Top 8 Most Common and Used Beta Blockers for Adult
ATENOLOL
Action of Atenolol
It is a cardioselective ß1 blocker, reduces resting, exercise-induced heart rate as also myocardial contractility. It reduce systolic and diastolic blood pressure. Anginal attacks are reduced in intensity and frequency and exercise tolerance is improved.
Indications/Use of Atenolol
- Hypertension
- Angina pectoris
- Myocardial Infarction
Dosage of Atenolol
| 1 | Hypertensive | PO 25-50 mg OD, max 100 mg OD after 1-2 weeks if required. |
| 2 | Angina | 25-50 mg OD, max 100 mg OD within 1 week if required |
| 3 | Acute MI | (with haemodynamic stability): IV ( if within 12 hrs) 5-10 mg at 1 mg/mins in a CCU setting, follow 10-15 mins by PO 50 mg q 12hrs for 24 hrs. follow by PO mg (1 or 2 divided doses)/day. |
| 4 | Arrhythmia | If urgent, IV 2.5 mg at 1mg/mins, repeat if required 5 mins upto 10 mg or infusion 150 mg/kg over 20 mins. Repeat the above 12 hrs if required. Maintain 50-100 mg/day. |
| 5 | Dialysis | 25-5- mg followed by every dialysis |
Contraindications of Atenolol
- Sinus bradycardia
- 2nd or 3rd-degree heart block
- Cardiogenic shock
- overt cardiac failure
- Anaemia
- hypersensitivity reaction
Onset of effect: within 2-4 hrs
Duration of Action: 20-30 hrs
Drug Interactions
- Antacids: reduced atenolol absorption.
- Antiarrhythmics: Increased cardiac adverse effects
- Indomethacin: Decreased antihypertensive effect
Adverse Effects of Atenolol
- Rash
- Breathing difficulty
- Headache
- Fatigue / depression
- Myalgia
- Nightmares sleeplessness
- cold hands & feet
- bronchospasm
- Constipation and Paresthesia
Special Precautions
Use cautiously in chronic renal or hepatic dysfunction, poor circulation, asthma or bronchitis. Atenolol may have to be stopped prior to any surgery with general anaesthesia.
CARVEDILOL
Action of Carvedilol
It exerts antihypertensive activity by partly reducing total peripheral resistance and vasodilation by blocking receptors and partly by inhibiting ß mediated compensatory mechanism.
Indications/Use of Carvedilol
- Hypertension
- Stable Angina
- Unstable Angina
- Acute Myocardial Infarction
- Congestive Heart Failure
Dosage of Carvedilol
| 1 | Hypertension | PO 12.5 mg OD, then 25 mg/day after 2 wk: 50 mg OD if required |
| 2 | Stable Angina | PO 25-50 mg BID |
| 3 | Controlled CHF | PO 3.125 mg BID |
Contraindications of Carvedilol
- III degree heart block
- Shock
- Severe bradycardia
- Bronchial asthma
- Decompensated heart failure
- COPD
- Hepatic impairment
Drug Interactions
- Clonidine: barbiturates, tricyclic antidepressants, phenothiazines, vasodilating drugs.
- Alcohol: Increased carvedilol antihypertensive effects.
- Nifedipine: Probable sudden hypotension.
- Hypoglycemics: Intensified insulin/OHA effects.
- Anaesthetics: Negative inotropic effects.
Adverse Effects ( usually in early treatment)
- Postural Hypotension
- Dizziness
- Headache
- Dyspnoea
- Bronchospasm
- Bradycardia
- Malaise
- Asthenia
Special Precautions
- Avoid abrupt withdrawal.
- Can precipitate thyroid storm or exacerbation of hyperthyroidism.
- Liver injury.
- Vascular disease.
- Renal failure.
- Diabetes.
ESMOLOL
Action of Esmolol
Cardioselective ß1 blocker causes rapid decrease in ventricular rate and also has antihypertensive action.
Indications/Use of Esmolol
- Supraventricular tachycardia
- Perioperative tachycardia
- wherever ↓ in ventricular rate urgently required
Dosage of Esmolol
Loading dose of 500 μg/kg/min as an infusion for 1-minute followed by 50 μg/kg/min infusion for 4 minutes as a maintenance dose. If required, repeat the same loading dose followed by infusion of 100 μg/kg/min as a maintenance dose.
Contraindications of Esmolol
- Sinus bradycardia
- Heart block
- Cardiogenic shock
- Overt heart failure
Onset of Effect: Within 5 mins.
Duration of Action: Approx 9 mins.
Drug Interactions
- Increased bradycardia with CCBs.
- Increased hypertension risk with inotropes, adrenaline or noradrenaline.
- Increased blood digoxin level.
- Prolong neuromuscular blockade of suxamethonium.
- Increased serum level with warfarin.
Adverse Effects of Esmolol
- Prolonged bradycardia and hypotension.
- Dizziness.
- Headache.
- Confusion.
- Fatigue.
- paresthesia.
- Asthenia.
- Depression.
- Bronchospasm.
- Blurred Vision.
Special Precaution
- Use cautiously in hypotension.
- Depressed cardiac contractility.
- Diabetes Mellitus.
- Renal Impairment.
- Pregnancy, lactation and children
METOPROLOL
Actions of Metoprolol
It inhibits ß1 receptors, causes reduced heart rate and decreased blood pressure. Cardiac output is reduced. Renin release is inhibited.
Indications/use of metoprolol
- Hypertension.
- Angina pectoris.
- Acute myocardial infarction.
- Migraine prophylaxis.
- Thyrotoxicosis.
Dosage and Routes of Metoprolol
| Hypertension | PO 50 MG BD or 100 mg/day; may give up to 100-450 mg in divided doses;
Metoprolol Extended-Release 25-100 mg daily, maximum dose 400 mg/day |
| Myocardial Infarction | IV bolus: 5mg every 2 minutes × 3 times, 50 mg per orally every 6 hours starting 15 minutes after the last IV dose and continued for 48 hours |
| Heart Failure | PO Extended-Release 25 mg daily × 2 weeks (class ll); 12.5 mg daily (class lll) |
| Angina | PO 100 mg/day as a single dose or in 2 divided doses, Metoprolol succinate extended-release tablets: 100 mg orally once a day Maintenance dose: 100 to 400 mg per day |
| Migraine Prevention (unlabeled) | PO 25-100 mg bid; 50-200 mg daily. |
Contraindications of Metoprolol
- Hypersensitivity.
- Congestive cardiac failure.
- Patients on oral hypoglycaemic agents.
- Cardiogenic shock.
- COPD.
- 2nd or 3rd-degree heart block.
- Peripheral arterial disorders.
Onset of Effect: Within 1 hrs.
Duration of Action: Dose-dependent, the higher the dose, the longer the duration: 4 to 16 hrs.
Drug Interactions: Increased effect with reserpine, diuretics, NSAIDs. Increased myocardial depression with general anaesthetics.
Adverse Effects of Metoprolol
- Nausea.
- Vomiting.
- Headache.
- Dizziness.
- Diarrhoea.
- Bradycardia.
- Hypotension
Special Precautions
- Use cautiously in COPD.
- Congestive heart failure.
- Atrioventricular (AV) conduction disorder.
- Bradycardia.
- Peripheral arterial disease.
- Liver cirrhosis.
NEBIVOLOL
Action of Nebivolol
Competitively blocks the stimulation of ß-adrenergic receptors within the vascular smooth muscle; decreases the rate of SA node discharge: Increase recovery time; slows conduction of AV node, thereby resulting in decreased heart rate, which decreases O2 consumption in myocardium due to ß1 receptor antagonism.
Indications/use of Nebivolol
Treatment of essential hypertension with endothelial dysfunction, e.g., diabetes mellitus or hypercholesterolaemia and in patients with ischaemic heart disease.
Dosage of Nebivolol
- 5 mg once daily preferably at the same time of day.
Contraindications of NEBIVOLOL
- Cardiogenic shock.
- Sinus bradycardia.
- 2nd and 3rd-degree heart block.
- Bronchial asthma.
- CHF
- Severe hypoglycemia.
- It is contraindicated in pregnancy and lactation.
Onset of Effect: Within 1-3 hrs.
Duration of Action: 18-24 hrs.
Drug Interactions: Levels with cimetidine and chlorpromazine. Digitalis and anaesthetic agents: reduced heart rate, cardiac output.
Adverse Effects of Nebivolol
- Headache.
- Dizziness.
- Tiredness.
- Paraesthesia.
- Nausea
Special Precautions
- Avoid sudden withdrawal of the drug.
- Use cautiously in renal dysfunction.
- Diabetes mellitus.
- Thyrotoxicosis.
PROPRANOLOL
Action of Propranolol
It is a nonselective beta-blocker and reduces heart rate and cardiac output. Also decreases peripheral resistance on long term use. Blood pressure is reduced. Myocardial workload is also reduced. Propranolol reduces plasma renin activity. It has a membrane stabilizing action and is useful in arrhythmias.
Uses/Indications of Propranolol
- Hypertension
- Treatment of angina pectoris
- Supraventricular arrhythmias
- Post myocardial Infarction
- Tachycardia
- Hypertrophic obstructive cardiomyopathy
- Pheochromocytoma
Dosage of Propranolol
| Hypertension | PO 10-40 mg 3-4 times daily. Slow releasing (SR) tablet of 60-240 mg OD. |
| Post MI | PO 180-240 mg OD in divided doses. Essential tremors 40 mg BD increasing up to 240 or 320 mg/day is divided doses. |
| Pheochromocytoma | PO Only in association with a blocker 60 mg OD in divided doses for 3 days before surgery. |
Contraindications of Propranolol
- Cardiogenic shock
- Sinus bradycardia
- 2nd and 3rd-degree heart block
- Bronchial asthma
- CHF
- Severe hypoglycemia
Onset of Effect: 1-2 hrs
Duration of action: About 6-12 hrs
Drug Interactions
Effects with indomethacin and other NSAIDs. Levels with cimetidine and chlorpromazine. Digitalis and anaesthetic agents: reduced heart rate and cardiac output.
Adverse Effects
- Ethargy/fatigue
- Rash
- Cold hands and feet
- Nausea
- Fainting
- Breathlessness
- Bronchospasm
Special Precautions
- Abrupt dose eduction
- Ischemic heart disease
- Congestive cardiac failure
- Use cautiously in renal/hepatic dysfunction
Atenolol
Action of Atenolol
Competitively blocks the stimulation of ß-adrenergic receptor within vascular smooth muscle, produce negative chronotropic activity (decrease the rate of SA node discharge, increase recovery time), slows conduction of AV node, decrease heart rate, negative inotropic activity decrease O2 consumption in myocardium, decrease the action of renin aldosterone-angiotensin system at high doses, inhibits ß2 receptors in bronchial system at higher doses.
Uses/Indications of Atenolol
- Hypertension
- Myocardial Infarction
- Angina pectoris
Dosage of Atenolol
| Hypertension | PO stage 1 hypertension 12.5-25 mg OD, stage ll hypertensiion 50mg OD |
| Angina | PO 50 mg/day, 100 mg/day as needed after 7 days, maximum 200 mg/day |
|
PO 50 mg orally twice a day or 100 mg orally once a day, may need for 1-3 years after MI |
Contraindications of Atenolol
- Hypersensitivity to Atenolol
- Second and third-degree heart block
- Cardiogenic shock
Drug Interactions of Atenolol
Concomitant administration of indomethacin may reduce the antihypertensive effect of Atenolol. Disopyramide when given in combination with atenolol depresses myocardial contractility and may precipitate cardiac failure.
Adverse Effects
Very rare adverse events were reported. Fatigue, cold extremities, bradycardia and heart failure.
Special Precautions
- Use cautiously in renal failure
- Diabetes mellitus
- Pregnancy and lactation
SOTALOL
Mechanism of Action of Sotalol
It prolongs the plateau phase of the cardiac action potential in the isolated myocyte, as well as in isolated tissue preparations of ventricular or atrial muscle (class lll activity). Increased sinus cycle length (slowed heart rate). Decreased AV nodal conduction and increased AV nodal refractoriness and produces significant reductions in both systolic and diastolic blood pressures.
Uses/Indications of Sotalol
- Life-threatening ventricular dysrhythmias
- Betapace AF: to maintain sinus rhythm with symptomatic atrial fibrillation/flutter
Dosage of Sotalol
Initial dose is 80 mg twice daily, increased if necessary to 240 or 320 mg/day. or 480-640 mg/day in life-threatening refractory arrhythmias. Dose should be modified when creatinine clearance is lower than 60 ml/min.
Contraindications of Sotalol
- Sinus bradycardia sick sinus syndrome or second or second and third-degree AV block
- Congenital or acquired long QT syndromes
- Baseline QT interval >450 msec
- Cardiogenic shock
- Uncontrolled heart failure
- Hypokalemia
- Hypersensitivity
Adverse Effects od Sotalol
- Ventricular arrhythmia and non-alergic bronchospasms
- Nausea
- Insomnia
- Mask early signs of hypoglycaemia