Drugs displacement

An aryloxypyrimi done has been described as an anti ulcer agent this activity is of note since the agent does not bear any structural relation to better known anti ulcer drugs. Displacement of halogen on the acetal of chloro-acetaldehyde by alkoxide from m-cresol gives the intermediate This affords enaminoaldehyde when subjected... 

MacKichan, J.J. (1989) Protein binding drug displacement interactions—fact or fiction Clin Pharmacokinet 16 65-73. 

MacKichan JJ. Protein binding drug displacement interactions fact or fiction Clin Pharmacokinei 1989 16 65-73. 

Drugs with high affinities for plasma albumin can also displace drugs with lower affinities. For example, sulfonamides bind to plasma proteins, but if phenylbutazone, which has a greater affinity for the binding sites, is administered, the concentration of the free sulfonamides in the plasma will increase due to drug displacement. 

BB Brodie. Clinical effects of interaction between drugs. Displacement of one drug by another from carrier or receptor sites. Proc R Soc Med 58 946, 1965. 

For a displacement interaction to become clinically important, a second mechanism usually operates sodium valproate can cause phenytoin toxicity because it both displaces phenytoin from its binding site on plasma albumin and inhibits its metabolism. Similarly aspirin and probenecid (and possibly other nonsteroidal anti-inflammatory drugs) displace the folic acid antagonist methotrexate from its protein-binding site and reduce its rate of active secretion by the renal tubules the result is serious methotrexate toxicity. 

There appear to be more cases of drug displacement involving drugs that are highly bound to albumin compared with drugs that bind to AAG and albumin. For example, the unbound free fraction of lidocaine can be increased significantly by therapeutic concentrations of bupivicaine of No significant... 

Denson DD, Myers JA, Coyle DE. The clinical relevance of the drug displacement interaction between meperidine and bupivacaine. Res Commun Chem Pathol Pharmacol 1984 45(3) 323-30. 

Warden WM. Drug displacement from protein binding source of the sulphadoxine liberated by phenylbutazone. Br J Pharmacol 1971 43(2) 325-34. 

Competition between drugs for plasma protein binding sites may increase the free fraction, possibly enhancing the effects of the drug displaced. 

Diphenylhydantoin, salicylates (07, W4), among other drugs, displace thyroxine from binding proteins in vitro and lower the PBI in vivo. This... 

---