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Generic Name: Betaxolol Hydrochloride
Class: beta-Adrenergic Blocking Agents
VA Class: CV100
Chemical Name: 2-Propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl) amino)-, hydrochloride
Molecular Formula: C18H29NO3•ClH
CAS Number: 63659-19-8
A β1-selective adrenergic blocking agent (β-blocker).1 2 3 4 5 6 7 8 9 10 24 25
Uses for Kerlone
Management of hypertension (alone or in combination with other classes of antihypertensive agents).1 500
β-Adrenergic blocking agents (β-blockers) generally not preferred for initial management of hypertension, but may be considered in patients who have a compelling indication (e.g., prior MI, ischemic heart disease, heart failure) for their use or as add-on therapy in those who do not respond adequately to the preferred drug classes (ACE inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, or thiazide diuretics).56 501 502 503 504 515 523 524 527 800
Black hypertensive patients generally tend to respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to β-blockers.38 42 43 500 501 504 However, diminished response to β-blockers is largely eliminated when administered concomitantly with a thiazide diuretic.500
Kerlone Dosage and Administration
Individualize dosage according to patient response and tolerance.1 30
If long-term therapy is discontinued, reduce dosage gradually over a period of about 2 weeks.1 (See Abrupt Withdrawal of Therapy under Cautions.)
BP Monitoring and Treatment Goals
Carefully monitor BP during initial titration or subsequent upward adjustment in dosage.500 501
When available, use evidence-based dosing information (i.e., dosages shown in randomized controlled trials to reduce complications of hypertension) to determine target dosages; target dosages usually can be achieved within 2–4 weeks but may take up to several months.501
Goal is to achieve and maintain optimal control of BP; individualize specific target BP based on consideration of multiple factors, including patient age and comorbidities, and currently available evidence from clinical studies.500 501
Administer orally;1 absorption does not appear to be affected by food or alcohol.1
Available as betaxolol hydrochloride; dosage expressed in terms of the salt.1 Commercially available tablets containing 10 or 20 mg of betaxolol hydrochloride contain 8.94 or 17.88 mg of betaxolol, respectively.1
Initially, 5–10 mg once daily, either alone or in combination with a diuretic.1 30 600 May double dosage after 7–14 days up to 20 mg daily.1 2 3 16 30 500 600
If intolerable adverse effects occur, consider dosage reduction; if adverse effects worsen or fail to resolve, may need to discontinue and switch to another antihypertensive drug class.501
Maximum 40 mg daily.1
Dosage reductions are not routinely necessary.1 Use with caution; monitor patients carefully.1
Initially, 5 mg once daily in those with severe impairment or undergoing dialysis.1 Increase dosage in increments of 5 mg daily, no more frequently than at 2-week intervals, up to a maximum of 20 mg daily.1
Initially, 5 mg daily.1
Use the lowest possible dosage (5–10 mg once daily).1
If dosage must be increased, consider divided administration of the daily dose to avoid the higher peak plasma concentrations associated with once-daily dosing.1
Cautions for Kerlone
Known hypersensitivity to betaxolol.1
Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, or overt cardiac failure.1
Possible precipitation of heart failure.1
Avoid use in patients with decompensated heart failure; may use cautiously in patients with inadequate myocardial function and, if necessary, in patients with well-compensated heart failure (e.g., those controlled with cardiac glycosides and/or diuretics).1
Adequate treatment (e.g., with a cardiac glycoside and/or diuretic) and close observation recommended if signs or symptoms of impending heart failure occur; if heart failure continues, discontinue therapy, gradually if possible.1
Abrupt Withdrawal of Therapy
Abrupt discontinuance of therapy is not recommended as it may exacerbate angina symptoms or precipitate MI in patients with CAD.1
Gradually decrease dosage over a period of about 2 weeks and monitor patients carefully; advise patients to temporarily limit their physical activity during Withdrawal of therapy.1
If exacerbation of angina occurs or acute coronary insufficiency develops, reinstitute therapy promptly and initiate appropriate measures for the management of unstable angina pectoris.1
Generally should not be used in patients with bronchospastic disease, but may be used with caution in such patients who do not respond to or cannot tolerate alternative treatment.1
Administer the lowest effective dosage (5–10 mg once daily); a bronchodilator (e.g., a β2-adrenergic agonist) should be available.1
Possible risks associated with general anesthesia (e.g., severe hypotension, difficulty maintaining heart beat) due to decreased ability of the heart to respond to reflex β-adrenergic stimuli.1 Use with caution in patients undergoing major surgery involving general anesthesia.1 Use particular care if anesthetics that depress the myocardium (e.g., cyclopropane, ether, trichloroethylene) are used.1
Diabetes and Hypoglycemia
Possible decreased signs and symptoms of hypoglycemia (e.g., may mask tachycardia but not sweating or dizziness).1
Use with caution in patients with diabetes mellitus receiving hypoglycemic drugs.1
Signs of hyperthyroidism (e.g., tachycardia) may be masked.1 Possible thyroid storm if therapy is abruptly withdrawn; carefully monitor patients having or suspected of developing thyrotoxicosis.1
Possible increased reactivity to repeated, accidental, diagnostic, or therapeutic challenges with a variety of allergens while taking β-blocking agents.1 Such patients may be unresponsive to usual doses of epinephrine.1
Possible reduction in intraocular pressure.1 May interfere with glaucoma screening test; Withdrawal of therapy may cause return to increased intraocular pressure.1 (See Interactions.)
Distributed into milk.1 Use with caution.1
Safety and efficacy not established.1
Possible increased incidence of bradycardia in patients >65 years of age compared with younger adults.1 Bradycardia (possibly dose related) may respond to dosage reduction.1 (See Geriatric Patients under Dosage and Administration.)
Although elimination half-life may be increased, clearance may remain unchanged, resulting in little change in the AUC.1 (See Hepatic Impairment under Dosage and Administration.)
Clearance may be decreased.1 Dosage adjustment may be needed based on degree of renal impairment.1 (See Renal Impairment under Dosage and Administration.)
Common Adverse Effects
Bradycardia, edema, headache, dizziness, fatigue, lethargy, insomnia, nervousness, bizarre dreams, impotence, dyspnea, pharyngitis, rhinitis, upper respiratory infection, dyspepsia, nausea, diarrhea, chest pain, arthralgia, rash.1
Interactions for Kerlone
β-Blockers (ophthalmic solution)
Possible additive effects on intraocular pressure or systemic β blockade1
Calcium-channel blocking agents
Potential hypotension, AV conduction disturbances, and left ventricular failure1
Avoid concomitant use in patients with impaired cardiac function1
Pharmacokinetic interaction unlikely1
Pharmacokinetic interaction unlikely1
β-Adrenergic blockade may exacerbate rebound hypertension following discontinuance of clonidinea
Discontinue β-blockers several days before initiating gradual Withdrawal of clonidine1
If replacing clonidine, delay initiation of the β-blocker for several days after stopping clonidinea
Pharmacokinetic interaction unlikely1
Pharmacokinetic interaction unlikely1
Monitor for signs of hypotension and bradycardia (e.g., vertigo, syncope, postural hypotension)1
No potentiation of anticoagulant effect1
Well absorbed following oral administration, with peak plasma concentration usually attained within 1.5–6 hours.1
Absolute bioavailability is 89%.1
Reductions in BP and heart rate observed within 24 hours after 5- to 40-mg doses (given once daily); these effects usually are maximal within 1 or 2 weeks.1
Food or alcohol does not appear to affect absorption.1
Distributed into milk.1
Plasma Protein Binding
Metabolized in the liver.1
Excreted in the urine as metabolites and unchanged drug.1
Clearance varies with the degree of renal impairment.1
In patients with hepatic impairment, half-life was increased by 33%, but clearance was unchanged.1
In geriatric patients, elimination may be reduced.1
Inhibits response to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium.1 Blocks β2-adrenergic receptors within the bronchial and vascular smooth muscle only at high doses.1
Decreases resting and exercise-stimulated heart rate, cardiac output, cardiac work, and reflex orthostatic tachycardia and inhibits isoproterenol-induced tachycardia.1
One of the most potent2 6 11 14 15 17 19 20 25 and selective2 11 14 15 17 20 25 β1-adrenergic blocking agents currently available.
No intrinsic sympathomimetic activity1 11 13 15 22 and little or no membrane-stabilizing effect on the heart.1 2 8 9 11 16 17 18 22 24 25
Reduces BP by decreasing cardiac output, decreasing sympathetic outflow from the CNS, and/or suppressing renin release.1
Advice to Patients
Importance of taking betaxolol exactly as prescribed.1
Importance of not interrupting or discontinuing therapy without consulting clinician; patients should temporarily limit their physical activity when discontinuing therapy.1
Importance of immediately informing clinician at the first sign or symptom of impending cardiac failure (e.g., weight gain, increased shortness of breath) or if any difficulty in breathing occurs.1
In patients with heart failure, importance of informing clinician of signs or symptoms of exacerbation (e.g., weight gain, difficulty in breathing).1
Importance of patients informing anesthesiologist or dentist that they are receiving betaxolol therapy prior to undergoing major surgery.1
Importance of informing patients with diabetes that the drug may mask signs and symptoms of hypoglycemia, including increased heart rate.1
Importance of avoiding some activities (e.g., operating machinery, driving a motor vehicle) until effects on the individual are known.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Betaxolol Hydrochloride Tablets
Betaxolol Hydrochloride Tablets
AHFS DI Essentials. © Copyright 2017, Selected Revisions March 1, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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