Elevated IOP in chronic open-angle glaucoma or ocular hypertension
1 drop in the affected eye(s) BID
IOP starts falling within 30 minutes, peaks at 2 hours, and a single dose lasts 12 hours.
Contraindications
Sinus bradycardia.
Second or third degree atrioventricular block.
Overt cardiac failure.
Cardiogenic shock.
Hypersensitivity to any component.
Available Forms
0.25% suspension (2.5 mg/mL betaxolol base), 10 mL, 15 mL
Mechanism of Action
Cardioselective (beta-1) adrenergic receptor inhibitor without significant membrane-stabilizing or intrinsic sympathomimetic activity; lowers IOP by reducing aqueous production, demonstrated by tonography and aqueous fluorophotometry. Onset within 30 minutes, maximum effect at 2 hours, and a single dose gives a 12-hour IOP reduction, though the response can take a few weeks to stabilize.
Warnings & Precautions
Systemic absorption: Topical dosing produces the same reactions as systemic beta-blockade, including death from bronchospasm in patients with asthma and death from cardiac failure reported with ophthalmic beta-blockers.
Cardiac failure: Minor effect on heart rate and blood pressure in clinical studies, but use caution with a history of cardiac failure or heart block and discontinue at the first signs of failure.
Bronchospasm and pulmonary distress: Asthmatic attacks and pulmonary distress have been reported during betaxolol treatment; rechallenge of some such patients did not adversely affect pulmonary function test results, but adverse pulmonary effects in patients sensitive to beta-adrenergic receptor inhibitors cannot be ruled out. Caution with excessive restriction of pulmonary function.
Diabetes mellitus: Masks the signs and symptoms of acute hypoglycemia; caution in labile diabetes and in patients on insulin or oral hypoglycemics.
Thyrotoxicosis: Masks tachycardia and other signs of hyperthyroidism; abrupt withdrawal may precipitate thyroid storm.
Muscle weakness: May potentiate myasthenic symptoms including diplopia, ptosis, and generalized weakness.
Surgical anesthesia: Impairs beta-mediated reflex cardiac response; protracted severe hypotension and difficulty restarting the heartbeat have been reported, so consider gradual withdrawal before elective surgery.
Atopy and anaphylaxis: Patients with atopy or prior severe anaphylaxis may be more reactive on repeat allergen challenge and unresponsive to usual epinephrine doses.
Angle-closure glaucoma: Little or no effect on the pupil, so it should not be used alone when the immediate objective is reopening the angle.
Vascular insufficiency: Consider alternative therapy if reduced cerebral blood flow or Raynaud's phenomenon develops after starting treatment.
Common Side Effects
Ocular: Transient ocular discomfort is the most frequent reaction; blurred vision, corneal punctate keratitis, foreign body sensation, photophobia, tearing, itching, dryness, erythema, inflammation, discharge, ocular pain, decreased visual acuity, and crusty lashes reported in small numbers of patients.
Systemic: Bradycardia, heart block, and congestive failure; pulmonary distress with dyspnea, bronchospasm, thickened bronchial secretions, asthma, and respiratory failure; insomnia, dizziness, vertigo, headache, depression, lethargy, and increased signs of myasthenia gravis; hives, toxic epidermal necrolysis, hair loss, glossitis, and perverted taste or smell.
Other betaxolol formulations: Allergic reactions, decreased corneal sensitivity, corneal punctate staining that may appear in dendritic formation, edema, and anisocoria.
Pregnancy & Lactation
Pregnancy: No adequate and well-controlled studies in pregnant women and only limited data with betaxolol eye drops; epidemiologic studies of oral beta-blockers show no malformative effect but do show a risk of intrauterine growth retardation. Use only if the potential benefit justifies the potential fetal risk.
Lactation: Beta-blockers are excreted in breast milk after oral dosing and can cause serious effects in a nursing infant; whether measurable levels reach milk after topical ocular use is unknown. Weigh the benefits of breastfeeding against the clinical need.
Pediatric Use
Safety and IOP-lowering effect demonstrated in a 3-month, multicenter, double-masked, active-controlled pediatric trial.
Bacterial keratitis: Reported with contaminated multidose containers, in most cases in eyes with concurrent corneal disease or epithelial disruption.
Choroidal detachment: Reported with aqueous suppressant therapy after filtration procedures.
Soft contact lenses: Benzalkonium chloride is absorbed by soft lenses; remove before instillation and reinsert after 15 minutes.