Sotalol
Sotalol
Generic Name
Sotalol
Mechanism
- β‑Blockade – Inhibits β₁ and β₂ adrenergic receptors, reducing sympathetic tone, slowing AV nodal conduction, and decreasing heart rate.
- Class III Activity – Prolongs repolarization by blocking potassium (K⁺) channels (IKr), lengthening the action potential and QT interval.
- Combined effect – Provides rate control in atrial fibrillation while preventing ventricular tachycardia via potassium‑channel blockade.
Pharmacokinetics
- Absorption – Oral bioavailability ≈ 90 %; peak plasma levels in 1–2 h.
- Distribution – Vd ≈ 0.7 L/kg; binds ≈ 10 % to plasma proteins.
- Metabolism – Minimal hepatic metabolism; primarily renal excretion.
- Half‑life – 12–18 h (IV) and 10–12 h (oral); dose accordingly in renal impairment.
- Drug interactions – Potentiation of β‑blocker β‑agonists; concomitant QT‑prolonging agents (e.g., erythromycin, azithromycin) ↑ arrhythmia risk.
Indications
- Atrial fibrillation/flutter – Maintenance of sinus rhythm, rate control in uncontrolled AF.
- Ventricular tachycardia – Prevents sustained monomorphic VT and degenerates into ventricular fibrillation.
- Post‑myocardial infarction – Secondary prevention of sudden cardiac death in high‑risk patients.
Contraindications
- Absolute contraindications
- Sick sinus syndrome (without pacemaker)
- Second‑ or third‑degree AV block (without pacemaker)
- Bradycardia < 50 bpm
- Severe hypotension or cardiogenic shock
- Warnings
- QT prolongation → torsades de pointes, especially with renal impairment or electrolyte abnormalities.
- Hypokalemia, hypomagnesemia, or hyperkalemia may compound QT changes.
- Concomitant use of other QT‑prolonging drugs.
Dosing
| Condition | Loading Dose | Maintenance Dose (oral) | Maintenance Dose (IV) |
| Atrial fibrillation | 80 mg PO BID (day 1), 80 mg QAM/PM (day 2–3) | 80 mg QAM/PM | 4 mg/kg IV over 48 h (in 250 mL NS) |
| Ventricular tachycardia | Same as AF | 80 mg QAM/PM | 4 mg/kg IV over 48 h |
• Renal: Reduce maintenance dose by 50 % when CrCl < 30 mL/min.
• Administration: Oral tablets; IV infusion over 48 h with continuous ECG monitoring.
Adverse Effects
- Common
- Fatigue, dizziness, bradycardia, hypotension, sinus node dysfunction.
- Gastrointestinal upset, nausea, bloating.
- Sleep disturbances (insomnia).
- Serious
- Torsades de pointes (QT > 500 ms).
- Severe sinus bradycardia or AV block.
- Hypotensive crisis.
- Severe electrolyte imbalance (esp. hypokalemia).
- Renal dysfunction (accumulation).
Monitoring
- Baseline
- ECG (QTc), electrolytes (K⁺, Mg²⁺, Ca²⁺), renal function.
- During therapy
- Twice daily ECG until QTc stabilizes < 450 ms (men) / < 460 ms (women).
- Renal function every 2–3 days for the first week, then every 2–4 weeks.
- Serum electrolytes when symptomatic or if QTc increases.
- Long‑term
- Annual ECG or sooner if symptoms develop.
Clinical Pearls
- Torsades Check – If the QTc > 500 ms, hold the drug, correct electrolytes, and consider alternative anti‑arrhythmic.
- Pacemaker Guidance – Patients with a pacing system may tolerate higher doses; nevertheless, monitor ECG closely for bradyarrhythmia.
- Renal Adjustment – Reduce the dose early; remember sotalol’s half‑life extends in CKD, raising systemic exposure.
- Drug‑Drug Caution – Avoid combining with other β‑blockers or K⁺‑channel blockers (e.g., amiodarone) unless on a carefully monitored regimen.
- Patient Education – Counsel patients on signs of bradycardia (dizziness, fainting) and to avoid sudden caffeine or alcohol cessation during initiation.
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• *For further reading, consult the latest guidelines from the American College of Cardiology/American Heart Association and UpToDate entries on sotalol therapy.*