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Betaxolol (EENT) (Monograph)

Brand name: Betoptic S
Drug class: beta-Adrenergic Blocking Agents
- Beta-Adrenergic Blocking Agents
- β-Adrenergic Blocking Agents

Medically reviewed by Drugs.com on Apr 10, 2024. Written by ASHP.

Introduction

β1-Selective adrenergic blocking agent.1 2 3 4 5 6 7 8 9 10 121 122

Uses for Betaxolol (EENT)

Ocular Hypertension and Glaucoma

Reduction of elevated IOP in patients with chronic open-angle glaucoma1 2 8 12 18 19 20 74 93 94 121 122 or ocular hypertension.1 2 9 10 11 94 121

As effective as timolol in reducing IOP in patients with chronic open-angle glaucoma1 2 12 18 19 74 93 but, unlike timolol,1 2 18 53 54 55 58 59 60 61 74 is associated with minimal adverse pulmonary1 2 9 12 14 18 21 96 97 110 121 122 or cardiovascular effects.1 2 8 9 11 12 14 110 121 122

Has been used safely in selected patients with reactive airway disease (e.g., asthma, chronic bronchitis, COPD).1 2 20 21 30 97 (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).130 132 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.130 131

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.130 131 132 134

Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.130 132

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma.130 131 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.130 131 132 Adjust target IOP up or down as needed over course of disease.130 131 132

Combination therapy with drugs from different therapeutic classes often required to control IOP.131 133

Betaxolol (EENT) Dosage and Administration

General

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution or suspension.1 2 7 8 9 10 11 12 14 18 19 20 21 74 93 121 122 126

Avoid contamination of the solution or suspension container.1 103 121 (See Bacterial Keratitis under Cautions.)

Shake suspension well prior to use.121 122

Administer any concomitant topical ophthalmic drugs ≥10 minutes before administering the suspension.121

Remove contact lenses before administering each betaxolol dose; may reinsert lenses 15 minutes after the dose.121 (See Contact Lenses under Cautions.)

Dosage

Available as betaxolol hydrochloride; dosage expressed in terms of betaxolol.1 121

Betaxolol 0.25% ophthalmic suspension is therapeutically equivalent (in terms of magnitude and duration of hypotensive effect) to the 0.5% solution.121 122 126

Pediatric Patients

Ocular Hypertension and Glaucoma
Ophthalmic

Betaxolol 0.25% ophthalmic suspension: 1 drop in the affected eye(s) twice daily.121

Adults

Ocular Hypertension and Glaucoma
Ophthalmic

Betaxolol 0.5% ophthalmic solution: 1 or 2 drops in the affected eye(s) twice daily.1 2 8 122

Betaxolol 0.25% ophthalmic suspension: 1 drop in the affected eye(s) twice daily.121 122

If target IOP not achieved, may initiate additional or alternative ocular hypotensive agents.130 131 133 (See Ocular Hypertension and Glaucoma under Uses.)

Detailed Betaxolol ophthalmic dosage information

Cautions for Betaxolol (EENT)

Contraindications

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.1 121

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.1 119 121

Cardiovascular Effects

Severe cardiac reactions, including death associated with cardiac failure, reported in patients receiving topical (ocular) β-adrenergic blocking agents.1 121

Minor effects on BP 1 2 8 9 22 23 93 110 121 122 and heart rate reported with topical betaxolol.1 2 8 9 22 23 93 110

Contraindicated in patients with AV block greater than first degree,1 18 121 cardiogenic shock,1 18 21 or overt cardiac failure1 121 that is not adequately compensated (e.g., treated with cardiac glycosides and/or diuretics).104 Use with caution in patients with a history of cardiac failure or heart block.1 119 121 Discontinue therapy at the first sign or symptom of cardiac failure.1 119 121

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.1 88 121

Thyrotoxicosis

β-Adrenergic blocking agents may mask signs of hyperthyroidism (e.g., tachycardia).1 121

Possible thyroid storm if β-adrenergic blocking agent is abruptly withdrawn; carefully monitor patients having or suspected of developing thyrotoxicosis.1 121

Muscle Weakness

β-Adrenergic blocking agents reported to potentiate muscle weakness consistent with certain myasthenic manifestations (e.g., diplopia, ptosis, generalized weakness).1 121

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.1 121

Need for withdrawal of β-adrenergic blocking agents prior to major surgery is controversial;87 100 113 121 consider gradual withdrawal of β-adrenergic blocking agents prior to elective surgery.1 121

If necessary during surgery, may reverse effects of β-adrenergic blocking agents by administering sufficient doses of adrenergic agonists.121

Respiratory Disease

Severe respiratory reactions, including death resulting from bronchospasm, reported in patients with asthma receiving topical (ocular) β-adrenergic blocking agents.1 121

Topical betaxolol has been used safely in selected patients with reactive airway disease;1 2 20 21 30 97 however, increased airway resistance and pulmonary distress (i.e., dyspnea, bronchospasm, thickened bronchial secretions, asthma, respiratory failure) also reported with the drug.1 21 95 121 122 Use caution in patients with evidence of reactive airway disease on pulmonary function testing or excessive restriction of pulmonary function.1 113 121 122

Angle-closure Glaucoma

Betaxolol has little to no effect on pupil size.1 2 8 9 11 12 18 93 99 121 122 Do not use alone in patients with angle-closure glaucoma; use only in combination with a miotic in these patients.1 121

Vascular Insufficiency

Caution advised in patients with vascular insufficiency due to the potential effects of β-adrenergic blocking agents on BP and pulse.121

Consider alternative therapy if signs or symptoms of Raynaud phenomenon or reduced cerebral blood flow occur.121

Bacterial Keratitis

Bacterial keratitis reported with use of multiple-dose containers of topical ophthalmic solutions.121 Containers were inadvertently contaminated by patients, most of whom had concurrent corneal disease or disruption of the ocular epithelial surface.121

Improper handling of ophthalmic preparations can result in contamination of the preparations by common bacteria known to cause ocular infections.121 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic preparations.121 (See Advice to Patients.)

Choroidal Detachment

Choroidal detachment after filtration procedures reported with the administration of aqueous suppressant therapy.121

Contact Lenses

Betaxolol ophthalmic solution and suspension contain benzalkonium chloride, which may be absorbed by soft contact lenses.1 121 Remove contact lenses before administering each betaxolol dose; may reinsert lenses 15 minutes after the dose.121

Specific Populations

Pregnancy

Category C.1 121

Use only if potential benefits justify possible risk to fetus.1 121

Lactation

Distributed into milk.83 Caution advised if used in nursing women.1 121

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.121

Betaxolol 0.5% solution: Manufacturer states that safety and efficacy not established in pediatric patients.1

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.121

Common Adverse Effects

Ocular stinging and discomfort on instillation.1 2 8 18 74 94 98 121 122 126 May be more common with solution than with suspension.1 2 121 122

Drug Interactions

Specific Drugs

Drug

Interaction

Comments

Adrenergic psychotropic agents

Possible antagonism of psychotropic agent1 121

Use concomitantly with caution1 121

β-Adrenergic blocking agents, systemic

Possible additive effects on IOP and/or systemic β-adrenergic blockade1 121

Antiarrhythmic agents (e.g., amiodarone)

Possible additive effects (e.g., hypotension, marked bradycardia)121

Calcium-channel blocking agents

Possible additive effects (e.g., hypotension, marked bradycardia)121

Cardiac glycosides

Possible additive effects (e.g., hypotension, marked bradycardia)121

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

Possible additive effects (e.g., hypotension, marked bradycardia); may be manifested as vertigo, syncope, or postural hypotension1 121

Observe closely1 121

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 reactions1 121
Betaxolol ophthalmic drug interactions (more detail)

Betaxolol (EENT) Pharmacokinetics

Absorption

Bioavailability

Extent of absorption following topical application not elucidated.104

Commercially available solution and suspension are bioequivalent.122 126

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.1 2 121

Duration

Reduction in IOP persists for ≥12 hours.1 2 121

Distribution

Extent

Distribution into human ocular tissues and fluids has not been characterized to date.104

Betaxolol crosses the placenta and is distributed into milk.83 108

Elimination

Metabolism

Systemically absorbed betaxolol is extensively metabolized to at least 5 metabolites.2 13 46

Stability

Storage

Ophthalmic

Solution

20–25°C.1

Suspension

Upright at 2–25°C.121

Actions

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

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 2024, Selected Revisions April 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

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