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Carvedilol

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Carvedilol, Coreg

  • See Also
  1. Beta Blocker
  2. Beta Blocker Overdose
  3. Labetalol
  4. Alpha Adrenergic Antagonist
  • Indication
  1. Stable Congestive Heart Failure (Compensated)
  2. Hypertension
  • Contraindications
  1. Asthma
  2. Bradycardia
  • Mechanism
  1. Combination of classes ("Third generation Beta Blocker", similar to Labetalol)
    1. Lowers Blood Pressure without reflex Tachycardia
    2. Nonselective Beta Blocker
      1. Binds vascular (and Bronchial) Smooth Muscle beta receptors
      2. Decreases Heart Rate, Cardiac Output and Blood Pressure
      3. Blunts sympathetic drive while still preserving cardiac contractility
    3. Selective Alpha-1 Adrenergic Antagonist (weak compared with beta activity)
      1. Competitively binds vascular Smooth Muscle alpha-1 Adrenergic Receptors
      2. Blocks peripheral blood vessel Vasoconstriction
  2. Other effects
    1. Does not affect Blood Glucose
  • Dosing
  • Carvedilol Regular Release (Coreg)
  1. Stable Congestive Heart Failure
    1. Start: 3.125 mg orally twice daily with food
    2. Titrate up by doubling dose every 2 weeks
    3. Maximum dose
      1. Weight <85 kg: 25 mg bid
      2. Weight >85 kg: 50 mg bid
  2. Hypertension
    1. Start: 6.25 orally twice daily with food
    2. Double dose as needed every 7-14 days to maximum of 25 mg orally twice daily
  3. Conversion from prior Beta Blocker
    1. No overlap from Metoprolol 50 mg or Atenolol 50 mg
      1. Start Carvedilol 6.25 mg bid and increase as above
    2. Overlap from Atenolol 50-150 or Metoprolol 100-200
      1. Add Carvedilol 3.125 mg bid for 2 weeks
      2. Raise Carvedilol and lower other Beta Blocker
        1. Double Carvedilol every two weeks
        2. Reduce Atenolol or Metoprolol by 50 mg q2 weeks
        3. When to stop other Beta Blocker
          1. After 2 weeks on Metoprolol 50 mg or
          2. After 2 weeks on Atenolol 25 mg
            1. Follows prior 2 weeks on Atenolol 50 mg
      3. Reference
        1. Abraham (2003) Congest Heart Fail 9:251-8 [PubMed]
  • Dosing
  • Carvedilol Sustained Release (Coreg CR)
  1. Stable Congestive Heart Failure
    1. Start: 10 mg orally daily
    2. Titrate up by doubling dose every 2 weeks as needed
    3. Maximum dose: 80 mg/day
  2. Hypertension
    1. Start: 20 mg orally daily
    2. Titrate up by doubling dose every 2 weeks as needed
    3. Maximum dose: 80 mg/day
  • Efficacy
  1. Carvedilol used in severe Congestive Heart Failure
    1. Findings
      1. Mean Ejection Fraction: 23%
      2. Studied over 6 months
      3. Overall mortality reduced (3.2% vs 7.8%)
    2. Reference
      1. Packer (1996) N Engl J Med 334:1349-55 [PubMed]
  2. Utah Study of Carvedilol in CHF
    1. Ejection Fraction improved 20% to 33%
  • Adverse Effects
  1. May worsen acute exacerbations of Congestive Heart Failure
  2. Fatigue
  3. Erectile Dysfunction
  4. Orthostatic Hypotension
  • Drug Interactions
  1. Systemic Beta Agonists
    1. Carvedilol blocks bronchodilation
  • References
  1. Olson (2020) Clinical Pharmacology, MedMaster, Miami, p. 66
  2. Hamilton (2020) Tarascon Pocket Pharmacopeia, Jones and Bartlett, accessed on IOS, 4/9/2021