Class: beta-Adrenergic Blocking Agents
VA Class: CV100
CAS Number: 29122-68-7
Brands: Tenoretic, Tenormin
β1-Selective adrenergic blocking agent.111 118 120 c
Uses for Atenolol
Management of hypertension; used alone or in combination with other classes of antihypertensive agents.108 109 110 111 153 154 155 156 157 158 159 171 172 173 500 501
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
Management of chronic stable angina pectoris.111 112 600 1101
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
Used during acute phase of MI to reduce cardiovascular mortality.111 113 120 122 123 124 134 135 147 527 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
β-Blockers may be useful in the management of certain forms of polymorphic VT† (e.g., associated with acute ischemia).401
Prophylaxis of migraine headache†.228
Not recommended for the treatment of a migraine attack that has already started.228
Management of acute alcohol withdrawal† in conjunction with a benzodiazepine.101 229
Atenolol should not be used as monotherapy for acute alcohol withdrawal†.229 230
Atenolol Dosage and Administration
Individualize dosage according to patient response.111
β1-Adrenergic blocking selectivity diminishes as dosage is increased.111 120
If long-term therapy is discontinued, reduce dosage gradually over a period of about 2 weeks.111 120
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; also has been administered by IV injection, however, a parenteral preparation no longer commercially available in US.111 120 401
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
Initially, 50 mg of atenolol and 25 mg of chlorthalidone once daily.118 If response is not optimal, 100 mg of atenolol and 25 mg of chlorthalidone once daily.118
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
In patients with definite or suspected MI, atenolol has been initiated with IV doses;113 120 however, a parenteral preparation no longer commercially available in US.Oral
Manufacturer recommends 50 mg twice daily or 100 mg once daily for at least 7 days.111 120
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
Some experts recommend an initial dose of 25–50 mg daily and usual maintenance dosage of 25–100 mg daily for ongoing therapy.300 301
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
Minimal hepatic metabolism; no dosage adjustment recommended.111 120
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
Patients with Clcr<15 mL/minute per 1.73 m2: Maximum 25 mg daily or 50 mg every other day.111 120
Hemodialysis patients: May administer 25 or 50 mg after each dialysis.111 Marked reductions in BP may occur; give under careful supervision.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
Do not use in patients with untreated pheochromocytoma.111 118 120
Hypersensitivity to atenolol or any ingredient in the formulation.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
Possible increased reactivity to a variety of allergens; patients may be unresponsive to usual doses of epinephrine used to treat anaphylactic reactions.111 118 120
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
If bronchospasm occurs, reduce dosage or discontinue atenolol (gradually if possible) and administer supportive treatment.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
Atenolol effects can be reversed by cautious administration of β-agonists (e.g., dobutamine, isoproterenol).111 120
Diabetes and Hypoglycemia
Possible decreased signs and symptoms of hypoglycemia, particularly tachycardia.111 120
β1-Selective atenolol does not potentiate insulin-induced hypoglycemia or delay recovery of blood glucose to normal levels.111 120
Signs of hyperthyroidism (e.g., tachycardia) may be masked.111 120
Possible thyroid storm if therapy is abruptly withdrawn; carefully monitor patients having or suspected of developing thyrotoxicosis.111 120
Peripheral Arterial Circulatory Disorders
May be aggravated.111 118 120
Atenolol shares the toxic potentials of β-blockers; observe usual precautions of these agents.c
When used in fixed combination with chlorthalidone, consider the cautions, precautions, and contraindications associated with thiazide diuretics.115 116 117 118
Category D.111 118 120
Distributed into milk;103 107 111 118 120 125 129 caution if used in nursing women.111 118 120 151
Safety and efficacy remain to be fully established in children;111 118 120 however, some experts have recommended dosages for hypertension based on current limited clinical experience.258
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.)
Decreased clearance; use with caution and adjust dosage based on degree of renal impairment.111 120 (See Renal Impairment 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
Potential additive effect111 120
Adjust initial and subsequent atenolol dosage downward based on clinical findings (e.g., BP, heart rate)111 120
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
Potential for bradycardia and heart block, increase in left ventricular end diastolic pressure111 120
Adjust dosage carefullyc
Patients with preexisting conduction abnormalities or left ventricular dysfunction particularly susceptible111 120
Catecholamine-depleting drugs (e.g., reserpine)
Potential for additive effects (increased hypotension and marked bradycardia)111 120
Monitor closely for symptoms (e.g., vertigo, syncope, postural hypotension)111 120
May exacerbate rebound hypertension following discontinuance of clonidine111 120
Discontinue atenolol therapy several days before clonidine discontinuance111 120
If replacing clonidine, delay initiation of atenolol for several days after stopping clonidine111 120
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)
Potential for decreased atenolol antihypertensive effect111 118 120
Studies indicate no clinically important interaction; concomitant administration appears safe and effective111 118 120
50–60% following oral administration.c
1 hour following oral administration.111 120 Within 5 minutes following IV administration.111 120
At least 24 hours following oral administration (antihypertensive and β-adrenergic blocking effects).111 120 About 12 hours following IV administration (effect on heart rate).120
In geriatric patients, plasma concentrations are increased.111 118 120
Well distributed into most tissues and fluids except brain and CSF.c
Readily crosses the placenta, has been detected in cord blood.102 111 118 120
Distributed into milk in concentrations higher than those in serum.103 107 111 118 120 125 129 131
Plasma Protein Binding
Approximately 6–16%.111 118 120
Little or no hepatic metabolism.c
40–50% excreted unchanged in urine following oral administration;c remainder in feces, principally as unabsorbed drug.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
In geriatric patients, total clearance is decreased by about 50%, plasma half-life is prolonged.111 118 120
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
Decreases resting and exercise-stimulated heart rate and reflex orthostatic tachycardia by about 25–35%.c Slows AV nodal conduction.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
In patients with angina pectoris, blocks catecholamine-induced increases in heart rate, myocardial contractility, and BP, resulting in decreased myocardial oxygen consumption.111 120 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 advising patients with coronary artery disease to temporarily limit their physical activity when discontinuing therapy.111 118 120
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 women informing clinicians if they are or plan to become pregnant or plan to breast-feed.111 118 120
Importance of clinician informing women who are or plan to become pregnant of risk to fetus.111 118 120
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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