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Publisher SummaryThis chapter discusses the physical properties, synthesis, stability, pharmacokinetics and metabolism, and analytical methods of isoproterenol. Isoproterenol is the most active of the sympathomimetic amines that act almost exclusively on β-receptors by virtue of their N-alkyl substitution. Isoproterenol gradually darkens on exposure to air and light. Aqueous solutions become pink to brownish pink on exposure to air and almost immediately when made alkaline. Solutions should contain an antioxidant, such as sodium metabisulphite, and contact with metals should be avoided as it causes discoloration and the loss of activity. Isoproterenol can be prepared by condensing 3,4-dihydroxy-α-chloroacetophenone and isopropylamine to form 3,4-dihydroxyisopropylaminoacetophenone. This gives the required product on catalytic reduction. Isoproterenol is readily absorbed when given parentrally or as an aerosol. The absorption of sublingual or oral doses is unreliable.The drug is poorly absorbed from stomach, but well absorbed from small intestine, proximal colon, rectum, and the mucous membrane of the trachea.


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