Betagan®

GoodRx

Levobunolol 0.25%, 0.5% · ophthalmic solution

Antiglaucoma

Approved uses

Elevated IOP in chronic open-angle glaucoma or ocular hypertension

1 to 2 drops of 0.5% in the affected eye(s) QD; BID in more severe or uncontrolled glaucoma

IOP falls within 1 hour, peaks at 2 to 6 hours, lasts 24 hours, and averages a 7 to 8 mmHg drop.

Elevated IOP, once-daily maintenance regimen

1 drop of 0.5% in the affected eye(s) QD

Once-daily dosing gives a 14% to 18% IOP reduction, matching twice-daily by 2 weeks.

Contraindications

Bronchial asthma or a history of bronchial asthma.
Severe chronic obstructive pulmonary disease.
Sinus bradycardia.
Second and third degree atrioventricular block.
Overt cardiac failure.
Cardiogenic shock.
Hypersensitivity to any component.

Available Forms

0.5% solution, 5 mL, 10 mL, 15 mL

Mechanism of Action

Noncardioselective beta-adrenoceptor blocker, equipotent at beta-1 and beta-2 receptors, without significant intrinsic sympathomimetic or membrane-stabilizing activity. Lowers IOP primarily by decreasing aqueous humor production, with onset within 1 hour, maximum effect at 2 to 6 hours, and a significant reduction maintained up to 24 hours after a single dose.

Warnings & Precautions

Systemic absorption: Topical dosing can produce the same reactions as systemic beta-blockade, including death from bronchospasm in patients with asthma and, rarely, death associated with cardiac failure; ophthalmic beta-blockers may also impair compensatory tachycardia and increase risk of hypotension.
Cardiac failure: Beta-blockade may precipitate more severe failure where sympathetic support of the circulation is needed, and continued myocardial depression can lead to failure even in patients with no prior history; discontinue at the first sign or symptom.
Obstructive pulmonary disease: Patients with mild or moderate COPD or nonasthmatic bronchospastic disease should in general not receive a beta-blocker; if used, it may block bronchodilation from endogenous and exogenous beta-2 stimulation.
Vascular insufficiency: May potentiate syndromes associated with vascular insufficiency such as Raynaud's phenomenon.
Cerebrovascular insufficiency: Consider alternative therapy if signs of reduced cerebral blood flow appear.
Major surgery: Beta-blockade impairs reflex cardiac response; protracted severe hypotension and difficulty restarting the heartbeat have been reported under general anesthesia, so gradual withdrawal before elective surgery may be appropriate.
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: Beta-blockade may potentiate myasthenic symptoms including diplopia, ptosis, and generalized weakness.
Increased allergen reactivity: Patients with a history of severe anaphylaxis may be more reactive on repeat challenge and unresponsive to usual epinephrine doses.
Angle-closure glaucoma: Little or no effect on the pupil; when used to lower IOP in a closed angle it must be followed with a miotic, not given alone.
Choroidal detachment: Reported with aqueous suppressant therapy after filtration procedures.
Sulfite content: Contains sodium metabisulfite, which can cause anaphylactic or life-threatening asthmatic reactions in susceptible people, seen more frequently in asthmatics.
Soft contact lenses: Benzalkonium chloride is absorbed by soft lenses; remove before instillation and reinsert after 15 minutes.

Common Side Effects

Ocular: Transient burning and stinging in up to 1 in 3 patients; blepharoconjunctivitis in up to 1 in 20; decreased corneal sensitivity in a small number of patients and possible after prolonged use; iridocyclitis reported rarely.
Systemic: Decreased heart rate and blood pressure; headache, transient ataxia, dizziness, lethargy, urticaria, and pruritus reported rarely.
Beta-blocker class reactions: Attributed by the label either to this drug or to ophthalmic use of other beta-blockers, comprising bradycardia, arrhythmia, heart block, hypotension, syncope, congestive heart failure, cardiac arrest, bronchospasm (predominantly in pre-existing bronchospastic disease), respiratory failure, depression, confusion, worsening myasthenia gravis, Stevens-Johnson syndrome, keratitis, blepharoptosis, diplopia, refractive changes, and impotence.

Pregnancy & Lactation

Pregnancy: No adequate and well-controlled studies in pregnant women; use only if the potential benefit justifies the potential fetal risk. Fetotoxicity (increased resorption sites) occurred in rabbits at 200 and 700 times the recommended glaucoma dose, with no fetotoxicity or malformations in rats up to 1,800 times.

Lactation: Excretion in human milk is unknown, but systemic beta-blockers and topical timolol are excreted in human milk; use caution in a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.