Dosing and uses of Sectral (acebutolol)
Adult dosage forms and strengths
capsule
- 200mg
- 400mg
Hypertension
400-1200 mg/day divided PO q12hr; not to exceed 1200 mg/day
Ventricular Arrhythmias
400-1200 mg/day divided PO q12hr; not to exceed 1200 mg/day
Angina
400-1200 mg/day divided PO q12hr; not to exceed 1200 mg/day
Renal Impairment
CrCl 25-49 mL/min: Reduce dose by 50%
CrCl < 25 mL/min: Reduce dose by 75%
Hepatic Impairment
Dose adjustment not necessary
Other Indications & Uses
Off-label: ventricular tachycardia, angina, essential tremor
Also used to control ventricular premature beats
Pediatric dosage forms and strengths
Safety and efficacy not established
Geriatric dosage forms and strengths
Hypertension
Initial dose: 200-400 mg PO daily; not to exceed 800 mg/day
Ventricular Arrhythmias
Initial dose: 200-400 mg PO daily; not to exceed 800 mg/day
Angina
Initial dose: 200-400 mg PO daily; not to exceed 800 mg/day
Sectral (acebutolol) adverse (side) effects
>10%
Fatigue (11%)
1-10%
Dizziness (6%)
Headache (6%)
Constipation (4%)
Diarrhea (4%)
Dyspnea (4%)
Dyspepsia (4%)
Nausea (4%)
Flatulence (3%)
Insomnia (3%)
Abdominal pain (2%)
Bradycardia (2%)
Chest pain (2%)
Dysuria (2%)
Edema (2%)
Heart failure (2%)
Hypotension (2%)
Impotence (2%)
Myalgia (2%)
Pharyngitis (2%)
Pruritus (2%)
Rhinitis (2%)
Vomiting (2%)
Wheezing (2%)
<1%
Hepatotoxicity
SLe
Frequency not defined
Bronchospasm, depression, decreased exercise tolerance, Raynaud's phenomenon
May increase triglyceride levels and insulin resistance, and decrease HDL levels
Warnings
Contraindications
Hypersensitivity
Asthma/COPD, severe bradycardia, 2°/3° heart block, cardiogenic shock, overt heart failure, sinus bradycardia, sick sinus syndrome without permanent pacemaker
Avoid during breastfeeding
Cautions
Anesthesia/surgery (myocardial depression); chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures
Bronchospastic disease, cerebrovascular insufficiency, DM, hyperthyroidism/thyrotoxicosis, liver disease, renal impairment, peripheral vascular disease, compromised left ventricular function, elderly, use in pheochromocytoma, IDDm
Avoid abrupt withdrawal; sudden discontinuation can exacerbate angina and lead to myocardial infarction
May increase risk of stroke after surgery
Pregnancy and lactation
Pregnancy category: B; D in 2nd and 3rd trimesters (expert analysis). Neonates of mothers who have received acebutolol during pregnancy have reduced birth weight, decreased blood pressure, and decreased heart rate.
Lactation: excreted into milk/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Sectral (acebutolol)
Mechanism of action
Cardioselective for beta-1 at low doses; has intrinsic sympathomimetic activity, ie, can lower BP with less decrease in Hr
Class 2 antiarrhythmic
Pharmacokinetics
Peak Plasma Time: 2-3 hr
Toxic range: acetabutalol >15-20 mcg/mL, & diacetolol (the active metabolite) < 90-150 mcg/mL
Onset: 1.5-3 hr (initial response); 3-8 hr (peak response)
Duration: 12-24 hr
Bioavailability: 40%
Absorption: 40% (oral)
Protein Bound: 10-26%
Vd: 1.2 L/kg
Metabolism: metabolized in the liver to active met, diacetoloL
Metabolites: diacetolol (active), free amine of acebutolol (inactive)
Excretion: principally in feces 56%, urine 30-40%, bile 3-8%
Dialyzable: Yes (HD)
Less effective than thiazide diuretics in black and geriatric patients Shown to decrease mortality in hypertension and post-myocardial infarction
Half-Life
- Parent drug (acebutalol): 3-4 hr
- Active metabolite (diacetolol): 8-13 hr
