Pharmacopeia

CWP-0164

METOPROLOL

Cardiovascular · Cardiovascular · Level 3

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%