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BETAXOLOL 0.5% EYE DROPS

Active substance(s): BETAXOLOL / BETAXOLOL HYDROCHLORIDE / BETAXOLOL / BETAXOLOL HYDROCHLORIDE / BETAXOLOL / BETAXOLOL HYDROCHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Betaxolol 0.5% Eye Drops

2

3.

QUALITATIVE AND QUANTITATIVE COMPOSITION
Active Ingredient
Betaxolol
5.0 mg/ml
(as Betaxolol hydrochloride
5.6 mg/ml)
Excipient(s) with known effect
Benzalkonium chloride 0.01%w/v
For a full list of excipients, see section 6.1
PHARMACEUTICAL FORM
Eye drops, solution.

4.

CLINICAL PARTICULARS

4.1.

Therapeutic Indications
Reduction of elevated intraocular pressure in conditions such as ocular
hypertension and chronic open-angle glaucoma.

4.2

Posology and method of administration
Adults (including the elderly): recommended therapy is one drop of Betaxolol
0.5% Eye Drops to be instilled into the affected eye(s) twice a day.
Children: No clinical studies have been performed to establish safety and
efficacy in children. Therefore, this product is currently 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.
Intraocular pressure should be reassessed approximately four weeks after
starting treatment because response to Betaxolol 0.5% Eye Drops may take a
few weeks to stabilise.
If necessary, concomitant treatment with miotics, adrenaline and/or carbonic
anhydrase inhibitors can be instituted. In order to prevent the active
substance(s) from being washed out when additional ophthalmic medication is

used, an interval of at least 10 minutes between each application is
recommended. The use of two topical beta-adrenergic agents is not
recommended.
Transfer from a single antiglaucoma agent: Continue the agent and add one
drop of Betaxolol 0.5% Eye Drops in each affected eye twice daily. On the
following day, discontinue the previous agent completely, and continue with
Betaxolol 0.5% Eye Drops.
When several antiglaucoma agents are being used, the patient should be
assessed on an individual basis. Adjustment should involve one agent at a
time at intervals of not less than one week.
Patients should be instructed to remove soft contact lenses before using
betaxolol.
4.3

Contraindications
Betaxolol 0.5% Eye Drops are contraindicated in patients with:
Sinus bradycardia, sick sinus syndrome, sino-atrial block;
Cardiogenic shock;
Overt cardiac failure;
Second or third degree AV block not controlled with pace-maker.;
Hypersensitivity to the active substance (betaxolol), to any of the
excipients listed in section 6. or other beta-blocking agents.
-

4.4

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

Special warnings and precautions for use
For ocular use only
General:
Like other topically applied ophthalmic drugs, betaxolol is absorbed
systemically. Due to 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 4.2.
Cardiac disorders:
In patients with cardiovascular diseases (e.g. coronary heart disease,
Prinzmetal's angina and cardiac failure) and hypotension therapy with betablockers 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 betablockers.
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 betablockers may mask the signs and symptoms of acute hypoglycaemia. While
Betaxolol has demonstrated a low potential for systemic effects, it should be
used with caution in patients suspected of developing thyrotoxicosis.
Hyperthyroidism:
Beta-blockers may also mask the signs of hyperthyroidism.
Muscle weakness:
Beta adrenergic blocking agents have been reported to potentiate muscle
weakness consistent with certain myasthenic symptoms (eg. diplopia, ptosis
and generalised weakness).
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, Betaxolol should be used with a miotic to
reduce elevated intraocular pressure in angle-closure glaucoma.
Ophthalmic β-blockers may induce dryness of eyes. Patients with corneal
diseases, Sicca Syndrome or similar tear film abnormalities should be treated
with caution.
Other beta-blocking agents:
The effect on intra-ocular pressure or the known effects of systemic betablockade 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 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:
β-blocking ophthalmological preparations may block systemic β-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.
Contact lenses:
This formulation of Betaxolol 0.5% Eye Drops contains benzalkonium
chloride as a preservative which may be deposited in soft contact lenses.
Hence, Betaxolol 0.5% Eye Drops should not be used while wearing these
lenses. The lenses should be removed before instillation of the drops and not
reinserted earlier than 15 minutes after use.
Patients should be instructed to avoid allowing the tip of the dispensing
container to contact the eye or surrounding structures.
Patients should also be instructed that ocular solutions, if handled improperly
can become contaminated by common bacteria known to cause ocular
infections. Serious damage to the eye and subsequent loss of vision may result
from using.
Patients should also be advised that if they develop any intercurrent ocular
condition (e.g. trauma, ocular surgery or infection), they should immediately
seek their physician's advice concerning the continued use of present multidose container.
There have been reports of bacterial keratitis associated with the use of topical
ophthalmic products.
4.5

4.6

Interaction with other medicinal products and other forms of interaction
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, antiarrhythmics (including amiodarone), digitalis glycosides,
parasympathomimetics and guanethidine. Close observation of the patient is
recommended.
Betablockers can decrease the response to adrenaline use to treat anaphylactic
reactions. Special caution should be exercised in patients with a history of
atophy or anaphylaxis.
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.
If more than one topical ophthalmic medicinal product is being used, the
medicines must be administered at least 5 minutes apart. Eye ointments should
be administered last.
Fertility, pregnancy and lactation
Fertility

There are no data on the effects of Betaxolol eye drops on human fertility.
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 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 Betaxolol Eye Drops is administered until delivery, the neonate
should be carefully monitored during the first days of life.
Lactation

4.7

Beta-blockers are excreted in breast milk, having the potential to cause serious
undesirable effects in the infant of nursing mother. 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 the systemic absorption, see 4.2.
Effects on ability to drive and use machines
Betaxolol eye drops, solution has no or negligible influence on the ability to
drive and use machines
Temporary blurred vision or other visual disturbances may affect the ability to
drive or use machines. If blurred vision occurs after instillation, the patient
must wait until the vision clears before driving or using machinery.

4.8

Undesirable effects
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 betablockers.
Summary of the safety profile
In clinical trials with Betaxolol eye drops the most common adverse reaction
was ocular discomfort, occurring in 12.0% of patients.

The following undesirable effects have been observed and reported with the
following frequencies: Very common (≥1/10); common (≥1/100 to <1/10);
uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000) and very rare
(<1/10000), not known (cannot be estimated from the available data).
Within each frequency-grouping, adverse reaction are presented in order of
decreasing seriousness.
System Organ Classification
MedDRA Preferred Term
Immune system disorders
Frequency unknown: hypersensitivity
Psychiatric disorders
Rare: anxiety, insomnia, depression
Nervous system disorders
Common: headache
Rare: syncope

Eye disorders

Frequency unknown: dizziness
Very common: ocular discomfort
Common: vision blurred, lacrimation
increased
Uncommon:
punctate
keratitis,
keratitis, conjunctivitis, blepharitis,
visual impairment, photophobia, eye
pain,
dry
eye,
asthenopia,
blepharospasm, eye pruritus, eye
discharge, eyelid margin crusting, eye
inflammation,
eye
irritation,
conjunctival disorder, conjunctival
oedema, ocular hyperaemia

Cardiac disorders

Rare: Cataract, decreased corneal
sensitivity, erythema of eyelid
Uncommon: bradycardia, tachycardia

Frequency unknown: arrhythmia
Vascular disorders
Rare: hypotension
Respiratory, thoracic and mediastinal Uncommon:
asthma,
dyspnoea,
Disorders
rhinitis

Gastrointestinal disorders

Rare: cough, rhinorrhea
Uncommon: nausea

Rare: dysgeusia
Skin and subcutaneous tissue Rare: dermatitis, rash, alopecia
disorders
Reproductive system and breast Rare: libido decreased
disorders
General disorders and administration Frequency unknown: asthenia
site
Conditions

Description of selected adverse reactions
Additional adverse reactions have been seen with ophthalmic beta-blockers
and may potentially occur with Betaxolol eye drops solution:
System Organ Classification
MedDRA Preferred Term
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:
Frequency unknown: nightmares,
memory loss, hallucinations,
psychoses, confusion.
Nervous system disorders:
Frequency unknown: cerebrovascular
accident, cerebral ischemia, increases
in signs and symptoms of myasthenia
gravis, paraesthesia
Eye disorders:
Frequency unknown: choroidal
detachment
following
filtration
surgery
(see 4.4 Special warnings and special
precautions for use), corneal erosion,
ptosis, diplopia
Cardiac disorders:
Frequency unknown: Chest pain,
palpitations, oedema, congestive heart
failure, atrioventricular block, cardiac
arrest, cardiac failure. A slowed AVconduction or increase of an existing
AV-block
Vascular disorders:
Frequency
unknown:
Raynaud's
phenomenon, cold and cyanotic hands
and feet, Increase of an existing
intermittent claudication.
Respiratory,
thoracic,
mediastinal disorders:

and Frequency unknown: Bronchospasm
(predominantly in patients with preexisting bronchspastic disease)

Gastrointestinal disorders:

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

Skin and
disorders:

subcutaneous

tissue Frequency unknown: Psoriasiform
rash or exacerbation of psoriasis

Musculoskeletal and connective
tissue disorders:
Reproductive system and breast
disorders:
General
disorders
and

Frequency unknown: Myalgia.
Frequency
unknown:
Sexual
dysfunction, impotence.
Frequency unknown: fatigue.

administration site conditions:
An increase in Anti Nuclear Antibodies (ANA) has been seen; its clinical
relevance is unclear.
Reporting of suspected adverse reactions:
Reporting suspected adverse reactions after authorisation of the medicinal
product is important. It allows continued monitoring of the benefit/risk balance
of the medicinal product. Healthcare professionals are asked to report any
suspected adverse reactions via Yellow card scheme at
www.mhra.gov.uk/yellowcard.
4.9

Overdose
In case of accidental ingestion, symptoms of overdose from betablockade may
include bradycardia, hypotension, cardiac failure and bronchospasm.
If overdose with Betaxolol eye drops occurs, treatment should be symptomatic
and supportive.

5.1

A topical overdose of Betaxolol eye drops may be flushed from the eye(s) with
warm tap water.
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
Benzalkonium chloride
Disodium edetate
Sodium chloride
Water for injection

6.2

Incompatibilities
Not known .

6.3.

Shelf Life
Unopened: 24 months
Opened:
28 days

6.4.

Special Precautions for Storage
Do not store above 30oC
To avoid contamination do not touch dropper tip to any surface

6.5.

Nature and Contents of Container
The container is a 5ml bottle of low density polyethylene (LDPE) with a
polystyrene spiked cap closure which contains Betaxolol 0.5% Eye Drops
solution.

6.6.

Instruction for Use/Handling and Disposal
No special instructions.

7

MARKETING AUTHORISATION HOLDER
FDC International Ltd
Unit 6 Fulcrum 1,
Solent Way,
Whiteley,
Fareham,
Hampshire
PO15 7FE
UK

8.

MARKETING AUTHORISATION NUMBER
PL 15872/0007

9.
DATE OF FIRST AUTHORISATION/RENEWAL OF
AUTHORISATION
29 July 2005

10

DATE OF REVISION OF THE TEXT
07/03/2017

Expand Transcript

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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