Pharmacopeia
VERAPAMIL
Core pharmacology
- Legacy Cicm Level
Level 3
- Introduction
Phenylalkylamine
(Non-dihydropyridine calcium channel blocker)Synthetic papaverine derivative
- Indications Uses
HTN
Angina
Paroxysmal SVT and AFib/Aflutter- Mechanism of action
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)- Protein binding
~90%
- Volume of distribution
3.89 L/kg
- Metabolism
Hepatic via multiple CYP isoenzymes, one active metabolite with 20% activity
- Excretion
Urine (70% metab, 3% to 4% unchanged); feces (16%)
- Half-life
3-7 hours
- Route And Dose
40mgPO or 5-10mg IV.
- Chemical Pharmaceutics
Racemic mixture.
- Onset Peak Duration
on/ dur 1-2 hrs / 6-8 hrs (PO)
Cardiovascular · Cardiovascular
- Class Group
(CCB) Ca channel blocker – Class I
Antiarrhythmic –
Vaughan Williams Class IV- Presentation
Racemic mixture. PO: 40-240mg. Also in combo w Trandolapril. IV Clear solution at 2.5mg/ml
- Physiological effects
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
- Adverse Effects Toxicity
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.- Absorption
PO/IV.
BA 20-25% Well absorbed with high fi¬rst pass metabolism
on/ dur 1-2 hrs / 6-8 hrs (PO)- Class Group
(CCB) Ca channel blocker – Class I
Antiarrhythmic –
Vaughan Williams Class IV- Introduction
Phenylalkylamine
(Non-dihydropyridine calcium channel blocker)Synthetic papaverine derivative
- Indications Uses
HTN
Angina
Paroxysmal SVT and AFib/Aflutter- Mechanism of action
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)- Adverse Effects Toxicity
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.- Absorption
PO/IV.
BA 20-25% Well absorbed with high fi¬rst pass metabolism
on/ dur 1-2 hrs / 6-8 hrs (PO)- Class Group
Antiarrhythmic –
Vaughan Williams Class IV(CCB) Ca channel blocker – Class I
- Presentation
PO: 40-240mg. Also in combo w Trandolapril. IV Clear solution at 2.5mg/ml
- Physiological effects
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
- Adverse Effects Toxicity
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.- Absorption
PO/IV.
BA 20-25% Well absorbed with high fi¬rst pass metabolism