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Long acting beta-adrenoceptor agonist: Wikis

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Long acting beta-adrenoceptor agonists are usually prescribed for moderate to severe persistent asthma patients or patients with COPD. They are designed to replace the shorter acting B2-agonists such as salbutamol, as they have a duration of action of approximately 12 hours in comparison with the 4-6 hour duration of salbutamol, making them ideal candidates for twice-daily administration. Long acting B2-agonists' long duration of action is due to the addition of a long, lipophilic side chain which binds to an exosite. This allows the active portion of the molecule to continually bind and unbind at B2 receptors in the smooth muscle in the lungs.

Some currently available long acting beta-adrenoceptor agonists are:

Studies are currently underway into ultra-long-acting beta-adrenoceptor agonists which would have a duration of action of 24 hours, allowing for once-daily dosing:[1]

Footnotes

  1. ^ Cazzola M, Matera MG, Lötvall J (July 2005). "Ultra long-acting beta 2-agonists in development for asthma and chronic obstructive pulmonary disease". Expert Opin Investig Drugs 14 (7): 775–83. doi:10.1517/13543784.14.7.775. PMID 16022567.  
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