Lyrica Drug Class
Lyrica (pregabalin) is classified as an anticonvulsant (antiepileptic drug) and is structurally a gamma-aminobutyric acid (GABA) analogue. 1, 2
Primary Classification
- Pregabalin is chemically described as (S)-3-(aminomethyl)-5-methylhexanoic acid, a synthetic GABA analogue with a molecular formula of C8H17NO2 1
- Despite being a GABA analogue structurally, pregabalin does NOT act as an agonist at GABAA or GABAB receptors and does NOT affect GABA binding, uptake, or degradation 3
Mechanism of Action
- Pregabalin binds to the α2δ subunit (specifically α2δ-1) of voltage-gated calcium channels in the central nervous system, reducing calcium influx and decreasing synaptic neurotransmitter release 3, 4
- This mechanism is shared with gabapentin, though pregabalin has greater binding affinity 3
- The drug acts presynaptically to modulate neurotransmitter release in hyperexcited neurons 4, 5
Therapeutic Classification
Pregabalin has multiple therapeutic applications based on its mechanism:
- Anticonvulsant/Antiepileptic: FDA-approved as adjunctive treatment for partial-onset seizures in adults 6, 5
- Analgesic for Neuropathic Pain: FDA-approved for diabetic peripheral neuropathy and postherpetic neuralgia 7, 2, 5
- Anxiolytic: Has demonstrated efficacy in generalized anxiety disorder and social anxiety disorder 2, 8, 5
- Fibromyalgia Treatment: FDA-approved for fibromyalgia management 7
Clinical Context
- The CDC guidelines classify pregabalin among "selected anticonvulsants" used for neuropathic pain management, alongside gabapentin and oxcarbazepine 7
- In geriatric medication appropriateness tools, pregabalin is specifically excluded from potentially inappropriate medication lists when prescribed for neuropathic pain management 7
- Pregabalin exhibits analgesic, anxiolytic, anticonvulsant, and sleep enhancement effects 8
Pharmacological Properties
- Pregabalin has linear pharmacokinetics with approximately 90% oral bioavailability and peak plasma levels occurring about 1 hour after oral administration 2
- The drug is not protein-bound, has a plasma half-life of approximately 6 hours, and undergoes negligible hepatic metabolism with 95% excreted unchanged in urine 2
- No significant drug interactions occur via CYP450 enzyme systems, as pregabalin does not inhibit or induce CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 1