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- l-Bunolol Hydrochloride
- Levobunolol Hydrochloride
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Ophthalmic, as hydrochloride:
Betagan: 0.5% (5 mL [DSC], 10 mL, 15 mL [DSC])
Generic: 0.25% (5 mL [DSC], 10 mL [DSC]); 0.5% (5 mL, 10 mL, 15 mL)
Brand Names: U.S.
- Beta-Adrenergic Blocker, Nonselective
- Ophthalmic Agent, Antiglaucoma
A nonselective beta-adrenergic blocking agent that lowers intraocular pressure by reducing aqueous humor production and possibly increases the outflow of aqueous humor
Onset of Action
Within 1 hour; Peak effect: 2-6 hours
Duration of Action
Up to 24 hours
Use: Labeled Indications
To lower intraocular pressure in chronic open-angle glaucoma or ocular hypertension
Hypersensitivity to levobunolol or any component of the formulation; bronchial asthma, severe COPD, sinus bradycardia, second- or third-degree AV block, overt cardiac failure, cardiogenic shock
Glaucoma (open-angle, chronic), intraocular hypertension: Ophthalmic:
0.25% solution: Instill 1-2 drops into affected eye(s) twice daily
0.5% solution: Instill 1-2 drops into affected eye(s) once daily; may increase to 1 drop twice daily in patients with severe or uncontrolled glaucoma; Maximum dose: Doses >1 drop twice daily (0.5%) are generally not more effective.
Refer to adult dosing.
Dosing: Renal Impairment
No dosage adjustment provided in manufacturer’s labeling.
Dosing: Hepatic Impairment
No dosage adjustment provided in manufacturer’s labeling.
For topical ophthalmic use only. Wash hands before and after use. Apply gentle pressure to lacrimal sac for 1 minute following instillation. Some solutions contain benzalkonium chloride; remove contact lens prior to administration. Do not touch tip of applicator to eye or other surfaces.
Store at 15°C to 30°C (59°F to 86°F). Protect from light.
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
Beta2-Agonists: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Beta2-Agonists. Avoid combination
Bradycardia-Causing Agents: May enhance the bradycardic effect of other Bradycardia-Causing Agents. Monitor therapy
Bretylium: May enhance the bradycardic effect of Bradycardia-Causing Agents. Bretylium may also enhance atrioventricular (AV) blockade in patients receiving AV blocking agents. Monitor therapy
Bupivacaine: Beta-Blockers may increase the serum concentration of Bupivacaine. Monitor therapy
Ceritinib: Bradycardia-Causing Agents may enhance the bradycardic effect 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. Avoid combination
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
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
Ivabradine: Bradycardia-Causing Agents may enhance the bradycardic effect of Ivabradine. Monitor therapy
Lacosamide: Bradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide. 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
Methoxyflurane: May enhance the hypotensive effect of Beta-Blockers. Monitor therapy
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
Opioids (Anilidopiperidine): May enhance the bradycardic effect of Beta-Blockers. Opioids (Anilidopiperidine) may enhance the hypotensive effect of Beta-Blockers. Monitor therapy
Regorafenib: May enhance the bradycardic effect of Beta-Blockers. Monitor therapy
Reserpine: May enhance the hypotensive effect of Beta-Blockers. Monitor therapy
Rivastigmine: May enhance the bradycardic effect of Beta-Blockers. Avoid combination
Ruxolitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Management: Ruxolitinib Canadian product labeling recommends avoiding use with bradycardia-causing agents to the extent possible. Monitor therapy
Theophylline Derivatives: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Theophylline Derivatives. Consider therapy modification
Tofacitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Monitor therapy
>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, headache, lethargy, paresthesia
Dermatologic: Alopecia, erythema, pruritus, skin rash, Stevens-Johnson syndrome, urticaria
Endocrine & metabolic: Hypoglycemia (masked)
Gastrointestinal: Diarrhea, nausea
Hypersensitivity: Hypersensitivity reaction
Neuromuscular & skeletal: Weakness
Ophthalmic: Blepharoptosis, conjunctivitis, decreased corneal sensitivity, diplopia, iridocyclitis, keratitis, visual disturbance
Respiratory: Bronchospasm, dyspnea, nasal congestion, respiratory failure
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.
• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring.
• Cerebrovascular insufficiency: Due to a possible effect on blood pressure and pulse, use with caution in patients with cerebrovascular insufficiency.
• Conduction abnormality: Consider pre-existing conditions such as sick sinus syndrome before initiating.
• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms.
• Heart failure (HF): Use with caution in patients with compensated HF and monitor for a worsening HF (diminished myocardial contractility may lead to more severe failure); patients without a history of HF should discontinue use with the first symptoms of heart failure. In a scientific statement from the American Heart Association, 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.
• Peripheral vascular disease (PVD): Use with caution in patients with PVD (including Raynaud's).
• Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression.
• Thyroid disease: May mask signs of hyperthyroidism (eg, tachycardia). If thyrotoxicosis is suspected, carefully manage and monitor; abrupt beta-adrenergic blocker withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm.
Concurrent drug therapy issues:
• Beta-blockers: Concomitant use with other topical beta-blockers should generally be avoided; monitor for increased effects (systemic or intraocular) with concomitant use of a systemic beta-blocker.
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Contact lens wearers: Some products contain benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration.
• Elderly: Use with caution in the elderly with other disease states or syndromes that may be affected by a beta-blocker (CHF, COPD, etc); systemic absorption may occur with ophthalmic administration; monitor closely.
Dosage form specific issues:
• Metabisulfite: Ophthalmic solutions contain metabisulfite, which may cause allergic reactions in some individuals.
• 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. Patients undergoing major surgery should be gradually tapered off therapy prior to procedure.
• Appropriate use: Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction).
Intraocular pressure, heart rate, funduscopic exam, visual field testing
Pregnancy Risk Factor
Adverse events have been observed in some animal reproduction studies. 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 punctual occlusion to decrease potential exposure to the fetus (Johnson 2001; Salim 2014; Samples 1988).
• 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 burning or stinging. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, muscle weakness, severe dizziness, passing out, bradycardia, shortness of breath, excessive weight gain, or swelling of arms or legs (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 healthcare 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.
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- Drug class: ophthalmic glaucoma agents
Other brands: Betagan