Betoptic 0.5% w/v eye drops, solution

Betaxolol 0.5% w/v (as hydrochloride)

Eye Drops, Solution

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

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.

When using nasolacrimal occlusion or closing the eyelids for 2 minutes, the systemic absorption is reduced. This may result in a decrease in systemic side effects and an increase in local activity.

• Hypersensitivity to the active substance or to any of the excipients.

• Reactive airway disease including severe bronchial asthma or a history of severe bronchial asthma, severe chronic obstructive pulmonary disease.

• Sinus bradycardia, sick sinus syndrome, sino-atrial block, second or third degree atrioventricular block not controlled with pace-maker. Overt cardiac failure, cardiogenic shock.

Like other topically applied ophthalmic agents, betaxolol is absorbed systemically. Due to the beta-adrenergic component, betaxolol, the same types of cardiovascular, pulmonary and other adverse reactions seen with systemic beta-adrenergic blocking agents may occur. Incidence of systemic ADRs after topical ophthalmic administration is lower than for systemic administration. To reduce the systemic absorption, see section 4.2.

Cardiac disorders: In patients with cardiovascular diseases (e.g. coronary heart disease, Prinzmetal's angina and cardiac failure) and hypotension, therapy with beta-blockers should be critically assessed and the therapy with other active substances should be considered. Patients with cardiovascular diseases should be watched for signs of deterioration of these diseases and of adverse reactions.

Due to its negative effect on conduction time, beta-blockers should only be given with caution to patients with first degree heart block.

Vascular disorders: Patients with severe peripheral circulatory disturbance/disorders (i.e. severe forms of Raynaud's disease or Raynaud's syndrome) should be treated with caution.

Respiratory disorders: Respiratory reactions, including death due to bronchospasm in patients with asthma have been reported following administration of some ophthalmic beta-blockers.

Patients with mild/moderate bronchial asthma, a history of mild/moderate bronchial asthma or, mild/moderate chronic obstructive pulmonary disease (COPD) should be treated with caution.

Hypoglycaemia/Diabetes: Beta-blockers should be administered with caution in patients subject to spontaneous hypoglycaemia or to patients with labile diabetes, as beta-blockers may mask the signs and symptoms of acute hypoglycaemia. While Betoptic has demonstrated a low potential for systemic effects, it should be used with caution in patients suspected of developing thyrotoxicosis.

Beta-blockers may also mask the signs of hyperthyroidism.

Corneal diseases: 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.

Ophthalmic beta-blockers may induce dryness of eyes. Caution should be exercised in the use of beta-blocking agents in patients with corneal diseases, Sicca Syndrome or similar tear film abnormalities.

Other beta-blocking agents: The effect on intra-ocular pressure or the known effects of systemic beta-blockade may be potentiated when betaxolol is given to the patients already receiving a systemic beta-blocking agent. The response of these patients should be closely observed. The use of two topical beta-adrenergic blocking agents is not recommended (see section 4.5)

Anaphylactic reactions: While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge with such allergens and unresponsive to the usual dose of adrenaline used to treat anaphylactic reactions.

Choroidal detachment: Choroidal detachment has been reported with administration of aqueous suppressant therapy (e.g. timolol, acetazolamide) after filtration procedures.

Surgical anaesthesia: Beta-blocking ophthalmological preparations may block systemic beta-agonist effects e.g. of adrenaline. The anaesthesiologist should be informed when the patient is receiving betaxolol. 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.

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

No specific drug interaction studies have been performed with betaxolol.

There is a potential for additive effects resulting in hypotension and/or marked bradycardia when ophthalmic beta-blockers solution is administered concomitantly with oral calcium channel blockers, beta-adrenergic blocking agents, anti-arrhythmics (including amiodarone), digitalis glycosides, parasympathomimetics, guanethidine and catecholamine-depleting drugs such as reserpine. Close observation of the patient is recommended. .

Caution should be exercised in patients using concomitant adrenergic psychotropic drugs.

mydriasis resulting from concomitant use of ophthalmic beta-blockers and adrenaline (epinephrine) has been reported occasionally.

Pregnancy

There are no adequate data for the use of betaxolol in pregnant women. Betaxolol should not be used during pregnancy unless clearly necessary. To reduce the systemic absorption, see section 4.2.

Epidemiological studies have not revealed malformative effects but show a risk for intra-uterine growth retardation when beta-blockers are administered by the oral route. In addition, signs and symptoms of beta-blockade (e.g. bradycardia, hypotension, respiratory distress and hypoglycaemia) have been observed in the neonate when beta-blockers have been administered until delivery. If BETOPTIC SOLUTION is administered until delivery, the neonate should be carefully monitored during the first days of life.

Lactation

Beta-blockers are excreted in breast milk. However, at therapeutic doses of betaxolol in eye drops, it is not likely that sufficient amounts would be present in breast milk to produce clinical symptoms of beta-blockade in the infant. To reduce systemic absorption, see section 4.2.

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

Like other topically applied ophthalmic drugs, betaxolol is absorbed into the systemic circulation. This may cause similar undesirable effects as seen with systemic beta-blocking agents. Incidence of systemic ADRs after topical ophthalmic administration is lower than for systemic administration. Listed adverse reactions include reactions seen within the class of ophthalmic beta-blockers

Additional adverse reactions have been seen with ophthalmic beta-blockers and may potentially occur with BETOPTIC SOLUTION:

Immune system disorders:

Frequency unknown: Systemic allergic reactions including angioedema, urticaria, localized and generalized rash, pruritus, anaphylactic reaction.

Metabolism and nutrition disorders:

Frequency unknown: Hypoglycaemia.

Psychiatric disorders:

Rare: insomnia, depression

Frequency unknown: nightmares, memory loss, hallucinations, psychoses, confusion.

Nervous system disorders:

Rare: headache

Frequency unknown: Syncope, cerebrovascular accident, cerebral ischemia, increases in signs and symptoms of myasthenia gravis, dizziness, paraesthesia.

Eye disorders:

Common: discomfort

Uncommon: tearing

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

Frequency unknown: Signs and symptoms of ocular irritation (e.g. burning, stinging, redness), blepharitis, blurred vision, and choroidal detachment following filtration surgery (see 4.4 Special warnings and special precautions for use), dry eyes, corneal erosion, ptosis, diplopia.

Cardiac disorders:

Rare: bradycardia

Frequency unknown: Chest pain, palpitations, oedema, arrhythmia, congestive heart failure, atrioventricular block, cardiac arrest, cardiac failure. A slowed AV-conduction or increase of an existing AV-block

Vascular disorders:

Frequency unknown: Hypotension, Raynaud's phenomenon, cold and cyanotic hands and feet, Increase of an existing intermittent claudication.

Respiratory, thoracic, and mediastinal disorders:

Rare: dyspnoea, asthma

Frequency unknown: Bronchospasm (predominantly in patients with pre-existing bronchospastic disease), cough.

Gastrointestinal disorders:

Frequency unknown: Dysgeusia, nausea, dyspepsia, diarrhoea, dry mouth, abdominal pain, vomiting.

Skin and subcutaneous tissue disorders:

Rare: alopecia

Frequency unknown: Psoriasiform rash or exacerbation of psoriasis, skin rash.

Musculoskeletal and connective tissue disorders:

Frequency unknown: Myalgia.

Reproductive system and breast disorders:

Frequency unknown: Sexual dysfunction, decreased libido, impotence.

General disorders and administration site conditions:

Frequency unknown: Asthenia/fatigue.

An increase in Anti Nuclear Antibodies (ANA) has been seen; its clinical relevance is unclear.

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

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.

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).

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

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

None known.

Unopened 36 months, after opening 28 days.

Do not store above 25°C.

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

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

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

Alcon Laboratories (UK) Ltd.

Pentagon Park

Boundary Way

HemelHempstead

Herts. HP2 7UD

PL 0649/0097

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

26^th March 2012