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

  1. Peripheral edema most common complaint — elevate legs, low-sodium diet
  2. Do not abruptly discontinue in angina
  3. Long half-life allows once-daily dosing and smooth 24-hour coverage
  4. 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

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