CYP3A4: The Liver Enzyme Behind Many Drug Interactions
[Glossary · How doses act in the body]

CYP3A4

Also called cytochrome P450 3A4, CYP3A4 inhibitor, CYP3A4 inducer · Reviewed

Definition: CYP3A4 is an enzyme in the body that breaks down many medicines. Drugs and foods that block it (inhibitors) can raise the level of another drug in the blood, and those that speed it up (inducers) can lower it. Labels name CYP3A4 when this changes the dose or safety.

Inhibitors raise levels

The Viagra label says ritonavir raised sildenafil blood levels about 11-fold, and saquinavir and erythromycin about 3-fold. With ritonavir the label caps the dose at 25 mg in 48 hours.

The Addyi label goes further. Moderate or strong CYP3A4 inhibitors are contraindicated because they can cause severe low blood pressure and fainting. Its examples:

  • ketoconazole and fluconazole (antifungals);
  • ritonavir (an HIV medicine);
  • clarithromycin (an antibiotic);
  • diltiazem and verapamil (heart medicines);
  • grapefruit juice, listed as a moderate inhibitor.

In one study on that label, fluconazole raised flibanserin exposure 7-fold and the study was stopped.

Inducers lower levels

The Addyi label lists rifampin, carbamazepine, phenytoin and St. John's Wort as CYP3A4 inducers that sharply lower flibanserin levels, and says using them together is not recommended. St. John's Wort is sold as a dietary supplement, which is a reminder that interactions are not limited to prescriptions.

Why it matters for your log

An interaction shows up when two things overlap in time. A log with every medicine and supplement, including short antibiotic courses, lets a pharmacist check them together. It can also explain why a familiar dose suddenly feels stronger or weaker, because the clearance of the drug has changed.

Read more on Dose Track: Viagra side effects · Addyi side effects · Tadalafil vs sildenafil · Interaction checker

General education drawn from labels and published studies, not personal medical advice. Your prescriber, pharmacist and the label that came with your product are the final word.

Frequently asked questions

Why does grapefruit juice matter for some drugs?+
The Addyi label lists grapefruit juice as a moderate CYP3A4 inhibitor. It can raise the level of drugs broken down by that enzyme.
Can a supplement cause a CYP3A4 interaction?+
Yes. The Addyi label names St. John's Wort as a CYP3A4 inducer that sharply lowers flibanserin levels.