Drilldown: Medicines

Gabapentin (1) · Pregabalin (1)

Lyrica (IR), Lyrica CR (1) · Neurontin (IR), Gralise (ER), Horizant (gabapentin enacarbil ER) (1)

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None (2)

'"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1) · '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"' (1)

300 mg PO at bedtime night 1, 300 mg BID day 2, 300 mg TID day 3; titrate to clinical effect, commonly 1800-3600 mg/day divided TID (1) · 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 (1)

Capsules 100, 300, 400 mg; tablets 600, 800 mg; oral solution 250 mg/5 mL; Gralise ER tablets 300, 600 mg (once-daily); Horizant ER tablets 300, 600 mg (gabapentin enacarbil, an inactive parent compound metabolized to gabapentin in vivo) (1) · Capsules 25, 50, 75, 100, 150, 200, 225, 300 mg; oral solution 20 mg/mL; Lyrica CR tablets 82.5, 165, 330 mg (1)

3600 mg/day; off-label doses higher are common but bioavailability saturates well below this (1) · 600 mg/day (seizures); 450 mg/day (fibromyalgia and neuropathic pain) (1)

Oral (2)

1-2 weeks for neuropathic pain and anxiolytic effect; anticonvulsant effect at therapeutic plasma level (1) · Neuropathic pain and fibromyalgia effect emerges over 1-2 weeks (1)

BID-TID dosing for IR; once-daily for CR (1) · TID dosing for IR; once-daily for ER formulations (1)

5-7 hours'"`UNIQ--ref-00000029-QINU`"' (1) · 6.3 hours'"`UNIQ--ref-00000026-QINU`"' (1)

'''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' (1) · ≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)'"`UNIQ--ref-00000027-QINU`"' (1)

Limited human data; some signal for cardiac malformations and developmental delay but confounded by maternal disease and polytherapy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for major congenital malformations; limited human data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

None (1) · '''[[USLegal:Schedule V|Schedule V controlled substance]] in US (federally)''', distinct from gabapentin which remains federally unscheduled'"`UNIQ--ref-00000028-QINU`"' (1)