In vitro displacement interaction of atenolol and amlodipine on binding with bovine serum albumin when co-administered

  • Md. Ashraful Alam Department of Pharmacology, Bangladesh Agricultural University, Mymensingh 2202
  • Md. Abdul Awal Department of Pharmacology, Bangladesh Agricultural University, Mymensingh 2202
  • Mahbub Mostofa Department of Pharmacology, Bangladesh Agricultural University, Mymensingh 2202
  • Md. Kamrul Islam Department of Physiology, Bangladesh Agricultural University, Mymensingh 2202
  • Nusrat Subhan Pharmacy Discipline, Khulna University, Khulna 9208
Keywords: Amlodipine, Atenolol, Equilibrium dialysis, Interaction

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.

Downloads

Download data is not yet available.
Abstract
814
Download
532 Read
172

References

Alderman M, Madhavan S, Cohen H. Calcium antagonists and cardiovascular events in patients with hypertension and diabetes. Lancet 1998; 351: 216-17.

American Diabetes Association. Treatment of hypertension in adults with diabetes. Diabetes Care. 2002; 25(Suppl 1): S71-73.

Andrzejczak DG, Rska D, Czarnecka E. Influence of amlodipine and atenolol on lipopolysaccharide (LPS)-induced serum concentrations of TNF-alpha, IL-1beta, IL-6 in spontaneously hypertensive rats (SHR). Pharmacol Rep. 2006; 58: 711-19.

Davies RF, Habibi H, Klinke WP, Dessain P, Nadeau C, Phaneuf DC, Lepage S, Raman S, Herbert M, Foris K, et al. Effect of amlodipine, atenolol and their combination on myocardial ischemia during treadmill exercise and ambulatory monitoring. Canadian Amlodipine/Atenolol in Silent Ischemia Study (CASIS) Investigators. J Am Coll Cardiol. 1995; 25: 619-25.

Epstein M, Sowers JR. Diabetes mellitus and hypertension. Hypertension 1992; 19: 403-18.

Epstein M. Calcium antagonists and renal protection: current status and future perspectives. Arch Intern Med. 1992; 152: 1573-84.

Grossman E, Messerli FH. Diabetic and hypertensive heart disease. Ann Intern Med. 1996; 125: 304-10.

Hansson L, Zanchetti A, Carruthers SG, Björn Dahlöf, Elmfeldt D, Julius S, Ménqrd J, Rahn KH, Wedel H, Westerling WS. Effects of intensive blood-pressure lowering and aspirin in patients with hypertension: Principal results of the Hypertension Optimal Treatment (HOT) randomized trial. Lancet 1998; 351: 1755-62.

Hober A, Sjoholm I. The binding sites on human serum albumin for some non-steroidal anti-inflammatory drugs. Mol Pharmacol. 1980; 18: 421-26.

Mangano DT, Browner WS, Hollenberg M, London MJ, Tubau JF, Tateo IM. Association of perioperative myocardial ischemia with cardiac morbidity and mortality in men undergoing noncardiac surgery. N Engl J Med. 1990; 323: 1781-88.

Pahor M, Kritchevsky SB, Zuccala G, Guralnik JM. Diabetes and risk of adverse events with calcium antagonists. Diabetes Care. 1998a; 21: 193-94.

Pahor M, Psaty BM, Furberg CD. Treatment of hypertensive patients with diabetes. Lancet 1998b; 351: 689-90.

Singlas E. In: Determination of protein binding and its characteristics: Protein binding of drugs. 2nd ed. Switzerland, Hoffmann-La Roche, 1987, pp 25-31.

Tatti P, Pahor M, Byington RB. Outcome results of the Fosinopril versus Amlodipine Cardiovascular Events Randomized Trial (FACET) in patients with hypertension and NIDDM. Diabetes Care. 1998; 21: 597-603.

Tumoliehto J, Rastenyte D, Birkenhanger WH, Thijs L, Antikainen R, Bulpitt CJ, Fletcher AE, Forette F, Goldhaber A, Palatini P, Sarti C, Fagard R. Effect of calcium-channel blockade in older patients with diabetes and systolic hypertension. N Engl J Med. 1999; 340: 677-84.

UK Prospective Diabetes Study Group. Efficacy of atenolol and captopril in reducing risk of macro-vascular and microvascular complications in type 2 diabetes. BMJ. 1998; 317: 713-20.

Woodmansey PA, Stewart AG, Morice AH, Channer KS. Amlodipine in patients with angina uncontrolled by atenolol. Eur J Clin Pharmacol. 1993; 45: 107-11.

Xu LP, Shen FM, Shu H, Miao CY, Jiang YY, Su DF. Synergism of atenolol and amlodipine on lowering and stabilizing blood pressure in spontaneously hypertensive rats. Fundamental Clin Pharmacol. 2004; 18: 33-38.

How to Cite
Alam, M., M. Awal, M. Mostofa, M. Islam, and N. Subhan. “In Vitro Displacement Interaction of Atenolol and Amlodipine on Binding With Bovine Serum Albumin When Co-Administered”. Bangladesh Journal of Pharmacology, Vol. 2, no. 1, 1, pp. 20-26, doi:10.3329/bjp.v2i1.496.
Section
Research Articles