Browse > Article

Antihypertensive Effects of Amlodipine Besylate and Its New Salts  

이병호 (한국과학연구원 생명의약부)
서호원 (한국과학연구원 생명의약부)
김맹섭 (한미약품(주)중앙연구소)
Publication Information
Biomolecules & Therapeutics / v.11, no.2, 2003 , pp. 133-138 More about this Journal
Abstract
The vascular relaxant and antihypertensive effects of newly developed salts of amlodipine-maleate and camsylate-were evaluated on isolated aorta from rats and in spontaneously hypertensive rats, and compared with those of amlodipine besylate, a standard drug. Amlodipine besylate concentration-dependently inhibited $Ca^{2＋}$-induced contraction in depolarised rat aorta($IC_{50}$/: 4.17 nM), with a very slow onset of action. Amlodipine maleate and amlodipine camsylate also showed vascular relaxant effect with a pattern and a potency similar to those of amlodipine besylate($IC_{50}$/: 3.62 and 3.28 nM, respectively). Amloclipine besylate produced a dose-dependent and long-lasting(>10∼24h) antihypertensive effect with a slow onset of action (ED$_{20}$: 2.31 mg/kg) in spontaneously hypertensive rats. Amlodipine maleate and amlodipine camsylate also exerted antihypertensive effects with a pattern and a potency similar to those of amlodipine besylate(ED$_{20}$: 2.09 and 2.21 mg/kg, respectively). These results suggest that amlodipine maleate and amlodipine camsylate are not statistically differ with amlodipine besylate in relaxant effect of $Ca^{2＋}$-induced contraction in depolarised rat aorta and in antihypertensive effect in spontaneously antihypertensive rats.
Keywords
antihypertension; amlodipine besylate; calcium antagonist;
Citations & Related Records
연도 인용수 순위
  • Reference
1 Meredith, P. A. and Elliott, H. L. (1992). Clinical pharmacokinetics of amlodipine. Clin. Phannacokinet. 22, 22-31   DOI   ScienceOn
2 Burges, R. A., Gardiner, D. G., Gwilt, M., Higgins, A. J., Blackburn, K. J., Campbell, S. F, Cross, P. E. and Stubbs. J. K. (1987). Calcium channel blocking properties of amlodipine in vascular smooth muscle and cardiac muscle in vitro: evidence for voltage modulation of vascular dihydropyridine receptors. J. Cardiovasc. Pharmacol. 9, 110-119
3 Burges, R. A., Dodd, M. G. and Gardiner. D. G. (1989). Pharmacologic profile of amlodipine. Am. J. Cardiol. 64, 10I-20I   DOI   ScienceOn
4 Burges, R. and Moisey, D. (1994). Unique pharmacologic properties of arnlodipine. Am. J. Cardiol. 73, 2A-9A
5 Dodd, M. G., Gardiner, D. G., Carter, A. J., Sutton, M. R. and Burges, R. A. (1989). The hemodynamic properties of amlodipine in anesthetised and conscious dogs: comparison with nitrendipine and influence of beta-adrenergic blockade. Cardiovasc. Drugs Ther: 3, 545-555.   DOI
6 Lee, B. H., Yoo, S. E. and Shin, H. S. (1998). Hemodynamic profile of SKP-450, a new potassium-channel activator. J. Cardiovasc. Pharmacol. 31, 85-94   DOI   ScienceOn
7 Lee, B. H., Seo, H. W., Kwon, K. J., Yoo, S. E. and Shin, H. S. (1999). In vivo pharmacologic profile of SK-1080, an orally active nonpeptidc ATI-receptor antagonist. J. Cardiovasc. Pharmacol. 33, 375-382   DOI   ScienceOn
8 Lee, B. H., Seo, H. W., Yoo, S. E., Kim, S. O., Lim, H. and Shin, H. S. (2001). Differential action of KR-31378, a novel potassium channel activator, on cardioprotective and hemodynamic effects. Drug Dev. Res. 54, 182-190   DOI   ScienceOn
9 Mathur, S., Syrne, H., Brown, C. A., Elliot, J., Moore, P. A., Newell, M. A., Munday, J. S., Cartier, L. M.. Sheldon, S. E. and Brown, S. A. (2002). Effects of the calcium channel antagonist amlodipine in cats with surgically induced hypertensive renal insufficiency. Am. J. Vel. Res. 63, 833-839   DOI   ScienceOn
10 Shin, H. S., Seo, H. W., Yoo, S. E. and Lee, B. H. (1998). Cardiovascular pharmacology of SKP-450, a new potassium channel activator, and its major metabolites SKP-818 and SKP- 310. Pharmacology 56, 111-124   DOI   ScienceOn
11 Stopher, D. A., Beresford, A. P., Macrae, P. V. and Humphrey, M. J. (1988). The metabolism and pharmacokinetics of amlodipine in humans and animals. J. Cardiovasc. Pharmacol. 12(Suppl 7), S55-559   DOI
12 Yamanaka, K., Suzuki, M., Munehasu, S. and Ishiko, J. (1991). Antihypertensive effects of amlodipine, a new calcium antagonist. Nippon Yakurigaku Zasshi 97, 115-126
13 Phillips, R. A., Kloner, R. A., Grimm, R. H. Jr. and Weinberger, M. (2003). The effects of amlodipine compared to losartan in patients with mild to moderately severe hypertension. J. Clin. Hypertens. (Greenwich) 5, 17-23