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
Brands: Kerlone
Introduction
A β1-selective adrenergic blocking agent.1 2 3 4 5 6 7 8 9 10 24 25
Uses for Betaxolol Hydrochloride
Hypertension
Management of hypertension (alone or in combination with other classes of antihypertensive agents).1 28
One of several preferred initial therapies in hypertensive patients with heart failure, postmyocardial infarction, ischemic heart disease, and/or diabetes mellitus.37
Can be used as monotherapy for initial management of uncomplicated hypertension; however, thiazide diuretics are preferred by JNC 7.37
Betaxolol Hydrochloride Dosage and Administration
General
Individualize dosage according to patient response and tolerance.1 28 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.)
Administration
Oral Administration
Administer orally;1 absorption does not appear to be affected by food or alcohol.1
Dosage
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
Adults
Hypertension
Oral
Initially, 5–10 mg once daily.1 28 30 37 Increase dosage gradually up to 20 mg daily.1 2 3 16 30 37
Prescribing Limits
Adults
Hypertension
Oral
Maximum 40 mg daily.1 28
Special Populations
Hepatic Impairment
Dosage reductions are not routinely necessary.1 Use with caution; monitor patients carefully.1
Renal Impairment
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
Geriatric Patients
Initially, 5 mg daily.1
Bronchospastic Disease
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 Betaxolol Hydrochloride
Contraindications
Known hypersensitivity to betaxolol.1
Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, or overt cardiac failure.1
Warnings/Precautions
Warnings
Cardiac Failure
Possible precipitation of CHF.1
Avoid use in patients with decompensated CHF; 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 cardiac failure occur; if cardiac 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
Bronchospastic Disease
Possible bronchoconstriction.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
Major Surgery
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
Thyrotoxicosis
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
Sensitivity Reactions
Anaphylactic Reactions
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
General Precautions
Intraocular Pressure
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.)
Specific Populations
Pregnancy
Category C.1
Lactation
Distributed into milk.1 Use with caution.1
Pediatric Use
Safety and efficacy not established.1
Geriatric Use
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.)
Hepatic Impairment
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.)
Renal Impairment
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 Betaxolol Hydrochloride
Specific Drugs
Drug | Interaction | Comments |
|---|---|---|
β-Adrenergic blocking agents (opthalmic 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 |
Chlorthalidone | Pharmacokinetic interaction unlikely1 | |
Cimetidine | Pharmacokinetic interaction unlikely1 | |
Clonidine | 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 |
Hydrochlorothiazide | Pharmacokinetic interaction unlikely1 | |
Nifedipine | Pharmacokinetic interaction unlikely1 | |
Reserpine | Additive effects1 | Monitor for signs of hypotension and bradycardia (e.g., vertigo, syncope, postural hypotension)1 |
Warfarin | No potentiation of anticoagulant effect1 |
Betaxolol Hydrochloride Pharmacokinetics
Absorption
Bioavailability
Well absorbed following oral administration, with peak plasma concentration usually attained within 1.5–6 hours.1
Absolute bioavailability is 89%.1
Onset
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
Food or alcohol does not appear to affect absorption.1
Distribution
Extent
Distributed into milk.1
Plasma Protein Binding
Approximately 50%.1
Elimination
Metabolism
Metabolized in the liver.1
Elimination Route
Excreted in the urine as metabolites and unchanged drug.1
Half-life
14–22 hours.1
Special Populations
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
Stability
Storage
Oral
Tablets
15–25°C.1
ActionsActions
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.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablets, film-coated | 10 mg* | Betaxolol Hydrochloride Tablets | Amide |
Kerlone | Sanofi-Synthelabo | |||
20 mg* | Betaxolol Hydrochloride Tablets | Amide | ||
Kerlone | Sanofi-Synthelabo |
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Betaxolol HCl 10MG Tablets (ACTAVIS TOTOWA): 30/$44.99 or 90/$113.97
Kerlone 10MG Tablets (SANOFI-AVENTIS U.S.): 30/$50.99 or 90/$134.97
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions July 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
References
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. [IDIS 151861] [PubMed 6124227]
9. Caldwell DR, Salisbury CR, Guzek JP. Effects of topical betaxolol in ocular hypertensive patients. Arch Ophthalmol. 1984; 102:539-40. [IDIS 183932] [PubMed 6704008]
10. Smith JP, Weeks RH, Newland EF et al. Betaxolol and acetazolamide: combined ocular hypotensive effect. Arch Ophthalmol. 1984; 102:1794-5. [IDIS 192616] [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. [IDIS 180348] [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. [IDIS 115944] [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. [IDIS 177952] [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. [IDIS 210401] [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.
28. Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure. The fifth report of the Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure (JNC V). Arch Intern Med. 1993; 153:154-83. [IDIS 309043] [PubMed 8422206]
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. [IDIS 452007] [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. [IDIS 490723] [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. [IDIS 490721] [PubMed 12479763]
37. 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 VII) Express. Bethesda, MD: May 14 2003. From NIH website. (). (Also published in JAMA. 2003; 289.
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.
39. Guidelines Committee. 2003 European Society of Hypertension–European Society of Cardiology guidelines for the management of arterial hypertension. J Hypertension. 2003; 21:1011-53.
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.
41. American Diabetes Association. Treatment of hypertension in adults with diabetes. Diabetes Care. 2003; 26(Suppl 1):S80-2.
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. [IDIS 531054] [PubMed 15811979]
43. Neaton JD, Kuller LH. Diuretics are color blind. JAMA. 2005; 293:1663-6. [IDIS 531056] [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. [IDIS 227948] [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. [IDIS 136600] [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. [IDIS 239050] [PubMed 2878346]
55. Frishman WH. Clinical differences between beta-adrenergic blocking agents: implications for therapeutic substitution. Am Heart J. 1987; 113:1190-8. [IDIS 229873] [PubMed 2883867]
a. AHFS Drug Information 2004. McEvoy GK, ed. Clonidine. American Society of Health-System Pharmacists; 2004:1648-55.
More Betaxolol Hydrochloride resources
- Betaxolol Hydrochloride Dosage
- Betaxolol Hydrochloride Use in Pregnancy & Breastfeeding
- Drug Images
- Betaxolol Hydrochloride Drug Interactions
- Betaxolol Hydrochloride Support Group
- 0 Reviews for Betaxolol Hydrochloride - Add your own review/rating
- Betaxolol Prescribing Information (FDA)
- Betaxolol MedFacts Consumer Leaflet (Wolters Kluwer)
- betaxolol Concise Consumer Information (Cerner Multum)
- betaxolol Advanced Consumer (Micromedex) - Includes Dosage Information
- Kerlone Prescribing Information (FDA)
Compare Betaxolol Hydrochloride with other medications
- Angina Pectoris Prophylaxis
- High Blood Pressure
No comments:
Post a Comment