BETOPTIC S contains betaxolol hydrochloride, a cardioselective beta-adrenergic receptor inhibitor, in a sterile resin suspension formulation. Betaxolol hydrochloride is a white, crystalline powder, with a molecular weight of 343.89 g/mol. The chemical structure is presented below. Empirical Formula: C 18 H 29 NO 3 •HCl Chemical Name: (±)-1-[p-[2-(cyclopropylmethoxy) ethyl]phenoxy]-3-(isopropylamino)-2-propanol hydrochloride. Each mL of BETOPTIC S contains: Active: betaxolol HCl 2.8 mg equivalent to 2.5 mg of betaxolol base. Preservative: benzalkonium chloride 0.01%. Inactives: carbomer 934P, edetate disodium, hydrochloric acid or sodium hydroxide (to adjust pH), mannitol, poly (styrene-divinyl benzene) sulfonic acid, and purified water. BETOPTIC S has pH of approximately 7.6 and an osmolality of approximately 290 mOsmol/kg. chemical

BETOPTIC S ® (betaxolol hydrochloride ophthalmic suspension) 0.25% is indicated for the treatment of elevated intraocular pressure (IOP) in patients with chronic open-angle glaucoma or ocular hypertension. BETOPTIC S is a beta-adrenergic receptor inhibitor indicated for the treatment of elevated intraocular pressure (IOP) in patients with chronic open-angle glaucoma or ocular hypertension.

Ophthalmic suspension containing 2.5 mg/mL of betaxolol as base (0.25%) in 10 mL and 15 mL bottles. Ophthalmic suspension: 2.5 mg/mL of betaxolol as base (0.25%).

Instill one drop of BETOPTIC S in the affected eye(s) twice daily. Shake well before using. BETOPTIC S may be used alone or in combination with other IOP lowering medications. Advise patients requiring concomitant topical ophthalmic medications to administer these at least 10 minutes before instilling BETOPTIC S. Instill one drop in the affected eye(s) twice daily.

Systemic Absorption : Same adverse reactions found with systemic administration of beta-adrenergic receptor inhibitors may occur with topical ophthalmic administration. Cardiac Failure : Discontinue treatment at the first signs of cardiac failure. Diabetes Mellitus : Beta-adrenergic receptor inhibitors may mask the signs and symptoms of acute hypoglycemia. Administer with caution in diabetic patients subject to hypoglycemia. Thyrotoxicosis : Beta-adrenergic receptor inhibitors may mask certain clinical signs (e.g., tachycardia) or hyperthyroidism. 5.1 Systemic Absorption As with many topically applied ophthalmic drugs, this drug is absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic receptor inhibitors may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and death due to cardiac failure, have been reported with topical application of beta-adrenergic receptor inhibitors

Cardiac Failure BETOPTIC S 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. Treatment with BETOPTIC S should be discontinued at the first signs of cardiac failure

Diabetes Mellitus Beta-adrenergic receptor inhibitors should be administered with caution in patients subject to hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. Beta-adrenergic receptor inhibitors may mask the signs and symptoms of acute hypoglycemia

Thyrotoxicosis Beta-adrenergic receptor inhibitors may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic receptor inhibitors, which might precipitate a thyroid storm

Muscle Weakness Beta-adrenergic receptor inhibitors have been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis, and generalized weakness)

Surgical Anesthesia The necessity or desirability of withdrawal of beta-adrenergic receptor inhibitors prior to major surgery is controversial. Beta-adrenergic receptor inhibitors impair the ability of the heart to respond to beta adrenergically mediated reflex stimuli. This may augment the risk of general anesthesia in surgical procedures. Some patients receiving beta-adrenergic receptor inhibitors have experienced protracted, severe hypotension during anesthesia. Difficulty in restarting and maintaining the heartbeat has also been reported. In patients undergoing elective surgery, consider gradual withdrawal of beta-adrenergic receptor inhibitors. If necessary during surgery, the effects of beta-adrenergic receptor inhibitors may be reversed by sufficient doses of adrenergic agonists

Bronchospasm and Obstructive Pulmonary Disease Caution should be exercised in the treatment of glaucoma patients with excessive restriction of pulmonary function. There have been reports of asthmatic attacks and pulmonary distress during betaxolol treatment. Although rechallenges of some such patients with ophthalmic betaxolol has not adversely affected pulmonary function test results, the possibility of adverse pulmonary effects in patients sensitive to beta-adrenergic receptor inhibitors cannot be ruled out

Atopy/Anaphylaxis While taking beta-adrenergic receptor inhibitors, patients with a history of atopy or a history of 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 epinephrine used to treat anaphylactic reactions

Angle-Closure Glaucoma In patients with angle-closure glaucoma, the immediate treatment objective is to reopen the angle. This may require constricting the pupil. Betaxolol has little or no effect on the pupil and should not be used alone in the treatment of angle-closure glaucoma

Vascular Insufficiency Because of potential effects of beta-adrenergic receptor inhibitors on blood pressure and pulse, these inhibitors should be used with caution in patients with vascular insufficiency. If signs or symptoms suggesting reduced cerebral blood flow or Raynaud’s phenomenon develop following initiation of therapy with BETOPTIC S, alternative therapy should be considered

Bacterial Keratitis Bacterial keratitis may occur with use of multiple dose containers of topical ophthalmic products when these containers are inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface. Instruct patients on appropriate instillation techniques

Choroidal Detachment Choroidal detachment after filtration procedures has been reported with the administration of aqueous suppressant therapy

Contact Lens Wear The preservative in BETOPTIC S, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of BETOPTIC S but may be reinserted 15 minutes after instillation .

Oral beta-adrenergic receptor inhibitors may have additive effects. (7.1 ) Catecholamine-depleting drugs may have additive effects. Concomitant adrenergic psychotropic drugs may have additive effects

Oral Beta-Adrenergic Receptor Inhibitors Patients who are receiving a beta-adrenergic receptor inhibitor orally and BETOPTIC S should be observed for a potential additive effect either on the IOP or on the known systemic effects of beta blockade

Catecholamine-Depleting Drugs Close observation of the patient is recommended when a beta-adrenergic receptor inhibitor 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

Concomitant Adrenergic Psychotropic Drugs Betaxolol is an adrenergic receptor inhibitor; therefore, caution should be exercised in patients using concomitant adrenergic psychotropic drugs

Calcium Antagonists, Antiarrhythmics and Digitalis The concomitant use of a beta-adrenergic receptor inhibitor with calcium antagonists, antiarrhythmics (including amiodarone) or digitalis may have additive effects resulting in hypotension and/or marked bradycardia.