Consumer medicine information

BETOPTIC Eye Drops 0.5%; BETOPTIC S Eye Drops 0.25%

Betaxolol

BRAND INFORMATION

Brand name

Betoptic 0.5% Eye Drops

Active ingredient

Betaxolol

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using BETOPTIC Eye Drops 0.5%; BETOPTIC S Eye Drops 0.25%.

What in this leaflet

Read this leaflet carefully before you start to use Betoptic.

This leaflet answers some common questions about Betoptic. It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

The information in this leaflet was last updated on the date listed on the final page. More recent information on the medicine may be available.

You should ensure that you speak to your pharmacist or doctor to obtain the most up to date information on the medicine.

You can also download the most up to date leaflet from www.novartis.com.au

The updates may contain important information about the medicine and its use of which you should be aware.

All medicines have risks and benefits. Your doctor has weighed the risks of you using Betoptic against the benefits they expect it will have for you.

If you have any concerns about using this medicine, ask your doctor or pharmacist.

Keep this leaflet with your medicine.

You may need to read it again.

What BETOPTIC is used for

Betoptic contains the active ingredient betaxolol hydrochloride. Betaxolol hydrochloride belongs to a class of medicines known as "beta-adrenergic blocking agents".

Your doctor has prescribed Betoptic for you because the pressure within your eye(s), known as "intraocular pressure" is higher than normal. This raised pressure may damage your eyesight and lead to a condition known as glaucoma.

There are usually no symptoms of glaucoma. If glaucoma is not treated it can lead to serious problems, including total blindness. Untreated glaucoma is one of the most common causes of blindness.

Betoptic is used, either alone or in combination with other medicines, to lower the raised pressure within your eye(s). Betoptic does this by reducing the amount of fluid produced within your eye(s).

Although Betoptic helps control your glaucoma it does not cure it. So you must keep using it until your doctor tells you to stop.

For more information about glaucoma, contact Glaucoma Australia Inc. (PO BOX 420, Crows Nest 1585 telephone 1800 500 880).

Ask your doctor if you have any questions about why Betoptic has been prescribed for you.

Your doctor may have prescribed it for another reason.

Use in Children

Betoptic is not recommended for use in children. The safety and effectiveness of Betoptic in children has not been established.

Before you use BETOPTIC

When you must not use it

Let your doctor know if any of the following applies to you before you start using Betoptic:

  • You are allergic to betaxolol hydrochloride or to any of the other ingredients in these eye drops that are listed under "Product Description".

Some of the symptoms of an allergic reaction may include:

  • shortness of breath
  • wheezing or difficulty breathing
  • swelling of the face, lips, tongue or other parts of the body
  • rash, itching or hives on the skin.

Tell your doctor if:

  • You have a very slow heartbeat or irregular heartbeat
  • You have cardiac failure or any other serious heart conditions.

If you have not told your doctor about any of the above, tell him/her before you start using Betoptic.

Do not use this medicine if the expiry date has passed, the packaging is torn or the safety seal around the closure and neck area is broken.

If it has expired or is damaged, return it to your pharmacist for disposal.

If you use your medicine after the expiry date has passed, it may not work as well.

Before you start to use it

Tell your doctor if:

  • You are pregnant, or intend to become pregnant

Your doctor will discuss the possible risks and benefits of using Betoptic during pregnancy.

  • You are breast-feeding or intend to breast-feed

Your doctor will discuss the possible risks and benefits of using Betoptic when you are breast-feeding.

Tell your doctor if have or have had any of the following medical conditions:

  • Any type of respiratory or breathing disorder (e.g. wheezing or asthma)
  • Diabetes
  • An overactive thyroid gland
  • Any form of muscle weakness
  • Heart failure or heart block or any heart condition
  • Severe circulation disorders e.g. Raynaud's disease or syndrome
  • A condition called phaeochromocytoma which is a tumour in the brain
  • Metabolic acidosis where the body produces excessive acid that is not cleared by the kidneys.

Tell your doctor if you are about to have either major surgery or eye surgery.

This includes those doctors treating you in hospital or in a clinic. Your dose of Betoptic may need to be adjusted or gradually stopped prior to surgery.

Tell your doctor if you are a contact lenses wearer.

This is particularly important if you are currently using any other type of anti-glaucoma medication or any other eye drops.

Do not put Betoptic into your eye(s) while you are wearing soft contact lenses.

The preservative in Betoptic, benzalkonium chloride, may be deposited in contact lenses.

You can put your soft contact lenses back into your eyes 15 minutes after you have used Betoptic.

If you are not sure if you should start using Betoptic, talk to your doctor.

Taking or using other medicines

Tell your doctor or pharmacist if you are taking or using other medicines, including medicines that you get without a doctor's prescription from a pharmacy, supermarket or health food shop.

Some medicines and Betoptic interfere with each other. These include:

  • other beta-blockers, calcium blockers, including amiodarone, and digitalis glycosides
  • certain medicines used to treat lower blood pressure e.g. reserpine
  • some medicines used to treat major mental illnesses.

These medicines may be affected by Betoptic or may affect how well it works. You may need different amounts of your medicines.

Your doctor or pharmacist have more information on medicines to be careful with or avoid while using this medicine.

How to use BETOPTIC

Follow all directions given to you by your doctor or pharmacist carefully.

They may differ from the information contained in this leaflet.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to use

It is important that you shake Betoptic or Betoptic S Eye Drops well before using them.

The usual dose of Betoptic or Betoptic S Eye Drops is one drop in the affected eye(s) two times each day. Your dosing instructions will be printed on the label your pharmacist puts on the bottle or carton.

Using your eye drops at the same time each day will have the best effect on your eye pressure. It will also help you remember when to use the eye drops.

Do not use Betoptic more often than your doctor or pharmacist has told you.

If you have been using any other eye drops for the treatment of raised intraocular pressure or glaucoma, it may take several days to change from the old drops to Betoptic or Betoptic S Eye Drops. It is important that you carefully follow your doctor's instructions for the changeover.

After using Betoptic wait at least 5 minutes before putting any other eye drops in your eye(s).

How to use it

Follow these steps to use Betoptic:

  1. Wash your hands thoroughly.
  2. Immediately before using a bottle for the first time, break the safety seal around the neck area and throw the loose plastic ring away.
  3. Shake the bottle well.
  4. Remove the cap from the bottle.
  5. Hold the bottle upside down in one hand between your thumb and middle finger (see Diagram 1).
  1. While tilting your head back, gently pull the lower eyelid of your eye down using the forefinger of your other hand.
  2. Place the dropper tip close to, but not touching, your lower eyelid and gently tap or press the base of the bottle with your forefinger to release one drop (see Diagrams 2 and 3).
  1. Close your eye gently without blinking and press on the inside corner of your eye with the pad of your index finger for two minutes.
  2. If necessary, repeat the above steps for your other eye.
  3. Place the cap on the bottle and close it tightly.
  4. Wash your hands again.

You may feel a slight burning sensation in the eye shortly after using Betoptic. If this persists, or is very uncomfortable, contact your doctor or pharmacist.

Do not touch the tip of the dropper to your eye or to any other surface.

This will help to prevent your eye drops becoming dirty or contaminated.

If you wear contact lenses take the lenses out before you use Betoptic. Wait 15 minutes before putting back your contact lenses.

How long to use it

Continue using Betoptic every day as long as your doctor prescribes.

Betoptic helps control your condition but does not cure it.

If you forget to use it

If you forget to use Betoptic, you should put the drops that you missed in as soon as you remember and then go back to using them normally. If it is almost time for your next dose, skip the dose that you have missed and take your next dose when you are due to.

Never use a double dose to make up for the one that you missed.

If you are not sure what to do, contact your doctor or pharmacist.

If you use too much (overdose)

If you accidentally put too many drops in your eye(s), immediately rinse your eye(s) with warm water or normal saline.

If anyone accidentally swallows Betoptic or Betoptic S Eye Drops, immediately telephone your doctor, the Poisons Information Centre on 13 11 26 766 or go to Accident and Emergency at the nearest hospital. Do this even if there are no signs of discomfort or poisoning.

While you are using BETOPTIC

Things you must do

To make sure that Betoptic is working properly, have your eye pressure checked regularly by your doctor.

Have your eyes checked for any other changes you experience.

Tell your doctor if you become pregnant while you are using Betoptic.

Tell your doctor and pharmacist that you are using Betoptic before you start taking or using any other medicines.

Things that you must not do

Do not let children handle Betoptic or Betoptic S Eye Drops. If a child accidentally swallows any of the drops read the instructions under "If you use too much (overdose)".

Do not give this medicine to anyone else, even if they appear to have the same condition as you.

Things to be careful of

Be careful driving or operation machinery until you know how Betoptic affects you.

As with any eye medicines, temporary blurred vision or other visual disturbances may affect the ability to drive and use machinery in some people. If blurred vision occurs when you use your drops, wait until your vision is clear before driving.

Side Effects

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Tell your doctor as soon as possible if you do not feel well while you are using Betoptic.

Most side effects from Betoptic occur in, or around, the eye.

These include:

  • Discomfort or pain in the eye(s)
  • A loss of feeling to the surface of the eye(s)
  • Redness, inflammation, irritation and/or itching in your eye(s), eyelids or the surrounding lining of the eyelids
  • Inflammation of the cornea (clear front portion of your eye) (punctuate keratitis)
  • Blurred vision and/or problems seeing clearly
  • A feeling that something is in your eye(s)
  • Eyelid spasms
  • A dry eye(s)
  • Crusty eyelash(es) or eyelids
  • Discomfort in the eye(s) due to a greater sensitivity to light
  • Weakness or easily fatigued eyes.

Occasionally, some people notice unwanted effects in the rest of their body as a result of using Betoptic.

Tell your doctor immediately if you notice any of the following effects:

  • Changes in breathing (e.g. wheezing or asthma)
  • Cough
  • Respiratory infection, sinusitis, runny nose
  • Circulation problems
  • Fast or slowing of heart beat, irregular heart beat
  • Nausea
  • Trouble sleeping
  • Headache
  • Dizziness
  • Fainting
  • Tiredness and/or depression
  • Decreased libido
  • Hives and more severe forms of skin rash
  • Flaking skin and/or hair loss
  • Sore tongue
  • Altered taste sensation.

These may be serious side effects. You may need urgent medical attention. Serious side effects are rare.

Other side effects not listed above may occur in some people.

After using BETOPTIC

Keep Betoptic and Betoptic S Eye Drops in a cool place, below 25°C. Do not freeze.

Store the bottle in the outer carton.

Do not leave Betoptic or Betoptic S Eye Drops in the bathroom or near a sink.

Do not leave it on a window sill or in the car.

Heat and dampness can destroy some medicines.

Keep Betoptic and Betoptic S Eye Drops, and all other medicines, in a safe place away from the sight or reach of children.

A locked cupboard at least one-and-a half metres above the ground is a good place to store medicines.

Discard each bottle of Betoptic or Betoptic S Eye Drops 4 weeks after it has been opened. Write the date the bottle was opened on the label to remind you when to discard the bottle.

Product Description

What it looks like

Betoptic Eye drops are a sterile isotonic solution supplied in a 5 mL Drop-Tainer® dispensing bottle.

Betoptic S Eye drops are a sterile ophthalmic resin suspension supplied in in a 5 mL Drop-Tainer® dispensing bottle.

Ingredients

The active ingredient in Betoptic Eye Drops is betaxolol hydrochloride equivalent to betaxolol 5mg/mL.

Betoptic Eye Drops also contain:

  • Benzalkonium chloride (as a preservative)
  • Disodium edetate
  • Sodium chloride
  • Purified water.

The active ingredient in Betoptic S Eye Drops is betaxolol hydrochloride equivalent to betaxolol 2.5mg/mL.

Betoptic S Eye drops also contain:

  • Benzalkonium chloride (as a preservative)
  • Polystyrene sulfonate hydrogen
  • Carbomer 934P
  • Sodium edetate
  • Mannitol
  • Purified water.

Supplier

This product is supplied in Australia by:

Novartis Pharmaceuticals Australia Pty Limited
ABN 18 004 244 160
54 Waterloo Road
Macquarie Park NSW 2113
Telephone No. 1800 671 203
www.novartis.com.au

Australian Registration Number

Betoptic Eye Drops: Aust R No. 25272

Betoptic S Eye Drops: Aust R No.42900

Date of Preparation

This leaflet was revised in July 2017.

® Registered Trademark.

© Novartis Pharmaceuticals Australia Pty Limited 2017

Internal document code:
(bet050717c_2) based on PI
(bet050717i)

BRAND INFORMATION

Brand name

Betoptic 0.5% Eye Drops

Active ingredient

Betaxolol

Schedule

S4

 

Name of the medicine

Betoptic Eye Drops 0.5%.

Betaxolol 5.0 mg/mL (as hydrochloride).

Betoptic S Eye Drops 0.25%.

Betaxolol 2.5 mg/mL (as hydrochloride).

Excipients.

Betoptic Eye Drops 0.5%.

Benzalkonium chloride 0.1 mg/mL (preservative), disodium edetate, sodium chloride and purified water.

Betoptic S Eye Drops 0.25%.

Benzalkonium chloride 0.1 mg/mL (preservative), mannitol, polystyrene sulfonate hydrogen, carbomer 934P, disodium edetate and purified water.

Description

Chemical name: (±)-1-[p-[2-(cyclopropylmethoxy)ethyl] phenoxy]-3-(isopropylamino)- 2-propanol hydrochloride. Molecular formula: C18H29NO3.HCl. MW: 343.89. CAS: 63659-19-8.
Betoptic Eye Drops 0.5% and Betoptic S Eye Drops 0.25% contain the equivalent of 5 mg/mL and 2.5 mg/mL betaxolol, respectively. They have been formulated as sterile, multiple dose products for topical ophthalmic use. Betoptic S Eye Drops 0.25% are presented as a sterile ophthalmic resin suspension, providing a clinically equivalent hypotensive effect to that seen with the sterile isotonic ophthalmic solution, Betoptic Eye Drops 0.5% (see Clinical Trials).
Betaxolol hydrochloride, a white crystalline powder soluble in water, is a cardioselective beta-1-adrenergic receptor blocking agent.
Betoptic Eye Drops 0.5% also contain benzalkonium chloride 0.1 mg/mL (preservative), disodium edetate, sodium chloride and purified water.
Betoptic S Eye Drops 0.25% also contain benzalkonium chloride 0.1 mg/mL (preservative), mannitol, polystyrene sulfonate hydrogen, carbomer 934P, disodium edetate and purified water.

Pharmacology

Betaxolol hydrochloride is a cardioselective (beta-1-adrenergic) receptor blocking agent. Orally administered beta-adrenergic blocking agents reduce cardiac output in healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta-adrenergic receptor antagonists may inhibit the sympathetic stimulatory effect necessary to maintain adequate cardiac function.
When instilled in the eye, Betoptic Eye Drops 0.5% and Betoptic S Eye Drops 0.25% have the action of reducing elevated intraocular pressure as well as normal intraocular pressure, whether or not accompanied by glaucoma.
Optic nerve head damage and visual field loss are a result of a sustained elevated intraocular pressure and poor ocular perfusion. The ocular hypotensive action of betaxolol appears to be mediated by a reduction of aqueous production as demonstrated by tonography and aqueous fluorophotometry. The onset of action with betaxolol can generally be noted within 30 minutes and the maximal effect can usually be detected two hours after topical administration. A single dose provides a twelve hour reduction in intraocular pressure.
Betaxolol has little or no effect on pupil size and does not produce accommodative spasm which are frequently seen with miotic agents. The blurred vision and night blindness often associated with standard miotic therapy are not associated with Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25%. Thus patients with central lenticular opacities avoid the visual impairment caused by a constricted pupil.
In clinical pharmacology studies, ophthalmic betaxolol has minimal effect on pulmonary and cardiovascular parameters.
Ophthalmic betaxolol hydrochloride solution at 1% (1 drop in each eye) was compared to placebo in a three way masked crossover study challenging nine patients with reactive airway disease1. Betaxolol hydrochloride has no significant effect on pulmonary function as measured by forced expiratory volume in one second (FEV1), forced vital capacity (FVC) and FEV1/FVC. Additionally, the action of isoprenaline, a beta-stimulant, administered at the end of the study was not inhibited by ophthalmic betaxolol hydrochloride. In contrast, ophthalmic timolol significantly decreased these pulmonary functions (see Table 1).
No evidence of cardiovascular beta-adrenergic blockade during exercise was observed with betaxolol in a double masked crossover study in 24 normal subjects comparing ophthalmic betaxolol hydrochloride solution 1.0% and placebo for effects on blood pressure and heart rate2. Mean arterial blood pressure was not affected by any treatment; however, ophthalmic timolol produced a significant decrease in the mean heart rate (see Table 2).

Clinical Trials

In controlled, doubled masked studies, the magnitude and duration of the ocular hypotensive effect of Betoptic Eye Drops 0.5% and Betoptic S Eye Drops 0.25% were clinically equivalent. Betoptic S Eye Drops 0.25% were significantly more comfortable than Betoptic Eye Drops 0.5%.
Clinical studies show that topical betaxolol reduces mean intraocular pressure 25% from baseline. In trials using 22 mmHg as a generally accepted index of intraocular pressure control, betaxolol hydrochloride solution was effective in more than 94% of the population studied, of which 73% were treated with the beta-blocker alone. In controlled double masked studies, the magnitude and duration of the ocular hypotensive effect of Betoptic Eye Drops 0.5% and ophthalmic timolol were clinically equivalent.
Clinical observation of glaucoma patients treated with betaxolol hydrochloride ophthalmic solution for up to three years shows that the intraocular pressure lowering effect is well maintained.
Ophthalmic betaxolol hydrochloride has also been used successfully in glaucoma patients who have undergone a laser trabeculoplasty and have needed additional long-term ocular hypotensive therapy. Ophthalmic betaxolol hydrochloride has been well tolerated in glaucoma patients wearing hard or soft contact lenses (see Dosage and Administration, Contact lenses) and in aphakic patients.

Indications

Betoptic Eye Drops 0.5% and Betoptic S Eye Drops 0.25% have been shown to be effective in lowering intraocular pressure and are indicated in the treatment of ocular hypertension or chronic open angle glaucoma. Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% may be used alone or in combination with other IOP lowering medication.

Contraindications

Hypersensitivity to any component of the product.
Betaxolol hydrochloride is contraindicated in patients with sinus bradycardia greater than a first degree block, cardiogenic shock, or patients with a history of overt cardiac failure.

Precautions

For ocular use only.

General.

Topically applied beta-adrenergic blocking agents may be absorbed systemically. The same types of cardiovascular and pulmonary and other adverse reactions found with systemic administration of these agents may occur with topical administration. For example, severe respiratory reactions, including death due to exacerbation of bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported with ophthalmic application of beta-adrenergic blocking agents.
While ophthalmic betaxolol hydrochloride has been shown to have a minor effect on heart rate and blood pressure in clinical studies, caution should be used in treating patients with a history of cardiac failure or heart block. When beginning therapy with betaxolol patients with a history of severe cardiac disease should be monitored closely for signs of cardiac failure. Treatment with ophthalmic betaxolol hydrochloride should be discontinued at the first sign of cardiac failure.
Because of potential effects of beta-blockers on blood pressure and pulse (e.g. hypotension, bradycardia), use with caution in patients with cerebrovascular insufficiency, untreated phaeochromocytoma or metabolic acidosis, since beta-adrenergic blocking agents can adversely affect such diseases. If signs or symptoms suggesting reduced cerebral blood flow develop, consider alternative therapy.
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.

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.

Pulmonary.

Caution should be exercised in the treatment of glaucoma patients with excessive restriction of pulmonary function. Exacerbation of asthma and bronchospasm have been reported in patients receiving betaxolol treatment. Although rechallenges of some such patients with ophthalmic betaxolol hydrochloride have not adversely affected pulmonary function test results, the possibility of adverse pulmonary effects in patients sensitive to beta-adrenergic blockers cannot be ruled out.

Diabetes mellitus.

While ophthalmic betaxolol hydrochloride has demonstrated a low potential for systemic effects, beta-adrenergic blocking agents should be used with caution in patients subject to spontaneous hypoglycaemia, or in diabetic patients (especially those with labile diabetes) receiving insulin or oral hypoglycaemic agents. Beta-adrenergic blocking agents may mask the signs and symptoms of acute hypoglycaemia.

Major surgery.

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

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.

Muscle weakness.

Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g. diplopia, ptosis and generalised weakness).

Ocular.

In patients with angle closure glaucoma, the immediate treatment objective is to reopen the angle by constriction of the pupil with a miotic agent. Betaxolol has little or no effect on the pupil, therefore Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% should be used with a miotic to reduce elevated intraocular pressure in angle closure glaucoma.
As with other antiglaucoma drugs, diminished responsiveness to ophthalmic betaxolol hydrochloride after prolonged therapy has been reported in some patients. However, in one long-term study in which 250 patients have been followed for up to three years, no significant difference in mean intraocular pressure has been observed after initial stabilisation.

Contact lenses.

Betaxolol eye drops contain benzalkonium chloride which may cause irritation and is known to discolour soft contact lenses. Avoid contact with soft contact lenses.
Patients must be instructed to remove contact lenses prior to application of eye drops containing betaxolol and wait at least 15 minutes before reinsertion.

Thyrotoxicosis.

Beta-adrenergic blocking agents may mask certain clinical signs of hyperthyroidism, e.g. tachycardia. Patients having or suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of these agents which might precipitate a thyroid storm.

Use in pregnancy.

(Category C)
There have been no adequate and well controlled studies in pregnant women. Studies in animals have shown reproductive toxicity. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly indicated. Betaxolol is not recommended during pregnancy.
Epidemiological studies show a risk for intrauterine 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.
Beta-adrenergic receptor blocking agents may cause bradycardia in the foetus and newborn infant. During the final part of pregnancy and parturition these drugs should therefore only be given after weighing the needs of the mother against the risk to the fetus. If betaxolol eye drops is administered until delivery, the neonate should be carefully monitored during the first days of life.

Use in lactation.

It is not known whether ophthalmic betaxolol hydrochloride is excreted in human milk following topical ocular administration. However, a risk to the suckling child cannot be excluded. Betaxolol concentrations in milk following oral administration may be up to three times those in maternal blood, having the potential to cause serious undesirable effects in the infant of the nursing mother. While it is unlikely that clinically important doses of the drug would be absorbed by breastfed infants during ophthalmic use in women, caution should be exercised when ophthalmic betaxolol hydrochloride is prescribed for breastfeeding women.
A decision must be made whether to discontinue breastfeeding or to discontinue/ abstain from betaxolol therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.

Paediatric use.

Clinical studies to establish the safety and efficacy in children have not been performed.

Animal studies.

Ocular anaesthesia has been observed in rabbit studies.

Carcinogenesis, mutagenesis, impairment of fertility.

There are no data on the effects of betaxolol eye drops on human fertility.
Lifetime studies with betaxolol hydrochloride have been completed in mice at oral doses of 6, 20 or 60 mg/kg/day and in rats at 3, 12 or 48 mg/kg/day; betaxolol hydrochloride demonstrated no carcinogenic effect. In a variety of in vitro and in vivo bacterial and mammalian cell assays, betaxolol hydrochloride was nonmutagenic.

Risk from anaphylactic reaction.

While taking beta blockers, patients with a history of atopy or severe anaphylactic reaction to a variety of allergens may be more reactive to repeated accidental, diagnostic or therapeutic challenge with such allergens. Such patients may be unresponsive to the usual doses of adrenaline used to treat anaphylactic reactions.
Caution should be used where a beta 2 agonist is administered concurrently with a beta blocker.
When used in conjunction with topical miotics and/or systemically administered carbonic anhydrase inhibitors, the effect of betaxolol eye drops in lowering IOP may be additive.
Ophthalmic beta-blockers and Phenothiazone compounds may have potential additive hypotensive effects due to mutual inhibition of metabolism.

Effects on ability to drive and use machines.

As with any eye drop, temporary blurred vision or other visual disturbances may affect the ability to drive or use machines.
If blurred vision occurs at instillation, the patient must wait until the vision clears before driving or using machinery.

Interactions

The potential exists for additive systemic and/or intraocular beta blockade effects either on the intraocular pressure or on the known systemic effects of beta blockade for patients receiving a beta-adrenergic receptor blocking agent orally and ophthalmically or with oral calcium channel blockers, antiarrhythmics (including amiodarone) or digitalis glycosides. Neither Betoptic Eye Drops 0.5% nor Betoptic S Eye Drops 0.25% should be used in conjunction with other topical beta-blocking agents. Coadministration of ophthalmic beta-blockers with digitalis may have additive effects in prolonging atrioventricular conduction time.
Although betaxolol hydrochloride used alone has little or no effect on pupil size, mydriasis resulting from concomitant therapy with betaxolol hydrochloride 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 which may result in vertigo, syncope, or postural hypotension. Caution should be exercised in patients using concomitant adrenergic psychotropic drugs.

Adverse Effects

Ocular.

In clinical trials the most frequent event associated with the use of ophthalmic betaxolol hydrochloride has been transient ocular discomfort. The incidence of discomfort was 16% in patients treated with Betoptic S and 25% in patients treated with Betoptic 0.5%. Decreased corneal sensitivity, erythema, itching sensation, corneal punctate keratitis, anisocoria, blurred vision, foreign body sensation, tearing, dryness of eyes, inflammation, discharge, ocular pain, decreased visual acuity, crusty lashes and photophobia have been reported in up to 4% of patients.

Systemic.

Systemic reactions following topical administration of Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% have been reported rarely and include the following.

Cardiovascular.

Bradycardia, heart block and congestive failure.

Pulmonary.

Pulmonary distress characterised by dyspnoea, bronchospasm, thickened bronchial secretions, asthma and respiratory failure.

Central nervous system.

Insomnia, dizziness, vertigo, headaches, depression, lethargy and an increase in the signs and symptoms of myasthenia gravis.

Other.

Hives, toxic epidermal necrolysis, hair loss, glossitis.

Postmarketing experience.

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. These may include bradycardia, a slowed AV (atrioventricular) conduction or increase of an existing AV block, hypotension, heart failure, cold and cyanotic extremities, Raynaud's phenomenon, paraesthesia of the extremities, increase of an existing intermittent claudication, fatigue, headaches, impaired vision, hallucinations, psychoses, confusion, impotence, dizziness, sleep disturbances, depression, nightmares, gastrointestinal 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.
The following adverse reactions are classified according to the following convention: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), or not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness. The adverse reactions were obtained from clinical trials and postmarketing spontaneous reports.

Eye disorders.

Very common (≥ 10%): ocular discomfort.
Common (≥ 1% to < 10%): vision blurred, lacrimation increased, foreign body sensation in eyes.
Uncommon (≥ 0.1% to < 1%): punctate keratitis, keratitis, conjunctivitis, blepharitis, visual acuity reduced, visual impairment, photophobia, eye pain, dry eye, asthenopia, blepharospasm, abnormal sensation in eye, eye pruritus, eye discharge, eyelid margin crusting, eye inflammation, eye irritation, conjunctival disorder, conjunctival oedema, ocular hyperaemia.
Rare (≥ 0.01% to < 0.1%): cataract, refraction disorder, eye disorder.
Not known: erythema of eyelid.

Cardiac disorders.

Uncommon (≥ 0.1% to < 1%): bradycardia, tachycardia.
Not known: arrhythmia.

Vascular disorders.

Rare (≥ 0.01% to < 0.1%): hypotension.

Nervous system disorders.

Common (≥ 1% to < 10%): headache.
Rare (≥ 0.01% to < 0.1%): syncope.
Not known: dizziness.

Psychiatric disorders.

Rare (≥ 0.01% to < 0.1%): anxiety.
Not known: insomnia, depression.

Immune system disorders.

Not known: hypersensitivity.

Respiratory, thoracic and mediastinal disorders.

Uncommon (≥ 0.1% to < 1%): asthma, dyspnoea, respiratory disorder, rhinitis.
Rare (≥ 0.01% to < 0.1%): cough, rhinorrhoea.

Gastrointestinal disorders.

Uncommon (≥ 0.1% to < 1%): nausea.
Rare (≥ 0.01% to < 0.1%): dysgeusia.

Skin and subcutaneous tissue disorders.

Rare (≥ 0.01% to < 0.1%): dermatitis, rash.
Not known: periorbital oedema, alopecia.

Infections and infestations.

Rare (≥ 0.01% to < 0.1%): influenza, infection, bronchitis, sinusitis.

Reproductive system and breast disorders.

Rare (≥ 0.01% to < 0.1%): libido decreased.

Surgical and medical procedures.

Rare (≥ 0.01% to < 0.1%): antral lavage.

General disorders and administration site conditions.

Not known: asthenia.

Dosage and Administration

Note.

Shake Betoptic S Eye Drops 0.25% well before use.
The usual dose is one drop of Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% in the affected eye(s) twice daily. In some patients, the intraocular pressure lowering response to Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% may require a few weeks to stabilise. Clinical follow up should include a determination of the intraocular pressure during the first month of treatment with Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25%. Thereafter, intraocular pressure should be determined on an individual basis at the judgement of the physician.
Because of diurnal variations of intraocular pressure in individual patients, satisfactory response to twice a day therapy is best determined by measuring intraocular pressure at different times during the day. Intraocular pressure ≤ 22 mmHg may not be optimal for control of glaucoma in each patient; therefore, therapy should be individualised.
If the intraocular pressure of the patient is not adequately controlled on this regimen, concomitant therapy with pilocarpine, other miotics, adrenaline or systemically administered carbonic anhydrase inhibitors can be instituted.
When a patient is transferred from several concomitantly administered antiglaucoma agents, individual adjustment is required. Adjustment should involve one agent at a time made at intervals of not less than one week. A recommended approach is to continue the agents being used and add one drop of Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% in the affected eye(s) twice a day. On the following day, discontinue one of the other antiglaucoma agents. The remaining antiglaucoma agents may be decreased or discontinued according to the patient's response to treatment. The physician may be able to discontinue some or all of the other antiglaucoma agents.
In order to minimise systemic absorption, apply pressure to the tear duct for two minutes immediately after administration.

Contact lenses.

Neither Betoptic Eye Drops 0.5% nor Betoptic S Eye Drops 0.25% should be instilled while the patient is wearing contact lenses.
If patients continue to wear soft (hydrophilic) contact lenses while under treatment with Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25%, they should remove their lens(es) prior to instilling the drops in the affected eye(s). Lens(es) should not be inserted into the eye(s) until 15 minutes after instillation of the drops.

Overdosage

No information is available on overdosage of humans. The oral LD50 of the drug ranged from 350 to 920 mg/kg in mice and 860 to 1,050 mg/kg in rats. The symptoms which might be expected with an overdose of a systemically administered beta-1-adrenergic receptor blocking agent are bradycardia, hypotension and acute cardiac failure.
A topical overdose of Betoptic Eye Drops 0.5% or Betoptic S Eye Drops 0.25% may be flushed from the eye(s) with warm water or normal saline (sodium chloride solution 0.9%). If accidentally ingested, efforts to decrease further absorption may be appropriate (gastric lavage). The most common signs and symptoms of overdosage from systemic beta-blockers are bradycardia, hypotension, bronchospasm, and acute cardiac failure. If these occur, discontinue therapy and initiate appropriate supportive therapy.
Contact the Poisons Information Centre on 131 126 for advice on management.

Presentation

Betoptic Eye Drops 0.5%: 5 mL (Drop-Tainer).
Betoptic S Eye Drops 0.25%: 5 mL (Drop-Tainer).

Storage

Store below 25°C.
Store the bottle in the outer carton.
Discard container four weeks after opening.
Consumer product information is supplied with these products.

References

1. Schoene RB et al., Am J Ophthal, 97, 86-92, 1984.
2. Atkins JM et al., Am J Ophthal, 99, 173-175, 1985.

Poison Schedule

S4.