Peringatan Keamanan

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

Sotalol

DB00489

small molecule approved

Deskripsi

Sotalol is a methanesulfonanilide developed in 1960.A178579 It was the first of the class III anti arrhythmic drugs.A178579 Sotalol was first approved as an oral tablet on 30 October 1992.L6334 A racemic mixture of sotalol is currently formulated as a tablet, oral solution, and intravenous injection indicated for life threatening ventricular arrhythmias and maintaining normal sinus rhythm in atrial fibrillation or flutter.Label,L6373,L6376

Struktur Molekul 2D

Berat 272.364
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (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]
Volume Distribusi The apparent volume of distribution is 1.2-2.4L/kg.[Label,A178483]
Klirens (Clearance) In patients with a creatinine clearance >80mL/min, the plasma clearance is 6.78±2.72L/h and the renal clearance is 4.99±1.43L/h.[A178483] In patients with a creatinine clearance 30-80mL/min, the plasma clearance is 2.74±0.53L/h and the renal clearance is 2.00±0.67L/h.[A178483] In patients with a creatinine clearance 10-30mL/min, the plasma clearance is 1.56±0.44L/h and the renal clearance is 0.65±0.31L/h.[A178483] In patients with a creatinine clearance <10mL/min, the plasma clearance is 0.65±0.20L/h and the renal clearance is 0.27±0.13L/h.[A178483]

Absorpsi

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

Metabolisme

Sotalol is not metabolized.Label,A178483

Rute Eliminasi

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

Interaksi Makanan

1 Data
  • 1. Take with or without food. Oral sotalol with a meal reduces absorption by 20%.

Interaksi Obat

1404 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Sotalol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Sotalol is combined with Levodopa.
Risperidone Sotalol may increase the hypotensive activities of Risperidone.
Ceritinib Sotalol may increase the bradycardic activities of Ceritinib.
Ivabradine Sotalol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Sotalol.
Amiodarone The therapeutic efficacy of Sotalol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Sotalol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Sotalol.
Fingolimod Sotalol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Sotalol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Sotalol.
Methacholine Sotalol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Sotalol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Sotalol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Sotalol.
Regorafenib Regorafenib may increase the bradycardic activities of Sotalol.
Reserpine Reserpine may increase the hypotensive activities of Sotalol.
Deserpidine Deserpidine may increase the hypotensive activities of Sotalol.
Guanethidine Guanethidine may increase the hypotensive activities of Sotalol.
Rivastigmine Sotalol may increase the bradycardic activities of Rivastigmine.
Mirabegron The serum concentration of Sotalol can be increased when it is combined with Mirabegron.
Magnesium oxide The serum concentration of Sotalol can be decreased when it is combined with Magnesium oxide.
Aluminum hydroxide The serum concentration of Sotalol can be decreased when it is combined with Aluminum hydroxide.
Magnesium hydroxide The serum concentration of Sotalol can be decreased when it is combined with Magnesium hydroxide.
Magnesium trisilicate The serum concentration of Sotalol can be decreased when it is combined with Magnesium trisilicate.
Magnesium carbonate The serum concentration of Sotalol can be decreased when it is combined with Magnesium carbonate.
Magnesium silicate The serum concentration of Sotalol can be decreased when it is combined with Magnesium silicate.
Aluminium acetoacetate The serum concentration of Sotalol can be decreased when it is combined with Aluminium acetoacetate.
Magnesium peroxide The serum concentration of Sotalol can be decreased when it is combined with Magnesium peroxide.
Aluminium glycinate The serum concentration of Sotalol can be decreased when it is combined with Aluminium glycinate.
Aluminium phosphate The serum concentration of Sotalol can be decreased when it is combined with Aluminium phosphate.
Nicorandil Nicorandil may increase the hypotensive activities of Sotalol.
Insulin argine Sotalol may increase the hypoglycemic activities of Insulin argine.
Carbamoylcholine The risk or severity of adverse effects can be increased when Sotalol is combined with Carbamoylcholine.
Bethanechol The risk or severity of adverse effects can be increased when Sotalol is combined with Bethanechol.
Pilocarpine The risk or severity of adverse effects can be increased when Sotalol is combined with Pilocarpine.
Varenicline The risk or severity of adverse effects can be increased when Sotalol is combined with Varenicline.
Acetylcholine The risk or severity of adverse effects can be increased when Sotalol is combined with Acetylcholine.
Arecoline The risk or severity of adverse effects can be increased when Sotalol is combined with Arecoline.
Lobeline The risk or severity of adverse effects can be increased when Sotalol is combined with Lobeline.
NGX267 The risk or severity of adverse effects can be increased when Sotalol is combined with NGX267.
GTS-21 The risk or severity of adverse effects can be increased when Sotalol is combined with GTS-21.
Epibatidine The risk or severity of adverse effects can be increased when Sotalol is combined with Epibatidine.
Xanomeline The metabolism of Sotalol can be decreased when combined with Xanomeline.
Nicotine The risk or severity of adverse effects can be increased when Sotalol is combined with Nicotine.
Thiethylperazine The serum concentration of Sotalol can be increased when it is combined with Thiethylperazine.
Triflupromazine The serum concentration of Sotalol can be increased when it is combined with Triflupromazine.
Trifluoperazine The serum concentration of Sotalol can be increased when it is combined with Trifluoperazine.
Acetophenazine The serum concentration of Sotalol can be increased when it is combined with Acetophenazine.
Periciazine The serum concentration of Sotalol can be increased when it is combined with Periciazine.
Acepromazine The serum concentration of Sotalol can be increased when it is combined with Acepromazine.
Thioproperazine The serum concentration of Sotalol can be increased when it is combined with Thioproperazine.
BL-1020 The serum concentration of Sotalol can be increased when it is combined with BL-1020.
Cyamemazine The serum concentration of Sotalol can be increased when it is combined with Cyamemazine.
Propiopromazine The serum concentration of Sotalol can be increased when it is combined with Propiopromazine.
Perazine The serum concentration of Sotalol can be increased when it is combined with Perazine.
Butaperazine The serum concentration of Sotalol can be increased when it is combined with Butaperazine.
Chlorproethazine The serum concentration of Sotalol can be increased when it is combined with Chlorproethazine.
Thiazinam The serum concentration of Sotalol can be increased when it is combined with Thiazinam.
Dixyrazine The serum concentration of Sotalol can be increased when it is combined with Dixyrazine.
Perphenazine enanthate The serum concentration of Sotalol can be increased when it is combined with Perphenazine enanthate.
Ouabain Sotalol may increase the bradycardic activities of Ouabain.
Oleandrin Sotalol may increase the bradycardic activities of Oleandrin.
Proscillaridin Sotalol may increase the bradycardic activities of Proscillaridin.
Lanatoside C Sotalol may increase the bradycardic activities of Lanatoside C.
Gitoformate Sotalol may increase the bradycardic activities of Gitoformate.
Peruvoside Sotalol may increase the bradycardic activities of Peruvoside.
Lidocaine The serum concentration of Lidocaine can be increased when it is combined with Sotalol.
Icosapent Icosapent may decrease the antihypertensive activities of Sotalol.
Mesalazine The risk or severity of hyperkalemia can be increased when Mesalazine is combined with Sotalol.
Indomethacin Indomethacin may decrease the antihypertensive activities of Sotalol.
Nabumetone Nabumetone may decrease the antihypertensive activities of Sotalol.
Ketorolac Ketorolac may decrease the antihypertensive activities of Sotalol.
Tenoxicam Tenoxicam may decrease the antihypertensive activities of Sotalol.
Celecoxib Celecoxib may decrease the antihypertensive activities of Sotalol.
Tolmetin Tolmetin may decrease the antihypertensive activities of Sotalol.
Rofecoxib Rofecoxib may decrease the antihypertensive activities of Sotalol.
Piroxicam Piroxicam may decrease the antihypertensive activities of Sotalol.
Fenoprofen Fenoprofen may decrease the antihypertensive activities of Sotalol.
Valdecoxib Valdecoxib may decrease the antihypertensive activities of Sotalol.
Diclofenac Diclofenac may decrease the antihypertensive activities of Sotalol.
Sulindac Sulindac may decrease the antihypertensive activities of Sotalol.
Flurbiprofen Flurbiprofen may decrease the antihypertensive activities of Sotalol.
Etodolac Etodolac may decrease the antihypertensive activities of Sotalol.
Mefenamic acid Mefenamic acid may decrease the antihypertensive activities of Sotalol.
Naproxen Naproxen may decrease the antihypertensive activities of Sotalol.
Sulfasalazine Sulfasalazine may decrease the antihypertensive activities of Sotalol.
Phenylbutazone Phenylbutazone may decrease the antihypertensive activities of Sotalol.
Meloxicam Meloxicam may decrease the antihypertensive activities of Sotalol.
Carprofen Carprofen may decrease the antihypertensive activities of Sotalol.
Diflunisal Diflunisal may decrease the antihypertensive activities of Sotalol.
Salicylic acid Salicylic acid may decrease the antihypertensive activities of Sotalol.
Meclofenamic acid Meclofenamic acid may decrease the antihypertensive activities of Sotalol.
Acetylsalicylic acid Acetylsalicylic acid may decrease the antihypertensive activities of Sotalol.
Oxaprozin Oxaprozin may decrease the antihypertensive activities of Sotalol.
Ketoprofen Ketoprofen may decrease the antihypertensive activities of Sotalol.
Balsalazide Balsalazide may decrease the antihypertensive activities of Sotalol.
Ibuprofen Ibuprofen may decrease the antihypertensive activities of Sotalol.
Lumiracoxib Lumiracoxib may decrease the antihypertensive activities of Sotalol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8346722
    Hanyok JJ: Clinical pharmacokinetics of sotalol. Am J Cardiol. 1993 Aug 12;72(4):19A-26A.
  • PMID: 30003959
    Valdes SO, Miyake CY, Niu MC, de la Uz CM, Asaki SY, Landstrom AP, Schneider AE, Rusin CG, Patel R, Lam WW, Kim JJ: Early experience with intravenous sotalol in children with and without congenital heart disease. Heart Rhythm. 2018 Dec;15(12):1862-1869. doi: 10.1016/j.hrthm.2018.07.010. Epub 2018 Jul 10.
  • PMID: 30008082
    Staudacher I, Illg C, Chai S, Deschenes I, Seehausen S, Gramlich D, Muller ME, Wieder T, Rahm AK, Mayer C, Schweizer PA, Katus HA, Thomas D: Cardiovascular pharmacology of K2P17.1 (TASK-4, TALK-2) two-pore-domain K(+) channels. Naunyn Schmiedebergs Arch Pharmacol. 2018 Oct;391(10):1119-1131. doi: 10.1007/s00210-018-1535-z. Epub 2018 Jul 14.
  • PMID: 30561737
    Orvos P, Kohajda Z, Szlovak J, Gazdag P, Arpadffy-Lovas T, Toth D, Geramipour A, Talosi L, Jost N, Varro A, Virag L: Evaluation of Possible Proarrhythmic Potency: Comparison of the Effect of Dofetilide, Cisapride, Sotalol, Terfenadine, and Verapamil on hERG and Native IKr Currents and on Cardiac Action Potential. Toxicol Sci. 2019 Apr 1;168(2):365-380. doi: 10.1093/toxsci/kfy299.
  • PMID: 21125979
    Gorre F, Vandekerckhove H: Beta-blockers: focus on mechanism of action. Which beta-blocker, when and why? Acta Cardiol. 2010 Oct;65(5):565-70. doi: 10.2143/AC.65.5.2056244.
  • PMID: 27261833
    Kpaeyeh JA Jr, Wharton JM: Sotalol. Card Electrophysiol Clin. 2016 Jun;8(2):437-52. doi: 10.1016/j.ccep.2016.02.007.
  • PMID: 2861072
    Mills GA, Horn JR: Beta-blockers and glucose control. Drug Intell Clin Pharm. 1985 Apr;19(4):246-51.

Contoh Produk & Brand

Produk: 220 • International brands: 14
Produk
  • Apo-sotalol
    Tablet • 160 mg • Oral • Canada • Generic • Approved
  • Apo-sotalol
    Tablet • 80 mg • Oral • Canada • Generic • Approved
  • Ava-sotalol
    Tablet • 80 mg • Oral • Canada • Generic • Approved
  • Ava-sotalol
    Tablet • 160 mg • Oral • Canada • Generic • Approved
  • Betapace
    Tablet • 80 mg/1 • Oral • US • Approved
  • Betapace
    Tablet • 80 mg/1 • Oral • US • Approved
  • Betapace
    Tablet • 120 mg/1 • Oral • US • Approved
  • Betapace
    Tablet • 160 mg/1 • Oral • US • Approved
Menampilkan 8 dari 220 produk.
International Brands
  • Biosotal — Sanofi-Aventis
  • Cardol — Alphapharm
  • Darob — Abbott
  • Darob mite — Abbott
  • Hipecor — Merck
  • Loritmik — Krka
  • Rytmobeta — Abbott
  • Sotacor — Bristol-Myers Squibb
  • Sotagard — GlaxoSmithKline
  • Sotalex — Bristol-Myers Squibb

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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