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Atenolol

C07A - Beta blocking agents ATC C07AB03 Small molecule approved 1981 Oral Parenteral Natural product Black-box warning

JFDA label: Loten-100mg tablet

⚠ Black-Box Warning
  • Cessation of therapy:

Mechanism of Action

Antagonist of Beta-1 adrenergic receptor — Beta-1 adrenergic receptor antagonist

TargetActionGene / class
Beta-1 adrenergic receptor efficacy ANTAGONIST ADRB1

Indications

Approved

  • Acute myocardial infarction
  • Angina pectoris caused by coronary atherosclerosis
  • Chronic kidney disease (CKD) and hypertension
  • Coronary artery disease (CAD) and hypertension
  • Hypertension
  • ST-elevation myocardial infarction

Off-label

  • Acute ethanol withdrawal (in combination with a benzodiazepine)
  • Atrial fibrillation (rate control)
  • Non-ST-elevation acute coronary syndrome
  • Pediatric hypertension
  • Thyrotoxicosis
  • Ventricular arrhythmias

Contraindications

Source: Lexicomp · Curated

  • Additional contraindications (not in US labeling): Bradycardia (regardless of origin) Absolute
  • Cardiogenic shock or decompensated heart failure Absolute
  • Hypersensitivity to atenolol or any component of the formulation Absolute
  • Pheochromocytoma (in the absence of alpha-blockade) Absolute
  • anesthesia with agents that produce myocardial depression Absolute
  • cardiogenic shock Absolute
  • cor pulmonale Absolute
  • heart block greater than first-degree (except in patients with a functioning artificial pacemaker) Absolute
  • hypotension Absolute
  • metabolic acidosis Absolute
  • severe peripheral arterial disorders Absolute
  • sinus bradycardia Absolute
  • sinus node dysfunction Absolute
  • uncompensated cardiac failure Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (10)

Common Bradycardia · Bradycardia (persistent) · cardiac failure · chest pain · cold extremities · complete atrioventricular block · edema · hypotension · Raynaud's phenomenon · second degree atrioventricular block

Vascular disorders (1)

Common Cold extremities

Nervous system disorders (10)

Common Confusion · decreased mental acuity · depression · Dizziness · dizziness · fatigue · headache · insomnia · lethargy · nightmares

Renal and urinary disorders (1)

Common Impotence

Gastrointestinal disorders (3)

Common Constipation · diarrhea · nausea

Psychiatric disorders (1)

Uncommon Depression

Reproductive system and breast disorders (1)

Common Erectile dysfunction

General disorders and administration site conditions (1)

Very Common Fatigue

Respiratory, thoracic and mediastinal disorders (1)

Uncommon Bronchospasm

Dosing

Source: Lexicomp

Hypertension: Oral: Initial: 25 to 50 mg once daily, after 1 to 2 weeks, may increase to 100 mg once daily; usual dose (ASH/ISH [Weber 2014]): 100 mg once daily; target dose (JNC 8 [James 2013]): 100 mg once daily. Doses >100 mg are unlikely to produce any further benefit. Angina pectoris: Oral: 50 mg once daily; may increase to 100 mg daily. Some patients may require 200 mg daily. Myocardial infarction (ST elevation MI or NSTE-ACS): Oral: Initial: 100 mg once daily or 50 mg twice daily according the manufacturer based on an early trial in this setting with an aggressive dosing regimen (ISIS-1 1986); may consider lower doses (eg, 25 mg twice daily) with titration. In general, oral beta-blockers should be initiated within the first 24 hours post myocardial infarction and continued indefinitely for most patients (ACC/AHA [Amsterdam 2014] ACCF/AHA [O’Gara 2013]). Atrial fibrillation (rate control) (off-label use): Usual maintenance dose: 25 to 100 mg once daily (AHA/ACC/HRS [January 2014]) Supraventricular tachycardia (off-label use): Oral: Initial: 25 to 50 mg daily; maximum maintenance dose: 100 mg/day (ACC/AHA/HRS [Page 2015]) Thyrotoxicosis (off-label use): Oral: 25 to 100 mg once or twice daily (Ross 2016)
(For additional information see "Atenolol: Pediatric drug information") Hypertension: Oral: Children and Adolescents: Initial: 0.5 to 1 mg/kg/dose either once daily or divided in doses twice daily; titrate dose to effect; usual range: 0.5 to 1.5 mg/kg/day; maximum dose: 2 mg/kg/day up to 100 mg/day (NHBPEP 2004; NLHBI 2011).
Refer to adult dosing. In the management of hypertension, consider lower initial doses and titrate to response (Aronow, 2011).
CrCl >35 mL/minute/1.73 m2: No dosage adjustment necessary. CrCl 15 to 35 mL/minute/1.73 m2: Maximum dose: 50 mg daily CrCl 2: Maximum dose: 25 mg daily Hemodialysis: Moderately dialyzable (20% to 50%) via hemodialysis; administer dose postdialysis or administer 25 to 50 mg supplemental dose. Peritoneal dialysis: Elimination is not enhanced; supplemental dose is not necessary.
There are no dosage adjustments provided in the manufacturer’s labeling; however, atenolol undergoes minimal hepatic metabolism.

Warnings & Precautions

Source: Lexicomp

Anaphylactic reactions

Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects. Disease-related concerns:

Bronchospastic disease

In general, patients with bronchospastic disease should not receive beta-blockers; however, atenolol, with B1 selectivity, has been used cautiously with close monitoring.

Conduction abnormality

Consider preexisting conditions such as sick sinus syndrome before initiating.

Diabetes

Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms.

Heart failure (HF)

Use with caution in patients with compensated heart failure and monitor for a worsening of the condition (efficacy of atenolol in HF has not been demonstrated).

Myasthenia gravis

Use with caution in patients with myasthenia gravis.

Peripheral vascular disease (PVD) and Raynaud disease

May precipitate or aggravate symptoms of arterial insufficiency in patients with PVD and Raynaud disease. Use with caution and monitor for progression of arterial obstruction.

Pheochromocytoma (untreated)

Adequate alpha-blockade is required prior to use of any beta-blocker.

Prinzmetal variant angina

Beta-blockers without alpha1-adrenergic receptor blocking activity should be avoided in patients with Prinzmetal variant angina since unopposed alpha1-adrenergic receptors mediate coronary vasoconstriction and can worsen anginal symptoms (Mayer, 1998).

Psoriasis

Beta-blocker use has been associated with induction or exacerbation of psoriasis, but cause and effect have not been firmly established.

Psychiatric disease

Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression.

Renal impairment

Use with caution in patients with renal impairment; dosage adjustment required.

Thyroid disease

May mask signs of hyperthyroidism (eg, tachycardia). If hyperthyroidism is suspected, carefully manage and monitor; abrupt withdrawal may precipitate thyroid storm. Alterations in thyroid function tests may be observed. Concurrent drug therapy issues:

Calcium channel blockers

Use with caution in patients on concurrent verapamil or diltiazem; bradycardia or heart block can occur.

Cardiac glycosides

Use with caution in patients receiving digoxin; bradycardia or heart block can occur.

Inhaled anesthetic agents

Use with caution in patients receiving inhaled anesthetic agents known to depress myocardial contractility. Special populations:

Elderly

Bradycardia may be observed more frequently in elderly patients (>65 years of age); dosage reductions may be necessary. Other warnings/precautions:

Abrupt withdrawal

Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia. Severe exacerbation of angina, ventricular arrhythmias, and myocardial infarction (MI) have been reported following abrupt withdrawal of beta-blocker therapy. Temporary but prompt resumption of beta-blocker therapy may be indicated with worsening of angina or acute coronary insufficiency.

Major surgery

Chronic beta-blocker therapy should not be routinely withdrawn prior to major surgery.

Pregnancy & Lactation

Pregnancy

FDA category D

Avoid

Most beta-blockers are class D. Atenolol specifically associated with IUGR in multiple studies. Use labetalol or methyldopa instead for hypertension in pregnancy

Lactation

Atenolol is excreted in breast milk. Bradycardia has been observed in some nursing infants and neonates may also be at risk for hypoglycemia. Adverse events may be more likely in premature infants or infants with impaired renal function. The manufacturer recommends that caution be used if administered to a nursing woman.

Monitoring

Clinical pearlAcute cardiac treatment: Monitor ECG and blood pressure

Chemistry & Properties

2D structure
FormulaC14H22N2O3
Molecular weight266.34 g/mol
IUPAC name2-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide
CAS29122-68-7
PubChem CID2249
InChIKeyMETKIMKYRPQLGS-UHFFFAOYSA-N
logP0.45 (XLogP 0.2)
Polar surface area84.58 Ų
H-bond acceptors / donors4 / 3
Drug-likeness (QED)0.64
Lipinski violations0
SMILESCC(C)NCC(O)COc1ccc(CC(N)=O)cc1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantYes (logBB -0.9)

Enzyme interactions

EnzymeRoleDetail
CYP2C19Substrate —
CYP2D6Substrate —
CYP3A4Substrate —

Receptor binding (top 2)

TargetActionAffinity
adrenergic Beta1 (ADRB1) Binding pKi 6.4
adrenergic Beta2 (ADRB2) Binding pKi 5.1

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)OCT1 (Inhibitor)OCT2 (Inhibitor)OCT3 (Inhibitor)OCTN2 (Inhibitor)P-gp (Inhibitor)MATE1 (Substrate)MATE2 (Substrate)MDR1 (Substrate)OATP1A2 (Substrate)OATP2B1 (Substrate)OCT1 (Substrate)OCT2 (Substrate)P-gp (Substrate)Transporter(unspecified) (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drugSeverityManagement
Aminophylline major
Ceritinib major
Dolasetron major
Dyphylline major
Fingolimod major
Methacholine major
Oxtriphylline major
Siponimod major
Theophylline major
Acetohexamide moderate
Aldesleukin moderate
Alectinib moderate
Alimemazine moderate
Amifostine moderate
Atropine moderate
Betamethasone moderate
Brigatinib moderate
Brimonidine (ophthalmic) moderate
Brimonidine (topical) moderate
Budesonide moderate
Bupropion moderate
Calcium Phosphate moderate
Calcium acetate moderate
Calcium carbonate moderate
Calcium citrate moderate
Calcium glubionate anhydrous moderate
Calcium gluconate moderate
Calcium lactate moderate
Canagliflozin moderate
Chlorphenesin moderate
Chlorpropamide moderate
Cimetidine moderate
Clidinium moderate
Codeine moderate
Corticotropin moderate
Crizotinib moderate
Dapagliflozin moderate
Deflazacort moderate
Dexamethasone moderate
Diatrizoate moderate

Showing 40 of 100+.

Registered Products (19)

BrandForm / strengthPackAgentCitizen (JOD)
Loten-100mg tablet Tablet 100 mg 10 tab pack varies AL-RAM PHARMA.INDUS.CO.LTD/JORDAN 1.360
Atelol Tablets Tablet 100 mg 14 tab The Arab Pharmaceutical Manufactruing Co. 1.900
Hypoten 100 Tablets Tablet 100 mg 14 tab pack varies Hikma Pharmaceuticals Co.Ltd/Jordan 1.900
Tenolol 100 Tablet Tablet 100 mg 14 tab pack varies UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN 1.900
TENORMIN TAB Tablet 100 mg 14 tab Shawi & Rushedat Drug Store 2.050
Atelol Tablets Tablet 50 mg 2x14's The Arab Pharmaceutical Manufactruing Co. 2.580
Hypoten 50 Tablets Tablet 50 mg 28 tab pack varies Hikma Pharmaceuticals Co.Ltd/Jordan 2.580
Tenolol 50 Tablets Tablet 50 mg 28 tab pack varies UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN 2.580
Hyporetic 100 Tablets Tablet 100 mg, 25 mg 14 tab Hikma Pharmaceuticals Co.Ltd/Jordan 2.610
Loten- Tablet 50 mg 30 tab pack varies AL-RAM PHARMA.INDUS.CO.LTD/JORDAN 2.760
Tenoretic Tablet Tablet 100 mg, 25 mg 14 tab Shawi & Rushedat Drug Store 2.800
Tenormin Tablet Tablet 50 mg 28 tab Shawi & Rushedat Drug Store 2.870
Loten-100mg tablet Tablet 100 mg 30 tab pack varies AL-RAM PHARMA.INDUS.CO.LTD/JORDAN 3.840
Hypoten 50 Tablets Tablet 50 mg 700 tab pack varies Hikma Pharmaceuticals Co.Ltd/Jordan 54.830
Tenolol 50 Tablets Tablet 50 mg 700 tab pack varies UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN 54.830
Loten- Tablet 50 mg 1000 tab pack varies AL-RAM PHARMA.INDUS.CO.LTD/JORDAN 78.200
Hypoten 100 Tablets Tablet 100 mg 700 tab pack varies Hikma Pharmaceuticals Co.Ltd/Jordan 80.750
Tenolol 100 Tablet Tablet 100 mg 700 tab pack varies UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN 80.750
Loten-100mg tablet Tablet 100 mg 1000 tab pack varies AL-RAM PHARMA.INDUS.CO.LTD/JORDAN 115.600