Pharmacokinetics of Bay g 2821 in the dog and in man

The pharmacokinetics of Bay g 2821, a new diuretic agent, were studied in dogs, healthy volunteers and in patients with renal insufficiency. The drug was rapidly absorbed after oral administration, peak plasma levels (approx. 0.4 microgram/ml) occurring within 1 hour. Elimination of the unchanged drug from plasma was biphasic - an initial rapid decline with a half-life of about 3 hours, followed by a longer second phase with a half-life of 13 to 17 hours. Results were similar in healthy volunteers and in patients with renal insufficiency. It is assumed that the drug is mainly eliminated in bile, probably after biotransformation, and elimination in the urine is a minor pathway.