sotalol indications/contra

Stem definitionDrug idCAS RN
aromatic ring -CH(-OH)-CH2-NH-R 2464 3930-20-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sotalol
  • DL-Sotalol
  • sotalol hydrochloride
  • sotylize
  • sotalol HCl
An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.
  • Molecular weight: 272.36
  • Formula: C12H20N2O3S
  • CLOGP: 0.23
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 3
  • TPSA: 78.43
  • ALOGS: -2.54
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.16 g O
0.16 g P

Approvals:

DateAgencyCompanyOrphan
Oct. 30, 1992 FDA COVIS PHARMA SARL

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
Electrocardiogram QT prolonged 512.90 44.91 115 977 10680 3374087
Torsade de pointes 511.98 44.91 93 999 2936 3381831
Bradycardia 488.69 44.91 120 972 16549 3368218
Ventricular tachycardia 313.07 44.91 69 1023 5793 3378974
Atrial fibrillation 246.27 44.91 76 1016 23865 3360902
Hypotension 235.56 44.91 88 1004 49426 3335341
Drug interaction 189.18 44.91 74 1018 46738 3338029
Cardiac arrest 183.97 44.91 63 1029 27256 3357511
Ventricular fibrillation 165.98 44.91 39 1053 4294 3380473
Completed suicide 146.11 44.91 55 1037 31059 3353708
Syncope 130.06 44.91 48 1044 25585 3359182
Cardiogenic shock 123.13 44.91 30 1062 3836 3380931
Toxicity to various agents 117.65 44.91 53 1039 47001 3337766
Dizziness 107.05 44.91 58 1034 76454 3308313
Drug ineffective 104.36 44.91 66 1026 116024 3268743
Arrhythmia 89.65 44.91 29 1063 10368 3374399
Foetal exposure during pregnancy 81.92 44.91 30 1062 15521 3369246
Acute kidney injury 81.55 44.91 42 1050 49641 3335126
Hyperkalaemia 79.36 44.91 27 1065 11267 3373500
Renal failure 78.61 44.91 36 1056 32904 3351863
Premature baby 78.18 44.91 24 1068 7229 3377538
Malaise 73.51 44.91 43 1049 65134 3319633
Presyncope 67.96 44.91 20 1072 5211 3379556
Loss of consciousness 67.85 44.91 31 1061 28116 3356651
Dyspnoea 66.89 44.91 48 1044 102886 3281881
Asthenia 65.38 44.91 40 1052 65625 3319142
Treatment failure 63.61 44.91 20 1072 6504 3378263
Ventricular extrasystoles 61.83 44.91 17 1075 3470 3381297
Urinary incontinence 56.81 44.91 18 1074 5994 3378773
Hypokalaemia 55.91 44.91 22 1070 13783 3370984

Pharmacologic Action:

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SourceCodeDescription
ATC C07AA07 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, non-selective
ATC C07BA07 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND THIAZIDES
Beta blocking agents, non-selective, and thiazides
ATC C07FX02 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents, other combinations
FDA EPC N0000175426 Antiarrhythmic
FDA PE N0000008330 Cardiac Rhythm Alteration
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
CHEBI has role CHEBI:35530 beta-adrenergic antagonist
CHEBI has role CHEBI:38070 anti-arrhythmia drug
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)

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DiseaseRelationSNOMED_IDDOID
Atrial fibrillation indication 49436004 DOID:0060224
Life-Threatening Ventricular Tachycardia indication
Bronchospasm contraindication 4386001
Complete atrioventricular block contraindication 27885002
Torsades de pointes contraindication 31722008
Sick sinus syndrome contraindication 36083008 DOID:13884
Anaphylaxis contraindication 39579001
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Sinus bradycardia contraindication 49710005
Diabetes mellitus contraindication 73211009 DOID:9351
Cardiogenic shock contraindication 89138009
Prolonged QT interval contraindication 111975006
Hypomagnesemia contraindication 190855004
Second degree atrioventricular block contraindication 195042002
Decompensated cardiac failure contraindication 195111005
Asthma contraindication 195967001 DOID:2841
Impaired renal function disorder contraindication 197663003
Pregnancy, function contraindication 289908002
Congenital long QT syndrome contraindication 442917000

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.95 acidic
pKa2 9.22 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
5MG/ML (5MG/ML) SOTYLIZE ARBOR PHARMS LLC N205108 Oct. 22, 2014 RX SOLUTION ORAL 9724297 Aug. 31, 2035 SOTYLIZE IS INDICATED FOR THE MAINTENANCE OF NORMAL SINUS RHYTHM [DELAY IN TIME TO RECURRANCE OF ATRIAL FIBRILLATION/ATRIAL FLUTTER (AFIB/AFL)] IN PATIENTS WITH SYMPTOMATIC AFIB/AFL WHO ARE CURRENTLY IN SINUS RHYTHM

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Potassium voltage-gated channel subfamily H member 2 Ion channel BLOCKER Ki 4 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR ANTAGONIST Ki 6.90 WOMBAT-PK CHEMBL
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 6.10 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR Kd 6.24 CHEMBL
Beta-2 adrenergic receptor GPCR IC50 5.30 CHEMBL

External reference:

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IDSource
DB00489 DRUGBANK_ID
4020814 VUID
N0000148334 NUI
C0037707 UMLSCUI
7297 IUPHAR_LIGAND_ID
D01026 KEGG_DRUG
CHEMBL471 ChEMBL_ID
5253 PUBCHEM_CID
4020814 VANDF
9947 RXNORM
372911006 SNOMEDCT_US
96301002 SNOMEDCT_US
d00371 MMSL
N0000006665 NDFRT
N0000148334 NDFRT
004111 NDDF
A6D97U294I UNII
2350 INN_ID
CHEBI:63622 CHEBI
CHEMBL1700 ChEMBL_ID
959-24-0 SECONDARY_CAS_RN
D013015 MESH_DESCRIPTOR_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-1060 TABLET 120 mg ORAL ANDA 17 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-1061 TABLET 80 mg ORAL ANDA 17 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-1062 TABLET 160 mg ORAL ANDA 17 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-1063 TABLET 240 mg ORAL ANDA 17 sections
sotalol hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0170 TABLET 120 mg ORAL ANDA 12 sections
sotalol hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0171 TABLET 80 mg ORAL ANDA 12 sections
sotalol hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0174 TABLET 240 mg ORAL ANDA 12 sections
sotalol hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0177 TABLET 160 mg ORAL ANDA 12 sections
Sorine HUMAN PRESCRIPTION DRUG LABEL 1 0245-0012 TABLET 80 mg ORAL ANDA 18 sections
Sorine HUMAN PRESCRIPTION DRUG LABEL 1 0245-0013 TABLET 120 mg ORAL ANDA 18 sections
Sorine HUMAN PRESCRIPTION DRUG LABEL 1 0245-0014 TABLET 160 mg ORAL ANDA 18 sections
Sorine HUMAN PRESCRIPTION DRUG LABEL 1 0245-0015 TABLET 240 mg ORAL ANDA 18 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-5123 TABLET 80 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-5124 TABLET 120 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-5125 TABLET 160 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0603-5769 TABLET 80 mg ORAL ANDA 18 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0603-5770 TABLET 120 mg ORAL ANDA 18 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0603-5771 TABLET 160 mg ORAL ANDA 18 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0603-5772 TABLET 240 mg ORAL ANDA 18 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-5552 TABLET 80 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7888 TABLET 80 mg ORAL ANDA 12 sections
sotalol hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 21695-397 TABLET 80 mg ORAL ANDA 12 sections
SOTYLIZE HUMAN PRESCRIPTION DRUG LABEL 1 24338-530 SOLUTION 5 mg ORAL NDA 19 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 35356-935 TABLET 80 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 35356-964 TABLET 160 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-121 TABLET 80 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-122 TABLET 120 mg ORAL ANDA 13 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-123 TABLET 160 mg ORAL ANDA 13 sections
sotalol hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 43063-133 TABLET 80 mg ORAL ANDA 12 sections
Sotalol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 43353-616 TABLET 80 mg ORAL ANDA 18 sections