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Pharmacokinetics of intravenous diltiazem and five of its metabolites in patients with chronic renal failure and in healthy volunteers
Author(s) -
Tawashi Maha,
Marcaurèle Julien,
Bichet Daniel,
Spénard Jean,
Larivière Lyne,
Plante Daniel,
Caillé Gilles
Publication year - 1991
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510120203
Subject(s) - diltiazem , pharmacokinetics , chronic renal failure , medicine , pharmacology , clinical pharmacology , metabolite , calcium
The pharmacokinetics of diltiazem were studied in seven patients with chronic renal failure (CRF) not requiring dialysis and in three healthy volunteers after a rapid i.v. infusion of 20mg. Mean plasma concentrations at the end of infusion were 3·15 times higher in patients with CRF than in healthy volunteers. From 0·5 to 12h post‐infusion, the difference remained between 25 per cent and 73 per cent. Mean AUC 0–∞ was statistically greater in patients than in volunteers while mean V area, CL tot , and CL ren were statistically lower. The t 1/2α and t β values were not significantly ( p > 0·05) different between patients and volunteers. Renal excretion was statistically more important in volunteers (6·6 per cent of the dose) than in patients (1·2 per cent of the dose). We therefore conclude that CRF does not influence t 1/2β of diltiazem but it interferes with the extent and possibly the rate of its extravascular distribution. That could result in transient high plasma concentrations after rapid i.v. infusion.