BETAGAN 0,5% LIQUIFILM

Indications

• Elevated intraocular pressure (IOP)
• Glaucoma
• Ocular hypertension

Dosage

Children: For children, refer to the BNF for Children for appropriate dosing information.

Adults: The recommended dosage for adults is one drop of levobunolol in the affected eye(s) once or twice daily, as directed by a healthcare professional.

Mechanism of action

Levobunolol's mechanism of action in reducing IOP is not clearly defined, but it is believed to block endogenous catecholamine-stimulated increases in cyclic adenosine monophosphate (AMP) concentrations within the ciliary processes, leading to decreased aqueous humor production.

Pharmacodynamics

Levobunolol is an ophthalmic beta-blocker that acts equally at beta(1)- and beta(2)-receptor sites. It is effective in lowering both elevated and normal IOP, with a mean reduction of approximately 25-40% from baseline in patients with elevated IOP. Due to its non-selective beta-adrenergic blocking properties, it may cause systemic effects such as bronchoconstriction, decreased heart rate, and lowered blood pressure following topical administration.

Pharmacokinetics

Levobunolol is absorbed through the cornea, with systemic absorption potentially leading to cardiovascular and pulmonary effects. The pharmacokinetics of levobunolol includes rapid onset of action; however, specific half-life and clearance data are not provided in the sources. Due to its topical application, systemic exposure is lower than with oral beta-blockers.

Adverse effects

• Bronchoconstriction
• Increased airway resistance
• Decreased blood pressure
• Decreased heart rate

Interactions

• propafenone+levobunolol: Unknown (increases risk of cardiovascular adverse effects)

Pregnancy

Safety in pregnancy has not been established. Use only if clearly needed.

Breast-feeding

Caution is advised as it is not known whether levobunolol is excreted in human milk.

Storage

Store at room temperature, away from light. Do not freeze.

Formulations

• Ophthalmic solution

Indications

• Chronic open-angle glaucoma
• Ocular hypertension

Dosage

Children: Refer to the BNF for Children for specific dosing information related to paediatric patients.

Adults: Instill 1 to 2 drops into the affected eye(s) once or twice daily, as directed by a healthcare provider.

Mechanism of action

Levobunolol exerts its therapeutic effects by blocking beta-adrenergic receptors in the eye. This action decreases aqueous humor production from the ciliary body and increases outflow, thus lowering intraocular pressure. The drug's efficacy is attributed to its ability to reduce the formation of aqueous humor, which is crucial in the regulation of intraocular pressure.

Pharmacodynamics

Levobunolol demonstrates a dose-dependent reduction in intraocular pressure, with its effects typically observed within 30 minutes of administration, peaking at around 2 hours. Its duration of action can last up to 24 hours, allowing for once or twice daily dosing. The systemic absorption of levobunolol through ocular administration can lead to side effects similar to those seen with systemic beta-blockers, including bradycardia and hypotension, although this is less common.

Pharmacokinetics

Levobunolol is rapidly absorbed through the ocular tissues, with peak plasma concentrations occurring shortly after administration. The drug undergoes hepatic metabolism, primarily via cytochrome P450 enzymes, with a significant portion excreted in the urine. Its elimination half-life is approximately 3 to 4 hours, but its clinical effects may persist longer due to its action in the eye.

Contra-indications

• Bradycardia
• Heart block
• Corneal disease
• Chronic open-angle glaucoma

Adverse effects

• Eye discomfort
• Dry eye
• Blurred vision
• Eyelid disorders

Interactions

• Other non-selective beta blockers

Precautions

• Systemic absorption can occur following topical application to the eyes; consider cautions listed for systemically administered beta blockers.

Pregnancy

Manufacturer advises avoidance during pregnancy.

Breast-feeding

Manufacturer advises avoidance during breastfeeding.

Storage

Store in a cool, dry place below 25°C. Protect from light.

Formulations

• Levobunolol hydrochloride 5 mg per 1 ml eye drops (0.5% solution)

Mechanism of action

Levobunolol's mechanism of action in reducing IOP is not clearly defined, but is believed to be due to a reduction of the production of aqueous humor via blockage of endogenous catecholamine-stimulated increases in cyclic adenosine monophosphate (AMP) concentrations within the ciliary processes.

Pharmacodynamics

Levobunolol is an ophthalmic beta-blocker, equally effective at β(1)- and β(2)-receptor sites. Levobunolol reduces both elevated and normal IOP in patients with or without glaucoma. In patients with elevated IOP, levobunolol reduces mean IOP by approximately 25-40% from baseline. As the drug is a nonselective &beta-adrenergic blocking agent, it can produce both systemic pulmonary and cardiovascular effects following topical application to the eye. These effects include adverse pulmonary effects (eg. bronchoconstriction, increased airway resistance), and a decrease in blood pressure and heart rate.