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PLASMA PROTEIN BINDING

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Introduction: It is binding of drug to plasma protein in blood component.  Binding of drugs to plasma proteins is reversible.  Various plasma protein to which drug binds includes Albumin, α1-Acid glycoprotein (orosomucoid), lipoprotein, globulins, etc.  Order of binding of drugs to various plasma proteins:  Albumin > α1-Acid glycoprotein (orosomucoid) > Lipoproteins > Globulins Such bound drug is both pharmacokinetically as well as pharmacodynamically inert i.e. a protein bound drug is neither metabolized nor excreted nor it  is pharmacologically active.  A bound drug is also restricted since it remains confined to a particular tissue for which it has greater affinity. Moreover, such bound drug because of its enormous size cannot undergo membrane transport & thus its half life is increased.  However this binding is rapidly reversible and non-specific – that is many drugs may bind to the same protein. Drug–plasma protein bindi...

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