Betaxolol

Pronunciation

(be TAKS oh lol)

U.S. Brand Names

Betoptic® S; Kerlone®

Synonyms

Betaxolol Hydrochloride

Generic Available

Yes: Solution, tablet

Canadian Brand Names

Betoptic® S

Use

Treatment of chronic open-angle glaucoma and ocular hypertension; management of hypertension

Pregnancy Risk Factor

C (manufacturer); D (2nd and 3rd trimesters - expert analysis)

Lactation

Oral: Enters breast milk/use caution

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; pulmonary edema; pregnancy (2nd and 3rd trimester)

Warnings/Precautions

Administer cautiously in compensated heart failure and monitor for a worsening of the condition. Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia. Use caution with concurrent use of beta-blockers and either verapamil or diltiazem; bradycardia or heart block can occur. Use caution in patients with PVD (can aggravate arterial insufficiency). In general, beta-blockers should be avoided in patients with bronchospastic disease. Betaxolol, with B1 selectivity, should be used cautiously in bronchospastic disease with close monitoring. Use cautiously in diabetics because it can mask prominent hypoglycemic symptoms. Can mask signs of thyrotoxicosis. Can cause fetal harm when administered in pregnancy. Dosage adjustment required in severe renal impairment and those on dialysis. Use care with anesthetic agents which decrease myocardial function.

Adverse Reactions

Ophthalmic:

>10%: Ocular: Conjunctival hyperemia

1% to 10%:

Ocular: Anisocoria, corneal punctate keratitis, keratitis, corneal staining, decreased corneal sensitivity, eye pain, vision disturbances

Systemic:

>10%:

Central nervous system: Drowsiness, insomnia

Endocrine & metabolic: Decreased sexual ability

1% to 10%:

Cardiovascular: Bradycardia, palpitation, edema, CHF, reduced peripheral circulation

Central nervous system: Mental depression

Gastrointestinal: Diarrhea or constipation, nausea, vomiting, stomach discomfort

Respiratory: Bronchospasm

Miscellaneous: Cold extremities

<1% (Limited to important or life-threatening): Chest pain, thrombocytopenia

Overdosage/Toxicology

Symptoms of significant overdose include bradycardia, hypotension, AV block, CHF, bronchospasm, hypoglycemia. Treat initially with fluids. Sympathomimetics (eg, epinephrine or dopamine), glucagon, or a pacemaker can be used to treat toxic bradycardia, asystole, and/or hypotension.

Drug Interactions

Substrate (major) of CYP1A2, 2D6; Inhibits CYP2D6 (weak)

Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.

CYP1A2 inducers: May decrease the levels/effects of betaxolol. Example inducers include aminoglutethimide, carbamazepine, phenobarbital, and rifampin.

CYP1A2 inhibitors: May increase the levels/effects of betaxolol. Example inhibitors include amiodarone, ciprofloxacin, fluvoxamine, ketoconazole, norfloxacin, ofloxacin, and rofecoxib.

CYP2D6 inhibitors: May increase the levels/effects of betaxolol. Example inhibitors include chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine, pergolide, quinidine, quinine, ritonavir, and ropinirole.

Clonidine; Hypertensive crisis after or during withdrawal of either agent.

Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.

Glucagon: Betaxolol may blunt the hyperglycemic action of glucagon.

Insulin and oral hypoglycemics: May mask tachycardia from hypoglycemia.

NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.

Salicylates may reduce the antihypertensive effects of beta-blockers.

Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.

Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.

Ethanol/Nutrition/Herb Interactions

Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe, ginseng (may worsen hypertension). Avoid garlic (may have increased antihypertensive effect).

Stability

Avoid freezing

Mechanism of Action

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

Pharmacodynamics/Kinetics

Onset of action: Ophthalmic: 30 minutes; Oral: 1-1.5 hours

Duration: Ophthalmic: 12 hours

Absorption: Ophthalmic: Some systemic; Oral: ~100%

Metabolism: Hepatic to multiple metabolites

Protein binding: Oral: 50%

Bioavailability: Oral: 89%

Half-life elimination: Oral: 12-22 hours

Time to peak: Ophthalmic: ~2 hours; Oral: 1.5-6 hours

Excretion: Urine

Dosage

Adults:

Ophthalmic: Instill 1 drop twice daily.

Oral: 5-10 mg/day; may increase dose to 20 mg/day after 7-14 days if desired response is not achieved. Initial dose in elderly: 5 mg/day.

Dosage adjustment in renal impairment: Administer 5 mg/day. Can increase every 2 weeks up to a maximum of 20 mg/day.

Clcr<10 mL/minute: Administer 50% of usual dose.

Administration

Ophthalmic: Shake 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.

Monitoring Parameters

Ophthalmic: Intraocular pressure. Systemic: Blood pressure, pulse

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber.

Oral: Use as directed and do not discontinue without consulting prescriber. May cause dizziness or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report chest pain, palpitations or irregular heartbeat; persistent GI upset (eg, nausea, vomiting, diarrhea, or constipation); unusual cough; respiratory difficulty; swelling or coolness of extremities; or unusual mental depression. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Ophthalmic: Shake suspension well before using. Tilt head back and instill in eye. Keep eye open; do not blink for 30 seconds. Apply gentle pressure to corner of eye for 1 minute. Wipe away excess from skin. Do not let tip of applicator touch eye; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). Report if condition does not improve or if you experience eye pain, vision changes, or other adverse eye response.

Nursing Implications

Monitor for systemic effect of beta-blockade

Anesthesia and Critical Care Concerns/Other Considerations

Due to alterations in the autonomic nervous system, beta-blockade may result in less hemodynamic response in the elderly. Studies indicate that despite decreased sensitivity to the chronotropic effects of beta-blockade with age, there appears to be an increased myocardial sensitivity to the negative inotropic effect.

Myocardial Infarction: Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.

Atrial Fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.

Cardiovascular Considerations

Hypertension: Beta-blocker therapy in the treatment of hypertension has been associated with improved cardiovascular outcomes. This class of drug is beneficial for elderly patients with hypertension. A recent UKPDS study showed that beta-blocker therapy (atenolol) was as effective as an ACE inhibitor in reducing cardiovascular events and that the benefits of therapy were related more to the degree of antihypertensive efficacy rather than the class of drug used.

Myocardial infarction: Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.

Atrial fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.

Angina: Beta-blockers are effective in the treatment of angina as monotherapy or when combined with nitrates and/or calcium channel blockers. In patients with severe intractable angina requiring negative cardiac chronotropic medications, pacemaker placement has been carried out to maintain heart rate in the setting of large doses of beta-blockers and/or calcium channel blockers. Beta-blockers are ineffective in the treatment of pure vasospastic (Prinzmetal) angina.

Unstable angina/non-ST-segment elevation MI: In the treatment of unstable angina/non-ST-segment elevation MI, a beta-blocker, with the first dose administered intravenously if there is ongoing chest pain, followed by oral administration, is recommended (in the absence of contraindications).

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.

Heart failure: There is emerging evidence that beta-blocker therapy, without intrinsic sympathomimetic activity (ISA), should be initiated in select patients with stable congestive heart failure (NYHA Class II-III). To date, carvedilol, sustained release metoprolol, and bisoprolol have demonstrated a beneficial effect on morbidity and mortality. It is important that beta-blocker therapy be instituted initially at very low doses with gradual and very careful titration.

Dental Health: Effects on Dental Treatment

Betaxolol is a cardioselective beta-blocker. Local anesthetic with vasoconstrictor can be safely used in patients medicated with betaxolol. Nonselective beta-blockers (ie, propranolol, nadolol) enhance the pressor response to epinephrine, resulting in hypertension and bradycardia; this has not been reported for betaxolol. Many nonsteroidal anti-inflammatory drugs, such as ibuprofen and indomethacin, can reduce the hypotensive effect of beta-blockers after 3 or more weeks of therapy with the NSAID. Short-term NSAID use (ie, 3 days) requires no special precautions in patients taking beta-blockers.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause drowsiness; rare reports of depression and hallucinations

Mental Health: Effects on Psychiatric Treatment

Has been used to treat akathisia; propranolol preferred

Dosage Forms

Solution, ophthalmic, as hydrochloride: 0.5% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]

Suspension, ophthalmic, as hydrochloride (Betoptic® S): 0.25% (2.5 mL, 5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]

Tablet, as hydrochloride (Kerlone®): 10 mg, 20 mg

References

Antman EM, Anbe SC, Alpert JS, et al, "ACC/AHA Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction - Executive Summary: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Writing Committee to Revise the 1999 Guidelines for the Management of Patients With Acute Myocardial Infarction)," Circulation , 2004, 110:588-636. Available at: http://www.circulationaha.org/cgi/content/full/110/5/588. Last accessed August 26, 2004.

Braunwald E, Antman EM, Beasley JW, et al, "ACC/AHA 2002 Guideline Update for the Management of Patients With Unstable Angina and Non-ST-Segment Elevation Myocardial Infarction - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Unstable Angina)," J Am Coll Cardiol , 2002, 40(7):1366-74. Available at: http://www.acc.org/clinical/guidelines/unstable/incorporated/index.htm. Accessed May 20, 2003.

Chobanian AV, Bakris GL, Black HR, et al, "The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: The JNC 7 Report," JAMA , 2003, 289(19):2560-71.

"Consensus Recommendations for the Management of Chronic Heart Failure. On Behalf of the Membership of the Advisory Council to Improve Outcomes Nationwide in Heart Failure," Am J Cardiol , 1999, 83(2A):1A-38A.

Gibbons RJ, Abrams J, Chatterjee K, et al, "ACC/AHA 2002 Guideline Update for the Management of Patients With Chronic Stable Angina - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Chronic Stable Angina)," J Am Coll Cardiol , 2003, 41(1):159-68.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings," Chest , 2003, 123(3):897-922.

Wong DG, Spence JD, Lamki L, et al, "Effect of Nonsteroidal Anti-inflammatory Drugs on Control of Hypertension of Beta-Blockers and Diuretics," Lancet , 1986, 1(8488):997-1001.

International Brand Names

Apo-Betaxolol® (NZ); Bemaz® (CL); Beof® (CL, EC); Betabion® (PL); Betasel® (AR); Betaxolol Alcon® (ES); Betaxolol® (CL, RO); Betaxolol L.CH.® (CL); Betoko® (YU); Betoptic® (AU, BE, BR, CH, CL, CZ, DK, ES, FI, FR, GB, HK, HR, HU, IE, IL, IT, LU, NL, NO, NZ, PL, PT, RO, RU, SE, SG, SI, TH, TR, ZA); Betoptic S® (AT, BD, BE, BR); Betoptic® S (CA); Betoptic S® (CL, CO, EC, FI, HU, IL, NO, PL, RO, RU, SE, SG, SI, YU); Betoptima® (DE, ID); Betoquin® (AU); Cloridrato de Betaxolol® (BR); Davixolol® (PT); Huma-Betaxolol® (HU); Kerlon® (DK, FI, IT, NL, SE); Kerlone® (BE, DE, GB, HK, IL, LU, RO, SG); Kerlong® (JP); Lokren® (CZ, HU, PL, RO, RU, YU); Optibetol® (PL); Optipres® (RO); Tonobexol® (AR)

A.D.A.M., Inc. is accredited by URAC, also known as the American Accreditation HealthCare Commission (www.urac.org). URAC's accreditation program is the first of its kind, requiring compliance with 53 standards of quality and accountability, verified by independent audit. A.D.A.M. is among the first to achieve this important distinction for online health information and services. Learn more about A.D.A.M.'s editorial process . A.D.A.M. is also a founding member of Hi-Ethics (www.hiethics.com) and subscribes to the principles of the Health on the Net Foundation (www.hon.ch).

The information provided herein should not be used during any medical emergency or for the diagnosis or treatment of any medical condition. A licensed medical professional should be consulted for diagnosis and treatment of any and all medical conditions. Call 911 for all medical emergencies. Links to other sites are provided for information only -- they do not constitute endorsements of those other sites. © 1997-2007 A.D.A.M., Inc. Any duplication or distribution of the information contained herein is strictly prohibited.

Home > Medical Reference > Complementary Medicine