Use - Unlabeled/Investigational
Acute ethanol withdrawal, supraventricular and ventricular arrhythmias, and migraine headache prophylaxis D Atenolol crosses the placenta; persistent beta-blockade, bradycardia, IUGR; IUGR probably related to maternal hypertension. Enters breast milk; use caution in breast-feeding women. Clinical effects on the infant: Symptoms have been reported of beta-blockade including cyanosis, hypothermia, bradycardia. Enters breast milk/use caution 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 Administer cautiously in compensated heart failure and monitor for a worsening of the condition (efficacy of atenolol in heart failure has not been established). Avoid abrupt discontinuation in patients with a history of CAD; slowly wean while monitoring for signs and symptoms of 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.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
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.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).
Protect from light Stable in D5W, NSY-site administration: Compatible: Meperidine, meropenem, morphine. Incompatible: Amphotericin B cholesteryl sulfate complex
Competitively blocks response to beta-adrenergic stimulation, selectively blocks beta1-receptors with little or no effect on beta2-receptors except at high dosesOnset 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)
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: 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.
Administer I.V. at 1 mg/minute; intravenous administration requires a cardiac monitor and blood pressure monitor Monitor blood pressure, apical and radial pulses, fluid I & O, daily weight, respirations, and circulation in extremities before and during therapy glucose;Modify dosage in patients with renal insufficiency; administer by slow I.V. injection at a rate not to exceed 1 mg/minute; the injection can be administered undiluted or diluted with a compatible I.V. solution
Monitor blood pressure, heart rate, fluid I & O, daily weight, respiratory rate
Anesthesia and Critical Care Concerns/Other Considerations
May potentiate hypoglycemia in a diabetic patient; may mask signs and symptoms of hypoglycemiaMyocardial 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.
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
Noncardioselective beta-blockers (ie, propranolol, nadolol) enhance the pressor response to epinephrine, resulting in hypertension and bradycardia. This has not been reported for atenolol, a cardioselective beta-blocker. Therefore, local anesthetic with vasoconstrictor can be safely used in patients medicated with 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 precautionsMental Health: Effects on Mental Status
May cause fatigue, insomnia, and confusion which can clinically look like depressionMental Health: Effects on Psychiatric Treatment
Concurrent use with other psychotropics may produce an additive hypotensive response (especially low potency antipsychotics and TCAs)Injection, solution: 0.5 mg/mL (10 mL)
Tablet: 25 mg, 50 mg, 100 mg
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.
"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals into Human Milk,"Pediatrics, 2001, 108(3):776-89.
Braunwald E, Antman EM, Beasley JW, et al, "ACC/AHA Guidelines for the Management of Patients With Unstable Angina and Non-ST-Segment Elevation Myocardial Infarction. 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, 2000, 36(3):970-1062.
"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, Chatterjee K, Daley J, et al, "ACC/AHA/ACP-ASIM Guidelines for the Management of Patients With Chronic Stable Angina: a Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines,"J Am Coll Cardiol, 1999, 33(7):2092-197.
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.
Ryan TJ, Anderson JL, Antman EM, et al, "ACC/AHA Guidelines for the Management of Patients With Acute Myocardial Infarction. A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Management of Acute Myocardial Infarction),"J Am Coll Cardiol, 1996, 28(5):1328-428.
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