atenolol indications/contra

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 255 29122-68-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • atenolol
  • (RS)-Atenolol
  • (+/-)-Atenolol
  • betablok
A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.
  • Molecular weight: 266.34
  • Formula: C14H22N2O3
  • CLOGP: -0.11
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 3
  • TPSA: 84.58
  • ALOGS: -2.79
  • ROTB: 8

Drug dosage:

DoseUnitRoute
75 mg O
75 mg P

Approvals:

DateAgencyCompanyOrphan
Aug. 19, 1981 FDA ALVOGEN IPCO SARL

FDA Adverse Event Reporting System

scroll-->
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
Bradycardia 3362.84 34.84 787 5140 15882 3364050
Completed suicide 2636.38 34.84 736 5191 30378 3349554
Hypotension 1605.53 34.84 564 5363 48950 3330982
Syncope 1064.22 34.84 353 5574 25280 3354652
Toxicity to various agents 924.02 34.84 373 5554 46681 3333251
Sinus bradycardia 916.57 34.84 205 5722 3174 3376758
Overdose 826.73 34.84 315 5612 33663 3346269
Drug interaction 628.25 34.84 284 5643 46528 3333404
Dizziness 561.98 34.84 308 5619 76204 3303728
Acute kidney injury 436.94 34.84 226 5701 49457 3330475
Cardiac arrest 433.91 34.84 187 5740 27132 3352800
Intentional overdose 426.30 34.84 157 5770 15068 3364864
Poisoning 418.00 34.84 119 5808 4993 3374939
Orthostatic hypotension 401.73 34.84 115 5812 4921 3375011
Hyperkalaemia 401.25 34.84 139 5788 11155 3368777
Fall 376.52 34.84 217 5710 58666 3321266
Shock 365.38 34.84 115 5812 6822 3373110
Hypertension 355.11 34.84 181 5746 38285 3341647
Suicide attempt 344.75 34.84 136 5791 15711 3364221
Loss of consciousness 330.02 34.84 156 5771 27991 3351941
Presyncope 276.50 34.84 87 5840 5144 3374788
Asthenia 272.38 34.84 184 5743 65481 3314451
Heart rate decreased 263.30 34.84 84 5843 5194 3374738
Dyspnoea 262.19 34.84 215 5712 102719 3277213
Drug hypersensitivity 250.30 34.84 140 5787 35540 3344392
Blood pressure increased 238.38 34.84 116 5811 22114 3357818
Malaise 238.12 34.84 169 5758 65008 3314924
Atrioventricular block complete 232.28 34.84 64 5863 2368 3377564
Circulatory collapse 228.33 34.84 78 5849 5971 3373961
Exposure via ingestion 227.88 34.84 57 5870 1436 3378496

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC C07AB03 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, selective
ATC C07BB03 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND THIAZIDES
Beta blocking agents, selective, and thiazides
ATC C07CB03 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND OTHER DIURETICS
Beta blocking agents, selective, and other diuretics
ATC C07CB53 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND OTHER DIURETICS
Beta blocking agents, selective, and other diuretics
ATC C07DB01 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, THIAZIDES AND OTHER DIURETICS
Beta blocking agents, selective, thiazides and other diuretics
ATC C07FB03 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents and calcium channel blockers
FDA EPC N0000175556 beta-Adrenergic Blocker
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D058671 Adrenergic beta-1 Receptor Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013565 Sympatholytics

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Myocardial infarction indication 22298006 DOID:5844
Hypertensive disorder indication 38341003 DOID:10763
Angina pectoris indication 194828000
Anuria contraindication 2472002 DOID:2983
Psoriasis contraindication 9014002 DOID:8893
Hypercholesterolemia contraindication 13644009
Complete atrioventricular block contraindication 27885002
Depressive disorder contraindication 35489007 DOID:2848
Hyperuricemia contraindication 35885006 DOID:1920
Anaphylaxis contraindication 39579001
Hypokalemia contraindication 43339004
Diabetes mellitus type 2 contraindication 44054006 DOID:9352
Diabetes mellitus type 1 contraindication 46635009 DOID:9744
Sinus bradycardia contraindication 49710005
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Hypercalcemia contraindication 66931009 DOID:12678
Hypochloremic alkalosis contraindication 70134007
Oliguria contraindication 83128009
Cardiogenic shock contraindication 89138009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Asthma contraindication 195967001 DOID:2841
Acute pancreatitis contraindication 197456007 DOID:2913
Raynaud's phenomenon contraindication 266261006
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Acutely Decompensated HF Requiring Parenteral Inotropic Therapy contraindication
First Degree Atrioventricular Heart Block contraindication
Chronic heart failure off-label use 48447003
Atrial fibrillation off-label use 49436004 DOID:0060224
Thyrotoxicosis off-label use 90739004 DOID:7997
Mitral valve prolapse off-label use 409712001 DOID:988
Diastolic heart failure off-label use 418304008 DOID:9775
Essential tremor off-label use 609558009 DOID:4990
Pheochromocytoma Adjunct Therapy off-label use
Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation off-label use
Migraine Prevention off-label use
Prevention of Congenital Long QT Syndrome associated Ventricular Arrhythmia off-label use

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.92 acidic
pKa2 9.19 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 7.30 WOMBAT-PK CHEMBL
Adenosine receptor A3 GPCR IC50 8.75 CHEMBL
Beta-2 adrenergic receptor GPCR Kd 5.80 WOMBAT-PK
Beta-2 adrenergic receptor GPCR Kd 5.93 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 7.62 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5 CHEMBL

External reference:

scroll-->
IDSource
DB00335 DRUGBANK_ID
548 IUPHAR_LIGAND_ID
4018460 VUID
N0000146784 NUI
C0004147 UMLSCUI
D00235 KEGG_DRUG
CHEMBL24 ChEMBL_ID
50VV3VW0TI UNII
3801 INN_ID
2249 PUBCHEM_CID
353 MMSL
1202 RXNORM
387506000 SNOMEDCT_US
87652004 SNOMEDCT_US
4225 MMSL
d00004 MMSL
4018460 VANDF
N0000146784 NDFRT
N0000006639 NDFRT
001855 NDDF
CHEBI:55352 CHEBI
D001262 MESH_DESCRIPTOR_UI
2TN PDB_CHEM_ID

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0093-0752 TABLET 50 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0093-0753 TABLET 100 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0093-0787 TABLET 25 mg ORAL ANDA 12 sections
TENORMIN HUMAN PRESCRIPTION DRUG LABEL 1 0310-0101 TABLET 100 mg ORAL NDA 12 sections
TENORMIN HUMAN PRESCRIPTION DRUG LABEL 1 0310-0105 TABLET 50 mg ORAL NDA 12 sections
TENORMIN HUMAN PRESCRIPTION DRUG LABEL 1 0310-0107 TABLET 25 mg ORAL NDA 12 sections
TENORETIC HUMAN PRESCRIPTION DRUG LABEL 2 0310-0115 TABLET 50 mg ORAL NDA 16 sections
TENORETIC HUMAN PRESCRIPTION DRUG LABEL 2 0310-0117 TABLET 100 mg ORAL NDA 16 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0378-0218 TABLET 25 mg ORAL ANDA 11 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0378-0231 TABLET 50 mg ORAL ANDA 11 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0378-0757 TABLET 100 mg ORAL ANDA 11 sections
Atenolol and Chlorthalidone HUMAN PRESCRIPTION DRUG LABEL 2 0378-2063 TABLET 50 mg ORAL ANDA 11 sections
Atenolol and Chlorthalidone HUMAN PRESCRIPTION DRUG LABEL 2 0378-2064 TABLET 100 mg ORAL ANDA 11 sections
Atenolol and Chlorthalidone HUMAN PRESCRIPTION DRUG LABEL 2 0591-5782 TABLET 50 mg ORAL ANDA 12 sections
Atenolol and Chlorthalidone HUMAN PRESCRIPTION DRUG LABEL 2 0591-5783 TABLET 100 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0615-3532 TABLET 50 mg ORAL ANDA 11 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0615-3533 TABLET 100 mg ORAL ANDA 11 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0615-3544 TABLET 25 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8026 TABLET 25 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8027 TABLET 50 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0781-1078 TABLET 25 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0781-1506 TABLET 50 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0781-1507 TABLET 100 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0781-5220 TABLET 25 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0781-5225 TABLET 50 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0781-5229 TABLET 100 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 0904-5392 TABLET 25 mg ORAL ANDA 12 sections
Atenolol and Chlorthalidone HUMAN PRESCRIPTION DRUG LABEL 2 0904-6200 TABLET 50 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 10544-031 TABLET 50 mg ORAL ANDA 12 sections
Atenolol HUMAN PRESCRIPTION DRUG LABEL 1 10544-126 TABLET 25 mg ORAL ANDA 12 sections