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

Department of Pharmacy, Stamford University Bangladesh, 51 Siddeswari Road, Dhaka 1217, Bangladesh.
Journal of Health Population and Nutrition (Impact Factor: 1.04). 03/2009; 27(1):20-30.
Source: PubMed


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-affinity 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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    • "On the basis of probe displacement method, it has been found that there are at least three relatively high specific drug binding sites on the human serum albumin (HSA) molecule[12]. "
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    ABSTRACT: Owing to the drug's favorable hydrophilic and pharmacokinetic characteristics, a number of case reports have demonstrated effective treatment of atenolol overdose with hemodialysis. However, the efficiency of atenolol clearance throughout hemodialysis treatments has not previously been examined. In this report, a patient with impaired renal function was successfully treated with two 5-hour intermittent high-flux high-efficiency hemodialysis therapies after atenolol overdose. Serial atenolol levels were measured during his hemodialysis treatments. We observed an over 50% plasma atenolol concentration reduction after each 5-hour hemodialysis therapy. Hemodialysis therapy is an effective treatment for atenolol overdose, especially in patients with impaired renal function.
    Hemodialysis International 01/2013; 17(4). DOI:10.1111/hdi.12020 · 1.24 Impact Factor


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