Levobunolol Hydrochloride

LEVOBUNOLOL HYDROCHLORIDE- levobunolol hydrochloride solution/ drops
Bausch & Lomb Incorporated

Rx only

FOR USE IN THE EYES ONLY

Description:

Levobunolol Hydrochloride Ophthalmic Solution, USP 0.5% is a noncardioselective beta-adrenoceptor blocking agent for ophthalmic use.

Levobunolol hydrochloride is represented by the following structural formula:

Levobunolol Hydrochloride (Structural formula)

C17 H25 NO3 •HCl

Mol. Wt. 327.85

Chemical Name: (-)-5-[3-(tert-Butylamino)-2-hydroxypropoxy]-3,4-dihydro-1(2H)-naphthalenone hydrochloride.

Each mL of 0.5% contains:

ACTIVE: Levobunolol Hydrochloride 0.5%; INACTIVES: Polyvinyl Alcohol 1.4%, Sodium Chloride, Dibasic Sodium Phosphate, Edetate Disodium, Sodium Metabisulfite, Monobasic Potassium Phosphate, and Purified Water. Hydrochloric Acid and/or Sodium Hydroxide may be added to adjust pH (5.5 — 7.5); PRESERVATIVE: Benzalkonium Chloride (0.004%).

Clinical Pharmacology:

Levobunolol hydrochloride is a noncardioselective beta-adrenoceptor blocking agent, equipotent at both beta1 and beta2 receptors. Levobunolol hydrochloride is greater than 60 times more potent than its dextro isomer in its beta-blocking activity, yet equipotent in its potential for direct myocardial depression. Accordingly, the levo isomer, levobunolol hydrochloride, is used. Levobunolol hydrochloride does not have significant local anesthetic (membrane-stabilizing) or intrinsic sympathomimetic activity.

Beta-adrenergic receptor blockade reduces cardiac output in both healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta-adrenergic receptor blockade may inhibit the stimulatory effect of the sympathetic nervous system necessary to maintain adequate cardiac function.

Beta-adrenergic receptor blockade in the bronchi and bronchioles results in increased airway resistance from unopposed parasympathetic activity. Such an effect in patients with asthma or other bronchospastic conditions is potentially dangerous.

Levobunolol Hydrochloride Ophthalmic Solution has been shown to be an active agent in lowering elevated as well as normal intraocular pressure (IOP) whether or not accompanied by glaucoma. Elevated IOP presents a major risk factor in glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.

The onset of action with one drop of Levobunolol Hydrochloride Ophthalmic Solution can be detected within one hour after treatment, with maximum effect seen between 2 and 6 hours.

A significant decrease in IOP can be maintained for up to 24 hours following a single dose.

In two separate, controlled studies (one three-month and one up to 12 months duration) Levobunolol Hydrochloride Ophthalmic Solution 0.25% twice a day controlled the IOP of approximately 64% and 70% of the subjects. The overall mean decrease from baseline was 5.4 mm Hg and 5.1 mm Hg respectively. In an open-label study Levobunolol Hydrochloride Ophthalmic Solution 0.25% daily controlled the IOP of 72% of the subjects while achieving an overall mean decrease of 5.9 mm Hg.

In controlled clinical studies of approximately two years duration, intraocular pressure was well-controlled in approximately 80% of subjects treated with Levobunolol Hydrochloride Ophthalmic Solution 0.5% twice a day. The mean IOP decrease from baseline was between 6.87 mm Hg and 7.81 mm Hg. No significant effects on pupil size, tear production or corneal sensitivity were observed. Levobunolol Hydrochloride Ophthalmic Solution at the concentrations tested, when applied topically, decreased heart rate and blood pressure in some patients. The IOP-lowering effect of levobunolol was well maintained over the course of these studies.

In a three-month clinical study, a single daily application of Levobunolol Hydrochloride Ophthalmic Solution 0.5% controlled the IOP of 72% of subjects achieving an overall mean decrease in IOP of 7.0 mm Hg.

The primary mechanism of the ocular hypotensive action of levobunolol hydrochloride in reducing IOP is most likely a decrease in aqueous humor production. Levobunolol Hydrochloride Ophthalmic Solution reduces IOP with little or no effect on pupil size or accommodation 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 and have not been reported with the use of Levobunolol Hydrochloride Ophthalmic Solution. This is particularly important in cataract patients with central lens opacities who would experience decreased visual acuity with pupillary constriction.

Indications and Usage:

Levobunolol Hydrochloride Ophthalmic Solution has been shown to be effective in lowering intraocular pressure and may be used in patients with chronic open-angle glaucoma or ocular hypertension.

Contraindications:

Levobunolol Hydrochloride Ophthalmic Solution is contraindicated in those individuals with bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS); sinus bradycardia; second and third degree atrioventricular block; overt cardiac failure (see WARNINGS); cardiogenic shock; or hypersensitivity to any component of these products.

Warnings:

As with other topically applied ophthalmic drugs, Levobunolol Hydrochloride Ophthalmic Solution 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 (see CONTRAINDICATIONS).

Cardiac Failure

Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe failure.

In Patients Without a History of Cardiac Failure

Continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. At the first sign or symptom of cardiac failure, Levobunolol Hydrochloride Ophthalmic Solution should be discontinued.

Obstructive Pulmonary Disease:

PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (e.g., CHRONIC BRONCHITIS, EMPHYSEMA) OF MILD OR MODERATE SEVERITY, BRONCHOSPASTIC DISEASE OR A HISTORY OF BRONCHOSPASTIC DISEASE (OTHER THAN BRONCHIAL ASTHMA OR A HISTORY OF BRONCHIAL ASTHMA, IN WHICH LEVOBUNOLOL HYDROCHLORIDE OPHTHALMIC SOLUTION IS CONTRAINDICATED, see CONTRAINDICATIONS), SHOULD IN GENERAL NOT RECEIVE BETA BLOCKERS, INCLUDING LEVOBUNOLOL HYDROCHLORIDE OPHTHALMIC SOLUTION. However, if Levobunolol Hydrochloride Ophthalmic Solution is deemed necessary in such patients, then it should be administered cautiously since it may block bronchodilation produced by endogenous and exogenous catecholamine stimulation of beta2 receptors.

Major Surgery

The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial. Beta-adrenergic receptor blockade impairs 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 blocking agents have been subject to protracted severe hypotension during anesthesia. Difficulty in restarting and maintaining the heartbeat has also been reported. For these reasons, in patients undergoing elective surgery, gradual withdrawal of beta-adrenergic blocking agents may be appropriate. If necessary during surgery, the effects of beta-adrenergic blocking agents may be reversed by sufficient doses of such agonists as isoproterenol, dopamine, dobutamine or levarterenol (see OVERDOSAGE).

Diabetes Mellitus

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 blocking agents may mask the signs and symptoms of acute hypoglycemia.

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