Trade Names:Betoptic- Solution 5.6 mg (equivalent to 5 mg base) per mL (0.5%)
Trade Names:Betoptic-S- Suspension 2.8 mg (equivalent to 2.5 mg base) per mL (0.25%)
Trade Names:Kerlone- Tablets 10 mg- Tablets 20 mg
Blocks beta receptors, primarily affecting cardiovascular system (decreases heart rate, cardiac contractility, and BP) and lungs (promotes bronchospasm). Ophthalmic use reduces IOP, probably by reducing aqueous production.
Bioavailability is about 89%, C max is about 21.6% ng/mL (10 mg dose), and T max is about 3 h.
Approximately 50% protein bound.
Metabolized in liver to inactive metabolites.
The t ½ is 14 to 22 h. More than 80% is recovered in urine as betaxolol and metabolites; about 15% excreted as unchanged drug.
Within 30 min.
7 to 14 days.Ophthalmic
In moderate to severe impairment, Cl is decreased significantly. In those undergoing dialysis, the t ½ and AUC are approximately doubled. Dosage adjustment required for those with severe renal function impairment and those undergoing dialysis.Hepatic Function Impairment
The t ½ may be prolonged but Cl is unchanged. Dosage adjustments not needed.Elderly
Elimination may be decreased. Dosage adjustment required.
Lowering IOP; ocular hypertension; chronic open-angle glaucoma.
Hypersensitivity to beta-blockers; sinus bradycardia; greater than first-degree heart block; CHF unless secondary to tachyarrhythmia treatable with beta-blockers; overt cardiac failure; cardiogenic shock.
PO 10 to 20 mg/day.Elderly
PO Reduce initial dose to 5 mg/day.GlaucomaAdults
Ophthalmic 1 to 2 drops twice daily in affected eye(s). Consider concomitant therapy if IOP is not at satisfactory level.
Store oral form in cool location. Store ophthalmic form at room temperature. Do not freeze.
May enhance or reverse antihypertensive effect; potentially life-threatening situations may occur, especially on withdrawal.NSAIDs
Some agents may impair antihypertensive effect.Prazosin
May increase postural hypotension.Verapamil
May increase effects of both drugs.
None well documented.
Hypotension; bradycardia; CHF; cold extremities; second- or third-degree heart block; arrhythmias; syncope.
Insomnia; fatigue; dizziness; depression; lethargy; drowsiness; forgetfulness; headache.
Rash; hives; alopecia.
Dry eyes; blurred vision; tinnitus; slurred speech; dry mouth; sore throat. Ophthalmic use may cause eye discomfort or stinging; tearing; keratitis; blepharoptosis; visual disturbances; diplopia; ptosis.
Nausea; vomiting; diarrhea; constipation.
Impotence; painful, difficult, or frequent urination.
Agranulocytosis; thrombocytopenic purpura.
Acidosis; diabetes; hypercholesterolemia; hyperlipidemia; increased LDH; hypokalemia.
Bronchospasm; dyspnea; wheezing.
Weight changes; fever; facial swelling; muscle weakness. Ophthalmic betaxolol may produce the same adverse drug reactions seen with systemic use; antinuclear antibodies may develop.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
Dosage reduction may be necessary.
Use with caution.
Use with caution.
Deaths have occurred with anaphylactic reactions to beta-blockers; aggressive therapy may be required.
To effectively reduce elevated IOP in angle-closure glaucoma, use with miotic agent.
Gradually withdraw over about 2 wk. Carefully observe patients and allow minimal physical activity.
Cautiously administer in patients whose CHF is controlled by digitalis and diuretics.
May mask symptoms of hypoglycemia (eg, tachycardia, BP changes). May potentiate insulin-induced hypoglycemia.
In general, beta-blockers are not given to patients with bronchospastic diseases.
May precipitate or aggravate symptoms of arterial insufficiency.
Ophthalmic betaxolol may produce same adverse reactions seen with systemic use because of absorption.
May mask clinical signs (eg, tachycardia) of developing or continuing hyperthyroidism. Abrupt withdrawal may exacerbate symptoms of hyperthyroidism, including thyroid storm.
Bradycardia, CHF, hypotension, bronchospasm, hypoglycemia.
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