Pioglitazone

pharmacological · endocrine · digestive · renal · musculoskeletal · Oral

Pioglitazone. Thiazolidinedione — PPAR-γ agonist; sensitizes muscle, adipose, and liver to insulin. CYP2C8 substrate (gemfibrozil DDI). Weight… Oral half-life 8.3 h.

Thiazolidinedione — PPAR-γ agonist; sensitizes muscle, adipose, and liver to insulin. CYP2C8 substrate (gemfibrozil DDI). Weight gain + edema; bladder cancer signal in some studies; bone loss.

PK: THE HALF-LIFE WAS REFUTED BY THE ABSTRACT THE RECORD ALREADY CITED, which states the control value verbatim in the course of reporting an interaction — "prolonged its elimination half-life (t (1/2) ) from 8.3 to 22.7 hours". The stored 7 matches that paper, nor a 4.9 h value at 30 mg, nor a review "about 9 hours". F 0.83 becomes verbatim from a paper that was not cited at all: "It is well-absorbed, with a mean absolute bioavailability of 83% and reaching maximum concentrations in around 1.5 hours". THAT SAME SENTENCE IS ALSO THE PROBABLE ORIGIN OF ka 1.5, WHERE 1.5 IS A Tmax — and as a rate it does not even reproduce it, peaking at 2.04 h where 1.5 h would need about 2.3. Flagged as a strong candidate rather than a certainty, because 1.5 is also a round default elsewhere in this catalog; the co-location of both stored numbers in one sentence of an uncited paper is what makes it hard to read otherwise. CLASS 12 IS ACQUITTED: the cited study shows a perpetrator raising exposure 3.2x and half-life 2.7x with "no significant effect on its peak concentration (C max)", a pure clearance effect, so one compartment describes this drug well. V 17 is in no abstract and is NOT called as class 6, because it matches no obvious multiple of the label apparent volume.

Pharmacokinetics

Sources: PMID:15900286