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Identification
NameBuspirone
Accession NumberDB00490  (APRD00222)
TypeSmall Molecule
GroupsApproved, Investigational
Description

An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. [PubChem]

Structure
Thumb
Synonyms
8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione
Buspiron
Buspirona
Buspirone
Buspironum
External Identifiers
  • MJ 90221-1
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Buspar Tab 10mgtablet10 mgoralBristol Myers Squibb Canada1989-12-312010-11-12Canada
Buspironetablet10 mgoralSanis Health Inc2016-02-17Not applicableCanada
Buspirone-10 - Tab 10mgtablet10 mgoralPro Doc Limitee1997-01-15Not applicableCanada
Bustabtablet10 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-05-272014-07-30Canada
Bustabtablet5 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-05-272014-07-30Canada
Co Buspironetablet10 mgoralCobalt Pharmaceuticals Company2005-11-092012-08-02Canada
Dom-buspironetablet10 mgoralDominion Pharmacal1999-10-25Not applicableCanada
Ftp-buspironetablet10 mgoralFtp Pharmacal Inc.1998-10-092004-08-03Canada
Linbuspironetablet10 mgoralLinson Pharma Co.1996-12-312006-05-29Canada
Mylan-buspironetablet10 mgoralMylan Pharmaceuticals Ulc1997-03-132010-08-04Canada
Nu-buspirone - Tab 10mgtablet10 mgoralNu Pharm Inc1996-12-312012-09-04Canada
Penta-buspironetablet10 mgoralPentapharm Ltd.Not applicableNot applicableCanada
PMS-buspironetablet10 mgoralPharmascience Inc1997-05-26Not applicableCanada
PMS-buspironetablet5 mgoralPharmascience Inc1997-06-05Not applicableCanada
Ratio-buspironetablet10 mgoralRatiopharm Inc Division Of Teva Canada Limited1998-06-102010-05-17Canada
Riva-buspirone 10 mgtablet10 mgoralLaboratoire Riva Inc2003-03-03Not applicableCanada
Teva-buspironetablet10 mgoralTeva Canada Limited1997-09-02Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-buspirone - Tab 10mgtablet10 mgoralApotex Inc1996-12-31Not applicableCanada
Buspironetablet10 mg/1oralSTAT Rx USA LLC2002-03-01Not applicableUs
Buspirone HCltablet10 mg/1oralDispensing Solutions, Inc.2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Buspirone HCltablet5 mg/1oralClinical Solutions Wholesale2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralbryant ranch prepack2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralAmerican Health Packaging2013-05-282015-12-29Us
Buspirone HCltablet5 mg/1oralPreferred Pharmaceuticals, Inc.2013-06-24Not applicableUs
Buspirone HCltablet5 mg/1oralRebel Distributors Corp.2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Buspirone HCltablet10 mg/1oralProficient Rx LP2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralRebel Distributors Corp.2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralWatson Laboratories, Inc.2001-03-28Not applicableUs
Buspirone HCltablet5 mg/1oralLake Erie Medical DBA Quality Care Products LLC2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralPd Rx Pharmaceuticals, Inc.2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralWatson Laboratories, Inc.2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralSTAT Rx USA LLC2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralRebel Distributors Corp.2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralProficient Rx LP2001-03-28Not applicableUs
Buspirone HCltablet5 mg/1oralWatson Laboratories, Inc.2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralUnit Dose Services2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralMedsource Pharmaceuticals2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralCardinal Health2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralTYA Pharmaceuticals2001-03-28Not applicableUs
Buspirone HCltablet10 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Buspirone HCltablet5 mg/1oralAmerican Health Packaging2013-05-282015-12-29Us
Buspirone HCltablet10 mg/1oralClinical Solutions Wholesale2001-03-28Not applicableUs
Buspirone HCltablet5 mg/1oralbryant ranch prepack2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralDispensing Solutions, Inc.2001-03-28Not applicableUs
Buspirone HCltablet15 mg/1oralAmerican Health Packaging2013-05-282015-12-29Us
Buspirone HCltablet5 mg/1oralTYA Pharmaceuticals2001-03-28Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralMc Kesson Contract Packaging2011-11-21Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2002-03-01Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2010-12-15Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralAccord Healthcare Inc.2015-09-15Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2011-10-13Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralClinical Solutions Wholesale, Llc2014-05-03Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralProficient Rx LP2002-03-01Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralAidarex Pharmaceuticals LLC2002-03-01Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralPar Pharmaceutical Inc.2012-04-23Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralPhysicians Total Care, Inc.2009-07-23Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralCarilion Materials Management2002-02-28Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralTeva Pharmaceuticals USA Inc2002-02-28Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralAccord Healthcare Inc.2015-09-15Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2005-06-01Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralStrides Arcolab Limited2014-09-05Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralMylan Pharmaceuticals Inc.2002-03-01Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2002-02-28Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralAphena Pharma Solutions Tennessee, Llc2002-03-21Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralMylan Institutional Inc.2002-12-01Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralDr. Reddy's Laboratories Ltd2009-03-04Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralREMEDYREPACK INC.2014-12-10Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2002-03-01Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralREMEDYREPACK INC.2010-12-15Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralSTAT Rx USA LLC2010-07-01Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2011-08-23Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralLake Erie Medical DBA Quality Care Products LLC2001-03-28Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralCadila Healthcare Limited2014-05-03Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralMc Kesson Contract Packaging2011-11-07Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralMylan Pharmaceuticals Inc.2013-07-08Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-04-23Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralAphena Pharma Solutions Tennessee, Llc2001-03-28Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralMylan Institutional Inc.2002-03-25Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralDr. Reddy's Laboratories Ltd2009-03-04Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralGolden State Medical Supply, Inc.2015-02-09Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralStrides Arcolab Limited2014-09-05Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-05-03Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralREMEDYREPACK INC.2010-12-15Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2011-03-23Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralH.J. Harkins Company, Inc.2010-12-23Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralDIRECT RX2015-01-01Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralCadila Healthcare Limited2014-05-03Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralPreferred Pharmaceuticals, Inc.2012-03-29Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralMylan Pharmaceuticals Inc.2002-03-01Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralRebel Distributors Corp2009-09-09Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-12-23Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralMylan Institutional Inc.2002-03-25Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralDr. Reddy's Laboratories Ltd2009-03-04Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralGolden State Medical Supply, Inc.2015-02-09Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralStrides Arcolab Limited2014-09-05Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-05-03Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralLake Erie Medical DBA Quality Care Products LLC2013-07-08Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2011-05-12Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2015-06-22Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralCardinal Health2010-03-31Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralDIRECT RX2014-01-01Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralCadila Healthcare Limited2014-05-03Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralPreferred Pharmaceuticals, Inc.2012-03-29Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralHeritage Pharmaceuticals Inc.2012-06-29Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralTeva Pharmaceuticals USA Inc2004-03-26Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-12-23Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralAv Kare, Inc.2013-10-17Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralMylan Institutional Inc.2001-04-15Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralDr. Reddy's Laboratories Ltd2009-03-04Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralGolden State Medical Supply, Inc.2015-02-09Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralStrides Arcolab Limited2014-09-05Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-05-03Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralREMEDYREPACK INC.2010-12-07Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralREMEDYREPACK INC.2013-05-02Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralCardinal Health2010-03-31Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralREMEDYREPACK INC.2015-03-07Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralCadila Healthcare Limited2014-05-03Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralPreferred Pharmaceuticals Inc.2015-08-19Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralHeritage Pharmaceuticals Inc.2012-06-29Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralSTAT Rx USA LLC2011-10-05Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralAv Kare, Inc.2013-08-28Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralPhysicians Total Care, Inc.2012-04-30Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralNew Horizon Rx Group, LLC2013-08-25Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralbryant ranch prepack2010-12-23Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-05-03Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralTeva Pharmaceuticals USA Inc2002-03-01Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralAccord Healthcare Inc.2015-09-15Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-12-23Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralREMEDYREPACK INC.2013-05-03Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralREMEDYREPACK INC.2015-01-12Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralPreferred Pharmaceuticals Inc.2015-10-08Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralMylan Pharmaceuticals Inc.2001-06-28Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralHeritage Pharmaceuticals Inc.2012-06-29Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralCarilion Materials Management2002-02-28Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2002-03-01Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralAidarex Pharmaceuticals LLC2002-02-28Not applicableUs
Buspirone Hydrochloridetablet7.5 mg/1oralAccord Healthcare Inc.2015-09-15Not applicableUs
Buspirone Hydrochloridetablet30 mg/1oralREMEDYREPACK INC.2012-03-29Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralPhysicians Total Care, Inc.2004-12-21Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralbryant ranch prepack2002-03-01Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralRebel Distributors Corp2010-12-23Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-11-16Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralPhysicians Total Care, Inc.2007-09-17Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralClinical Solutions Wholesale, Llc2014-05-03Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralTeva Pharmaceuticals USA Inc2002-02-28Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralAccord Healthcare Inc.2015-09-15Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-12-23Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralPreferred Pharmaceuticals, Inc.2012-03-29Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralMylan Pharmaceuticals Inc.2001-03-28Not applicableUs
Buspirone Hydrochloridetablet5 mg/1oralHeritage Pharmaceuticals Inc.2012-06-29Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralMajor Pharmaceuticals2009-08-09Not applicableUs
Buspirone Hydrochloridetablet10 mg/1oralAphena Pharma Solutions Tennessee, Llc2002-03-21Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralNorthwind Pharmaceuticals, LLC2015-02-25Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralCardinal Health2001-03-28Not applicableUs
Buspirone Hydrochloridetablet15 mg/1oralREMEDYREPACK INC.2015-01-12Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnsialRontag
AnxironValeant
AnxutEisai
BesparNot Available
BuscalmWockhardt
BuspHexal
BusparBristol-Myers Squibb
BusponDeva
DalpasBiotech
EpsilatCoup
PasrinAspen Pharmacare
SpamilanAnpharm
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Buspirone Hydrochloride
33386-08-2
Thumb
  • InChI Key: RICLFGYGYQXUFH-UHFFFAOYSA-N
  • Monoisotopic Mass: 421.224453
  • Average Mass: 421.964
DBSALT000313
Categories
UNIITK65WKS8HL
CAS number36505-84-7
WeightAverage: 385.5031
Monoisotopic: 385.247775261
Chemical FormulaC21H31N5O2
InChI KeyInChIKey=QWCRAEMEVRGPNT-UHFFFAOYSA-N
InChI
InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2
IUPAC Name
8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
SMILES
O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)C1=NC=CC=N1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentN-arylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • Azaspirodecanedione
  • Azaspirodecane
  • Dialkylarylamine
  • Piperidinedione
  • N-alkylpiperazine
  • Piperidinone
  • Dicarboximide
  • Delta-lactam
  • Pyrimidine
  • Piperidine
  • Carboxylic acid imide, n-substituted
  • Heteroaromatic compound
  • Carboxylic acid imide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.
PharmacodynamicsBuspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.
Mechanism of actionBuspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced.
Related Articles
AbsorptionRapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism.
Volume of distributionNot Available
Protein binding95% (approximately 70% bound to albumin, 30% bound to alpha 1 -acid glycoprotein)
Metabolism

Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP)

SubstrateEnzymesProduct
Buspirone
1-PyrimidinylpiperazineDetails
Buspirone
Buspirone N-oxideDetails
Buspirone
3′-HydroxybuspironeDetails
Buspirone
5-HydroxybuspironeDetails
Buspirone
6'-HydroxybuspironeDetails
Route of eliminationIn a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose.
Half life2-3 hours (although the action of a single dose is much longer than the short halflife indicates).
ClearanceNot Available
ToxicityOral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9935
Blood Brain Barrier+0.9839
Caco-2 permeable-0.538
P-glycoprotein substrateSubstrate0.5726
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IINon-inhibitor0.8282
Renal organic cation transporterInhibitor0.598
CYP450 2C9 substrateNon-substrate0.8703
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.6728
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorInhibitor0.7186
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8681
Ames testNon AMES toxic0.6277
CarcinogenicityNon-carcinogens0.8959
BiodegradationNot ready biodegradable0.987
Rat acute toxicity2.8167 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7042
hERG inhibition (predictor II)Inhibitor0.6914
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Bristol myers squibb co pharmaceutical research institute
  • Actavis totowa llc
  • Apotex inc
  • Dr reddys laboratories ltd
  • Egis pharmaceuticals
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Kv pharmaceutical co
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg
Tabletoral10 mg/1
Tabletoral15 mg/1
Tabletoral30 mg/1
Tabletoral5 mg/1
Tabletoral7.5 mg/1
Tabletoral5 mg
Prices
Unit descriptionCostUnit
Wellbutrin xl 300 mg tablet8.68USD tablet
Wellbutrin xl 150 mg tablet6.58USD tablet
Buspar 30 mg tablet5.52USD tablet
Buspirone hcl powder4.74USD g
Buspirone hcl 30 mg tablet3.71USD tablet
Buspar 15 mg tablet3.07USD tablet
Buspirone hcl 15 mg tablet2.16USD tablet
Buspar 10 mg tablet2.05USD tablet
Buspirone hcl 7.5 mg tablet1.62USD tablet
Buspirone hcl 10 mg tablet1.42USD tablet
Buspar 5 mg tablet1.18USD tablet
Vanspar 7.5 mg tablet1.18USD tablet
Buspar 10 mg Tablet1.12USD tablet
Buspirone hcl 5 mg tablet0.79USD tablet
Apo-Buspirone 10 mg Tablet0.62USD tablet
Novo-Buspirone 10 mg Tablet0.62USD tablet
Nu-Buspirone 10 mg Tablet0.62USD tablet
Pms-Buspirone 10 mg Tablet0.62USD tablet
Ratio-Buspirone 10 mg Tablet0.62USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point201.5-202.5 °CNot Available
water solubility21.4 mg/LNot Available
logP2.63TAKACS-NOVAK,K 1995 (IN PRESS)
Predicted Properties
PropertyValueSource
Water Solubility0.588 mg/mLALOGPS
logP1.95ALOGPS
logP1.78ChemAxon
logS-2.8ALOGPS
pKa (Strongest Basic)7.62ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area69.64 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity108.89 m3·mol-1ChemAxon
Polarizability44.12 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-004i-6940000000-197b8ea9ac79cbda753bView in MoNA
References
Synthesis Reference

DrugSyn.org

US3717634
General ReferencesNot Available
External Links
ATC CodesN05BE01
AHFS Codes
  • 28:24.92
PDB EntriesNot Available
FDA labelDownload (275 KB)
MSDSDownload (75.6 KB)
Interactions
Drug Interactions
Drug
AcepromazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Buspirone is combined with Amisulpride.
AprepitantThe serum concentration of Buspirone can be increased when it is combined with Aprepitant.
AripiprazoleThe risk or severity of adverse effects can be increased when Buspirone is combined with Aripiprazole.
AzelastineBuspirone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Buspirone.
BenzquinamideThe risk or severity of adverse effects can be increased when Buspirone is combined with Benzquinamide.
BexaroteneThe serum concentration of Buspirone can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Buspirone can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
BuprenorphineBuspirone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CarphenazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Buspirone is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Buspirone is combined with Chlorprothixene.
CitalopramBuspirone may increase the serotonergic activities of Citalopram.
ClarithromycinThe metabolism of Buspirone can be decreased when combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Buspirone is combined with Clozapine.
ConivaptanThe serum concentration of Buspirone can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Buspirone can be decreased when it is combined with Dabrafenib.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Buspirone.
DasatinibThe serum concentration of Buspirone can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Buspirone can be decreased when it is combined with Deferasirox.
DiltiazemThe metabolism of Buspirone can be decreased when combined with Diltiazem.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
ErythromycinThe metabolism of Buspirone can be decreased when combined with Erythromycin.
EscitalopramBuspirone may increase the serotonergic activities of Escitalopram.
EthanolBuspirone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FencamfamineThe risk or severity of adverse effects can be increased when Buspirone is combined with Fencamfamine.
FluconazoleThe metabolism of Buspirone can be decreased when combined with Fluconazole.
FluoxetineBuspirone may increase the serotonergic activities of Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Buspirone is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Buspirone is combined with Fluspirilene.
FluvoxamineBuspirone may increase the serotonergic activities of Fluvoxamine.
FosaprepitantThe serum concentration of Buspirone can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Buspirone can be increased when it is combined with Fusidic Acid.
GranisetronGranisetron may increase the serotonergic activities of Buspirone.
HaloperidolThe risk or severity of adverse effects can be increased when Buspirone is combined with Haloperidol.
HydrocodoneBuspirone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
IdelalisibThe serum concentration of Buspirone can be increased when it is combined with Idelalisib.
Ioflupane I 123Buspirone may decrease effectiveness of Ioflupane I 123 as a diagnostic agent.
IsocarboxazidThe risk or severity of adverse effects can be increased when Buspirone is combined with Isocarboxazid.
ItraconazoleThe metabolism of Buspirone can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Buspirone can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Buspirone can be decreased when combined with Ketoconazole.
LinezolidThe risk or severity of adverse effects can be increased when Buspirone is combined with Linezolid.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Buspirone.
LoxapineThe risk or severity of adverse effects can be increased when Buspirone is combined with Loxapine.
LuliconazoleThe serum concentration of Buspirone can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
MesoridazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Methotrimeprazine.
Methylene blueBuspirone may increase the serotonergic activities of Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Buspirone is combined with Metoclopramide.
MetyrosineBuspirone may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Buspirone can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
MitotaneThe serum concentration of Buspirone can be decreased when it is combined with Mitotane.
MoclobemideThe risk or severity of adverse effects can be increased when Buspirone is combined with Moclobemide.
MolindoneThe risk or severity of adverse effects can be increased when Buspirone is combined with Molindone.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
NefazodoneBuspirone may increase the serotonergic activities of Nefazodone.
NelfinavirThe metabolism of Buspirone can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Buspirone can be increased when it is combined with Netupitant.
OlanzapineThe risk or severity of adverse effects can be increased when Buspirone is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Buspirone is combined with Ondansetron.
OrphenadrineBuspirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Buspirone can be increased when it is combined with Palbociclib.
PaliperidoneThe risk or severity of adverse effects can be increased when Buspirone is combined with Paliperidone.
ParaldehydeBuspirone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineBuspirone may increase the serotonergic activities of Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
PerphenazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Perphenazine.
PhenelzineThe risk or severity of adverse effects can be increased when Buspirone is combined with Phenelzine.
PhenytoinThe metabolism of Buspirone can be increased when combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Buspirone is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Piperacetazine.
PosaconazoleThe metabolism of Buspirone can be decreased when combined with Posaconazole.
PramipexoleBuspirone may increase the sedative activities of Pramipexole.
ProcarbazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Procarbazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Buspirone is combined with Quetiapine.
RasagilineThe risk or severity of adverse effects can be increased when Buspirone is combined with Rasagiline.
RemoxiprideThe risk or severity of adverse effects can be increased when Buspirone is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Buspirone is combined with Reserpine.
RifabutinThe serum concentration of Buspirone can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Buspirone can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Buspirone can be decreased when it is combined with Rifapentine.
RisperidoneThe risk or severity of adverse effects can be increased when Buspirone is combined with Risperidone.
RopiniroleBuspirone may increase the sedative activities of Ropinirole.
RotigotineBuspirone may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Buspirone.
SelegilineThe risk or severity of adverse effects can be increased when Buspirone is combined with Selegiline.
SertindoleThe risk or severity of adverse effects can be increased when Buspirone is combined with Sertindole.
SertralineBuspirone may increase the serotonergic activities of Sertraline.
SiltuximabThe serum concentration of Buspirone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Buspirone can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
St. John's WortThe serum concentration of Buspirone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Buspirone can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Buspirone is combined with Sulpiride.
SuvorexantBuspirone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Buspirone is combined with Tedizolid Phosphate.
TelithromycinThe metabolism of Buspirone can be decreased when combined with Telithromycin.
ThalidomideBuspirone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Buspirone is combined with Thiothixene.
TocilizumabThe serum concentration of Buspirone can be decreased when it is combined with Tocilizumab.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Buspirone.
TranylcypromineThe risk or severity of adverse effects can be increased when Buspirone is combined with Tranylcypromine.
TrazodoneBuspirone may increase the serotonergic activities of Trazodone.
TrifluoperazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Buspirone is combined with Triflupromazine.
VerapamilThe metabolism of Buspirone can be decreased when combined with Verapamil.
VilazodoneBuspirone may increase the serotonergic activities of Vilazodone.
VoriconazoleThe metabolism of Buspirone can be decreased when combined with Voriconazole.
VortioxetineBuspirone may increase the serotonergic activities of Vortioxetine.
YohimbineThe therapeutic efficacy of Buspirone can be decreased when used in combination with Yohimbine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Buspirone is combined with Ziprasidone.
ZolpidemBuspirone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Buspirone is combined with Zuclopenthixol.
Food Interactions
  • Always take at the same time with respect to meals.
  • Avoid alcohol.
  • Avoid taking grapefruit or grapefruit juice throughout treatment.
  • Take with food.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. de Boer SF, Lesourd M, Mocaer E, Koolhaas JM: Selective antiaggressive effects of alnespirone in resident-intruder test are mediated via 5-hydroxytryptamine1A receptors: A comparative pharmacological study with 8-hydroxy-2-dipropylaminotetralin, ipsapirone, buspirone, eltoprazine, and WAY-100635. J Pharmacol Exp Ther. 1999 Mar;288(3):1125-33. [PubMed:10027850 ]
  2. Rehman J, Kaynan A, Christ G, Valcic M, Maayani S, Melman A: Modification of sexual behavior of Long-Evans male rats by drugs acting on the 5-HT1A receptor. Brain Res. 1999 Mar 13;821(2):414-25. [PubMed:10064829 ]
  3. Liang KC: Pre- or post-training injection of buspirone impaired retention in the inhibitory avoidance task: involvement of amygdala 5-HT1A receptors. Eur J Neurosci. 1999 May;11(5):1491-500. [PubMed:10215901 ]
  4. Becker C, Hamon M, Benoliel JJ: Prevention by 5-HT1A receptor agonists of restraint stress- and yohimbine-induced release of cholecystokinin in the frontal cortex of the freely moving rat. Neuropharmacology. 1999 Apr;38(4):525-32. [PubMed:10221756 ]
  5. Dupuis DS, Tardif S, Wurch T, Colpaert FC, Pauwels PJ: Modulation of 5-HT1A receptor signalling by point-mutation of cysteine351 in the rat Galpha(o) protein. Neuropharmacology. 1999 Jul;38(7):1035-41. [PubMed:10428422 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Osei-Owusu P, Scrogin KE: Buspirone raises blood pressure through activation of sympathetic nervous system and by direct activation of alpha1-adrenergic receptors after severe hemorrhage. J Pharmacol Exp Ther. 2004 Jun;309(3):1132-40. Epub 2004 Feb 9. [PubMed:14769835 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Malt EA, Olafsson S, Aakvaag A, Lund A, Ursin H: Altered dopamine D2 receptor function in fibromyalgia patients: a neuroendocrine study with buspirone in women with fibromyalgia compared to female population based controls. J Affect Disord. 2003 Jun;75(1):77-82. [PubMed:12781354 ]
  2. Boido A, Boido CC, Sparatore F: Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes. Farmaco. 2001 Apr;56(4):263-75. [PubMed:11421254 ]
  3. Nader MA, Hannemann M: Interactions of buspirone or gepirone with nicotine on schedule-controlled behavior of pigeons. Behav Pharmacol. 1993 Jun;4(3):263-268. [PubMed:11224194 ]
  4. Pache DM, Fernandez-Perez S, Sewell RD: Buspirone differentially modifies short-term memory function in a combined delayed matching/non-matching to position task. Eur J Pharmacol. 2003 Sep 23;477(3):205-11. [PubMed:14522358 ]
  5. Fernandez-Perez S, Pache DM, Sewell RD: Co-administration of fluoxetine and WAY100635 improves short-term memory function. Eur J Pharmacol. 2005 Oct 17;522(1-3):78-83. Epub 2005 Oct 7. [PubMed:16214127 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J: Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7. Epub 2005 Jan 7. [PubMed:15640381 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J: Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7. Epub 2005 Jan 7. [PubMed:15640381 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J: Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7. Epub 2005 Jan 7. [PubMed:15640381 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524 ]
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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:22