Levobunolol

Mechanism-of-action class: Adrenergic beta-Antagonists.

• Levobunolol hydrochloride ophthalmic solution has been shown to be effective in lowering intraocular pressure and may be used in patients with chronic open-angle glaucoma or ocular hypertension.ICD-10: H40.059, H40.9

• Levobunolol hydrochloride ophthalmic solution is contraindicated in those individuals with bronchial asthma, or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS ); sinus bradycardia; second and third degree atrioventricular block; overt cardiac failure (see WARNINGS ); cardiogenic shock; or hypersensitivity to any component of these products.contraindicated

The recommended starting dose is one to two drops of levobunolol hydrochloride ophthalmic solution, 0.5% in the affected eye(s) once a day. In patients with more severe or uncontrolled glaucoma, levobunolol hydrochloride ophthalmic solution, 0.5% can be administered twice a day. As with any new medication, careful monitoring of patients is advised. Dosages above one drop of levobunolol hydrochloride ophthalmic solution, 0.5% twice a day are not generally more effective. If the patient's IOP is not at a satisfactory level on this regimen, concomitant therapy with other ophthalmic IOP-lowering agents can be instituted. Patients should not typically use two or more topical ophthalmic beta-adrenergic blocking agents simultaneously.

As with other topically applied ophthalmic drugs, levobunolol hydrochloride ophthalmic solution may be absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported with topical application of beta-adrenergic blocking agents (see CONTRAINDICATIONS ). Additionally, ophthalmic beta-blockers may impair compensatory tachycardia and increase risk of hypotension. Cardiac Failure Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe failure. In Patients Without a History of Cardiac Failure Continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. At the first sign or symptom of cardiac failure, levobunolol hydrochloride ophthalmic solution should be discontinued (see CONTRAINDICATIONS ). Potentiation of Vascular Insufficiency Levobunolol hydrochloride ophthalmic solution may potentiate syndromes associated with vascular insufficiency (i.e. Raynaud’s phenomenon), and therefore, should be used with caution in these patients.

In clinical trials the use of levobunolol hydrochloride ophthalmic solution has been associated with transient ocular burning and stinging in up to 1 in 3 patients, and with blepharoconjunctivitis in up to 1 in 20 patients. Decreases in heart rate and blood pressure have been reported (see CONTRAINDICATIONS and WARNINGS ). The following adverse reactions have been reported rarely with the use of levobunolol hydrochloride ophthalmic solution: iridocyclitis, headache, transient ataxia, dizziness, lethargy, urticaria, and pruritus. Decreased corneal sensitivity has been noted in a small number of patients. Although levobunolol has minimal membrane-stabilizing activity, there remains a possibility of decreased corneal sensitivity after prolonged use. The following additional adverse reactions have been reported either with levobunolol hydrochloride ophthalmic solution or ophthalmic use of other beta-adrenergic receptor blocking agents: BODY AS A WHOLE: Headache, asthenia, chest pain. CARDIOVASCULAR: Bradycardia, arrhythmia, hypotension, syncope, heart block, cerebral vascular accident, cerebral ischemia, congestive heart failure, palpitation, cardiac arrest. DIGESTIVE: Nausea, diarrhea. PSYCHIATRIC: Depression, confusion, increase in signs and symptoms of myasthenia gravis, paresthesia. SKIN: Hypersensitivity, including localized and generalized rash, alopecia, Stevens-Johnson Syndrome. RESPIRATORY: Bronchospasm (predominantly in patients with pre-existing bronchospastic disease), respiratory failure, dyspnea, nasal congestion. UROGENITAL: Impotence.

Pregnancy Fetotoxicity (as evidenced by a greater number of resorption sites) has been observed in rabbits when doses of levobunolol hydrochloride equivalent to 200 and 700 times the recommended dose for the treatment of glaucoma were given. No fetotoxic effects have been observed in similar studies with rats at up to 1,800 times the human dose for glaucoma. Teratogenic studies with levobunolol in rats at doses up to 25 mg/kg/day (1,800 times the recommended human dose for glaucoma) showed no evidence of fetal malformations. There were no adverse effects on postnatal development of offspring. It appears when results from studies using rats and studies with other beta-adrenergic blockers are examined, that the rabbit may be a particularly sensitive species. There are no adequate and well-controlled studies in pregnant women. Levobunolol hydrochloride ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

No data are available regarding overdosage in humans. Should accidental ocular overdosage occur, flush eye(s) with water or normal saline. If accidentally ingested, efforts to decrease further absorption may be appropriate (gastric lavage). The most common signs and symptoms to be expected with overdosage with administration of a systemic beta-adrenergic blocking agent are symptomatic bradycardia, hypotension, bronchospasm, and acute cardiac failure. Should these symptoms occur, discontinue levobunolol hydrochloride ophthalmic solution therapy and initiate appropriate supportive therapy. The following supportive measures should be considered: 1. Symptomatic bradycardia: Use atropine sulfate intravenously in a dosage of 0.25 mg to 2 mg to induce vagal blockade. If bradycardia persists, intravenous isoproterenol hydrochloride should be administered cautiously. In refractory cases the use of a transvenous cardiac pacemaker should be considered. 2. Hypotension: Use sympathomimetic pressor drug therapy, such as dopamine, dobutamine or levarterenol. In refractory cases the use of glucagon hydrochloride may be useful. 3. Bronchospasm: Use isoproterenol hydrochloride.

• Mar 4, 1994ANDAANDA074326Bausch And Lomb Inc

1. 1Nausea1212%
2. 2Eye Irritation88.2%
3. 3Fatigue88.2%
4. 4Headache88.2%
5. 5Acute Generalised Exanthematous Pustulosis77.2%
6. 6Dizziness77.2%
7. 7Iridocyclitis77.2%
8. 8Diarrhoea66.2%
9. 9Asthenia55.2%
10. 10Eye Pain55.2%
11. 11Ocular Hyperaemia55.2%
12. 12Abdominal Pain44.1%
13. 13Depressed Level Of Consciousness44.1%
14. 14Hypertension44.1%
15. 15Pain44.1%

Recent PubMed references pinned to Levobunolol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Levobunolol-imprinted polymer: a theoretical study.
  Journal of molecular modeling · 2023 · Maia PP, Guimarães L, Nascimento CS Jr, et al.
  PMID 37861808DOI 10.1007/s00894-023-05757-4
• Identification of potential biomarkers and pathogenesis in neutrophil-predominant severe asthma: A comprehensive bioinformatics analysis.
  Medicine · 2022 · Xu S, Chen Z, Ge L, et al.
  PMID 36197221DOI 10.1097/MD.0000000000030661
• Superior oblique myokymia treated with levobunolol.
  Journal of AAPOS : the official publication of the American Association for Pediatric Ophthalmology and Strabismus · 2018 · Zhang M, Gilbert AL, Hunter DG, et al.
  PMID 29277497DOI 10.1016/j.jaapos.2017.08.010
• Ocular Metabolism of Levobunolol: Historic and Emerging Metabolic Pathways.
  Drug metabolism and disposition: the biological fate of chemicals · 2016 · Argikar UA, Dumouchel JL, Dunne CE, et al.
  PMID 27190057DOI 10.1124/dmd.116.070458
• Allergic contact dermatitis caused by timolol with cross-sensitivity to levobunolol.
  Contact dermatitis · 2015 · Horcajada-Reales C, Rodríguez-Soria VJ, Suárez-Fernández R, et al.
  PMID 26227808DOI 10.1111/cod.12448
• Bradyarrhythmias secondary to topical levobunolol hydrochloride solution.
  Clinical interventions in aging · 2014 · Lin L, Wang Y, Chen Y, et al.
  PMID 25342892DOI 10.2147/CIA.S69420
• Effects of topical 0.5% levobunolol alone or in association with 2% dorzolamide compared with a fixed combination of 0.5% timolol and 2% dorzolamide on intraocular pressure and heart rate in dogs without glaucoma.
  Veterinary therapeutics : research in applied veterinary medicine · 2010 · Scardillo A, Pugliese M, De Majo M, et al.
  PMID 20960417
• Comparison of effects of topical levobunolol to a combination of timolol-dorzolamide on intraocular pressure and pulse rate of healthy dogs.
  Veterinary research communications · 2009 · Pugliese M, Scardillo A, Niutta PP, et al.
  PMID 19626454DOI 10.1007/s11259-009-9273-9

The 2 most recently updated of 2 ClinicalTrials.gov registrations naming Levobunolol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Morphological and Functional Evaluation of Irvine-Gass Syndrome
  Completed · Observational · 50 enrolled · Medical University of Vienna
  NCT01504074updated 2015-09-24
• Coreg and HSRs-Updated Analysis
  Completed · Observational · 1 enrolled · GlaxoSmithKline
  NCT01316952updated 2015-04-15

Frequently asked questions

How does Levobunolol work?

Mechanism-of-action class: Adrenergic beta-Antagonists.

What is Levobunolol used for?

According to FDA labeling, Levobunolol carries indications including: Levobunolol hydrochloride ophthalmic solution has been shown to be effective in lowering intraocular pressure and may be used in patients with chronic open-angle glaucoma or ocular hypertension.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Levobunolol?

Levobunolol is classified as Beta blocking agents, beta-Adrenergic Blocker, Adrenergic beta-Antagonists, Decreased Intraocular Aqueous Secretion.

What are the brand names for Levobunolol?

Levobunolol is marketed under brand names including Betagan.

What are the contraindications for Levobunolol?

Levobunolol labeling lists contraindications including: Levobunolol hydrochloride ophthalmic solution is contraindicated in those individuals with bronchial asthma, or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS ); sinus bradycardia; second and third degree atrioventricular block; overt cardiac failure (see WARNINGS ); cardiogenic shock; or hypersensitivity to any component of these products.. Always consult the full prescribing information and a clinician.