Betoptic Eye Drops Solution

1. Name Of The Medicinal Product

Betoptic 0.5% w/v eye drops, solution

2. Qualitative And Quantitative Composition

Betaxolol 0.5% w/v (as hydrochloride)

3. Pharmaceutical Form

Eye Drops, Solution

4. Clinical Particulars

4.1 Therapeutic Indications

Betoptic is indicated for the reduction of elevated intraocular pressure in patients with ocular hypertension and chronic open angle glaucoma.

4.2 Posology And Method Of Administration

Adults (including the elderly)

The usual dose is one drop to be instilled into the affected eye(s) twice daily.

Children

Betoptic is not recommended for use in children.

4.3 Contraindications

Betoptic is contraindicated in patients with sinus bradycardia greater than a first degree block, cardiogenic shock or a history of overt cardiac failure and in patients with hypersensitivity to any component.

4.4 Special Warnings And Precautions For Use

Patients who are receiving a beta-adrenergic blocking agent orally and Betoptic should be observed for potential additive effect either on intraocular pressure or the known systemic effects of beta-blockade.

While Betoptic has demonstrated a low potential for systemic effects, it should be used with caution in patients with diabetes (especially labile diabetes) or in patients suspected of developing thyrotoxicosis.

Consideration should be given to the gradual withdrawal of beta-adrenergic blocking agents prior to general anaesthesia because of the reduced ability of the heart to respond to beta-adrenergically mediated sympathetic reflex stimuli.

Betoptic, a cardioselective beta-blocker, has produced only minimal effects in patients with reversible airway obstruction; however, caution should be exercised in the treatment of patients with a history of obstructive pulmonary disease.

In patients with angle-closure glaucoma, the immediate treatment objective is to re-open the angle by constriction of the pupil with a miotic agent, betaxolol has no effect on the pupil, therefore, Betoptic should be used with a miotic to reduce elevated intraocular pressure in angle-closure glaucoma.

This product contains benzalkonium chloride and is not recommended for use when soft contact lenses are being worn.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Although Betoptic used alone has little or no effect on pupil size, mydriasis resulting from concomitant therapy with Betoptic and adrenaline has been reported occasionally.

Close observation of the patient is recommended when a beta blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or bradycardia. Caution should be exercised in patients using concomitant adrenergic psychotropic drugs.

4.6 Pregnancy And Lactation

Although animal studies have not demonstrated any specific hazard there are no adequate and well-controlled studies in pregnant women. Because animal studies are not always predictive of human response this drug should be used during pregnancy only if clearly indicated.

It is not known whether Betoptic is excreted in human milk, caution should therefore be exercised when Betoptic is administered to nursing mothers.

4.7 Effects On Ability To Drive And Use Machines

No effects on ability to drive and use machines have been reported.

4.8 Undesirable Effects

Although Betoptic is generally well tolerated, discomfort of short duration may be experienced by some patients upon instillation and occasional tearing has been reported.

Ocular Effects

Common: discomfort

Uncommon: tearing

Rare: decreased corneal sensitivity, erythema, itching, corneal punctate staining, keratitis, anisocoria and photophobia.

Systemic reactions following topical administration of betaxolol have been rarely reported.

Systemic Effects:

Nervous:

Rare: insomnia, depression

Body as a Whole:

Rare: headache

Cardiovascular:

Rare: bradycardia

Respiratory:

Rare: dyspnoea, asthma

Skin and Appendages:

Rare: alopecia

Since topically applied beta-adrenergic blocking agents may be absorbed systemically, adverse reactions found with systemic administration of beta₁-adrenergic blocking agents may occur with topical administration (see 4.4 Special Warnings).

These may include bradycardia, a slowed AV-conduction or increase of an existing AV-block, hypotension, heart failure, cold and cyanotic extremities, Raynaud phenomenon, paraesthesia of the extremities, increase of an existing intermittent claudication, fatigue, headaches, impaired vision, hallucinations, psychoses, confusion, impotence, dizziness, sleep disturbances, depression, nightmares, gastro-intestinal problems, nausea, vomiting, diarrhoea, bronchospasm in patients with bronchial asthma or a history of asthmatic complaints, disorder of the skin, especially rash, and dry eyes. Beta blockers may mask the symptoms of thyrotoxicosis or hypoglycemia. An increase in Anti Nuclear Antibodies (ANA) has been seen; its clinical relevance is unclear.

4.9 Overdose

A topical overdose of Betoptic may be flushed from the eye(s) with warm tap water.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Ophthalmologicals: Antiglaucoma Preparations & Miotics.

ATC Code: SO1E D02

Betaxolol is a cardioselective Beta₁ receptor blocker which, when applied topically to the eye, lowers intraocular pressure. It is thought to produce this effect by reducing the rate of production of aqueous humour.

Clinical Pharmacology

Several studies have indicated that betaxolol may have a beneficial effect on visual function for up to 48 months in patients with chronic open-angle glaucoma and up to 60 months in patients with ocular hypertension. Moreover there is evidence that betaxolol maintains or increases ocular blood flow/perfusion.

5.2 Pharmacokinetic Properties

Betaxolol is highly lipophilic which results in good permeation of the cornea, allowing high intraocular levels of the drug. Betaxolol is characterised by its good oral absorption, low first pass loss and a relatively long half-life of approx 16-22 hours. The elimination of betaxolol is primarily by the renal rather than faecal route. The major metabolic pathways yield two carboxylic acid forms plus unchanged betaxolol in the urine (approx. 16% of the administered dose).

5.3 Preclinical Safety Data

There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Disodium edetate, sodium chloride, benzalkonium chloride, sodium hydroxide, hydrochloric acid, purified water.

6.2 Incompatibilities

None known.

6.3 Shelf Life

Unopened 36 months, after opening 28 days.

6.4 Special Precautions For Storage

Do not store above 25°C.

Keep in the outer carton in order to protect from light.

6.5 Nature And Contents Of Container

5 ml & 10 ml LDPE bottles (10 ml present in 15 ml container) with natural LDPE plug and blue polystyrene or polypropylene cap.

6.6 Special Precautions For Disposal And Other Handling

Do not touch the top of the bottle to any surface as this may contaminate the contents.

7. Marketing Authorisation Holder

Alcon Laboratories (UK) Ltd.

Pentagon Park

Boundary Way

HemelHempstead

Herts. HP2 7UD

8. Marketing Authorisation Number(S)

PL 0649/0097

9. Date Of First Authorisation/Renewal Of The Authorisation

19^th August 1986 / 14^th November 2001.

10. Date Of Revision Of The Text

May 2010