Steady-state intravenous pharmacokinetics of pirenzepine in patients with hepatic insufficiency and combined renaland hepatic insufficiency
The steady-state intravenous pharmacokinetics of pirenzepine has been investigated in patients with chronic liver disease and others with combined chronic liver disease and renal sufficiency.
The plasma clearance (CL) of Pirenzepine, steady-state plasma concentration Cmin(ss) and dominant half life t1/2γ were not significantly altered in the chronic liver disease group. In patients with renal and hepatic insufficiency, CL was reduced, t1/2γ was prolonged from 11.1 to 19.4 h and Cmin(ss) was elevated from 36 ng/ml to 66 ng/ml compared to healthy controls. Plasma concentrations remained in the therapeutic range and the dosage regimen was well tolerated.
Adjustment of the dose of pirenzepine need be considered only in cases of severe impairment of both renal and hepatic elimination.
Key wordspirenzepine hepatic insufficiency hepato-renal insufficiency pharmacokinetics
Unable to display preview. Download preview PDF.
- 1.Carmine AA, Brogden RN (1985) Pirenzepine: A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases. Drugs 30: 85–126Google Scholar
- 2.Krakamp B, Tanswell P, Vogel H, Bozler G (1989) Steady-state pharmacokinetics of pirenzepine in patients with differing degrees of renal function impairment. Eur J Clin Pharmacol 36: 75–78Google Scholar
- 3.Hammer R, Bozler G, Zimmer A, Koss FW (1977) Pharmakokinetik und Metabolismus von L-S 519 CL2 (Pirenzepin) beim Menschen. Therapiewoche 27: 1575–1593Google Scholar
- 4.Kühn HA, Wernze H (1979) Klinische Hepatologie. Thieme, Stuttgart New YorkGoogle Scholar
- 5.Tanswell P, Kasper W, Zahn G (1986) Automated monoclonal radioimmunoassays for pirenzepine, a selective muscarinic receptor antagonist, in plasma and urine. J Immunol Methods 93: 247–258Google Scholar
- 6.Lauterbach F (1987) Intestinal permeation of nonquarternary amines: A study with telenzepine and pirenzepine int he isolated mucosa of guinea pig jejunum and colon. J Pharmacol Exp Ther 243: 1121–1130Google Scholar