2018
DOI: 10.1111/bcpt.13126
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Pharmacogenetics‐based population pharmacokinetic analysis of gabapentin in patients with chronic pain: Effect of OCT2 and OCTN1 gene polymorphisms

Abstract: Gabapentin (GAB) is eliminated unchanged in urine, and organic cation transporters (OCT2 and OCTN1) have been shown to play a role in GAB renal excretion. This prospective clinical study aimed to evaluate the genetic polymorphisms effect on GAB pharmacokinetic (PK) variability using a population pharmacokinetic approach. Data were collected from 53 patients with chronic pain receiving multiple doses of GAB. Patients were genotyped for SLC22A2 c.808G>T and SLC22A4 c.1507C>T polymorphisms. Both polymorphisms' di… Show more

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Cited by 13 publications
(22 citation statements)
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“…All participants were genotyped for the SNPs 808G > T (rs316019) of SLC22A2 gene and 1507C > T (rs1050152) of SLC22A4, as previously reported. 45,49 The Hardy-Weinberg equilibrium was evaluated using the χ 2 test. The clinical history and the use of concomitant drugs were registered for all participants.…”
Section: Clinical Protocolmentioning
confidence: 99%
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“…All participants were genotyped for the SNPs 808G > T (rs316019) of SLC22A2 gene and 1507C > T (rs1050152) of SLC22A4, as previously reported. 45,49 The Hardy-Weinberg equilibrium was evaluated using the χ 2 test. The clinical history and the use of concomitant drugs were registered for all participants.…”
Section: Clinical Protocolmentioning
confidence: 99%
“…GBP was determined in plasma by high-performance liquid chromatography-UV (Shimadzu Inc., Kyoto, Japan), as described previously. 45,49 In summary, the analytes were resolved on short-term, long-term, post-processing and freeze-thaw cycles).…”
Section: Analysis Of Gbp On Plasma By Highperformance Liquid Chromamentioning
confidence: 99%
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“…Gabapentinoids are also substrate of drug transporters OCTN1 and OCT2; gabapentin bioavailability has recently been found to have no association with OCTN1 1507C˃T polymorphism and mainly influenced by renal functions. However, the study did not correlate the pharmacogenetic and pharmacokinetic parameters with clinical outcomes 31 …”
Section: Discussionmentioning
confidence: 95%
“…In contrast, gabapentinoids (gabapentin, pregabalin) are neither activators/inhibitors of the cytochrome P450 system nor subject to hepatic metabolism [119,120], but are instead excreted in urine. This process is under the influence of organic cation transporters OCTN1 and OCT2 coded by SLC22A4 and SLC22A2 genes, respectively [121][122][123]. However, the genotype of an individual (e.g., OCTN1 polymorphism) was found to have a negligible role in gabapentin clearance and was much more affected by the renal function and absorption process [123].…”
Section: Pharmacogenomics In Management Of Clbpmentioning
confidence: 99%