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Levobunolol (ophthalmic): Drug information

Levobunolol (ophthalmic): Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Levobunolol (ophthalmic): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Pharmacologic Category
  • Beta-Blocker, Nonselective;
  • Ophthalmic Agent, Antiglaucoma
Dosing: Adult
Elevated intraocular pressure

Elevated intraocular pressure: Ophthalmic: Instill 1 to 2 drops into affected eye(s) once daily; may increase to 1 drop twice daily in patients with severe or uncontrolled glaucoma. Doses >1 drop twice daily are generally not more effective.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Ophthalmic: Burning sensation of eyes (≤33%), stinging of eyes (≤33%)

1% to 10%: Ophthalmic: Blepharoconjunctivitis (5%)

Frequency not defined:

Cardiovascular: Bradycardia, cardiac arrhythmia, cardiac failure, cerebral ischemia, cerebrovascular accident, chest pain, heart block, hypotension, palpitations, syncope

Central nervous system: Ataxia (transient), confusion, depression, dizziness, exacerbation of myasthenia gravis, foreign body sensation of eye, headache, lethargy, paresthesia

Dermatologic: Alopecia, pruritus, skin rash, Stevens-Johnson syndrome, urticaria

Endocrine & metabolic: Hypoglycemia (masked)

Gastrointestinal: Diarrhea, nausea

Genitourinary: Impotence

Hypersensitivity: Hypersensitivity reaction

Neuromuscular & skeletal: Weakness

Ophthalmic: Blepharoptosis, decreased corneal sensitivity, diplopia, iridocyclitis, keratitis, ocular allergy, visual disturbance

Respiratory: Bronchospasm, dyspnea, nasal congestion, respiratory failure

Contraindications

Hypersensitivity to levobunolol or any component of the formulation; bronchial asthma or history of bronchial asthma; severe COPD; sinus bradycardia; second- or third-degree atrioventricular block; overt heart failure; cardiogenic shock

Warnings/Precautions

Concerns related to adverse events:

• Anaphylactic reactions: Instill with caution in patients with history of severe anaphylaxis to a variety of 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.

• Choroidal detachment: Beta-blockade and/or other aqueous suppressive therapy has been associated with choroidal detachment following filtration procedures.

Disease-related concerns:

• Cerebrovascular disease: Use with caution in cerebrovascular insufficiency; consider alternative therapy for patients with signs/symptoms of decreased cerebral blood flow after therapy initiation.

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

• Heart failure: Use with caution in patients with compensated heart failure and monitor for a worsening of the condition; may lead to heart failure in patients without a history of heart failure (discontinue use at first sign or symptoms of heart failure). Use is contraindicated in overt heart failure. In a scientific statement from the AHA, levobunolol has been determined to be an agent that may exacerbate underlying myocardial dysfunction (magnitude: major) (AHA [Page 2016]).

• Myasthenia gravis: Use with caution in patients with myasthenia gravis; may worsen disease or other myasthenic symptoms (eg, diplopia, ptosis, generalized weakness).

• Peripheral vascular disease and Raynaud disease: Can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease or Raynaud disease. Use with caution and monitor for progression of arterial obstruction.

• Respiratory disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring. Severe respiratory reactions, including fatalities due to bronchospasm in patients with asthma, have been reported with ophthalmic use. Use is contraindicated in bronchial asthma or history of bronchial asthma and severe COPD.

• 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: Some products may contain benzalkonium chloride, which may be absorbed by soft contact lenses. Remove lens prior to administration and wait 15 minutes before reinserting.

Dosage form specific issues:

• Metabisulfite: Ophthalmic solutions may contain metabisulfite, which may cause allergic reactions in susceptible individuals.

Other warnings/precautions:

• Absorption: Systemic absorption of levobunolol and adverse effects may occur with ophthalmic use, including respiratory and cardiovascular effects (including bradycardia and/or hypotension). Beta-blocker therapy should not be withdrawn abruptly in order to avoid acute tachycardia, hypertension, and/or ischemia.

• Appropriate use: Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction). Concomitant use of 2 topical beta-blockers is not recommended. Multidose vials have been associated with development of bacterial keratitis; avoid contamination.

• Surgery: May block systemic effects of beta agonists (eg, epinephrine, norepinephrine); notify anesthesiologist if patient is receiving ophthalmic beta-blocker therapy. Patients undergoing planned major surgery should be gradually tapered off therapy (if possible) prior to procedure. If necessary during surgery, effects of beta-blocker therapy may be reversed by adrenergic agonists.

Dosage Forms: US

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

Solution, Ophthalmic, as hydrochloride:

Generic: 0.5% (5 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Levobunolol HCl Ophthalmic)

0.5% (per mL): $4.84

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

For topical ophthalmic use only. Wash hands before and after use. Some solutions contain benzalkonium chloride; remove contact lens prior to administration. Wait 15 minutes before reinserting. Do not touch tip of applicator to eye or other surfaces. Do not administer 2 or more ophthalmic beta-adrenergic blocking agents simultaneously.

Use: Labeled Indications

Elevated intraocular pressure: Treatment of elevated intraocular pressure in patients with ocular hypertension or chronic open-angle glaucoma.

Medication Safety Issues
Sound-alike/look-alike issues:

Levobunolol may be confused with levocabastine

Betagan may be confused with Betadine, Betoptic S

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Amiodarone: May increase bradycardic effects of Beta-Blockers. Possibly to the point of cardiac arrest. Amiodarone may increase serum concentration of Beta-Blockers. Risk C: Monitor

Antidiabetic Agents: Beta-Blockers (Nonselective) may increase hypoglycemic effects of Antidiabetic Agents. Beta-Blockers (Nonselective) may increase adverse/toxic effects of Antidiabetic Agents. Specifically, beta-blockers may mask the hypoglycemic symptoms of antidiabetic agents. Risk C: Monitor

Beta2-Agonists: Beta-Blockers (Nonselective) may decrease bronchodilatory effects of Beta2-Agonists. Risk X: Avoid

Bradycardia-Causing Agents: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor

Cafedrine: May increase bradycardic effects of Beta-Blockers. Beta-Blockers may decrease therapeutic effects of Cafedrine. Risk C: Monitor

Cannabis: Beta-Blockers may increase adverse/toxic effects of Cannabis. Specifically, the risk of hypoglycemia may be increased. Risk C: Monitor

Ceritinib: Bradycardia-Causing Agents may increase bradycardic effects of Ceritinib. Management: If this combination cannot be avoided, monitor patients for evidence of symptomatic bradycardia, and closely monitor blood pressure and heart rate during therapy. Risk D: Consider Therapy Modification

Cholinergic Agonists: Beta-Blockers may increase adverse/toxic effects of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Risk C: Monitor

DOBUTamine: Beta-Blockers may decrease therapeutic effects of DOBUTamine. Risk C: Monitor

Dronedarone: May increase bradycardic effects of Beta-Blockers. Dronedarone may increase 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. Increase monitoring for clinical response and adverse effects. Risk D: Consider Therapy Modification

EPHEDrine (Systemic): Beta-Blockers may decrease therapeutic effects of EPHEDrine (Systemic). Risk C: Monitor

EPINEPHrine (Nasal): Beta-Blockers (Nonselective) may increase hypertensive effects of EPINEPHrine (Nasal). Risk C: Monitor

EPINEPHrine (Oral Inhalation): Beta-Blockers (Nonselective) may increase hypertensive effects of EPINEPHrine (Oral Inhalation). Risk C: Monitor

EPINEPHrine (Systemic): Beta-Blockers (Nonselective) may increase hypertensive effects of EPINEPHrine (Systemic). Risk C: Monitor

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Beta-Blockers may increase vasoconstricting effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor

Etilefrine: Beta-Blockers may decrease therapeutic effects of Etilefrine. Etilefrine may increase bradycardic effects of Beta-Blockers. Risk C: Monitor

Etofylline: Beta-Blockers may decrease therapeutic effects of Etofylline. Risk X: Avoid

Etrasimod: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor

Fexinidazole: Bradycardia-Causing Agents may increase arrhythmogenic effects of Fexinidazole. Risk X: Avoid

Fingolimod: Bradycardia-Causing Agents may increase bradycardic effects of Fingolimod. Management: Consult with the prescriber of any bradycardia-causing agent to see if the agent could be switched to an agent that does not cause bradycardia prior to initiating fingolimod. If combined, perform continuous ECG monitoring after the first fingolimod dose. Risk D: Consider Therapy Modification

Grass Pollen Allergen Extract (5 Grass Extract): Beta-Blockers may increase adverse/toxic effects 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. Management: Consider alternatives to either grass pollen allergen extract (5 grass extract) or beta-blockers in patients with indications for both agents. Canadian product labeling specifically lists this combination as contraindicated. Risk D: Consider Therapy Modification

Insulin: Beta-Blockers (Nonselective) may increase hypoglycemic effects of Insulin. Beta-Blockers (Nonselective) may decrease therapeutic effects of Insulin. Risk C: Monitor

Isoproterenol: Beta-Blockers may decrease therapeutic effects of Isoproterenol. Risk C: Monitor

Ivabradine: Bradycardia-Causing Agents may increase bradycardic effects of Ivabradine. Risk C: Monitor

Lacosamide: Bradycardia-Causing Agents may increase AV-blocking effects of Lacosamide. Risk C: Monitor

Landiolol: Bradycardia-Causing Agents may increase bradycardic effects of Landiolol. Risk X: Avoid

Mavacamten: Beta-Blockers may increase adverse/toxic effects of Mavacamten. Specifically, negative inotropic effects may be increased. Risk C: Monitor

Methacholine: Beta-Blockers may increase adverse/toxic effects of Methacholine. Risk C: Monitor

Midodrine: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor

Mivacurium: Beta-Blockers may increase therapeutic effects of Mivacurium. Risk C: Monitor

NIFEdipine (Topical): May increase adverse/toxic effects of Beta-Blockers. Risk C: Monitor

NIFEdipine: May increase hypotensive effects of Beta-Blockers. NIFEdipine may increase negative inotropic effects of Beta-Blockers. Risk C: Monitor

Nitrendipine: May increase therapeutic effects of Beta-Blockers. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents (Topical): May decrease therapeutic effects of Beta-Blockers. Risk C: Monitor

Opipramol: Beta-Blockers may increase serum concentration of Opipramol. Opipramol may increase serum concentration of Beta-Blockers. Risk C: Monitor

Ozanimod: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor

Ponesimod: Bradycardia-Causing Agents may increase bradycardic effects of Ponesimod. Management: Avoid coadministration of ponesimod with drugs that may cause bradycardia when possible. If combined, monitor heart rate closely and consider obtaining a cardiology consult. Do not initiate ponesimod in patients on beta-blockers if HR is less than 55 bpm. Risk D: Consider Therapy Modification

Reserpine: May increase hypotensive effects of Beta-Blockers. Reserpine may increase bradycardic effects of Beta-Blockers. Risk C: Monitor

Rivastigmine: May increase bradycardic effects of Beta-Blockers. Risk X: Avoid

Siponimod: Bradycardia-Causing Agents may increase bradycardic effects of Siponimod. Management: Avoid coadministration of siponimod with drugs that may cause bradycardia. If combined, consider obtaining a cardiology consult regarding patient monitoring. Risk D: Consider Therapy Modification

Succinylcholine: Beta-Blockers may increase neuromuscular-blocking effects of Succinylcholine. Risk C: Monitor

Sulfonylureas: Beta-Blockers (Nonselective) may increase hypoglycemic effects of Sulfonylureas. Beta-Blockers (Nonselective) may decrease therapeutic effects of Sulfonylureas. Risk C: Monitor

Tasimelteon: Beta-Blockers may decrease therapeutic effects of Tasimelteon. Management: Consider avoiding nighttime administration of beta-blockers during tasimelteon therapy due to the potential for reduced tasimelteon efficacy. Risk D: Consider Therapy Modification

Theodrenaline: May increase bradycardic effects of Beta-Blockers. Beta-Blockers may decrease therapeutic effects of Theodrenaline. Risk C: Monitor

Theophylline Derivatives: Beta-Blockers (Nonselective) may decrease bronchodilatory effects of Theophylline Derivatives. Risk C: Monitor

White Birch Allergen Extract: Beta-Blockers may increase adverse/toxic effects of White Birch Allergen Extract. Specifically, beta-blockers may reduce the effectiveness of beta-agonists that may be required to treat systemic reactions to white birch allergen extract. Risk X: Avoid

Pregnancy Considerations

The same adverse effects observed with systemic administration of beta-blockers may occur following ophthalmic use of levobunolol. If ophthalmic agents are needed for the treatment of glaucoma during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Johnson 2001; Salim 2014; Samples 1988).

Breastfeeding Considerations

It is not known if levobunolol is present in breast milk; however, systemic beta-blockers and topical timolol are present in breast milk. The minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the breastfeeding infant (Johnson 2001, Salim 2014, Samples 1988). The manufacturer recommends that caution be exercised when administering levobunolol to breastfeeding women.

Monitoring Parameters

Intraocular pressure, heart rate, funduscopic exam, visual field testing

Mechanism of Action

Blocks both beta1- and beta2-adrenergic receptors and reduces intraocular pressure by reducing aqueous humor production or possibly increases the outflow of aqueous humor.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Within1 hour

Peak effect: 2 to 6 hours

Duration: Up to 24 hours

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Betagan;
  • (AR) Argentina: Betagan | Levunolol;
  • (AT) Austria: Vistagan;
  • (AU) Australia: Betagan;
  • (BD) Bangladesh: Betagan;
  • (BE) Belgium: Betagan;
  • (BR) Brazil: B tablock | Betagan;
  • (CH) Switzerland: Vistagan;
  • (CL) Chile: Betagen;
  • (CN) China: Betagan | Levobunolol;
  • (CO) Colombia: Vistagan;
  • (CZ) Czech Republic: Vistagan;
  • (DE) Germany: Vistagan;
  • (DO) Dominican Republic: Betagan;
  • (EC) Ecuador: Betagan;
  • (EE) Estonia: Betagan;
  • (EG) Egypt: Betagan | Mascglucom;
  • (ES) Spain: Betagan;
  • (FI) Finland: Betagan;
  • (FR) France: Betagan;
  • (GB) United Kingdom: Betagan | Levobunolol | Levobunolol kent;
  • (GR) Greece: Levobunolol | Vistagan;
  • (HK) Hong Kong: Betagan;
  • (HR) Croatia: Vistagan;
  • (HU) Hungary: Huma-levobunolol | Vistagan;
  • (IE) Ireland: Betagan;
  • (IL) Israel: Betagan;
  • (IN) India: Betagan | Loben;
  • (IT) Italy: Vistagan;
  • (JO) Jordan: Betagan;
  • (JP) Japan: Mirol;
  • (KE) Kenya: Betagan;
  • (KR) Korea, Republic of: Betagan | Glabunol;
  • (KW) Kuwait: Betagan;
  • (LB) Lebanon: Betagan;
  • (LT) Lithuania: Betagan;
  • (LU) Luxembourg: Betagan;
  • (LV) Latvia: Betagan;
  • (MA) Morocco: Betagan;
  • (MX) Mexico: Betagan;
  • (MY) Malaysia: Betagan;
  • (NL) Netherlands: Betagan;
  • (NZ) New Zealand: Betagan | Levobunolol;
  • (PE) Peru: Vistagan;
  • (PH) Philippines: Betagan;
  • (PK) Pakistan: Betagan | Levob | Levoptic | Levosan | Ophth-Levo | Orbunol | Vistagan | Voben;
  • (PL) Poland: Vistagan;
  • (PR) Puerto Rico: Akbeta | Betagan | Levobunolol HCL;
  • (PT) Portugal: Betagan;
  • (SA) Saudi Arabia: Betagan;
  • (SE) Sweden: Betagan;
  • (SG) Singapore: Betagan;
  • (SK) Slovakia: Vistagan;
  • (TH) Thailand: Betagan;
  • (TN) Tunisia: Betagan;
  • (TR) Turkey: Betagan;
  • (TW) Taiwan: Bunolgan | Vistagan;
  • (UY) Uruguay: Betagan;
  • (VE) Venezuela, Bolivarian Republic of: Vistagan;
  • (ZA) South Africa: Betagan | Betagan c;
  • (ZW) Zimbabwe: Betagan
  1. Betagan (levobunolol) [prescribing information]. Madison, NJ: Allergan USA Inc; September 2021.
  2. Johnson SM, Martinez M, and Freedman S, "Management of Glaucoma in Pregnancy and Lactation," Surv Ophthalmol, 2001, 45(5):449-54. [PubMed 11274697]
  3. Page RL 2nd, O'Bryant CL, Cheng D, et al; American Heart Association Clinical Pharmacology and Heart Failure and Transplantation Committees of the Council on Clinical Cardiology; Council on Cardiovascular Surgery and Anesthesia; Council on Cardiovascular and Stroke Nursing; and Council on Quality of Care and Outcomes Research. Drugs That May Cause or Exacerbate Heart Failure: A Scientific Statement From the American Heart Association [published correction appears in Circulation. 2016;134(12):e261]. Circulation. 2016;134(6):e32-e69. [PubMed 27400984]
  4. Salim S. Glaucoma in pregnancy. Curr Opin Ophthalmol. 2014;25(2):93-97. [PubMed 24469077]
  5. Samples JR and Meyer SM, “Use of Ophthalmic Medications in Pregnant and Nursing Women,” Am J Ophthalmol, 1988, 106(5):616-23. [PubMed 2903673]
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