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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Should atenolol be used for hypertension?
From American Family Physician, 3/15/05 by Henry Barry

Study Question: Does atenolol reduce cardiovascular morbidity and mortality in patients with hypertension? Setting: Various (meta-analysis)

Study Design: Systematic review

Synopsis: The authors of this briefly described systematic review evaluated the effect of atenolol on cardiovascular morbidity and mortality in patients with hypertension. However, the search strategy may have prematurely restricted the field, causing the authors to miss potentially relevant studies. Their search strategy allowed them to include only studies of atenolol versus placebo and five other studies that compared atenolol with other drugs. More than 23,000 patients who were evaluated for an average of 4.6 years were involved in these studies.

Compared with placebo, atenolol lowered systolic blood pressure by approximately 10 mm Hg and diastolic blood pressure by 6 mm Hg. Atenolol and the other drugs, however, had approximately the same effect on lowering blood pressure. In the placebo-controlled trials, atenolol had no effect on all-cause mortality, cardiovascular mortality, myocardial infarction, or stroke. In the studies using other drugs, one study--the Losartan Intervention For Endpoint (LIFE) reduction in hypertension study--included as many patients as the rest combined. The authors analyzed the studies with and without the LIFE data. When the LIFE study was included, no significant differences in all-cause mortality, cardiovascular mortality, myocardial infarction, or stroke were evident. When the LIFE data were not included, atenolol increased all-cause mortality (number needed to treat to harm [NNH] = 110 for 4.6 years; 95 percent confidence interval [CI], 59 to 798) and stroke (NNH = 79 for 4.6 years; 95 percent CI, 51 to 176).

The authors included several studies, including the LIFE trial, with questionable designs. One study was unblinded, two studies recruited patients with transient ischemic stroke or minor stroke, and one included only patients with left ventricular hypertrophy. Although most of the patients had hypertension, those studies were inappropriate to include as prevention trials. If these studies are excluded from the analysis, the authors' point that the data supporting the use of atenolol are limited is well taken.

Bottom Line: If these authors have identified all relevant research, it appears that atenolol is more effective than placebo in lowering blood pressure. It is not more effective than other medications, however. Furthermore, it does not appear to reduce the rates of cardiovascular morbidity or mortality. (Level of Evidence: 1a-)

Study Reference: Carlberg B, et al. Atenolol in hypertension: is it a wise choice? Lancet November 6, 2004;364:1684-9.

Used with permission from Barry H. Should atenolol be used for HTN? Accessed online December 28, 2004, at: http://www.InfoPOEMs.com.

COPYRIGHT 2005 American Academy of Family Physicians
COPYRIGHT 2005 Gale Group

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