Serum protein, binding

M24. Mendel, C. M., Laughton, C. W., McMahon, F. A., and Cavalieri, R. R., Inability to detect an inhibitor to thyroxine-serum protein binding in sera from patients with nonthyroidal illness. Metabolism 40, 152-159 (1991). 

Kanapilly, G. M. and Chimenti, R. A. (1972). In vitro serum protein binding of some citrated lanthanon nuclides and the behavior of 144Ce(III) and 9,Y(III) as citrated and serum protein bound forms in beagle dogs after injection, page 96 in Fission Product Inhalation Program Annual Report 1971-1972, Report No. LF-45 (Lovelace Foundation, Albuquerque, New Mexico). 

Reigner, B.G., J.F. Rigod, and T.N. Tozer. 1992b. Disposition, bioavailability, and serum protein binding of pentachlorophenol in B6C3F1 mouse. Pharmaceut. Res. 9 1053-1057. 

Serum protein binding is an important contributor to distribution and clearance in vivo. In addition, results from in vitro tests of compounds with high serum protein binding are expected to be sensitive to the presence of serum or other proteins in assay incubations. 

Lalezari and Lalezari synthesized urea derivatives of bezafibrate, and, with Perutz, determined the binding site of the most potent derivatives to be the same as that we had discovered for bezafibrate [35], Although all of these compounds were extremely potent, they were not suitable clinical candidates on account of being hampered again by serum protein binding [36, 37]. 

A rapid spectrofluorimetric technique for determining drag-serum protein binding in high throughput mode has been described [32]. 

In a pharmacokinetic study [49], this and related aspects of doxycycline were studied in man. Although the degree of serum protein binding as estimated by these workers was lower than in the report [41] discussed above, the differences seem inadequate to call in question the validity of their conclusions in addition, serum levels and protein binding data are not, of themselves, reliable indicators of therapeutic potential. 

Absorptlon/Dlstrlbutlon - Fenofibrate is well absorbed from the Gl tract. Peak plasma levels of fenofibric acid occur within 4 to 8 hours after administration. Serum protein binding is approximately 99%. 

Pharmacokinetics Misoprostol is extensively absorbed, with a time-to-reaoh peak eoneentration of misoprostol aeid of 12 minutes and a terminal half-life of 20 to 40 minutes. Plasma steady-state was aehieved within 2 days. The serum protein binding of misoprostol aeid is less than 90%. 

Distribution - Daptomycin is reversibly bound to human plasma proteins, primarily to serum albumin, in a concentration-independent manner. The mean serum protein binding of daptomycin was approximately 92% in healthy adults. 

Naive Bayesian classifier Intestinal absorption (passive), blood-brain barrier penetration, serum protein binding Classifier No [17]... 

Drug, Trade Name Preferred Route Serum half-life (hr) Serum protein binding (%)... 

The serum-protein binding ability, which varies between animals and is also influenced by the disease state of the animal, will also determine the free diffusible concentration. This, in turn, will have an effect on the elimination of drug residues as well as on their penetration in eggs or milk. This effect will be more pronounced for drugs with a higher tendency for protein binding such as sulfonamides, doxycycline, and cloxacillin (47). 

The half-life in diluted human serum was the same or longerthan in phosphate buffer, indicating that it is unlikely that an enzyme-catalyzed reaction occurs to release the parent drug. Indeed, the authors observed a longer half-life as the serum content was increased, which they believed was indicative of serum protein binding, affording protection from hydrolysis. 

Yokel RA, McNamara PJ. 1988. Influence of renal impairment, chemical form, and serum protein binding on intravenous and oral aluminum kinetics in the rabbit. Toxicol Appl Pharmacol 95 32-43. 

Blood. Limited serum protein binding capacity. Greater cutaneous blood flow Potential for greater amount of fi ee toxicant and greater distribution Greater percutaneous absorption... 

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