Atenolol

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Atenolol
Systematic (IUPAC) name
(RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide
Clinical data
Trade namesTenormin
AHFS/Drugs.commonograph
MedlinePlusa684031
Licence dataUS FDA:link
Pregnancy cat.C (AU) D (US)
Legal status Prescription only
RoutesOral or IV
Pharmacokinetic data
Bioavailability40-50%
Protein binding6-16%
MetabolismHepatic <10%
Half-life6-7 hours
ExcretionRenal
Lactic (In lactiferous females)
Identifiers
CAS number29122-68-7 YesY
ATC codeC07AB03
PubChemCID 2249
IUPHAR ligand548
DrugBankDB00335
ChemSpider2162 YesY
UNII50VV3VW0TI YesY
KEGGD00235 YesY
ChEBICHEBI:2904 YesY
ChEMBLCHEMBL24 YesY
Chemical data
FormulaC14H22N2O3 
Mol. mass266.336 g/mol
 YesY (what is this?)  (verify)
 
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Atenolol
Systematic (IUPAC) name
(RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide
Clinical data
Trade namesTenormin
AHFS/Drugs.commonograph
MedlinePlusa684031
Licence dataUS FDA:link
Pregnancy cat.C (AU) D (US)
Legal status Prescription only
RoutesOral or IV
Pharmacokinetic data
Bioavailability40-50%
Protein binding6-16%
MetabolismHepatic <10%
Half-life6-7 hours
ExcretionRenal
Lactic (In lactiferous females)
Identifiers
CAS number29122-68-7 YesY
ATC codeC07AB03
PubChemCID 2249
IUPHAR ligand548
DrugBankDB00335
ChemSpider2162 YesY
UNII50VV3VW0TI YesY
KEGGD00235 YesY
ChEBICHEBI:2904 YesY
ChEMBLCHEMBL24 YesY
Chemical data
FormulaC14H22N2O3 
Mol. mass266.336 g/mol
 YesY (what is this?)  (verify)

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. The chemical works by slowing down the heart and reducing its workload. Unlike propranolol, atenolol does not pass through the blood–brain barrier thus avoiding various 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. The role for β-blockers in hypertension was downgraded in June 2006 in the United Kingdom to fourth-line, as they perform less appropriately or effectively than newer drugs, particularly in the elderly.

Medical uses[edit]

Atenolol is used for a number of conditions including: hypertension, angina, Long cough, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.[2]

It is also used to treat the symptoms of Graves' disease until antithyroid medication can take effect.

Due to its hydrophilic 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.[citation needed]

Hypertension[edit]

Atenolol is currently recommended only in special circumstances as complementary medication in hypertension. More frequently one or more of ACE Inhibitors, calcium antagonists and or diuretics are used as first line therapy.

Contraindications[edit]

Side effects[edit]

Atenolol causes significantly fewer central nervous system side effects (depression, nightmares).

It 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.[3]

In addition, β-blockers blunt the usual sympathetic nervous system response to hypoglycemia (i.e. sweating, agitation, tachycardia). These drugs therefore have an ability to mask a dangerously low blood sugar, which further decreases their safety and utility in diabetic patients.

Side effects include:[citation needed]

These side effects may or may not be experienced, but if they are, you should notify your doctor.

More serious side effects can include:[citation needed]

Serious side effects may require urgent medical attention. Some of these side effects are rare and others (not mentioned in the above list) can occur in some people.

Atenolol is classified as a β1-selective (or 'cardioselective') drug, one that exerts greater blocking activity on myocardial β1-receptors than on β2 receptors in the lung. The β2 receptors are responsible for keeping the bronchial system open. If these receptors are blocked, bronchospasm with serious lack of oxygen in the body can result. However, due to its cardioselective properties, the risk of bronchospastic reactions if using atenolol is reduced compared to nonselective drugs as propranolol. Nonetheless, this reaction may also be encountered with atenolol at high doses. Although traditionally β-blockers have been contraindicated when a person carries a diagnosis of asthma, recent studies have revealed that at moderate doses selective β-blockers such as Atenolol are well tolerated.

Provisional data suggests that 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. However, controlled studies are lacking.[4]

Unlike most other commonly used β-blockers, atenolol is excreted almost exclusively by the kidneys. This makes it attractive for use in individuals with end-stage liver disease.

Overdose[edit]

Symptoms of overdose are due to excessive pharmacodynamic actions on β1 and also β2-receptors. These include bradycardia, severe hypotension with shock, acute heart failure, hypoglycemia and bronchospastic reactions. Treatment is largely symptomatic. Hospitalization and intensive monitoring is indicated. In early cases emesis can be induced. 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.[5][6]

Pharmacokinetic data[edit]

References[edit]

  1. ^ 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. ^ "Atenolol". The American Society of Health-System Pharmacists. Retrieved 3 April 2011. 
  3. ^ Sheetal Ladva (2006-06-28). "NICE and BHS launch updated hypertension guideline". National Institute for Health and Clinical Excellence. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ R. Baselt (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, CA: Biomedical Publications. pp. 116–117. 

External links[edit]