Abstract The renin-angiotensin system can be inhibited through inhibition of angiotensin I generation from angiotensinogen by direct renin inhibitors, inhibition of angiotensin II generation from angiotensin I by angiotensin-converting enzyme inhibitors and by direct inhibition of the action of angiotensin II receptor level. Aliskiren, the first direct renin inhibitor to reach the market, is a low molecular weight, orally active, hydrophilic nonpeptide. It blocks angiotensin I generation, while plasma renin concentration increases because the drugs blocks the negative feed-back exerted by angiotensin II on renin synthesis. Aliskiren is suitable for once-daily administration because of its long pharmacological half-life. Because of its mechanism of action, aliskiren may provide the additional opportunity to inhibit progression of atherosclerosis at tissue level. Hypertension is an approved indication for aliskiren, which is also promising for the treatment of heart failure and diabetic nephropathy. The efficacy of this drug on major clinical events is being tested in large ongoing clinical trials.

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