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European Journal of Clinical Pharmacology

, Volume 15, Issue 2, pp 105–108 | Cite as

Pharmacokinetics of a single oral dose of muzolimine in cardiac failure

  • O. Brørs
  • S. Jacobsen
  • E. Arnesen
Originals

Summary

The pharmacokinetics of a new “high ceiling” diuretic, muzolimine (Bay g 2821), were investigated after a single oral dose of 40 mg in 7 patients with cardiac failure (Stages I–IV, New York Heart Association classification), and in 2 healthy subjects. Plasma concentrations peaked 1–3 h after administration and declined according to a two-compartment model. The α-phase (distribution phase) lasted until 12–16 h after administration and the mean t1/2α was 3.6 h (range 2.3–4.7) in patients, and 2.6 h (range 2.3–2.9) in healthy subjects. The mean t1/2β was 13.5 h (range 7.4–22.4) in the patients and 14.0 h (range 12.4–14.6) in healthy subjects. T1/2β was not correlated with the degree of heart failure or with the area beneath the plasma concentration curve, which varied three-fold. The renal clearance of muzolimine was in the range 2.7–15.3 ml · min−1 in 5 subjects in whom it was investigated. The pharmacokinetics of muzolimine appear not to be significantly altered by cardiac failure. The prolonged half-lives of the drug are probably responsible for the longer duration of diuretic action reported for muzolimine than for furosemide and bumetamide.

Key words

muzolimine cardiac failure pharmacokinetics high ceiling diuretics 

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Copyright information

© Springer-Verlag 1979

Authors and Affiliations

  • O. Brørs
    • 1
  • S. Jacobsen
    • 1
  • E. Arnesen
    • 2
  1. 1.Institute of PharmacologyUniversity of OsloOsloNorway
  2. 2.Medical Department 7Ullevål HospitalOsloNorway

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