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.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
5.31 null [pKi] | |||
141.0 nM [Kd] | |||
Target ID: CHEMBL240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11090546 |
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 |
---|---|---|
Sequential map-guided endocardial resection for ventricular tachycardia improves outcome. | 2001 Apr |
|
The class III antiarrhythmic drugs dofetilide and sotalol prevent AF induction by atrial premature complexes at doses that fail to terminate AF. | 2001 Apr |
|
Control of vascular tone in notothenioid fishes is determined by phylogeny, not environmental temperature. | 2001 Apr |
|
Quantitative structure-retention and retention-activity relationships of beta-blocking agents by micellar liquid chromatography. | 2001 Apr 6 |
|
The effects of C-type natriuretic peptide on catecholamine release in the pacific spiny dogfish (Squalus acanthias). | 2001 Aug |
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Amplified effects of d,l-sotalol in canine dilated cardiomyopathy. | 2001 Dec |
|
Control of heart rate during thermoregulation in the heliothermic lizard Pogona barbata: importance of cholinergic and adrenergic mechanisms. | 2001 Dec |
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A review of class III antiarrhythmic agents for atrial fibrillation: maintenance of normal sinus rhythm. | 2001 Dec |
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Sotalol in treatment of pediatric cardiac arrhythmias. | 2001 Dec |
|
[Chronic hepatitis ascribed to the use of sotalol]. | 2001 Dec 1 |
|
[Atrial fibrillation successfully converted. A new standard in the prevention of recurrence?]. | 2001 Dec 13 |
|
Meta-analysis of the Risk of Torsades de Pointes in patients treated with intravenous racemic sotalol. | 2001 Feb |
|
[Supraventricular tachycardia and premature atrial contractions in fetus]. | 2001 Feb 17 |
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Mechanisms of action of antiarrhythmic drugs relative to the origin and perpetuation of cardiac arrhythmias. | 2001 Jan |
|
Sotalol vs metoprolol for ventricular rate control in patients with chronic atrial fibrillation who have undergone digitalization: a single-blinded crossover study. | 2001 Jan |
|
Evidence for the binding of beta-adrenoceptor blockers to microsomal Na+/K+-ATPase in guinea pig heart preparations. | 2001 Jan |
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Efficacy of sequential antiarrhythmic treatment in sinus rhythm maintenance after successful electrocardioversion in patients with chronic non-valvular atrial fibrillation. | 2001 Jan-Feb |
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Shortening the second phase duration of biphasic shocks: effects of class III antiarrhythmic drugs on defibrillation efficacy in humans. | 2001 Jul |
|
d,l-sotalol enhances baroreflex sensitivity in conscious rats surviving acute myocardial infarction. | 2001 Jul |
|
What niche will newer class III antiarrhythmic drugs occupy? | 2001 Jul |
|
Oral amiodarone and atrial fibrillation. | 2001 Jul 14 |
|
Transplacental treatment of fetal tachycardia: implications of drug transporting proteins in placenta. | 2001 Jun |
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Permanent junctional reciprocating tachycardia in infants and children: effectiveness of medical and non-medical treatment. | 2001 Jun |
|
Comparison of class III antiarrhythmic drugs versus digoxin for the reversion of new-onset atrial fibrillation. | 2001 Jun |
|
Phase 2 early afterdepolarization as a trigger of polymorphic ventricular tachycardia in acquired long-QT syndrome : direct evidence from intracellular recordings in the intact left ventricular wall. | 2001 Jun 12 |
|
[Protocols for the treatment of supraventricular tachycardias in the fetus]. | 2001 Jun 23 |
|
Does prophylaxis against atrial fibrillation after cardiac surgery reduce length of stay or hospital costs? | 2001 Mar |
|
Development and validation of an automated method for the liquid chromatographic determination of sotalol in plasma using dialysis and trace enrichment on a cation-exchange pre-column as on-line sample preparation. | 2001 Mar |
|
Pharmacokinetics and pharmacodynamics of sotalol in a pediatric population with supraventricular and ventricular tachyarrhythmia. | 2001 Mar |
|
Moxifloxacin: clinical efficacy and safety. | 2001 Mar 1 |
|
Termination of automatic atrial tachycardia in an infant by adequate sotalol dosing. Indication of clinically relevant age-dependent pharmacokinetics of sotalol. | 2001 May |
|
Non-invasive testing of acquired long QT syndrome: evidence for multiple arrhythmogenic substrates. | 2001 May |
|
Post-training injections of catecholaminergic drugs do not modulate fear conditioning in rats and mice. | 2001 May 4 |
|
Amiodarone -- waxed and waned and waxed again. | 2001 Nov |
|
An improved HPLC-fluorescence stereoselective method for analysis of (+)-S- and (-)-R-sotalol enantiomers in plasma sample. | 2001 Nov-Dec |
|
Atrial fibrillation: a risk factor for increased mortality--an AVID registry analysis. | 2001 Sep |
|
Long-term efficacy and safety of propafenone and sotalol for the maintenance of sinus rhythm after conversion of recurrent symptomatic atrial fibrillation. | 2001 Sep 15 |
|
Sotalol: the mechanism of its antiarrhythmic-defibrillating effect. | 2001 Summer |
|
Standardised in vitro electrophysiologic measurements using isolated perfused porcine hearts--assessment of QT interval alterations. | 2002 |
|
Amiodarone vs. sotalol as prophylaxis against atrial fibrillation/flutter after heart surgery: a meta-analysis. | 2002 Apr |
|
Dauricine-induced changes in monophasic action potentials and effective refractory period of rabbit left ventricle in situ. | 2002 Apr |
|
Flecainide and sotalol: a new combination therapy for refractory supraventricular tachycardia in children <1 year of age. | 2002 Feb 6 |
|
Comparison of the affinity of beta-blockers for two states of the beta 1-adrenoceptor in ferret ventricular myocardium. | 2002 Jan |
|
Rapid determination of partition coefficients between n-octanol/water for cardiovascular therapies. | 2002 Jan-Feb |
|
[Sudden cardiac death (part 2)]. | 2002 Mar |
|
Antidysrhythmic agents at the turn of the twenty-first century: a current review. | 2002 Mar |
|
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6259068
Sotalol caused significant stimulation of neutrophil motility at concentrations of more than 10−4 M.
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
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Record UNII |
A6D97U294I
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QC07AA57
Created by
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NDF-RT |
N0000175426
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NCI_THESAURUS |
C72900
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WHO-ATC |
C07BA07
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 |
QC07AA07
Created by
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FDA ORPHAN DRUG |
247707
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 |
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 | ||
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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 | ||
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DTXSID0023589
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PRIMARY | |||
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C61949
Created by
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PRIMARY | |||
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N0000008330
Created by
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PRIMARY | Cardiac Rhythm Alteration [PE] | ||
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A6D97U294I
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PRIMARY | |||
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D013015
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PRIMARY | |||
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SUB10607MIG
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PRIMARY | |||
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100000083797
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PRIMARY | |||
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9947
Created by
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PRIMARY | RxNorm | ||
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CHEMBL471
Created by
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PRIMARY | |||
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63622
Created by
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PRIMARY | |||
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SOTALOL
Created by
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PRIMARY | |||
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Sotalol
Created by
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PRIMARY | |||
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2464
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PRIMARY | |||
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5253
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PRIMARY | |||
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3930-20-9
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PRIMARY | |||
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DB00489
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PRIMARY | |||
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2350
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PRIMARY | |||
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A6D97U294I
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PRIMARY |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR | |||
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ENANTIOMER -> RACEMATE | |||
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TARGET -> INHIBITOR |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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