Drugs in the body are bound to metabolizing enzymes, targets/receptors and transport proteins in certain extent. The binding of drugs to targets or receptors is mainly specific and responsible for its pharmacological ...Drugs in the body are bound to metabolizing enzymes, targets/receptors and transport proteins in certain extent. The binding of drugs to targets or receptors is mainly specific and responsible for its pharmacological and therapeutic effects. The metabolizing of drugs by enzyme involves both specific and non-specific binding. Drugs interact to a different degree with proteins in blood non-specifically, which affects the distribution, metabolism, elimination, and pharmacological action. These binding properties are characteristic for a particular drug. Therefore, characterization of protein binding of drugs is important not only in therapeutic drug monitoring but also in early drug development. The binding of drugs to various proteins has been extensively studied. However, drugs may interact with each other in these binding reactions. Simultaneous administration of drugs influences their protein binding behavior, subsequently their absorption, excretion, distribution, efficacy and toxicity, which has been observed in many cases such as warfarin and phenylbutazone[1], cefazolin and cefoperazone[2]. Depending on the concentrations and their relative affinities for the binding sites, one drug may compete with another and displace it from the binding sites. The purpose of this study is emphasized on the evaluation of drug interaction in binding to protein.展开更多
文摘Drugs in the body are bound to metabolizing enzymes, targets/receptors and transport proteins in certain extent. The binding of drugs to targets or receptors is mainly specific and responsible for its pharmacological and therapeutic effects. The metabolizing of drugs by enzyme involves both specific and non-specific binding. Drugs interact to a different degree with proteins in blood non-specifically, which affects the distribution, metabolism, elimination, and pharmacological action. These binding properties are characteristic for a particular drug. Therefore, characterization of protein binding of drugs is important not only in therapeutic drug monitoring but also in early drug development. The binding of drugs to various proteins has been extensively studied. However, drugs may interact with each other in these binding reactions. Simultaneous administration of drugs influences their protein binding behavior, subsequently their absorption, excretion, distribution, efficacy and toxicity, which has been observed in many cases such as warfarin and phenylbutazone[1], cefazolin and cefoperazone[2]. Depending on the concentrations and their relative affinities for the binding sites, one drug may compete with another and displace it from the binding sites. The purpose of this study is emphasized on the evaluation of drug interaction in binding to protein.
