atenolol (Tenormin)
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Introduction
Tradename: Tenormin. A selective beta-1 antagonist.
Indications
- management of hypertension & angina
- control of ventricular rate in atrial fibrillation or atrial flutter
- does not reduce all-cause mortality, cardiovascular mortality or myocardial infarction[5][8]
- less effective than losartin in preventing stroke[7]
- myocardial infarction[9]
- chronic heart failure
- mitral valve prolapse
- migraine prophylaxis
- essential tremor
- thyrotoxicosis
- pheochromocytoma[7]
- long QT syndrome[7] (generally non-selective beta-blocker used)
Contraindications
Dosage
Tabs: 25, 50, 100 mg.
Caution:
- taper, do not discontinue abruptly: may result in rebound hypertension or angina
Dosage adjustment in renal failure
Table
| glomerular filtration rate | dose |
|---|---|
| > 35 mL/min | 50 mg QD |
| 15-35 mL/min | 50 mg QD |
| < 15 mL/min | 50 mg QID |
Pharmacokinetics
- food impairs absorption[4]
- protein binding 3-15%[6]
- does NOT cross blood brain barrier[6]
- 1/2 life 6-9 hours, increased with renal insufficiency 16-27 hours with creatinine clearance of 15-35 mL/min[6]
elimination via kidney
protein binding = <5 %
elimination by hemodialysis = +
Adverse effects
- most common (1-10%)
- uncommon (<1%)
- cold extremities, dyspnea (dose-dependent), wheezing & exacerbation of obstructive airway disease
- 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 adverse effects of beta-adrenergic receptor antagonists
- drug adverse effects of beta-1 adrenergic receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
- co-administration with other anti-hypertensives my cause hypotension
- co-administration with negative inotropic agents may cause diminished cardiac output
- hydroxide-containing antacids may decrease atenolol bioavailability
- phenothiazines may increase atenolol concentrations
- drug interaction(s) of antiarrhythmic agents in combination with diuretics
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with thyroid hormone
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfinpyrazone
- drug interaction(s) of beta-adrenergic receptor antagonists with salicylate
- drug interaction(s) of beta-adrenergic receptor antagonists with rifampin
- drug interaction(s) of beta-adrenergic receptor antagonists with ampicillin
- drug interaction(s) of beta-adrenergic receptor antagonists with colestipol
- drug interaction(s) of beta-adrenergic receptor antagonists with cholestyramine
- drug interaction(s) of beta-adrenergic receptor antagonists with barbiturates
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium salts
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum carbonate
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum hydroxide
- drug interaction(s) of beta-adrenergic receptor antagonists with prazosin
- drug interaction(s) of beta-adrenergic receptor antagonists with lidocaine
- drug interaction(s) of beta-adrenergic receptor antagonists with ergot alkaloids
- drug interaction(s) of beta-adrenergic receptor antagonists with clonidine
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of beta-adrenergic receptor antagonists with quinidine
- drug interaction(s) of beta-adrenergic receptor antagonists with propafenone
- drug interaction(s) of beta-adrenergic receptor antagonists with phenothiazines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of beta-adrenergic receptor antagonists with loop diuretics
- drug interaction(s) of beta-adrenergic receptor antagonists with hydralazine
- drug interaction(s) of beta-adrenergic receptor antagonists with histamine H2 receptor antagonists
- drug interaction(s) of beta-adrenergic receptor antagonists with haloperidol
- drug interaction(s) of beta-adrenergic receptor antagonists with flecainide
- drug interaction(s) of beta-adrenergic receptor antagonists with oral contraceptives
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of spironolactone with beta blockers
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs & antihypertensives
Laboratory
- methods: TLC, GC, HPLC
- 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
- selectively inhibits beta-1 adrenergic receptors at low doses
- negative inotropic effects
- negative chronotropic effects
- at high doses (> 100 mg/day), competitively inhibits beta-1 & beta-2 adrenergic receptors
- suppresses renin activity: may lead to minimal reduction in renal blood flow & glomerular filtration
- not lipid soluble; does not cross blood brain barrier.
More general terms
Additional terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1990, pg 230
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 4.0 4.1 Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 470
- ↑ 5.0 5.1 Prescriber's Letter 11(12): 2004 Atenolol and Its Use in Hypertension Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=201215&pb=PRL (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: https://www.ncbi.nlm.nih.gov/pubmed/15530629 - ↑ 6.0 6.1 6.2 6.3 Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 7.0 7.1 7.2 7.3 Prescriber's Letter 12(4): 2005
- ↑ 8.0 8.1 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: https://www.ncbi.nlm.nih.gov/pubmed/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: https://www.ncbi.nlm.nih.gov/pubmed/16153995 - ↑ 9.0 9.1 Deprecated Reference
- ↑ Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019
- ↑ Department of Veterans Affairs, VA National Formulary