Sotalol

Source: Wikipedia, the free encyclopedia.
Sotalol
Clinical data
Trade namesBetapace, Sorine, Sotylize, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa693010
License data
Pregnancy
category
  • AU: C
By mouth
Drug classBeta blocker
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability90–100%[3]
MetabolismNot metabolized[3]
Elimination half-life12 hours[3]
ExcretionKidney
Mammary gland (In lactating individuals)[3]
Identifiers
  • (RS)-N-{4-[1-hydroxy-2-(propan-2-ylamino)ethyl]phenyl}methanesulfonamide
JSmol)
ChiralityRacemic mixture
  • O=S(=O)(Nc1ccc(cc1)C(O)CNC(C)C)C
  • InChI=1S/C12H20N2O3S/c1-9(2)13-8-12(15)10-4-6-11(7-5-10)14-18(3,16)17/h4-7,9,12-15H,8H2,1-3H3 checkY
  • Key:ZBMZVLHSJCTVON-UHFFFAOYSA-N checkY
  (verify)

Sotalol, sold under the brand name Betapace among others, is a medication used to treat and prevent

injection into a vein.[1]

Common side effects include a

Sotalol was first described in 1964 and came into medical use in 1974.

generic medication.[4] In 2020, it was the 296th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[6][7]

Medical uses

According to the U.S.

ventricular arrhythmias (e.g., ventricular tachycardia), or very symptomatic atrial fibrillation or flutter.[8] Due to the risk of serious side effects, the FDA states that sotalol should generally be reserved for people whose ventricular arrhythmias are life-threatening, or whose fibrillation/flutter cannot be resolved using the Valsalva maneuver or another simple method.[8] Sotalol has shown some potential efficacy against symptoms of essential tremor due to its binding to the β2-adrenergic receptor but this remains an off-label use.[9]

Contraindications

According to the FDA, sotalol should not be used in people with a waking heart rate lower than 50 beats per minute.

pacemaker is present.[8]

Since sotalol is removed from the body through the kidneys, it should not be used in people with a

breastfeed while taking sotalol.[8]

Since sotalol prolongs the QT interval, the FDA recommends against using it in conjunction with other medications that prolong the QT interval.[8] Studies have found serious side effects to be more common in individuals also taking digoxin, possibly because of pre-existing heart failure in those people.[8] As with other beta blockers, it may interact with calcium channel blockers, catecholamine-depleting drugs, insulin or antidiabetic drugs, β2-adrenergic receptor agonists, and clonidine.[8]

Some evidence suggests that sotalol should be avoided in the setting of heart failure with a reduced ejection fraction (resulting in the heart squeezing little blood out into the circulation with each pump) due to an increased risk of death.[10]

Adverse effects

Over 10% of oral sotalol users experience

a sensation of the heart beating too hard, fast, or irregularly, or chest pain. Higher doses of sotalol increase the risk for all of these possible side effects.[3]

In rare cases, the

congestive heart failure.[3] The incidence of TdP for sustained ventricular tachycardia patients was 0% with an 80 mg daily dose, 0.5% at 160 mg, 1.6% at 320 mg, 4.4% at 480 mg, 3.7% at 640 mg, and 5.8% at doses greater than 640 mg.[3] Due to this risk, the U.S. Food and Drug Administration requires affected individuals to be hospitalized for at least three days in a facility that can provide cardiac resuscitation and continuous electrocardiographic monitoring upon starting or restarting sotalol.[3]

Pharmacology

Mechanisms of action

Beta-blocker action

Sotalol is a

Without the binding of catecholamines to the β-adrenergic receptor, the

cyclic AMP, which is responsible for turning on calcium inflow channels.[13] A decrease in activation of calcium channels will therefore result in a decrease in intracellular calcium. In heart cells, calcium is important in generating electrical signals for heart muscle contraction, as well as generating force for this contraction.[14] In consideration of these important properties of calcium, two conclusions can be drawn. First, with less calcium in the cell, there is a decrease in electrical signals for contraction, thus allowing time for the heart's natural pacemaker to rectify arrhythmic contractions.[15] Secondly, lower calcium means a decrease in strength and rate of the contractions, which can be helpful in treatment of abnormally fast heart rates.[15]

Type III antiarrhythmic action

Sotalol also acts on potassium channels and causes a delay in relaxation of the ventricles.[16] By blocking these potassium channels, sotalol inhibits efflux of K+ ions, which results in an increase in the time before another electrical signal can be generated in ventricular myocytes.[14] This increase in the period before a new signal for contraction is generated, helps to correct arrhythmias by reducing the potential for premature or abnormal contraction of the ventricles but also prolongs the frequency of ventricular contraction to help treat tachycardia.[medical citation needed]

Pharmacokinetics

Sotalol is classified as a beta blocker with low

neuropsychiatric side effects.[12]

History

Sotalol was first synthesized in 1960 by A. A. Larsen of Mead-Johnson Pharmaceutical.[17] It was originally recognized for its blood pressure lowering effects and its ability to reduce the symptoms of angina.[18] It was made available in the United Kingdom and France in 1974, Germany in 1975, and Sweden in 1979.[18] It became widely used in the 1980s.[15] In the 1980s, its antiarrhythmic properties were discovered.[18] The United States approved the drug in 1992.[19]

Society and culture

Brand names

Trade names for Sotalol include Betapace and Betapace AF (

Bristol-Myers Squibb), and Sotylize (Arbor Pharmaceuticals).[8]

References

  1. ^ a b c d e f "Sotalol Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
  2. FDA
    . Retrieved 22 Oct 2023.
  3. ^ a b c d e f g h i U.S. Food and Drug Administration (July 2009). "Sotalol: Full Prescribing Information" (PDF). Retrieved 23 April 2015.
  4. ^ .
  5. .
  6. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  7. ^ "Sotalol - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  8. ^ a b c d e f g h i j k "Sotylize- sotalol hydrochloride solution". DailyMed. 3 December 2018. Retrieved 1 June 2020.
  9. PMID 6310053
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  20. ^ "Betapace- sotalol hydrochloride tablet Betapace AF- sotalol hydrochloride tablet". DailyMed. 10 August 2018. Retrieved 1 June 2020.