Skip to main content
OpenTrials
Completed

NCT Number: NCT02977208

Impact of Polymorphisms of OCT2 and OCTN1 on the Kinetic Disposition of Gabapentin in Patients Undergoing Chronic Use

This study aims to evaluate the influence of genetic polymorphisms of OCTN1 and OCT2 and other possible covariates on the kinetic disposition of GAB in patients undergoing GAB chronic treatment. Thus, patients treated with GAB, for at least one week, are being investigated.

Completed

Looking for future studies?

Notify Me

Key information

Conditions

Epilepsy Brain Diseases Central Nervous System Diseases Chronic Pain Nervous System Diseases Neurologic Manifestations Pain Pathological Conditions, Signs and Symptoms Signs and Symptoms

Age range

18 year and older

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 4

Primary location

Universidade Estadual Paulista Júlio de Mesquita Filho

Araraquara, São Paulo, 14800903, Brazil

About this study

Gabapentin (GAB), an anticonvulsant used for the treatment of epilepsy and chronic pain, has nonlinear kinetics, it is not metabolized and it is mainly eliminated by renal excretion. Studies suggest that the renal excretion of GAB is dependent on active secretion by organic cation transporter 2 (OCT2) and organic cation/ergothioneine transporter 1 (OCTN1). These transporters are expressed at the membrane of the renal proximal tubules and they are involved in the elimination of endogenous compounds and many drugs. The genetic polymorphism of drug transporters has been studied to explain the kinetic disposition variability of their substrates. The objective of this study is to investigate the influence of genetic polymorphisms of OCTN1 and OCT2 and other possible covariates (e.g., sex, age, creatinine clearance, body mass index) on the kinetic disposition of GAB in patients undergoing GAB chronic treatment. Patients treated with GAB, for at least one week, are being investigated. Blood and urine samples are being collected to GAB pharmacokinetic analysis, serum creatinine analysis and for genotyping. The plasma concentration of GAB will be assessed using liquid chromatography with UV detection (LC-UV).

Who can participate

Healthy volunteers accepted: No

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Patients with 18 years old or older, both gender.
  • Patients undergoing chronic use of gabapentin (at least one week).

Exclusion criteria

  • Pregnant and lactating patients.
  • Patients who were in use of OCT2 and OCTN1 inhibitors.
  • Patients who disagree to continue the study.

Treatment and study plan

Sparse blood sampling

Procedure

Blood samples are being collected at times 0, 90 and 240 minutes after gabapentin administration.

Urine sampling

Procedure

Urine samples are being collected during the dosing interval, only in patients hospitalized at Hospital Estadual de Américo Brasiliense (HEAB).

DNA extraction

Procedure

Blood sample are being collected for DNA extraction. DNA are being extracted from the whole blood of all patients for genotyping of the SLC22A2 c.808G>T and SLC22A4 c.1507C>T polymorphisms

Gabapentin

Drug

All patients undergoing chronic treatment with gabapentin are being recruited.

Other names: GAB

Primary outcomes

  1. Gabapentin plasma concentration.

    Time frame: Up to 240 minutes after gabapentin administration.

    Blood samples will be collected at 0, 90 and 240 minutes after gabapentin administration. The gabapentin plasma concentration will be assessed using liquid chromatography with UV detection (LC-UV).

  2. OCT2 and OCTN1 genotyping

    Time frame: Up to 5 minutes before gabapentin administration

    The single nucleotide polymorphisms of SLC22A2 gene (c.808G>T) and SLC22A4 (c.1507C>T) are being evaluated in all included patients.

Sponsors and collaborators

Lead sponsor

São Paulo State University

Other

Collaborators

  • University of Sao Paulo

Registry information

Official study title

Impact of Genetic Polymorphisms of OCT2 and OCTN1 on the Kinetic Disposition of Gabapentin in Patients Undergoing Chronic Use of the Drug

Important dates

Study start
2016
Primary completion
2018
Study completion
2018
First posted
Nov 30, 2016
Registry last updated
Apr 18, 2018

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

Related clinical trials

Published trials that share one or more normalized conditions with this study.