Skip to Content
Get key facts and figures about chronic dry eye

Betaxolol (Ophthalmic)

Pronunciation

(be TAKS oh lol)

Index Terms

  • Betaxolol HCl
  • Betaxolol Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Generic: 0.5% (5 mL, 10 mL, 15 mL)

Suspension, Ophthalmic:

Betoptic-S: 0.25% (10 mL, 15 mL)

Brand Names: U.S.

  • Betoptic-S

Pharmacologic Category

  • Ophthalmic Agent, Antiglaucoma

Pharmacology

Competitively blocks beta1-receptors, with little or no effect on beta2-receptors; with ophthalmic use, reduces intraocular pressure by reducing the production of aqueous humor

Absorption

Rapidly absorbed into the systemic circulation (concentrations ~1/10 to 1/20 of oral dosing) (Vainio-Jylhä, 2001)

Excretion

Urine (>80%, as unchanged drug [15%] and inactive metabolites)

Onset of Action

Within 30 minutes; Peak effect: Intraocular pressure reduction: ~2 hours

Duration of Action

≥12 hours

Use: Labeled Indications

Treatment of chronic open-angle glaucoma or ocular hypertension

Contraindications

Hypersensitivity to betaxolol or any component of the formulation; sinus bradycardia; heart block greater than first-degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; uncompensated cardiac failure

Dosing: Adult

Glaucoma: Ophthalmic:

Solution: Instill 1-2 drops into affected eye(s) twice daily.

Suspension (Betoptic® S): Instill 1 drop into affected eye(s) twice daily.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Elevated intraocular pressure: Ophthalmic suspension (Betoptic® S): Instill 1 drop into affected eye(s) twice daily.

Administration

Shake suspension well before using. Tilt head back and instill in eye. Keep eye open and do not blink for 30 seconds. Apply gentle pressure to lacrimal sac for 1 minute. Wipe away excess from skin. Do not touch applicator to eye and do not contaminate tip of applicator.

Storage

Store ophthalmic suspension upright at 2°C to 25°C (36°F to 77°F). Store ophthalmic solution at 20°C to 25°C (68°F to 77°F).

Drug Interactions

Abiraterone Acetate: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of Beta-Blockers. Monitor therapy

Alpha-/Beta-Agonists (Direct-Acting): Beta-Blockers may enhance the vasopressor effect of Alpha-/Beta-Agonists (Direct-Acting). Epinephrine used as a local anesthetic for dental procedures will not likely cause clinically relevant problems. Some beta-adrenoceptor mediated effects of Alpha-/Beta-Agonists (Direct-Acting), including anti-anaphylactic effects of epinephrine, may be diminished by Beta-Blockers. Management: Cardioselective beta-blockers and lower doses of epinephrine may confer a more limited risk. Patients who may require acute subcutaneous epinephrine (e.g., bee sting kits) should probably avoid beta blockers. Exceptions: Dipivefrin. Consider therapy modification

Alpha1-Blockers: Beta-Blockers may enhance the orthostatic hypotensive effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Monitor therapy

Alpha2-Agonists: May enhance the AV-blocking effect of Beta-Blockers. Sinus node dysfunction may also be enhanced. Beta-Blockers may enhance the rebound hypertensive effect of Alpha2-Agonists. This effect can occur when the Alpha2-Agonist is abruptly withdrawn. Management: Closely monitor heart rate during treatment with a beta blocker and clonidine. Withdraw beta blockers several days before clonidine withdrawal when possible, and monitor blood pressure closely. Recommendations for other alpha2-agonists are unavailable. Exceptions: Apraclonidine. Consider therapy modification

Aminoquinolines (Antimalarial): May decrease the metabolism of Beta-Blockers. Monitor therapy

Amiodarone: May enhance the bradycardic effect of Beta-Blockers. Possibly to the point of cardiac arrest. Amiodarone may increase the serum concentration of Beta-Blockers. Monitor therapy

Anilidopiperidine Opioids: May enhance the bradycardic effect of Beta-Blockers. Anilidopiperidine Opioids may enhance the hypotensive effect of Beta-Blockers. Monitor therapy

Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Beta-Blockers. Beta-Blockers may decrease the metabolism of Antipsychotic Agents (Phenothiazines). Antipsychotic Agents (Phenothiazines) may decrease the metabolism of Beta-Blockers. Monitor therapy

Barbiturates: May decrease the serum concentration of Beta-Blockers. Monitor therapy

Beta2-Agonists: Beta-Blockers (Beta1 Selective) may diminish the bronchodilatory effect of Beta2-Agonists. Of particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-blockers. Monitor therapy

Bupivacaine: Beta-Blockers may increase the serum concentration of Bupivacaine. Monitor therapy

Calcium Channel Blockers (Nondihydropyridine): May enhance the hypotensive effect of Beta-Blockers. Bradycardia and signs of heart failure have also been reported. Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Beta-Blockers. Exceptions: Bepridil. Monitor therapy

Cardiac Glycosides: Beta-Blockers may enhance the bradycardic effect of Cardiac Glycosides. Monitor therapy

Cholinergic Agonists: Beta-Blockers may enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Management: Administer these agents in combination with caution, and monitor for conduction disturbances. Avoid methacholine with any beta blocker due to the potential for additive bronchoconstriction. Monitor therapy

CYP1A2 Inhibitors (Moderate): May decrease the metabolism of CYP1A2 Substrates. Monitor therapy

CYP1A2 Inhibitors (Strong): May decrease the metabolism of CYP1A2 Substrates. Consider therapy modification

Deferasirox: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Dipyridamole: May enhance the bradycardic effect of Beta-Blockers. Monitor therapy

Disopyramide: May enhance the bradycardic effect of Beta-Blockers. Beta-Blockers may enhance the negative inotropic effect of Disopyramide. Monitor therapy

Dronedarone: May enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6. Management: Use lower initial beta-blocker doses; adequate tolerance of the combination, based on ECG findings, should be confirmed prior to any increase in beta-blocker dose. Consider therapy modification

Ergot Derivatives: Beta-Blockers may enhance the vasoconstricting effect of Ergot Derivatives. Exceptions: Nicergoline. Consider therapy modification

Fingolimod: Beta-Blockers may enhance the bradycardic effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and beta-blockers if possible. If coadministration is necessary, patients should have overnight continuous ECG monitoring conducted after the first dose of fingolimod. Monitor patients for bradycardia. Consider therapy modification

Floctafenine: May enhance the adverse/toxic effect of Beta-Blockers. Avoid combination

Grass Pollen Allergen Extract (5 Grass Extract): Beta-Blockers may enhance the adverse/toxic effect of Grass Pollen Allergen Extract (5 Grass Extract). More specifically, Beta-Blockers may inhibit the ability to effectively treat severe allergic reactions to Grass Pollen Allergen Extract (5 Grass Extract) with epinephrine. Some other effects of epinephrine may be unaffected or even enhanced (e.g., vasoconstriction) during treatment with Beta-Blockers. Consider therapy modification

Insulin: Beta-Blockers may enhance the hypoglycemic effect of Insulin. Monitor therapy

Lidocaine (Systemic): Beta-Blockers may increase the serum concentration of Lidocaine (Systemic). Monitor therapy

Lidocaine (Topical): Beta-Blockers may increase the serum concentration of Lidocaine (Topical). Monitor therapy

Mepivacaine: Beta-Blockers may increase the serum concentration of Mepivacaine. Monitor therapy

Methacholine: Beta-Blockers may enhance the adverse/toxic effect of Methacholine. Avoid combination

Midodrine: Beta-Blockers may enhance the bradycardic effect of Midodrine. Monitor therapy

NIFEdipine: May enhance the hypotensive effect of Beta-Blockers. NIFEdipine may enhance the negative inotropic effect of Beta-Blockers. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Beta-Blockers. Monitor therapy

Obeticholic Acid: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Peginterferon Alfa-2b: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Propafenone: May increase the serum concentration of Beta-Blockers. Propafenone possesses some independent beta blocking activity. Monitor therapy

Regorafenib: May enhance the bradycardic effect of Beta-Blockers. Monitor therapy

Reserpine: May enhance the hypotensive effect of Beta-Blockers. Monitor therapy

Rifamycin Derivatives: May decrease the serum concentration of Beta-Blockers. Exceptions: Rifabutin. Monitor therapy

Rivastigmine: May enhance the bradycardic effect of Beta-Blockers. Avoid combination

Sulfonylureas: Beta-Blockers may enhance the hypoglycemic effect of Sulfonylureas. Cardioselective beta-blockers (eg, acebutolol, atenolol, metoprolol, and penbutolol) may be safer than nonselective beta-blockers. All beta-blockers appear to mask tachycardia as an initial symptom of hypoglycemia. Ophthalmic beta-blockers are probably associated with lower risk than systemic agents. Monitor therapy

Theophylline Derivatives: Beta-Blockers (Beta1 Selective) may diminish the bronchodilatory effect of Theophylline Derivatives. Management: Monitor for reduced theophylline efficacy during concomitant use with any beta-blocker. Beta-1 selective agents are less likely to antagonize theophylline than nonselective agents, but selectivity may be lost at higher doses. Monitor therapy

Vemurafenib: May increase the serum concentration of CYP1A2 Substrates. Management: Consider alternatives to such combinations whenever possible, particularly if the CYP1A2 substrate has a relatively narrow therapeutic index. Consider therapy modification

Adverse Reactions

Frequency not always defined.

Ophthalmic: Eye discomfort (≤25%; short-term), anisocoria, blurred vision, choroidal detachment, corneal staining, crusting of eyelash, decreased corneal sensitivity, decreased visual acuity, eye discharge, eye pain, eye pruritus, eye redness, foreign body sensation of eye, hypersensitivity reaction (ophthalmic), keratitis, lacrimation, ocular edema, ophthalmic inflammation, photophobia, punctate corneal staining (with or without dendritic formations), superficial punctate keratitis, xerophthalmia

<1% (Limited to important or life-threatening): Alopecia, altered sense of smell, asthma, bradycardia, bronchospasm, cardiac failure, depression, dizziness, dysgeusia, dyspnea, exacerbation of myasthenia gravis, glossitis, heart block, headache, insomnia, lethargy, respiratory failure, thickening of bronchial secretions, toxic epidermal necrolysis, urticaria, vertigo

Warnings/Precautions

Concerns related to adverse events:

• Anaphylactic reactions: Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.

Disease-related concerns:

• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring; asthma exacerbation and pulmonary distress has been reported during betaxolol use.

• Cardiovascular insufficiency: Use with caution in patients with cardiovascular insufficiency; if signs of decreased cerebral blood flow occur, consider alternative therapy.

• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms.

• Heart failure: Use with caution in patients with compensated heart failure (HF) and monitor for a worsening of the condition. Discontinue at the first signs of cardiac failure.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis; may worsen disease.

• Thyroid disease: May mask signs of hyperthyroidism (eg, tachycardia). If thyrotoxicosis is suspected, carefully manage and monitor; abrupt withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm.

Special populations:

• Contact lens wearers: Ophthalmic solution/suspension contains benzalkonium chloride which may be absorbed by contact lenses; remove contact lens prior to administration and wait 15 minutes before reinserting.

Dosage form specific issues:

• Ophthalmic: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis. Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction). Choroidal detachment has been reported with aqueous suppressant therapy after filtration procedures.

Other warnings/precautions:

• Absorption: Systemic absorption of betaxolol and adverse effects may occur with ophthalmic use, including severe respiratory and cardiac reactions.

Monitoring Parameters

Intraocular pressure

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted with the ophthalmic drops. When administered orally, betaxolol crosses the placenta and can be detected in the amniotic fluid and umbilical cord blood (Morselli 1990). The amount of betaxolol available systemically following topical application of the ophthalmic drops is significantly less in comparison to oral doses (Vainio-Jylhä 2001). However, the same adverse effects observed with systemic administration may occur. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctual occlusion to decrease potential exposure to the fetus (Johnson 2001; Salim 2014; Samples 1988).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience short-term pain. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, shortness of breath, excessive weight gain, swelling of arms or legs, bradycardia, or muscle weakness (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Hide