METOPROLOL
“LOPRESOR”
1) Action
• Selective
Beta Adrenergic Blocker [Class II antiarrhythmic]
2) Mechanism
• Antagonises catecholamines at b1 adrenoreceptors [to a much lesser degree than propranolol it blocks 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 [may convert AF & Af to SR, reduce PVCs]
• Migraines
• May be used in hypertensive patients suffering from asthma or diabetes
5) Toxic effects/ precautions with administration
• Caution when used with calcium channel blockers
• Caution when given to diabetics
• Caution when given to asthmatics
• 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, IV
• 1mg/1ml ampoule
9) Drug’s metabolism—Drug’s excretion—Half life (pharmacokinetics)
• Elimination half life: 3-4 hours
• Metabolised in liver