BUPROPION MALEATE

First approved in 1985

Details

Stereochemistry	RACEMIC
Molecular Formula	C13H18ClNO.C4H4O4
Molecular Weight	355.813
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C/C(O)=O.CC(NC(C)(C)C)C(=O)C1=CC(Cl)=CC=C1

InChI

InChIKey=NJJFBMJGOYCQCX-BTJKTKAUSA-N

InChI=1S/C13H18ClNO.C4H4O4/c1-9(15-13(2,3)4)12(16)10-6-5-7-11(14)8-10;5-3(6)1-2-4(7)8/h5-9,15H,1-4H3;1-2H,(H,5,6)(H,7,8)/b;2-1-

HIDE SMILES / InChI

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Molecular Formula	C13H18ClNO
Molecular Weight	239.741
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/018644s039s040.pdf | http://www.emedexpert.com/facts/bupropion-facts.shtml
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB01156 | http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm103318.htm

Bupropion, an antidepressant of the aminoketone class and a non-nicotine aid to smoking cessation, is chemically unrelated to tricyclic, tetracyclic, selective serotonin re-uptake inhibitor, or other known antidepressant agents. Compared to classical tricyclic antidepressants, Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine, serotonin, and dopamine. In addition, Bupropion does not inhibit monoamine oxidase. Bupropion produces dose-related central nervous system (CNS) stimulant effects in animals, as evidenced by increased locomotor activity, increased rates of responding in various schedule-controlled operant behavior tasks, and, at high doses, induction of mild stereotyped behavior. Bupropion is marketed as Wellbutrin, Zyban, and generics. Bupropion is indicated for the treatment of major depressive disorder (MDD). WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL are not approved for smoking cessation treatment, but bupropion under the name ZYBAN is approved for this use.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dopamine transporter 172 Target ID: CHEMBL238 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/018644s039s040.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/19497387 \| https://www.ncbi.nlm.nih.gov/pubmed/9862757	Inhibitor 8146		550.0 nM [IC50]
Norepinephrine transporter 183 Target ID: CHEMBL222 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/018644s039s040.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/19497387 \| https://www.ncbi.nlm.nih.gov/pubmed/9862757	Inhibitor 8146		443.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Major depressive disorder 172 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/018644s039s040.pdf	Primary		Approved 8307	WELLBUTRIN Approved Use INDICATIONS & USAGE Major Depressive Disorder:Bupropion hydrochloride extended-release tablets (XL) are indicated for the treatment of major depressive disorder. The efficacy of bupropion in the treatment of a major depressive episode was established in two 4-week controlled trials of inpatients and in one 6-week controlled trial of outpatients whose diagnoses corresponded most closely to the Major Depression category of the APA Diagnostic and Statistical Manual (DSM) (seeCLINICAL TRIALS). A major depressive episode (DSM-IV) implies the presence of 1) depressed mood or 2) loss of interest or pleasure; in addition, at least 5 of the following symptoms have been present during the same 2-week period and represent a change from previous functioning: depressed mood, markedly diminished interest or pleasure in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, a suicide attempt, or suicidal ideation. The efficacy of bupropion in maintaining an antidepressant response for up to 44 weeks following 8 weeks of acute treatment was demonstrated in a placebo-controlled trial with the sustained-release formulation of bupropion (seeCLINICAL TRIALS). Nevertheless, the physician who elects to use bupropion hydrochloride extended-release tablets (XL) for extended periods should periodically reevaluate the long-term usefulness of the drug for the individual patient. Seasonal Affective Disorder:Bupropion hydrochloride extended-release tablets (XL) are indicated for the prevention of seasonal major depressive episodes in patients with a diagnosis of seasonal affective disorder. The efficacy of bupropion hydrochloride extended-release tablets (XL) for the prevention of seasonal major depressive episodes was established in 3 controlled trials of adult outpatients with a history of major depressive disorder with an autumn-winter seasonal pattern as defined by Diagnostic and Statistical Manual of Mental Disorders, 4th edition (DSM-IV) criteria (seeCLINICAL TRIALS). Seasonal affective disorder is characterized by recurrent major depressive episodes, most commonly occurring during the autumn and/or winter months. Episodes may last up to 6 months in duration, typically beginning in the autumn and remitting in the springtime. Although patients with seasonal affective disorder may have depressive episodes during other times of the year, the diagnosis of seasonal affective disorder requires that the number of seasonal episodes substantially outnumber the number of non-seasonal episodes during the individual's lifetime. Launch Date 5.04748802E11
Nicotine dependence 32 Sources: https://www.drugs.com/pro/zyban.html http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020711s034REMSZyban.pdf	Primary		Approved 8307	ZYBAN Approved Use Zyban is indicated as an aid to smoking cessation treatment. Launch Date 5.04748802E11

C_max

Value	Dose	Analyte	Population
134 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28685396	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BUPROPION plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
93 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28685396	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
136 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020711s026lbl.pdf	150 mg 2 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
91 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020711s026lbl.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
688 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28685396	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		BUPROPION plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
469 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28685396	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:		BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
10 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28685396	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BUPROPION plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28685396	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
21 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020711s026lbl.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
16% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020711s026lbl.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		BUPROPION HYDROCHLORIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
900 mg 1 times / day multiple, oral Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 214 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 214 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	Other AEs: Seizures... Other AEs: Seizures (2.8%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf
600 mg 1 times / day multiple, oral (max) Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 2400 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 2400 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	Disc. AE: Neuropsychiatric symptoms, Gastrointestinal disturbance... Other AEs: Neuropsychiatric symptoms... AEs leading to discontinuation/dose reduction: Neuropsychiatric symptoms (3%) Gastrointestinal disturbance (2.1%) Neurological disorder NOS (1.7%) Skin and subcutaneous tissue disorders (1.4%) Other AEs: Neuropsychiatric symptoms Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf

AEs

AE	Significance	Dose	Population
Seizures	2.8%	900 mg 1 times / day multiple, oral Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 214 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 214 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf
Neuropsychiatric symptoms		600 mg 1 times / day multiple, oral (max) Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 2400 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 2400 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf
Skin and subcutaneous tissue disorders	1.4% Disc. AE	600 mg 1 times / day multiple, oral (max) Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 2400 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 2400 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf
Neurological disorder NOS	1.7% Disc. AE	600 mg 1 times / day multiple, oral (max) Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 2400 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 2400 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf
Gastrointestinal disturbance	2.1% Disc. AE	600 mg 1 times / day multiple, oral (max) Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 2400 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 2400 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf
Neuropsychiatric symptoms	3% Disc. AE	600 mg 1 times / day multiple, oral (max) Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf	unhealthy, adult n = 2400 Health Status: unhealthy Condition: depression Age Group: adult Sex: unknown Population Size: 2400 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018644s043lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1670	substrate 985	inhibitor 1789	inhibitor 1570

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1401 OCT2 630	CYP2B6 648 P-gp 1491 CYP1A2 1013 CYP2A6 510 CYP2E1 633 CYP 252

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
P-gp 1588	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021515_Wellbutrin_biopharmr.PDF Page: 30.0	inconclusive
OCT2 631	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/200063Orig1s000ClinPharmR.pdf Page: 15.0	yes [IC50 9.3 uM]
CYP2D6 1826	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/200063Orig1s000ClinPharmR.pdf Page: 90.0	yes	yes (co-administration study) Comment: from FDA label https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021515s040lbl.pdf: coadministration with desipramine increased the Cmax of desipramine by 2-fold, and AUC by 5-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/200063Orig1s000ClinPharmR.pdf Page: 90.0

Drug as victim

Target	Modality	Activity	Clinical evidence
P-gp 1491	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021515_Wellbutrin_biopharmr.PDF Page: 30.0	inconclusive
CYP 252	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022497Orig1s000ClinPharmR.pdf Page: 4, 43	likely
CYP1A2 1013	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20711_ZYBAN,%20100MG%20AND%20150MG_BIOPHARMR.PDF Page: 10.0	minor
CYP2A6 510	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20711_ZYBAN,%20100MG%20AND%20150MG_BIOPHARMR.PDF Page: 10.0	minor
CYP2C9 985	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20711_ZYBAN,%20100MG%20AND%20150MG_BIOPHARMR.PDF Page: 10.0	minor
CYP2E1 633	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20711_ZYBAN,%20100MG%20AND%20150MG_BIOPHARMR.PDF Page: 10.0	minor
CYP3A4 1670	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20711_ZYBAN,%20100MG%20AND%20150MG_BIOPHARMR.PDF Page: 10.0	minor
CYP2B6 648	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/200063Orig1s000ClinPharmR.pdf Page: 10.0	yes	yes (co-administration study) Comment: from FDA label https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021515s040lbl.pdf: coadministration with ticlopidine increased buproprion Cmax 38% and AUC by 85% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/200063Orig1s000ClinPharmR.pdf Page: 10.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1603	inhibitor 1584 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/200063Orig1s000PharmR.pdf Page: 46.0

Sourcing

Vendor/Aggregator	ID	URL
ChemIDplus	93109989	https://chem.nlm.nih.gov/chemidplus/id/0093109989
PubChem	12882211	https://pubchem.ncbi.nlm.nih.gov/compound/12882211
SureChEMBL	SCHEMBL1235744	https://www.surechembl.org/chemical/SCHEMBL1235744

PubMed

Title	Date	PubMed
Algorithm for the treatment of chronic depression.	2001	11310816
Nortriptyline toxicity secondary to interaction with bupropion sustained-release.	2001	11233461
Health-related quality-of-life measure enhances acute treatment response prediction in depressed inpatients.	2001 Apr	11379840
Bupropion sustained release for bereavement: results of an open trial.	2001 Apr	11379835
Modification of norepinephrine and serotonin, but not dopamine, neuron firing by sustained bupropion treatment.	2001 Apr	11374336
[Pharmacologic therapy for smoking cessation].	2001 Apr	11347035
Bupropion overdose in an adolescent.	2001 Apr	11334088
Does pretreatment anxiety predict response to either bupropion SR or sertraline?	2001 Apr	11292522
Effects of sustained-release bupropion and supportive group therapy on cigarette consumption in patients with schizophrenia.	2001 Apr	11282701
Effects of bupropion SR on anterior paralimbic function during waking and REM sleep in depression: preliminary findings using.	2001 Apr 10	11306249
Bupropion hydrochloride: the development of a chiral separation using an ovomucoid column.	2001 Apr 13	11355823
Antidepressants in the treatment of patients with COPD: possible associations between smoking cigarettes, COPD and depression.	2001 Aug	11462058
Evaluation of the contribution of cytochrome P450 3A4 to human liver microsomal bupropion hydroxylation.	2001 Aug	11454731
[Zyban in smoking cessation].	2001 Feb 10	11255877
[Risk of convulsions due to the use of bupropion as an aid for smoking cessation].	2001 Feb 10	11236375
Smoking cessation. Pulling out the stops.	2001 Feb 15	11246826
Treatment of attention-deficit hyperactivity disorder.	2001 Jan	11237228
A 25-year-old woman with bipolar disorder.	2001 Jan 24-31	11242431
Single-dose pharmacokinetics of bupropion in adolescents: effects of smoking status and gender.	2001 Jul	11452710
Effects of cocaine prior to and during bupropion maintenance in cocaine-abusing volunteers.	2001 Jul 1	11376920
Bupropion manic induction during euthymia, but not during depression.	2001 Jun	11465677
Seizure during combination of trimipramine and bupropion.	2001 Jun	11465529
The Stanley Foundation Bipolar Network. I. Rationale and methods.	2001 Jun	11450179
Bupropion SR as an aid to smoking cessation in smokers treated previously with bupropion: a randomized placebo-controlled study.	2001 Jun	11406741
Bupropion-induced erythema multiforme.	2001 Jun	11393509
Variations in treatment benefits influence smoking cessation: results of a randomised controlled trial.	2001 Jun	11387540
Bupropion sustained-release for the treatment of dysthymic disorder: an open-label study.	2001 Jun	11386496
A practical guide to tobacco cessation in dental offices.	2001 Mar	11315394
Tobacco-use cessation programs and policies at the University of Manitoba's faculty of dentistry.	2001 Mar	11315393
Substitution of an SSRI with bupropion sustained release following SSRI-induced sexual dysfunction.	2001 Mar	11305705
Smoking cessation in the hospitalized patient using the transtheoretical model of behavior change.	2001 Mar-Apr	11248718
Type II error and antidepressants.	2001 May	11411822
Relationship between drug exposure and the efficacy and safety of bupropion sustained release for smoking cessation.	2001 May	11403727
Bupropion SR worsens mood during marijuana withdrawal in humans.	2001 May	11401006
Late-term smoking cessation despite initial failure: an evaluation of bupropion sustained release, nicotine patch, combination therapy, and placebo.	2001 May	11394732
Acute myocardial ischemia associated with ingestion of bupropion and pseudoephedrine in a 21-year-old man.	2001 May	11381283
The use of bupropion in the treatment of restlessness after a traumatic brain injury.	2001 May	11350660
Use of bupropion SR in a pharmacist-managed outpatient smoking-cessation program.	2001 May	11349752
Bupropion for smoking cessation : predictors of successful outcome.	2001 May	11348939
New recommendations from the 1999 American College of Cardiology/American Heart Association acute myocardial infarction guidelines.	2001 May	11346067
Sustained-release bupropion for selective serotonin reuptake inhibitor-induced sexual dysfunction: a randomized, double-blind, placebo-controlled, parallel-group study.	2001 May	11329407
Identification and treatment of depression in a cohort of patients maintained on chronic peritoneal dialysis.	2001 May	11325684
Smoking cessation in patients with chronic obstructive pulmonary disease: a double-blind, placebo-controlled, randomised trial.	2001 May 19	11377644
Place of bupropion in smoking-cessation therapy.	2001 May 19	11377641
Newly available treatments for nicotine addiction. Smokers wanting help with stopping now have effective treatment options.	2001 May 5	11337422
Bupropion and serum sickness-like reaction.	2001 May 7	11386597
Bupropion sustained release (SR) for the treatment of hypoactive sexual desire disorder (HSDD) in nondepressed women.	2001 May-Jun	11354935
Pharmacologic treatments for the nicotine dependent smoker.	2001 May-Jun	11322615
Pharmacological aids for smoking cessation.	2001 Spring	11326710
Pharmacokinetic interactions between cyclosporine and bupropion or methylphenidate.	2001 Summer	11436960

Patents

Sample Use Guides

In Vivo Use Guide

The usual adult dose is 300 mg/day, given 3 times daily. Dosing should begin at 200 mg/day, given as 100 mg twice daily. Based on clinical response, this dose may be increased to 300 mg/day, given as 100 mg 3 times daily, no sooner than 3 days after beginning therapy.

Route of Administration: Oral

In Vitro Use Guide

Bupropion (10 uM) significantly decreased nicotine-evoked [(3)H]dopamine release by approximately 50% in rat striatal synaptosomes and slices.

Substance Class	Chemical Created by `admin` on `Sat Dec 17 21:10:14 UTC 2022` Edited by `admin` on `Sat Dec 17 21:10:14 UTC 2022`
Record UNII	26NV8NXO4A
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BUPROPION MALEATE

Common Name

English

1-PROPANONE, 1-(3-CHLOROPHENYL)-2-((1,1-DIMETHYLETHYL)AMINO)-, (2Z)-2-BUTENEDIOATE (1:1)

Systematic Name

English

Code System Code Type Description

CAS

1013636-49-1

Created by admin on Sat Dec 17 21:10:14 UTC 2022 , Edited by admin on Sat Dec 17 21:10:14 UTC 2022

NON-SPECIFIC STOICHIOMETRY

CAS

93109-98-9

Created by admin on Sat Dec 17 21:10:14 UTC 2022 , Edited by admin on Sat Dec 17 21:10:14 UTC 2022

PRIMARY

FDA UNII

26NV8NXO4A

Created by admin on Sat Dec 17 21:10:14 UTC 2022 , Edited by admin on Sat Dec 17 21:10:14 UTC 2022

PRIMARY

PUBCHEM

12882211

Created by admin on Sat Dec 17 21:10:14 UTC 2022 , Edited by admin on Sat Dec 17 21:10:14 UTC 2022

PRIMARY

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MALEIC ACID

PARENT -> SALT/SOLVATE

Details

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator