Naslov
Displacement of Drugs from Human Serum Albumin: From Molecular Interactions to Clinical Significance

Autori
Rimac, Hrvoje ; Debeljak, Željko ; Bojić, Mirza ; Miller, Larisa

Izvornik
Current medicinal chemistry (0929-8673) 24 (2017), 18; 1930-1947

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Human serum albumin ; Drug displacement ; Pharmacokinetic interactions ; Free concentration ; Drug design ; Sudlow’s site I ; Sudlow’s site II

Sažetak
Background: Human serum albumin (HSA) is the most abundant protein in human serum. It has numerous functions, one of which is transport of small hydrophobic molecules, including drugs, toxins, nutrients, hormones and metabolites. HSA has the ability to interact with a wide variety of structurally different compounds. This promiscuous, nonspecific affinity can lead to sudden changes in concentrations caused by displacement, when two or more compounds compete for binding to the same molecular site. Objective: It is important to consider drug combinations and their binding to HSA when defining dosing regimens, as this can directly influence drug’s free, active concentration in blood. Conclusion: In present paper we review drug interactions with potential for displacement from HSA, situations in which they are likely to occur and their clinical significance. We also offer guidelines in designing drugs with decreased binding to HSA.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija

POVEZANOST RADA