Class: beta-Adrenergic Blocking Agents
VA Class: CV100
CAS Number: 29122-68-7
Medically reviewed on October 30, 2017
Uses for Atenolol
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).237 501 502 503 504 515 523 524 527 800
Black hypertensive patients generally tend to respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to β-blockers.232 259 260 500 501 504 However, diminished response to β-blockers is largely eliminated when administered concomitantly with a thiazide diuretic.500
Chronic Stable Angina
β-Blockers are recommended as first-line anti-ischemic drugs in most patients with chronic stable angina; despite differences in cardioselectivity, intrinsic sympathomimetic activity, and other clinical factors, all β-blockers appear to be equally effective for this use.1101
Non-ST-Segment-Elevation Acute Coronary Syndromes (NSTE ACS)
Used as part of the standard therapeutic measures for managing NSTE ACS, which include unstable angina and non-ST-segment-elevation MI (NSTEMI).1100
Expert guidelines recommend initiation of oral β-blocker therapy within the first 24 hours in patients who do not have manifestations of heart failure, evidence of low-output state, increased risk of cardiogenic shock, or any other contraindications to β-blocker therapy.1100
Continue β-blocker therapy for secondary prevention in patients with stabilized heart failure and reduced systolic function (preferably with bisoprolol, carvedilol, or metoprolol succinate because of proven mortality benefit).1100
Expert guidelines recommend initiation of oral β-blocker therapy within the first 24 hours in patients who do not have manifestations of heart failure, evidence of low-output state, increased risk of cardiogenic shock, or any other contraindications to β-blocker therapy.527 1100 Because of conflicting evidence of benefit and potential for harm (e.g., cardiogenic shock), experts recommend limiting use of IV β-blockers to patients with refractory hypertension or ongoing ischemia at time of presentation.527
Continue β-blocker therapy for secondary prevention in post-MI patients with left ventricular systolic dysfunction (preferably with bisoprolol, carvedilol, or metoprolol succinate because of proven mortality benefit).525 Although benefits of long-term β-blockade in patients with normal left ventricular function are less well established, experts recommend continuing β-blocker therapy for at least 3 years in such patients.525
Has been used in the treatment of supraventricular tachycardia† (SVT) (e.g., atrial flutter†, junctional tachycardia†, focal atrial tachycardia†, paroxysmal supraventricular tachycardia [PSVT]†).300 301 401
Vagal maneuvers and/or IV adenosine are considered first-line interventions for acute treatment of SVT when clinically indicated; if such measures are ineffective or not feasible, may consider an IV β-adrenergic blocking agent.300 Oral β-blockers may be used for ongoing management.300 Although evidence of efficacy is limited, experts state that overall safety of β-adrenergic blockers warrants use.300
β-Blockers have been used in patients with cardiac arrest precipitated by ventricular fibrillation† or pulseless VT†; however, routine administration after cardiac arrest is potentially harmful and not recommended.400
Not recommended for the treatment of a migraine attack that has already started.228
Atenolol Dosage and Administration
Individualize dosage according to patient response.111
BP Monitoring and Treatment Goals
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
Once-daily dosing usually is sufficient in the management of hypertension.c
Some experts recommend an initial dosage of 0.5–1 mg/kg daily given as a single dose or in 2 divided doses.258 Increase dosage as necessary up to a maximum dosage of 2 mg/kg (up to 100 mg) daily given as a single dose or in 2 divided doses.258
JNC 8 expert panel recommends initial dosage of 25–50 mg once daily and target dosage of 100 mg once daily based on dosages used in randomized controlled studies.501
Manufacturer recommends initial dosage of 50 mg once daily, alone or in combination with a diuretic; full hypotensive effect usually seen within 1–2 weeks.600 If necessary, may increase dosage to 100 mg once daily.600
Some experts state usual dosage range is 25–100 mg daily.500
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
Atenolol/Chlorthalidone Fixed-combination TherapyOral
Manufacturer states fixed-combination preparation is not recommended for initial therapy; administer each drug separately, then use the fixed combination if the optimum maintenance dosage corresponds to the ratio of drugs in the combination preparation.118 c
May add another antihypertensive agent when necessary (gradually using half of the usual initial dosage to avoid an excessive decrease in BP).118
Chronic Stable Angina
Initially, 50 mg once daily.111
If optimum response is not achieved within 1 week, increase to 100 mg once daily.111
Some patients may require 200 mg once daily for optimum effect.111
May initiate therapy as soon as possible after patient's hemodynamic condition has stabilized.600
Long-term Secondary PreventionOral
Optimal duration of therapy for secondary prevention remains to be clearly established.111 120 527 802 804 Experts generally recommend long-term therapy in post-MI patients with left ventricular systolic dysfunction, and at least 3 years of therapy in those with normal left ventricular function.525 802 804 1101
SVT (e.g., PSVT†, Atrial Flutter†, Junctional Tachycardia†, Atrial Tachycardia†) or Atrial Fibrillation†Oral
Prevention of Common Migraine†Oral
Dosage has not been established; in clinical studies 100 mg daily was usual effective dosage.228
Maximum 2 mg/kg (up to 100 mg) daily.258
Increasing beyond 100 mg daily usually does not result in further improvement in BP control.600
Modify doses and/or frequency of administration in response to the degree of renal impairment.c
Initial dosage of 25 mg daily may be necessary.111
Measure BP just prior to the dose to ensure persistence of adequate BP reduction.111
Patients with Clcr 15–35 mL/minute per 1.73 m2: Maximum 50 daily.111
Modification of dosage may be necessary because of age-related decreases in renal function.111
Initially, 25 mg daily may be necessary.111
Measure BP just prior to a dose to ensure persistence of adequate BP reduction.111
Initially, 50 mg daily and use lowest possible dosage.111 If dosage must be increased, consider administering in 2 divided doses daily to decrease peak blood levels.111 A β2-adrenergic agonist bronchodilator should be available.111 (See Bronchospastic Disease under Cautions.)
Cautions for Atenolol
Patients with sinus bradycardia,111 118 120 220 AV block greater than first degree,111 118 120 220 274 cardiogenic shock,111 118 120 220 overt or decompensated cardiac failure. Patients with acute MI not promptly and effectively controlled by 80 mg IV furosemide or equivalent therapy.111 118 120 220
Possible precipitation of heart failure; possible decreased exercise tolerance in patients with left ventricular dysfunction.
Initiate therapy and subsequent dosage adjustments in patients with heart failure under close medical supervision. Prior to initiation of the drug, stabilize patient on other therapy (e.g., ACE inhibitor, diuretic, and/or cardiac glycoside). Symptomatic improvement may not be evident for 2–3 months after initiating therapy.
Avoid use in patients with decompensated heart failure; use cautiously in patients with inadequate myocardial function and, if necessary, in patients with well-compensated heart failure (e.g., those controlled with ACE inhibitors, cardiac glycosides, and/or diuretics); use with extreme caution in patients with substantial cardiomegaly.
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.
History of Anaphylactic Reactions
Calcium-channel Blocking Agents
Concomitant use may cause bradycardia, heart block, increased left ventricular and diastolic blood pressure, particularly in patients with preexisting conduction abnormalities or left ventricular dysfunction.111 120 (See Specific Drugs under Interactions.)
Possible bronchoconstriction, especially at dosages >100 mg daily.c Cautious use recommended in patients with bronchospastic disease (patients who do not respond to or cannot tolerate other hypotensive agents).111 120
Initiate therapy with 50 mg daily and use lowest possible dosage; β1-selectivity is not absolute.111 120 Twice-daily dosing and concomitant use of a β2-adrenergic agonist bronchodilator may minimize risk of bronchospasm.111 120 c
Anesthesia and Major Surgery
Possible increased risks associated with general anesthesia.111 (See Specific Drugs under Interactions.)
Withdrawal of β-blocker prior to surgery is not recommended in most patients.111
Correct vagal dominance (if any) with atropine (1–2 mg IV).111
Diabetes and Hypoglycemia
Peripheral Arterial Circulatory Disorders
Atenolol shares the toxic potentials of β-blockers; observe usual precautions of these agents.c
Response in patients ≥65 years of age does not appear to differ from that in younger adults; however, use with caution due to greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.111 118 120
Consider age-related decreases in renal function when selecting dosage and adjust dosage if necessary.111 Evaluation of geriatric patients with hypertension or MI should always include assessment of renal function.111 120 (See Geriatric Patients under Dosage and Administration.)
Common Adverse Effects
Tiredness,111 120 hypotension,111 120 heart failure,111 120 bradycardia,111 113 120 124 ventricular tachycardia,111 120 dizziness,111 120 cold extremities,111 120 depression,111 120 supraventricular tachycardia (atrial fibrillation or flutter),111 120 bundle branch block and major axis deviation,111 120 fatigue,111 120 dyspnea.111 120
Interactions for Atenolol
Anesthetics, general (myocardial depressant)
Increased risk of hypotension and heart failurec
Use with caution111 (see Anesthesia and Major Surgery under Cautions)
Calcium-channel blockers (e.g., verapamil, diltiazem)
Additive hypotensive effect; may be used to therapeutic advantagec
Adjust dosage carefullyc
Catecholamine-depleting drugs (e.g., reserpine)
Additive hypotensive effect; may be used to therapeutic advantagec
Adjust dosage carefullyc
Additive or potentiated hypotensive effect; may be used to therapeutic advantagec
Adjust dosage carefully when used concurrentlyc
NSAIAs (e.g., indomethacin, aspirin)
50–60% following oral administration.c
Well distributed into most tissues and fluids except brain and CSF.c
Plasma Protein Binding
Little or no hepatic metabolism.c
In patients with Clcr 15–35 mL/minute per 1.73 m2, plasma half-life is increased to 16–27 hours; in progressive renal impairment plasma half-life is >27 hours.c
Hemodialysis: 1–12% removed.c
Tight, light-resistant containers at 20–25°.111
Tablets (Atenolol and Chlorthalidone)
Tight, light-resistant containers at 20–25°.111
Inhibits response to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium.c Blocks β2-adrenergic receptors within bronchial and vascular smooth muscle only in high doses (e.g., >100 mg daily).c
No intrinsic sympathomimetic activity and little or no membrane-stabilizing effect on the heart.c
Reduces BP by decreasing cardiac output, suppressing renin release, and/or decreasing sympathetic outflow from the CNS.c
Possibly increases oxygen requirements in patients with heart failure due to increased left ventricular fiber length and end diastolic pressure.111
Increases airway resistance (at doses >100 mg) in patients with asthma and/or COPD.c
Produces little or no changes in serum insulin concentrations, time to recovery from insulin-induced hypoglycemia, or free fatty acid response to hypoglycemia.c
Advice to Patients
Importance of taking medication exactly as prescribed.c
Importance of not interrupting or discontinuing therapy without consulting clinician.c
If a dose is missed, importance of patient taking only the next scheduled dose (i.e., the next dose should not be doubled).c
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.c
Importance of patients undergoing major surgery informing anesthesiologist or dentist they are receiving the drug.c
Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs.c
Importance of informing patient of other important precautionary information. (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
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
50 mg with Chlorthalidone 25 mg*
Atenolol and Chlorthalidone Tablets
100 mg with Chlorthalidone 25 mg*
Atenolol and Chlorthalidone Tablets
AHFS DI Essentials. © Copyright 2018, Selected Revisions October 30, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
Only references cited for selected revisions after 1984 are available electronically.
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