Pharmacokinetic profile and tolerability of pimobendan in patients with terminal renal insufficiency.
The pharmacokinetics of an i.v. bolus of pimobendan (P) 2.5 mg and 5.0 mg, its tolerability and the effect on heart rate and blood pressure have been studied in 12 subjects (42-70 y) suffering from severe terminal renal impairment. Plasma level data were compared with those obtained in a previous investigation in healthy volunteers. Pharmacokinetics were dose linear and were comparable to those in healthy subjects. No adjustment of the dose of P is necessary in patients with severe renal impairment. Tolerability of P, observed by means of blood pressure monitoring, clinical chemistry tests, electrocardiography and subjective judgement resulted in 4 complaints out of 12 patients: three suffered from orthostatic problems and vomiting, and one patient had nausea. Mean heart rate was elevated by 19% (2.5 mg) and 16% (5.0 mg). Blood pressure was significantly reduced after 2.5 mg P (23% systolic and 26% diastolic pressure), and after 5.0 mg P by 25% systolic and 23% diastolic pressure.
Przechera
M
M
Abteilung III, Medizinische Universitätsklinik, Tübingen, FRG.
Roth
W
W
Kühlkamp
V
V
Risler
T
T
Haehl
M
M
D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D002316:Cardiotonic Agents / Q000493:pharmacokinetics*; D004361:Drug Tolerance; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007676:Kidney Failure, Chronic / Q000378:metabolism*; D008297:Male; D011724:Pyridazines / Q000009:adverse effects / Q000493:pharmacokinetics*; D014665:Vasodilator Agents / Q000493:pharmacokinetics*
D002316:Cardiotonic Agents; D011724:Pyridazines; D014665:Vasodilator Agents; C041648:pimobendan