Atenolol chemical structure
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Atenolol

Atenolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. Introduced in 1976, Atenolol was developed as a replacement for propanolol in the treatment of hypertension. Hypertension is a clinical condition in which the arterial blood pressure in rest exceeds constantly 140/90 mm Hg (as defined by the World Health Organization). Hypertension is a risk factor for stroke, myocardial infarction (heart attack), and serious renal damage. more...

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Propranolol is known to readily cross the blood-brain barrier (BBB) and can pass into the brain, causing side-effects such as depression and nightmares; atenolol was specifically developed to be unable to pass through the blood-brain barrier in order to prevent this effect.

Pharmacology and Indications

Atenolol can be used to treat cardiovascular diseases such as hypertension, coronary heart disease, arrhythmias, and treatment of myocardial infarction after the acute event. Patients with compensated congestive heart failure may be treated with Atenolol as a comedication (usually together with an ACE inhibitor, a diuretic and a digitalis-glycosid, if indicated). In patients with congestive heart failure, it reduces the need for and the consumption of oxygen of the heart muscle. It is very important to start with low doses, as atenolol reduces also the muscular power of the heart, which is an undesired effect in congestive heart failure.

The drug is also used to treat other conditions, including dysautonomia, anxiety and hyperthyroidism (overfunction of the thyroid gland).

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 (see below).

Atenolol is a so-called beta1-selective (or 'cardioselective') drug. That means that it exerts greater blocking activity on myocardial beta1-receptors than on beta2 ones in the lung. The beta2 receptors are responsible to keep the bronichal 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, particularly with high doses. Extreme caution should be exerted if Atenolol is given to asthma patients, who are particularly at risk; the dose should be as low as possible. If an asthma attack occurs, the inhalation of an beta2-mimetic antiasthmatic, such as hexoprenalin or salbutamol, will usually suppress the symptoms.

Provisonal 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 particular, diuretics are superior. Propranolol and metoprolol might also be better alternatives. However, controlled studies are lacking (CARLBERG, B. et al.: Lancet 2004; 364: 1684-9).

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

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Losartan trumps atenolol - Primary Care: Cardiology
From OB/GYN News, 5/1/02 by Sally Koch Kubetin

Losartan was associated with marked reductions in stroke and new-onset diabetes, compared with atenolol, in a landmark clinical trial of patients with hypertension.

"I think these results have immediate applicability to clinical practice. The message is that it matters how you lower blood pressure. We now have a treatment with benefit beyond blood pressure lowering," Dr. Bjorn Dahlof said at the annual meeting of the American College of Cardiology.

A total of 9,197 American, Scandinavian, and British patients with essential hypertension and left ventricular hypertrophy, all older than age 55, were randomized to either 50-100 mg/day of the angiotensin receptor blocker (ARB) losartan or the [beta]-blocker atenolol, with hydrochlorothiazide added as needed to reach blood pressure goals.

Achieved blood pressures were virtually identical in the two groups.

After a mean 4.8 years of therapy in the double-blind trial, which was sponsored by Merck & Co., patients in the losartan group had a highly significant 13% reduction in the composite primary study end point--cardiovascular death, stroke, or acute MI--compared with those on atenolol.

There was a 25% reduction in strokes with the ARB beyond the reduction achieved with [beta]-blocker therapy The losartan group also had an 11.4% greater reduction in cardiovascular mortality and a 7.3% reduction in acute MIs, compared with the atenolol group, neither of which reached statistical significance.

Losartan-treated patients had a striking 25% reduction in new-onset diabetes. Losartan also significantly reduced left ventricular hypertrophy, based on annual ECG results, said Dr. Dahlof, who is chair of the trial and a cardiologist at the University of Goteborg (Sweden).

COPYRIGHT 2002 International Medical News Group
COPYRIGHT 2002 Gale Group

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