Dosing and uses of Betoptic S, Kerlone (betaxolol)
Adult dosage forms and strengths
tablet
- 10mg
- 20mg
Hypertension
5-20 mg PO qDay
Renal Impairment
Severe impairment: 5 mg PO qDay; may increase every 2 weeks to maximum 20 mg/day
Other Information
Less effective than thiazide diuretics in black and geriatric patients
Shown to decrease mortality in hypertension and post-myocardial infarction
Pediatric dosage forms and strengths
Hypertension
Safety and efficacy not established
Geriatric dosage forms and strengths
Hypertension: 5 mg PO qDay
Consideration should be given to reducing the starting dose to 5 mg in elderly patients
Elderly are especially prone to beta-blocker–induced bradycardia, which appears to be dose related and sometimes responds to reductions in dose
Betoptic S, Kerlone (betaxolol) adverse (side) effects
2-10%
Fatigue (2-10%)
Bradycardia (6-8%)
Chest pain (2-7%)
Dyspepsia (2-5%)
Lethargy (3%)
Cold extremeties (2%)
Diarrhea (2%)
Dyspnea (2%)
Edema (2%)
Palpitation (2%)
Pharyngitis (2%)
<2% (selected)
Angina
Arrhythmia
Flushing
Depression
Fever
Hallucinations
Malaise
Neuropathy
Rash
Diabetes
Hyperglycemia
Anemia
Hypercholesterolemia
Hyperlipidemia
Leukocytosis
cataracts
Constipation
Dysphagia
Libido decreased
Proteinuria
Bronchospams
Cough
Frequency not defined
Decreased exercise tolerance, Raynaud's phenomenon
May increase triglyceride levels and insulin resistance, and decrease HDL levels
Warnings
Contraindications
Sinus bradycardia, 2°/3° heart block, cardiogenic shock, overt cardiac failure, hypersensitivity, sick sinus syndrome without permanent pacemaker
Cautions
Bronchospastic disease, cerebrovascular insufficiency, CHF, cardiomegaly, DM, hyperthyroidism/thyrotoxicosis, liver disease, renal impairment, peripheral vascular disease (potential risk of reduced placental perfusion, fetal bradycardia, hypoglycemia), use in pheochromocytoma, IDDm
Surgery/Anesthesia: Chronically administered beta-blockers should not be routinely withdrawn prior to major surgery; however, impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures
Pregnancy and lactation
Pregnancy category: C
Lactation: excreted in milk; use caution
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 Betoptic S, Kerlone (betaxolol)
Mechanism of action
Beta adrenergic receptor blocker; cardioselective for Beta-1 receptor at low doses
Pharmacokinetics
Half-Life: 14-22 hr
Bioavailability: 89%
Protein Bound: 50%
Excretion: Urine
Onset of action: 1-1.5hr
Peak Plasma
- Time: 3 hr
- Concentration: 21.6 ng/mL
