Abstract

The binding of atenolol (selective ?1-blocker) and amlodipine (calcium channel blocker) to bovine serum albumin (BSA) was studied by equilibrium dialysis method in order to have an insight into the binding chemistry of these two to BSA. Free atenolol concentration was increased due to addition of amlodipine which reduced the binding of the compounds to BSA. However, the free fraction was increased to a level as it was expected from direct competitive displacement while the free atenolol concentration was increased according to increasing the amlodipine concentration when only the BSA was present. The result obtained when the binding site was blocked by sufficient amount of amlodipine was that the increment of free concentration of atenolol was prominent. When no amlodipine was added the free concentration of atenolol was only 28% whereas this release was 93 % to 98.01% when amlodipine was added with increasing concentration.

Highlights

  • It has been revealed by many epidemiological studies including the Framingham study that diabetes mellitus and hypertension are respectively risk factors of cardiovascular diseases and that the coexistence of diabetes mellitus with hypertension considerably increases the risk of cardiovascular diseases. (Epstein and Sowers, 1992; Grossman and Messerli, 1996; American Diabetes Association, 2002) The result of the U.K

  • The results of the Hypertension Optimal Treatment (HOT)-study on the correlation between optimum target blood pressure levels and the occurrence of cardiovascular events suggest that it is useful for hypertensive patients with diabetes mellitus to set the target levels lower than those for general hypertension patients (Hansson et al, 1998)

  • The drug-drug interaction study of atenolol and amlodipine bound to bovine serum albumin (BSA) was conducted in the presence and absence of site specific probe at 27°C and pH 7.4

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Summary

Introduction

It has been revealed by many epidemiological studies including the Framingham study that diabetes mellitus and hypertension are respectively risk factors of cardiovascular diseases and that the coexistence of diabetes mellitus with hypertension considerably increases the risk of cardiovascular diseases. (Epstein and Sowers, 1992; Grossman and Messerli, 1996; American Diabetes Association, 2002) The result of the U.K. (Epstein and Sowers, 1992; Grossman and Messerli, 1996; American Diabetes Association, 2002) The result of the U.K. Prospective Diabetes Study (UKPDS) suggests that blood pressure control, rather than blood glucose control, is efficient for prevention of macrovascular complications of those of diabetes mellitus, which include stroke and myocardial infarction ǃ-adrenoceptor blocking drugs are widely used for the treatment of cardiovascular diseases such as arterial hypertension, coronary heart disease and supraventricular and ventricular tachyarrhythmias. They may be beneficial in the hyperkinetic heart syndrome, hypotensive circulatory disorders, portal hyper-. You must attribute the work in the manner specified by the author or licensor

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