Pregabalin: Difference between revisions

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{{MedTemplate

| generic = Pregabalin

| brand = Lyrica

| brand = Lyrica (IR), Lyrica CR

| 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 =~~

~~| pregnancy_details =~~

~~| monitoring~~ =

~~| counseling~~ =

~~| anecdotes =~~

~~| seealso =~~

~~| references~~ =

}}

[[Category:~~Sedative-Hypnotics~~]]

== References ==

[[Category:Gabapentinoids]]

[[Category:Anticonvulsants]]

[[Category:Neuropathic pain medicines]]

[[Category:Schedule V controlled substances]]

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