Pharmacopeia
METOPROLOL
Core pharmacology
- Legacy Cicm Level
Level 3
- Introduction
relatively selective beta blocker with no intrinsic sympathomimetic activity.
- Presentation
available in oral form as an immediate release or sustained release in
increments of 25mg.
It is also available as an IV formulation usually 1mg/ml- Physiological effects
It produces
decreases in heart rate and cardiac output and myocardial oxygen consumption.Whilst it does have some β 2 action it has little or no effect on these receptors
at doses less than 100mg- Adverse Effects Toxicity
- Withdrawal
- Care with: Opioids, Halo, OAD, CCB
- Use with Ca Channel blockers may result in complete heart block
- Distribution
lipid solubility is high so it crosses the BBB
- Protein binding
10-20% to albumin
- Volume of distribution
5.5 L/Kg
- Metabolism
hepatic or renal Extensively hepatic via CYP2D6
- Excretion
urine 5-10% unchanged
- Half-life
3-8hours
- Route And Dose
PO or IV
dose Orally in 12.5mg increments, IV in 1-2mg boluses
Cardiovascular · Cardiovascular
- Class Group
Beta Blocker
- Indications Uses
- Early use of metoprolol in haemodynamically stable myocardial infarction reduces infarct size and incidence of VF.
- rate control in atrial fibrillation
- hypertension- Mechanism of action
Beta blockage leads to ↓Gs activity in receptor associated organs and
associated ↓in adenylyl cyclase and intracellular Ca2+.- Absorption
bioavailabilty Absoption is rapid and complete, however there is extensive first pass metabolism bioavailability = 50%
- Class Group
Antiarrhythmic –
Vaughan Williams Class II
Beta blocker- Indications Uses
- Early use of metoprolol in haemodynamically stable myocardial infarction reduces infarct size and incidence of VF.
- rate control in atrial -fibrillation
- hypertension- Mechanism of action
Beta blockage leads to ↓Gs activity in receptor associated organs and
associated ↓ in adenylyl cyclase and intracellular Ca2+.- Absorption
bioavailabilty Absoption is rapid and complete, however there is extensive fi¬rst pass metabolism bioavailability = 50%