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P-glycoprotein (P-gp) inhibitors, inducers and substrates

P-glycoprotein (P-gp) is a transporter, not a CYP enzyme. It sits in the gut wall, liver, kidney and the blood-brain barrier and pumps drugs out of cells: back into the gut, into bile and urine, and away from the brain. Blocking it can raise levels of digoxin and dabigatran; inducing it can lower them. Many drugs that act on CYP3A4 act on P-gp too: verapamil blocks it and rifampin induces it.

This is the desk's mapped set for P-gp, taken from the same catalog the desk uses to grade pairs. It is not a complete list. A drug that isn't listed here hasn't been cleared as safe; it just isn't on this list.

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What inhibition and induction mean

Inhibition. An inhibitor slows P-gp. Drugs that depend on P-gp can build up, so their levels and effects can rise. The effect starts as the inhibitor builds up and fades as it clears.

Induction. An inducer makes the body produce more P-gp. Levels of drugs that depend on P-gp can fall, and so can their effect. Induction builds over days to weeks and takes about as long to fade after the inducer stops.

Strong, moderate and weak are the desk's own grades for P-gp.

Names with a solid underline open that drug's page of label-sourced pairs. Names with a dotted underline open the desk with that drug.

P-gp inhibitors (39)

Strong inhibitors (8)

Moderate inhibitors (23)

Weak inhibitors (8)

P-gp inducers (6)

Strong inducers (2)

Moderate inducers (4)

P-gp substrates (34)

Sensitive substrates (4)

Exposure rises the most when P-gp is blocked.

Major-pathway substrates (22)

P-gp is one of the main routes for these.

Minor-pathway substrates (8)

P-gp is a smaller route for these; other routes carry most of the load.

Educational reference only. Not FDA-cleared. The Prescribing Information governs.