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Saturday, August 9, 2025

Group II antiarrhythmics


Generic and Brand Names

  • Propranolol — Inderal, Inderal LA

  • Metoprolol — Lopressor, Toprol-XL

  • Esmolol — Brevibloc

  • Atenolol — Tenormin

  • Nadolol — Corgard

  • Bisoprolol — Zebeta


Class

  • Vaughan Williams Class II antiarrhythmics

  • Beta-adrenergic receptor antagonists (beta-blockers)

  • May be cardioselective (β1) or nonselective (β1 + β2)


Mechanism of Action

  • Block beta-adrenergic receptors, reducing sympathetic stimulation of the heart

  • Primary cardiac effects:

    • Decrease SA node automaticity → slower heart rate

    • Slow AV node conduction → increased refractory period

    • Reduce myocardial contractility (negative inotropy)

  • Reduce oxygen demand and suppress catecholamine-induced arrhythmias


Indications

  • Supraventricular arrhythmias (especially rate control in atrial fibrillation/flutter)

  • Ventricular arrhythmias precipitated by catecholamines (e.g., post-MI)

  • Prevention of sudden cardiac death in post-MI and heart failure patients

  • Long QT syndrome (congenital) to reduce arrhythmia risk

  • Rate control in inappropriate sinus tachycardia


Dosage and Administration

Propranolol

  • Oral: 10–40 mg 3–4 times daily or LA formulation 80–320 mg daily

  • IV (acute arrhythmia): 1 mg over 1 min, may repeat q2min up to 5 mg

Metoprolol

  • Oral: 25–100 mg 2–3 times daily (tartrate) or 50–200 mg once daily (succinate)

  • IV: 2.5–5 mg q2–5min up to 15 mg total

Esmolol

  • IV only: Bolus 500 mcg/kg over 1 min, then infusion 50–300 mcg/kg/min

  • Ultra–short acting, ideal for acute perioperative arrhythmia control

Atenolol

  • Oral: 25–100 mg once daily


Monitoring

  • Heart rate, blood pressure

  • ECG (PR interval, QRS duration, rhythm)

  • Signs of heart failure

  • Blood glucose in diabetic patients (masking of hypoglycaemia)


Contraindications

  • Severe bradycardia

  • 2nd- or 3rd-degree AV block without pacemaker

  • Sick sinus syndrome without pacemaker

  • Cardiogenic shock

  • Uncompensated heart failure

  • Severe asthma or COPD (nonselective beta-blockers)


Precautions

  • Use cardioselective agents in patients with mild-moderate reactive airway disease

  • Taper gradually to avoid rebound tachycardia, hypertension, and arrhythmia

  • Adjust dose in renal impairment for renally cleared agents (atenolol, nadolol)

  • Use with caution in diabetes — masks hypoglycaemic symptoms

  • Avoid abrupt discontinuation, especially in ischemic heart disease


Adverse Effects

  • Bradycardia, hypotension, fatigue, dizziness

  • Worsening heart failure in susceptible patients

  • Bronchospasm (nonselective agents)

  • Depression, vivid dreams (lipophilic agents like propranolol)

  • Sexual dysfunction, cold extremities


Drug Interactions

  • Calcium channel blockers (verapamil, diltiazem): Additive bradycardia, AV block, hypotension

  • Other antihypertensives: Additive hypotensive effect

  • Antiarrhythmics: Additive conduction suppression

  • Insulin/oral hypoglycaemics: Masking of hypoglycaemia symptoms

  • Clonidine: Rebound hypertension risk if clonidine withdrawn abruptly while on beta-blocker


Overdose

  • Manifestations: Severe bradycardia, hypotension, cardiogenic shock, bronchospasm, hypoglycaemia

  • Management:

    • Atropine for bradycardia

    • IV fluids and vasopressors for hypotension

    • Glucagon (increases cAMP independent of beta-receptors)

    • High-dose insulin–glucose therapy for severe cardiogenic shock

    • Temporary pacing if required


Patient Counselling

  • Take medication consistently at the same time each day

  • Do not stop suddenly without medical advice

  • Monitor pulse — report if <50 bpm with symptoms

  • In diabetes, monitor blood sugar closely — symptoms of low blood sugar may be masked

  • Report signs of worsening breathing difficulty (nonselective agents)



Comparison Table — Cardioselective vs Nonselective Beta-blockers

FeatureCardioselective (β1) — e.g., Metoprolol, Atenolol, BisoprololNonselective (β1 + β2) — e.g., Propranolol, Nadolol
Primary Cardiac EffectAV nodal slowing, reduced HR, ↓ contractilitySame, plus β2 blockade
Bronchospasm RiskLower (still possible at high doses)Higher
Use in Asthma/COPDPreferred (with caution)Avoid
Lipid SolubilityVaries — metoprolol (moderate), atenolol (low)Propranolol (high) — more CNS effects
Half-lifeAtenolol, bisoprolol: long; metoprolol: intermediateNadolol: long; propranolol: intermediate
Extra UsesPost-MI, heart failure, rate controlMigraine prophylaxis, essential tremor, thyrotoxicosis



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