Pharmacokinetic Consequences of Plasma Protein Binding of Drugs

Schoenemann, Paul T.; Yesair, David W.; Coffey, John J.; Bullock, F. J.

doi:10.1111/j.1749-6632.1973.tb20479.x

Cited by 28 publications

(5 citation statements)

References 6 publications

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“…Dosage schedules that have been empirically devised for highly albumin-bound drugs are based on normal concentrations and drug-binding behavior of albumin. HSA has a limited number of binding sites for endogenous [22][23][24][25][26][27][28][29][30][31][32][33] and exogenous 26,[34][35][36][37][38][39][40][41][42][43][44] ligands (Table 1 and 2), so that drug binding to the protein may be affected by a variety of factors. The effect on pharmacokinetics of drugdrug competition for the same sites on HSA are generally held to be of little clinical importance.…”

Section: Fatty Acid Bindingmentioning

confidence: 99%

Ligand binding strategies of human serum albumin: How can the cargo be utilized?

et al. 2009

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Human serum albumin (HSA), being the most abundant carrier protein in blood and a modern day clinical tool for drug delivery, attracts high attention among biologists. Hence, its unfolding/refolding strategies and exogenous/endogenous ligand binding preference are of immense use in therapeutics and clinical biochemistry. Among its fellow proteins albumin is known to carry almost every small molecule. Thus, it is a potential contender for being a molecular cargo/or nanovehicle for clinical, biophysical and industrial purposes. Nonetheless, its structure and function are largely regulated by various chemical and physical factors to accommodate HSA to its functional purpose. This multifunctional protein also possesses enzymatic properties which may be used to convert prodrugs to active therapeutics. This review aims to highlight current overview on the binding strategies of protein to various ligands that may be expected to lead to significant clinical applications.

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Section: Fatty Acid Bindingmentioning

confidence: 99%

Ligand binding strategies of human serum albumin: How can the cargo be utilized?

et al. 2009

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“…The pharmacokinetic consequences of plasma protein binding were examined for one-and two-compartment models (29). The computer-simulated data treatment suggested that, if an elimination process operates on bound drug in the plasma for either the one-or two-compartment case, considerable alterations in half-life and area under the free drug concentration-time curve would be seen.…”

Section: Physical Significance Of Protein Bindingmentioning

confidence: 99%

Binding of Drugs by Albumin Plasma Protein

Vallner

1977

Journal of Pharmaceutical Sciences

325

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“…No information is available, however, on the binding of VPA in disease states such as renal failure or hepatic disease, which have been described to be associated with reduced binding of phenytoin (Reidenberg, Odar-Cederlof, von Bahr, Borga & Sjoqvist, 1971;Hooper, Bochner, Eadie & Tyrer, 1974). Alterations in protein binding may be of considerable importance, since they can profoundly affect the pharmacokinetics of drugs (Schoenemann, Yesair, Coffey & Bullock, 1973;Gugler, Shoeman, Huffman, Cohlmia & Azarnoff, 1975). Furthermore, the interpretation of drug plasma levels can become meaningless, if changes in protein binding are not taken into consideration .…”

Section: Introduction Methodsmentioning

confidence: 99%

Plasma protein binding of valproic acid in healthy subjects and in patients with renal disease.

Gugler¹,

Muêller²

1978

Brit J Clinical Pharma

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1 Based on the Scatchard plot of the binding data of valproic acid (VPA) it is concluded that the drug is bound by two groups of binding sites with the association constants K1=40.0 X 10(‐3) and K2=0.39 X 10(3), and the number of binding sites n1=1.5 and n2=6.8. 2 The binding is dependent on dialysis time, on temperature, on the drug concentration, and on the protein concentration in plasma. 3 At therapeutic plasma concentrations unbound VPA is 8.4 +/− 2.5%, but is increased to 20.3 +/− 4.7% in patients with significant impairment of renal function (P less than 0.001). 4 In patients with renal disease a good correlation is found between unbound VPA and serum creatinine, creatinine clearance, blood nitrogen and uric acid, respectively. A poor correlation is seen between unbound VPA and total protein or albumin concentration in plasma.

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Pharmacokinetic Consequences of Plasma Protein Binding of Drugs

Cited by 28 publications

References 6 publications

Ligand binding strategies of human serum albumin: How can the cargo be utilized?

Ligand binding strategies of human serum albumin: How can the cargo be utilized?

Binding of Drugs by Albumin Plasma Protein

Plasma protein binding of valproic acid in healthy subjects and in patients with renal disease.

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