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

NCT03047278 | Completed Phase 4

• 1 other identifier: GBPDIABETCET
• Study Type: interventional
• Target: 29
• Locations: 0 countries
• Sites: N/A

Brief Summary

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.

Conditions

Neuropathic Pain; Type 2 Diabetes Mellitus; Diabetic Neuropathy, Painful

Outcome Measures

Primary Outcomes (1)

• Pharmacokinetic parameter (AUC)

  Area under the plasma concentration versus time (AUC)

  Up to 36 hours after gabapentin (300 mg) administration

Secondary Outcomes (4)

• Pharmacokinetic parameter (Total clearance)

  Up to 36 hours after gabapentin (300 mg) administration

• Pharmacokinetic parameter (Renal clearance)

  Up to 36 hours after gabapentin (300 mg) administration

• Pharmacokinetic parameter (Vd)

  Up to 36 hours after gabapentin (300 mg) administration

• Pharmacokinetic parameter (Elimination half-life)

  Up to 36 hours after gabapentin (300 mg) administration

Study Arms (3)

Control Group

ACTIVE COMPARATOR

Adult patients (18 - 59 years old) with neuropathic pain of score ≥ 4 that do not use gabapentin were recruited. All patients received oral single dose of gabapentin (300 mg) as capsules after 12 hour-fasting (phase I). To investigate GBP pharmacokinetics, blood samples were collected in heparinized tubes up to 36 hours after GBP administration. The urine of the patients was collected up to 36 hours after GBP administration. The intensity of pain was evaluated in each time of blood sampling through the visual analog scale (0-10). In phase II, after 15 days (wash-out) from phase I, cetirizine hydrochloride (10 mg) was administered orally, twice a day, as pills, for five days. On the last day of cetirizine treatment, an oral single dose of gabapentin (300 mg), as capsule, was administered. Serial blood and urine samples were collected up to 36 hours after GBP administration. The intensity of pain was evaluated in each time of blood sampling.

Procedure: Serial Blood Samples; Procedure: Serial Urine Samples; Drug: Gabapentin 300 mg; Drug: Cetirizine Hydrochloride 10 mg

Controlled Diabetes Group

EXPERIMENTAL

Adult patients (18 - 59 years old) with controlled type 2 diabetes (glycated hemoglobin ≤ 8.0%) and diabetic neuropathy of score ≥ 4 that do not use gabapentin were recruited. All patients received oral single dose of gabapentin (300 mg) as capsules after 12 hour-fasting. To investigate GBP pharmacokinetics, blood samples were collected in heparinized tubes up to 36 hours after GBP administration. The urine of the patients was collected up to 36 hours after GBP administration. The intensity of pain was evaluated in each time of blood sampling through the visual analog scale (0-10).

Procedure: Serial Blood Samples; Procedure: Serial Urine Samples; Drug: Gabapentin 300 mg

Uncontrolled Diabetes Group

EXPERIMENTAL

Adult patients (18 - 59 years old) with uncontrolled type 2 diabetes (glycated hemoglobin ≥ 8.0%) and diabetic neuropathy of score ≥ 4 that do not use gabapentin were recruited. All patients received oral single dose of gabapentin (300 mg) as capsules after 12 hour-fasting. To investigate GBP pharmacokinetics, blood samples were collected in heparinized tubes up to 36 hours after GBP administration. The urine of the patients was collected up to 36 hours after GBP administration. The intensity of pain was evaluated in each time of blood sampling through the visual analog scale (0-10).

Procedure: Serial Blood Samples; Procedure: Serial Urine Samples; Drug: Gabapentin 300 mg

Interventions

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.

Control Group; Controlled Diabetes Group; Uncontrolled Diabetes Group

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.

Control Group; Controlled Diabetes Group; Uncontrolled Diabetes Group

Gabapentin 300 mg DRUG

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

Control Group; Controlled Diabetes Group; Uncontrolled Diabetes Group

Cetirizine Hydrochloride 10 mg DRUG

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

Control Group

Eligibility Criteria

• Age: 18 Years - 59 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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)

Sponsors & Collaborators

• Natalia Valadares de Moraes: lead
• University of Sao Paulo: collaborator

MeSH Terms

Conditions

Neuralgia; Diabetes Mellitus, Type 2; Diabetic Neuropathies

Interventions

Gabapentin; Cetirizine

Condition Hierarchy (Ancestors)

Peripheral Nervous System Diseases; Neuromuscular Diseases; Nervous System Diseases; Pain; Neurologic Manifestations; Signs and Symptoms; Pathological Conditions, Signs and Symptoms; Diabetes Mellitus; Glucose Metabolism Disorders; Metabolic Diseases; Nutritional and Metabolic Diseases; Endocrine System Diseases; Diabetes Complications

Intervention Hierarchy (Ancestors)

Amines; Organic Chemicals; gamma-Aminobutyric Acid; Aminobutyrates; Butyrates; Acids, Acyclic; Carboxylic Acids; Cyclohexanecarboxylic Acids; Acids, Carbocyclic; Cyclohexanes; Cycloparaffins; Hydrocarbons, Alicyclic; Hydrocarbons, Cyclic; Hydrocarbons; Amino Acids; Amino Acids, Peptides, and Proteins; Hydroxyzine; Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Design

• Study Type: interventional
• Phase: phase 4
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: OTHER
• Responsible Party: SPONSOR INVESTIGATOR
• PI Title: Assistant Professor

Study Record Dates

• First Submitted: February 2, 2017
• First Posted: February 8, 2017
• Study Start: November 1, 2015
• Primary Completion: May 1, 2018
• Study Completion: July 1, 2019
• Last Updated: July 5, 2019

Record last verified: 2019-07