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Influence of congestive heart failure on prazosin kinetics
Author(s) -
Jaillon Patrice,
Rubin Peter,
Yee Yin-Gail,
Ball Robert,
Kates Robert,
Harrison Donald,
Blaschke Terrence
Publication year - 1979
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1979256790
Subject(s) - prazosin , heart failure , medicine , endocrinology , chemistry , pharmacology , antagonist , receptor
The kinetics of oral prazosin was studied in 10 healthy normal subjects (NS) and in 9 patients with congestive heart failure (CHF). NS received a single 5‐mg dose, and blood concentrations of prazosin (C B ) were measured, using a specific HPLC assay, during an 8‐hr period. CHF patients received a 2‐mg dose after which C B was measured for 10 hr. These patients then received 2 to 5 mg prazosin every 8 hr for 48 hr. After the last dose of prazosin, C B was measured for 24 hr. After the initial dose, time to peak C B did not differ significantly between that of the NS (123 ± 19 SEM min) and of patients with CHF (132 ± 31.3 min). AUC/mg prazosin was greater (p < 0.001) in patients with CHF (3,385 ± 380 ng < min/ml) than in NS (1,603 ± 208 ng × min/ml). Elimination of prazosin from blood was slower in CHF patients (t½ = 374 ± 33.4 min) than in NS (t½ = 144.5 ± 4.3 min) (p < 0.001). These data suggest that in patients with CHF the elimination of prazosin is substantially slower than in NS and therefore higher steady‐state prazosin concentrations can be expected in CHF patients than in NS.

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