bupropion and Nausea studies

Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.
bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring.

Nausea: An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.

Research Excerpts

Excerpt	Relevance	Reference
"This study assessed the effects of 32 mg naltrexone sustained release (SR)/360 mg bupropion SR (NB) on body weight in adults with obesity, with comprehensive lifestyle intervention (CLI), for 78 weeks."	9.24	Method-of-use study of naltrexone sustained release (SR)/bupropion SR on body weight in individuals with obesity. ( Fujioka, K; Gilder, K; Halseth, A; Shan, K; Walsh, B, 2017)
"CONTRAVE Obesity Research-II (COR-II) was a double-blind, placebo-controlled study of 1,496 obese (BMI 30-45 kg/m(2) ) or overweight (27-45 kg/m(2) with dyslipidemia and/or hypertension) participants randomized 2:1 to combined naltrexone sustained-release (SR) (32 mg/day) plus bupropion SR (360 mg/day) (NB32) or placebo for up to 56 weeks."	9.17	A randomized, phase 3 trial of naltrexone SR/bupropion SR on weight and obesity-related risk factors (COR-II). ( Apovian, CM; Aronne, L; Burns, C; Dunayevich, E; Kim, D; Rubino, D; Still, C; Wyatt, H, 2013)
"These preliminary results support the feasibility and safety of conducting adequately powered, placebo-controlled efficacy studies of varenicline and bupropion XL for adolescent smoking cessation."	9.16	Varenicline versus bupropion XL for smoking cessation in older adolescents: a randomized, double-blind pilot trial. ( Carpenter, MJ; Gray, KM; Klintworth, EM; Lewis, AL; Upadhyaya, HP, 2012)
"The authors reanalyzed data from the 17 placebo-controlled randomized controlled trials (N=8,027) of varenicline conducted by Pfizer, using complete intent-to-treat person-level longitudinal data to assess smoking abstinence and reports of suicidal thoughts and behavior, depression, aggression/agitation, and nausea and to compare effects in patients with (N=1,004) and without (N=7,023) psychiatric disorders."	7.79	Varenicline, smoking cessation, and neuropsychiatric adverse events. ( Gibbons, RD; Mann, JJ, 2013)
"This study assessed the effects of 32 mg naltrexone sustained release (SR)/360 mg bupropion SR (NB) on body weight in adults with obesity, with comprehensive lifestyle intervention (CLI), for 78 weeks."	5.24	Method-of-use study of naltrexone sustained release (SR)/bupropion SR on body weight in individuals with obesity. ( Fujioka, K; Gilder, K; Halseth, A; Shan, K; Walsh, B, 2017)
"CONTRAVE Obesity Research-II (COR-II) was a double-blind, placebo-controlled study of 1,496 obese (BMI 30-45 kg/m(2) ) or overweight (27-45 kg/m(2) with dyslipidemia and/or hypertension) participants randomized 2:1 to combined naltrexone sustained-release (SR) (32 mg/day) plus bupropion SR (360 mg/day) (NB32) or placebo for up to 56 weeks."	5.17	A randomized, phase 3 trial of naltrexone SR/bupropion SR on weight and obesity-related risk factors (COR-II). ( Apovian, CM; Aronne, L; Burns, C; Dunayevich, E; Kim, D; Rubino, D; Still, C; Wyatt, H, 2013)
"These preliminary results support the feasibility and safety of conducting adequately powered, placebo-controlled efficacy studies of varenicline and bupropion XL for adolescent smoking cessation."	5.16	Varenicline versus bupropion XL for smoking cessation in older adolescents: a randomized, double-blind pilot trial. ( Carpenter, MJ; Gray, KM; Klintworth, EM; Lewis, AL; Upadhyaya, HP, 2012)
"Outpatients with moderate to severe major depressive disorder (DSM-IV) received bupropion SR (100-300 mg/day) or sertraline (50-200 mg/day) for 16 weeks."	5.08	Double-blind comparison of bupropion sustained release and sertraline in depressed outpatients. ( Ascher, JA; Hughes, AR; Johnston, JA; Kavoussi, RJ; Segraves, RT, 1997)
"In this global health case study, we describe a case of nicotine addiction due to chronic use of electronic cigarettes (e-cigarette) and discuss the beliefs on safety and awareness of their side effects."	3.88	Beliefs and reality of e-cigarette smoking. ( Inzamam Ali, M; Menakuru, S, 2018)
"The authors reanalyzed data from the 17 placebo-controlled randomized controlled trials (N=8,027) of varenicline conducted by Pfizer, using complete intent-to-treat person-level longitudinal data to assess smoking abstinence and reports of suicidal thoughts and behavior, depression, aggression/agitation, and nausea and to compare effects in patients with (N=1,004) and without (N=7,023) psychiatric disorders."	3.79	Varenicline, smoking cessation, and neuropsychiatric adverse events. ( Gibbons, RD; Mann, JJ, 2013)
"The incidence of seizures after unintentional bupropion ingestion in children aged < 6 years has been reported as 0."	3.76	Unintentional ingestion of bupropion in children. ( Baker, SD; Beuhler, M; Bosse, GM; Gray, T; Spiller, HA, 2010)
"Unintentional bupropion pediatric exposures uncommonly report severe clinical effects such as seizures."	3.76	The outcome of unintentional pediatric bupropion ingestions: a NPDS database review. ( Beuhler, MC; Sasser, HC; Spiller, HA, 2010)
"Bupropion was studied in four double-blind, placebo-controlled trials (N = 360) at dosages of 300-750 mg/day."	2.65	Methodologic approach to adverse events applied to bupropion clinical trials. ( Cato, AE; Cook, L; Heatherington, D; Starbuck, R, 1983)
"For a population with a yearly recurrence rate of 30%, the NNTB is 8 (95% CI 6 to 12)."	2.61	Second-generation antidepressants for preventing seasonal affective disorder in adults. ( Forneris, CA; Gartlehner, G; Gaynes, BN; Greenblatt, A; Lux, LJ; Morgan, LC; Nussbaumer-Streit, B; Van Noord, MG; Winkler, D; Wipplinger, J, 2019)
"Bupropion is a cytochrome p450 2D6 inhibitor and care must be taken when coprescribing with drugs cleared by this enzyme and when coprescribing with drugs that lower seizure threshold."	2.43	Bupropion. ( Wilkes, S, 2006)
" Potential pharmacokinetic advantages of these formulations include lower peak plasma drug concentrations and smaller fluctuations between peak and trough plasma drug concentrations, which might influence the tolerability of these medications."	2.42	Immediate-release versus controlled-release formulations: pharmacokinetics of newer antidepressants in relation to nausea. ( DeVane, CL, 2003)
"Study data demonstrate that seizure incidence, which is a concern with high-dose IR, is substantially lower with the new SR formulation."	2.40	Bupropion sustained release: side effect profile. ( Settle, EC, 1998)

Research

Studies (17)

Authors

Clinical Trials (2)

Trial Overview

Trial Outcomes

Body Weight- Mean Percent Change From Baseline to Week 56

Timeframe	Studies, this research(%)	All Research%
pre-1990	1 (5.88)	18.7374
1990's	2 (11.76)	18.2507
2000's	4 (23.53)	29.6817
2010's	10 (58.82)	24.3611
2020's	0 (0.00)	2.80

Authors	Studies
Ahn, BJ	1
Kwon, KY	1
Menakuru, S	1
Inzamam Ali, M	1
Gartlehner, G	1
Nussbaumer-Streit, B	1
Gaynes, BN	1
Forneris, CA	1
Morgan, LC	1
Greenblatt, A	1
Wipplinger, J	1
Lux, LJ	1
Van Noord, MG	1
Winkler, D	1
Apovian, CM	1
Aronne, L	1
Rubino, D	1
Still, C	1
Wyatt, H	1
Burns, C	1
Kim, D	1
Dunayevich, E	1
Gibbons, RD	1
Mann, JJ	1
Hong, K	1
Herrmann, K	1
Dybala, C	1
Halseth, AE	1
Lam, H	1
Foreyt, JP	1
Halseth, A	1
Shan, K	1
Walsh, B	1
Gilder, K	1
Fujioka, K	1
Spiller, HA	2
Bosse, GM	1
Beuhler, M	1
Gray, T	1
Baker, SD	1
Beuhler, MC	1
Sasser, HC	1
Gray, KM	1
Carpenter, MJ	1
Lewis, AL	1
Klintworth, EM	1
Upadhyaya, HP	1
DeVane, CL	1
Wilkes, S	1
Menza, MA	1
Dobkin, RD	1
Marin, H	1
Cato, AE	1
Cook, L	1
Starbuck, R	1
Heatherington, D	1
Kavoussi, RJ	1
Segraves, RT	1
Hughes, AR	1
Ascher, JA	1
Johnston, JA	1
Settle, EC	1
Lara, DR	1
Busnello, ED	1
Souza, DO	1

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Multicenter, Randomized, Double Blind, Placebo Controlled Study Comparing the Safety and Efficacy of Naltrexone Sustained Release (SR)/Bupropion Sustained Release (SR) and Placebo in Obese Subjects[NCT00567255]	Phase 3	1,496 participants (Actual)	Interventional	2007-12-31	Completed
A Multicenter, Randomized, Open-Label, Controlled, Method-of-Use Study Assessing the Effect of Naltrexone Sustained Release (SR)/Bupropion SR on Body Weight and Cardiovascular Risk Factors in Overweight and Obese Subjects (The Ignite Study)[NCT01764386]	Phase 3	242 participants (Actual)	Interventional	2013-02-28	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

"Beginning at Week 28 through Week 44, NB32-treated subjects who failed to achieve or maintain at least 5% body weight loss from baseline were re-randomized (1:1 ratio) to continue NB32 or begin treatment with a higher dose of naltrexone SR - naltrexone SR 48 mg/bupropion SR 360 mg (referred to as NB48) (daily dose of bupropion SR was 360 mg for NB32 and NB48).The analysis of NB32 vs. placebo at Week 56 was completed using a weighted analysis. This analysis was referred to as the weighted LOCF analysis.~Subjects treated with NB32 who were re-randomized to NB48 were not included. Subjects re-randomized to NB32 were double-weighted and subjects who were not re-randomized were single-weighted. Subjects in the placebo group were single-weighted. The double weighting analysis restored the influence of poor performers at Weeks 28 to 44 in the NB32 group without including any data from the higher dose group (NB48)." (NCT00567255)
Timeframe: Baseline, 56 weeks

Body Weight- Proportion of Subjects With ≥10% Decrease From Baseline to Week 28

Body Weight- Proportion of Subjects With ≥5% Decrease From Baseline to Week 56

Intervention	percentage of body weight (Least Squares Mean)
NB32	-6.40
Placebo	-1.23

Intervention	percentage of participants (Number)
NB32	27.27
Placebo	7.02

Change in Diastolic Blood Pressure

Change in Fasting Blood Glucose Levels

Change in Fasting HDL Cholesterol Levels

Change in Fasting Insulin Levels, Using Log-transformed Data

Change in Fasting LDL Cholesterol Levels

Change in Fasting Triglycerides Levels, Using Log-transformed Data

Change in Food Craving Inventory Carbohydrates Subscale Score

Intervention	percentage of participants (Number)
NB32	50.48
Placebo	17.11

Intervention	mm Hg (Least Squares Mean)
NB32	0.20
Placebo	-0.67

Intervention	mg/dL (Least Squares Mean)
NB32	-2.11
Placebo	-1.73

Intervention	mg/dL (Least Squares Mean)
NB32	1.19
Placebo	-1.40

Intervention	percent change (Least Squares Mean)
NB32	-14.14
Placebo	-0.50

Intervention	mg/dL (Least Squares Mean)
NB32	-4.36
Placebo	0.00

Intervention	percent change (Least Squares Mean)
NB32	-7.32
Placebo	-1.36

The Food Craving Inventory is a 33-item self-report measure designed to assess specific food cravings and is organized into 4 subscales (high fats, sweets, carbohydrates/starches, and fast-food fats). A craving was defined as an intense desire to consume a particular food (or food type) that was difficult to resist over the past month. Subjects rated their frequency of cravings for each of the 33 items using a 5-point scale, where 1=never, 2=rarely, 3=sometimes, 4=often, and 5=always. The carbohydrates subscale consisted of 8 items and the score ranges from 8 (better outcome) to 40 (worse outcome). (NCT00567255)
Timeframe: Baseline, 28 weeks

Change in Food Craving Inventory Sweets Subscale Score

Intervention	units on a scale (Least Squares Mean)
NB32	-2.68
Placebo	-2.20

The Food Craving Inventory is a 33-item self-report measure designed to assess specific food cravings and is organized into 4 subscales (high fats, sweets, carbohydrates/starches, and fast-food fats). A craving was defined as an intense desire to consume a particular food (or food type) that was difficult to resist over the past month. Subjects rated their frequency of cravings for each of the 33 items using a 5-point scale, where 1=never, 2=rarely, 3=sometimes, 4=often, and 5=always. The sweets subscale consisted of 8 items and the score ranges from 8 (better outcome) to 40 (worse outcome). (NCT00567255)
Timeframe: Baseline, 28 weeks

Change in High-sensitivity C Reactive Protein (Hs-CRP) Levels, Using Log-transformed Data

Change in HOMA-IR Levels, Using Log-transformed Data

Intervention	units on a scale (Least Squares Mean)
NB32	-3.20
Placebo	-3.18

Intervention	percent change (Least Squares Mean)
NB32	-9.38
Placebo	-1.14

HOMA-IR= Homeostasis Model Assessment-Insulin Resistance (NCT00567255)
Timeframe: Baseline, 28 weeks

Change in IDS-SR Total Score

Intervention	percent change (Least Squares Mean)
NB32	-16.44
Placebo	-4.15

IDS-SR= Inventory of Depressive Symptoms-Subject Rated IDS-SR total score is based on 30 items. The total score can range from 0-84, with 0 being no depressive symptoms and 84 being very severe depressive symptoms. A total score ≤ 13 indicates no depression. (NCT00567255)
Timeframe: Baseline, 28 weeks

Change in IWQOL-Lite Total Scores

Intervention	units on a scale (Least Squares Mean)
NB32	-0.23
Placebo	-0.28

IWQOL-Lite= Impact of Weight on Quality of Life-Lite Questionnaire Total score is based on a scale from 0 to 100, with 0 representing the poorest and 100 the best quality of life and where a score of 71-79 indicates moderate impairment (NCT00567255)
Timeframe: Baseline, 28 weeks

Change in Question 19 From 21-Item COE (Control of Eating) Questionnaire

Intervention	units on a scale (Least Squares Mean)
NB32	9.94
Placebo	6.17

Question 19: Generally, how difficult has it been to control your eating? Scoring: 0=not at all difficult; 100=extremely difficult (NCT00567255)
Timeframe: Baseline, 28 weeks

Change in Systolic Blood Pressure

Change in Waist Circumference

Co-primary: Body Weight- Mean Percent Change From Baseline to Week 28

Co-primary: Body Weight- Proportion of Subjects With ≥5% Decrease From Baseline to Week 28

Absolute Change in Body Weight From Baseline to Week 26

Change Fasting Insulin From Baseline to Week 26

Change in Diastolic Blood Pressure From Baseline to Week 26

Change in Fasting High-density Lipoprotein Cholesterol From Baseline to Week 26

Change in Fasting Low-density Lipoprotein Cholesterol From Baseline to Week 26

Change in Fasting Plasma Glucose From Baseline to Week 26

Change in Fasting Triglycerides From Baseline to Week 26

Change in Heart Rate From Baseline to Week 26

Change in Homeostasis Model Assessment-insulin Resistance (HOMA-IR) From Baseline to Week 26

Intervention	units on a scale (Least Squares Mean)
NB32	-18.32
Placebo	-11.09

Intervention	mm Hg (Least Squares Mean)
NB32	-0.93
Placebo	-1.23

Intervention	cm (Least Squares Mean)
NB32	-6.16
Placebo	-2.74

Intervention	percentage of body weight (Least Squares Mean)
NB32	-6.45
Placebo	-1.89

Intervention	percentage of participants (Number)
NB32	55.64
Placebo	17.54

Intervention	kg (Least Squares Mean)
NB + CLI	-9.7
Usual Care	-1.0

Intervention	uIU/mL (Least Squares Mean)
NB + CLI	-7.5
Usual Care	-3.4

Intervention	mm Hg (Least Squares Mean)
NB + CLI	-1.7
Usual Care	-1.3

Intervention	mg/dL (Least Squares Mean)
NB + CLI	4.1
Usual Care	0.1

Intervention	mg/dL (Least Squares Mean)
NB + CLI	-2.0
Usual Care	-1.9

Intervention	mg/dL (Least Squares Mean)
NB + CLI	-2.9
Usual Care	1.6

Intervention	mg/dL (Least Squares Mean)
NB + CLI	-13.6
Usual Care	2.8

Intervention	bpm (Least Squares Mean)
NB + CLI	1.7
Usual Care	-0.3

HOMA-IR is an insulin sensitivity index that is calculated as HOMA-IR = (Glucose * Insulin) / 405, where glucose is in mass units (mg/dL) and insulin is in µIU/mL. Higher values indicate lower insulin sensitivity. (NCT01764386)
Timeframe: Baseline to Week 26

Change in Patient-reported Arizona Sexual Experiences Scale (ASEX) Total Scores From Baseline to Week 26

Intervention	units on a scale (Least Squares Mean)
NB + CLI	-2.0
Usual Care	-0.8

Arizona Sexual Experiences (ASEX) scale is a 5-item rating scale that quantifies sex drive, arousal, vaginal lubrication/penile erection, ability to reach orgasm, and satisfaction from orgasm. Possible total scores range from 5 to 30, with the higher scores indicating more sexual dysfunction. (NCT01764386)
Timeframe: Baseline to Week 26

Change in Patient-reported Binge Eating Scale (BES) Total Scores From Baseline to Week 26

Intervention	units on a scale (Least Squares Mean)
NB + CLI	-2.2
Usual Care	-0.1

The BES is a 16-item questionnaire that identifies different levels of binge-eating severity, with total scores ranging between 0-46. BES scores were categorized as follows: None = Scores ≤17 indicated no significant binge eating, Moderate = scores from 18 to 26 (inclusive), Severe = scores ≥27 indicated severe levels of binge eating. (NCT01764386)
Timeframe: Baseline to Week 26

Change in Patient-reported Impact of Weight on Quality of Life-Lite Questionnaire (IWQOL-Lite) Total Score From Baseline to Week 26

Intervention	units on a scale (Least Squares Mean)
NB + CLI	-6.8
Usual Care	1.1

Impact of Weight on Quality of Life-Lite Questionnaire (IWQOL-Lite) is a self-reported assessment of perceived effect of weight on quality of life. It consists of 31 items organized in 5 domains (physical function, self-esteem, sexual life, public distress and work). IWQOL-Lite total score is based on a scale from 0 to 100, with 0 representing the poorest and 100 the best quality of life and where a score of 71-79 indicates moderate impairment. (NCT01764386)
Timeframe: Baseline to Week 26

Article	Year
Second-generation antidepressants for preventing seasonal affective disorder in adults. The Cochrane database of systematic reviews, 2019, 03-18, Volume: 3 Topics: Adult; Antidepressive Agents, Second-Generation; Bupropion; Diarrhea; Headache; Humans; Incidence; N	2019
Immediate-release versus controlled-release formulations: pharmacokinetics of newer antidepressants in relation to nausea. The Journal of clinical psychiatry, 2003, Volume: 64 Suppl 18 Topics: Antidepressive Agents; Bupropion; Cyclohexanols; Delayed-Action Preparations; Drug Tolerance; Half-L	2003
Bupropion. Drugs of today (Barcelona, Spain : 1998), 2006, Volume: 42, Issue:10 Topics: Antidepressive Agents, Second-Generation; Bupropion; Dizziness; Headache; Humans; Models, Biological	2006
Bupropion sustained release: side effect profile. The Journal of clinical psychiatry, 1998, Volume: 59 Suppl 4 Topics: Antidepressive Agents, Second-Generation; Antidepressive Agents, Tricyclic; Bupropion; Delayed-Actio	1998

Article	Year
A randomized, phase 3 trial of naltrexone SR/bupropion SR on weight and obesity-related risk factors (COR-II). Obesity (Silver Spring, Md.), 2013, Volume: 21, Issue:5 Topics: Adult; Anti-Obesity Agents; Bupropion; Cardiovascular Diseases; Delayed-Action Preparations; Dopamin	2013
Naltrexone/Bupropion extended release-induced weight loss is independent of nausea in subjects without diabetes. Clinical obesity, 2016, Volume: 6, Issue:5 Topics: Adult; Anti-Obesity Agents; Body Mass Index; Bupropion; Combined Modality Therapy; Delayed-Action Pr	2016
Method-of-use study of naltrexone sustained release (SR)/bupropion SR on body weight in individuals with obesity. Obesity (Silver Spring, Md.), 2017, Volume: 25, Issue:2 Topics: Adolescent; Adult; Body Weight; Bupropion; Delayed-Action Preparations; Dopamine Uptake Inhibitors;	2017
Varenicline versus bupropion XL for smoking cessation in older adolescents: a randomized, double-blind pilot trial. Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco, 2012, Volume: 14, Issue:2 Topics: Adolescent; Benzazepines; Bupropion; Double-Blind Method; Female; Humans; Male; Nausea; Pilot Projec	2012
An open-label trial of aripiprazole augmentation for treatment-resistant generalized anxiety disorder. Journal of clinical psychopharmacology, 2007, Volume: 27, Issue:2 Topics: Adolescent; Adult; Aged; Akathisia, Drug-Induced; Antidepressive Agents, Second-Generation; Antipsyc	2007
Methodologic approach to adverse events applied to bupropion clinical trials. The Journal of clinical psychiatry, 1983, Volume: 44, Issue:5 Pt 2 Topics: Akathisia, Drug-Induced; Antidepressive Agents; Bupropion; Clinical Trials as Topic; Depressive Diso	1983
Double-blind comparison of bupropion sustained release and sertraline in depressed outpatients. The Journal of clinical psychiatry, 1997, Volume: 58, Issue:12 Topics: 1-Naphthylamine; Adolescent; Adult; Aged; Ambulatory Care; Antidepressive Agents; Bupropion; Delayed	1997

Article	Year
Elderly woman presenting with unusual propriospinal myoclonus triggered by drug-induced nausea and vomiting. Geriatrics & gerontology international, 2018, Volume: 18, Issue:3 Topics: Aged, 80 and over; Alzheimer Disease; Bupropion; Dopamine Agents; Dopamine Uptake Inhibitors; Female	2018
Beliefs and reality of e-cigarette smoking. BMJ case reports, 2018, Oct-02, Volume: 2018 Topics: Adult; Antidepressive Agents, Second-Generation; Bupropion; Chills; Depressive Disorder; Electronic	2018
Varenicline, smoking cessation, and neuropsychiatric adverse events. The American journal of psychiatry, 2013, Volume: 170, Issue:12 Topics: Adult; Aggression; Akathisia, Drug-Induced; Benzazepines; Bupropion; Depression; Female; Humans; Mal	2013
Unintentional ingestion of bupropion in children. The Journal of emergency medicine, 2010, Volume: 38, Issue:3 Topics: Bupropion; Child, Preschool; Dopamine Uptake Inhibitors; Female; Hallucinations; Humans; Hypertensio	2010
The outcome of unintentional pediatric bupropion ingestions: a NPDS database review. Journal of medical toxicology : official journal of the American College of Medical Toxicology, 2010, Volume: 6, Issue:1 Topics: Accidents; Adrenergic Uptake Inhibitors; Adverse Drug Reaction Reporting Systems; Affect; Age Factor	2010
Ondansetron rather than metoclopramide for bupropion-induced nausea. Canadian journal of psychiatry. Revue canadienne de psychiatrie, 2001, Volume: 46, Issue:4 Topics: Adult; Antiemetics; Bupropion; Depressive Disorder; Drug Interactions; Female; Humans; Metoclopramid	2001

bupropion and Nausea