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.
1. Sanofi-Synthelabo. Kerlone (betaxolol hydrochloride) tablets prescribing information. New York, NY; 2003 Mar.
2. Alcon Laboratories. Betoptic product monograph. In: Barnhart ER, publisher. Physicians’ desk reference for ophthalmology. 19th ed. Oradell, NJ: Medical Economics Company Inc; 1991:211-2.
3. Weiner N. Drugs that inhibit adrenergic nerves and block adrenergic receptors. In: Gilman AG, Goodman LS, Rall TW et al, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 7th ed. New York: Macmillan Publishing Company; 1985:181-214.
4. Windholz M, ed. The Merck index. 10th ed. Rahway, NJ: Merck & Co, Inc; 1983:169.
5. Reynolds JEF, ed. Martindale: the extra pharmacopoeia. 28th ed. London: The Pharmaceutical Press; 1982:1684.
6. Manoury P. Betaxolol: chemistry and biological profile in relation to its physicochemical properties. In: Morselli PL, ed. LERS monograph series. Vol 1. New York: Raven Press; 1983:13-9.
7. Reiss GR, Brubaker RF. The mechanism of betaxolol, a new ocular hypotensive agent. Ophthalmology. 1983; 90:1369-72. [PubMed 6664677]
8. Berrospi R, Leibowitz HM. Betaxolol: a new beta-adrenergic blocking agent for treatment of glaucoma. Arch Ophthalmol. 1982; 100:943-6. [PubMed 6124227]
9. Caldwell DR, Salisbury CR, Guzek JP. Effects of topical betaxolol in ocular hypertensive patients. Arch Ophthalmol. 1984; 102:539-40. [PubMed 6704008]
10. Smith JP, Weeks RH, Newland EF et al. Betaxolol and acetazolamide: combined ocular hypotensive effect. Arch Ophthalmol. 1984; 102:1794-5. [PubMed 6391442]
11. Cavero I, Lefeevre-Borg F, Manoury P et al. In vitro and in vivo pharmacological evaluation of betaxolol, a new, potent, and selective beta1-adrenoceptor antagonist. In: Morselli PL, ed. LERS monograph series. Vol 1. New York: Raven Press; 1983:31-42.
12. Levy NS, Boone L. Effect of 0.25% betaxolol v placebo. Glaucoma. 1983; 5:230-2.
13. Vareilles P, Silverstone D, Plazonnet B et al. Comparison of the effects of timolol and other adrenergic agents on intraocular pressure in the rabbit. Invest Ophthalmol Vis Sci. 1977; 16:987-96. [PubMed 21145]
14. Shanks RG. Comparison of betaxolol with other beta-blocking drugs in healthy volunteers. In: Morselli PL, ed. LERS monograph series. Vol 1. New York: Raven Press; 1983:133-41.
15. Cadigan PJ, London D, Pentecost BL. Effects of betaxolol, given in single doses by mouth, on pulse rate and blood pressure in normal subjects. In: Morselli PL, ed. LERS monograph series. Vol 1. New York: Raven Press; 1983:101-7.
16. Berry DP Jr, Van Buskirk EM, Shields MB. Betaxolol and timolol: a comparison of efficacy and side effects. Arch Ophthalmol. 1984; 102:42-5. [PubMed 6367723]
17. Boudot JP, Cavero I, Feenard S et al. Preliminary studies on SL 75212, a new potent cardioselective beta-adrenoceptor antagonist. Br J Pharmacol. 1979; 66:445P. [PubMed 43176]
18. Cadigan PJ, London DR, Pentecost BL et al. Cardiovascular effects of single oral doses of the new beta-adrenoceptor blocking agent betaxolol (SL 75212) in healthy volunteers. Br J Clin Pharmacol. 1980; 9:569-75. [PubMed 6104498]
19. Morselli PL, Thiercelin JF, Padovani P et al. Comparative pharmacokinetics of several beta-blockers in renal and hepatic insufficiency. In: Morselli PL, ed. LERS monograph series. Vol 1. New York: Raven Press; 1983:233-41.
20. Warrington SJ, Taylor EA, Kilborn JR. Comparison of pharmacodynamic effects of betaxolol with atenolol, practolol, and propranolol given intravenously. In: Morselli PL, ed. LERS monograph series. Vol 1. New York: Raven Press; 1983:109-22.
21. Machin PJ, Hurst DN, Bradshaw RN et al. β1-Selective adrenoceptor antagonists. 2: 4-ether-linked phenoxypropanolamines. J Med Chem. 1983; 26:1570-6. [PubMed 6138435]
22. Beresford R, Heel RC. Betaxolol: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in hypertension. Drugs. 1986; 31:6-28. [PubMed 2866947]
23. Durand A, Pauloin D, Bernard F et al. In vitro metabolism of betaxolol and metoprolol: influence of the structure. Proceedings of World Conference on Clinical Pharmacology and Therapeutics. Washington, DC; 1983 July 31-August 5. Abstract No. N568.
24. Alcon Laboratories. Betoptic S (betaxolol hydrochloride) suspension prescribing information. Fort Worth, TX; 1991 Aug.
25. Alcon Laboratories. Betoptic S (betaxolol hydrochloride) product monograph. Fort Worth, TX; 1990 Feb.
26. The USP Drug Nomenclature Committee. Nomenclature policies and recommendations: I. Review and current proposals and decisions. Pharmacopeial Forum. 1991; 17:1509-11.
27. The United States Pharmacopeia, 23rd rev, and The national formulary, 18th ed. Rockville, MD: The United States Pharmacopeial Convention, Inc; 1995:198.
29. Anon. Drugs for hypertension. Med Lett Drugs Ther. 1993; 35:55-60. [PubMed 8099706]
30. National Heart, Lung, and Blood Institute National High Blood Pressure Education Program. The sixth report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC VI). Bethesda, MD: National Institutes of Health; 1997 Nov. (NIH publication No. 98-4080.)
31. Izzo JL, Levy D, Black HR. Importance of systolic blood pressure in older Americans. Hypertension. 2000; 35:1021-4. [PubMed 10818056]
32. Frohlich ED. Recognition of systolic hypertension for hypertension. Hypertension. 2000; 35:1019-20. [PubMed 10818055]
33. Bakris GL, Williams M, Dworkin L et al. Preserving renal function in adults with hypertension and diabetes: a consensus approach. Am J Kidney Dis. 2000; 36:646-61. [PubMed 10977801]
34. Associated Press (American Diabetes Association). Diabetics urged: drop blood pressure. Chicago, IL; 2000 Aug 29. Press Release from web site.
35. Appel LJ. The verdict from ALLHAT—thiazide diuretics are the preferred initial therapy for hypertension. JAMA. 2002; 288:3039-60. [PubMed 12479770]
36. The ALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group. Major outcomes in high-risk hypertensive patients randomized to angiotensin-converting enzyme inhibitor or calcium channel blocker vs diuretic: the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT). JAMA. 2002; 288:2981-97. [PubMed 12479763]
38. Douglas JG, Bakris GL, Epstein M et al. Management of high blood pressure in African Americans: Consensus statement of the Hypertension in African Americans Working Group of the International Society on Hypertension in Blacks. Arch Intern Med. 2003; 163:525-41.
40. The Guidelines Subcommitee of the WHO/ISH Mild Hypertension Liaison Committee. 1999 guidelines for the management of hypertension. J Hypertension. 1999; 17:392-403.
42. Wright JT, Dunn JK, Cutler JA et al. Outcomes in hypertensive black and nonblack patients treated with chlorthalidone, amlodipine, and lisinopril. JAMA. 2005; 293:1595-607. [PubMed 15811979]
43. Neaton JD, Kuller LH. Diuretics are color blind. JAMA. 2005; 293:1663-6. [PubMed 15811986]
44. Thadani U. Beta blockers in hypertension. Am J Cardiol. 1983; 52:10-5D.
45. Conolly ME, Kersting F, Dollery CT. The clinical pharmacology of beta-adrenoceptor-blocking drugs. Prog Cardiovasc Dis. 1976; 19:203-34. [PubMed 10600]
46. Shand DG. State-of-the-art: comparative pharmacology of the β-adrenoceptor blocking drugs. Drugs. 1983; 25(Suppl 2):92-9.
47. Breckenridge A. Which beta blocker? Br Med J. 1983; 286:1085-8. (IDIS 169422)
48. Anon. Choice of a beta-blocker. Med Lett Drugs Ther. 1986; 28:20-2. [PubMed 2869400]
49. Wallin JD, Shah SV. β-Adrenergic blocking agents in the treatment of hypertension: choices based on pharmacological properties and patient characteristics. Arch Intern Med. 1987; 147:654-9. [PubMed 2881524]
50. McDevitt DG. β-Adrenoceptor blocking drugs and partial agonist activity: is it clinically relevant? Drugs. 1983; 25:331-8.
51. McDevitt DG. Clinical significance of cardioselectivity: state-of-the-art. Drugs. 1983; 25(Suppl 2):219-26.
52. Frishman WH. β-Adrenoceptor antagonists: new drugs and new indications. N Engl J Med. 1981; 305:500-6. [PubMed 6114433]
53. Thadani U, Davidson C, Chir B et al. Comparison of the immediate effects of five β-adrenoceptor-blocking drugs with different ancillary properties in angina pectoris. N Engl J Med. 1979; 300:750-5. [PubMed 581782]
54. Lewis RV, McDevitt DG. Adverse reactions and interactions with β-adrenoceptor blocking drugs. Med Toxicol. 1986; 1:343-61. [PubMed 2878346]
55. Frishman WH. Clinical differences between beta-adrenergic blocking agents: implications for therapeutic substitution. Am Heart J. 1987; 113:1190-8. [PubMed 2883867]
56. Dahlof B, Devereux RB, Kjeldsen SE, et al. Cardiovascular morbidity and mortality in the Losartan Intervention For Endpoint Reduction in Hypertension Study (LIFE). Lancet. 2002;359:995-1003. [PubMed 11937178]
500. National Heart, Lung, and Blood Institute National High Blood Pressure Education Program. The seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC 7). Bethesda, MD: National Institutes of Health; 2004 Aug. (NIH publication No. 04-5230.)
501. James PA, Oparil S, Carter BL et al. 2014 evidence-based guideline for the management of high blood pressure in adults: report from the panel members appointed to the Eighth Joint National Committee (JNC 8). JAMA. 2014; 311:507-20. [PubMed 24352797]
502. Mancia G, Fagard R, Narkiewicz K et al. 2013 ESH/ESC Guidelines for the management of arterial hypertension: the Task Force for the management of arterial hypertension of the European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). J Hypertens. 2013; 31:1281-357. [PubMed 23817082]
503. Go AS, Bauman MA, Coleman King SM et al. An effective approach to high blood pressure control: a science advisory from the American Heart Association, the American College of Cardiology, and the Centers for Disease Control and Prevention. Hypertension. 2014; 63:878-85. [PubMed 24243703]
504. Weber MA, Schiffrin EL, White WB et al. Clinical practice guidelines for the management of hypertension in the community: a statement by the American Society of Hypertension and the International Society of Hypertension. J Clin Hypertens (Greenwich). 2014; 16:14-26. [PubMed 24341872]
515. Thomas G, Shishehbor M, Brill D et al. New hypertension guidelines: one size fits most?. Cleve Clin J Med. 2014; 81:178-88. [PubMed 24591473]
523. Fihn SD, Gardin JM, Abrams J et al. 2012 ACCF/AHA/ACP/AATS/PCNA/SCAI/STS guideline for the diagnosis and management of patients with stable ischemic heart disease: a report of the American College of Cardiology Foundation/American Heart Association task force on practice guidelines, and the American College of Physicians, American Association for Thoracic Surgery, Preventive Cardiovascular Nurses Association, Society for Cardiovascular Angiography and Interventions, and Society of Thoracic Surgeons. Circulation. 2012; 126:e354-471. [PubMed 23166211]
524. WRITING COMMITTEE MEMBERS, Yancy CW, Jessup M et al. 2013 ACCF/AHA guideline for the management of heart failure: a report of the American College of Cardiology Foundation/American Heart Association Task Force on practice guidelines. Circulation. 2013; 128:e240-327. [PubMed 23741058]
527. O'Gara PT, Kushner FG, Ascheim DD et al. 2013 ACCF/AHA guideline for the management of ST-elevation myocardial infarction: a report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines. Circulation. 2013; 127:e362-425. [PubMed 23247304]
600. Epic Pharma. Betaxolol tablets prescribing information. Laurelton, NY; 2011 Sep.
800. Yancy CW, Jessup M, Bozkurt B et al. 2016 ACC/AHA/HFSA Focused Update on New Pharmacological Therapy for Heart Failure: An Update of the 2013 ACCF/AHA Guideline for the Management of Heart Failure: A Report of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines and the Heart Failure Society of America. Circulation. 2016; :. [PubMed 27208050]
a. AHFS Drug Information 2004. McEvoy GK, ed. Clonidine. American Society of Health-System Pharmacists; 2004:1648-55.
More about Kerlone (betaxolol)
- Side Effects
- During Pregnancy or Breastfeeding
- Dosage Information
- Drug Images
- Drug Interactions
- Support Group
- En Español
- 0 Reviews – Add your own review/rating
- Drug class: cardioselective beta blockers