In-vitro Relationship between Protein-binding and Free Drug Concentrations of a Water-soluble Selective Beta-adrenoreceptor Antagonist (Atenolol) and Its Interaction with Arsenic

The degree of binding of a drug to plasma proteins has a marked effect on its distribution, elimination, and pharmacological effect since only the unbound fraction is available for distribution into extra-vascular space. The protein-binding of atenolol was measured by equilibrium dialysis in the bov...

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Veröffentlicht in:Journal of health, population and nutrition population and nutrition, 2009-02, Vol.27 (1), p.20-30
Hauptverfasser: Alam, M.A, Awal, M.A, Subhan, N, Mostofa, M
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creator Alam, M.A
Awal, M.A
Subhan, N
Mostofa, M
description The degree of binding of a drug to plasma proteins has a marked effect on its distribution, elimination, and pharmacological effect since only the unbound fraction is available for distribution into extra-vascular space. The protein-binding of atenolol was measured by equilibrium dialysis in the bovine serum albumin (BSA). Free atenolol concentration was increased due to addition of arsenic which reduced the binding of the compounds to BSA. During concurrent administration, arsenic displaced atenolol from its high-affini-ty binding Site I, and free concentration of atenolol increased from 4.286±0.629% and 5.953±0.605% to 82.153±1.924% and 85.486±1.158% in absence and presence of Site I probe respectively. Thus, it can be suggested that arsenic displaced atenolol from its binding site resulting in an increase of the free atenolol concentration in plasma.
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subjects Adrenergic beta-Antagonists - chemistry
Adrenergic beta-Antagonists - pharmacokinetics
Albumins
Animals
Antagonist drugs
Arsenic
Arsenic - chemistry
Arsenic - pharmacokinetics
Atenolol
Atenolol - chemistry
Atenolol - pharmacokinetics
Binding Sites
Binding, Competitive
Biological Availability
Blood proteins
Bovine serum albumin
Cattle
Concentration
Dialysis
Drug Interactions
Elimination
Humans
Hypertension
Original Papers
Pharmacokinetics
Pharmacology
Physiological aspects
Plasma
Plasma protein-binding
Protein binding
Proteins
Serum
Serum Albumin - chemistry
Serum Albumin - pharmacokinetics
Serum albumins
Sodium
Ungulates
title In-vitro Relationship between Protein-binding and Free Drug Concentrations of a Water-soluble Selective Beta-adrenoreceptor Antagonist (Atenolol) and Its Interaction with Arsenic
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