Prucalopride
Prucalopride. Selective serotonin 5-HT4 receptor agonist; prokinetic for chronic idiopathic constipation. Largely excreted unchanged in urine. Oral half-life 24 h.
Selective serotonin 5-HT4 receptor agonist; prokinetic for chronic idiopathic constipation. Largely excreted unchanged in urine.
F 0.9 RETAINED but it is not a measurement: the label states "The absolute oral bioavailability is > 90%", a lower BOUND whose boundary the stored value sits exactly on. F 1.0 is as consistent with that label as 0.9. Kept because the bound is real and the direction is known, and flagged here so no later pass reads it as measured. PK from FDA prescribing information (DailyMed setid af559917-802b-486c-9f7b-b770115acac8): absolute bioavailability >90% (F 0.9), steady-state Vd 567 L, terminal t½ ~1 day (24 h), Tmax 2–3 h, 60–65% excreted unchanged in urine. ka_hr 1.5 derived from Tmax ~2.5 h (ke from t½ 24 h). PK: IT STAYS A LABEL ROW, AND THE SEARCH IS LOGGED RATHER THAN PAPERED OVER. A systematic chase — including the development code name and the sponsor pharmacokinetics authors — found NO PubMed abstract stating an absolute bioavailability, a volume of distribution or a terminal half-life for this drug. The label ">90%" is an INEQUALITY BOUND stored as a point estimate, which is a confirmed collision shape, and that is now said in the row own provenance text. ka 1.5 is a back-derivation that does not even reproduce its own note claim, implying 2.69 h against the 2.5 h asserted; the one verbatim Tmax available is a median of 2 h. A MATRIX FLAG IS RECORDED: "a mean blood-to-plasma concentration ratio of 1.9 indicated uptake of prucalopride into blood cells", so a plasma-referenced volume is not interchangeable with whole-blood quantities.
Pharmacokinetics
- Oral — t½ 24 h · F 90% · Vd 567 L
Sources: PMID:22943932, PMID:27614912, PMID:11438309