MT Cardio


Renin inhibitors: pharmacokinetic, pharmacodynamic and efficacity in arterial hypertension treatment Volume 3, issue 4, Juillet-Août 2007


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Service de néphrologie, CHU Dupuytren, avenue Martin Luther-King, 87042 Limoges

Blood pressure is regulated to a large extent by the renin-angiotensin-aldosterone system, and current cardiovascular therapies antagonize this system by inhibiting the generation or action of angiotensin II. Aliskiren is the first drug in a new class of antihypertensive agents that directly inhibit the action of renin, the rate-limiting step in the system, thus theoretically antagonizing the renin-angiotensin system to a greater extent than current treatments. The high potency of aliskiren against human renin compensates for its low absolute bioavailability; at steady state its mean terminal half-life is 23 to36 hours. Aliskiren has a blood pressure-lowering effect similar to or better than that of hydrochlorothiazide, ramipril, irbesartan, losartan and valsartan and provides additional blood pressure reductions when used in combination with hydrochlorothiazide and with valsartan. Aliskiren is well tolerated, with non-specific adverse events occurring at a rate similar to that seen with placebo and other comparable drugs.