title: The influence of infusion rate on the pharmacokinetics and haemodynamic effects of nisoldipine in man.
abstract: 1. The pharmacokinetics and haemodynamic effects of nisoldipine on long term i.v. infusion of 2.40 mg and 9.59 mg in 25 h were studied in six healthy subjects. Liver blood flow at 0.8 and 24 h was assessed by measuring indocyanine green (ICG) clearance. 2. After high-dose nisoldipine, systemic clearance was 0.99 +/- 0.16 1 min-1, volume of distribution was 5.8 +/- 1.5 1 kg-1 and elimination half-life was 10.7 +/- 2.4 h. The pharmacokinetic parameters were similar after low-dose nisoldipine. 3. No significant changes in apparent liver blood flow were observed after either high-dose or low-dose nisoldipine. 4. Systolic blood pressure did not change, whereas diastolic blood pressure decreased by approximately 10% during both treatments. Maximal increase in heart rate was approximately 37% at high-dose infusion, whereas this was one half lower during the low-dose regimen. 5. Increased infusion rate results in an unfavourable shift in the haemodynamic effect profile of nisoldipine.
authors.affiliation: Center for Bio-Pharmaceutical Sciences, Division of Pharmacology, Leiden, The Netherlands.
authors.forename: J
authors.initials: J
authors.lastname: van Harten
authors.forename: P
authors.initials: P
authors.lastname: van Brummelen
authors.forename: R R
authors.initials: RR
authors.lastname: Zeegers
authors.forename: M
authors.initials: M
authors.lastname: Danhof
authors.forename: D D
authors.initials: DD
authors.lastname: Breimer
mesh_terms: D000327:Adsorption; D000328:Adult; D005260:Female; D006439:Hemodynamics / Q000187:drug effects*; D006801:Humans; D007208:Indocyanine Green; D007262:Infusions, Intravenous; D008102:Liver Circulation / Q000187:drug effects; D008297:Male; D009543:Nifedipine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D015737:Nisoldipine; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D014665:Vasodilator Agents; D015737:Nisoldipine; D009543:Nifedipine; D007208:Indocyanine Green