Betagan Unit Dose

Levobunolol hydrochloride 0.5% USP

Eye drops, solution.

Clear, greenish-yellow to light greenish-yellow solution.

Sterile aqueous ophthalmic solution.

Reduction of intraocular pressure in chronic open-angle glaucoma and ocular hypertension.

Adults (including the elderly)

The recommended adult dose is one drop of Betagan Unit Dose once or twice daily in the affected eye(s). Discard product after use.

Children

Use in children is not currently recommended.

Bronchial asthma; history of bronchial asthma; chronic obstructive pulmonary disease; sinus bradycardia; second and third degree atrioventricular block; cardiac failure; cardiogenic shock; hypersensitivity to any component.

As with other topically applied ophthalmic drugs, Betagan may be absorbed systemically.

Betagan may have additive effects in patients taking systemic antihypertensive drugs. These possible additive effects may include hypotension, including orthostatic hypotension, bradycardia, dizziness, and/ or syncope. Conversely, systemic beta-adrenoceptor blocking agents may potentiate the ocular hypotensive effect of Betagan.

Betagan may potentially add to the effects of oral calcium antagonists, rauwolfia alkaloids or beta blockers to induce hypotension and/ or marked bradycardia.

There are no adequate and well-controlled studies in pregnant women. Levobunolol should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.

It is not known whether this drug is excreted in human milk. Systemic beta-blockers and topical Timolol maleate are known to be excreted in human milk. Because similar drugs are excreted in human milk, caution should be exercised when Betagan is administered to a nursing woman.

None known.

Blepharoconjunctivitis, transient ocular burning, stinging, and decreases in heart rate and blood pressure have been reported occasionally with the use of Betagan. Urticaria has been reported rarely with the use of Betagan.

The following adverse effects have been reported rarely and a definite relationship with the use of Betagan has not been established: change in heart rhythm, iridocyclitis, browache, transient ataxia, lethargy, urticaria, elevated liver enzymes, eructation, dizziness and itching.

The following additional adverse reactions have been reported with ophthalmic use of beta₁ and beta₂ non selective blocking agents:

Special senses: conjunctivitis, blepharitis, keratitis and decreased corneal sensitivity, visual disturbances, including refractory changes, diplopia and ptosis.

Cardiovascular: bradycardia, hypotension, syncope, heartblock, cerebrovascular accident, cerebral ischaemia, congestive heart failure, palpitation and cardiac arrest.

Respiratory: bronchospasm, respiratory failure and dyspenea.

Body as a whole: asthenia, nausea and depression.

There are no data available on human overdosage with Betagan which is unlikely to occur via the ocular route. Should accidental ocular overdosage occur, flush the eye(s) with water or normal saline. If accidentally ingested, efforts to decrease further absorption may be appropriate.

Levobunolol is a non-cardioselective beta-adrenoceptor blocking agent, equipotent at both beta₁ and beta₂ receptors. Levobunolol is greater than 60 times more potent than its dextro isomer in its beta-blocking activity. In order to obtain the highest degree of beta-blocking potential without increasing the potential for direct myocardial depression, the levo isomer, levobunolol, is used. Levobunolol does not have significant local anaesthetic (membrane-stabilising) or intrinsic sympathomimetic activity. Betagan has shown to be as effective as Timolol in lowering intraocular pressure.

Betagan when instilled in the eye will lower elevated intraocular pressure as well as normal intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure presents a major risk factor in the pathogenesis of glaucomatous field loss. The higher the level of intraocular pressure, the likelihood of optic nerve damage and visual field loss.

The primary mechanism of action of levobunolol in reducing intraocular pressure is most likely a decrease in aqueous humor production. Betagan reduces intraocular pressure with little or no effect on pupil size in contrast to the miosis which cholinergic agents are known to produce.

The blurred vision and night blindness often associated with miotics would not be expected with the use of Betagan. Patients with cateracts avoid the inability to see around lenticular opacities caused by pupil constriction.

The onset of action with one drop of Betagan can be detected within one hour of treatment, with maximum effect seen between two and six hours. A significant decrease can be maintained for up to 24 hours following a single dose.

Not applicable

Polyvinyl alcohol USP

Sodium chloride EP

Disodium edetate EP

Sodium phosphate dibasic, heptahydrate USP

Potassium phosphate monobasic NF

Sodium hydroxide or hydrochloric acid (to adjust pH) EP

Purified water EP

No major incompatibilities have been reported from topical use of levobunolol.

24 months.

Store at or below 25°.

Protect from light.

Discard after use.

Low density polyethylene (LDPE) blow-fill-seal unit dose container (0.9 ml volume) filled with 0.4 ml solution.

Unit dose containers are packaged into a foil covered pouch (5 containers per pouch).

Pouches are packaged into cartons such that each carton contains 30 or 60 unit dose containers.

None.

Allergan Limited

Marlow International

The Parkway

Marlow

Bucks

SL7 1YL

UK

PL 00426/0072

20^th April 1993 / 26^th July 2003

24^th April 2008