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Current Drug Therapy

Editor-in-Chief

ISSN (Print): 1574-8855
ISSN (Online): 2212-3903

Studies on Drug-Drug Interactions, Presence and Absence of Diazepam (Site-II Specific Probe) Propranolol and Amitriptyline at Binding Sites of Bovine Serum Albumin

Author(s): Shazid Md. Sharker, Monoara Khatun, Nazim Uddin, M. Shafiqul Hasan, Shomabash Chakma and Ahmed Ayedur Rahman

Volume 4, Issue 2, 2009

Page: [144 - 147] Pages: 4

DOI: 10.2174/157488509788185178

Price: $65

Abstract

The binding of Beta Adrenoceptor antagonist, propranolol and anti-depressant drug, amitriptyline, to bovine serum albumin (BSA) was studied by equilibrium dialysis (ED) method. During concurrent administration, it was found that amitriptyline has the capacity to release propranolol from its binding site on BSA, causing reduced binding of propranolol to BSA. This increment in free concentration of propranolol was from 5.15% to 9.15%, upon the addition of increased concentration of only amitriptyline 0x10-5M to 20x10-5 M, and in the presence of site-II specific probe (diazepam), it was from 6.95% to 10.45%. On the other hand, the release of amitriptyline from the binding sites on BSA was increased from 3.08% to 4.28% upon the addition of increased concentration of only propranolol 0x10-5 M to 20x10-5 M, and in the presence of site-II specific probe (diazepam), it was 0.51% to 4.75%. This form of drug-drug interaction at binding sites on BSA has been termed as site-to-site displacement. Drug-drug interactions, more specifically, displacement interaction will affect the free concentrations drugs in blood. Since the pharmacologic activity of a drug is a function of free drug concentration, the displacement of even a small amount of drug bound to plasma protein could produce considerable increase in activity.

Keywords: Propranolol, amitriptyline, diazepam, BSA, interaction, equilibrium dialysis


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