Pharm

Amlodipine

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Amlodipine, Norvasc, Katerzia

  • See Also
  1. Dihydropyridine Calcium Channel Blocker
  2. Calcium Channel Blocker
  3. Calcium Channel Blocker Overdose
  4. Non-Dihydropyridine Calcium Channel Blocker
  5. Nifedipine
  6. Diltiazem
  7. Verapamil
  8. Mibefradil
  9. Nicardipine
  10. Clevidipine
  11. Nimodipine (Nymalize)
  • Mechanism
  1. See Dihydropyridine Calcium Channel Blocker
  2. Dihydropyridines are primarily active at vascular Smooth Muscle
    1. Contrast with Non-Dihydropyridines which are also active at cardiac Smooth Muscle
  3. Amlodipine is a preferred first line oral antihypertensive Calcium Channel Blocker
    1. Long acting and less reflex Tachycardia than other Dihydropyridines, with improved cardiovascular outcomes
    2. Does not exacerbate Left Ventricular Dysfunction
  • Contraindications
  1. Consider avoiding in Diabetes Mellitus (relative contraindication)
    1. May increase Proteinuria
  2. NOT contraindicated in combination with Beta Blockers
    1. Contrast with Non-Dihydropyridine Calcium Channel Blockers (Diltiazem, Verapamil) which slow AV nodal conduction
  3. Relative contraindications (Exercise caution)
    1. Aortic Stenosis
    2. Severe Coronary Artery Disease
  • Drug Interactions
  1. See Dihydropyridine Calcium Channel Blocker
  2. Clarithromycin
    1. Increases Calcium Channel Blocker levels via CYP3A4 inhibition especially with Dihydropyridines and over age 65 years
      1. Provokes Hypotension and Bradycardia
      2. Risk of Acute Kidney Injury (often requiring hospitalization)
    2. References
      1. Gandhi (2013) JAMA 310(23):2544-53 [PubMed]
  3. Simvastatin
    1. Limit Simvastatin to a maximum of 20 mg daily
  4. May increase other drug levels
    1. Cyclosporine
    2. Tacrolimus
  5. Potentiates other medications
    1. Digoxin
    2. Beta Blockers
  1. Typical dose: 5 mg orally daily
    1. Start at 2.5 mg daily in elderly, frail patients or hepatic insufficiency
  2. Maximum: 10 mg orally daily (little benefit over 5 mg, but increased edema)
  1. Available as an oral suspension 1 mg/ml (Katerzia)
  2. Age under 6 years (NOT FDA approved)
    1. Start 0.1 to 0.2 mg/kg/day orally daily
    2. Maximum 0.3 mg/kg/day up to 10 mg orally daily
  3. Age 6 to 17 years old
    1. Start 2.5 mg orally daily
    2. May advance to 5 mg orally daily
  • Medications
  • Combinations
  1. Amlodipine/Olmesartan (Azor)
  2. Amlodipine/Atorvastatin (Caduet)
  3. Amlodipine/Valsartan (Exforge)
  4. Amlodipine/Valsartan/Hydrochlorothiazide (Exforge HCT)
  5. Amlodipine/Benazepril (Lotrel)
  • Adverse Effects
  1. See Calcium Channel Blocker
  2. Peripheral Edema
    1. Occurs more commonly in women
    2. Occurs more commonly on Norvasc doses >5 mg
    3. Adding ACE Inhibitor to regimen decreases edema
    4. Avoid Diuretics to reduce Dihydropyridine -induced edema
      1. Dihydropyridine-induced edema mechanism is vasodilation fluid leak into interstitium, NOT Sodium and water retention
  • Pharmacokinetics
  1. Slowest onset of action, but longest half life of the Dihydropyridine Calcium Channel Blockers
  • Safety
  1. Pregnancy Category C
  2. Avoid in Lactation
  • Resources
  1. Amlodipine Besylate Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3d14c6b5-a70a-477f-b332-fa5b93a6296f
  • References
  1. (2022) Presc Lett 29(11): 64-5
  2. (2022) Presc Lett, Resource #381108, Comparison of Calcium Channel Blockers
  3. (2020) Med Lett Drugs Ther 62(1598): 73-80
  4. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 70-1
  5. Hamilton (2020) Tarascon Pocket Pharmacopoeia