TY - JOUR
T1 - Angiotensin II type 1 receptor blockade with 80 and 160 mg valsartan in healthy, normotensive subjects
AU - Latif, Farhana
AU - Tandon, Suman
AU - Obeleniene, Rimvida
AU - Hankins, Shelley R.
AU - Berlowitz, Michael S.
AU - Ennezat, Pierre Vladimir
AU - Le Jemtel, Thierry H.
PY - 2001
Y1 - 2001
N2 - Background: An 80-mg dose once or twice daily is the dose of valsartan frequently administered for treatment of hypertension. The target dose selected for the Val-HeFT trial in patients with chronic heart failure is 160 mg twice daily. The level and time course of angiotensin II type 1 (AT1)-receptor blockade achieved by 160 mg valsartan have not been reported. Methods and Results: Seven normotensive healthy subjects were assigned in random order to receive a single dose of placebo, 80 mg valsartan, and 160 mg valsartan at 7- to 10-day intervals. AT1-receptor blockade level (%) was determined by the pressure response to administration of exogenous angiotensin II. The pressure response to angiotensin II was measured at baseline and 2, 6, 12, and 24 hours after oral administration of placebo, 80 mg valsartan, and 160 mg valsartan. Eighty and 160 mg valsartan resulted in a significant and similar level of AT1-receptor blockade at 2 and 6 hours compared with placebo. The 160-mg dose resulted in a significantly greater level of AT1-receptor blockade than 80 mg at 12 and 24 hours. Conclusions: During the first 6 hours after oral administration of 80 and 160 mg valsartan the level of AT1-receptor blockade is similar. However, only 160 mg valsartan provides sustained AT1-receptor blockade over 24 hours.
AB - Background: An 80-mg dose once or twice daily is the dose of valsartan frequently administered for treatment of hypertension. The target dose selected for the Val-HeFT trial in patients with chronic heart failure is 160 mg twice daily. The level and time course of angiotensin II type 1 (AT1)-receptor blockade achieved by 160 mg valsartan have not been reported. Methods and Results: Seven normotensive healthy subjects were assigned in random order to receive a single dose of placebo, 80 mg valsartan, and 160 mg valsartan at 7- to 10-day intervals. AT1-receptor blockade level (%) was determined by the pressure response to administration of exogenous angiotensin II. The pressure response to angiotensin II was measured at baseline and 2, 6, 12, and 24 hours after oral administration of placebo, 80 mg valsartan, and 160 mg valsartan. Eighty and 160 mg valsartan resulted in a significant and similar level of AT1-receptor blockade at 2 and 6 hours compared with placebo. The 160-mg dose resulted in a significantly greater level of AT1-receptor blockade than 80 mg at 12 and 24 hours. Conclusions: During the first 6 hours after oral administration of 80 and 160 mg valsartan the level of AT1-receptor blockade is similar. However, only 160 mg valsartan provides sustained AT1-receptor blockade over 24 hours.
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U2 - 10.1054/jcaf.2001.26242
DO - 10.1054/jcaf.2001.26242
M3 - Article
C2 - 11561228
AN - SCOPUS:0034827191
SN - 1071-9164
VL - 7
SP - 265
EP - 268
JO - Journal of Cardiac Failure
JF - Journal of Cardiac Failure
IS - 3
ER -