Pregabalin
Prescription gabapentinoid anxiolytic that inhibits the α2δ calcium channel subunit.
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Pharmacology
Contents
WHAT IS PREGABALIN?
Detailed overview
Pregabalin (Lyrica) is a prescription gabapentinoid, a structural analogue of GABA that nonetheless does not act on GABA receptors but instead binds the α2δ-1 subunit of voltage-gated calcium channels. By reducing calcium influx at overactive synapses it dampens the release of excitatory neurotransmitters (glutamate, noradrenaline, substance P) without broadly suppressing normal neural signaling. In the EU it is approved for generalized anxiety disorder (GAD), neuropathic pain and fibromyalgia, and as adjunctive therapy for epilepsy. In randomized trials it significantly reduced anxiety scores versus placebo within the first week. It can cause physical dependence, so it requires gradual tapering and cautious use.
Mechanism
α2δ-1 calcium channel ligand
Half-life
About 6 hours
Legal status
Prescription drug (EU: approved for GAD)
Receptor profile
- α2δ-1 calcium channel subunitStrong
- Glutamate and noradrenaline release (reduces)Moderate
- Substance P releaseModerate
- GABA receptors (no direct binding)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Drowsiness, dizziness and sedation, especially in the first weeks of treatment
- Cognitive clouding, difficulty concentrating, blurred vision
- Weight gain, peripheral oedema (limb swelling), dry mouth
- Euphoria and mood elevation: potential for recreational misuse
- Physical dependence: withdrawal syndrome on abrupt cessation (anxiety, insomnia, sweating, nausea)
- Increased risk of respiratory depression when combined with opioids or other sedatives
Contraindications · 5
- Impaired kidney function: dose must be reduced according to creatinine clearance
- History of substance use disorder: heightened misuse and dependence risk
- Concurrent opioids, benzodiazepines or alcohol: additive sedation and respiratory depression
- Pregnancy and breastfeeding: only after clear benefit-risk assessment under medical supervision
- Do not stop abruptly: treatment should be tapered gradually over at least one week
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Pregabalin for treatment of generalized anxiety disorder: a 4-week, multicenter, double-blind, placebo-controlled trial of pregabalin and alprazolam
Rickels K, Pollack MH, Feltner DE, et al.
Comparative efficacy of pregabalin and benzodiazepines in treating the psychic and somatic symptoms of generalized anxiety disorder
Lydiard RB, Rickels K, Herman B, Feltner DE
A meta-analysis of the efficacy of pregabalin in the treatment of generalized anxiety disorder
Boschen MJ
Adjunctive therapy with pregabalin in generalized anxiety disorder patients with partial response to SSRI or SNRI treatment
Rickels K, Shiovitz TM, Ramey TS, et al.
Efficacy and safety of pregabalin in generalised anxiety disorder: A critical review of the literature
Frampton JE
FAQ
FAQ
Prescription gabapentinoid anxiolytic that inhibits the α2δ calcium channel subunit.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.