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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/06/18 17:25:06」(JST)
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Sotalol
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|
Systematic (IUPAC) name |
(RS)-N-{4-[1-hydroxy-2-(propan-2-ylamino)ethyl]phenyl}methanesulfonamide |
Clinical data |
Trade names |
Betapace |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a693010 |
Pregnancy cat. |
B (US) |
Legal status |
℞ Prescription only |
Routes |
oral |
Pharmacokinetic data |
Bioavailability |
>95% |
Metabolism |
Not metabolized[citation needed] |
Half-life |
12 hours |
Excretion |
Renal
Lactic (In lactating females) |
Identifiers |
CAS number |
3930-20-9 Y |
ATC code |
C07AA07 |
PubChem |
CID 5253 |
DrugBank |
DB00489 |
ChemSpider |
5063 Y |
UNII |
A6D97U294I Y |
KEGG |
D08525 Y |
ChEMBL |
CHEMBL471 Y |
Chemical data |
Formula |
C12H20N2O3S |
Mol. mass |
272.3624 g/mol |
SMILES
- O=S(=O)(Nc1ccc(cc1)C(O)CNC(C)C)C
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InChI
-
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 Y
Key:ZBMZVLHSJCTVON-UHFFFAOYSA-N Y
|
Y (what is this?) (verify) |
Sotalol is a drug used in individuals with rhythm disturbances (cardiac arrhythmias) of the heart, and to treat hypertension in some individuals. It is a non-selective competitive β-adrenergic receptor blocker that also exhibits Class III antiarrhythmic properties by its inhibition of potassium channels.[1][2] Because of this dual action, Sotalol prolongs both the PR interval and the QT interval. Originally discovered around 1960, sotalol became widely used first as a β-blocker in the 1980s, and its function as an antiarrhythmic drug was discovered soon after.[3] Due to the dual action of sotalol, it is often used preferentially to other β-blockers as treatment for both ventricular fibrillation and ventricular tachycardia.[1][4]
Trade names for Sotalol include Betapace and Betapace AF (Berlex Laboratories), and Sotalex and Sotacor (Bristol-Myers Squibb).
Contents
- 1 Indications
- 1.1 Ventricular Fibrillation and Tachycardia
- 2 Mechanisms of Action
- 2.1 β-Blocker Action
- 2.2 Type III Antiarrhythmic Action
- 3 References
Indications
Sotalol is used to treat ventricular tachycardias[5] as well as atrial fibrillation.[6] Betapace AF is specifically labeled for atrial fibrillation.
Some evidence suggests that sotalol should be avoided in the setting of decreased ejection fraction due to an increased risk of death.[7]
It has also been suggested that it be used in the prevention of atrial fibrillation.[8]
Ventricular Fibrillation and Tachycardia
Ventricular fibrillation is an uncontrolled and asynchronous series of contractions of the ventricles resulting in poor cardiac output. It is often associated with factors that affect the electrical signal for contraction and trigger a premature contraction before complete relaxation.[9] Ventricular tachycardia is closely associated with ventricular fibrillation and is an abnormally high rate of contraction from the ventricles often resulting from increased intracellular calcium levels. This increase in cytosolic calcium leads to an increase in calcium release from the sarcoplasmic reticulum, which increases rate of contraction by providing more calcium for interaction with force-generating filaments in the muscle cell for a prolonged period of time.[10]
Mechanisms of Action
β-Blocker Action
Sotalol non-selectively binds to both β1- and β2-adrenergic receptors preventing activation of the receptors by their stimulatory ligand1. Without the binding of this ligand to the receptor, the G-protein complex associated with the receptor cannot activate production of cyclic AMP, which is responsible for turning on calcium inflow channels.[11] A decrease in activation of calcium channels will therefore result in a decrease in intracellular calcium. In cardiac cells, calcium is important in generating electrical signals for contraction, as well as generating force for contraction.[12] In consideration of these important properties of calcium, two conclusions can be drawn. Firstly, 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 contractions3. Secondly, lower calcium means a decrease in strength and rate of the contractions, which can be helpful in treatment of abnormally high heart rates in patients with tachycardia3.
Type III Antiarrhythmic Action
Sotalol also acts on potassium channels and causes a delay in relaxation of the ventricles2. 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 myocytes8. 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.
References
- ^ a b Bertrix, Lucien et al. Protection against ventricular and atrial fibrillation by sotalol. Cardiovascular Research 1986; 20, 358-363.
- ^ Edvardsson, N et al. Sotalol-induced delayed ventricular repolarization in man. European Heart Journal 1980; 1, 335-343
- ^ Antonaccio M, Gomoll A. Pharmacologic basis of the antiarrhythmic and hemodynamic effects of sotalol. Am J Cardiol 1993; 72, 27A-37A
- ^ Dorian P, Newman D. Effect of sotalol on ventricular fibrillation and defibrillation in humans. Am J Cardiol 1993; 72, 72A-79A
- ^ Boriani G, Lubinski A, Capucci A, et al. (December 2001). "A multicentre, double-blind randomized crossover comparative study on the efficacy and safety of dofetilide vs sotalol in patients with inducible sustained ventricular tachycardia and ischaemic heart disease". Eur. Heart J. 22 (23): 2180–91. doi:10.1053/euhj.2001.2679. PMID 11913480.
- ^ Singh BN, Singh SN, Reda DJ, et al. (May 2005). "Amiodarone versus sotalol for atrial fibrillation". N. Engl. J. Med. 352 (18): 1861–72. doi:10.1056/NEJMoa041705. PMID 15872201.
- ^ Waldo A, Camm A, deRuyter H, Friedman P, MacNeil D, Pauls J, Pitt B, Pratt C, Schwartz P, Veltri E (1996). "Effect of d-sotalol on mortality in patients with left ventricular dysfunction after recent and remote myocardial infarction. The SWORD Investigators. Survival With Oral d-Sotalol". Lancet 348 (9019): 7–12. doi:10.1016/S0140-6736(96)02149-6. PMID 8691967.
- ^ Patel A, Dunning J (April 2005). "Is Sotalol more effective than standard beta-blockers for the prophylaxis of atrial fibrillation during cardiac surgery". Interact Cardiovasc Thorac Surg 4 (2): 147–50. doi:10.1510/icvts.2004.102152. PMID 17670378.
- ^ Wiggers, C. The mechanism and nature of ventricular fibrillation. The American Heart Journal 1940; 20, 399-412
- ^ Priori, S et al. Mutations in the cardiac ryanodine receptor gene (hRyR2) underlie catecholaminergic polymorphic ventricular tachycardia. Circulation 2001; 103, 196-200
- ^ Charnet, P et al. cAMP-dependent phosphorylation of the cardiac L-type Ca channel: A missing link? Biochimie 1995; 77, 957-962
- ^ Kassotis, J et al. Beta receptor blockade potentiates the antiarryhthmic actions of d-sotalol on re-entrant ventricular tachycardia in a canine model of myocardial infarction. Journal of Cardiovascular Electrophysiology 2003; 14, 1233-1244
Beta blockers (C07)
|
|
Beta, nonselective |
- Alprenolol
- Bopindolol
- Bupranolol
- Carteolol
- Cloranolol
- Mepindolol
- Nadolol
- Oxprenolol
- Penbutolol
- Pindolol
- Propranolol
- Sotalol
- Tertatolol
- Timolol
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|
Beta1 selective |
- Acebutolol
- Atenolol
- Betaxolol
- Bevantolol
- Bisoprolol
- Celiprolol
- Epanolol
- Esmolol
- Nebivolol
- Metoprolol
- Practolol
- S-atenolol
- Talinolol
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|
Alpha + beta |
|
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Other/ungrouped |
|
|
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anat (a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot
|
noco/syva/cong/lyvd/tumr, sysi/epon, injr
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proc, drug (C2s+n/3/4/5/7/8/9)
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|
|
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Channel blockers
|
|
Calcium (Ca2+) |
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Potassium (K+) |
- 3,4-Diaminopyridine
- 4-Aminopyridine
- Amiodarone
- Bretylium
- Bunaftine
- Charybdotoxin
- Conotoxins
- Dofetilide
- Dronedarone
- E-4031
- Ibutilide
- Linopirdine
- Maurotoxin
- Nifekalant
- Paxilline
- Sotalol
- Tedisamil
- Tetraethylammonium
- Vernakalant
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Sodium (Na+) |
- Antiarrhythmics: Ajmaline
- Aprindine
- Disopyramide
- Dronedarone
- Encainide
- Flecainide
- Lidocaine
- Lorajmine
- Lorcainide
- Mexiletine
- Moricizine
- Phenytoin
- Pilsicainide
- Prajmaline
- Procainamide
- Propafenone
- Quinidine
- Sparteine
- Tocainide
- Anticonvulsants: Carbamazepine
- Eslicarbazepine acetate
- Ethotoin
- Fosphenytoin
- Licarbazepine
- Mephenytoin
- Oxcarbazepine
- Oxitriptyline
- Phenytoin
- Rufinamide
- Topiramate
- Sodium valproate
- Valnoctamide
- Valproate pivoxil
- Valproate semisodium
- Valproic acid
- Valpromide
- Diuretics: Amiloride
- Benzamil
- Triamterene
- Local anesthetics: pFBT
- Amylocaine
- Articaine
- Benzocaine
- Bupivacaine (Levobupivacaine, Ropivacaine)
- Butacaine
- Butamben
- Chloroprocaine
- Cinchocaine
- Cocaine
- Cyclomethycaine
- Dimethocaine
- Diphenhydramine
- Etidocaine
- Hexylcaine
- Iontocaine
- Lidocaine
- Mepivacaine
- Meprylcaine
- Metabutoxycaine
- Orthocaine
- Piperocaine
- Prilocaine
- Procaine
- Propoxycaine
- Proxymetacaine
- Risocaine
- Tetracaine
- Trimecaine
- Toxins: Conotoxins
- Neosaxitoxin
- Saxitoxin
- Tetrodotoxin
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Other |
- Uncategorized: Ethadione
- Paramethadione
- Phenacemide
- Pheneturide
- Trimethadione
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Antiarrhythmic agents (C01B)
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|
Channel blockers |
class I
(Na+ channel blockers)
|
class Ia (Phase 0→ and Phase 3→)
|
- Ajmaline
- Disopyramide
- Lorajmine
- Prajmaline
- Procainamide#
- Quinidine#
- Sparteine
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class Ib (Phase 3←)
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- IV (Lidocaine#)
- enteral (Aprindine
- Mexiletine
- Tocainide)
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class Ic (Phase 0→)
|
- Encainide‡
- Ethacizine
- Flecainide
- Indecainide‡
- Lorcainide
- Moracizine‡
- Propafenone
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|
|
class III
(Phase 3→, K+ channel blockers)
|
- Amiodarone
- Bretylium
- Bunaftine
- Dofetilide
- Dronedarone
- E-4031†
- Ibutilide
- Nifekalant
- Sotalol
- Tedisamil
- Vernakalant
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class IV
(Phase 4→, Ca2+ channel blockers)
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Receptor agonists
and antagonists |
class II
(Phase 4→, β blockers)
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- Nadolol
- Pindolol
- Propranolol
- cardioselective (Acebutolol
- Atenolol
- Esmolol
- Metoprolol)
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A1 agonist
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- Adenosine
- Benzodiazepines
- Barbiturates
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M2
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- muscarinic antagonist: Atropine
- Disopyramide
- Quinidine
muscarinic agonist: Digoxin
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α receptors
|
- Amiodarone
- Bretylium
- Quinidine
- Verapamil
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Ion transporters |
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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noco/cong/tumr, sysi/epon, injr
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proc, drug (C1A/1B/1C/1D), blte
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UpToDate Contents
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英文文献
- Analysis of unipolar electrograms in rabbit heart demonstrated the key role of ventricular apicobasal dispersion in arrhythmogenicity.
- Guérard N1, Jordaan P, Dumotier B.
- Cardiovascular toxicology.Cardiovasc Toxicol.2014 Dec;14(4):316-28. doi: 10.1007/s12012-014-9254-2.
- Reduced repolarization reserve and increased transmural dispersion of repolarization (TDR) are known risk factors for Torsade de Pointes development, but less is known about the role of apex-to-base (apicobasal) repolarization in arrhythmogenesis. Three needles were inserted in rabbit left ventricle
- PMID 24740433
- Atrial fibrillation (acute onset).
- Lip GY1, Apostolakis S.
- Clinical evidence.Clin Evid (Online).2014 Nov 27;2014. pii: 0210.
- INTRODUCTION: Acute atrial fibrillation is rapid, irregular, and chaotic atrial activity of recent onset. Various definitions of acute atrial fibrillation have been used in the literature, but for the purposes of this review we have included studies where atrial fibrillation may have occurred up to
- PMID 25430048
- Cost-effectiveness analysis of dronedarone versus amiodarone, propafenone and sotalol in patients with atrial fibrillation: results for Serbia.
- Tesic D1, Kostic M, Paunovic D, M Jankovic S.
- Kardiologia polska.Kardiol Pol.2014 Nov 27. doi: 10.5603/KP.a2014.0228. [Epub ahead of print]
- BACKGROUND AND AIM: Recent studies have shown that dronedarone was associated with significantly fewer adverse effects and treatment discontinuations and a trend toward reduced all-cause mortality compared with amiodarone. Introduction of dronedarone in clinical practice is limited by its higher cos
- PMID 25428811
和文文献
- Differing responses of human stem cell-derived cardiomyocytes to arrhythmogenic drugs, determined using impedance measurements
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関連リンク
-
- Sotalol Sotalol はa である 薬剤 リズムの妨害の個人で使用される(心臓不整脈) の 中心。 それはクラスにの分類される ベータブロッカー (及びクラスII antiarrhythmic 代理店) の第一次行為のためにか。-adrenergic 受容器 中心。 中心のベータ受 ...
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- 4040 円で安心の個人輸入!!心室期外収縮、心室頻拍、心房細動、心室細動などの不整脈治療薬!β受容体遮断による心房の心拍数減少効果と、カリウムチャンネルを遮断して刺激伝導による不応期を延長する事で心室細動を効果的に阻害!
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