Category: pharmacological
Aliases: Avandia
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 Withdrawn EU 2010 after Nissen meta-analysis flagged a cardiovascular mortality signal; US restriction lifted 2013 with REMS modification.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).
PO: 3.5h