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Pharmacokinetics of intravenous cilazaprilat in normal volunteers.
Author(s) -
Whitehead EM,
Walters GE,
Williams PE,
Johnston GD
Publication year - 1989
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1989.tb03453.x
Subject(s) - pharmacokinetics , pharmacology , renal physiology , excretion , plasma clearance , medicine , plasma concentration , hemodynamics , metabolic clearance rate , clearance , renal function , urine , volunteer , chemistry , urology , biology , agronomy
The pharmacokinetics of 1 mg, 2 mg and 4 mg of cilazaprilat administered intravenously were determined in a group of eight volunteers. The fall in plasma concentration was polyphasic. Elimination was predominantly by renal excretion of the unchanged drug. The mean renal clearance values following 1 mg, 2 mg and 4 mg doses were 5.3 +/‐ 0.5, 8.1 +/‐ 0.5, and 9.8 +/‐ 0.5 l h‐1 and plasma clearances were 7.8 +/‐ 0.5, 10.4 +/‐ 0.5 and 11.8 +/‐ 0.6 l h‐1, respectively. Thus, plasma and renal clearances were dose dependent. ACE inhibition was greater than 82% for the first 4 h and about 55% at 24 h, after all three doses. There were no significant haemodynamic effects at any dose.

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