General
Preferred name
SOTALOL
Synonyms
SOTALOL HYDROCHLORIDE ()
(±)-Sotalol hydrochloride ()
DEXSOTALOL ()
MJ-1999 ()
Sotalol HCl ()
Betapace ()
Betapace AF ()
Sotalol,(+) ()
Sotalol,(-) ()
Sotylize ()
Sorine ()
MJ 1999 ()
Sotacor ()
Beta-Cardone ()
Sotalex ()
DL-MJ-1999 ()
NSC-760358 ()
Darob ()
NSC-337251 ()
Darob mite ()
Dl-sotalol ()
C07AA07 ()
Sotalol (hydrochloride) ()
Sotalol-d6 (hydrochloride) ()
P&D ID
PD009998
CAS
959-24-0
27948-47-6
3930-20-9
1246820-85-8
Tags
natural product
drug
available
Approved by
FDA
First approval
1992
Drug Status
approved
Drug indication
Sinus rhythm disorder
Anti-Adrenergic (beta-receptor)
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS
Sotalol is a competitive inhibitor of the rapid potassium channel.[A178522] This inhibition lengthens the duration of action potentials and the refractory period in the atria and ventricles.[A178540,A178561] The inhibition of rapid potassium channels is increases as heart rate decreases, which is why adverse effects like torsades de points is more likely to be seen at lower heart rates.[A178579] L-sotalol also has beta adrenergic receptor blocking activity seen above plasma concentrations of 800ng/L.[A178579] The beta blocking ability of sotalol further prolongs action potentials.[A178579] D-sotalol does not have beta blocking activity but also reduces a patient's heart rate while standing or exercising.[A178579] These actions combine to produce a negative inotropic effect that reduces the strength of contractility of muscle cells in the heart.[A178522] Extension of the QT interval is also adversely associated with the induction of arrhythmia in patients.[A178561]; ; Hyperglycemia is a greater risk for non insulin dependant diabetics than insulin dependant diabetics.[A33725] Beta blockers inhibit insulin secretion which may cause hyperglycemia in type II diabetes mellitus.[A33725] The risk of hypoglycemia is higher in insulin dependant diabetes than non insulin dependant diabetics.[A33725] Beta blockers decrease secretion of insulin, which may mask hypoglycemia in an insulin dependant patient.[A33725] Beta blockers also increase glucose uptake into cells which may prolong or potentiate hypoglycemia.[A33725]; ; Further information regarding adverse reactions can be found here.[L6379]
MOA
Sotalol inhibits beta-1 adrenoceptors in the myocardium as well as rapid potassium channels to slow repolarization, lengthen the QT interval, and slow and shorten conduction of action potentials through the atria.[A178522,A178540,A178561,A34177] The action of sotalol on beta adrenergic receptors lengthens the sinus node cycle, conduction time through the atrioventricular node, refractory period, and duration of action potentials.[A178579]
INDICATION
Sotalol is indicated to treat life threatening ventricular arrhytmias and maintain normal sinus rhythm in patients with atrial fibrillation or flutter.[Label] There are also oral solutions and intravenous injections indicated for patients requiring sotalol, but for whom a tablet would not be appropriate.[Label,L6373,L6376]
ROE
80-90% of a given dose is excreted in the urine as unchanged sotalol.[Label,A178483] A small fraction of the doses is excreted in the feces as unchanged sotalol.[Label,A178483]
TOXICITY
Patients experiencing an overdose may present with bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia.[Label] Larger intentional overdoses may present as hypotension, bradycardia, cardiac asystole, prolonged QT interval, torsade de pointes, ventricular tachycardia, and premature ventricular complexes.[Label] Stop administering sotalol and observe the patient until the QT interval returns to normal and the heart rate rises above 50 beats per minute.[Label] Hemodialysis may help lower plasma concentrations of sotalol as it is not bound to plasma proteins.[Label] Bradycardia and cardiac asystole may be treated with [atropine], other anticholinergic drugs, beta adrenergic agonists, or transvenous cardiac pacing.[Label]. Second or third degree heart block may be treated with a transvenous cardiac pacemaker.[Label] Hypotension may be treated with [epinephrine] or [norepinephrine].[Label] Bronchospasm may be treated with [aminophylline] or a beta-2 agonist, possibly at higher than normal doses.[Label] Torsade de pointes may be treated with DC cardioversion, transvenous cardiac pacing, epinephrine, or [magnesium sulfate].[Label]; ; The oral LD50 for rats is 3450mg/kg, intraperitoneal LD50 for rats is 680mg/kg, oral LD50 for mice is 2600mg/kg, and intraperitoneal LD50 for mice is 670mg/kg.[MSDS]; ; Pregnant rabbits given 6 times the maximum recommended human dose showed an increase in fetal death and maternal toxicity, while rats given 18 times the maximum recommended human dose had an increased number of fetal resorptions.[Label] Sotalol is present in human breast milk so patients taking sotalol should not breast feed.[Label]; ; Sotalol has not been found to be carcinogenic.[Label] No studies have been performed regarding mutagenicity or clastogenicity.[Label] In animal studies, sotalol was not associated with a reduction in fertility aside from smaller litter sizes.[Label]; ; Further information regarding adverse reactions can be found here.[L6379]
METABOLISM
Sotalol is not metabolized.[Label,A178483]
ABSORPTION
Sotalol is 90-100% bioavailable.[Label,A178483] When taken with a meal, adsorption is lowered by 18%.[Label,A178483]; In patients with a creatinine clearance >80mL/min, the maximum concentration is 6.25±2.19.[A178483]
HALF-LIFE
The terminal elimination half life is 10-20 hours in healthy patients.[Label,A178483] In patients with a creatinine clearance >80mL/min, the half life is 17.5±0.97h.[A178483] In patients with a creatinine clearance 30-80mL/min, the half life is 22.7±6.4h.[A178483] In patients with a creatinine clearance 10-30mL/min, the half life is 64±27.2h.[A178483] In patients with a creatinine clearance <10mL/min, the half life is 97.9±57.3h.[A178483]
DESCRIPTION
Sotalol is a β-blocker & potassium channel blocker.
Marketed formulations may contain sotalol hydrochloride (PubChem CID 66245). (GtoPdb)
Marketed formulations may contain sotalol hydrochloride (PubChem CID 66245). (GtoPdb)
DESCRIPTION
5-HT1A partial agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Potent beta-adrenoceptor antagonist, a class III antiarrythmic; prolongs the action potential and increases the refractory period
(LOPAC library)
DESCRIPTION
β antagonist
(Tocriscreen Total)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
29
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
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Drug Repurposing Hub
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DrugBank Approved Drugs
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DrugCentral Approved Drugs
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DrugMAP Approved Drugs
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
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Ki Database
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
68
Molecular Weight
272.12
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
3
Rotatable Bonds
6
Ring Count
1
Aromatic Ring Count
1
cLogP
1.09
TPSA
78.43
Fraction CSP3
0.5
Chiral centers
1.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
beta
Pathway
GPCR/G protein
Membrane Transporter/Ion Channel
Target
??-adrenergic receptor
Potassium Channel
ADRB1, ADRB2, KCNH2
Adrenergic Receptor
Primary Target
Non-selective Adrenergic ? Receptors
MOA
Antagonist
Adrenergic Receptor antagonist
Indication
atrial fibrillation (AF), ventricular arrhythmias
Therapeutic Class
Antiarrhythmic Agents
Source data
