adenosine indications/contra

Stem definitionDrug idCAS RN
90 58-61-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • adenosine
  • adenine riboside
  • riboadenosine
  • beta-Adenosine
  • beta-D-Adenosine
  • adenoscan
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
  • Molecular weight: 267.25
  • Formula: C10H13N5O4
  • CLOGP: -2.16
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 4
  • TPSA: 139.54
  • ALOGS: -1.28
  • ROTB: 2

Drug dosage:

DoseUnitRoute
15 mg P

Approvals:

DateAgencyCompanyOrphan
Oct. 30, 1989 FDA ASTELLAS

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
Bronchospasm 182.10 54.81 37 508 4257 3381057
Drug hypersensitivity 177.62 54.81 55 490 35625 3349689
Dyspnoea 147.07 54.81 63 482 102871 3282443
Arteriospasm coronary 126.41 54.81 22 523 1080 3384234
Cardiac arrest 114.15 54.81 37 508 27282 3358032
Ventricular tachycardia 94.87 54.81 23 522 5839 3379475
Respiratory arrest 88.81 54.81 25 520 11343 3373971
Atrioventricular block complete 85.54 54.81 18 527 2414 3382900
Infusion related reaction 83.74 54.81 24 521 11597 3373717
Atrioventricular block 75.99 54.81 16 529 2148 3383166
Hypotension 75.48 54.81 32 513 49482 3335832
Supraventricular tachycardia 74.86 54.81 17 528 3239 3382075
Bradycardia 71.08 54.81 23 522 16646 3368668
Cardio-respiratory arrest 56.51 54.81 19 526 15421 3369893

Pharmacologic Action:

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SourceCodeDescription
ATC C01EB10 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
OTHER CARDIAC PREPARATIONS
Other cardiac preparations
FDA EPC N0000178375 Adenosine Receptor Agonist
FDA MoA N0000175788 Adenosine Receptor Agonists
MeSH PA D000700 Analgesics
MeSH PA D000889 Anti-Arrhythmia Agents
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35480 analgesic
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D058905 Purinergic Agents
MeSH PA D058913 Purinergic Agonists
MeSH PA D058906 Purinergic P1 Receptor Agonists
MeSH PA D018689 Sensory System Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Paroxysmal supraventricular tachycardia indication 67198005
Myocardial Perfusion Imaging Adjunct indication
Pericarditis contraindication 3238004 DOID:1787
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Disorder of autonomic nervous system contraindication 15241006
Complete atrioventricular block contraindication 27885002
Hypovolemia contraindication 28560003
Acute cerebrovascular insufficiency contraindication 29322000
Transplantation of heart contraindication 32413006
Sick sinus syndrome contraindication 36083008 DOID:13884
Low blood pressure contraindication 45007003
Aortic valve stenosis contraindication 60573004 DOID:1712
Left to right cardiovascular shunt contraindication 66130006
Mitral valve stenosis contraindication 79619009 DOID:1754
Pulmonary emphysema contraindication 87433001
Respiratory alkalosis contraindication 111378004
Second degree atrioventricular block contraindication 195042002
Asthma contraindication 195967001 DOID:2841
Left main coronary artery disease contraindication 371804009
Acute coronary syndrome contraindication 394659003
Respiratory insufficiency contraindication 409623005
Syncope due to Bradycardia contraindication
Supraventricular tachycardia off-label use 6456007

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.67 acidic
pKa2 12.33 acidic
pKa3 13.34 acidic
pKa4 3.95 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
Adenosine receptor A2a GPCR AGONIST EC50 6.15 WOMBAT-PK CHEMBL
Adenosine receptor A1 GPCR AGONIST EC50 6.51 WOMBAT-PK CHEMBL
Adenosine receptor A2b GPCR AGONIST EC50 4.62 WOMBAT-PK CHEMBL
Glyceraldehyde-3-phosphate dehydrogenase liver Enzyme IC50 4.46 CHEMBL
Adenosine deaminase Enzyme Kd 4.60 WOMBAT-PK
Adenosine kinase Kinase IC50 6 WOMBAT-PK
Adenosylhomocysteinase Enzyme Km 5.80 WOMBAT-PK
Adenosine receptor A3 GPCR AGONIST Ki 6.54 IUPHAR
Phosphatidylinositol 4-kinase type 2-alpha Kinase INHIBITOR IC50 4.75 IUPHAR
Phosphatidylinositol 4-kinase type 2-beta Kinase INHIBITOR IC50 4.75 IUPHAR
Adenosine kinase Kinase Ki 5.05 CHEMBL
Adenosine receptor A2a GPCR Ki 7.52 CHEMBL
Adenosine A2 receptor GPCR Ki 8.30 CHEMBL
Adenosine receptor A3 GPCR Ki 7 CHEMBL
Adenosine receptor A1 GPCR Ki 8.29 CHEMBL
cAMP-dependent protein kinase A Unclassified Ki 4.82 CHEMBL

External reference:

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IDSource
2844 IUPHAR_LIGAND_ID
4019507 VUID
N0000147627 NUI
C0001443 UMLSCUI
D00045 KEGG_DRUG
CHEMBL477 ChEMBL_ID
DB00640 DRUGBANK_ID
60961 PUBCHEM_CID
4019507 VANDF
57772 MMSL
N0000147627 NDFRT
N0000007355 NDFRT
004537 NDDF
003603 NDDF
004813 NDDF
296 RXNORM
35431001 SNOMEDCT_US
4135 MMSL
d00164 MMSL
108502004 SNOMEDCT_US
CHEBI:16335 CHEBI
K72T3FS567 UNII
D000241 MESH_DESCRIPTOR_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 0409-1932 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 17 sections
Adenoscan HUMAN PRESCRIPTION DRUG LABEL 1 0469-0871 SOLUTION 3 mg INTRAVENOUS NDA 17 sections
Adenocard HUMAN PRESCRIPTION DRUG LABEL 1 0469-8234 SOLUTION 3 mg INTRAVENOUS NDA 12 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 0641-6113 INJECTION 3 mg INTRAVENOUS ANDA 13 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 0703-8776 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 17 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 0703-8777 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 17 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 10019-063 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 13 sections
MISSHA Time Revolution Night Repair Science Activator Ampoule HUMAN OTC DRUG LABEL 2 13733-360 LIQUID 20 mg TOPICAL unapproved drug other 13 sections
MISSHA TIME REVOLUTION NIGHT REPAIR NEW SCIENCE ACTIVATOR AMPOULE MASK HUMAN OTC DRUG LABEL 2 13733-361 PATCH 0.13 g TOPICAL unapproved drug other 13 sections
MISSHA Time Revolution The First Treatment Essence Intensive HUMAN OTC DRUG LABEL 2 13733-370 LIQUID 0.06 g TOPICAL unapproved drug other 13 sections
MISSHA Time Revolution The First Treatment Essence Mask HUMAN OTC DRUG LABEL 1 13733-371 PATCH 13.20 mg TOPICAL unapproved drug other 13 sections
MISSHA TIME REVOLUTION VITALITY SERUM HUMAN OTC DRUG LABEL 1 13733-380 LIQUID 16 mg TOPICAL unapproved drug other 13 sections
MISSHA Time Revolution Vitality Eye Cream HUMAN OTC DRUG LABEL 1 13733-381 CREAM 10 mg TOPICAL unapproved drug other 13 sections
MISSHA Time Revolution Immortal Youth Blue Essence HUMAN OTC DRUG LABEL 2 13733-382 EMULSION 32 mg TOPICAL unapproved drug other 13 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 17478-542 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 13 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 17478-544 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 16 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 17478-953 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 12 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 23155-258 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 17 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 23155-259 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 17 sections
adenosine HUMAN PRESCRIPTION DRUG LABEL 1 25021-301 INJECTION 3 mg INTRAVENOUS ANDA 13 sections
Adenosine HUMAN PRESCRIPTION DRUG LABEL 1 25021-307 INJECTION, SOLUTION 3 mg INTRAVENOUS ANDA 17 sections
Dr G deWrinkle BOOSTER ample by EGF HUMAN OTC DRUG LABEL 2 43948-3001 SOLUTION/ DROPS 0.04 mL TOPICAL OTC monograph final 4 sections
Dr G deWrinkle FORTIFIER by EGF HUMAN OTC DRUG LABEL 2 43948-3002 CREAM 0.01 mL TOPICAL OTC monograph final 4 sections
Dr G deWrinkle REFORMER by EGF HUMAN OTC DRUG LABEL 2 43948-3003 CREAM 0.02 mL TOPICAL OTC monograph final 4 sections
HANSKIN BIO ORIGIN THE HUMAN OTC DRUG LABEL 2 47469-250 CREAM 0.02 g TOPICAL unapproved drug other 8 sections
HANSKIN REAL COMPLEXION CRE AM EX HUMAN OTC DRUG LABEL 2 47469-350 CREAM 0.02 g TOPICAL unapproved drug other 8 sections
Hanskin Vstra toning water radiance HUMAN OTC DRUG LABEL 2 47469-390 CREAM 0.02 g TOPICAL unapproved drug other 8 sections
Hanskin Vistra toner mask pad HUMAN OTC DRUG LABEL 2 47469-400 LIQUID 0.10 g TOPICAL unapproved drug other 8 sections
HANSKIN SUPER THREE SOLU TION AQUA FIRMING SHEET MASK HUMAN OTC DRUG LABEL 1 47469-470 PATCH 0.01 g TOPICAL unapproved drug other 8 sections
Super Plus Beblesh Balm Triple Functions SPF50 Plus PA 3Plus (40g) HUMAN OTC DRUG LABEL 6 49715-007 CREAM 0.02 g TOPICAL OTC monograph final 10 sections