Propranolol

Propranolol- Antianginal Drugs for the management of heart disorders

ParametersDetails
Category of DrugPropranolol is Antianginal Drugs (beta-adrenergic receptor antagonist)
Mechanism of ActionPropranolol is a nonselective β-adrenergic receptor antagonist. It blocks β-adrenergic receptors leading to vasoconstriction. It also inhibits vascular endothelial growth factor.
StructureThumb
Indications (1)Propranolol is used for
1. Cardiac arrhythmias
2. Tachycardia
3. Hypertrophic obstructive cardiac myopathy
4. Pheochromocytoma
5. Thrombosis
6. Management of angina
7. essential and renal hypertension
8. Prophylaxis of migraine
Pharmacokinetic properties1. Tmax – 2 hours
2. Vd- 4L/kg
3. Protein binding- Approximately 90% of propranolol is protein-bound in plasma.
4. Metabolism- 17% of a dose undergoes glucuronidation and 42% undergo ring oxidation.
5. Route of elimination- 91% in the urine
6. Half-life- 8 hours.
Well Known
Pharmaceutical Brands
1. CIPLAR- CIPLA
2. BETACAP-TR- SUN
3. INDERAL- ABBOTT
4. PROVANOL- INTAS PHARMA
Available dosage forms1. TABLETS
2. CAPSULES
3. INJECTION

7-month suspension for pharmacist whose dispensing error led to death |  Chemist+Druggist
DoseOral dose- initially 40 mg 2 to 3 times a day. Maintenance dose 80 to 160 mg daily.
Contraindications 1. Asthma
2. Uncontrolled heart failure
3. Prinzmetal’s angina
4. Marked bradycardia
5. Hypotension
6. Sick sinus syndrome
7. Second- or third-degree AV block
8. Cardiogenic shock
9. Metabolic acidosis
10. Severe peripheral arterial disease
11. Pheochromocytoma
Precautions 1. Avoid abrupt withdrawal especially in ischaemic heart disease
2. First-degree AV block
3. Portal hypertension
4. Diabetes
5. History of obstructive airways disease
6. Myasthenia gravis
7. Symptoms of hypoglycaemia and thyrotoxicosis may be masked
8. History of hypersensitivity-
may increase sensitivity to allergens and result in more serious hypersensitivity response
9. Also may reduce response to
adrenaline
Adverse Effects 1. Gastrointestinal disturbances
2. Bradycardia
3. Heart failure
4. Hypotension
5. Conduction disorders
6. Peripheral vasoconstriction
7. Bronchospasm
8. Dyspnoea
9. Headache
10. Fatigue
11. Sleep disturbances
12. Paraesthesia
13. Dizziness
14. Vertigo
15. Psychosis
16. sexual dysfunction
17. Purpura
Pregnancy Category C

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