TY - JOUR
T1 - Pyrazinoylguanidine
T2 - Antihypertensive, hypocholesterolemic, and renin effects
AU - Chambers, C. E.
AU - Vesell, E. S.
AU - Helm, C.
AU - Passananti, G. T.
AU - Beyer, K. H.
PY - 1992/12/1
Y1 - 1992/12/1
N2 - In a single-blind, placebo-controlled study of 12 subjects diagnosed as having mild to moderate hypertension and hypercholesterolemia, pyrnzinoylguanidine (PZG) in a dose of 600mg twice daily for 4 weeks reduced systolic blood pressure and heart rate. Pyrazinoylguanidine also reduced diastolic pressures, but to a lesser extent. Pyrazinoylguanidine reduced total serum cholesterol and low-density lipoprotein (LDL). Regression analysis indicated a dose-dependent reduction of both total cholesterol and LDL by PZG, i.e., the higher the presenting serum concentration, the greater the reduction by PZG. The extent of the reductions produced by PZG in elevated cholesterols and LDLs was highly correlated (r=.949). Normal high-density lipoprotein levels were unchanged by PZG. Pyrazinoylguanidine increased 24-hour urine volume and urinary excretion of sodium. Serum Na+, K+, or Cl- concentrations were unaltered. Means for plasma aldosterone and renin activities tended to decrease, but these trends did not attain statistical significance. Pyrazinoylguanidine was well tolerated. An activity profile that includes antihypertensive effects as well as reduction in hypercholesterolemia without major impact on serum renin or electrolyte balance makes PZG an attractive candidate for the management of hypertension.
AB - In a single-blind, placebo-controlled study of 12 subjects diagnosed as having mild to moderate hypertension and hypercholesterolemia, pyrnzinoylguanidine (PZG) in a dose of 600mg twice daily for 4 weeks reduced systolic blood pressure and heart rate. Pyrazinoylguanidine also reduced diastolic pressures, but to a lesser extent. Pyrazinoylguanidine reduced total serum cholesterol and low-density lipoprotein (LDL). Regression analysis indicated a dose-dependent reduction of both total cholesterol and LDL by PZG, i.e., the higher the presenting serum concentration, the greater the reduction by PZG. The extent of the reductions produced by PZG in elevated cholesterols and LDLs was highly correlated (r=.949). Normal high-density lipoprotein levels were unchanged by PZG. Pyrazinoylguanidine increased 24-hour urine volume and urinary excretion of sodium. Serum Na+, K+, or Cl- concentrations were unaltered. Means for plasma aldosterone and renin activities tended to decrease, but these trends did not attain statistical significance. Pyrazinoylguanidine was well tolerated. An activity profile that includes antihypertensive effects as well as reduction in hypercholesterolemia without major impact on serum renin or electrolyte balance makes PZG an attractive candidate for the management of hypertension.
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M3 - Article
C2 - 1487552
AN - SCOPUS:0027052889
SN - 0091-2700
VL - 32
SP - 1128
EP - 1134
JO - Journal of Clinical Pharmacology
JF - Journal of Clinical Pharmacology
IS - 12
ER -