acebutolol (Sectral, Monitran, Rhotral)
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Introduction
Tradename: Sectral. A selective beta-1 antagonist.
Indications
- hypertension
- ventricular arrhythmias
- angina pectoris (not FDA approved use)
- secondary prevention in patients with cardiovascular disease[3]
- anxiety[3]
- thyrotoxicosis[3]
- mitral valve prolapse
Contraindications
- uncompensated heart failure
- cardiogenic shock
- bradycardia, heart block
- 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.
Dosage adjustment in renal failure
- Reduce dose to 50% for creatinine clearance 25-49*
- Reduce dose to 25% for creatinine clearance <25*
* mL/min/1.73 m2
Pharmacokinetics
- 90% absorption, extensive 1st pass metabolism
- bioavailability increased in the elderly (2-fold)
- substrate of CYP1A2 & CYP2E1
- protein binding 25%
- peak levels 2-4 hours after oral dose
- 1/2life 3-4 hours
- excreted by the bile & intestinal wall (50-60%)
- renal excretion (30-40%)
elimination via liver
elimination via kidney
Adverse effects
- cardiovascular:
- bradycardia, torsades de pointes, ventricular arrhythmias, dyspnea, heart block, hypotension, chest pain, edema, heart failure, Raynuad's phenomenon, facial edema
- central nervous system:
- dermatologic: rash, pruritus
- gastrointestinal:
- genitourinary:
- impotence, decreased libido, urinary retention, polyuria
- neuromuscular & skeletal
- ocular: blurred vision, visual disturbance
- other: Raynuad's phenomenon
- drug adverse effects of beta-adrenergic receptor antagonists
- drug adverse effects of beta-1 adrenergic receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
(see beta blockers, general)
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with thyroid hormone
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfinpyrazone
- drug interaction(s) of beta-adrenergic receptor antagonists with salicylate
- drug interaction(s) of beta-adrenergic receptor antagonists with rifampin
- drug interaction(s) of beta-adrenergic receptor antagonists with ampicillin
- drug interaction(s) of beta-adrenergic receptor antagonists with colestipol
- drug interaction(s) of beta-adrenergic receptor antagonists with cholestyramine
- drug interaction(s) of beta-adrenergic receptor antagonists with barbiturates
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium salts
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum carbonate
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum hydroxide
- drug interaction(s) of beta-adrenergic receptor antagonists with prazosin
- drug interaction(s) of beta-adrenergic receptor antagonists with lidocaine
- drug interaction(s) of beta-adrenergic receptor antagonists with ergot alkaloids
- drug interaction(s) of beta-adrenergic receptor antagonists with clonidine
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of beta-adrenergic receptor antagonists with quinidine
- drug interaction(s) of beta-adrenergic receptor antagonists with propafenone
- drug interaction(s) of beta-adrenergic receptor antagonists with phenothiazines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of beta-adrenergic receptor antagonists with loop diuretics
- drug interaction(s) of beta-adrenergic receptor antagonists with hydralazine
- drug interaction(s) of beta-adrenergic receptor antagonists with histamine H2 receptor antagonists
- drug interaction(s) of beta-adrenergic receptor antagonists with haloperidol
- drug interaction(s) of beta-adrenergic receptor antagonists with flecainide
- drug interaction(s) of beta-adrenergic receptor antagonists with oral contraceptives
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of spironolactone with beta blockers
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- selective beta-1 adrenergic receptor antagonist
- intrinsic membrane stabilizing activity
- intrinsic sympathomimetic activity