Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution contains Betaxolol (Betaxolol hydrochloride) hydrochloride, a cardioselective beta-adrenergic receptor blocking agent, in a sterile isotonic solution. Betaxolol (Betaxolol hydrochloride) hydrochloride is a white, crystalline powder, soluble in water, with a molecular weight of 343.89. The chemical structure is presented below:

Empirical Formula:

CHNO•HCl

Chemical Name:

(±)-1-[p-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol hydrochloride.

Each mL of Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution (0.5%) contains: 5.6 mg Betaxolol (Betaxolol hydrochloride) hydrochloride equivalent to Betaxolol (Betaxolol hydrochloride) base 5 mg. Benzalkonium Chloride 0.01%. Edetate Disodium, Sodium Chloride, Hydrochloric Acid and/or Sodium Hydroxide (to adjust pH), and Purified Water.

Betaxolol (Betaxolol hydrochloride) Hydrochloride, a cardioselective (beta-1-adrenergic) receptor blocking agent, does not have significant membrane-stabilizing (local anesthetic) activity and is devoid of intrinsic sympathomimetic action. Orally administered beta-adrenergic blocking agents reduce cardiac output in healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta-adrenergic receptor antagonists may inhibit the sympathetic stimulatory effect necessary to maintain adequate cardiac function.

When instilled in the eye, Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution has the action of reducing elevated as well as normal intraocular pressure, whether or not accompanied by glaucoma. Ophthalmic Betaxolol (Betaxolol hydrochloride) has minimal effect on pulmonary and cardiovascular parameters.

Ophthalmic Betaxolol (Betaxolol hydrochloride) (one drop in each eye) was compared to timolol and placebo in a three-way crossover study challenging nine patients with reactive airway disease who were selected on the basis of having at least a 15% reduction in the forced expiratory volume in one second (FEV) after administration of ophthalmic timolol. Betaxolol (Betaxolol hydrochloride) HCl had no significant effect on pulmonary function as measured by FEV, Forced Vital Capacity (FVC) and FEV/VC. Additionally, the action of isoproterenol, a beta stimulant, administered at the end of the study was not inhibited by ophthalmic betaxolol. In contrast, ophthalmic timolol significantly decreased these pulmonary functions.

*Timolol statistically different from Betaxolol (Betaxolol hydrochloride) and placebo (p

No evidence of cardiovascular beta-adrenergic blockade during exercise was observed with Betaxolol (Betaxolol hydrochloride) in a double-masked, three-way crossover study in 24 normal subjects comparing ophthalmic betaxolol, timolol and placebo for effect on blood pressure and heart rate. Mean arterial blood pressure was not affected by any treatment; however, ophthalmic timolol produced a significant decrease in the mean heart rate.

*Mean pulse rate significantly lower for timolol than Betaxolol (Betaxolol hydrochloride) or placebo (p

Clinical studies show that topical Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution reduces mean intraocular pressure 25% from baseline. In trials using 22 mmHg as a generally accepted index of intraocular pressure control, Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution was effective in more than 94% of the population studied, of which 73% were treated with the beta blocker alone. In controlled, double-masked studies, the magnitude and duration of the ocular hypotensive effect of Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution and ophthalmic timolol solution were clinically equivalent.

Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution has also been used successfully in glaucoma patients who have undergone a laser trabeculoplasty and have needed additional long-term ocular hypotensive therapy.

Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution has been well tolerated in glaucoma patients wearing hard or soft contact lenses and in aphakic patients.

Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution does not produce miosis or accommodative spasm which are frequently seen with miotic agents. The blurred vision and night blindness often associated with standard miotic therapy are not associated with Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution. Thus, patients with central lenticular opacities avoid the visual impairment caused by a constricted pupil.

Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution has been shown to be effective in lowering intraocular pressure and is indicated in the treatment of ocular hypertension and chronic open-angle glaucoma. It may be used alone or in

combination with other anti-glaucoma drugs.

In clinical studies, Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution was safely used to lower intraocular pressure in 47 patients with both glaucoma and reactive airway disease who were followed for a mean period of 15 months. However, caution should be used in treating patients with severe reactive airway disease or a history of asthma.

Hypersensitivity to any component of this product. Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution is contraindicated in patients with sinus bradycardia, greater than a first degree atrioventricular block, cardiogenic shock, or patients with overt cardiac failure.

Topically applied beta-adrenergic blocking agents may be absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported with topical application of beta-adrenergic blocking agents.

Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution 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 Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution should be discontinued at the first signs of cardiac failure.

Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents.

Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycemia.

Patients who are receiving a beta-adrenergic blocking agent orally and Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of beta blockade.

Close observation of the patient is recommended when a beta blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or bradycardia.

Betaxolol (Betaxolol hydrochloride) is an adrenergic blocking agent; therefore, caution should be exercised in patients using concomitant adrenergic psychotropic drugs.

Lifetime studies with Betaxolol (Betaxolol hydrochloride) HCl have been completed in mice at oral doses of 6, 20 or 60 mg/kg/day and in rats at 3, 12 or 48 mg/kg/day; Betaxolol (Betaxolol hydrochloride) HCl demonstrated no carcinogenic effect. Higher dose levels were not tested.

In a variety of and bacterial and mammalian cell assays, Betaxolol (Betaxolol hydrochloride) HCl was nonmutagenic.

Pregnancy Category C.

It is not known whether Betaxolol (Betaxolol hydrochloride) HCl is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution is administered to nursing women.

Safety and effectiveness in pediatric patients have not been established.

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

The following adverse reactions have been reported in clinical trials with Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution.

Additional medical events reported with other formulations of Betaxolol (Betaxolol hydrochloride) include blurred vision, foreign body sensation, dryness of the eyes, inflammation, discharge, ocular pain, decreased visual acuity, and crusty lashes.

No information is available on overdosage of humans. The oral LD of the drug ranged from 350-920 mg/kg in mice and 860-1050 mg/kg in rats. The symptoms which might be expected with an overdose of a systemically administered beta-1-adrenergic receptor blocker agent are bradycardia, hypotension and acute cardiac failure. A topical overdose of Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution may be flushed from the eye(s) with warm tap water.

The recommended dose is one to two drops of Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution in the affected eye(s) twice daily. In some patients, the intraocular pressure lowering responses to Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution may require a few weeks to stabilize. As with any new medication, careful monitoring of patients is advised.

If the intraocular pressure of the patient is not adequately controlled on this regimen, concomitant therapy with pilocarpine and other miotics, and/or epinephrine and/or carbonic anhydrase inhibitors can be instituted.

Betaxolol (Betaxolol hydrochloride) Hydrochloride Ophthalmic Solution is a sterile, isotonic, aqueous solution of Betaxolol (Betaxolol hydrochloride) hydrochloride. Supplied as follows: 5, 10 and 15 mL in plastic ophthalmic DROP-TAINER* dispensers.

  5 mL: 61314-245-01               15 mL: 61314-245-02

10 mL: 61314-245-03

*DROP-TAINER is a registered trademark of Alcon Manufacturing, Ltd.

Dist. by:

Fort Worth, Texas 76134

Mfd. by:

Fort Worth, Texas 76134 USA

Printed in USA

AFFILATE OF                  QUALITY RX

ALCON

LABORATORIES, INC.