PROPRANOLOL
“INDERAL”
1) Action
• Non
selective Beta Adrenergic Blocker [Class II antiarrhythmic]
2) Mechanism
• Antagonises catecholamines at both b1 & b2 adrenoreceptors
• Ameliorates hypertension by: reduction of CO, reduction of SVR, inhibition of the renin production by catecholamines (mediated by b1 receptors)
3) Indications
• Angina pectoris (decrease cardiac work & reduce oxygen demand)
• Myocardial infarction
• Hypertension
• Arrhythmias [tachycardias 2° anxiety, adrenaline, digitalis]
• Migraines
• Phaeochromocytoma
• Hypertrophic
subaortic stenosis (increase SV by reducing
HR)
• Dissecting aortic aneurysms (reduce rate of systolic pressure development)
4) Effects on organs—side effects
• b2 blockade in lungs —> increased airway resistance
• Inhibit sympathetic stimulation of lipolysis
• Reduce insulin & glucagon secretion
5) Toxic effects/ precautions with administration
• Caution when used with calcium channel blockers
• Caution when given to diabetics
• May reduce sympathetic response during myocardial depressive drugs given during anaesthesia
6)
Contraindications
• CCF: patients depends on sympathetic drive to maintain CO
• Sinus bradycardia; heart blocks
• Asthma; bronchospasm
• Right ventricular hypertrophy 2° pulmonary hypertension
7) Reversal, antagonism or antidote
• Hypotension: Adrenaline, Noradrenaline
• Bradycardia: Atropine, glucagon
• Cardiac failure: digoxin
• Bronchospasm: isoprenaline, aminophylline
8) Loading dose, maintenance dose, frequency &
method of administration
• Oral
• Injection: 1mg/ml [1ml]
9) Drug’s metabolism—Drug’s excretion—Half life (pharmacokinetics)
• Elimination half life: 4 hours
• % plasma protein bound: 93
• Metabolised in liver