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Re: Cardioselectivity

Posted by ed_uk on February 2, 2005, at 9:09:06

In reply to Re: Beta Blockers and Tachycardia » KaraS, posted by ed_uk on February 2, 2005, at 7:22:06

Beta blockers....

By convention, a beta blocker is described as being 'cardioselective' when it has a greater affinity for beta-1 receptors than beta-2 receptors. The majority of beta-1 receptors are found in the heart (not all beta-1 receptors are found in the heart however). Beta-2 receptors are present in the airways, the heart, the uterus, peripheral blood vessels etc.

Nebivolol, bisoprolol, atenolol, metoprolol, acebutolol are all beta-1 selective. They are not totally specific for beta-1 receptors however, because they also have low affinity for beta-2 receptors.

Most beta-1 selective.... nebivolol > bisoprolol > atenolol, metoprolol > acebutolol ....least beta-1 selective.

Whether or not a beta-blocker penetrates the blood brain barrier in large quantities does NOT have anything to do with its cardioselectivity (its beta-1 selectivity). Lipophilic beta-blockers such as propranolol can readily enter the brain, water soluble beta blockers such as atenolol enter the brain in small quanties only.

Ed.


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