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Bupropion Stereoselective Disposition and CYP2D6-mediated Drug Interactions in Healthy Volunteers

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ClinicalTrials.gov Identifier: NCT03420469
Recruitment Status : Recruiting
First Posted : February 2, 2018
Last Update Posted : July 23, 2018
Sponsor:
Collaborator:
National Institute of General Medical Sciences (NIGMS)
Information provided by (Responsible Party):
Zeruesenay Desta, Indiana University

Brief Summary:

Primary objectives:

  1. To comprehensively characterize steady state stereoselective pharmacokinetics of bupropion and its primary and secondary metabolites in healthy volunteers
  2. To prospectively determine the time course (onset), extent and offset of CYP2D6 inhibition in relation to the pharmacokinetic profiles of bupropion and metabolites.

Condition or disease Intervention/treatment Phase
Adverse Effect of Drug Therapy Metabolism Medications (Diagnosis) Drug: Bupropion Not Applicable

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Study Type : Interventional  (Clinical Trial)
Estimated Enrollment : 29 participants
Intervention Model: Sequential Assignment
Intervention Model Description: This is an open-label, four-phases, fixed sequence healthy volunteers study investigating: the steady state stereoselective disposition of bupropion and metabolites; and effect of multiple doses of bupropion on CYP2D6 activity, as measured by the metabolism and pharmacokinetics of a single dose of dextromethorphan
Masking: None (Open Label)
Primary Purpose: Basic Science
Official Title: Bupropion Stereoselective Disposition and CYP2D6-mediated Drug Interactions in Healthy Volunteers
Actual Study Start Date : June 5, 2018
Estimated Primary Completion Date : May 1, 2020
Estimated Study Completion Date : May 1, 2020

Resource links provided by the National Library of Medicine

MedlinePlus related topics: Drug Reactions

Arm Intervention/treatment
Experimental: Single Group
CYP2D6 activity will be determined on three occasions using a single oral dose of dextromethorphan (30 mg PO) as a probe drug: 1) at baseline (control); 2) with a single dose of bupropion (150 mg PO) (single dose inhibition); and 3) after 14 days pretreatment with bupropion (150 mg twice daily PO) (multiple dose inhibition). Single dose and steady state pharmacokinetics of bupropion will also be determined.
Drug: Bupropion
Phase 1: Baseline CYP2D6 activity, using dextromethorphan (30 mg single dose PO) as a probe drug Phase 2: Single dose bupropion pharmacokinetics and its effect on CYP2D6 activity (determined by dextromethorphan 30 mg single dose PO) Phase 3: Bupropion treatment to steady state (150 mg twice daily for 14 days PO) Phase 4: Steady state disposition of bupropion and its interaction with CYP2D6 activity (30 mg single dose PO)




Primary Outcome Measures :
  1. Exposure [ Time Frame: Through study completion, an average of 2 year ]
    Area under the plasma concentration versus time curves (AUC0-inf) of bupropion and its metabolites as well as CYP2D6 activity measured by dextromethorphan to dextrorphan



Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Male and female (approximately 1:1) volunteers between the age of 18 and 55 years old and within 32% of your ideal body weight.
  • Judged healthy without any significant medical condition as determined by and decided from a pre-enrollment screening session that include medical history, laboratory tests such as blood and urine tests, and an electrical tracing of the heart beat (electrocardiogram, EKG).
  • Individuals who agree to refrain from taking any prescriptions medications, over-the-counter medications, and herbal, dietary, and alternative supplements that may interact with the metabolism of those study drugs at least 2 weeks prior to the start of the study and until study completion.
  • Nonsmoker or individuals willing to refrain from smoking or use of tobacco or marijuana for at least two weeks prior to and until the completion of the study (the entire study lasts for approximately 32 days).
  • Willing to commit the time requested for this study

Exclusion Criteria:

Subjects will be excluded from the study if they:

  • Are underweight (weigh less than 52 kg or 114 lb) or overweight [body mass index (BMI) greater than 32].
  • Have laboratory results that do not fall in a healthy range (e.g., blood hemoglobin less than 12.0 mg/dl).
  • Have baseline EKG readings that are abnormal that could place the patient at the higher risk as decided by the study medical doctor (MD)
  • Have history of intolerance, allergic reactions (e.g. rash) or other forms of hypersensitivities to any of the study medications (dextromethorphan and bupropion).
  • Have current alcohol (more than 4 alcoholic drinks per day on a regular basis) or drug abuse.
  • Have history or current gastrointestinal (digestive) disorders such as persistent diarrhea or malabsorption that would interfere with the absorption of orally administered drugs
  • Have history or current seizures, hypertension and heart disease or any other cardiovascular disorders
  • Have history or current psychiatric (mental or brain) disorders (e.g., feeling sad or unhappy, loss of interest in normal activities, worried) such as depression, anxiety, or suicidality or suicide attempts.
  • Have significantly compromised liver and/or kidney functions.
  • Have participated in a research study involving intensive blood sampling or have donated blood within the past two months
  • Are unable or unwilling to stop taking other substances that may interfere with the metabolism of the study drugs (bupropion and dextromethorphan) two weeks prior to and during the entire study period, including prescription medications, over-the-counter medications, herbal or dietary supplements, and alternative medicines.
  • Are employees or students under supervision of any of the study investigators.
  • Cannot state a good understanding of this study including risks and requirements; are unable to follow the rules of this study.
  • Cannot commit the time requested for this study.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT03420469


Contacts
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Contact: Zeruesenay Desta 3172742823 zdesta@iu.edu

Locations
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United States, Indiana
Indiana Clinical Research Center (ICRC) Recruiting
Indianapolis, Indiana, United States, 46202
Contact: Zeruesenay Desta, PhD    317-274-2823    zdesta@iu.edu   
Principal Investigator: Zeruesenay Desta, PhD         
Sponsors and Collaborators
Indiana University
National Institute of General Medical Sciences (NIGMS)

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Responsible Party: Zeruesenay Desta, Professor of Medicine, Pharmacology and Toxicology, Indiana University
ClinicalTrials.gov Identifier: NCT03420469     History of Changes
Other Study ID Numbers: 1R01GM121707-01A1 ( U.S. NIH Grant/Contract )
First Posted: February 2, 2018    Key Record Dates
Last Update Posted: July 23, 2018
Last Verified: July 2018
Individual Participant Data (IPD) Sharing Statement:
Plan to Share IPD: No

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Studies a U.S. FDA-regulated Drug Product: No
Studies a U.S. FDA-regulated Device Product: No

Additional relevant MeSH terms:
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Drug-Related Side Effects and Adverse Reactions
Chemically-Induced Disorders
Bupropion
Dextromethorphan
Antidepressive Agents, Second-Generation
Antidepressive Agents
Psychotropic Drugs
Dopamine Uptake Inhibitors
Neurotransmitter Uptake Inhibitors
Membrane Transport Modulators
Molecular Mechanisms of Pharmacological Action
Dopamine Agents
Neurotransmitter Agents
Physiological Effects of Drugs
Cytochrome P-450 CYP2D6 Inhibitors
Cytochrome P-450 Enzyme Inhibitors
Enzyme Inhibitors
Antitussive Agents
Respiratory System Agents
Excitatory Amino Acid Antagonists
Excitatory Amino Acid Agents