buspirone indications/contra

Stem definitionDrug idCAS RN
anxiolytics, buspirone derivatives 437 36505-84-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • buspirone
  • buspin
  • buspirone hydrochloride
  • buspirone HCl
An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.
  • Molecular weight: 385.51
  • Formula: C21H31N5O2
  • CLOGP: 2.19
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 0
  • TPSA: 69.64
  • ALOGS: -2.82
  • ROTB: 6

Drug dosage:

DoseUnitRoute
30 mg O

Approvals:

DateAgencyCompanyOrphan
Sept. 29, 1986 FDA

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 1487.42 57.29 307 503 30807 3354242
Toxicity to various agents 376.85 57.29 114 696 46940 3338109
Respiratory arrest 325.85 57.29 76 734 11292 3373757
Cardiac arrest 277.66 57.29 80 730 27239 3357810
Cardio-respiratory arrest 205.36 57.29 56 754 15384 3369665
Overdose 201.76 57.29 66 744 33912 3351137
Poisoning 198.81 57.29 44 766 5068 3379981
Serotonin syndrome 132.32 57.29 32 778 5391 3379658
Death 93.96 57.29 61 749 152263 3232786
Hypothermia 88.82 57.29 21 789 3194 3381855
Mydriasis 80.17 57.29 19 791 2915 3382134
Depressed level of consciousness 78.63 57.29 25 785 11440 3373609
Drug abuse 78.34 57.29 28 782 18302 3366747
Anxiety 76.23 57.29 34 776 39595 3345454
Intentional overdose 71.67 57.29 25 785 15200 3369849
Cerebellar infarction 69.28 57.29 13 797 644 3384405
Coma 68.38 57.29 23 787 12529 3372520
Psychotic disorder 68.02 57.29 21 789 8713 3376336
Anoxia 64.95 57.29 10 800 147 3384902
Rhabdomyolysis 63.30 57.29 23 787 15706 3369343
Exposure via ingestion 58.64 57.29 13 797 1480 3383569
Sedation 57.50 57.29 17 793 6084 3378965

Pharmacologic Action:

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SourceCodeDescription
ATC N05BE01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Azaspirodecanedione derivatives
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D018490 Serotonin Agents
MeSH PA D017366 Serotonin Receptor Agonists
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:35941 serotonergic agonist
CHEBI has role CHEBI:35717 sedative
CHEBI has role CHEBI:35474 anxiolytic drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Generalized anxiety disorder indication 21897009 DOID:14320
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.51 Basic
pKa2 2.23 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 1A GPCR PARTIAL AGONIST EC50 7.25 WOMBAT-PK CHEMBL
D(4) dopamine receptor GPCR Ki 7 WOMBAT-PK
Alpha-1D adrenergic receptor GPCR Ki 6.28 DRUG MATRIX
D(2) dopamine receptor GPCR Ki 7.68 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 6.44 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR Ki 6.04 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 6.41 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR Ki 6.60 WOMBAT-PK
Cytochrome P450 3A4 Enzyme Ki 5.13 WOMBAT-PK
Solute carrier family 22 member 2 Transporter IC50 4.92 CHEMBL
D(3) dopamine receptor GPCR Ki 6.18 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.40 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 4.34 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.77 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.32 WOMBAT-PK
Membrane-associated progesterone receptor component 1 Membrane receptor IC50 5.47 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.32 CHEMBL
D(1A) dopamine receptor GPCR Ki 5.21 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 6.86 CHEMBL
D(2) dopamine receptor GPCR Ki 7.36 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 6.76 CHEMBL
Dopamine receptor GPCR IC50 6.92 CHEMBL
Adrenergic receptor alpha-2 GPCR IC50 5 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 4.80 CHEMBL
Alpha-2A adrenergic receptor GPCR IC50 5 CHEMBL
Serotonin 1 (5-HT1) receptor GPCR IC50 7.02 CHEMBL
5-hydroxytryptamine receptor 1B GPCR Ki 7.77 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 8.42 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 6.75 CHEMBL
D(2) dopamine receptor GPCR Ki 6.92 CHEMBL
5-hydroxytryptamine receptor 2C GPCR IC50 6 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 6.32 CHEMBL
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 6.40 IUPHAR
5-hydroxytryptamine receptor 7 GPCR AGONIST Ki 6.40 IUPHAR

External reference:

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IDSource
DB00490 DRUGBANK_ID
36 IUPHAR_LIGAND_ID
4019646 VUID
N0000147739 NUI
C0006462 UMLSCUI
D00702 KEGG_DRUG
CHEMBL49 ChEMBL_ID
207LT9J9OC UNII
33386-08-2 SECONDARY_CAS_RN
4019646 VANDF
N0000007480 NDFRT
N0000147739 NDFRT
1827 RXNORM
387523009 SNOMEDCT_US
91452003 SNOMEDCT_US
d00182 MMSL
004586 NDDF
2477 PUBCHEM_CID
CHEMBL1200399 ChEMBL_ID
D002065 MESH_DESCRIPTOR_UI
3456 INN_ID
CHEBI:3223 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0053 TABLET 5 mg ORAL ANDA 14 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0054 TABLET 10 mg ORAL ANDA 14 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-1003 TABLET 15 mg ORAL ANDA 14 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5200 TABLET 30 mg ORAL ANDA 14 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 0115-1690 TABLET 5 mg ORAL ANDA 14 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 0115-1691 TABLET 10 mg ORAL ANDA 14 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 0115-1692 TABLET 15 mg ORAL ANDA 14 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-1140 TABLET 5 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-1145 TABLET 7.50 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-1150 TABLET 10 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-1165 TABLET 15 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-1175 TABLET 30 mg ORAL ANDA 15 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 0591-0657 TABLET 5 mg ORAL ANDA 14 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 0591-0658 TABLET 10 mg ORAL ANDA 14 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 0591-0718 TABLET 15 mg ORAL ANDA 14 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-4575 TABLET 10 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-4595 TABLET 5 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-4596 TABLET 15 mg ORAL ANDA 15 sections
BusPIRone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-5548 TABLET 7.50 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7633 TABLET 5 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7634 TABLET 10 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7635 TABLET 15 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7689 TABLET 15 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7714 TABLET 5 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7718 TABLET 10 mg ORAL ANDA 15 sections
Buspirone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-6061 TABLET 15 mg ORAL ANDA 15 sections
Buspirone HCl HUMAN PRESCRIPTION DRUG LABEL 1 10544-176 TABLET 10 mg ORAL ANDA 14 sections
BUSPIRONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 16590-375 TABLET 30 mg ORAL ANDA 15 sections
BUSPIRONE HCl HUMAN PRESCRIPTION DRUG LABEL 1 16590-579 TABLET 15 mg ORAL ANDA 13 sections
BUSPIRONE HUMAN PRESCRIPTION DRUG LABEL 1 16590-600 TABLET 10 mg ORAL ANDA 13 sections