1. Name Of The Medicinal Product
Betagan Unit Dose
2. Qualitative And Quantitative Composition
One ml solution contains 5.0 mg levobunolol hydrochloride, equivalent to 4.4 mg levobunolol.
For a full list of excipients, see section 6.1.
3. Pharmaceutical Form
Eye Drops, solution.
A clear, colourless to brown solution.
4. Clinical Particulars
4.1 Therapeutic Indications
Reduction of intraocular pressure in chronic open-angle glaucoma and ocular hypertension.
4.2 Posology And Method Of Administration
Adults (including the elderly)
The recommended adult dose is one drop of Betagan once or twice daily in the affected eye(s). Discard product after use.
Children
Betagan is not recommended for use in children due to lack of safety and efficacy data.
Method of administration: topical into the conjunctival sac.
Concurrent therapy may be used where necessary.
As with any eye drops, to reduce possible systemic absorption, it is recommended that the lachrymal sac be compressed at the medial canthus (punctual occlusion) for one minute. This should be performed immediately following the instillation of each drop.
4.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Bronchial asthma (or a history of bronchial asthma) or chronic obstructive pulmonary disease
Uncontrolled cardiac failure.
History of sinus bradycardia, second and third degree atrioventricular block, overt cardiac failure or cardiogenic shock.
4.4 Special Warnings And Precautions For Use
As with other topically applied ophthalmic drugs, Betagan may be absorbed systemically and adverse reactions typical of oral beta-adrenoceptor agents may occur.
Respiratory and cardiac reactions have been reported including, rarely, death due to bronchospasm or associated with cardiac failure.
Congestive heart failure should be adequately controlled before beginning therapy with Betagan. In patients with a history of cardiac disease, pulse rates should be monitored.
Beta-blockers may mask the symptoms of thyrotoxicosis. Because these agents may block the systemic effects of hypoglycaemia they should be used with caution in diabetic patients who use insulin or oral hypoglycaemic drugs. Diabetic control should be monitored during Betagan therapy in patients with labile diabetes.
Stevens-Johnson syndrome has been reported following the use of levobunolol; however a causal relationship has not been established.
Beta-blockers have been associated with alopecia. Alopecia has been shown to be reversible upon levobunolol withdrawal.
Betagan has little or no effect on pupil size and if administered in angle-closure glaucoma, for reduction of intraocular pressure, must only be given in combination with a miotic.
Diminished response after prolonged therapy has been reported in some patients. If necessary, concomitant therapy can be instituted. In patients with peripheral circulatory disorders (Raynaud's disease or syndrome, intermittent claudication), beta-blockers should be used with great caution as aggravation of these disorders may occur.
Beta-blockers may induce bradycardia. If the pulse rate decreases to less than 50-55 beats per minute at rest and the patient experiences symptoms related to the bradycardia, review of intraocular pressure lowering therapy may be required.
Due to its negative effect on conduction time, beta-blockers should only be given with caution to patients with first degree heart block.
Beta-blockers may increase both the sensitivity towards allergens and the seriousness of anaphylactic reactions.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Betagan may have additive effects in patients taking systemic antihypertensive drugs. These possible additive effects may include hypotension, including orthostatic hypotension, bradycardia, dizziness, and/ or syncope. Conversely, systemic beta-adrenoceptor blocking agents may potentiate the ocular hypotensive effect of Betagan.
4.6 Pregnancy And Lactation
For levobunolol hydrochloride no clinical data on exposed pregnancies are available.
Betagan should not be used during pregnancy unless clearly necessary.
If treatment with levobunolol hydrochloride during lactation is considered necessary for the benefit of the mother, consideration should be given to the cessation of breast feeding.
4.7 Effects On Ability To Drive And Use Machines
Betagan may cause dizziness, fatigue and/or drowsiness, which may impair the ability to drive or operate machinery.
Betagan may cause blurred and/or abnormal vision, which may also impair the ability to drive or to use machinery, especially at night or in reduced lighting. The patient should wait until these symptoms have cleared before driving or using machinery.
4.8 Undesirable Effects
Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness. The following terminologies have been used in order to classify the occurrence of undesirable effects: Very Common (
Immune System Disorders
Not known: Hypersensitivity
Psychiatric Disorders
Not known: Depression
Nervous System Disorders
Not known: Ataxia, Confusion, Dizziness, Lethargy, Headache, Hallucinations, Impotence, Sleep disorder, Paraesthesia
Eye Disorders
Very Common: Eye irritation, Conjunctival irritation
Common: Blepharitis, Conjunctivitis
Not known: Dry eye, Corneal reflex decreased, Iridocyclitis, Keratitis, Visual disturbance, Eye/Eyelids pruritus, Eye/Eyelid oedema, Eye discharge, Lacrimation increased
Cardiac Disorders
Not known: Syncope, Bradycardia, Atrioventricular block, Palpitations
Vascular Disorders
Not known: Hypotension
Respiratory, Thoracic, and Mediastinal Disorders
Not known: Asthma, Dyspnoea, Throat irritation, Nasal discomfort
Gastrointestinal Disorders
Not known: Nausea, Vomiting, Diarrhoea, Eructation
Hepato-biliary Disorders
Not known: Elevated liver enzymes
Skin and Subcutaneous Tissue Disorders
Not known: Urticaria, Dermatitis, Rash, Erythema, Skin exfoliation, Lichenoid keratosis, Pruritus
General Disorders and Administration Site Conditions
Not known: Face oedema, Asthenia
The following additional adverse reactions have been reported with ophthalmic use of beta1 and beta2 (non selective) blocking agents:
Eye disorders: including refractory changes, diplopia and ptosis
Cardiovascular: cerebrovascular accident, cerebral ischaemia, congestive heart failure, cardiac arrest
Respiratory: bronchospasm, respiratory failure
4.9 Overdose
There are no data available on human overdosage with Betagan which is unlikely to occur via the ocular route. Should accidental ocular overdosage occur, flush the eye(s) with water or normal saline. If accidentally ingested, systemic symptoms may result and efforts to decrease further absorption may be appropriate. The symptoms associated with systemic overdosage are most likely to be bradycardia, hypotension, bronchospasm and cardiac failure. Therapy for overdosage of a beta-adrenergic agent should be instituted, such as intravenous administration of atropine sulphate 0.25 to 2 mg to induce vagal blockade. Conventional therapy for hypotension, bronchospasm, heart block and cardiac failure may be necessary.
5. Pharmacological Properties
Pharmacotherapeutic group: Beta blocking agents
ATC code: S01ED 03
5.1 Pharmacodynamic Properties
Levobunolol is a non-cardioselective beta-adrenoceptor blocking agent, equipotent at both beta1 and beta2 receptors. Levobunolol is greater than 60 times more potent than its dextro isomer in its beta-blocking activity. In order to obtain the highest degree of beta-blocking potential without increasing the potential for direct myocardial depression, the levo isomer, levobunolol, is used. Levobunolol does not have significant local anaesthetic (membrane-stabilising) or intrinsic sympathomimetic activity. Betagan has shown to be as effective as Timolol in lowering intraocular pressure.
Betagan when instilled in the eye will lower elevated intraocular pressure as well as normal intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure presents a major risk factor in the pathogenesis of glaucomatous field loss. The higher the level of intraocular pressure, the likelihood of optic nerve damage and visual field loss.
The primary mechanism of action of levobunolol in reducing intraocular pressure is most likely a decrease in aqueous humor production. Betagan reduces intraocular pressure with little or no effect on pupil size in contrast to the miosis which cholinergic agents are known to produce.
The blurred vision and night blindness often associated with miotics would not be expected with the use of Betagan. Patients with cataracts avoid the inability to see around lenticular opacities caused by pupil constriction.
5.2 Pharmacokinetic Properties
The onset of action with one drop of Betagan can be detected within one hour after instillation, with maximum effect seen between two and six hours. A significant decrease can be maintained for up to 24 hours following a single dose.
5.3 Preclinical Safety Data
Not applicable.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Poly(vinyl alcohol)
Sodium chloride
Disodium edetate
Sodium phosphate dibasic, heptahydrate
Potassium phosphate monobasic
Sodium hydroxide (to adjust pH) or hydrochloric acid (to adjust pH)
Purified water
6.2 Incompatibilities
No major incompatibilities have been reported from topical use of levobunolol.
6.3 Shelf Life
24 months.
The eye drop solution should be used immediately after opening. Any unused solution should be discarded.
6.4 Special Precautions For Storage
Do not store above 25°C.
Keep the container in the outer carton in order to protect from light.
6.5 Nature And Contents Of Container
Low density polyethylene (LDPE) blow-fill-seal unit dose container (0.9 ml volume) filled with 0.4 ml solution.
Unit dose containers are packaged into a foil covered pouch (5 containers per pouch).
Pouches are packaged into cartons such that each carton contains 30 or 60 unit dose containers.
6.6 Special Precautions For Disposal And Other Handling
Ensure that the single dose container is intact before use. Discard any unused solution (i.e. once opened do not re-use container for subsequent doses).
7. Marketing Authorisation Holder
Allergan Limited
Marlow International
The Parkway
Marlow
Buckinghamshire, SL7 1YL
United Kingdom
8. Marketing Authorisation Number(S)
PL 00426/0072
9. Date Of First Authorisation/Renewal Of The Authorisation
20th April 1993 / 26th July 2003
10. Date Of Revision Of The Text
23rd September 2009
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