Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C12H20N2O3S |
| Molecular Weight | 272.364 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)NCC(O)C1=CC=C(NS(C)(=O)=O)C=C1
InChI
InChIKey=ZBMZVLHSJCTVON-UHFFFAOYSA-N
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
| Molecular Formula | C12H20N2O3S |
| Molecular Weight | 272.364 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/sotalol.html
http://www.rxlist.com/betapace-drug.htm
http://www.wikidoc.org/index.php/Sotalol
Curator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/sotalol.html
http://www.rxlist.com/betapace-drug.htm
http://www.wikidoc.org/index.php/Sotalol
Sotalol has both beta-adrenoreceptor blocking and cardiac action potential duration prolongation antiarrhythmic properties. 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. It is FDA approved for the treatment of ventricular arrhythmias, symptomatic atrial fibtillation, symptomatic atriall flutter. Common adverse reactions include bradyarrhythmia, chest pain, lightheadedness, palpitations, rash, nausea, dizziness, headache, dyspnea, fatigue. Proarrhythmic events were more common in sotalol treated patients also receiving digoxin. Sotalol should be administered with caution in conjunction with calcium blocking drugs because of possible additive effects on atrioventricular conduction or ventricular function. Patients treated with sotalol plus a catecholamine depletor should therefore be closely monitored for evidence of hypotension and/or marked bradycardia which may produce syncope.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 5.31 null [pKi] | |||
| 141.0 nM [Kd] | |||
Target ID: CHEMBL240 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | BETAPACE Approved UseOral sotalol hydrochloride is indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that in the judgment of the physician are life-threatening. Because of the proarrhythmic effects of sotalol (see WARNINGS ), including a 1.5 to 2% rate of torsade de pointes or new VT/VF in patients with either NSVT or supraventricular arrhythmias, its use in patients with less severe arrhythmias, even if the patients are symptomatic, is generally not recommended. Treatment of patients with asymptomatic ventricular premature contractions should be avoided. Initiation of sotalol treatment or increasing doses, as with other antiarrhythmic agents used to treat life-threatening arrhythmias, should be carried out in the hospital. The response to treatment should then be evaluated by a suitable method (e.g., PES or Holter monitoring) prior to continuing the patient on chronic therapy. Various approaches have been used to determine the response to antiarrhythmic therapy, including sotalol. In the ESVEM Trial, response by Holter monitoring was tentatively defined as 100% suppression of ventricular tachycardia, 90% suppression of non-sustained VT, 80% suppression of paired VPCs, and 75% suppression of total VPCs in patients who had at least 10 VPCs/hour at baseline; this tentative response was confirmed if VT lasting 5 or more beats was not observed during treadmill exercise testing using a standard Bruce protocol. The PES protocol utilized a maximum of three extrastimuli at three pacing cycle lengths and two right ventricular pacing sites. Response by PES was defined as prevention of induction of the following: 1) monomorphic VT lasting over 15 seconds; 2) non-sustained polymorphic VT containing more than 15 beats of monomorphic VT in patients with a history of monomorphic VT; 3) polymorphic VT or VF greater than 15 beats in patients with VF or a history of aborted sudden death without monomorphic VT; and 4) two episodes of polymorphic VT or VF of greater than 15 beats in a patient presenting with monomorphic VT. Sustained VT or NSVT producing hypotension during the final treadmill test was considered a drug failure. In a multicenter open-label long-term study of sotalol in patients with life-threatening ventricular arrhythmias which had proven refractory to other antiarrhythmic medications, response by Holter monitoring was defined as in ESVEM. Response by PES was defined as non-inducibility of sustained VT by at least double extrastimuli delivered at a pacing cycle length of 400 msec. Overall survival and arrhythmia recurrence rates in this study were similar to those seen in ESVEM, although there was no comparative group to allow a definitive assessment of outcome. Antiarrhythmic drugs have not been shown to enhance survival in patients with ventricular arrhythmias. Sotalol is also indicated for the maintenance of normal sinus rhythm [delay in time to recurrence of atrial fibrillation/atrial flutter (AFIB/AFL) Launch Date1992 |
|||
| Primary | BETAPACE Approved UseOral sotalol hydrochloride is indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that in the judgment of the physician are life-threatening. Because of the proarrhythmic effects of sotalol (see WARNINGS ), including a 1.5 to 2% rate of torsade de pointes or new VT/VF in patients with either NSVT or supraventricular arrhythmias, its use in patients with less severe arrhythmias, even if the patients are symptomatic, is generally not recommended. Treatment of patients with asymptomatic ventricular premature contractions should be avoided. Initiation of sotalol treatment or increasing doses, as with other antiarrhythmic agents used to treat life-threatening arrhythmias, should be carried out in the hospital. The response to treatment should then be evaluated by a suitable method (e.g., PES or Holter monitoring) prior to continuing the patient on chronic therapy. Various approaches have been used to determine the response to antiarrhythmic therapy, including sotalol. In the ESVEM Trial, response by Holter monitoring was tentatively defined as 100% suppression of ventricular tachycardia, 90% suppression of non-sustained VT, 80% suppression of paired VPCs, and 75% suppression of total VPCs in patients who had at least 10 VPCs/hour at baseline; this tentative response was confirmed if VT lasting 5 or more beats was not observed during treadmill exercise testing using a standard Bruce protocol. The PES protocol utilized a maximum of three extrastimuli at three pacing cycle lengths and two right ventricular pacing sites. Response by PES was defined as prevention of induction of the following: 1) monomorphic VT lasting over 15 seconds; 2) non-sustained polymorphic VT containing more than 15 beats of monomorphic VT in patients with a history of monomorphic VT; 3) polymorphic VT or VF greater than 15 beats in patients with VF or a history of aborted sudden death without monomorphic VT; and 4) two episodes of polymorphic VT or VF of greater than 15 beats in a patient presenting with monomorphic VT. Sustained VT or NSVT producing hypotension during the final treadmill test was considered a drug failure. In a multicenter open-label long-term study of sotalol in patients with life-threatening ventricular arrhythmias which had proven refractory to other antiarrhythmic medications, response by Holter monitoring was defined as in ESVEM. Response by PES was defined as non-inducibility of sustained VT by at least double extrastimuli delivered at a pacing cycle length of 400 msec. Overall survival and arrhythmia recurrence rates in this study were similar to those seen in ESVEM, although there was no comparative group to allow a definitive assessment of outcome. Antiarrhythmic drugs have not been shown to enhance survival in patients with ventricular arrhythmias. Sotalol is also indicated for the maintenance of normal sinus rhythm [delay in time to recurrence of atrial fibrillation/atrial flutter (AFIB/AFL) Launch Date1992 |
|||
| Primary | BETAPACE Approved UseOral sotalol hydrochloride is indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that in the judgment of the physician are life-threatening. Because of the proarrhythmic effects of sotalol (see WARNINGS ), including a 1.5 to 2% rate of torsade de pointes or new VT/VF in patients with either NSVT or supraventricular arrhythmias, its use in patients with less severe arrhythmias, even if the patients are symptomatic, is generally not recommended. Treatment of patients with asymptomatic ventricular premature contractions should be avoided. Initiation of sotalol treatment or increasing doses, as with other antiarrhythmic agents used to treat life-threatening arrhythmias, should be carried out in the hospital. The response to treatment should then be evaluated by a suitable method (e.g., PES or Holter monitoring) prior to continuing the patient on chronic therapy. Various approaches have been used to determine the response to antiarrhythmic therapy, including sotalol. In the ESVEM Trial, response by Holter monitoring was tentatively defined as 100% suppression of ventricular tachycardia, 90% suppression of non-sustained VT, 80% suppression of paired VPCs, and 75% suppression of total VPCs in patients who had at least 10 VPCs/hour at baseline; this tentative response was confirmed if VT lasting 5 or more beats was not observed during treadmill exercise testing using a standard Bruce protocol. The PES protocol utilized a maximum of three extrastimuli at three pacing cycle lengths and two right ventricular pacing sites. Response by PES was defined as prevention of induction of the following: 1) monomorphic VT lasting over 15 seconds; 2) non-sustained polymorphic VT containing more than 15 beats of monomorphic VT in patients with a history of monomorphic VT; 3) polymorphic VT or VF greater than 15 beats in patients with VF or a history of aborted sudden death without monomorphic VT; and 4) two episodes of polymorphic VT or VF of greater than 15 beats in a patient presenting with monomorphic VT. Sustained VT or NSVT producing hypotension during the final treadmill test was considered a drug failure. In a multicenter open-label long-term study of sotalol in patients with life-threatening ventricular arrhythmias which had proven refractory to other antiarrhythmic medications, response by Holter monitoring was defined as in ESVEM. Response by PES was defined as non-inducibility of sustained VT by at least double extrastimuli delivered at a pacing cycle length of 400 msec. Overall survival and arrhythmia recurrence rates in this study were similar to those seen in ESVEM, although there was no comparative group to allow a definitive assessment of outcome. Antiarrhythmic drugs have not been shown to enhance survival in patients with ventricular arrhythmias. Sotalol is also indicated for the maintenance of normal sinus rhythm [delay in time to recurrence of atrial fibrillation/atrial flutter (AFIB/AFL) Launch Date1992 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
781 ng/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOTALOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
10402 ng × h/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOTALOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
12 h |
160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOTALOL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
Disc. AE: Lethargy, Bradycardia... Other AEs: Hypotension, Loss of taste... AEs leading to discontinuation/dose reduction: Lethargy (13 patients) Other AEs:Bradycardia (11 patient) Bronchospasm (6 patients) Nausea and vomiting (2 patients) Erectile dysfunction (2 patients) Visual disturbance (1 patient) Depression (1 patient) Hypotension (1 patient) Sources: Loss of taste (1 patient) |
640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
Other AEs: Chest pain, Dyspnea... Other AEs: Chest pain (15.4%) Sources: Dyspnea (20.5%) Palpitation (5.1%) Vasodilation (5.1%) Asthenia (20.5%) Dizziness (17.9%) Fatigue (25.6%) Headache (7.7%) Light-headed (5.1%) Sleep problem (7.7%) Upper respiratory tract signs and symptoms (12.8%) |
240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
Other AEs: Bradycardia, Diarrhea... Other AEs: Bradycardia (13.1%) Sources: Diarrhea (5.2%) Nausea and vomiting (7.8%) Abdominal pain NOS (3.9%) Fatigue (19.6%) Hyperhidrosis (5.2%) Weakness (5.2%) Musculoskeletal pain (2.6%) Dizziness (16.3%) Headache (3.3%) Cough (3.3%) Dyspnea (9.2%) |
320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
Other AEs: Bradycardia, Diarrhea... Other AEs: Bradycardia (12.3%) Sources: Diarrhea (5.7%) Nausea and vomiting (5.7%) Abdominal pain NOS (2.5%) Fatigue (18.9%) Hyperhidrosis (4.9%) Weakness (4.9%) Musculoskeletal pain (4.1%) Dizziness (13.1%) Headache (11.5%) Cough (2.5%) Dyspnea (9.8%) |
320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
Other AEs: Chest pain, Dyspnea... Other AEs: Chest pain (7.9%) Sources: Dyspnea (18.4%) Palpitation (7.9%) Asthenia (10.5%) Dizziness (13.2%) Fatigue (26.3%) Headache (5.3%) Light-headed (15.8%) Sleep problem (2.6%) Upper respiratory tract signs and symptoms (2.6%) Visual disturbance NOS (5.3%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Hypotension | 1 patient | 60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Loss of taste | 1 patient | 60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Depression | 1 patient Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Visual disturbance | 1 patient Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Bradycardia | 11 patient Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Lethargy | 13 patients Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Erectile dysfunction | 2 patients Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Nausea and vomiting | 2 patients Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Bronchospasm | 6 patients Disc. AE |
60 mg 2 times / day multiple, oral (mean) Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 31.8 years (range: 10-67 years) n = 82 Health Status: unhealthy Condition: congenital heart disease Age Group: 31.8 years (range: 10-67 years) Population Size: 82 Sources: |
| Upper respiratory tract signs and symptoms | 12.8% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Chest pain | 15.4% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Dizziness | 17.9% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Asthenia | 20.5% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Dyspnea | 20.5% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Fatigue | 25.6% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Light-headed | 5.1% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Palpitation | 5.1% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Vasodilation | 5.1% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Headache | 7.7% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Sleep problem | 7.7% | 640 mg/day multiple, oral Highest studied dose Dose: 640 mg/day Route: oral Route: multiple Dose: 640 mg/day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 39 Sources: |
| Bradycardia | 13.1% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Dizziness | 16.3% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Fatigue | 19.6% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Musculoskeletal pain | 2.6% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Cough | 3.3% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Headache | 3.3% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Abdominal pain NOS | 3.9% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Diarrhea | 5.2% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Hyperhidrosis | 5.2% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Weakness | 5.2% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Nausea and vomiting | 7.8% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Dyspnea | 9.2% | 240 mg/day multiple, oral (max) Recommended Dose: 240 mg/day Route: oral Route: multiple Dose: 240 mg/day Sources: |
unhealthy, adult n = 153 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 153 Sources: |
| Headache | 11.5% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Bradycardia | 12.3% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Dizziness | 13.1% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Fatigue | 18.9% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Abdominal pain NOS | 2.5% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Cough | 2.5% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Musculoskeletal pain | 4.1% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Hyperhidrosis | 4.9% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Weakness | 4.9% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Diarrhea | 5.7% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Nausea and vomiting | 5.7% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Dyspnea | 9.8% | 320 mg/day multiple, oral (max|total daily dose) Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 122 Health Status: unhealthy Condition: atrial fibrillation (AFIB) | atrial flutter (AFL) Age Group: adult Population Size: 122 Sources: |
| Asthenia | 10.5% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Dizziness | 13.2% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Light-headed | 15.8% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Dyspnea | 18.4% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Sleep problem | 2.6% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Upper respiratory tract signs and symptoms | 2.6% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Fatigue | 26.3% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Headache | 5.3% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Visual disturbance NOS | 5.3% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Chest pain | 7.9% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
| Palpitation | 7.9% | 320 mg/day multiple, oral Recommended Dose: 320 mg/day Route: oral Route: multiple Dose: 320 mg/day Sources: |
unhealthy, adult n = 38 Health Status: unhealthy Condition: ventricular ectopy Age Group: adult Population Size: 38 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no [IC50 >100 uM] | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Cardiac arrhythmias in pregnancy]. | 2001 |
|
| Quantitative structure-retention and retention-activity relationships of beta-blocking agents by micellar liquid chromatography. | 2001 Apr 6 |
|
| A case series of drug-induced long QT syndrome and Torsade de Pointes. | 2001 Dec |
|
| Control of heart rate during thermoregulation in the heliothermic lizard Pogona barbata: importance of cholinergic and adrenergic mechanisms. | 2001 Dec |
|
| A review of class III antiarrhythmic agents for atrial fibrillation: maintenance of normal sinus rhythm. | 2001 Dec |
|
| Pharmacologic management of atrial fibrillation: current therapeutic strategies. | 2001 Feb |
|
| Meta-analysis of the Risk of Torsades de Pointes in patients treated with intravenous racemic sotalol. | 2001 Feb |
|
| Which beta-blocker? | 2001 Feb 5 |
|
| The frequency analysis of signal-averaged ECG of P wave as predictor of efficacy of class III antiarrhythmic drugs to maintain sinus rhythm in recurrent idiopathic atrial fibrillation. | 2001 Jan |
|
| Developmental toxicity in the pregnant rabbit by the class III antiarrhythmic drug sotalol. | 2001 Jan |
|
| Efficacy of sequential antiarrhythmic treatment in sinus rhythm maintenance after successful electrocardioversion in patients with chronic non-valvular atrial fibrillation. | 2001 Jan-Feb |
|
| Permanent junctional reciprocating tachycardia in infants and children: effectiveness of medical and non-medical treatment. | 2001 Jun |
|
| [Protocols for the treatment of supraventricular tachycardias in the fetus]. | 2001 Jun 23 |
|
| Termination of automatic atrial tachycardia in an infant by adequate sotalol dosing. Indication of clinically relevant age-dependent pharmacokinetics of sotalol. | 2001 May |
|
| The canine Purkinje fiber: an in vitro model system for acquired long QT syndrome and drug-induced arrhythmogenesis. | 2001 May |
|
| Effect of Sotalol in the prevention of atrial fibrillation following coronary artery bypass grafting. | 2001 Oct |
|
| Drug treatment of fetal tachycardias. | 2002 |
|
| [Why is QT interval interesting?]. | 2002 Feb 4 |
|
| Flecainide and sotalol: a new combination therapy for refractory supraventricular tachycardia in children <1 year of age. | 2002 Feb 6 |
|
| Combination IK1 and IKr channel blockade: no additive lowering of the defibrillation threshold. | 2002 Jan |
|
| The cellular electrophysiologic effect of a new amiodarone like antiarrhythmic drug GYKI 16638 in undiseased human ventricular muscle: comparison with sotalol and mexiletine. | 2002 Jan |
|
| Rapid determination of partition coefficients between n-octanol/water for cardiovascular therapies. | 2002 Jan-Feb |
|
| Unique topographical distribution of M cells underlies reentrant mechanism of torsade de pointes in the long-QT syndrome. | 2002 Mar 12 |
|
| [Advanced prehospital treatment of heart arrest by the mobile emergency unit in Aarhus. 1-year survival after out-of-hospital heart arrest--with focus on response time, survival, the given treatment and admission]. | 2002 Mar 4 |
|
| Prenatal ultrasound may predict fetal response to therapy in non-hydropic fetuses with supraventricular tachycardia. | 2002 Mar-Apr |
|
| Preconditioning attenuates the shortening of recovery during coronary occlusion in isolated rabbit hearts with D-sotalol-induced long QT intervals. | 2002 May |
Sample Use Guides
In Vivo Use Guide
Curator's Comment: The recommended initial intravenous dose of sotalol is 75 mg (once or twice daily). The 75 mg dose can be titrated upward to 112.5 or 150 mg after at least 3 days.
https://www.drugs.com/pro/sotalol-injection.html
Initial dosage in adults is 80 mg twice daily. Increase the dose as needed in increments of 80 mg/day, every 3 days to a maximum 320 mg total daily dose.
Route of Administration:
Other
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 17:52:27 GMT 2023
by
admin
on
Sat Dec 16 17:52:27 GMT 2023
|
| Record UNII |
A6D97U294I
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| Record Status |
Validated (UNII)
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| Record Version |
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-
Download
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Brand Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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WHO-VATC |
QC07AA57
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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NDF-RT |
N0000175426
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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NCI_THESAURUS |
C72900
Created by
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WHO-ATC |
C07BA07
Created by
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WHO-VATC |
QC07AA07
Created by
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FDA ORPHAN DRUG |
247707
Created by
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NCI_THESAURUS |
C93038
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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WHO-VATC |
QC07BA07
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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WHO-ATC |
C07AA07
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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|
WHO-ATC |
C07AA57
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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|
WHO-ATC |
C07FX02
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
|
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|
LIVERTOX |
NBK548262
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
7297
Created by
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PRIMARY | |||
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m10124
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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PRIMARY | Merck Index | ||
|
DTXSID0023589
Created by
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PRIMARY | |||
|
C61949
Created by
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|
PRIMARY | |||
|
N0000008330
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
|
PRIMARY | Cardiac Rhythm Alteration [PE] | ||
|
A6D97U294I
Created by
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PRIMARY | |||
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D013015
Created by
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PRIMARY | |||
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SUB10607MIG
Created by
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|
PRIMARY | |||
|
100000083797
Created by
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PRIMARY | |||
|
9947
Created by
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PRIMARY | RxNorm | ||
|
CHEMBL471
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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PRIMARY | |||
|
63622
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
|
PRIMARY | |||
|
SOTALOL
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
|
PRIMARY | |||
|
Sotalol
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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PRIMARY | |||
|
2464
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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PRIMARY | |||
|
5253
Created by
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PRIMARY | |||
|
3930-20-9
Created by
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PRIMARY | |||
|
DB00489
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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PRIMARY | |||
|
2350
Created by
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PRIMARY | |||
|
A6D97U294I
Created by
admin on Sat Dec 16 17:52:28 GMT 2023 , Edited by admin on Sat Dec 16 17:52:28 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
TARGET -> INHIBITOR |
|
||
|
|
SALT/SOLVATE -> PARENT | |||
|
TARGET -> INHIBITOR | |||
|
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ENANTIOMER -> RACEMATE | |||
|
|
TARGET -> INHIBITOR |
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Biological Half-life | PHARMACOKINETIC |
|
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