Atenolol

Atenolol is a beta blocker medication primarily used to treat high blood pressure and heart-associated chest pain.[1] Atenolol, however, does not seem to improve mortality in those with high blood pressure.[2][3] Other uses include the prevention of migraines and treatment of certain irregular heart beats.[1][4] It is taken by mouth or by injection into a vein.[1][4] It can also be used with other blood pressure medications.[4]

Atenolol
Clinical data
Trade namesTenormin, others
AHFS/Drugs.comMonograph
MedlinePlusa684031
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth, Intravenous (IV)
Drug classSelective β1 receptor antagonist
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability40–50%
Protein binding6–16%
MetabolismLiver <10%
Elimination half-life6–7 hours
ExcretionKidney
Identifiers
IUPAC name
  • (RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.044.941
Chemical and physical data
FormulaC14H22N2O3
Molar mass266.341 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O=C(N)Cc1ccc(cc1)OCC(O)CNC(C)C
  • InChI=1S/C14H22N2O3/c1-10(2)16-8-12(17)9-19-13-5-3-11(4-6-13)7-14(15)18/h3-6,10,12,16-17H,7-9H2,1-2H3,(H2,15,18) Y
  • Key:METKIMKYRPQLGS-UHFFFAOYSA-N Y
  (verify)

Common side effects include feeling tired, heart failure, dizziness, depression, and shortness of breath.[1] Other serious side effects include bronchospasm.[1] Use is not recommended during pregnancy[1] and alternative drugs are preferred when breastfeeding.[5] It works by blocking β1-adrenergic receptors in the heart, thus decreasing the heart rate and workload.[1]

Atenolol was patented in 1969 and approved for medical use in 1975.[6] It is on the World Health Organization's List of Essential Medicines.[7] It is available as a generic medication.[1] In 2020, it was the 53rd most commonly prescribed medication in the United States, with more than 12 million prescriptions.[8][9]

Medical uses

Atenolol is used for a number of conditions including hyperthyroidism,[10] hypertension, angina, long QT syndrome, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.[11]

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 other agents such as ACE inhibitors, calcium channel blockers, thiazide diuretics and angiotensin receptor blockers, particularly in the elderly.[12][13][14]

Side effects
See also: Beta blocker

Hypertension treated with a β-blocker such as atenolol, alone or in conjunction with a thiazide diuretic, is associated with a higher incidence of new onset type 2 diabetes mellitus compared to those treated with an ACE inhibitor or angiotensin receptor blocker. [15][16]

β-blockers, of which atenolol is mainly studied, provides weaker protection against stroke and mortality in patients over 60 years old compared to other antihypertensive medications.[17][18][19][12] Diuretics may be associated with better cardiovascular and cerebrovascular outcomes than β-blockers in the elderly.[20]

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.[21][22]

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 not as effective as others in treating some conditions.[23] In 2012, 33.8 million prescriptions were written to American patients for this drug.[23] In 2014, it was in the top (most common) 1% of drugs prescribed to Medicare patients.[23] Although the number of prescriptions has been declining steadily since limited evidence articles contesting its efficacy was published, it has been estimated that it would take 20 years for doctors to stop prescribing it for hypertension.[23] Despite its diminished efficacy when compared to newer antihypertensive drugs, atenolol and other beta blockers are still a relevant clinical choice for treating some conditions, since beta blockers are a diverse group of medicines with different properties that still requires further research.[12] As consequence, reasons for the popularity of beta blockers cannot be fully attributed to a slow healthcare system – patient compliance factor, such as treatment cost and duration, also affect adherence and popularity of therapy.[24]

References
  1. "Atenolol Monograph for Professionals". Drugs.com. AHFS. Archived from the original on 18 April 2019. Retrieved 23 December 2018.
  2. 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.
  3. DiNicolantonio JJ, Fares H, Niazi AK, Chatterjee S, D'Ascenzo F, Cerrato E, et al. (2015). "β-Blockers in hypertension, diabetes, heart failure and acute myocardial infarction: a review of the literature". Open Heart. 2 (1): e000230. doi:10.1136/openhrt-2014-000230. PMC 4371808. PMID 25821584.
  4. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 151–153. ISBN 9780857113382.
  5. "Atenolol use while Breastfeeding". Drugs.com. Archived from the original on 23 December 2018. Retrieved 23 December 2018.
  6. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.
  7. World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  8. "The Top 300 of 2020". ClinCalc. Archived from the original on 18 March 2020. Retrieved 7 October 2022.
  9. "Atenolol - Drug Usage Statistics". ClinCalc. Archived from the original on 11 April 2020. Retrieved 7 October 2022.
  10. Rehman, B; Sanchez, DP; Shah, S (2021), "article-655", Atenolol, Treasure Island (FL): StatPearls Publishing, PMID 30969666, archived from the original on 10 October 2022, retrieved 5 September 2021
  11. "Atenolol". The American Society of Health-System Pharmacists. Archived from the original on 18 April 2019. Retrieved 8 May 2018.
  12. Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH (January 2017). "Beta-blockers for hypertension". The Cochrane Database of Systematic Reviews. 1: CD002003. doi:10.1002/14651858.CD002003.pub5. PMC 5369873. PMID 28107561. Further research should be of high quality and should explore whether there are differences between different subtypes of beta-blockers or whether beta-blockers have differential effects on younger and older people [...] Beta-blockers were not as good at preventing the number of deaths, strokes, and heart attacks as other classes of medicines such as diuretics, calcium-channel blockers, and renin-angiotensin system inhibitors. Most of these findings come from one type of beta-blocker called atenolol. However, beta-blockers are a diverse group of medicines with different properties, and we need more well-conducted research in this area." (p. 2-3)
  13. 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.
  14. Cruickshank JM (August 2007). "Are we misunderstanding beta-blockers". International Journal of Cardiology. 120 (1): 10–27. doi:10.1016/j.ijcard.2007.01.069. PMID 17433471.
  15. Lindholm LH, Ibsen H, Borch-Johnsen K, Olsen MH, Wachtell K, Dahlöf B, et al. (September 2002). "Risk of new-onset diabetes in the Losartan Intervention For Endpoint reduction in hypertension study". Journal of Hypertension. 20 (9): 1879–86. doi:10.1097/00004872-200209000-00035. PMID 12195132. S2CID 23613019.
  16. Elliott WJ, Meyer PM (January 2007). "Incident diabetes in clinical trials of antihypertensive drugs: a network meta-analysis". Lancet. 369 (9557): 201–7. doi:10.1016/s0140-6736(07)60108-1. PMID 17240286. S2CID 37044384.
  17. Lindholm LH, Carlberg B, Samuelsson O (October 2005). "Should β blockers remain first choice in the treatment of primary hypertension? A meta-analysis". The Lancet. 366 (9496): 1545–1553. doi:10.1016/S0140-6736(05)67573-3. PMID 16257341. S2CID 34364430.
  18. Khan N, McAlister FA (June 2006). "Re-examining the efficacy of beta-blockers for the treatment of hypertension: a meta-analysis". CMAJ. 174 (12): 1737–42. doi:10.1503/cmaj.060110. PMC 1471831. PMID 16754904.
  19. Kuyper LM, Khan NA (May 2014). "Atenolol vs nonatenolol β-blockers for the treatment of hypertension: a meta-analysis". The Canadian Journal of Cardiology. 30 (5 Suppl): S47-53. doi:10.1016/j.cjca.2014.01.006. PMID 24750981.
  20. Messerli FH, Grossman E, Goldbourt U (June 1998). "Are beta-blockers efficacious as first-line therapy for hypertension in the elderly? A systematic review". JAMA. 279 (23): 1903–7. doi:10.1001/jama.279.23.1903. PMID 9634263.
  21. DeLima LG, Kharasch ED, Butler S (July 1995). "Successful pharmacologic treatment of massive atenolol overdose: sequential hemodynamics and plasma atenolol concentrations". Anesthesiology. 83 (1): 204–7. doi:10.1097/00000542-199507000-00025. PMID 7605000.
  22. Baselt R (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, Calif.: Biomedical Publications. pp. 116–117.
  23. Epstein D (22 July 2017). "When Evidence Says No, But Doctors Say Yes". The Atlantic. Archived from the original on 9 May 2018. Retrieved 8 May 2018.
  24. Choi HY, Oh IJ, Lee JA, Lim J, Kim YS, Jeon TH, et al. (November 2018). "Factors Affecting Adherence to Antihypertensive Medication". Korean Journal of Family Medicine. 39 (6): 325–332. doi:10.4082/kjfm.17.0041. PMC 6250947. PMID 30384549.
  • "Atenolol". Drug Information Portal. U.S. National Library of Medicine.
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