Berberine: benefits, dosage, contraindications
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Phytochemicals
Indications
Scoring methodology
EFSA approval.
Type 2 diabetes ✪✪✪✪✪
Clinical research shows that taking berberine at 500 mg 2 to 3 times per day for 2 to 3 months can reduce glycated hemoglobin (HbA1c), fasting blood glucose, and postprandial blood glucose in patients with type 2 diabetes, compared with placebo, and may be as effective as metformin (drug) at 500 mg 2 to 3 times per day or rosiglitazone (drug) at 4 mg per day. A meta-analysis confirms that berberine, taken at 900 mg to 3 g per day for 1 to 11 months, reduces fasting blood glucose, postprandial blood glucose, and HbA1c compared with lifestyle interventions alone. Similarly, taking berberine in combination with oral hypoglycemic agents appears to have better results compared with hypoglycemic agents alone.
Posologie
Oral
900 - 1500 mg
Effects of berberine on blood glucose in patients with type 2 diabetes mellitus: a systematic literature review and a meta-analysis
Efficacy of berberine in patients with type 2 diabetes mellitus
Berberine lowers blood glucose in patients with type 2 diabetes mellitus by increasing insulin receptor expression
Treatment of type 2 diabetes and dyslipidemia with the natural plant alkaloid berberine
Meta-analysis of the effect and safety of berberine in the treatment of type 2 diabetes mellitus, hyperlipidemia, and hypertension
Effect of a New Formulation of Nutraceuticals as an Add-On to Metformin Monotherapy for Patients with Type 2 Diabetes and Suboptimal Glycemic Control: A Randomized Controlled Trial
Combined berberine and probiotic treatment as an effective regimen for improving postprandial hyperlipidemia in type 2 diabetes patients: a double blinded placebo controlled randomized study
Hypercholesterolemia ✪✪✪✪✪
Clinical studies conducted in people with hyperlipidemia show that berberine, alone or in combination with lipid-lowering medications, can reduce total cholesterol, triglycerides, and LDL cholesterol, while increasing (the "good") HDL cholesterol by 2 to 3 mg/dL. These results are more significant compared with placebo or lifestyle interventions. In another meta-analysis, berberine alone was as effective as simvastatin (the drug). The berberine dosage used in these studies was 500 mg twice daily, or 200 to 500 mg three times daily for 6 to 24 months. Berberine has also been studied in combination with other supplements. Taking a combined product containing 500 mg of berberine, 10 mg of policosanol, and 200 mg of red yeast rice per day for up to 12 months reduces total cholesterol and LDL levels compared with placebo or ezetimibe 10 mg. Daily intake of another combination product containing berberine, red yeast rice, policosanol, folic acid, coenzyme Q10 and astaxanthin, for up to 12 months, reduces total cholesterol by 10 to 13% and LDL cholesterol by 14 to 21%, and increases HDL cholesterol by 4 to 5% compared with baseline or placebo. These effects are comparable to those observed with pravastatin 10 mg per day. It is possible that the majority of the therapeutic effect is due to an ingredient in red yeast rice (monacolin K) that is identical to lovastatin.
Posologie
Oral
500 - 1500 mg
Synergies
Nutraceutical pill containing berberine versus ezetimibe on plasma lipid profile in hypercholesterolemic subjects and its additive effect in patients with familial hypercholesterolemia on stable cholesterol-lowering treatment
The effects of berberine on blood lipids: a systematic review and meta-analysis of randomized controlled trials
Nutraceutical approach to moderate cardiometabolic risk: results of a randomized, double-blind and crossover study with Armolipid Plus
Efficacy and Safety of Berberine Alone or Combined with Statins for the Treatment of Hyperlipidemia: A Systematic Review and Meta-Analysis of Randomized Controlled Clinical Trials
Long-term effects of nutraceuticals (berberine, red yeast rice, policosanol) in elderly hypercholesterolemic patients
Meta-analysis of the effect and safety of berberine in the treatment of type 2 diabetes mellitus, hyperlipidemia and hypertension
Efficacy and Safety of Berberine for Dyslipidemias: A Systematic Review and Meta-Analysis of Randomized Clinical Trials
Effects of a nutraceutical combination (berberine, red yeast rice and policosanols) on lipid levels and endothelial function: randomized, double-blind, placebo-controlled study
Effects of a nutraceutical combination containing berberine (BRB), policosanol, and red yeast rice (RYR) on lipid profile in hypercholesterolemic patients: A meta-analysis of randomized controlled trials
Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins
Polycystic ovary syndrome ✪✪✪✪✪
Clinical research conducted in women with polycystic ovary syndrome (PCOS) and insulin resistance shows that taking 500 mg of berberine three times a day for 3 to 6 months before controlled ovarian stimulation for in vitro fertilization reduces fasting glucose, markers of insulin resistance, total cholesterol, low-density lipoprotein cholesterol (LDL), triglycerides, testosterone levels, and waist-to-hip ratio compared with placebo. It may also increase high-density lipoprotein cholesterol (good HDL cholesterol) and sex hormone–binding globulin (SHBG). Low concentrations of SHBG are indicators of insulin resistance, which is common in PCOS.nnThe effect of berberine on pregnancy and live birth rates in women with PCOS is unclear. One clinical trial shows that taking berberine 500 mg three times a day for three months before controlled ovarian stimulation nearly doubled the number of clinical pregnancies and live births compared with placebo. These effects are comparable to taking 500 mg of metformin three times a day for three months.
Posologie
Oral
1500 mg
The use of berberine for women with polycystic ovary syndrome undergoing IVF treatment
A clinical study on the short-term effect of berberine in comparison to metformin on the metabolic characteristics of women with polycystic ovary syndrome
Randomized controlled trial of letrozole, berberine, or a combination for infertility in the polycystic ovary syndrome
Metabolic syndrome ✪✪✪✪✪
A preliminary clinical study conducted in adults with metabolic syndrome shows that taking 500 mg of berberine hydrochloride three times daily before meals for 3 months reduces body mass index by 0.6 kg/m2, systolic blood pressure by 8 mmHg, triglycerides by 18 mg/dL and serum glucose levels by 2 mg/dL, and may also improve insulin sensitivity compared with baseline. The validity of these results is limited by the absence of a control group. Other still preliminary clinical research shows that taking a combination containing 500 mg of berberine, 200 mg of red yeast rice, 10 mg of policosanol, 0.2 mg of folic acid, 2 mg of coenzyme Q10 and 0.5 mg of astaxanthin per day for 18 weeks improves systolic blood pressure, left ventricular mass and flow-mediated dilation in patients with metabolic syndrome compared with the control group.
Posologie
Orally
1500 mg
Synergies
Effects of a nutraceutical combination on left ventricular remodeling and vasoreactivity in subjects with the metabolic syndrome
Effect of berberine administration on metabolic syndrome, insulin sensitivity, and insulin secretion
The effect of berberine supplementation on obesity parameters, inflammation and liver function enzymes: A systematic review and meta-analysis of randomized controlled trials
Helicobacter pylori infection ✪✪✪✪✪
Preliminary clinical research shows that, in people with duodenal ulcers associated with H. pylori, taking berberine at 300 mg three times a day for 6 weeks is more effective at eradicating H. pylori than taking ranitidine (drug) at 150 mg twice a day, but is less effective at promoting ulcer healing. Other preliminary research shows that taking berberine at 100 mg twice a day in combination with esomeprazole, clarithromycin, and amoxicillin for 14 days is not inferior to bismuth tartrate at 220 mg per day for eradication of H. pylori. Another open-label clinical study in patients infected with H. pylori shows that taking 300 mg of berberine three times a day with amoxicillin and 10 mg of rabeprazole for 14 days is not inferior to the quadruple therapy that includes amoxicillin, rabeprazole, clarithromycin, and bismuth tartrate. In addition, the berberine-containing triple therapy may be better tolerated than the quadruple therapy.
Posologie
Oral
900 mg
[Comparison of acid and Helicobacter pylori in ulcerogenesis of duodenal ulcer disease]
Efficacy and safety of triple therapy containing berberine hydrochloride, amoxicillin, and rabeprazole in the eradication of Helicobacter pylor
Liver disorders ✪✪✪✪✪
Preliminary clinical research shows that taking berberine at a dose of one gram per day for two months reduces blood glucose, triglycerides, and markers of liver injury, including aspartate aminotransferase (AST) and alanine aminotransferase (ALT), in subjects with type 2 diabetes and hepatitis B compared with the control group. Other preliminary clinical research shows that taking 600 mg of berberine twice daily for 12 weeks reduces blood lipids and markers of liver injury, including aspartate aminotransferase (AST) and alanine aminotransferase (ALT), compared with baseline values in patients with nonalcoholic fatty liver disease and type 2 diabetes. Other preliminary clinical research shows that taking 500 mg of berberine three times daily for 16 weeks reduces hepatic fat content by 21% compared with a lifestyle modification. Berberine also appears to reduce hepatic fat content, AST, and ALT similarly to pioglitazone (drug) 15 mg per day, while reducing body weight, body mass index, and total cholesterol to a greater extent than pioglitazone.
Posologie
Oral
1200 mg
[Research on therapeutic effect and hemorrheology change of berberine in new diagnosed patients with type 2 diabetes combining nonalcoholic fatty liver disease]
Efficacy of Berberine in Patients with Non-Alcoholic Fatty Liver Disease
Aphthous ulcers ✪✪✪✪✪
Clinical research shows that applying a gel containing berberine at 5 mg/g four times a day for 5 days can reduce pain, inflammation, and ulcer size by 30% compared with placebo in patients with recurrent minor aphthous ulcers.nn
Posologie
Buccal route
High blood pressure ✪✪✪✪✪
A meta-analysis shows that daily intake of 900 mg of berberine in combination with amlodipine (a medication) for 2 months reduces systolic blood pressure by 5 mmHg and diastolic blood pressure by 2 mmHg compared with amlodipine alone.nn
Posologie
Oral administration
900 mg
Properties
Hypoglycemic
The hypoglycemic effect of berberine has been attributed to its ability to increase the expression of insulin receptors in peripheral blood lymphocytes of patients with type 2 diabetes. In addition, in vitro and animal studies suggest that berberine increases the activity of AMP-activated protein kinase (AMPK), which may stimulate glucose uptake in skeletal muscle, increase fatty acid oxidation in adipose tissue, and reduce glucose production in the liver. Other in vivo animal studies suggest that berberine increases secretion of glucagon-like peptide-1 (GLP-1). GLP-1 is a hormone that plays a role in maintaining blood glucose control. nn
Usages associés
Anticancer
In vitro studies show that berberine can reduce tumor cell proliferation by inducing cell cycle arrest or causing apoptosis. Some studies suggest that berberine may also inhibit tumor cell progression by inhibiting the activity of arylamine N-acetyltransferase (an enzyme involved in resistance to anticancer drugs). Moreover, in vivo animal studies show that berberine can inhibit metastasis of lung cancer to lymph nodes. Other in vitro studies also show that berberine can inhibit metastasis of melanoma cells. In addition to its anticancer effects, berberine may enhance the effects of conventional anticancer treatments, including radiotherapy and chemotherapy, against certain types of cancer. Indeed, berberine increases the effectiveness of tamoxifen against breast cancer cells by inducing upregulation of the cyclin-dependent kinase inhibitor P21, which is involved in the growth and development of breast cancer and plays a role in tamoxifen resistance.
Cardiovascular
Berberine may be effective in congestive heart failure and arrhythmia, as it possesses positive inotropic, negative chronotropic, antiarrhythmic and vasodilatory properties.nnIn humans, berberine reduces myocardial injury and appears to have an antihypertensive, effect due to its ability to block alpha-adrenergic activity.nnOther in vivo animal studies suggest that berberine may reduce oxidative stress and vascular inflammation. nn
Usages associés
Anti-aging
Berberine helps reduce metabolic problems related to aging through its action on AMPK activation.nnIt is known that metabolic dysregulation can lead to cancer; it appears that berberine is also an excellent agent for fighting cancers. nnBerberine is particularly promising in several types of cancer, such as brain, breast, cervical, colon, liver, lymphoma, oral, and thyroid cancers.nnOne strategy to fight cancer cells is to deprive these cells of glucose. Berberine can help in this regard thanks to its hypoglycemic properties.nn
CANCER: A SIMPLE AND NON-TOXIC TREATMENT - Dr. Lauent Schwartz
Berberine ameliorates cellular senescence and extends the lifespan of mice via regulating p16 and cyclin protein expression
Anti-inflammatory
Two meta-analyses show that berberine may lead to a slight reduction in C-reactive protein levels, a marker of systemic inflammation. Evidence from animal research shows that berberine can reduce chemically induced swelling, probably by inhibiting the expression of various cytokines. Preliminary and human research suggests that berberine blocks the production of the pro-inflammatory cytokines interleukin-1 (IL-1) beta and tumor necrosis factor (TNF)-alpha, probably by blocking nuclear factor kappa B, the transcription factor responsible for regulating cytokine production. Consequently, berberine could be useful in the treatment of alcoholic liver disease, which is associated with increased levels of IL-1 beta and TNF-alpha. Berberine also appears to decrease the production of IL-8, which is involved in inflammatory processes. Preliminary research suggests that berberine selectively inhibits the expression of cyclooxygenase (COX)-2.nn
Effect of Berberine on C-reactive protein: A systematic review and meta-analysis of randomized controlled trials
Efficacy and safety of berberine for several cardiovascular diseases: A systematic review and meta-analysis of randomized controlled trials
Antimicrobial
Berberine has antimicrobial effects, including antibacterial and antifungal effects and some antimycobacterial and antiprotozoal activity. Berberine is active against Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Shigella boydii, Vibrio cholerae, Mycobacterium tuberculosis, Candida albicans, Candida tropicalis, Trichophyton mentagrophytes, Microsporum gypseum, Cryptococcus neoformans, Sporotrichum schenckii, Entamoeba histolytica, Giardia lamblia, Entamoeba histolytica, Trichomonas vaginalis, Helicobacter pylori, Clostridium perfringens, Clostridium paraputrificum, Aspergillus species, Leishmania donovani, and Plasmodium falciparum. Preliminary research suggests that berberine may inhibit bacterial sortase, a protein responsible for anchoring Gram-positive bacteria to cell membranes. nn
Usages associés
Hepatoprotective
Preliminary research suggests that berberine may protect the liver from toxins. In an animal model, berberine reduced liver injury induced by N-nitrosodiethylamine. Other animal studies show that berberine prevents increases in alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) when given prior to exposure to acetaminophen or carbon tetrachloride.nnOther animal studies suggest that berberine has anti-fibrotic effects and may increase the excretion of bilirubin by the liver. nn
Usages associés
Hormonal metabolism
In women with polycystic ovary syndrome, berberine has been shown to increase sex hormone-binding globulin levels and decrease the free androgen index.
Usages associés
Safe dosage
Adults 18 years and older: 900 mg - 1500 mg
The standard dose of berberine is 900 to 1500 mg per day, divided into three or four doses.nnBerberine should be taken with a meal, or shortly afterward, to take advantage of the postprandial peak in blood glucose and blood lipids. nn
Interactions
Médicaments
Cytochrome P450 2C9: moderate interaction
Preliminary clinical research shows that berberine may inhibit CYP2C9. Taking berberine with drugs metabolized by CYP2C9 could increase drug concentrations and raise the risk of adverse effects. Example: CYP2C9 is the enzyme that metabolizes coumarin anticoagulants such as acenocoumarol or warfarin.
Cyclosporine: strong interaction
Berberine may reduce the metabolism and increase serum levels of cyclosporine. Berberine can inhibit cytochrome P450 3A4 (CYP3A4), which metabolizes cyclosporine.
CYTOCHROME P450 2D6: moderate interaction
In vitro research and preliminary clinical data show that berberine may inhibit CYP2D6. Taking berberine together with drugs metabolized by CYP2D6 could increase drug concentrations and raise the risk of adverse effects. Example: codeine, which is metabolized to morphine, dextromethorphan, or antidepressants, antipsychotics, and beta-blockers.
Cytochrome P450 3A4: moderate interaction
In vitro studies and preliminary clinical research show that berberine moderately inhibits CYP3A4. Using berberine with drugs metabolized by CYP3A4 could increase drug concentrations and raise the risk of adverse effects. Example: cardiovascular drugs; antiarrhythmics: quinidine, lidocaine, amiodarone; statins: simvastatin, atorvastatin; calcium channel blockers: nifedipine, nitrendipine, nimodipine, amlodipine, felodipine, verapamil, diltiazem...
Dextromethorphan: moderate interaction
Preliminary clinical research shows that berberine may inhibit the activity of cytochrome P450 2D6 (CYP2D6) and reduce the metabolism of dextromethorphan. This may increase the side effects of dextromethorphan.
Midazolam: moderate interaction
Preliminary clinical research shows that berberine may inhibit the activity of cytochrome P450 3A4 (CYP3A4) and reduce the metabolism of midazolam.
Tacrolimus: weak interaction
Increased circulating tacrolimus levels after berberine administration, with increased renal toxicity of this drug.
Statins: weak interaction
Possible increase in statin concentrations.
Contraindications
Children up to 6 years: contraindicated
The use of oral berberine in newborns can be dangerous. Berberine can cause kernicterus (brain injury caused by deposition of unconjugated bilirubin in the basal ganglia and brainstem nuclei), particularly in premature newborns with hyperbilirubinemia. nn
Pregnant women: contraindicated
Berberine can cross the placenta and cause harm to the fetus. Kernicterus (brain damage caused by deposition of unconjugated bilirubin in the basal ganglia and brainstem nuclei) has developed in newborns exposed to berberine. In addition, berberine may stimulate uterine contractions.
Breastfeeding: contraindicated
Berberine can pass into breast milk.
