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HomeMedicine NoteTop 8 Most Common and Used Beta Blockers for Adult, Atenolol, Carvedilol,...

Top 8 Most Common and Used Beta Blockers for Adult, Atenolol, Carvedilol, Esmolol, Metoprolol, Nebivolol, Propranolol, Atenolol, Sotalol

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

  1. Sinus bradycardia
  2. 2nd or 3rd-degree heart block
  3. Cardiogenic shock
  4. overt cardiac failure
  5. Anaemia
  6. 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

  1. Hypertension
  2. Stable Angina
  3. Unstable Angina
  4. Acute Myocardial Infarction
  5. 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

  1. III degree heart block
  2. Shock
  3. Severe bradycardia
  4. Bronchial asthma
  5. Decompensated heart failure
  6. COPD
  7. 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)

  1. Postural Hypotension
  2. Dizziness
  3. Headache
  4. Dyspnoea
  5. Bronchospasm
  6. Bradycardia
  7. Malaise
  8. Asthenia

Special Precautions

  1. Avoid abrupt withdrawal.
  2. Can precipitate thyroid storm or exacerbation of hyperthyroidism.
  3. Liver injury.
  4. Vascular disease.
  5. Renal failure.
  6. Diabetes.

ESMOLOL

 Action of Esmolol

Cardioselective ß1 blocker causes rapid decrease in ventricular rate and also has antihypertensive action.

Indications/Use of Esmolol

  1. Supraventricular tachycardia
  2. Perioperative tachycardia
  3. 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
  • Myocardial Infarction
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
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