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Completed

NCT Number: NCT03047278

Transporters for Organic Cations and Glycemic Control in Patients With Neuropathic Pain.

This study aimed to investigate the influence of the glycemic control of type 2 diabetes (DM2) and of cetirizine (OCTs inhibitor) on gabapentin kinetics disposition and pharmacodynamics (PK-PD) in patients with neuropathic pain. Thus, non-diabetic patients (Control Group, n=10), patients with controlled diabetes (n=9) and patients with uncontrolled diabetes (n=10), all with neuropathic pain of intensity ≥ 4 in pain visual analog scale (0-10) were investigated.

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Key information

Conditions

Neuropathic Pain Diabetes Complications Diabetes Mellitus Diabetes Mellitus, Type 2 Diabetic Neuropathies Diabetic Neuropathy, Painful Endocrine System Diseases Glucose Metabolism Disorders Metabolic Diseases Nervous System Diseases Neuralgia Neurologic Manifestations Neuromuscular Diseases Nutritional and Metabolic Diseases Pain Pathological Conditions, Signs and Symptoms Peripheral Nervous System Diseases Signs and Symptoms Type 2 Diabetes Mellitus

Age range

18 year–59 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 4

About this study

Gabapentin (GBP), anticonvulsant used to neuropathic pain treatment, is mainly eliminated unchanged in urine. Renal active tubular secretion has been suggested to contribute on GBP excretion by renal excretion. Studies performed on rats with experimental diabetes suggest that hyperglycemia reduces the activity of organic cation transporters (Oct). Thus, the aim of the study was to investigate the role of OCTs on kinetic disposition and pharmacodynamics of GBP in patients with neuropathic pain and to verify the regulation of these transporters' activity by glycemic control in diabetes. A cross-over clinical study was performed in patients with neuropathic pain (n=10, Control) to evaluate the influence of CTZ on GBP kinetic disposition. To evaluate the effect of glycemic control, patients with controlled DM2 (DC, n=9) and uncontrolled DM2 (DNC, n=10) were investigated. All participants investigated had neuropathic pain of intensity ≥ 4 evaluated by analogue visual scale (EVA) and were treated with oral single-dose of 300 mg of GBP (Phase 1) or cetirizine (20 mg/day) for 5 days and single-dose of GBP on the last day (Phase 2). Only participants of Control group participated of Phase 2. Serial blood and urine samples were collected up to 36 hours after GBP administration. The intensity of pain was evaluated at the same time of blood sampling, using the visual analog scale. GBP concentration in plasma and urine was validated by JPLC-UV. All participants were genotyped for polymorphisms SLC22A2 808G>T and SLC22A4 1507C>T. The pharmacokinetic parameters were estimated by non-compartmental analysis.

Who can participate

Healthy volunteers accepted: No

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

Inclusion criteria

  • Adult patients, both gender
  • Patients with neuropathic pain with score ≥ 4 in visual analog scale
  • Patients with controlled type 2 diabetes (glycated hemoglobin ≤ 8.0%) and diabetic neuropathy with score ≥ 4 in visual analog scale
  • Patients with uncontrolled type 2 diabetes (glycated hemoglobin ≥ 8.0%) and diabetic neuropathy with score ≥ 4 in visual analog scale
  • Patients that suspend the use of analgesics for 10 times half-life before starting the protocol

Exclusion criteria

  • Patients with acute or chronicle severe renal failure (creatinine clearance ≤ 30 mL/min)
  • Patients with gastrointestinal diseases
  • Patients with history of alcohol and drug abuse
  • Patients with acute myocardial insufficiency
  • Patients with another kind of chronicle pain as severe as neuropathic pain
  • Patients in chronicle use of drugs that interact with gabapentin (antacids and cimetidine)

Treatment and study plan

Serial Blood Samples

Procedure

Serial blood samples were collected at times 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24 and 36 hours after gabapentin administration, for all patients.

Serial Urine Samples

Procedure

Serial urine samples were collected at intervals 0-8 hours, 8-16 hours, 16-24 hours and 24-36 hours after gabapentin administration, for all patients.

Gabapentin 300 mg

Drug

All patients were treated with oral single dose of gabapentin 300 mg.

Cetirizine Hydrochloride 10 mg

Drug

Patients of control group were treated with cetirizine hydrochloride, 10 mg, twice as day, orally, for five days.

Primary outcomes

  1. Pharmacokinetic parameter (AUC)

    Time frame: Up to 36 hours after gabapentin (300 mg) administration

    Area under the plasma concentration versus time (AUC)

Secondary outcomes

  1. Pharmacokinetic parameter (Total clearance)

    Time frame: Up to 36 hours after gabapentin (300 mg) administration

    Total clearance

  2. Pharmacokinetic parameter (Renal clearance)

    Time frame: Up to 36 hours after gabapentin (300 mg) administration

    Renal clearance

  3. Pharmacokinetic parameter (Vd)

    Time frame: Up to 36 hours after gabapentin (300 mg) administration

    Volume of distribution (Vd)

  4. Pharmacokinetic parameter (Elimination half-life)

    Time frame: Up to 36 hours after gabapentin (300 mg) administration

    Elimination half-life

Sponsors and collaborators

Lead sponsor

Natalia Valadares de Moraes

Other

Collaborators

  • University of Sao Paulo

Registry information

Official study title

Gabapentin Kinetic Disposition and Renal Excretion: Role of Transporters for Organic Cations and the Effect of Glycemic Control in Patients With Neuropathic Pain.

Important dates

Study start
2015
Primary completion
2018
Study completion
2019
First posted
Feb 8, 2017
Registry last updated
Jul 5, 2019

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.

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