Tìm theo
Sotalol
Các tên gọi khác (5 ) :
  • 4'-(1-Hydroxy-2-(isopropylamino)ethyl)methane sulfonanilide
  • beta-Cardone
  • Sotalol
  • Sotalolo
  • Sotalolum
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 3930-20-9
ATC: C07AA07, C07AA57
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C12H20N2O3S
PTK: 272.364
An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H20N2O3S
Phân tử khối
272.364
Monoisotopic mass
272.119463206
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
InChI Key
InChIKey=ZBMZVLHSJCTVON-UHFFFAOYSA-N
IUPAC Name
N-(4-{1-hydroxy-2-[(propan-2-yl)amino]ethyl}phenyl)methanesulfonamide
Traditional IUPAC Name
sotalol
SMILES
CC(C)NCC(O)C1=CC=C(NS(C)(=O)=O)C=C1
Độ tan chảy
206.5-207 °C
Độ hòa tan
Soluble (5510 mg/L)
logP
0.24
logS
-2.5
pKa (strongest acidic)
10.07
pKa (Strongest Basic)
9.43
PSA
78.43 Å2
Refractivity
71.12 m3·mol-1
Polarizability
29.34 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
4
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias. [PubChem] 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. Sotalol inhibits response to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium and β2-adrenergic receptors within bronchial and vascular smooth muscle. The electrophysiologic effects of sotalol may be due to its selective inhibition of the rapidly activating component of the potassium channel involved in the repolarization of cardiac cells. The class II electrophysiologic effects are caused by an increase in sinus cycle length (slowed heart rate), decreased AV nodal conduction, and increased AV nodal refractoriness, while the class III electrophysiological effects include prolongation of the atrial and ventricular monophasic action potentials, and effective refractory period prolongation of atrial muscle, ventricular muscle, and atrio-ventricular accessory pathways (where present) in both the anterograde and retrograde directions.
Dược Động Học :
▧ 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.
▧ Protein binding :
Sotalol does not bind to plasma proteins.
▧ Metabolism :
Sotalol is not metabolized.
▧ Route of Elimination :
Excretion is predominantly via the kidney in the unchanged form. Sotalol is excreted in the milk of laboratory animals and has been reported to be present in human milk.
▧ Half Life :
Mean elimination half-life is 12 hours. Impaired renal function in geriatric patients can increase the terminal elimination half-life.
Độc Tính : 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.
Chỉ Định : 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.
Tương Tác Thuốc :
  • Acetohexamide The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Aminophylline Antagonism of action and increased effect of theophylline
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Chlorpropamide The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Clarithromycin Increased risk of cardiotoxicity and arrhythmias
  • Clonidine Increased hypertension when clonidine stopped
  • Dihydroergotamine Ischemia with risk of gangrene
  • Disopyramide The beta-blocker, sotalol, may increase the toxicity of disopyramide.
  • Epinephrine Hypertension, then bradycardia
  • Ergotamine Ischemia with risk of gangrene
  • Erythromycin Increased risk of cardiotoxicity and arrhythmias
  • Fenoterol Antagonism
  • Fingolimod Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Formoterol Antagonism
  • Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Gliclazide The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Glyburide The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Ibuprofen Risk of inhibition of renal prostaglandins
  • Indomethacin Risk of inhibition of renal prostaglandins
  • Insulin Glargine The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Methyldopa Possible hypertensive crisis
  • Methysergide Ischemia with risk of gangrene
  • Moxifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Orciprenaline Antagonism
  • Oxtriphylline Antagonism of action and increased effect of theophylline
  • Pipobroman Antagonism
  • Piroxicam Risk of inhibition of renal prostaglandins
  • Prazosin Risk of hypotension at the beginning of therapy
  • Ranolazine Possible additive effect on QT prolongation
  • Repaglinide The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Telithromycin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Terbutaline Antagonism
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Theophylline Antagonism of action and increased effect of theophylline
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Berlex
    Sản phẩm biệt dược : Betapace
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Biosotal
  • Công ty : Alphapharm
    Sản phẩm biệt dược : Cardol
  • Công ty : Abbott
    Sản phẩm biệt dược : Darob
  • Công ty : Abbott
    Sản phẩm biệt dược : Darob mite
  • Công ty : Merck
    Sản phẩm biệt dược : Hipecor
  • Công ty : Krka
    Sản phẩm biệt dược : Loritmik
  • Công ty : Abbott
    Sản phẩm biệt dược : Rytmobeta
  • Công ty : Upsher-Smith
    Sản phẩm biệt dược : Sorine
  • Sản phẩm biệt dược : Sotacor
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Sotagard
  • Sản phẩm biệt dược : Sotalex
  • Sản phẩm biệt dược : Sotapor
  • Công ty : Adeka
    Sản phẩm biệt dược : Talozin
  • Sản phẩm biệt dược : Tan Shi
  • Sản phẩm biệt dược : Xi An Lin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00489
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5253
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505012
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07309
ChemSpider
http://www.chemspider.com/Chemical-Structure.5063.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25762
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0245-0012-11
PharmGKB
http://www.pharmgkb.org/drug/PA451457
Wikipedia
http://en.wikipedia.org/wiki/Sotalol
RxList
http://www.rxlist.com/cgi/generic/betapaceaf.htm
Drugs.com
http://www.drugs.com/cdi/sotalol.html
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