β Adrenergic Blocking Drugs

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Chapter: Essential pharmacology : Antiadrenergic Drugs (Adrenergic Receptor Antagonists) And Drugs For Glaucoma

The dichloro derivative of isoprenaline was the first compound found in 1958 to block adrenergic responses which could not be blocked till then by the available adrenergic antagonists.


β ADRENERGIC BLOCKING DRUGS

 

These drugs inhibit adrenergic responses mediated through the β receptors.

 

The dichloro derivative of isoprenaline was the first compound found in 1958 to block adrenergic responses which could not be blocked till then by the available adrenergic antagonists. However, it was not suitable for clinical use. Propranolol introduced in 1963 was a therapeutic breakthrough. Since then, drugs in this class have proliferated and diversified.

 

All β blockers are competitive antagonists. Propranolol blocks β1 and β 2 receptors but has weak activity on β3 subtype. It is also an inverse agonist: reduces resting heart rate as well.

 

CLASSIFICATION

 

Nonselective (β1 and β2)

 

      a.  Without intrinsic sympathomimetic activity

               Propranolol, Sotalol, Timolol.

 

a.      With intrinsic sympathomimetic activity

              Pindolol

 

b.     With additional α blocking property

     Labetalol, Carvedilol

 

Cardioselective 1)

 

Metoprolol, Atenolol, Acebutolol, Bisoprolol, Esmolol, Betaxolol, Celiprolol, Nebivolol

 

 

Another system of classifying β blockers into 3 generations has been proposed.


 

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