Piperine

Category: alkaloid

Aliases: BioPerine, Black pepper extract

Pharmacological Mechanism

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.

Half-Life (t½)

PO: 2.5h

Dosing Guidelines

• PO: Typical 10 mg (Range: 5–20 mg)

Target Organ Systems

• digestive

Interactions

• Quercetin (synergistic): Piperine increases quercetin F; standard bioavailability-enhancer pairing.
• Colchicine (caution): Piperine is a noncompetitive CYP3A4 inhibitor in HLM. Volak 2008: Ki 5.4 ± 0.3 µM (IC50 5.5 µM). Raises colchicine exposure toward toxic range; concurrent dosing with high-piperine spices (black pepper, "BioPerine" supplements) is worth flagging in patients on chronic colchicine.
• Curcumin (synergistic): Canonical bioavailability-enhancer pair.

Pathways It Modulates

• Acetylcholine synthesis + degradation (inhibitor) — CYP3A4 + UGT inhibitor (black pepper)

Chemical Identifiers

• PubChem CID: 638024
• Formula: C17H19NO3
• Molecular weight: 285.34 g/mol
• InChIKey: MXXWOMGUGJBKIW-YPCIICBESA-N
• SMILES: C1CCN(CC1)C(=O)/C=C/C=C/C2=CC3=C(C=C2)OCO3

References

• PMID 9619120