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Levobunolol

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Last Updated: 05 November 2020

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General | Latest Info

Levobunolol

Chemical and physical data
3D model ( JSmol )Interactive image
FormulaC 17 H 25 N O 3
Melting point209 to 211 C (408 to 412 F) ( hydrochloride )
Molar mass291.391 gmol 1
Solubility in watersoluble (hydrochloride)
Clinical data
AHFS / Drugs.comMonograph
ATC codeS01ED03 ( WHO )
MedlinePlusa686011
Pregnancy categoryC
Routes of administrationTopical ( eye drops )
Trade namesAKBeta, Betagan, Vistagan, others
Identifiers
CAS Number47141-42-4 Y
ChEBICHEBI:6438 Y
ChEMBLChEMBL1201237 N
ChemSpider36089 Y
CompTox Dashboard ( EPA )DTXSID1043833
DrugBankDB01210 Y
IUPHAR/BPS570
KEGGD08115 Y
PubChem CID39468
UNIIG6317AOI7K
Legal status
Legal statusUS : -only
Pharmacokinetic data
Bioavailability7.5% (rabbit eye)
Duration of actionup to 16 hours
Elimination half-life6 hours
Excretionmostly renal
Metabolitesdihydrolevobunolol (equally active)
Onset of action1 hour

LEVOBUNOLOL hydrochloride and timolol maleate are being compared in an ongoing, double-mask, randomized study OF 141 PATIENTS WITH ocular hypertension or CHRONIC open-angle glaucoma. Baseline intraocular pressure in three treatment groups range from 26 to 27 mm Hg. During the first 15 months of study, two drugs have not proven to be significantly different in ocular hypotensive efficacy, WITH overall mean IOP decreases OF 6. 8 to 7. 6 mm Hg. In addition, two concentrations of LEVOBUNOLOL have been equally effective in controlling IOP. Neither drug has been associated with any significant ocular side effects. Both drugs have produced significant decreases in the mean heart rate. The effect on mean blood pressure has been less pronounced: overall decreases have been less THAN 4 mm Hg for both systolic and diastolic blood pressure. Results of this ongoing study suggest that LEVOBUNOLOL IS AS effective and AS safe AS timolol for long-term control OF IOP.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Contraindications

Levobunolol IS OPHTHALMIC BETA-blocker. It IS 'nonselective'. Levobunolol IS a levorotatory isomer OF bunolol, WHICH IS structurally similar to propranolol. Levobunolol has 60-fold and 3-fold greater potency compared WITH dextrorotatory isomer and racemic compound, respectively. Only levo isomer IS Use clinically AS OPHTHALMIC agent for treatment of increased IOP due to open-angle glaucoma or ocular hypertension. Levobunolol was approved by the FDA in December 1985. During clinical trials, transient ocular irritation occurred in up to 33 % OF PATIENTS using Levobunolol. Blepharoconjunctivitis was reported in up to 1 in 20 PATIENTS. ADVERSE effects such as foreign BODY sensation in the eye, keratitis, blepharoptosis, and visual disturbances INCLUDING refractive changes have been reported WITH Use OF OPHTHALMIC BETA-BLOCKERS. OPHTHALMIC BETA-BLOCKERS may potentiate certain myasthenic symptoms, INCLUDING diplopia and ptosis. Rarely, uveitis or iridocyclitis have been reported WITH Levobunolol Use. Prolong Use has been associated WITH decreased corneal sensitivity in a small number OF PATIENTS. Systemic REACTIONS may occur WITH OPHTHALMIC administration OF Levobunolol. Although ADVERSE effects of Levobunolol are generally MILD and temporary, chest pain, sinus Bradycardia, arrhythmia exacerbation, hypotension, syncope, AV block, cerebral vascular accident, cerebral ischemia, stroke, congestive heart failure, palpitations, and cardiac arrest have been reported WITH Use OF OPHTHALMIC BETA-BLOCKERS. Rarely, heart failure associated death been reported WITH topical application OF BETA-BLOCKERS. Levobunolol SHOULD be discontinued immediately if signs or symptoms of heart failure present. Consider alternative therapy if signs or symptoms suggesting reduced cerebral blood flow develop. Headache, transient ataxia, dizziness, and lethargy have been rarely reported WITH use OF Levobunolol. OTHER centrally-mediate effects reported WITH Use OF OPHTHALMIC BETA-BLOCKERS include asthenia, Depression, confusion, paresthesias, and increase in signs and symptoms OF myasthenia gravis. BETA-BLOCKERS may potentiate muscle weakness consistent WITH certain myasthenic symptoms. Systemic REACTIONS may occur WITH OPHTHALMIC administration OF Levobunolol. Although ADVERSE effects OF Levobunolol are generally MILD and temporary, nasal congestion, dyspnea, Bronchospasm, and RESPIRATORY arrest / failure have been reported WITH Use OF OPHTHALMIC BETA-BLOCKERS. Rarely, death due to Bronchospasm in asthmatic PATIENTS occur. Hypersensitivity REACTIONS INCLUDING rash, alopecia, and Stevens-Johnson Syndrome have been reported WITH Use OF OPHTHALMIC BETA-BLOCKERS. Urticaria and pruritus have been rarely reported WITH Levobunolol Use. Levobunolol OPHTHALMIC SOLUTION contains sodium metabisulfite, WHICH may cause anaphylaxis / anaphylactoid REACTIONS in susceptible individuals. Impotence has been reported WITH Use OF OPHTHALMIC BETA-BLOCKERS. Nausea and diarrhea have been reported WITH use OF OPHTHALMIC BETA-BLOCKERS. AS levobunololol has been shown to be absorb systemically, all OF precautions and CONTRAINDICATIONS pertaining to systemically-administer BETA-BLOCKERS SHOULD be carefully considered prior to using Levobunolol. Levobunolol SHOULD not be used in PATIENTS WITH preexisting cardiac DISEASE, such AS severe Bradycardia, sick sinus Syndrome, advance AV block, cardiogenic shock, coronary artery DISEASE, vasospastic angina, or overt congestive heart failure, particularly those WITH severe leave ventricular dysfunction. Treatment WITH Levobunolol SHOULD be discontinued at first signs of cardiac failure.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Interactions

As levobunololol has been shown to be absorb systemically, all of the precautions and contraindications pertaining to systemically-administer beta-blockers should be carefully considered prior to using levobunolol. Levobunolol should not be used in patients with preexisting cardiac disease, such as severe bradycardia, sick sinus syndrome, advance AV block, cardiogenic shock, coronary artery disease, vasospastic angina, or overt congestive heart failure, particularly those with severe leave ventricular dysfunction. Treatment with levobunolol should be discontinued at first signs of cardiac failure. Rare deaths have been reported in patients at high risk for cardiac or pulmonary complications secondary to treatment with beta-blockers. Beta-blockers should also be used with caution in patients with other circulatory disorders including hypotension, peripheral vascular disease, and Raynaud's phenomenon. Because of the potential effects of beta-blockade on blood pressure and pulse, beta-blockers such as levobunolol, should be used with caution in patients with cerebrovascular insufficiency or stroke. If signs or symptoms suggesting reduced cerebral blood flow develop following initiation of beta-blocker, alternative therapy should be consider. As with all beta-blockers, levobunolol should be used with caution in patients with pheochromocytoma if effective blockade of alpha and beta receptors is not achieve, because of risk of hypertension. As with all beta-blockers, levobunolol should be used with caution in patients with hyperthyroidism or thyrotoxicosis because beta-blockade can mask tachycardia, which is a useful monitoring parameter in thyroid disease. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-blocker therapy that might precipitate thyroid storm. Although levobunolol is administered ophthalmically, potential for systemic adverse reactions still exist. Levobunolol should be used with caution in patients with diabetes mellitus because the drug can mask symptoms of hypoglycemia such as tachycardia, palpitations, blood pressure changes, tremor, and anxiety. Levobunolol is contraindicate in patients with bronchial asthma, history of bronchial asthma, or severe chronic obstructive pulmonary disease. Use levobunolol with caution in patients with other pulmonary disease in which acute bronchospasm would put them at risk. Ophthalmic formulations of levobunolol contain metabisulfite. Patients with sulfite hypersensitivity may develop local or systemic allergic reaction, including anaphylaxis. Asthmatic patients appear to be at higher risk than the general population for development of this reaction. Levobunolol is contraindicate in patients exhibiting hypersensitivity to drug or any of its excipients. Levobunolol is relatively contraindicate in hepatic impairment because of possible decreased clearance of drug since it is principally metabolize by liver. Dosage adjustment may be necessary in patients with hepatic disease. Levobunolol may produce myasthenic condition which manifest as ptosis, weakness of limbs, and double vision; therefore levobunolol should be avoided in patients with myasthenia gravis. Levobunolol is an ophthalmic beta-blocker which may be systemically absorb. General anesthetics can potentiate antihypertensive effects of beta-blockers and can produce prolonged hypotension. Patients receiving beta-blockers before or during surgery involving use of general anesthetics that possess negative inotropic effects should be monitored closely for signs of heart failure. The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Pharmacology

Levobunolol is a non-selective 1-and 2-adrenergic antagonist that lacks intrinsic sympatho-mimetic activity and local anesthetic properties. 119 120 drug is used systemically to treat hypertension, ventricular arrhythmias, and angina. Levobunolol is supplied as either 0. 25 % or 0. 5 % Solution, which is administered every 12-24 hours. The drugs appear to be similar to timolol with regard to both efficacy and safety. 121-124 It has been suggested that Levobunolol is more likely than timolol to control IOP with once-daily administration. 125 However, two drugs seem to have similar durations of action. 126 Levobunolol produces blepharoconjunctivitis more frequently than does timolol. The 127 128 metabolites of Levobunolol also appear to have ocular hypotensive effects.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Uses

Ophthalmic levobunolol comes as a solution to instill in the eyes. Levobunolol eye drops are usually instill once or twice a day. Follow directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use levobunolol eye drop exactly as direct. Do not use more or less of them or use them more often than prescribed by your doctor. Levobunolol eye drops control glaucoma but do not cure it. Continue to use levobunolol eye drops even if you feel well. Do not stop using levobunolol eye drops without talking to your doctor.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Pregnancy

Mechanism of Action: Although levobunolol's exact mechanism of Action has not been fully determine, it is believed to be due to reduction of production of aqueous humor via inhibition of adrenergically drive processes within ciliary processes. As result of levobunolol's actions, IOP is reduced in patients with either elevated or normal IOP. This reduction occurs irrespective of the presence of glaucoma. Visual acuity, pupil size, and accommodation do not appear to be affected by levobunolol. Because levobunolol has no effect on pupil size, it should be used only in conjunction with topical miotic, such as pilocarpine, to reduce IOP in patients with angle-closure glaucoma. Levobunolol has the capacity to decrease IOP in the contralateral, untreated eye to a lesser extent than in the treated eye. Delay tolerance to effects of levobunolol can occur after > 2 years of continuous use. Levobunolol does not possess local anesthetic or intrinsic sympathomimetic activity. Several mechanisms of action have been proposed to explain the systemic effects of beta-blockers. Beta-adrenergic antagonists counter the effect of sympathomimetic neurotransmitters by competing for receptor sites. Similar to propranolol and timolol, levobunolol blocks sympathetic stimulation mediated by beta1-adrenergic receptors in the heart and vascular smooth muscle. The Pharmacodynamic consequences of this activity can be reduce resting and exercise heart rate and reduce systolic and diastolic blood pressure. Reflex orthostatic hypotension also may be reduce. In addition, levobunolol can competitively block beta2-adrenergic responses in bronchial smooth muscle, potentially inducing bronchospasm.


CONTRAINDICATIONS / PRECAUTIONS

Fetotoxicity has been observed in rabbits when doses of levobunolol HCl equivalent to 200 and 700 times the recommended dose for treatment of glaucoma were give. 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 show 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 examine, that rabbits may be a particularly sensitive species. There are no adequate and well-control studies in pregnant women. BETAGAN ophthalmic solution should be used during pregnancy only if potential benefit justifies potential risk to the fetus.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Proper Use

In deciding to use medicine, risks of taking medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, following should be consider: tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully. Appropriate studies have not been performed on the relationship of age to the effects of Levobunolol eye drops in the pediatric population. Safety and efficacy have not been establish. Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of Levobunolol eye drops in the elderly. Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines list below. Following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive. Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both medicines. Ceritinib Crizotinib Diltiazem Dronedarone Epinephrine Fenoldopam Fingolimod Indacaterol Iobenguane I 131 Iohexol Lacosamide Oxymetazoline Rivastigmine Verapamil using this medicine with any of the following medicines may cause increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both medicines. Acarbose Aceclofenac Acemetacin Albiglutide Alfuzosin Alogliptin Amtolmetin Guacil Arbutamine Aspirin Bromfenac Bufexamac Bunazosin Canagliflozin Celecoxib Chlorpropamide Choline Salicylate Clonixin Dapagliflozin Dexibuprofen Dexketoprofen Diclofenac Diflunisal Dipyrone Doxazosin Droxicam Dulaglutide Empagliflozin Ertugliflozin Etodolac Etofenamate Etoricoxib Exenatide Felbinac Fenoprofen Fepradinol Feprazone Floctafenine Flufenamic Acid Flurbiprofen Glimepiride Glipizide Glyburide Ibuprofen Indomethacin Insulin Aspart, Recombinant Insulin Degludec Insulin Detemir Insulin Glargine, Recombinant Insulin Glulisine Insulin Human inhale Insulin Human Isophane Insulin Human Regular Insulin Lispro, Recombinant Ketoprofen Ketorolac Linagliptin Liraglutide Lixisenatide Lornoxicam Loxoprofen Lumiracoxib Meclofenamate Mefenamic Acid Meloxicam Metformin Mibefradil Miglitol Morniflumate Moxisylyte Nabumetone Naproxen Nateglinide Nepafenac Niflumic Acid Nimesulide Nimesulide Beta Cyclodextrin Oxaprozin Oxyphenbutazone Parecoxib Phenoxybenzamine Phentolamine Phenylbutazone Piketoprofen Pioglitazone Piroxicam Pramlintide Pranoprofen Prazosin Proglumetacin Propyphenazone Proquazone Repaglinide Rofecoxib Rosiglitazone Salicylic Acid Salsalate Saxagliptin Sitagliptin Sodium Salicylate John's Wort Sulindac Tamsulosin Tenoxicam Terazosin Tiaprofenic Acid Tolazamide Tolbutamide Tolfenamic Acid Tolmetin Trimazosin Urapidil Valdecoxib Vildagliptin certain medicines should not be use at or around time of eating food or eating certain types of food since interactions may occur.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Precautions

It is very important that your eye doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects. Do not use this medicine if you are also using beta-blocker medicine that is taken by mouth. If itching, redness, swelling, or other signs of eye or eyelid irritation occur, check with your doctor right away. This may mean that you are allergic to this medicine. Levobunolol may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort, dilate neck veins, extreme fatigue, irregular breathing, irregular heartbeat, shortness of breath, swelling of face, fingers, feet, or lower legs, or weight gain. This medicine may cause changes in your blood sugar levels. It may also cover up signs of low blood sugar, such as rapid pulse rate. Check with your doctor if you have these problems or if you notice change in results of your blood or urine sugar tests. This medicine may cause choroidal detachment. Talk to your doctor if you have concerns. Make sure any doctor or dentist who treats you knows that you are using this medicine. You may need to stop using this medicine several days before having surgery. Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription-medicines and herbal or vitamin supplements. Copyright 2020 IBM Watson Health. All rights reserve. Information is for the end user's use only and may not be sell, redistributed or otherwise used for commercial purposes.


General

BETAGAN steriles should be used with caution in patients with known hypersensitivity to other beta-adrenoceptor blocking agents. Use with caution in patients with diminished pulmonary function. BETAGAN should be used with caution in patients who are receiving beta-adrenergic blocking agent orally, because of the potential for additive effects on systemic beta-blockade or on intraocular pressure. Patients should not typically use two or more topical ophthalmic beta-adrenergic blocking agents simultaneously. Because of the potential effects of beta-adrenergic blocking agents on blood pressure and pulse rates, these medications must be used cautiously in patients with cerebrovascular insufficiency. Should signs or symptoms develop that suggest reducing cerebral blood flow while using BETAGAN ophthalmic solution, alternative therapy should be consider. In patients with angle-closure glaucoma, immediate objective of treatment is to reopen the angle. This require, in most cases, constricting pupils with miotic. BETAGAN ophthalmic solution has little or no effect on pupil. When BETAGAN is used to reduce elevated intraocular pressure in angle-closure glaucoma, it should be followed with medicine and not alone. Preservative in BETAGAN, benzalkonium chloride, may be absorbed by soft contact lenses. Patients wearing soft contact lenses should be instructed to remove contact lenses before administration of solution and wait at least 15 minutes after instilling BETAGAN before reinserting soft contact lenses.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Sources

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

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