Hypertension, Vol 4, 93-101, Copyright © 1982 by American Heart Association
P Larochelle, P du Souich, P Hamet, P Larocque and J Armstrong
Prazosin was administered to 16 patients with essential hypertension in an
initial dose of 0.5 mg, after which the blood pressure (BP), pulse, and
plasma concentrations of prazosin were measured at 0, 0.5, 1, 1.5, 2, 2.5,
3, 4, 6, 8, and 24 hours. The dose of prazosin was then increased over 16
to 20 weeks, and similar sequences of measurements were obtained twice.
Eleven patients completed the 20-week course. All patients did not respond
in a similar way; two distinct patterns of BP and pulse response emerged,
although there was no significant difference in the pharmacokinetic
parameters, namely, absorption rate constant (Ka), maximum plasma
concentration (Cpmax), time to reach the maximum concentration (Tmax),
prazosin plasma half-life (T 1/2), elimination rate constant (kel),
prazosin plasma concentration-time curve (AUC), and clearance. Patients in
Group 1 had a marked reduction (52/30 mm Hg) of BP after the first dose of
prazosin, no pulse increase, and needed a small dose of prazosin to
maintain an adequate BP response. Patients in Group 3 had a minimal
reduction in BP (14/13 mm Hg) after a first dose, a significant pulse
increase, and needed a high dose of prazosin to control their BP. We
conclude that this effect might be due to a different drug-receptor
interaction, and the BP response and dose could be predicted from the
response of the first dose of prazosin.
ARTICLES
Prazosin plasma concentration and blood pressure reduction
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