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Pregabalin: Difference between revisions

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Dedupe migration per interface-claude 2026-05-20: Anticonvulsants / Antiepileptics merged into canonical Anticonvulsants. Member retagged.
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{{MedTemplate
{{MedTemplate
| generic           = Pregabalin
| generic           = Pregabalin
| brand             = Lyrica
| brand             = Lyrica (IR), Lyrica CR
| structure         =  
| structure         =
| classes           = Gabapentinoid, Anticonvulsant
| classes           = [[:Category:Gabapentinoids|Gabapentinoid]], [[:Category:Anticonvulsants|Anticonvulsant]], [[:Category:Neuropathic pain medicines|Neuropathic pain medicine]], [[:Category:Schedule V controlled substances|Schedule V controlled substance]]
| mechanism          = Alpha-2-delta voltage-gated calcium channel ligand
| uses              = <vote slug="postherpetic-neuralgia-use">Postherpetic neuralgia (FDA)</vote>, <vote slug="diabetic-peripheral-neuropathy-use">Diabetic peripheral neuropathy (FDA)</vote>, <vote slug="fibromyalgia-pregabalin-use">Fibromyalgia (FDA; the only gabapentinoid with FDA approval for this indication)</vote>, <vote slug="partial-seizures-adjunct-use">Partial-onset seizures (FDA, adjunct)</vote>, <vote slug="sci-neuropathic-pain-use">Spinal-cord-injury neuropathic pain (FDA)</vote>, <vote slug="generalized-anxiety-disorder-use">Generalized anxiety disorder (EU approval; off-label in US)</vote>, <vote slug="social-anxiety-disorder-use">Social anxiety disorder (EU; off-label in US)</vote>
| uses              =  
| starting_dose    = Neuropathic pain: 75 mg PO BID, titrate to 150 mg BID after 1 week. Fibromyalgia: 75 mg PO BID, titrate to 150 mg BID. Anxiety (off-label): 75-150 mg/day divided BID-TID
| starting_dose     =  
| preparations     = Capsules 25, 50, 75, 100, 150, 200, 225, 300 mg; oral solution 20 mg/mL; Lyrica CR tablets 82.5, 165, 330 mg
| preparations      =  
| fda_max          = 600 mg/day (seizures); 450 mg/day (fibromyalgia and neuropathic pain)
| fda_max           =  
| pill_id           =
| routes             =  
| routes           = Oral
| onset             =  
| onset             = Neuropathic pain and fibromyalgia effect emerges over 1-2 weeks
| duration           =  
| duration         = BID-TID dosing for IR; once-daily for CR
| halflife           =
| halflife          = 6.3 hours<ref name="lyrica-label">FDA Prescribing Information, Lyrica (pregabalin), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021446s035,022488s013lbl.pdf</ref>
| bioavailability    =
| bioavailability  = ≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)<ref name="lyrica-label" />
| pregnancy         =  
| pregnancy        = Some signal for major congenital malformations; limited human data.{{citation needed}}
| legal              =  
| legal             = '''[[USLegal:Schedule V|Schedule V controlled substance]] in US (federally)''', distinct from gabapentin which remains federally unscheduled<ref name="lyrica-label" />
| intro              =  
| mechanism         = <vote slug="pregabalin-mech-claim">Binds the α2δ-1 auxiliary subunit of voltage-gated calcium channels with approximately 6-fold higher affinity than gabapentin, reducing presynaptic Ca²⁺ influx and excitatory neurotransmitter release (glutamate, substance P, norepinephrine, calcitonin gene-related peptide). Despite the gabapentinoid class name, pregabalin does '''not''' bind GABA receptors or affect GABA reuptake.</vote> Linear pharmacokinetics across the dosing range with non-saturable transport, in sharp contrast to gabapentin where bioavailability falls steeply with dose. Renally eliminated essentially unchanged; dose adjustment required in renal impairment<ref name="lyrica-label" />.
| pharmacokinetics   =  
| pharmacodynamics  =  
| indications        =
| dosing             =  
| effects            =  
| interactions      = <pharmaInteractions/>
| pregnancy_details  =
| monitoring         =  
| counseling        =  
| anecdotes          =
| seealso            =
| references        =  
}}
}}


[[Category:GABAergics]]
== References ==
[[Category:Sedative-Hypnotics]]
<references />
[[Category:Calcium channel blockers (T-type or N/P/Q-type)]]
 
[[Category:Gabapentinoids]]
[[Category:Anticonvulsants]]
[[Category:Anticonvulsants]]
[[Category:Neuropathic pain medicines]]
[[Category:Schedule V controlled substances]]

Latest revision as of 06:49, 23 May 2026

Gabapentinoid, Anticonvulsant, Neuropathic pain medicine, Schedule V controlled substance
Pregabalin
Lyrica (IR), Lyrica CR

Experience

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Problems

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Titration strategies

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Effects

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Summary
Classes
Gabapentinoid, Anticonvulsant, Neuropathic pain medicine, Schedule V controlled substance
Common uses
Postherpetic neuralgia (FDA)0, Diabetic peripheral neuropathy (FDA)0, Fibromyalgia (FDA; the only gabapentinoid with FDA approval for this indication)0, Partial-onset seizures (FDA, adjunct)0, Spinal-cord-injury neuropathic pain (FDA)0, Generalized anxiety disorder (EU approval; off-label in US)0, Social anxiety disorder (EU; off-label in US)0
Pharmacy
Starting dose
Neuropathic pain: 75 mg PO BID, titrate to 150 mg BID after 1 week. Fibromyalgia: 75 mg PO BID, titrate to 150 mg BID. Anxiety (off-label): 75-150 mg/day divided BID-TID
Preparations
Capsules 25, 50, 75, 100, 150, 200, 225, 300 mg; oral solution 20 mg/mL; Lyrica CR tablets 82.5, 165, 330 mg
US FDA Max
600 mg/day (seizures); 450 mg/day (fibromyalgia and neuropathic pain)
Pharmacology
Routes
Oral
Onset
Neuropathic pain and fibromyalgia effect emerges over 1-2 weeks
Duration
BID-TID dosing for IR; once-daily for CR
Half-life
6.3 hours[1]
Bioavailability
≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)[1]
Pregnancy
Some signal for major congenital malformations; limited human data.[citation needed]
Legal status
Schedule V controlled substance in US (federally), distinct from gabapentin which remains federally unscheduled[1]
Purported mechanism
Binds the α2δ-1 auxiliary subunit of voltage-gated calcium channels with approximately 6-fold higher affinity than gabapentin, reducing presynaptic Ca²⁺ influx and excitatory neurotransmitter release (glutamate, substance P, norepinephrine, calcitonin gene-related peptide). Despite the gabapentinoid class name, pregabalin does not bind GABA receptors or affect GABA reuptake.0 Linear pharmacokinetics across the dosing range with non-saturable transport, in sharp contrast to gabapentin where bioavailability falls steeply with dose. Renally eliminated essentially unchanged; dose adjustment required in renal impairment[1].

References

  1. ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Lyrica (pregabalin), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021446s035,022488s013lbl.pdf
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