Piperine

alkaloid · digestive · Oral

Piperine, an alkaloid. CYP3A4 and P-glycoprotein inhibitor (also inhibits UGT glucuronidation). Dramatically increases systemic exposure of… Oral half-life 2.5 h.

CYP3A4 and P-glycoprotein inhibitor (also inhibits UGT glucuronidation). Dramatically increases systemic exposure of co-administered CYP3A4 substrates — famously raises curcumin AUC ~20-fold. Also enhances intestinal epithelial absorption by increasing membrane permeability. The same mechanisms create real drug-interaction risk with narrow-therapeutic-index CYP3A4 substrates.

Pharmacokinetics

• Oral — t½ 2.5 h · F 25% · Vd 49 L

Related compounds

• Quercetin — synergistic
• Colchicine — caution
• Curcumin — synergistic

Sources: PMID:9619120