ArticlePharmaceutical research2001
Mucosal uptake of gabapentin (neurontin) vs. pregabalin in the small intestine.
Article in Pharmaceutical research, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 53 citations in OpenAlex.
- Molecular Variability in Levodopa Absorption and Clinical Implications for the Management of Parkinson's Disease.Journal of Parkinson's disease · 2024Review
- The Effect of Oral Gabapentin and Pregabalin as a Prodrug in Pain Control after Orthopedic Surgery on the Upper Limb: A Double-Blind Parallel Randomized Clinical Trial Study.Anesthesiology research and practice · 2024Article
- Pregabalin for chemotherapy-induced neuropathy: background and rationale for further study.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2022Review
- Development of a Novel Controlled-Release Tablet of Pregabalin: Formulation Variation and Pharmacokinetics in Dogs and Humans.Drug design, development and therapy · 2020Article
- In vivo and in vitro evaluations of intestinal gabapentin absorption: effect of dose and inhibitors on carrier-mediated transport.Pharmaceutical research · 2015Article
- Pregabalin: latest safety evidence and clinical implications for the management of neuropathic pain.Therapeutic advances in drug safety · 2014Review
- Diabetic peripheral neuropathy: should a chaperone accompany our therapeutic approach?Pharmacological reviews · 2012Review
- Elucidating the mechanism of action of pregabalin: α(2)δ as a therapeutic target in anxiety.CNS drugs · 2012Review
- Pregabalin in acute and chronic pain.Journal of anaesthesiology, clinical pharmacology · 2011Article
- A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin.Clinical pharmacokinetics · 2010Review
- Pregabalin for the management of partial epilepsy.Neuropsychiatric disease and treatment · 2008Article
- In vivo effects of glycyl-glutamate and glycyl-sarcosine on gabapentin oral absorption in rat.Pharmaceutical research · 2007Article
- PEPT1 enhances the uptake of gabapentin via trans-stimulation of b0,+ exchange.Pharmaceutical research · 2007Article
- Pregabalin for neuropathic pain based on recent clinical trials.Current pain and headache reports · 2006Review
- Vigabatrin transport across the human intestinal epithelial (Caco-2) brush-border membrane is via the H+ -coupled amino-acid transporter hPAT1.British journal of pharmacology · 2006Article
- PREGABALIN TREATMENT OF PERIPHERAL NERVE DAMAGE IN A MURINE DIABETIC PERIPHERAL NEUROPATHY MODEL.Acta endocrinologica (Bucharest, Romania : 2005)Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo compare the mucosal membrane transport of gabapentin and pregabalin in animal small intestine.
methodsUptake of the two drugs by brush-border membrane vesicles (BBMV) from rat and rabbit small intestine was studied as a function of temperature, uptake-medium sodium content, and intestinal region. Amino acid inhibition studies were conducted with pregabalin.
resultsGabapentin uptake by rat and rabbit jejunal BBMV was sodium independent, whereas pregabalin uptake was sodium dependent. Uptake of both drugs in rabbit small intestinal vesicles was greater at 25 degrees C than at 4 degrees C in the absence of sodium and an additional increase in uptake was observed for pregabalin at 25 degrees C in the presence of sodium. Pregabalin uptake in rabbit duodenal, jejunal, and ileal BBMV was equivalent, whereas gabapentin uptake was greater in duodenal and ileal BBMV, compared with jejunal BBMV. Although inhibition is weak, a decrease in BBMV uptake of pregabalin is observed with coincubation of high concentrations of both neutral and basic amino acids.
conclusionsAmino acid carriers mediate the apical uptake of both drugs in the small intestine. Although gabapentin and pregabalin are structurally similar, their small intestinal mucosal uptake differs in sodium dependence and region dependence. Gabapentin uptake is likely mediated by system b0,+, whereas pregabalin uptake is also mediated by B0 and/or B0,+.
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