Gabapentinoids: Difference between revisions

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Pregabalin has demonstrated significantly greater potency (about 2.5-fold) than gabapentin in clinical studies.<ref>Schifano F, D'Offizi S, Piccione M, Corazza O, Deluca P, Davey Z, Di Melchiorre G, Di Furia L, Farré M, Flesland L, Mannonen M, Majava A, Pagani S, Peltoniemi T, Siemann H, Skutle A, Torrens M, Pezzolesi C, van der Kreeft P, Scherbaum N (2011). "Is there a recreational misuse potential for pregabalin? Analysis of anecdotal online reports in comparison with related gabapentin and clonazepam data". ''Psychother Psychosom''. '''80''' (2): 118–22. doi:10.1159/000321079. hdl:2299/9328. <nowiki>PMID 21212719</nowiki>. S2CID 11172830.</ref>

Gabapentin and pregabalin are absorbed from the intestines by an active transport process mediated via the large neutral amino acid transporter 1 (LAT1, SLC7A5), a transporter for amino acids such as <small>L</small>-leucine and <small>L</small>-phenylalanine.<ref name=":1">Calandre EP, Rico-Villademoros F, Slim M (2016). "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". ''Expert Rev Neurother''. '''16''' (11): 1263–1277. doi:10.1080/14737175.2016.1202764. <nowiki>PMID 27345098</nowiki>. S2CID 33200190.</ref> The oral bioavailability of gabapentin is approximately 80% at 100 mg administered three times daily once every 8 hours, but decreases to 60% at 300 mg, 47% at 400 mg, 34% at 800 mg, 33% at 1,200 mg, and 27% at 1,600 mg, all with the same dosing schedule.<ref>Bockbrader HN, Wesche D, Miller R, Chapel S, Janiczek N, Burger P (2010). "A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin". ''Clin Pharmacokinet''. '''49''' (10): 661–9. doi:10.2165/11536200-000000000-00000. <nowiki>PMID 20818832</nowiki>. S2CID 16398062.</ref>

Gabapentin, pregabalin, and phenibut all undergo little or no metabolism. Conversely, gabapentin enacarbil, which acts as a prodrug of gabapentin, must undergo enzymatic hydrolysis to become active. This is done via non-specific esterases in the intestines and to a lesser extent in the liver.<ref name=":1" />

==Examples==

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 Pregabalin has demonstrated significantly greater potency (about 2.5-fold) than gabapentin in clinical studies.<ref>Schifano F, D'Offizi S, Piccione M, Corazza O, Deluca P, Davey Z, Di Melchiorre G, Di Furia L, Farré M, Flesland L, Mannonen M, Majava A, Pagani S, Peltoniemi T, Siemann H, Skutle A, Torrens M, Pezzolesi C, van der Kreeft P, Scherbaum N (2011). "Is there a recreational misuse potential for pregabalin? Analysis of anecdotal online reports in comparison with related gabapentin and clonazepam data". ''Psychother Psychosom''. '''80''' (2): 118–22. doi:10.1159/000321079. hdl:2299/9328. <nowiki>PMID 21212719</nowiki>. S2CID 11172830.</ref>
+Gabapentin and pregabalin are absorbed from the intestines by an active transport process mediated via the large neutral amino acid transporter 1 (LAT1, SLC7A5), a transporter for amino acids such as <small>L</small>-leucine and <small>L</small>-phenylalanine.<ref name=":1">Calandre EP, Rico-Villademoros F, Slim M (2016). "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". ''Expert Rev Neurother''. '''16''' (11): 1263–1277. doi:10.1080/14737175.2016.1202764. <nowiki>PMID 27345098</nowiki>. S2CID 33200190.</ref> The oral bioavailability of gabapentin is approximately 80% at 100 mg administered three times daily once every 8 hours, but decreases to 60% at 300 mg, 47% at 400 mg, 34% at 800 mg, 33% at 1,200 mg, and 27% at 1,600 mg, all with the same dosing schedule.<ref>Bockbrader HN, Wesche D, Miller R, Chapel S, Janiczek N, Burger P (2010). "A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin". ''Clin Pharmacokinet''. '''49''' (10): 661–9. doi:10.2165/11536200-000000000-00000. <nowiki>PMID 20818832</nowiki>. S2CID 16398062.</ref>
+Gabapentin, pregabalin, and phenibut all undergo little or no metabolism. Conversely, gabapentin enacarbil, which acts as a prodrug of gabapentin, must undergo enzymatic hydrolysis to become active. This is done via non-specific esterases in the intestines and to a lesser extent in the liver.<ref name=":1" />
 ==Examples==