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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 on Apr 10, 2024. Written by ASHP.


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



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.)


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

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


Ocular Hypertension and Glaucoma

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)



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.


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


Category C.

Use only if potential benefits justify possible risk to fetus.


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.

Drug Interactions

Specific Drugs




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


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



Extent of absorption following topical application not elucidated.

Commercially available solution and suspension are bioequivalent.


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.


Reduction in IOP persists for ≥12 hours.



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

Betaxolol crosses the placenta and is distributed into milk.



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







Upright at 2–25°C.


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.


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


Dosage Forms


Brand Names




0.5% (of betaxolol)*

Betaxolol Hydrochloride Ophthalmic Solution


0.25% (of betaxolol)

Betoptic S


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.

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