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Betaxolol (EENT)

Class: beta-Adrenergic Blocking Agents
- Beta-Adrenergic Blocking Agents
- β-Adrenergic Blocking Agents
ATC Class: S01ED52
VA Class: OP101
Molecular Formula: C18H29NO3•ClH
CAS Number: 63659-19-8
Brands: Betoptic S

Medically reviewed by Drugs.com on Dec 14, 2020. Written by ASHP.

Introduction

β1-Selective adrenergic blocking agent.

Uses for Betaxolol (EENT)

Ocular Hypertension and Glaucoma

Reduction of elevated IOP in patients with chronic open-angle glaucoma or ocular hypertension.

As effective as timolol in reducing IOP in patients with chronic open-angle glaucoma but, unlike timolol, is associated with minimal adverse pulmonary or cardiovascular effects.

Has been used safely in selected patients with reactive airway disease (e.g., asthma, chronic bronchitis, COPD). (See Respiratory Disease under Cautions.)

When selecting an initial ocular hypotensive agent, consider extent of the required IOP reduction, coexisting medical conditions, and drug characteristics (e.g., dosing frequency, adverse effects, cost). With single-agent regimens, the reduction in IOP is approximately 25–33% with topical prostaglandin analogs; 20–25% with topical β-adrenergic blocking agents, α-adrenergic agonists, or miotic (parasympathomimetic) agents; 20–30% with oral carbonic anhydrase inhibitors; 18% with topical rho kinase inhibitors; and 15–20% with topical carbonic anhydrase inhibitors.

A prostaglandin analog frequently is considered for initial therapy in the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal) because of relatively greater activity, once-daily administration, and low frequency of systemic adverse effects; however, ocular adverse effects can occur.

Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma. Set an initial target IOP (based on extent of optic nerve damage and/or visual field loss, baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations) and reduce IOP toward this goal. Adjust target IOP up or down as needed over course of disease.

Combination therapy with drugs from different therapeutic classes often required to control IOP.

Betaxolol (EENT) Dosage and Administration

General

  • Adjust dosage to individual requirements and response of patient as determined by tonometric readings before and during therapy.

  • Because of diurnal variations in IOP, measure IOP at different times during the day to determine if an adequate hypotensive effect is maintained. IOP may not stabilize for a few weeks after initiating therapy.

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution or suspension.

Avoid contamination of the solution or suspension container. (See Bacterial Keratitis under Cautions.)

Shake suspension well prior to use.

Administer any concomitant topical ophthalmic drugs ≥10 minutes before administering the suspension.

Remove contact lenses before administering each betaxolol dose; may reinsert lenses 15 minutes after the dose. (See Contact Lenses under Cautions.)

Dosage

Available as betaxolol hydrochloride; dosage expressed in terms of betaxolol.

Betaxolol 0.25% ophthalmic suspension is therapeutically equivalent (in terms of magnitude and duration of hypotensive effect) to the 0.5% solution.

Pediatric Patients

Ocular Hypertension and Glaucoma
Ophthalmic

Betaxolol 0.25% ophthalmic suspension: 1 drop in the affected eye(s) twice daily.

Adults

Ocular Hypertension and Glaucoma
Ophthalmic

Betaxolol 0.5% ophthalmic solution: 1 or 2 drops in the affected eye(s) twice daily.

Betaxolol 0.25% ophthalmic suspension: 1 drop in the affected eye(s) twice daily.

If target IOP not achieved, may initiate additional or alternative ocular hypotensive agents. (See Ocular Hypertension and Glaucoma under Uses.)

Cautions for Betaxolol (EENT)

Contraindications

  • Known hypersensitivity to betaxolol or any ingredient in the formulation.

  • Sinus bradycardia or AV block greater than first degree.

  • Cardiogenic shock or overt cardiac failure that is not adequately compensated. (See Cardiovascular Effects under Cautions.)

Warnings/Precautions

Sensitivity Reactions

History of Atopy or Anaphylactic Reactions

Patients with a history of atopy or severe anaphylactic reaction to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenges with such allergens while taking β-adrenergic blocking agents; such patients may be unresponsive to usual doses of epinephrine used to treat anaphylactic reactions.

Systemic Effects

May be absorbed systemically following topical application to the eye; consider the usual precautions associated with systemic use of β-adrenergic blocking agents when using topical betaxolol.

Cardiovascular Effects

Severe cardiac reactions, including death associated with cardiac failure, reported in patients receiving topical (ocular) β-adrenergic blocking agents.

Minor effects on BP and heart rate reported with topical betaxolol.

Contraindicated in patients with AV block greater than first degree, cardiogenic shock, or overt cardiac failure that is not adequately compensated (e.g., treated with cardiac glycosides and/or diuretics). Use with caution in patients with a history of cardiac failure or heart block. Discontinue therapy at the first sign or symptom of cardiac failure.

Diabetes Mellitus

β-Adrenergic blocking agents may mask signs and symptoms of acute hypoglycemia; administer with caution in patients subject to hypoglycemia and in diabetic patients (especially those with labile diabetes) who are receiving hypoglycemic agents.

Thyrotoxicosis

β-Adrenergic blocking agents may mask signs of hyperthyroidism (e.g., tachycardia).

Possible thyroid storm if β-adrenergic blocking agent is abruptly withdrawn; carefully monitor patients having or suspected of developing thyrotoxicosis.

Muscle Weakness

β-Adrenergic blocking agents reported to potentiate muscle weakness consistent with certain myasthenic manifestations (e.g., diplopia, ptosis, generalized weakness).

Major Surgery

Possible increased risks associated with general anesthesia (e.g., severe, protracted hypotension; difficulty restarting or maintaining heart beat) due to decreased ability of the heart to respond to reflex β-adrenergic stimuli.

Need for withdrawal of β-adrenergic blocking agents prior to major surgery is controversial; consider gradual withdrawal of β-adrenergic blocking agents prior to elective surgery.

If necessary during surgery, may reverse effects of β-adrenergic blocking agents by administering sufficient doses of adrenergic agonists.

Respiratory Disease

Severe respiratory reactions, including death resulting from bronchospasm, reported in patients with asthma receiving topical (ocular) β-adrenergic blocking agents.

Topical betaxolol has been used safely in selected patients with reactive airway disease; however, increased airway resistance and pulmonary distress (i.e., dyspnea, bronchospasm, thickened bronchial secretions, asthma, respiratory failure) also reported with the drug. Use caution in patients with evidence of reactive airway disease on pulmonary function testing or excessive restriction of pulmonary function.

Angle-closure Glaucoma

Betaxolol has little to no effect on pupil size. Do not use alone in patients with angle-closure glaucoma; use only in combination with a miotic in these patients.

Vascular Insufficiency

Caution advised in patients with vascular insufficiency due to the potential effects of β-adrenergic blocking agents on BP and pulse.

Consider alternative therapy if signs or symptoms of Raynaud phenomenon or reduced cerebral blood flow occur.

Bacterial Keratitis

Bacterial keratitis reported with use of multiple-dose containers of topical ophthalmic solutions. Containers were inadvertently contaminated by patients, most of whom had concurrent corneal disease or disruption of the ocular epithelial surface.

Improper handling of ophthalmic preparations can result in contamination of the preparations by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic preparations. (See Advice to Patients.)

Choroidal Detachment

Choroidal detachment after filtration procedures reported with the administration of aqueous suppressant therapy.

Contact Lenses

Betaxolol ophthalmic solution and suspension contain benzalkonium chloride, which may be absorbed by soft contact lenses. Remove contact lenses before administering each betaxolol dose; may reinsert lenses 15 minutes after the dose.

Specific Populations

Pregnancy

Category C.

Use only if potential benefits justify possible risk to fetus.

Lactation

Distributed into milk. Caution advised if used in nursing women.

Pediatric Use

Betaxolol 0.25% suspension: Safety and efficacy in pediatric patients established in a 3-month, active-controlled clinical trial; adverse effects comparable to those observed in adults.

Betaxolol 0.5% solution: Manufacturer states that safety and efficacy not established in pediatric patients.

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.

Common Adverse Effects

Ocular stinging and discomfort on instillation. May be more common with solution than with suspension.

Interactions for Betaxolol (EENT)

Specific Drugs

Drug

Interaction

Comments

Adrenergic psychotropic agents

Possible antagonism of psychotropic agent

Use concomitantly with caution

β-Adrenergic blocking agents, systemic

Possible additive effects on IOP and/or systemic β-adrenergic blockade

Antiarrhythmic agents (e.g., amiodarone)

Possible additive effects (e.g., hypotension, marked bradycardia)

Calcium-channel blocking agents

Possible additive effects (e.g., hypotension, marked bradycardia)

Cardiac glycosides

Possible additive effects (e.g., hypotension, marked bradycardia)

Catecholamine-depleting drugs (e.g., reserpine)

Possible additive effects (e.g., hypotension, marked bradycardia); may be manifested as vertigo, syncope, or postural hypotension

Observe closely

Epinephrine

Atopic individuals and those with a history of severe anaphylactic reactions may not respond to usual doses of epinephrine used in the treatment of anaphylactic reactions

Betaxolol (EENT) Pharmacokinetics

Absorption

Bioavailability

Extent of absorption following topical application not elucidated.

Commercially available solution and suspension are bioequivalent.

Onset

Following topical application to the eye with either the 0.25% suspension or the 0.5% solution, reduction in IOP usually evident within 0.5–1 hour and reaches a maximum within 2 hours.

Duration

Reduction in IOP persists for ≥12 hours.

Distribution

Extent

Distribution into human ocular tissues and fluids has not been characterized to date.

Betaxolol crosses the placenta and is distributed into milk.

Elimination

Metabolism

Systemically absorbed betaxolol is extensively metabolized to at least 5 metabolites.

Stability

Storage

Ophthalmic

Solution

20–25°C.

Suspension

Upright at 2–25°C.

Actions

  • Selective β1-adrenergic blocking agent that does not exhibit intrinsic β1-agonist or membrane stabilizing (local anesthetic) activity.

  • One of the most potent and selective β1-adrenergic blocking agents currently available.

  • Reduces both elevated and normal IOP without affecting pupillary size or accommodation and without producing miosis and/or ciliary spasm associated with miotic agents.

  • Reduces IOP by about 20–35% from baseline in patients with elevated IOP.

  • Exact mechanism of action not fully elucidated; tonography and fluorophotometric studies suggest that reduced aqueous humor formation is the principal effect.

  • May block endogenous catecholamine-stimulated increases in cyclic adenosine monophosphate (AMP) concentrations within the ciliary processes and subsequent formation of aqueous humor.

  • Does not appear to affect aqueous outflow resistance.

  • IOP-lowering effect maintained for ≥4 years of continuous use in some patients.

Advice to Patients

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the solution or suspension with common bacteria that can cause ocular infections. Instruct patients that the tip of the dispensing container should not touch the eye or surrounding structures. Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic preparations.

  • Advise patients to immediately contact their clinician for advice regarding continued use of the current multidose container if they experience an intercurrent ocular condition (e.g., trauma, infection) or require ocular surgery.

  • Importance of removing contact lenses before administering each betaxolol dose and delaying reinsertion for at least 15 minutes after the dose.

  • Importance of administering any concomitant topical ophthalmic drugs ≥10 minutes before administering betaxolol suspension.

  • Advise patients that betaxolol suspension may cause temporary blurring of vision following instillation and to use caution when driving or operating machinery.

  • Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Betaxolol Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.5% (of betaxolol)*

Betaxolol Hydrochloride Ophthalmic Solution

Suspension

0.25% (of betaxolol)

Betoptic S

Alcon

AHFS DI Essentials™. © Copyright 2022, Selected Revisions December 14, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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