PMID: 9530986Apr 8, 1998Paper

Pharmacokinetics and haemodynamic effect of diltiazem in rats: effect of route of administration

The Journal of Pharmacy and Pharmacology
B C TsuiP K Yeung

Abstract

Diltiazem is a calcium antagonist widely used for the treatment of angina and hypertension. Previous studies in patients have shown that the haemodynamic effects of diltiazem are greater after parenteral rather than oral administration. The rat has been used as an animal model to determine the effect of the route of administration on the pharmacokinetic and haemodynamic effects of diltiazem. The results showed that plasma concentrations of diltiazem were more than 10 times higher after the intra-arterial dose. The plasma concentrations of the major metabolites were also higher after intra-arterial administration, although only for deacetyl diltiazem (M1) did the difference reach statistical significance (P < 0.05). The haemodynamic effects (on blood pressure and heart rate) of diltiazem were considerably greater after intra-arterial administration; this was attributed mainly to the much higher plasma concentrations of diltiazem. The hypotensive and chronotropic effects of diltiazem were similar; Emax and EC50 for diastolic blood pressure were 72+/-19% and 4.4+/-5.9 microg mL(-1); for heart rate they were 77+/-32% and 10.0+/-11.7 microg mL(-1), respectively. The haemodynamic effects of diltiazem are much greater after intra-arte...Continue Reading

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Citations

Jun 15, 2007·Journal of Pharmacological and Toxicological Methods·Facundo M BerteraChristian Höcht
Feb 26, 2008·Journal of Pharmaceutical and Biomedical Analysis·Pollen YeungWilliam L Casley
Nov 12, 2010·ACS Nano·Nicolas BertrandJean-Christophe Leroux

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