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Atenolol (Monograph)

Brand name: Tenormin
Drug class: alpha-Adrenergic Blocking Agents

Medically reviewed by Drugs.com on Apr 10, 2024. Written by ASHP.

Introduction

β1-Selective adrenergic blocking agent.111 118 120 c

Uses for Atenolol

Hypertension

Management of hypertension, alone or in combination with other classes of antihypertensive agents.108 109 110 111 153 154 155 156 157 158 159 171 172 173 501 1200

β-Adrenergic blocking agents (β-blockers) generally not preferred for first-line therapy of hypertension according to current evidence-based hypertension guidelines, 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 1200 A 2017 ACC/AHA multidisciplinary hypertension guideline states that β-blockers used for ischemic heart disease that are also effective in lowering BP include bisoprolol, carvedilol, metoprolol succinate, metoprolol tartrate, nadolol, propranolol, and timolol.1200

Some experts state that use of atenolol for hypertension should be avoided in patients with ischemic heart disease because the drug is less effective than placebo in reducing cardiovascular events and not as effective in treating hypertension as other antihypertensive drugs.1200

Individualize choice of therapy; consider patient characteristics (e.g., age, ethnicity/race, comorbidities, cardiovascular risk) as well as drug-related factors (e.g., ease of administration, availability, adverse effects, cost).501 502 503 504 515 1200 1201

The 2017 ACC/AHA hypertension guideline classifies BP in adults into 4 categories: normal, elevated, stage 1 hypertension, and stage 2 hypertension.1200 (See Table 1.)

Source: Whelton PK, Carey RM, Aronow WS et al. 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults: a report of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines. Hypertension. 2018;71:e13-115

Individuals with SBP and DBP in 2 different categories (e.g., elevated SBP and normal DBP) should be designated as being in the higher BP category (i.e., elevated BP).

Table 1. ACC/AHA BP Classification in Adults1200

Category

SBP (mm Hg)

DBP (mm Hg)

Normal

<120

and

<80

Elevated

120–129

and

<80

Hypertension, Stage 1

130–139

or

80–89

Hypertension, Stage 2

≥140

or

≥90

The goal of hypertension management and prevention is to achieve and maintain optimal control of BP.1200 However, the BP thresholds used to define hypertension, the optimum BP threshold at which to initiate antihypertensive drug therapy, and the ideal target BP values remain controversial.501 503 504 505 506 507 508 515 523 526 530 1200 1201 1207 1209 1222 1223 1229

The 2017 ACC/AHA hypertension guideline generally recommends a target BP goal (i.e., BP to achieve with drug therapy and/or nonpharmacologic intervention) <130/80 mm Hg in all adults regardless of comorbidities or level of atherosclerotic cardiovascular disease (ASCVD) risk.1200 In addition, an SBP goal of <130 mm Hg generally is recommended for noninstitutionalized ambulatory patients ≥65 years of age with an average SBP of ≥130 mm Hg.1200 These BP goals are based upon clinical studies demonstrating continuing reduction of cardiovascular risk at progressively lower levels of SBP.1200 1202 1210

Other hypertension guidelines generally have based target BP goals on age and comorbidities.501 504 536 Guidelines such as those issued by the JNC 8 expert panel generally have targeted a BP goal of <140/90 mm Hg regardless of cardiovascular risk and have used higher BP thresholds and target BPs in elderly patients501 504 compared with those recommended by the 2017 ACC/AHA hypertension guideline.1200

Some clinicians continue to support previous target BPs recommended by JNC 8 due to concerns about the lack of generalizability of data from some clinical trials (e.g., SPRINT study) used to support the 2017 ACC/AHA hypertension guideline1200 and potential harms (e.g., adverse drug effects, costs of therapy) versus benefits of BP lowering in patients at lower risk of cardiovascular disease.1222 1223 1224 1229

Consider potential benefits of hypertension management and drug cost, adverse effects, and risks associated with the use of multiple antihypertensive drugs when deciding a patient’s BP treatment goal.1200 1220 1229

For decisions regarding when to initiate drug therapy (BP threshold), the 2017 ACC/AHA hypertension guideline incorporates underlying cardiovascular risk factors.1200 1207 ASCVD risk assessment recommended by ACC/AHA for all adults with hypertension.1200

ACC/AHA currently recommend initiation of antihypertensive drug therapy in addition to lifestyle/behavioral modifications at an SBP ≥140 mm Hg or DBP ≥90 mm Hg in adults who have no history of cardiovascular disease (i.e., primary prevention) and a low ASCVD risk (10-year risk <10%).1200

For secondary prevention in adults with known cardiovascular disease or for primary prevention in those at higher risk for ASCVD (10-year risk ≥10%), ACC/AHA recommend initiation of antihypertensive drug therapy at an average SBP ≥130 mm Hg or an average DBP ≥80 mm Hg.1200

Adults with hypertension and diabetes mellitus, chronic kidney disease (CKD), or age ≥65 years are assumed to be at high risk for cardiovascular disease; ACC/AHA states that such patients should have antihypertensive drug therapy initiated at a BP ≥130/80 mm Hg.1200 Individualize drug therapy in patients with hypertension and underlying cardiovascular or other risk factors.502 1200

In stage 1 hypertension, experts state that it is reasonable to initiate drug therapy using the stepped-care approach in which one drug is initiated and titrated and other drugs are added sequentially to achieve the target BP.1200 Initiation of antihypertensive therapy with 2 first-line agents from different pharmacologic classes recommended in adults with stage 2 hypertension and average BP >20/10 mm Hg above BP goal.1200

Black hypertensive patients generally tend to respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to β-blockers.232 259 260 501 504 1200 However, diminished response to β-blockers is largely eliminated when administered concomitantly with a thiazide diuretic.500

Chronic Stable Angina

Long-term management of stable angina pectoris due to coronary atherosclerosis.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

Acute MI

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

Supraventricular Arrhythmias

Has been used in the treatment of supraventricular tachycardia† [off-label] (SVT) (e.g., atrial flutter† [off-label], junctional tachycardia† [off-label], focal atrial tachycardia† [off-label], paroxysmal supraventricular tachycardia [PSVT]† [off-label]).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

Used to slow ventricular rate in patients with atrial fibrillation† or flutter†.300 301

Ventricular Arrhythmias

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

Vascular Headache

Prophylaxis of migraine headache†.228

Not recommended for the treatment of a migraine attack that has already started.228

Alcohol Withdrawal

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

General

BP Monitoring and Treatment Goals

Administration

Administer orally; also has been administered by IV injection, however, a parenteral preparation no longer commercially available in US.111 120 401

Oral Administration

Once-daily dosing usually is sufficient in the management of hypertension.c

Dosage

Pediatric Patients

Hypertension†
Oral

Some experts have recommended 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

Adults

Hypertension
Atenolol Therapy
Oral

Initially, 50 mg once daily, alone or in combination with a diuretic recommended by manufacturer; full hypotensive effect usually seen within 1–2 weeks.600 If necessary, may increase dosage to 100 mg once daily.600

Usual dosage range: Some experts state 25–100 mg daily, administered in 2 divided doses.1200

Atenolol/Chlorthalidone Fixed-combination Therapy
Oral

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
Oral

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

Acute MI
Early Treatment

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 Prevention
Oral

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

Supraventricular Arrhythmias†
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

Vascular Headache†
Prevention of Common Migraine†
Oral

Dosage has not been established; in clinical studies 100 mg daily was usual effective dosage.228

Prescribing Limits

Pediatric Patients

Hypertension†
Oral

Maximum 2 mg/kg (up to 100 mg) daily.258

Adults

Hypertension
Monotherapy
Oral

Increasing dosage beyond 100 mg daily usually does not result in further improvement in BP control.600

Special Populations

Hepatic Impairment

Minimal hepatic metabolism; no dosage adjustment recommended.111 120

Renal Impairment

Hypertension
Oral

Modify dose 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

Geriatric Patients

Hypertension

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

Bronchospastic Disease

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.)

Detailed Atenolol dosage information

Cautions for Atenolol

Contraindications

Warnings/Precautions

Warnings

Heart Failure

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.)

Bronchospastic Disease

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

Thyrotoxicosis

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

General Precautions

Peripheral Arterial Circulatory Disorders

May be aggravated.111 118 120

Other Precautions

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

Specific Populations

Pregnancy

Category D.111 118 120

Lactation

Distributed into milk;103 107 111 118 120 125 129 caution if used in nursing women.111 118 120 151

Pediatric Use

Safety and efficacy remain to be fully established in children;111 118 120 however, some experts have recommended dosages for hypertension based on clinical experience.258

Geriatric Use

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.)

Renal Impairment

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

Drug Interactions

Specific Drugs

Drug

Interaction

Comments

β-Blockers

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

Clonidine

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

Hydralazine

Additive hypotensive effect; may be used to therapeutic advantagec

Adjust dosage carefullyc

Methyldopa

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
Atenolol drug interactions (more detail)

Atenolol Pharmacokinetics

Absorption

Bioavailability

50–60% following oral administration.c

Onset

1 hour following oral administration.111 120 Within 5 minutes following IV administration.111 120

Duration

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

Special Populations

In geriatric patients, plasma concentrations are increased.111 118 120

Distribution

Extent

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

Elimination

Metabolism

Little or no hepatic metabolism.c

Elimination Route

40–50% excreted unchanged in urine following oral administration;c remainder in feces, principally as unabsorbed drug.c

Half-life

6–7 hours.c

Special Populations

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

Stability

Storage

Oral

Tablets

Tight, light-resistant containers at 20–25°.111

Tablets (Atenolol and Chlorthalidone)

Tight, light-resistant containers at 20–25°.111

Actions

Advice to Patients

Preparations

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

Atenolol

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

25 mg*

Atenolol Tablets

Tenormin

AstraZeneca

50 mg*

Atenolol Tablets

Tenormin (scored)

AstraZeneca

100 mg*

Atenolol Tablets

Tenormin

AstraZeneca

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Atenolol Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

50 mg with Chlorthalidone 25 mg*

Atenolol and Chlorthalidone Tablets

Tenoretic (scored)

AstraZeneca

100 mg with Chlorthalidone 25 mg*

Atenolol and Chlorthalidone Tablets

Tenoretic

AstraZeneca

AHFS DI Essentials™. © Copyright 2024, Selected Revisions April 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

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