Atenolol is a beta blocker medication primarily used to treat high blood pressure and angina.[ Although used to treat high blood pressure, it does not seem to improve mortality rate in those with the condition.][ It can also be used with other blood pressure medications.][
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Common include feeling tired, heart failure, dizziness, depression, and shortness of breath.[ Other serious side effects include bronchospasm.][ Use is not recommended during pregnancy][ and alternative drugs are preferred when breastfeeding.][
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Atenolol was patented in 1969 and approved for medical use in 1975.
Medical uses
Atenolol is used for a number of conditions including hyperthyroidism,
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.
Atenolol has been used to treat , such as generalized anxiety disorder and social anxiety disorder.
Contraindications
of atenolol include sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt heart failure.
Side effects
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.
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.
Rarely, atenolol has been associated with induction of acute delirium.
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 such 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.
Interactions
Drug interaction with atenolol include catecholamine-depleting drugs like reserpine, calcium channel blockers, disopyramide, amiodarone, clonidine, prostaglandin synthase inhibitors like indomethacin, and digitalis glycosides.
Atenolol is mainly eliminated kidney without being metabolism by the liver or by cytochrome P450 .
Beta blockers like atenolol can reduce or block the cardiovascular effects of and amphetamines, such as hypertension and tachycardia.
Atenolol has been found to be safe in combination with the non-selective monoamine oxidase inhibitor (MAOI) phenelzine and actually improved orthostatic hypotension and hypertension reactions with phenelzine.
Pharmacology
Pharmacodynamics
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Notes: Values are Ki (nM), unless otherwise noted. The smaller the value, the more avidly the drug binds to the site. Refs: [
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Atenolol is a beta blocker; that is, an antagonist of the β-adrenergic receptors.
Beta-blocking effects of atenolol include reduction in resting and exercise heart rate and cardiac output, reduction of systolic and diastolic blood pressure at rest and with exercise, inhibition of tachycardia induced by isoproterenol (a non-selective β-adrenergic receptor agonist), and reduction of reflex orthostatic tachycardia.
The beta-blocking effects of atenolol, as measured by reduction of exercise-related tachycardia, are apparent within 1hour and are maximal within 2 to 4hours following a single oral dose.
Pharmacokinetics
Absorption
The oral bioavailability of atenolol is approximately 50 to 60%.
Distribution
The plasma protein binding of atenolol is 6 to 16%.
Atenolol is classified as a hydrophilic beta blocker with low lipophilicity and hence lower potential for crossing the blood–brain barrier and entering the brain.
Metabolism
Atenolol undergoes minimal or negligible drug metabolism by the liver.
Elimination
Instead of by hepatic metabolism, atenolol is eliminated from the blood mainly via kidney excretion.
The elimination half-life of atenolol is about 6 to 7hours.
The elimination of atenolol is slowed in renal impairment, with the elimination rate being closely related to the glomerular filtration rate (GFR) and with significant accumulation occurring when the creatinine clearance rate is under 35mL/min/1.73m2.
Chemistry
Atenolol is a substituted phenethylamine derivative.
The experimental log P of atenolol is 0.16 and its predicted log P ranges from −0.03 to 0.57.
History
Atenolol was in 1969 and was approved for medical use in 1975.
Society and culture
Changing medical practices
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.
