Atenolol

Atenolol
Systematic (IUPAC) name
(RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide
Clinical data
Trade names Tenormin
AHFS/Drugs.com monograph
MedlinePlus a684031
License data
Pregnancy
category
  • AU: C
  • US: D (Evidence of risk)
Routes of
administration		 Oral or IV
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 40-50%
Protein binding 6-16%
Metabolism Hepatic <10%
Biological half-life 6-7 hours
Excretion Renal
Lactic (In lactiferous females)
Identifiers
CAS Number 29122-68-7 YesY
ATC code C07AB03 (WHO)
PubChem CID 2249
IUPHAR/BPS 548
DrugBank DB00335 YesY
ChemSpider 2162 YesY
UNII 50VV3VW0TI YesY
KEGG D00235 YesY
ChEBI CHEBI:2904 YesY
ChEMBL CHEMBL24 YesY
Chemical data
Formula C14H22N2O3
Molar mass 266.336 g/mol
Chirality Racemic mixture
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Atenolol is a selective β1 receptor antagonist, a drug belonging to the group of beta blockers (sometimes written β-blockers), a class of drugs used primarily in cardiovascular diseases. Introduced in 1976, atenolol was developed as a replacement for propranolol in the treatment of hypertension. It works by slowing down the heart and reducing its workload. Unlike propranolol, atenolol does not readily pass through the blood–brain barrier, thus decreasing the incidence of central nervous system side effects.[1]

Atenolol is one of the most widely used β-blockers in the United Kingdom and was once the first-line treatment for hypertension. However, recent studies indicate that atenolol may not reduce morbidity or mortality when used to treat hypertension, and may even increase mortality in some subgroups.[2] In addition, 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 newer drugs, particularly in the elderly.

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.[3]

Off-label uses of Atenolol, as with other cardioselective β-blockers, include symptomatic treatment of psychological issues such as anxiety. β-blockers are effective for some in treating the somatic (physical) effects of anxiety. In these instances, dosing is used as needed instead of regular daily dosing.

Due to its hydrophilic (water-attracting) properties, the drug is less suitable in migraine prophylaxis compared to propranolol, because, for this indication, atenolol would have to reach the brain in high concentrations, which is not the case, because atenolol does not pass through the blood–brain barrier.[1]

Side effects

See also: Beta blocker

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.[4]

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.[5] In addition, atenolol has been found to lack mortality benefits[6][7] and even to increase mortality in older adults.[2]

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.[8][9]

References

  1. 1 2 Agon P, Goethals P, Van Haver D, Kaufman JM (August 1991). "Permeability of the blood–brain barrier for atenolol studied by positron emission tomography". J. Pharm. Pharmacol. 43 (8): 597–600. doi:10.1111/j.2042-7158.1991.tb03545.x. PMID 1681079.
  2. 1 2 Geriatr Gerontol Int. 2014 Jan;14(1):153-8. doi: 10.1111/ggi.12073. Epub 2013 Apr 15. Atenolol use is associated with long-term mortality in community-dwelling older adults with hypertension. Testa G1, Cacciatore F, Della-Morte D, Mazzella F, Mastrobuoni C, Galizia G, Gargiulo G, Rengo F, Bonaduce D, Abete P. http://www.ncbi.nlm.nih.gov/pubmed/23581644
  3. ↑ "Atenolol". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
  4. ↑ Sheetal Ladva (2006-06-28). "NICE and BHS launch updated hypertension guideline". National Institute for Health and Clinical Excellence.
  5. ↑ Carlberg B, Samuelsson O, Lindholm LH (2004). "Atenolol in hypertension: is it a wise choice?". Lancet 364 (9446): 1684–9. doi:10.1016/S0140-6736(04)17355-8. PMID 15530629.
  6. ↑ Beta-Blockers in the Management of Hypertension and/or Chronic Kidney Disease Hirofumi Tomiyama* and Akira Yamashina Int J Hypertens. 2014; 2014: 919256. Published online 2014 Jan 30. doi: 10.1155/2014/919256 PMCID: PMC3941231 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3941231/
  7. ↑ Open Heart. 2015; 2(1): e000230. Published online 2015 Mar 21. doi: 10.1136/openhrt-2014-000230 β-Blockers in hypertension, diabetes, heart failure and acute myocardial infarction: a review of the literature James J DiNicolantonio,1 Hassan Fares,2 Asfandyar K Niazi,3 Saurav Chatterjee,4 Fabrizio D'Ascenzo,5 Enrico Cerrato,5 Giuseppe Biondi-Zoccai,6 Carl J Lavie,2,7 David S Bell,8 and James H O'Keefe9 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4371808/
  8. ↑ 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.
  9. ↑ R. Baselt (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, CA: Biomedical Publications. pp. 116–117.

External links

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