration with bioavailability ≥90%
Peak Levels
1-1.5 hours after administration
Half-life
6.3 hours in healthy individuals
Elimination
Primarily unchanged through kidneys (98%)
Available Formulations
Immediate-Release Capsules
Available in: 25mg, 50mg, 75mg, 100mg, 150mg, 200mg, 225mg, 300mg
Extended-Release Tablets (Lyrica CR)
Available in: 82.5mg, 165mg, 330mg
Oral Solution
20mg/mL concentration
Clinical Development
Pregabalin was developed by Northwestern University medicinal chemist Richard Bruce Silverman. The compound underwent extensive clinical trials before receiving FDA approval. Key milestones include:
- 1990s: Initial discovery and development
- 2004: FDA approval for neuropathic pain and seizures
- 2007: Approval for fibromyalgia
- 2017: Extended-release formulation approved
- 2019: Generic versions became available
Important Considerations
⚠️ Important Safety Information
- Pregabalin is a controlled substance (Schedule V) due to potential for abuse and dependence
- May cause serious allergic reactions
- Can cause suicidal thoughts or behavior
- Requires dose adjustment in kidney impairment
- Should not be stopped abruptly