amlodipine
Brand: Norvasc
Prototype Drug
Drug Class: calcium channel blocker
Drug Family: antihypertensive
Subclass: dihydropyridine CCB (long-acting)
Organ Systems: cardiovascular
Mechanism of Action
Blocks L-type calcium channels in vascular smooth muscle causing vasodilation; high vascular selectivity with minimal cardiac effect at therapeutic doses.
L-type voltage-gated calcium channel (vascular smooth muscle)
Indications
- hypertension
- chronic stable angina
- vasospastic (Prinzmetal) angina
- coronary artery disease
Contraindications
- cardiogenic shock
- severe aortic stenosis (relative)
Adverse Effects
Common
- peripheral edema (dose-dependent)
- flushing
- headache
- dizziness
Serious
- hypotension
- reflex tachycardia (mild)
- gingival hyperplasia (rare)
Pharmacokinetics (ADME)
| Absorption | 64-90% oral bioavailability; not affected by food |
| Distribution | high protein binding; large Vd |
| Metabolism | hepatic CYP3A4 (to inactive metabolites) |
| Excretion | renal 60% |
| Half-life | 30-50 hours |
| Onset | hours |
| Peak | 6-12 hours |
| Duration | 24 hours |
| Protein Binding | 93-98% |
| Vd | 21 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP3A4 inhibitors (clarithromycin, grapefruit) | increased amlodipine AUC | moderate |
| simvastatin | amlodipine inhibits CYP3A4, increasing simvastatin risk | moderate |
| cyclosporine | amlodipine increases cyclosporine levels | moderate |
Nursing Considerations
- Peripheral edema most common complaint — elevate legs, low-sodium diet
- Do not abruptly discontinue in angina
- Long half-life allows once-daily dosing and smooth 24-hour coverage
- ASCOT-BPLA: amlodipine-based regimen superior to atenolol-based for CV events
Clinical Pearls
- ASCOT trial: superior CV outcomes vs atenolol-based regimen in hypertension
- Longest half-life CCB — forgiveness for missed doses
- Peripheral edema from precapillary vasodilation — managed with ACE inhibitor (venoconstriction)
- Safe in HF unlike non-dihydropyridines
Safety Profile
Pregnancy use-with-caution
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.