Atenolol
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| Clinical data | |
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| Trade names | Tenormin, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a684031 |
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| Routes of administration | By mouth, IV |
| Drug class | Selective β1 receptor antagonist |
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| Pharmacokinetic data | |
| Bioavailability | 40–50% |
| Protein binding | 6–16% |
| Metabolism | Liver <10% |
| Elimination half-life | 6–7 hours |
| Excretion | Kidney |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.044.941 |
| Chemical and physical data | |
| Formula | C14H22N2O3 |
| Molar mass | 266.336 g/mol g·mol−1 |
| 3D model (JSmol) | |
| Chirality | Racemic mixture |
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Atenolol is a beta blocker medication primarily used to treat high blood pressure and heart-associated chest pain.[2] Other uses include the prevention of migraines and treatment of certain irregular heart beats.[2][3] It is taken by mouth or by injection into a vein.[2][3] It can also be used with other blood pressure medications.[3]
Common side effects include feeling tired, heart failure, dizziness, depression, and shortness of breath.[2] Other serious side effects include bronchospasm.[2] Use is not recommended during pregnancy.[2] Other medications are preferred when breastfeeding a young baby.[4] It works by blocking β1-adrenergic receptors in the heart, thus decreasing the heart rate and workload.[2]
Atenolol was patented in 1969 and approved for medical use in 1975.[5] It is available as a generic medication.[2] In the United States, the wholesale cost per month is less than 15 USD as of 2018.[6] In the United Kingdom, a month of treatment costs the NHS less than 5 pounds.[3] In 2016, it was the 20th most prescribed medication in the United States, with more than 26 million prescriptions.[7]
Medical uses
Atenolol is used for a number of conditions including hypertension, angina, long QT syndrome, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.[8]
Atenolol is one of the most widely used β-blockers in the United Kingdom and was once the first-line treatment for hypertension.[citation needed] The role for β-blockers in general in hypertension was downgraded in June 2006 in the United Kingdom, and later in the United States, as they are less appropriate than calcium channel blockers, thiazide diuretics, angiotension converting enzyme (ACE) inhibitors, and angiotensin receptor blockers, particularly in the elderly.[citation needed]
Off-label uses of atenolol, as with other cardioselective β-blockers, include symptomatic treatment of anxiety. β-blockers are effective for some of the physical effects of anxiety. In these instances, dosing is used as needed instead of regular daily dosing.
Side effects
Atenolol was the main β-blocker identified as carrying a higher risk of provoking type 2 diabetes, leading to its downgrading in the United Kingdom in June 2006 to fourth-line agent in the management of hypertension.[9]
Antihypertensive therapy with atenolol provides weaker protective action against cardiovascular complications (e.g. myocardial infarction and stroke) compared to other antihypertensive drugs. In some cases, diuretics are superior.[10] In addition, atenolol has been found to lack mortality benefits[11][12] and even to increase mortality in older adults.[13]
Overdose
Symptoms of overdose are due to excessive pharmacodynamic actions on β1 and also β2-receptors. These include bradycardia (slow heartbeat), severe hypotension with shock, acute heart failure, hypoglycemia and bronchospastic reactions. Treatment is largely symptomatic. Hospitalization and intensive monitoring is indicated. Activated charcoal is useful to absorb the drug. Atropine will counteract bradycardia, glucagon helps with hypoglycemia, dobutamine can be given against hypotension and the inhalation of a β2-mimetic as hexoprenalin or salbutamol will terminate bronchospasms. Blood or plasma atenolol concentrations may be measured to confirm a diagnosis of poisoning in hospitalized patients or to assist in a medicolegal death investigation. Plasma levels are usually less than 3 mg/L during therapeutic administration, but can range from 3–30 mg/L in overdose victims.[14][15]
Society and culture
Atenolol has been given as an example of how slow healthcare providers are to change their prescribing practices in the face of medical evidence that indicates that a drug is ineffective.[16] In 2012, 33.8 million prescriptions were written to American patients for this drug.[16] In 2014, it was in the top (most common) 1% of drugs prescribed to Medicare patients.[16] Although the number of prescriptions has been declining steadily since the evidence against its efficacy was published, it has been estimated that it would take 20 years for doctors to stop prescribing it for hypertension.[16]
References
- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
- ^ a b c d e f g h "Atenolol Monograph for Professionals". Drugs.com. AHFS. Retrieved 23 December 2018.
- ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 151–153. ISBN 9780857113382.
- ^ "Atenolol use while Breastfeeding". Drugs.com. Retrieved 23 December 2018.
- ^ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.
- ^ "NADAC as of 2018-12-19". Centers for Medicare and Medicaid Services. Retrieved 22 December 2018.
- ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
- ^ "Atenolol". The American Society of Health-System Pharmacists. Retrieved 8 May 2018.
- ^ Sheetal Ladva (28 June 2006). "NICE and BHS launch updated hypertension guideline". National Institute for Health and Clinical Excellence. Archived from the original on 11 May 2008. Retrieved 19 August 2012.
- ^ Carlberg B, Samuelsson O, Lindholm LH (2004). "Atenolol in hypertension: is it a wise choice?". The Lancet. 364 (9446): 1684–9. doi:10.1016/S0140-6736(04)17355-8. PMID 15530629.
- ^ Tomiyama H, Yamashina A (2014). "Beta-Blockers in the Management of Hypertension and/or Chronic Kidney Disease". International Journal of Hypertension. 2014: 919256. doi:10.1155/2014/919256. PMC 3941231. PMID 24672712.
{{cite journal}}: CS1 maint: unflagged free DOI (link) - ^ DiNicolantonio JJ, Fares H, Niazi AK, Chatterjee S, D'Ascenzo F, Cerrato E, Biondi-Zoccai G, Lavie CJ, Bell DS, O'Keefe JH (2015). "β-Blockers in hypertension, diabetes, heart failure and acute myocardial infarction: a review of the literature". Open Heart. 2: e000230. doi:10.1136/openhrt-2014-000230. PMC 4371808. PMID 25821584.
- ^ Testa G, Cacciatore F, Della-Morte D, Mazzella F, Mastrobuoni C, Galizia G, Gargiulo G, Rengo F, Bonaduce D, Abete P (2014). "Atenolol use is associated with long-term mortality in community-dwelling older adults with hypertension". Geriatrics & Gerontology International. 14: 153–8. doi:10.1111/ggi.12073. PMID 23581644.
- ^ DeLima LG, Kharasch ED, Butler S (1995). "Successful pharmacologic treatment of massive atenolol overdose: sequential hemodynamics and plasma atenolol concentrations". Anesthesiology. 83 (1): 204–207. doi:10.1097/00000542-199507000-00025. PMID 7605000.
- ^ R. Baselt (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, Calif.: Biomedical Publications. pp. 116–117.
- ^ a b c d Epstein, David; ProPublica (22 July 2017). "When Evidence Says No, But Doctors Say Yes". The Atlantic. Retrieved 8 May 2018.
