PHARMACOLOGICAL ACTION: Betaxolol HCl is a cardioselective (beta-1-adrenergic) receptor blocking agent. When instilled in the eye, betaxolol reduces elevated as well as normal intraocular pressure. The mechanism of ocular hypotensive action appears to be 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 2 hours after topical administration. A single dose provides a 12 hour reduction in intraocular pressure. Betaxolol does not produce miosis or accommodative spasm.
During therapy with betaxolol, no negative effect on the blood supply to the optic nerve has been observed.
INDICATIONS: BETOPTIC S Single Dose has been shown to be effective in lowering intraocular pressure and is indicated in the treatment of:
Patients with chronic open-angle glaucoma.
Patients with elevated intraocular pressure (ocular hypertensive patients).
CONTRA-INDICATIONS: Hypersensitivity to any component of this product.
BETOPTIC S Single Dose is contra-indicated in patients with sinus bradycardia, an uncorrected greater than first degree atrioventricular block, cardiogenic shock, or patients with cardiac failure unless or until signs of failure are controlled with appropriate medicine.
WARNINGS: Caution should be used in treating patients with a history of cardiac failure or heart block. Treatment with BETOPTIC S Single Dose should be discontinued at the first signs of cardiac failure. 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 S Single Dose should be used with a miotic to reduce elevated intraocular pressure in angle-closure glaucoma. The ability to drive and use machines is unlikely to be affected following the use of BETOPTIC S Single Dose.
DOSAGE AND DIRECTIONS FOR USE: SHAKE WELL BEFORE USE.
The usual dose is one drop of BETOPTIC S Single Dose in the affected eye(s) twice daily.
In some patients, the intraocular pressure lowering response to BETOPTIC S Single Dose may require a few weeks to stabilize. Careful monitoring of patients is advised. Clinical follow up should include a determination of the intraocular pressure during the first month of treatment with BETOPTIC S Single Dose. Thereafter, intraocular pressures should be determined on an individual basis at the judgement of the physician.
When a patient is transferred from a single anti-glaucoma non beta-blocking agent, continue the agent already used and add one drop of BETOPTIC S Single Dose in the affected eye(s) twice a day. On the following day, discontinue the previous anti-glaucoma agent completely and continue with BETOPTIC S Single Dose. 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. Therapy should be individualised.
If the intraocular pressure of the patient is not adequately controlled on this regimen, concomitant therapy with pilocarpine, other miotics, epinephrine or systemically administered carbonic anhydrase inhibitors can be instituted.
When a patient is transferred from several concomitantly administered anti-glaucoma agents, individualization 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 S Single Dose in the affected eye(s) twice a day. On the following day, discontinue one of the other anti-glaucoma agents. The remaining anti-glaucoma agents may be decreased or discontinued according to the patient's response to treatment.
SIDE EFFECTS AND SPECIAL PRECAUTIONS:
SIDE-EFFECTS: The following adverse reactions have been reported following topical administration of BETOPTIC S Single Dose: Ocular: Transient ocular discomfort, such as ocular stinging and burning, blurred vision, corneal disease such as corneal punctate staining, superficial punctate keratitis, foreign body sensation, photophobia, tearing, itching, erythema, allergic reaction, decreased corneal sensitivity and dryness of eyes. Systemic: Insomnia, bradycardia, dyspnea, asthma, headaches and depression.
Other systemic side-effects which may occur with the oral use of beta-blockers are: Congestive cardiac failure and marked bradycardia, exacerbation of peripheral vascular disease, or the development of Raynaud's phenomenon (due to unopposed arteriolar-alpha-sympatic activation), sexual impotence, hypoglycaemia, skeletal muscle weakness and gastro-intestinal disturbances. Severe peripheral vascular disease and even peripheral gangrene may be precipitated. Neuropsychiatric disorders ranging from vague fatigue and malaise, vivid dreams and nightmares to overt psychosis. Infants of mothers administered beta-blockers shortly before giving birth, or during labour may be born hypotonic, collapsed and hypoglycaemic. Adverse reactions are more common in patients with renal decompensation.
PRECAUTIONS: Patients who are receiving a beta-adrenergic blocking agent orally and BETOPTIC S Single Dose should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of beta blockade. Diabetes Mellitus: Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients who are receiving insulin or oral hypoglycaemic agents. Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycaemia. Thyrotoxicosis: Beta-adrenergic blocking agents may mask certain clinical signs (eg. tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents, which might precipitate a thyroid storm. Major Surgery: 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. Pulmonary: Caution should be exercised in patients with bronchial asthma, chronic bronchitis and hypersensitive airways as bronchoconstriction may be aggravated by BETOPTIC S Single Dose. Drug interactions: Although ophthalmic betaxolol used alone has little or no effect on pupil size, mydriasis resulting from concomitant therapy with ophthalmic betaxolol and epinephrine has been reported.
Close observation of the patient is recommended when a beta-blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine and various antiarrhythmic agents because of possible additive effects and the production of hypotension and/or bradycardia.
Caution should be exercised in patients using concomitant adrenergic psychotropic drugs. Pregnancy: Safety in pregnancy has not yet been established. Nursing Mothers: It is not known whether betaxolol HCl is excreted in human milk.
Caution should be exercised when BETOPTIC S Single Dose is administered to nursing women. Usage in Children: Clinical studies to establish the safety and efficacy in children have not been performed. Long-term use: The long-term safety of beta-blockers has not yet been established. Diminished responsiveness to ophthalmic betaxolol following long-term therapy has been reported.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT: No information is available on overdosage of humans. 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 S Single Dose may be flushed from the eye(s) with warm tap water.
IDENTIFICATION: A white to off-white suspension.
PRESENTATION: Carton containing 50 natural low density polyethylene single dose containers with a nominal fill of 0,25 mL in cards of 5 units, packed in aluminium foil pouches.
STORAGE INSTRUCTIONS: Store at room temperature, below 25°C.
KEEP OUT OF REACH OF CHILDREN. FOR SINGLE USE ONLY.
Discard unused portion of suspension immediately after use.
REGISTRATION NUMBER: 28/15.4/0716
NAME AND BUSINESS ADDRESS OF THE APPLICANT: Alcon Laboratories (S.A.)(Pty) Ltd.
DATE OF PUBLICATION OF THIS PACKAGE INSERT: 19 May 1999