Atenolol
Pronunciation
(a TEN oh lole)
U.S. Brand Names
Tenormin®
Generic Available
Yes: Tablet
Canadian Brand Names
Apo-Atenol®; Gen-Atenolol; Novo-Atenol; Nu-Atenol; PMS-Atenolol; Rhoxal-atenolol; Tenolin; Tenormin®
Use
Treatment of hypertension, alone or in combination with other agents; management of angina pectoris, postmyocardial infarction patients
Use - Unlabeled/Investigational
Acute ethanol withdrawal, supraventricular and ventricular arrhythmias, and migraine headache prophylaxis
Pregnancy Risk Factor
D
Pregnancy Implications
Atenolol crosses the placenta; beta-blockers have been associated with persistent bradycardia, hypotension, and IUGR; IUGR is probably related to maternal hypertension. Available evidence suggests beta-blockers are generally safe during pregnancy (JNC 7). Cases of neonatal hypoglycemia have been reported following maternal use of beta-blockers at parturition or during breast-feeding. Monitor breast-fed infant for symptoms of beta-blockade.
Lactation
Enters breast milk/use caution
Contraindications
Hypersensitivity to atenolol or any component of the formulation; sinus bradycardia; sinus node dysfunction; heart block greater than first-degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; uncompensated cardiac failure; pulmonary edema; pregnancy
Warnings/Precautions
Administer cautiously in compensated heart failure and monitor for a worsening of the condition (efficacy of atenolol in heart failure has not been established). Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia. Use caution with concurrent use of beta-blockers and either verapamil or diltiazem; bradycardia or heart block can occur. Avoid concurrent I.V. use of both agents. Beta-blockers should be avoided in patients with bronchospastic disease (asthma) and peripheral vascular disease (may aggravate arterial insufficiency). Atenolol, with B1 selectivity, has been used cautiously in bronchospastic disease with close monitoring. Use cautiously in diabetics - may mask hypoglycemic symptoms. May mask signs of thyrotoxicosis. May cause fetal harm when administered in pregnancy. Use cautiously in the renally impaired (dosage adjustment required). Use care with anesthetic agents which decrease myocardial function. Caution in myasthenia gravis.
Adverse Reactions
1% to 10%:
Cardiovascular: Persistent bradycardia, hypotension, chest pain, edema, heart failure, second- or third-degree AV block, Raynaud's phenomenon
Central nervous system: Dizziness, fatigue, insomnia, lethargy, confusion, mental impairment, depression, headache, nightmares
Gastrointestinal: Constipation, diarrhea, nausea
Genitourinary: Impotence
Miscellaneous: Cold extremities
<1% (Limited to important or life-threatening): Alopecia, dyspnea (especially with large doses), elevated liver enzymes, hallucinations, impotence, lupus syndrome, Peyronie's disease, positive ANA, psoriaform rash, psychosis, thrombocytopenia, wheezing
Overdosage/Toxicology
Symptoms of toxicity include lethargy, respiratory drive disorder, wheezing, sinus pause and bradycardia. Additional effects associated with any beta-blocker are congestive heart failure, hypotension, bronchospasm, and hypoglycemia. Treatment includes removal of unabsorbed drug by induced emesis, gastric lavage, or administration of activated charcoal and symptomatic treatment of toxic responses. Atenolol can be removed by hemodialysis.
Drug Interactions
Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.
Ampicillin, in single doses of 1 gram, decrease atenolol's pharmacologic actions.
Antacids (magnesium-aluminum, calcium antacids or salts) may reduce the bioavailability of atenolol.
Clonidine: Hypertensive crisis after or during withdrawal of either agent.
Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.
Glucagon: Atenolol may blunt the hyperglycemic action of glucagon.
Insulin and oral hypoglycemics: Atenolol masks the tachycardia that usually accompanies hypoglycemia.
NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.
Salicylates may reduce the antihypertensive effects of beta-blockers.
Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.
Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.
Ethanol/Nutrition/Herb Interactions
Food: Atenolol serum concentrations may be decreased if taken with food.
Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe, ginseng (may worsen hypertension). Avoid garlic (may have increased antihypertensive effect).
Stability
Protect from light
Compatibility
Stable in D5W, NS
Y-site administration: Compatible:
Meperidine, meropenem, morphine.
Incompatible:
Amphotericin B cholesteryl sulfate complex
Mechanism of Action
Competitively blocks response to beta-adrenergic stimulation, selectively blocks beta1-receptors with little or no effect on beta2-receptors except at high doses
Pharmacodynamics/Kinetics
Onset of action: Peak effect: Oral: 2-4 hours
Duration: Normal renal function: 12-24 hours
Absorption: Incomplete
Distribution: Low lipophilicity; does not cross blood-brain barrier
Protein binding: 3% to 15%
Metabolism: Limited hepatic
Half-life elimination: Beta:
Neonates:
35 hours; Mean: 16 hours
Children: 4.6 hours; children >10 years may have longer half-life (>5 hours) compared to children 5-10 years (<5 hours)
Adults: Normal renal function: 6-9 hours, prolonged with renal impairment; End-stage renal disease: 15-35 hours
Excretion: Feces (50%); urine (40% as unchanged drug)
Dosage
Oral:
Children: 0.8-1 mg/kg/dose given daily; range of 0.8-1.5 mg/kg/day; maximum dose: 2 mg/kg/day
Adults:
Hypertension: 25-50 mg once daily, may increase to 100 mg/day. Doses >100 mg are unlikely to produce any further benefit.
Angina pectoris: 50 mg once daily, may increase to 100 mg/day. Some patients may require 200 mg/day.
Postmyocardial infarction: Follow I.V. dose with 100 mg/day or 50 mg twice daily for 6-9 days postmyocardial infarction.
I.V.:
Hypertension: Dosages of 1.25-5 mg every 6-12 hours have been used in short-term management of patients unable to take oral enteral beta-blockers
Postmyocardial infarction: Early treatment: 5 mg slow I.V. over 5 minutes; may repeat in 10 minutes. If both doses are tolerated, may start oral atenolol 50 mg every 12 hours or 100 mg/day for 6-9 days postmyocardial infarction.
Dosing interval for oral atenolol in renal impairment:
Clcr 15-35 mL/minute: Administer 50 mg/day maximum.
Clcr<15 mL/minute: Administer 50 mg every other day maximum.
Hemodialysis: Moderately dialyzable (20% to 50%) via hemodialysis; administer dose postdialysis or administer 25-50 mg supplemental dose.
Peritoneal dialysis: Elimination is not enhanced; supplemental dose is not necessary.
Administration
When administered acutely for cardiac treatment, monitor ECG and blood pressure. The injection can be administered undiluted or diluted with a compatible I.V. solution. May administer by rapid infusion (I.V. push) at a rate of 1 mg/minute or by slow infusion over ~30 minutes. Necessary monitoring for surgical patients who are unable to take oral beta-blockers (prolonged ileus) has not been defined. Some institutions require monitoring of baseline and postinfusion heart rate and blood pressure when a patient's response to beta-blockade has not been characterized (ie, the patient's initial dose or following a change in dose). Consult individual institutional policies and procedures.
Monitoring Parameters
Acute cardiac treatment: Monitor ECG and blood pressure with I.V. administration; heart rate and blood pressure with oral administration
Test Interactions
Increased glucose; decreased HDL
Dietary Considerations
May be taken without regard to meals.
Patient Education
Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take exactly as directed; with or without regard to meals; do not take with antacids. Do not adjust dosage or discontinue without consulting prescriber. Take pulse daily (prior to medication) and follow prescriber's instruction about holding medication. If you have diabetes, monitor serum sugar closely (drug may alter glucose tolerance or mask signs of hypoglycemia). May cause fatigue, dizziness, or postural hypotension (use caution when changing position from lying or sitting to standing, when driving, or climbing stairs until response to medication is known). Alteration in sexual performance (reversible); or constipation (increased dietary bulk and fluids and exercise may help). Report unresolved swelling of extremities, respiratory difficulty or new cough, unresolved fatigue, unusual weight gain, unresolved constipation, or unusual muscle weakness.
Pregnancy/breast-feeding precautions:
Do not get pregnant or cause a pregnancy (males) while using this medication. Consult prescriber for appropriate contraceptive measures. Consult prescriber if breast-feeding.
Anesthesia and Critical Care Concerns/Other Considerations
Atenolol may mask signs and symptoms of hypoglycemia; may potentiate hypoglycemia in a diabetic patient.
Myocardial Infarction:
Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block.
Surgery:
Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.
Withdrawal:
Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.
Cardiovascular Considerations
Hypertension: Beta-blocker therapy in the treatment of hypertension has been associated with improved cardiovascular outcomes. This class of drug is beneficial for elderly patients with hypertension. A recent UKPDS study showed that beta-blocker therapy (atenolol) was as effective as an ACE inhibitor in reducing cardiovascular events and that the benefits of therapy were related more to the degree of antihypertensive efficacy rather than the class of drug used.
Myocardial infarction: Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block.
Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.
Atrial fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.
Angina: Beta-blockers are effective in the treatment of angina as monotherapy or when combined with nitrates and/or calcium channel blockers. In patients with severe intractable angina requiring negative cardiac chronotropic medications, pacemaker placement has been carried out to maintain heart rate in the setting of large doses of beta-blockers and/or calcium channel blockers. Beta-blockers are ineffective in the treatment of pure vasospastic (Prinzmetal) angina.
Unstable angina/non-ST-segment elevation MI: In the treatment of unstable angina/non-ST-segment elevation MI, a beta-blocker, with the first dose administered intravenously if there is ongoing chest pain, followed by oral administration, is recommended (in the absence of contraindications).
Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.
Heart failure: There is emerging evidence that beta-blocker therapy, without intrinsic sympathomimetic activity (ISA), should be initiated in select patients with
stable
congestive heart failure (NYHA Class II-III). To date, carvedilol, sustained release metoprolol, and bisoprolol have demonstrated a beneficial effect on morbidity and mortality. It is important that beta-blocker therapy be instituted initially at very low doses with gradual and very careful titration.
Dental Health: Effects on Dental Treatment
Atenolol is a cardioselective beta-blocker. Local anesthetic with vasoconstrictor can be safely used in patients medicated with atenolol. Nonselective beta-blockers (ie, propranolol, nadolol) enhance the pressor response to epinephrine, resulting in hypertension and bradycardia; this has not been reported for atenolol. Many nonsteroidal anti-inflammatory drugs, such as ibuprofen and indomethacin, can reduce the hypotensive effect of beta-blockers after 3 or more weeks of therapy with the NSAID. Short-term NSAID use (ie, 3 days) requires no special precautions in patients taking beta-blockers.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause fatigue, insomnia, and confusion which can clinically look like depression
Mental Health: Effects on Psychiatric Treatment
Concurrent use with other psychotropics may produce an additive hypotensive response (especially low potency antipsychotics and TCAs)
Dosage Forms
Injection, solution: 0.5 mg/mL (10 mL)
Tablet: 25 mg, 50 mg, 100 mg
Extemporaneously Prepared
A 2 mg/mL atenolol oral liquid compounded from tablets and a commercially available oral diluent was found to be stable for up to 40 days when stored at 5°C or 25°C.
Garner SS, Wiest DB, and Reynolds ER, "Stability of Atenolol in an Extemporaneously Compounded Oral Liquid,"
Am J Hosp Pharm
, 1994, 51(4):508-11.
References
"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,"
Pediatrics
, 2001, 108(3):776-89.
Antman EM, Anbe SC, Alpert JS, et al, "ACC/AHA Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction - Executive Summary: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Writing Committee to Revise the 1999 Guidelines for the Management of Patients With Acute Myocardial Infarction),"
Circulation
, 2004, 110:588-636. Available at: http://www.circulationaha.org/cgi/content/full/110/5/588. Last accessed August 26, 2004.
Braunwald E, Antman EM, Beasley JW, et al, "ACC/AHA 2002 Guideline Update for the Management of Patients With Unstable Angina and Non-ST-Segment Elevation Myocardial Infarction - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Unstable Angina),"
J Am Coll Cardiol
, 2002, 40(7):1366-74. Available at: http://www.acc.org/clinical/guidelines/unstable/incorporated/index.htm. Accessed May 20, 2003.
Chobanian AV, Bakris GL, Black HR, et al, "The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: The JNC 7 Report,"
JAMA
, 2003, 289(19):2560-71.
"Consensus Recommendations for the Management of Chronic Heart Failure. On Behalf of the Membership of the Advisory Council to Improve Outcomes Nationwide in Heart Failure,"
Am J Cardiol
, 1999, 83(2A):1A-38A.
Gibbons RJ, Abrams J, Chatterjee K, et al, "ACC/AHA 2002 Guideline Update for the Management of Patients With Chronic Stable Angina - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Chronic Stable Angina),"
J Am Coll Cardiol
, 2003, 41(1):159-68.
Mangano DT, Layug EL, Wallace A, et al, "Effect of Atenolol on Mortality and Cardiovascular Morbidity After Noncardiac Surgery. Multicenter Study of Perioperative Ischemia Research Group,"
N Engl J Med
, 1996, 335(23):1713-20.
Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings,"
Chest
, 2003, 123(3):897-922.
International Brand Names
Ablok® (BR); Adco-Atenolol® (ZA); Alonet® (SG); Amolin® (IE); Anetol® (BD); Angipress® (BR); Anselol® (AU, NZ); Apo-Atenol® (CA, PL, SG, TR); Apo-Atenolol® (CZ, NZ, ZA); Arcablock® (AT); Ate AbZ® (DE); Atebeta® (DE); Ateblocor® (CZ); Atecard® (IN); Atecor® (IE); Atehexal® (AT, AU, CZ, DE, LU, PL); Atel® (AR); Ate Lich® (DE); Atenblock® (FI); Atendol® (DE, PL); Atenet® (DK); Ate-Nife® (IE); Ateni® (IE); Atenil® (CH, RO); Aten® (IN); Atenix® (GB); Atenobal® (BR); Ateno-basan® (CH); Atenobene® (AT, CZ, HU); Atenoblock® (AR); Atenoblok® (ZA); Atenocor® (RO); Atenodan® (DK); Atenogamma® (DE); Atenogen® (IE); Ateno-ISIS® (DE); Atenolan® (AT, RU); Atenol® (BR, FI, IT, TH); Atenolol 1A Pharma® (AT, DE); Atenolol acis® (DE); Atenolol AL® (DE, HU); Atenolol Alpharma ApS® (SG); Atenolol Alter® (ES, PT); Atenolol Atid® (DE); Atenolol-BC (AU); Atenolol Beacons® (SG); Atenolol Bexal® (ES); Atenolol® (BG, BR, CL, CZ, GB, NO, PL, RO, RU, SI, YU); Atenolol-B® (HU); Atenolol Biochemie® (DK, FI, SE); Atenolol Biotenk® (AR); Atenolol Cinfa® (ES); Atenolol-Cophar® (CH); Atenolol ct® (CZ); Atenolol Edigen® (ES); Atenolol EG® (BE); Atenolol Fabra® (AR); Atenolol Fada® (AR); Atenolol Fecofar® (AR); Atenolol Gador® (AR); Atenolol Geminis® (ES); Atenolol Genericon® (AT, CH); Atenolol Gen Med® (AR); Atenolol HelvePharm® (CH); Atenolol Heumann® (DE); Atenolol Hexan® (IT); Atenolol L.CH.® (CL); Atenolol Lindo® (DE); Atenolol-Mepha® (CH); Atenolol Microsules® (AR); Atenolol MK® (CO); Atenolol Mundogen® (ES); Atenolol NM® (DK); Atenolol NM Pharma® (SE); Atenolol Nordic® (SE); Atenolol Normon® (ES); Atenololo DOC® (IT); Atenololo EG® (IT); Atenololo Hexan® (IT); Atenololo Merck® (IT); Atenololo Pliva® (IT); Atenololo-ratiopharm® (IT); Atenololo RK® (IT); Atenololo Teva® (IT); Atenololo Union Health® (IT); Atenolol PB® (DE); Atenolol Pharmavit® (HU); Atenolol Pliva® (HR, SI); Atenolol Quesada® (AR); Atenolol Ratiopharm® (AT); Atenolol-ratiopharm® (BE, DE); Atenolol Ratiopharm® (ES); Atenolol-ratiopharm® (RU); Atenolol Sandoz® (DE, FI); Atenolol Stada® (AT, DE); Atenolol Vannier® (AR); Atenolol von ct® (DE, LU); Atenolol-Wolff® (DE); Atenomel® (HU, IE); Atenor® (DK); Atenoric® (BR); Atenosan® (RO, RU); Atenotop® (BE); Atenotyrol (AT); Atenova® (RO); Atephar® (BE); Atermin® (IT); Athenol® (BE); Atin® (BD); Azectol® (RO); Beta-Adalat® (IE); Betablok® (ID); Beta-bloquin® (DO); Betacard® (RU); Betanol® (BD); Betasec® (BD); Betasyn® (AT); Betatop® (FR); Blocotenol® (DE); Blokium® (BE, EG, ES, HU, MX, PT); Cardaxen® (CH); Cardipro® (BD); Carsec® (BD); Catenol® (CZ); Chem mart Atenolol® (AU); Coratol® (TH); Corotenol® (CY, EG, JO, KW, LB); Cuxanorm® (DE); DBL Atenolol® (AU); Docateno® (BE); duratenol® (DE); Ephitensin® (RO); Evitocor® (DE); Fabotenol® (AR); Falitonsin® (DE); Farnormin® (ID); Felobits® (AR); Gen-Atenolol (CA); GenRX Atenolol® (AU); Global Atenolol® (NZ); Grifotenol® (CL); Healthsense Atenolol® (AU); Hexa-Blok® (ZA); Hiblok® (ID); Huma-Atenol® (HU); Hypernol® (SG); Hypoten® (EG, KW, LB, RO, SY); Internolol® (ID); Ivax-Atenolol® (ZA); Janol® (BD); Jenatenol® (DE); Juvental® (DE); Labotensil® (CL); Lorten® (BD); Lo-Ten® (NZ); Merck-Atenolol® (BE); Myocord® (AR); Neatenol® (ES); Neotenol® (BR); New Formula Amolin® (IE); Nif-ten® (IE); Nolol® (DO, TH); Normalol® (IL); Normaten® (BD, SG); Normiten® (IL); Normocard® (PL); Norpress® (BD); Nortan® (TR); Noten® (AU, SG); Novo-Atenol (CA, RO); Nu-Atenol (CA); Oraday® (TH); Ormidol® (HR, RU, SI); Panapres® (YU); Plenacor® (AR, BR); PMS-Atenolol (CA); Precinol® (BD); Prenolol® (SG, TH); Prenormine® (AR); Primatenol® (CH); Prinorm® (HU, RO, YU); Rhoxal-atenolol (CA); Rolab-Atenolol® (ZA); Seles Beta® (IT); Selobloc® (CH); Servitenol® (CH); Stadmed Beta® (IN); Synarome® (RO); Tanser® (ES); Telvodin® (AR); Ten-Bloka® (ZA); Tenoblock® (FI); Tenocard® (BD); Tenocor® (TH); Tenolin (CA); Tenoloc® (BD); Tenolol® (IN, LU, RU, SG, TH); Tenol-T® (BD); Tenol® (TH); Tenomax® (IT); Tenoprin® (FI); Tenoren® (BD); Tenoret® (CY, KW, LB, MT); Tenoretic® (AT, CY, KW, LB, MT); Tenormin® (AT, AU, BE, BG, CA, CH, CL, CY, CZ, DE, DK, EC, ES, GB, HK, HR, ID, IE, IN, IT, KW, LB, LU, MT, MX, NL, NO, NZ, PL, PT, RO, RU, SE, SG, SI, TH, YU, ZA); Ténormine® (FR); Tensig® (AU); Tensinorm® (ID); Tensinor® (TR); Tessifol® (PT); Trantalol® (IE); Tredol® (BG, KW, LB, MA, MY, SY); Unibloc® (NL); Uniloc® (DK, NO, RU, SE); Vascoten® (HK, JO, RO, RU, SG, TH); Velorin® (CY, SI, TH); Venapulse® (ZA); Vericordin® (AR); Zumablok® (ID)
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