Drug/Small Molecule:
sotalol

2D structure

Overview

Generic Names: Sotalol HCL
Trade Names: Betapace; Betapace AF; Sorine
PharmGKB Accession Id: PA451457

Description

An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias. PubChem (source: Drug Bank)

Indication

For the maintenance of normal sinus rhythm delay in time to recurrence of atrial fibrillation/atrial flutter (AFIB/AFL) in patients with symptomatic AFIB/AFL who are currently in sinus rhythm. Also for the treatment of documented life-threatening ventricular arrhythmias. (source: Drug Bank)

ATC Therapeutic Category

  • C07AA:Beta blocking agents, non-selective

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Sotalol has both beta-adrenoreceptor blocking (Vaughan Williams Class I) and cardiac action potential duration prolongation (Vaughan Williams Class I) antiarrhythmic properties. Sotalol is a racemic mixture of d- and l-sotalol. Both isomers have similar Class I antiarrhythmic effects, while the l-isomer is responsible for virtually all of the beta-blocking activity. (source: Drug Bank)

Pharmacology

Sotalol is an antiarrhythmic drug. It falls into the class of beta blockers (and class II antiarrhythmic agents) because of its primary action on the β-adrenergic receptors in the heart. In addition to its actions on the beta receptors in the heart, sotalol inhibits the inward potassium ion channels of the heart. In so doing, sotalol prolongs repolarization, therefore lengthening the QT interval and decreasing automaticity. It also slows atrioventricular (AV) nodal conduction. Because of these actions on the cardiac action potential, it is also considered a class III antiarrhythmic agent. The beta-blocking effect of sotalol is non-cardioselective, half maximal at about 80mg/day and maximal at doses between 320 and 640 mg/day. Sotalol does not have partial agonist or membrane stabilizing activity. Although significant beta-blockade occurs at oral doses as low as 25 mg, significant Class Ieffects are seen only at daily doses of 160 mg and above. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Sotalol is not metabolized. (source: Drug Bank)

Protein Binding

Sotalol does not bind to plasma proteins. (source: Drug Bank)

Absorption

In healthy subjects, the oral bioavailability of sotalol is 90-100%. Absorption is reduced by approximately 20% compared to fasting when administered with a standard meal. (source: Drug Bank)

Toxicity

The most common signs to be expected are bradycardia, congestive heart failure, hypotension, bronchospasm and hypoglycemia. In cases of massive intentional overdosage (2-16 grams) of sotalol the following clinical findings were seen: hypotension, bradycardia, cardiac asystole, prolongation of QT interval, Torsade de Pointes, ventricular tachy-cardia, and premature ventricular complexes. (source: Drug Bank)

Isomeric SMILES Code:

CC(C)NCC(c1ccc(cc1)NS(=O)(=O)C)O (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
KCNH2
  •   
  • PD
  •   
  • FA
  • GN
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
KCNH2 Uncurated Annotation (source: Drug Bank)

PharmGKB Curated Pathways

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Atrial Fibrillation
  •   
  •   
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Torsades de Pointes
  •   
  •   
  •   
  • FA
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Genetic Associations in Drug-induced QT Prolongation and Torsades
  2. Measured and Predicted Changes in QT Intervals During Atrial Fibrillation
  3. Physicochemical determinants of human renal clearance
  4. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00489
KEGG Compound ID:
C07309
PubChem Compound ID:
5253
PubChem Substance ID:
9517

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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