Sulindac
Sulindac. Prodrug NSAID (sulfoxide) reversibly reduced to the active sulindac sulfide (non-selective COX inhibitor) and irreversibly oxidized to… Oral half-life 18 h.
Prodrug NSAID (sulfoxide) reversibly reduced to the active sulindac sulfide (non-selective COX inhibitor) and irreversibly oxidized to inactive sulfone. The long-lived active sulfide drives efficacy; BID dosing.
PK: THE CLEANEST CHIMERA IN THE AUDIT — ONE NUMBER, ONE SENTENCE, ENTERED TWICE. The cited abstract contains exactly one half-life and it is explicitly the METABOLITE: "The latter, which all available evidence indicates to be the pharmacologically active form of sulindac ... has an apparent terminal half-life of 18.2 hr". There is no parent half-life in that paper at all. That single figure was entered once correctly as the sulfide in the effect note and once incorrectly as the parent oral half-life. The stored mass of 356.41 is the parent sulfoxide while the sulfide is 340.42, so the record mass and its half-life describe DIFFERENT MOLECULES — and the record itself contained the evidence. The value is retained, now labelled as the active sulfide, and the parent value of about 1.98 h is recorded in prose. F 0.88 IS A FRACTION ABSORBED WITH ITS HEDGE STRIPPED — "a MINIMUM OF APPROXIMATELY 88% of an oral dose is ABSORBED" — which is not bioavailability for a drug cleared by hepatic oxidation and reduction. ABOUT HALF THE ACTIVE SULFIDE IS MADE BY COLONIC BACTERIA: in ileostomy patients the late exposure fraction falls from 55% to 7%. A first-order gastric rate is the wrong model in kind, and ka 1.18 is dropped. V 15 L is unsourced and no intravenous study exists. MASS: THE ONLY ONE OF THE FOUR LIVE RECORDS IN THIS CLASS STILL MISMATCHED, AND THE DISAGREEMENT IS INTERNAL. Its occupancy row converted a published whole-blood inhibitory concentration using the SULFIDE mass, which is right — that is the species the assay measured and the species this record pk_analyte declares — while the record own molecular weight was the PARENT. Since the app back-converts the stored concentration for display USING THE RECORD MASS, the round trip did not close and the screen showed an affinity 4.5 percent away from what the source states. The stored mass is now the one the row itself used, so the record closes on itself exactly.
Pharmacokinetics
- Oral — t½ 18.2 h · F 88%
Sources: PMID:300048, PMID:10377455, PMID:4042521, PMID:8366178