Pharm

Acebutolol

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Acebutolol, Sectral

  • See Also
  1. Beta Blocker
  • Indications
  1. Hypertension
  • Mechanism
  1. See Beta Adrenergic ReceptorAntagonist
  2. Acebutolol is unique in that it also has weak intrinsic Sympathomimetic activity (partial beta Agonist)
    1. Similar intrinsic Sympathomimetic activity (ISA) is seen with Pindolol
    2. Other selective Beta Blockers without ISA activity are preferred in Coronary Artery Disease
  3. Like other Selective Beta Antagonists, it primarily inhibits B1 activity by blocking B1 Receptors
    1. Reduces Myocardial Contractility, Blood Pressure, myocardial oxygen demand
    2. Also Antiarrhythmic and slows ventricular response in Atrial Fibrillation
  4. Contrast with non-selective Beta Blockers (e.g. Propranolol)
    1. Non-selective Beta Blockers also act at B2 Receptors (bronchoconstriction) and B3 Receptors (block lipolysis)
  • Adverse Effects
  1. See Beta Blocker
  • Drug Interactions
  1. See Beta Blocker
  • Dosing
  1. Start: 400 mg orally daily or divided 200 mg orally twice daily
    1. Better efficacy when divided twice daily
  2. Target: 400 to 800 mg/day
  3. Maximum: 1200 mg/day
  • Safety
  1. Pregnancy Category B
  2. Avoid in Lactation
  • Metabolism
  1. Not lipophilic
  2. Bioavailability 40%
    1. High first pass hepatic metabolism to a renally excreted metabolite
  • Resources
  1. Acebutolol (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=28f8c26c-a1e1-4485-a45f-05c82f7a34b5
  • References
  1. (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
  2. (2020) Med Lett Drugs Ther 62(1598): 73-80
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 66-7
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia