Excretion balance and urinary metabolic pattern of [3H]cabergoline in man.
After oral administration of [3H]cabergoline to man at a single nominal dose of 0.6 mg/subject radioactivity is mainly eliminated by the faecal route (72% of the dose after 10 days). Urine contains 18% of the dose after the same period. The unchanged drug and metabolites present in urine were identified by comparison with reference compounds and quantified by radio-TLC analysis. Cabergoline is extensively metabolized. Unchanged drug in 0-24 h urine represents less than 14% of urinary radioactivity, reaching 20% in 0-96 h urine. The acid derivative FCE 21589 is the main metabolite, amounting to 38% and 30% of the urinary radioactivity in 0-24 h and 0-96 h urine, respectively. The amide derivative FCE 21590 appears to be present in only a small amount, accounting for no more than 4% of the urinary radioactivity in the urine of the first 24 hours after administration and increasing to about 8% in the 0-96 h urine.
Cocchiara
G
G
Department of Pharmacokinetics and Metabolism, Farmitalia Carlo Erba, Erbamont Group, Milan, Italy.
Benedetti
M S
MS
D000328:Adult; D000077465:Cabergoline; D004355:Drug Stability; D004873:Ergolines / Q000493:pharmacokinetics* / Q000652:urine; D005243:Feces / Q000737:chemistry; D006801:Humans; D008297:Male; D011388:Prolactin / Q000378:metabolism*; D012588:Scintillation Counting; D014316:Tritium
D004873:Ergolines; D014316:Tritium; D011388:Prolactin; D000077465:Cabergoline