Pharmacopeia

Canonical comparison

Master Compare

Compare candidate-facing canonical Pharmacopeia fields side by side. Isolated AI-draft proposals are never included.

2selected
Comparing 2 of 2 drugs
× ×
Change selection
2 drug columns · use arrows or scrollbar
Field METOPROLOL
Cardiovascular · Cardiovascular · Level 3
VERAPAMIL
Cardiovascular · Cardiovascular · Level 3
Mechanism of action

Beta blockage leads to ↓Gs activity in receptor associated organs and
associated ↓in adenylyl cyclase and intracellular Ca2+.


Cardiovascular · Cardiovascular

Beta blockage leads to ↓Gs activity in receptor associated organs and
associated ↓ in adenylyl cyclase and intracellular Ca2+.

Binds to V binding site of L-type channel.
Levoisomer: main effects (arterial vasodilation). Slows conduction through the AV and SA node to a greater extent than other CCBs.
Dextro: Only acts on fast sodium channels, accounting for local anesthetic effects (1.6x potent as procaine)


Cardiovascular · Cardiovascular

Binds to V binding site of L-type channel.
Levoisomer: main effects (arterial vasodilation). Slows conduction through the AV and SA node to a greater extent than other CCBs.
Dextro: Only acts on fast sodium channels, accounting for local anesthetic effects (1.6x potent as procaine)

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

CVS: slow conduction of AP at SA and AV node, negatively inotropic, peripheral vasodilation (↓SVR), arrhythmia (heart block, VF in WPW). CNS: ↑CBF, may potentiate effects of depol/NDMBs. GIT - Constipn/Nausea


Cardiovascular · Cardiovascular

CVS: slow conduction of AP at SA and AV node, negatively inotropic, peripheral vasodilation (↓ SVR), arrhythmia (heart block, VF in WPW). CNS: ↑ CBF, may potentiate effects of depol/NDMBs. GIT - Constipn/Nausea

Absorption

bioavailabilty Absoption is rapid and complete, however there is extensive first pass metabolism bioavailability = 50%


Cardiovascular · Cardiovascular

bioavailabilty Absoption is rapid and complete, however there is extensive fi¬rst pass metabolism bioavailability = 50%

Completely absorbed orally. Oral bioavailability 10-22% because of significant first-pass metabolism.


Cardiovascular · Cardiovascular

PO/IV.
BA 20-25% Well absorbed with high fi¬rst pass metabolism
on/ dur 1-2 hrs / 6-8 hrs (PO)


Cardiovascular · Cardiovascular

PO/IV.
BA 20-25% Well absorbed with high fi¬rst pass metabolism
on/ dur 1-2 hrs / 6-8 hrs (PO)


Cardiovascular · Cardiovascular

PO/IV.
BA 20-25% Well absorbed with high fi¬rst pass metabolism

Distribution

lipid solubility is high so it crosses the BBB

—
Protein binding

10-20% to albumin

~90%

Volume of distribution

5.5 L/Kg

3.89 L/kg

Metabolism

hepatic or renal Extensively hepatic via CYP2D6

Hepatic via multiple CYP isoenzymes, one active metabolite with 20% activity

Excretion

urine 5-10% unchanged

Urine (70% metab, 3% to 4% unchanged); feces (16%)

Half-life

3-8hours

3-7 hours

Adverse Effects Toxicity

- Withdrawal

- Care with: Opioids, Halo, OAD, CCB

- Use with Ca Channel blockers may result in complete heart block

Dizziness, nausea, flushing, postural hypotension.
in patients without CCF: ↑LV fn by improving ischemia. In pts with CCF: ↓contractility and LV fn. Should be avoided in pts with WPW- cause VT/VF.
Inhibits CYP3A4.


Cardiovascular · Cardiovascular

Dizziness, nausea, flushing, postural hypotension.
in patients without CCF: ↑LV fn by improving ischemia. In pts with CCF: ↓contractility and LV fn. Should be avoided in pts with WPW- cause VT/VF.
Inhibits CYP3A4.


Cardiovascular · Cardiovascular

Dizziness, nausea, flushing, postural hypotension.
in patients without CCF: ↑ LV fn by improving ischemia. In pts with CCF: ↓ contractility and LV fn. Should be avoided in pts with WPW- cause VT/VF.
Inhibits CYP3A4.

Chemical Pharmaceutics —

Racemic mixture.

Class Group

Selective beta1-adrenoceptor antagonist; Vaughan Williams class II antiarrhythmic.


Cardiovascular · Cardiovascular

Beta Blocker


Cardiovascular · Cardiovascular

Antiarrhythmic –
Vaughan Williams Class II
Beta blocker

Non-dihydropyridine calcium-channel blocker; Vaughan Williams class IV antiarrhythmic.


Cardiovascular · Cardiovascular

(CCB) Ca channel blocker – Class I

Antiarrhythmic –
Vaughan Williams Class IV


Cardiovascular · Cardiovascular

(CCB) Ca channel blocker – Class I

Antiarrhythmic –
Vaughan Williams Class IV


Cardiovascular · Cardiovascular

Antiarrhythmic –
Vaughan Williams Class IV

(CCB) Ca channel blocker – Class I

Indications Uses

- Early use of metoprolol in haemodynamically stable myocardial infarction reduces infarct size and incidence of VF.
- rate control in atrial fibrillation
- hypertension


Cardiovascular · Cardiovascular

- Early use of metoprolol in haemodynamically stable myocardial infarction reduces infarct size and incidence of VF.
- rate control in atrial -fibrillation
- hypertension

HTN
Angina
Paroxysmal SVT and AFib/Aflutter


Cardiovascular · Cardiovascular

HTN
Angina
Paroxysmal SVT and AFib/Aflutter

Introduction

relatively selective beta blocker with no intrinsic sympathomimetic activity.

Phenylalkylamine
(Non-dihydropyridine calcium channel blocker)

Synthetic papaverine derivative


Cardiovascular · Cardiovascular

Phenylalkylamine
(Non-dihydropyridine calcium channel blocker)

Synthetic papaverine derivative

Legacy Cicm Level

Level 3

Level 3

Onset Peak Duration —

on/ dur 1-2 hrs / 6-8 hrs (PO)

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

Available in oral immediate/modified-release formulations and as an IV preparation; exact strengths vary by product.


Cardiovascular · Cardiovascular

Racemic mixture. PO: 40-240mg. Also in combo w Trandolapril. IV Clear solution at 2.5mg/ml


Cardiovascular · Cardiovascular

PO: 40-240mg. Also in combo w Trandolapril. IV Clear solution at 2.5mg/ml

Route And Dose

PO or IV
dose Orally in 12.5mg increments, IV in 1-2mg boluses

40mgPO or 5-10mg IV.