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acebutolol (Sectral, Monitran, Rhotral)

Tradename: Sectral. A selective beta-1 antagonist. Indications: 1) hypertension 2) ventricular arrhythmias 3) angina pectoris (not FDA approved use) 4) secondary prevention in patients with cardiovascular disease [3] 5) anxiety [3] 6) thyrotoxicosis [3] 7) mitral valve prolapse Contraindications: 1) uncompensated heart failure 2) cardiogenic shock 3) bradycardia, heart block 4) sinus node dysfunction Dosage: Start 400 mg PO QD or 200 mg PO BID, max 1200 mg/day Dose reduction in the elderly, 50% Tabs: 200, 400 mg. Pharmacokinetics: 1) 90% absorption, extensive 1st pass metabolism 2) bioavailability increased in the elderly (2-fold) 3) substrate of CYP1A2 & CYP2E1 4) protein binding 25% 5) peak levels 2-4 hours after oral dose 6) 1/2life 3-4 hours 7) excreted by the bile & intestinal wall (50-60%) 8) renal excretion (30-40%) Dosage adjustment in renal failure: 1) Reduce dose to 50% for creatinine clearance 25-49* 2) Reduce dose to 25% for creatinine clearance <25* * mL/min/1.73 m2 Adverse effects: 1) cardiovascular: - bradycardia, torsades de pointes, ventricular arrhythmias, dyspnea, heart block, hypotension, chest pain, edema, heart failure, Raynuad's phenomenon, facial edema 2) central nervous system: - depression, confusion, dizziness, insomnia, lethargy, headache, nightmares, fatigue 3) dermatologic: rash, pruritus 4) gastrointestinal: - constipation, diarrhea, nausea, xerostomia, gastritis, anorexia 5) genitourinary: - impotence, decreased libido, urinary retention, polyuria 6) neuromuscular & skeletal - arthralgia, muscle cramps 7) ocular: blurred vision, visual disturbance 8) other: Raynuad's phenomenon Drug interactions: (see beta blockers, general) Mechanism of action: 1) selective beta-1 adrenergic receptor antagonist 2) intrinsic membrane stabilizing activity 3) intrinsic sympathomimetic activity

Interactions

drug interactions drug adverse effects (more general classes)

General

amide beta-1 adrenergic receptor antagonist (beta-1 blocker) ether ketone propanolamine

Properties

MISC-INFO: elimination route LIVER KIDNEY pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. Geriatric Dosage Handbook, 6th edition, Selma et al eds,
  2. Lexi-Comp, Cleveland, 2001
  3. Deprecated Reference