berberine

Macrolide antibiotics

Possibly Safe 135 PubMed studies PubChem 2353 ↗

Contraindications & warnings

Consult a healthcare professional before use if pregnant, breastfeeding, taking prescription medications, or if you have a medical condition. Keep out of reach of children.

About

Monitor for increased side effects of both compounds

Mechanism of action

Activates AMPK via mitochondrial Complex I inhibition, mimicking metformin. Downregulates PCSK9 increasing hepatic LDL receptor expression. Inhibits CYP3A4, CYP2D6, and P-glycoprotein. Stimulates GLP-1 secretion from intestinal L-cells.

Safety by population

Population	Safety rating	Max safe dose
Diabetes	Possibly safe	500mg 2-3x/day under medical supervision
May reduce HbA1c similarly to metformin. Medical supervision required — can cause hypoglycaemia.
General	Possibly safe	1500mg/day
Avoid in pregnancy. May interact with multiple medications via CYP3A4. Short-term (3 months) data available.
Pregnancy	Possibly unsafe	Avoid
May be toxic to fetus; crosses placental barrier. Contraindicated in pregnancy.

Effectiveness

No peer-reviewed clinical trial data found for this ingredient.

Drug interactions 14

Immunosuppressants

Berberine significantly inhibits CYP3A4, increasing cyclosporine plasma levels and toxicity risk.

Multiple drug classes

Berberine is a potent CYP3A4, CYP2D6, and P-glycoprotein inhibitor; increases plasma levels of many medications including statins, cyclosporine, and tacrolimus.

Cardiac glycosides

P-gp inhibition increases digoxin plasma levels

Antidiabetics

AMPK activation equivalent to metformin — additive hypoglycemia

Immunosuppressants

CYP3A4 and P-gp inhibition increases tacrolimus levels

Calcium channel blockers

CYP3A4 inhibition + direct vasodilation

Antiplatelet drugs

Antiplatelet activity via thromboxane inhibition

Chemotherapy

CYP3A4 + P-gp inhibition alters chemotherapy exposure

Antidepressants

CYP2D6 inhibition increases SSRI levels

Thyroid medications

Berberine reduces T3/T4 levels at high doses

Biguanides (diabetes)

Both berberine and metformin activate AMPK. Additive hypoglycaemic effect — risk of hypoglycaemia.

Beta-blockers

CYP2D6 inhibition increases metoprolol + negative chronotropic effects

Statins

CYP3A4 inhibition increases statin levels

Anticoagulant

CYP2C9 inhibition increases warfarin exposure, raising bleeding risk.

Medical disclaimer: This information is for educational purposes only. It does not constitute medical advice. Always consult a qualified healthcare professional before taking any supplement or changing your medication.

Data by supplement.ge — Public Health Institute of Georgia (PHIG)