Betagan0.5%

Betagan is a non-selective beta-adrenergic blocking agent formulated as an ophthalmic (eye) solution. It is FDA-approved for the following uses:

• Chronic open-angle glaucoma: Established use of Betagan for lowering elevated intraocular pressure (IOP).
• Ocular hypertension: Established use of Betagan for reducing elevated IOP in patients without glaucomatous field loss, to reduce the risk of progression to glaucoma.

Betagan may also be used as adjunctive therapy in combination with other IOP-lowering agents (for example, prostaglandin analogues or carbonic anhydrase inhibitors) when a single agent does not adequately control intraocular pressure. Betagan is not indicated as monotherapy for acute angle-closure glaucoma and is not an antibiotic or anti-infective agent.

Each mL of Levobunolol ophthalmic solution contains levobunolol hydrochloride equivalent to 0.5% (5 mg/mL) or 0.25% (2.5 mg/mL) of Levobunolol base, with inactive ingredients typically including polyvinyl alcohol, sodium chloride, edetate disodium, sodium metabisulfite, and benzalkonium chloride as a preservative.

Betagan is a synthetic, non-selective (non-cardioselective) beta-adrenergic receptor blocking agent that is equipotent at beta-1 and beta-2 receptors. Betagan is administered topically to the eye as an ophthalmic solution to lower intraocular pressure, without significant local anesthetic (membrane-stabilizing) activity at usual doses and without significant intrinsic sympathomimetic activity.

Betagan belongs to the therapeutic class of ophthalmic non-selective beta-adrenergic blocking agents (anti-glaucoma agents), used to reduce intraocular pressure.

Levobunolol is a non-cardioselective beta-adrenoceptor antagonist that blocks both beta-1 and beta-2 receptors. When applied topically to the eye, Levobunolol reduces production of aqueous humor by the ciliary epithelium, which lowers intraocular pressure. Unlike miotic agents, Levobunolol produces little or no effect on pupil size or accommodation.

The onset of action of Levobunolol can be detected within one hour after a single drop, with a duration of effect that supports once- or twice-daily dosing.

For topical ophthalmic use only. Wash hands before use. Tilt the head back, pull down the lower eyelid to form a pocket, and instill the prescribed number of drops of Betagan into the eye without touching the dropper tip to the eye or any other surface. Close the eye gently for 1-2 minutes and apply gentle pressure to the inner corner of the eye (nasolacrimal occlusion) to minimize systemic absorption. Betagan is not for injection or oral use.

• Oral beta-blockers: Concomitant use with Betagan may produce additive effects on intraocular pressure and on systemic beta-blockade (for example, additive bradycardia or hypotension).
• Calcium channel blockers: Co-administration with Betagan may increase the risk of atrioventricular conduction disturbances, left ventricular failure, and hypotension.
• Digitalis glycosides: Both digitalis and Betagan slow atrioventricular conduction; concurrent use may have additive effects.
• Catecholamine-depleting drugs (e.g., reserpine): Concurrent use with Betagan may produce additive effects such as marked hypotension and/or bradycardia.
• Other topical ophthalmic agents: If used with other eye medications, administer at least 5 minutes apart from Betagan to avoid washout.

The most common effect of Betagan is transient ocular burning and stinging upon instillation (reported in up to about 1 in 3 patients), and blepharoconjunctivitis (in up to about 1 in 20 patients).

Less common effects reported with Betagan include:

• Ocular: iridocyclitis, decreased corneal sensitivity, conjunctival hyperemia, blurred vision
• Cardiovascular: bradycardia, hypotension, syncope, heart block (see Contraindications and Precautions)
• Respiratory: bronchospasm, dyspnea (see Contraindications)
• Systemic/other: headache, dizziness, transient ataxia, lethargy, urticaria, pruritus, depression, confusion, muscle weakness

Betagan should be used during pregnancy only if the potential benefit to the mother clearly justifies the potential risk to the fetus; a physician should be consulted before use in pregnancy. It is not fully known whether topically applied Betagan is excreted in human milk, but systemically administered beta-blockers are known to appear in breast milk; caution is advised and a physician should be consulted before using Betagan while breastfeeding.

Cardiac effects: Sympathetic stimulation may be essential for supporting circulation in patients with diminished myocardial contractility. Beta-blockade with Betagan, even at usual ophthalmic doses, carries a risk of inducing cardiac failure in susceptible patients and should be used with caution in those with a history of cardiac failure.

Respiratory reactions: Although Betagan is contraindicated in bronchial asthma and severe COPD (see Contraindications), respiratory reactions including bronchospasm have rarely been reported, and caution is warranted in patients with any degree of bronchospastic disease.

Masking of hypoglycemia and hyperthyroidism: Beta-blockade with Betagan may mask signs and symptoms of acute hypoglycemia in diabetic patients and may mask certain clinical signs of hyperthyroidism (e.g., tachycardia); use cautiously in these patients.

Anesthesia and major surgery: Betagan may blunt the cardiac response needed during anesthesia and major surgery; gradual withdrawal may be considered before elective surgery.

Contact lenses: The formulation contains benzalkonium chloride, which may be absorbed by soft contact lenses; remove lenses before instilling Betagan and wait at least 15 minutes before reinserting them.

There is limited clinical experience with overdose of Betagan. Systemic overdosage may be expected to produce symptoms of beta-adrenergic blockade such as symptomatic bradycardia, hypotension, bronchospasm, and acute cardiac failure. If accidental ingestion or overdose of Betagan occurs, or if severe symptoms develop, seek immediate medical attention or contact a poison control center right away; treatment is generally supportive and should be managed by a physician in a medical facility. Do not attempt to manage a suspected overdose at home without medical guidance.

Store Betagan ophthalmic solution between 15°C and 25°C (59°F to 77°F), protected from light. Keep the bottle tightly closed when not in use and keep out of reach of children.

Pediatric use: Safety and effectiveness of Betagan in children have not been established.

Geriatric use: No overall differences in safety or effectiveness have been observed between elderly and younger adult patients using Betagan.

Renal/hepatic impairment: No well-established dose-adjustment guidelines exist for Betagan in renal or hepatic impairment; use with caution and physician supervision given the potential for systemic beta-blocker effects.

See Pregnancy and Lactation for use of Betagan during pregnancy and breastfeeding.

Betagan is typically used long-term for chronic management of open-angle glaucoma and ocular hypertension, since these are chronic conditions requiring ongoing intraocular pressure control. Duration of therapy with Betagan should be determined by the prescribing ophthalmologist based on regular monitoring of intraocular pressure and optic nerve status; treatment should not be stopped abruptly without medical advice.

Levobunolol belongs to the class of non-selective (non-cardioselective) beta-adrenergic receptor blocking agents used ophthalmically.

Levobunolol works by blocking beta-1 and beta-2 adrenergic receptors in the ciliary epithelium of the eye, thereby decreasing the rate of aqueous humor production. This reduction in aqueous humor formation lowers intraocular pressure, without significantly affecting pupil size (miosis) or accommodation.

C

Safety and effectiveness of Betagan in pediatric patients have not been established. Betagan should be used in children only under close physician supervision, if the potential benefit is judged to outweigh potential risk, since systemic beta-blocker absorption may occur even with topical ophthalmic use.