Betoptic 0.5% w/v eye drops, solution
Betaxolol 0.5% w/v (as hydrochloride).
Excipients with known effect: 1ml of solution contains 0.1mg benzalkonium chloride.
For a full list of excipients see Section 6.1
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.
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.
After the cap is removed, if the tamper-evident snap collar is loose, remove before using a product.
• Hypersensitivity to the active substance or to any of the excipients listed in section 6.
• 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.
For ocular use only.
General: 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 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 (e.g. 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, 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 intraocular 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 anesthesiologist 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: 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 Betaxolol Eye Drops and wait at least 15 minutes before reinsertion.
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 and guanethidine. Close observation of the patient is recommended.
Beta-blockers can decrease the response to adrenaline used to treat anaphylactic reactions. Special caution should be exercised in patients with a history of atrophy or anaphylaxis.
Caution should be exercised in patients using concomitant adrenergic psychotropic drugs.
Mydriasis resulting from the 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.
There are no data on the effects of Betaxolol Eye Drops on human fertility.
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 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. If BETOPTIC SOLUTION is administered until delivery, the neonate should be carefully monitored during the first days of life.
Beta-blockers are excreted in breast milk, having the potential to cause serious undesirable effects in the infant of the 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 systemic absorption, see section 4.2.
Betoptic 0.5% eye drops, the 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.
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.
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 adverse reactions have been reported during clinical trials or post-marketing surveillance with Betaxolol eye drops and are classified according to the subsequent 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) and frequency unknown/cannot be estimated from the available data.
Within each frequency-grouping, adverse reactions are presented in order of decreasing seriousness.
|System Organ Classification||MedDRA Preferred Term (V 13.0)|
|Inmmune system disorders||Frequency unknown: hypersensitivity|
|Psychiatric disorders||Rare: anxiety, insomnia, depression|
|Nervous system disorders||Common: headache
Frequency unknown: dizziness
|Eye disorders||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
Rare: Cataract, decreased corneal sensitivity, erythema of the eyelid
|Cardiac disorders||Uncommon: bradycardia, tachycardia
Frequency unknown: arrhythmia
|Vascular disorders||Rare: hypotension|
|Respiratory, thoracic and mediastinal disorders||Uncommon: asthma, dyspnoea, rhinitis,
Rare: cough, rhinorrhea
|Gastrointestinal disorders||Uncommon: nausea
|Skin and subcutaneous tissue disorders||Rare: dermatitis, rash, alopecia|
|Reproductive system and breast disorders||Rare: libido decreased|
|General disorders and administration site conditions||Frequency unknown: asthenia|
Description of selected adverse reactions
Additional adverse reactions have been seen with ophthalmic beta-blockers and may potentially occur with BETOPTIC SOLUTION:
|System Organ Classification||MedDRA Preferred Term (V13.0)|
|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 AV-conduction or increase of an existing AV-block|
|Vascular disorders:||Frequency unknown: Raynaud’s phenomenon, cold and cyanotic hands and feet, Increase of existing intermittent claudication.|
|Respiratory, thoracic, and mediastinal disorders:||Frequency unknown: Bronchospasm (predominantly in patients with pre-existing bronchspastic disease)|
|Gastrointestinal disorders:||Frequency unknown: dyspepsia, diarrhoea, dry mouth, abdominal pain, vomiting.|
|Skin and subcutaneous tissue disorders:||Frequency unknown: Psoriasiform rash or exacerbation of psoriasis|
|Musculoskeletal and connective tissue disorders:||Frequency unknown: Myalgia.|
|Reproductive system and breast disorders:||Frequency unknown: Sexual dysfunction, impotence.|
|General disorders and administration site conditions:||Frequency unknown: fatigue.|
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 the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
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.
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.
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.