Rosiglitazone
Rosiglitazone. Thiazolidinedione (TZD) PPAR-γ agonist for type 2 diabetes — improves insulin sensitivity in muscle and adipose tissue without… Oral half-life 3.6 h.
Thiazolidinedione (TZD) PPAR-γ agonist for type 2 diabetes — improves insulin sensitivity in muscle and adipose tissue without directly increasing insulin secretion. Major CYP2C8 substrate; CYP2C9 contributes minor pathway. Withdrawn EU 2010 after Nissen meta-analysis flagged a cardiovascular mortality signal; US restriction lifted 2013 with REMS modification. Currently rare in clinical use, having been largely displaced by pioglitazone and the GLP-1/SGLT2 classes. PK (Avandia label, 4 mg PO qd): Cmax peak 1 h post-dose, t½ 3-4 h (dose-independent), F 99%, Vss/F 17.6 L, protein binding 99.8%. Food ↓Cmax 28% + delays Tmax to 1.75 h but doesn't change overall AUC. CYP2C8 substrate — gemfibrozil 2.3× AUC bump (Niemi 2003 PMID:12898007).
PK: MOSTLY RIGHT, WITH TWO SUB-FIVE-PERCENT CORRECTIONS RECORDED SO NOBODY LATER OVER-CORRECTS THEM. Bioavailability is verbatim twice over. The half-life was A MIDPOINT — its citation says "3-7 h" and this record own prose says three to four — and the verbatim replacement was ALREADY SITTING IN ITS REFERENCE LIST, in the control arm of a same-dose interaction study: "prolonged the elimination half-life (t(1/2)) of rosiglitazone from 3.6 to 7.6 h". The volume was unsupported AND CONTRADICTED BY THIS RECORD OWN MECHANISM TEXT, which states a figure two tenths of a litre larger — a transcription slip, now reconciled to the prose. Both changes are worth about three percent and neither is a defect of substance; the clearance already sat within noise of the published figure. MY PIOGLITAZONE-SHAPED PRIOR DOES NOT FIT HERE: the absorption rate matches no peak time in any cited abstract, so it is unsourced rather than misattributed.
Pharmacokinetics
- Oral — t½ 3.6 h · F 99% · Vd 17.4 L
Sources: PMID:12898007, PMID:15371985, PMID:10859151