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Pharmacogenetics of Bupropion Metabolism

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT00791869
Recruitment Status : Completed
First Posted : November 17, 2008
Last Update Posted : May 22, 2013
Information provided by (Responsible Party):
University of California, San Francisco

Brief Summary:
The aim of the investigators research is to see if variants in a particular gene (named CYP2B6) affect how the body metabolizes (breaks down) certain medications, including the drug bupropion. Bupropion is widely used in the treatment of depression and for helping people quit smoking. Genes are portions of DNA that code for particular proteins in the body. The investigators are studying the gene that codes for a protein called CYP2B6. Differences in the structure of the gene are called variants and may mean that a person metabolizes a drug faster or slower than a person with a different variant.

Condition or disease
Metabolism Pharmacokinetics

Detailed Description:

Bupropion is widely used in the treatment of depression and for smoking cessation. It's most abundant metabolite, hydroxybupropion, may be responsible for most of the therapeutic effect of bupropion under conditions of long term dosing. Because the primary enzyme involved in metabolism of bupropion to hydroxybupropion is the liver enzyme CYP2B6, we propose to study the effect of different CYP2B6 genotypes on the metabolism of bupropion. These data will guide the use of genotypes as a surrogate for measuring drug blood levels in studying genetic determinants of outcomes for bupropion treatment.

A minimum of Forty-four subjects with 4 different CYP2B6 genotypes will participate in a 7-day study in which they take bupropion as outpatients for 6 days (to achieve steady state drug levels) and then come to the San Francisco General Hospital (SFGH) Clinical Research Center for a 1-day admission during which multiple blood and urine samples will be collected for pharmacokinetic analysis.

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Study Type : Observational
Actual Enrollment : 43 participants
Observational Model: Case-Only
Time Perspective: Cross-Sectional
Official Title: Pharmacogenetics of Bupropion Metabolism
Study Start Date : June 2008
Actual Primary Completion Date : March 2010
Actual Study Completion Date : November 2010

Resource links provided by the National Library of Medicine

Drug Information available for: Bupropion

Primary Outcome Measures :
  1. Area under the plasma concentration versus time curve (AUC) for bupropion [ Time Frame: 0, 4, 8, 12, 16,24 hours from steady state ]
    Subjects took bupropion daily for 7 days as outpatients prior to the study day to allow them to reach steady state concentrations of bupropion and its metabolites. The time frame shown is measured from 08:00 on the morning of inpatient admission.

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 65 Years   (Adult, Older Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes
Sampling Method:   Non-Probability Sample
Study Population
Healthy subjects with selected CYP2B6 genotypes.

Inclusion Criteria:

  • Age: 18 - 65 years
  • Gender: Either
  • Ethnic/Racial Group: Any
  • Smoking Status: Both smokers and non-smokers are eligible
  • CYP2B6 genotype: CYP2B6 *1/*1 (11 subjects); *4, *5 and *6 alleles (11 each) [44 subjects total] Up to 15 additional subjects may be studied with genotypes that do not fall into one of the primary groups.

Exclusion Criteria:

  • Medical: Exclude most any chronic illness requiring regular medication.
  • Cardiac: History of angina or other serious heart disease; ECG abnormalities on screening.
  • Hypertension: screening visit BP of 150/95 or more after 5 min rest
  • Respiratory: Asthma - acceptable if in remission, otherwise exclude.
  • Systemic: "Morbidly Obese" Exclude if BMI > 35
  • Diabetes: By history
  • Chronic Active Hepatitis: By history; elevated Liver Function Tests
  • Cancers: By history
  • Pregnancy/breastfeeding: By history; positive urine pregnancy test
  • Seizures: individuals with a history of seizures will be excluded (risk factor for bupropion-induced seizures)
  • Eating Disorders: individuals with a history of eating disorders will be excluded (risk factor for bupropion-induced seizures)
  • Head Trauma: individuals with a history of head trauma will be excluded (risk factor for bupropion-induced seizures)
  • Other tobacco users (pipe, cigar, chewing tobacco, snuff users
  • Medications/Supplements: General Exclusion = "any regular oral and/or prescription drug use"; current use of oral contraceptives or other female hormones.
  • Drug/alcohol use: no alcohol abuse by history, no regular recreational drug use, any intravenous drug abuse, recent history of Treatment program

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 identifier (NCT number): NCT00791869

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United States, California
San Francisco General Hospital-Clinical Research Ward
San Francisco, California, United States, 94110
Sponsors and Collaborators
University of California, San Francisco
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Principal Investigator: Neal L Benowitz, MD University of California, San Francisco
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Responsible Party: University of California, San Francisco Identifier: NCT00791869    
Other Study ID Numbers: H133-31868
U01DA020830 ( U.S. NIH Grant/Contract )
First Posted: November 17, 2008    Key Record Dates
Last Update Posted: May 22, 2013
Last Verified: May 2013
Keywords provided by University of California, San Francisco:
Pharmacokinetics of bupropion