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atenolol (Tenormin)

Tradename: Tenormin. A selective beta-1 antagonist. Indications: 1) management of hypertension & angina 2) control of ventricular rate in atrial fibrillation or atrial flutter 3) does not reduce all-cause mortality, cardiovascular mortality or myocardial infarction [5,8] 4) less effective than losartin in preventing stroke [7] 5) myocardial infarction [9] 6) chronic heart failure - left ventricular diastolic dysfunction 7) mitral valve prolapse 8) migraine prophylaxis 9) essential tremor 10) thyrotoxicosis 11) pheochromocytoma [7] 12) long QT syndrome [7] (generally non-selective beta-blocker used) Contraindications: - use with caution in patients with COPD or asthma Dosage: 1) acute MI: 5 mg IV over 5 min, repeat in 10 min. 2) HTN: start 50 mg PO QD, max 200 mg/day. Tabs: 25, 50, 100 mg. Caution: - taper, do not discontinue abruptly: may result in rebound hypertension or angina Pharmacokinetics: 1) food impairs absorption [4] 2) protein binding 3-15% [6] 3) does NOT cross blood brain barrier [6] 4) 1/2 life 6-9 hours, increased with renal insufficiency 16-27 hours with creatinine clearance of 15-35 mL/min [6] Dosage adjustment in renal failure: glomerular filtration rate dose > 35 mL/min 50 mg QD 15-35 mL/min 50 mg QD < 15 mL/min 50 mg QID Adverse effects: 1) most common (1-10%) - bradycardia, hypotension, chest pain, edema, heart failure, 2nd or 3rd degree AV block, Raynaud's phenomenon, dizziness, fatigue, insomnia, lethargy, confusion, mental impairment, depression, headache, nightmares, constipation, diarrhea, nausea, impotence 2) uncommon (<1%) - cold extremities, dyspnea (dose-dependent), wheezing & exacerbation of obstructive airway disease 3) other - may affect fetal hemodynamics & fetal growth, best NOT used in women at risk of pregnancy - may elevate serum lipid levels - xerosis resulting in pruritus Drug interactions: 1) co-administration with other anti-hypertensives my cause hypotension 2) co-administration with negative inotropic agents may cause diminished cardiac output 3) hydroxide-containing antacids may decrease atenolol bioavailability 4) phenothiazines may increase atenolol concentrations Laboratory: 1) methods: TLC, GC, HPLC 2) atenolol in specimen - atenolol in hair - atenolol in blood - atenolol in serum/plasma (EDTA, heparin) - serum levels do NOT correlate with therapeutic effect - atenolol in urine Mechanism of action: 1) selectively inhibits beta-1 adrenergic receptors at low doses a) negative inotropic effects b) negative chronotropic effects 2) at high doses (> 100 mg/day), competitively inhibits beta-1 & beta-2 adrenergic receptors 4) suppresses renin activity: may lead to minimal reduction in renal blood flow & glomerular filtration 3) not lipid soluble; does not cross blood brain barrier.

Interactions

drug interactions drug adverse effects (more general classes)

Related

ASCOT BPLA trial (atenolol vs amlodipine)

General

antiarrhythmic agent, Group II beta-1 adrenergic receptor antagonist (beta-1 blocker) propanolamine

Properties

MISC-INFO: elimination route KIDNEY 1/2life 6.3 +/- 1.8 HOURS therapeutic-range 200-500 NG/ML protein-binding <5% elimination by hemodialysis + pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1990, pg 230
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  4. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 470
  5. Prescriber's Letter 11(12): 2004 Atenolol and Its Use in Hypertension Detail-Document#: 201215 (subscription needed) http://www.prescribersletter.com - Journal Watch 24(24):182, 2004 Carlberg B, Samuelsson O, Lindholm LH. Atenolol in hypertension: is it a wise choice? Lancet. 2004 Nov 6;364(9446):1684-9. PMID: 15530629
  6. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  7. Prescriber's Letter 12(4): 2005
  8. Dahlof B et al. for the ASCOT Investigators. Prevention of cardiovascular events with an antihypertensive regimen of amlodipine adding perindopril as required versus atenolol adding bendroflumethiazide as required, in the Anglo-Scandinavian Cardiac Outcomes Trial-Blood Pressure Lowering Arm (ASCOT-BPLA): A multicentre randomised controlled trial. PMID: 16154016 Lancet 2005 Sep 10; 366:895-906. - Staessen JA and Birkenhager WH. Evidence that new antihypertensives are superior to older drugs. Lancet 2005 Sep 10; 366:869-71. PMID: 16153995
  9. Deprecated Reference
  10. Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019
  11. Department of Veterans Affairs, VA National Formulary

Component-of

atenolol/chlorthalidone (Tenoretic) atenolol/metoprolol