Synonyms
Acetone, berberine,
barberry, benzophenanthridine alkaloid, berberin, berberin hydrochloride, berberine alkaloid, berberine bisulfate, berberine
chloride, berberine complex, berberine hydrochloride, berberine iodide, berberine
sulfate, berberine tannate,
Berberis aquifolium,
Berberis aristata,
Berberis vulgaris,
Coptis chinensis, coptis, goldenthread,
goldenseal,
Hydrastis canadensis, jiang tang san, Oregon grape, protoberberine, protoberberinium salts, tree
turmeric.
Background
Berberine is a bitter-tasting, yellow, plant alkaloid with a long
history of medicinal use in Chinese and Ayurvedic medicine. Berberine is
present in the roots, rhizomes and stem bark of various plants
including
Hydrastis canadensis (goldenseal),
Coptis chinensis (coptis or goldenthread),
Berberis aquifolium (Oregon grape),
Berberis vulgaris (barberry), and
Berberis aristata (tree turmeric). Berberine has also been used historically as a dye, due to its yellow color.
Clinical trials have been conducted using berberine. There is some evidence to support its use in the treatment of
trachomas (eye infections), bacterial diarrhea, and
leishmaniasis (
parasitic disease). Berberine has also shown antimicrobial activity against bacteria,
viruses, fungi, protozoans, helminths (
worms), and
chlamydia (
STD). Future clinical research is warranted in these areas, as well as
cardiovascular disease,
skin disorders, and
liver disorders.
Berberine has been shown to be safe in the majority of clinical
trials. However, there is a potential for interaction between berberine
and many prescription medications, and berberine should not be used by
pregnant or
breastfeeding women, due to potential for adverse effects in the newborn.
Evidence
DISCLAIMER:
These uses have been tested in humans or animals. Safety and
effectiveness have not always been proven. Some of these conditions are
potentially serious, and should be evaluated by a qualified healthcare
provider.
Heart failure:
Preliminary research suggests that berberine, in addition to a standard
prescription drug regimen for chronic congestive heart failure (
CHF),
may improve quality of life and heart function, and improve mortality.
Further research is necessary before a firm conclusion can be drawn in
this area.
Grade: B
Chloroquine-resistant malaria:
One trial has assessed the use of berberine in combination with
pyrimethamine in the treatment of chloroquine-resistant malaria. Well-designed clinical trials are still required in this field.
Grade: C
Diabetes (type 2):
Historically, berberine has been suggested to aid in glycemic
regulation. The safety and effectiveness of berberine for this
indication remains unclear. More research is needed in this area.
Grade: C
Glaucoma:
Preliminary study of berberine does not appear to reduce intraocular
pressure in patients with glaucoma. The safety and effectiveness of
berberine for this indication remains unclear. Additional study is
needed in this area.
Grade: C
H. pylori infection:
Berberine has been compared with antibacterial drugs and
ranitidine in stimulation of ulcer healing and
Helicobacter pylori clearance. Berberine was suggested to be less effective at ulcer healing than ranitidine, but potentially more effective at
Helicobacter pylori clearance. Additional study is needed in this area.
Grade: C
Hypercholesterolemia (high cholesterol):
Berberine may reduce
triglycerides, serum cholesterol, and
LDL cholesterol. Higher quality trials are needed before berberine's cholesterol-lowering effect can be established.
Grade: C
Infectious diarrhea:
Berberine has been evaluated as a treatment for infectious diarrhea,
including choleric diarrhea, although the data is conflicting.
Therefore, there is currently insufficient evidence regarding the
efficacy of berberine in the management of infectious diarrhea.
Grade: C
Parasitic infection (leishmania):
The benefits of berberine in the treatment of leishmaniasis are widely
accepted. Berberine is thought to be equally efficacious as the standard
drug treatment of cutaneous leishmaniasis, antimonite (sulfide
mineral),
although limited study of this treatment probably limits its widespread
use. Additional study is needed to confirm these results.
Grade: C
Thrombocytopenia (low platelet count):
Berberine has been shown to significantly increase platelet production
in individuals with thrombocytopenia both as monotherapy and adjunctive
therapy. Additional human study is needed to confirm these results.
Grade: C
Trachoma (eye disease):
Berberine has been found to possess antimicrobial properties, and there
is limited evidence of anti-inflammatory properties as well. Preliminary
evidence suggests that berberine eye preparations may be beneficial for
trachoma. However, the safety and efficacy of berberine for this
indication remains unclear.
Grade: C
Tradition
WARNING:
DISCLAIMER:
The below uses are based on tradition, scientific theories, or
limited research. They often have not been thoroughly tested in humans,
and safety and effectiveness have not always been proven. Some of these
conditions are potentially serious, and should be evaluated by a
qualified healthcare provider. There may be other proposed uses that are
not listed below.
Alcoholic liver disease, antibacterial,
anticonvulsant,
antifungal, anti-inflammatory, antimicrobial (typanosomes),
antioxidant,
antiviral,
arthritis, bile secretion,
burns, cancer,
cardiovascular disease, dental conditions (
root canal), dental hygiene, eye infections (general), fatigue, fever,
headaches,
high blood pressure,
immunostimulant,
irritable bowel syndrome (
IBS),
leukemia, leukopenia, liver disease (alcoholic),
osteoporosis, respiratory disorders,
sedative, skin infections,
urinary tract infection,
ventricular tachyarrhythmias, yeast infections.
Dosing
Adults (18 years and older)
A wide range of doses has been studied for berberine, although no
dose has been proven effective. Berberine is possibly safe when taken by
mouth in doses up to 2 grams daily for eight weeks. For
hypercholesterolemia (
high cholesterol), 0.5 gram of berberine twice daily for three months has been used. For infectious diarrhea, berberine
sulfate 400 milligrams as a single dose has been used. For
thrombocytopenia, berberine bisulfate 5 milligrams, three times daily (20 minutes before meals) for 15 days has been used.
As an injection into the vein, berberine has been infused at a rate
of 0.2 milligrams/kilogram per minute for 30 minutes. Injections should
only be given under the supervision of a qualified healthcare
professional, including a pharmacist.
For
trachoma, 0.2% berberine
eye drops have been studied for eight weeks.
Children (younger than 18 years)
There is no proven effective dose for berberine in children.
Nonetheless, berberine is possibly safe when used in otherwise healthy
children, as young as two months, at recommended doses for treatment of
diarrhea up to six days.
Safety
DISCLAIMER:
Many complementary techniques are practiced by healthcare
professionals with formal training, in accordance with the standards of
national organizations. However, this is not universally the case, and
adverse effects are possible. Due to limited research, in some cases
only limited safety information is available.
Allergies
Avoided in individuals with a known allergy or
hypersensitivity to berberine, to plants that contain berberine [
Hydrastis canadensis (
goldenseal),
Coptis chinensis (coptis or goldenthread),
Berberis aquifolium (Oregon grape),
Berberis vulgaris (
barberry), and
Berberis aristata (tree
turmeric)], or to members of the Berberidaceae family.
Allergic reactions have been reported, with symptoms of vomiting, itching, and a feeling of faintness.
Side Effects and Warnings
Berberine has been reported to cause nausea, vomiting,
hypertension (high blood pressure),
respiratory failure
and paresthesias (abnormal sensations such as numbness or tingling);
however, clinical evidence of such adverse effects is not prominent in
the literature. Rare adverse effects including headache, skin
irritation, facial flushing, headache, bradycardia (slowed heart rate)
have also been reported with the use of berberine. Use cautiously when
taking berberine for longer than eight weeks due to theoretical changes
in bacterial gut flora.
Use cautiously in individuals with
diabetes, as both human and animal studies indicate that berberine may decrease
blood sugar levels. Also use cautiously in individuals with hypotension (low blood pressure), as berberine may have antihypertensive effects.
Patients with cardiovascular disease should also use caution as
berberine has been associated with the development of ventricular
arrhythmias in subjects with
congestive heart failure.
Although not well studied in humans, berberine may also theoretically
cause delays in small intestinal transit time or increase the risk of
bleeding.
Berberine may cause abortion, eye or kidney irritation, nephritis
(inflamed kidneys), dyspnea (difficulty breathing), flu-like symptoms,
giddiness, lethargy, or liver toxicity.
Patients with leukopenia (abnormally low white blood cell count)
should use cautiously due to the potential for development of leukopenia
symptoms.
When injected under the skin, berberine may cause hyperpigmentation
in the arm. Use berberine cautiously in individuals with high exposure
to sunlight or artificial light due to potential for adverse
phototoxic reactions.
Avoid in newborns due to potential for increase in free bilirubin,
jaundice, and development of
kernicterus (brain damage caused by severe newborn jaundice). Use berberine cautiously in children due to a lack of safety information.
Pregnancy and Breastfeeding
Berberine is not recommended in
pregnant or
breastfeeding
women due to a lack of available scientific evidence. Although not well
studied in humans, berberine has been suggested to have anti-fertility,
abortifacient (
abortion inducing), and uterine stimulant activity.
Berberine may cause kernicterus (brain damage) when used in newborn jaundiced babies, such as
bilirubin encephalopathy (degenerative brain disease).
Interactions with Drugs
Berberine may counter or prevent irregular heartbeat. Caution is
advised when taking berberine with other agents that alter heart rate.
Berberine may decrease the efficacy of
tetracycline; in theory, berberine may decrease the efficacy of other agents with antibacterial activity.
Berberine bisulfate may stimulate platelet formation, and berberine
may have an antiheparin action. Thus, berberine may interact with
certain drugs that increase the risk of bleeding, and reduce their
effectiveness. Some examples include
aspirin,
anticoagulants ("
blood thinners") such as
warfarin (Coumadin®) or
heparin,
anti-platelet drugs such as
clopidogrel (Plavix®), and non-steroidal anti-inflammatory drugs (NSAIDS) such as
ibuprofen (Motrin®, Advil®) or
naproxen (Naprosyn®, Aleve®). However, berberine may be hepatoprotective (liver protective) when administered before toxic doses of
acetaminophen.
Berberine may lower
blood sugar levels. Caution is advised when using medications that may also lower blood sugar. Patients taking drugs for
diabetes by mouth or
insulin
should be monitored closely by a qualified healthcare professional,
including a pharmacist. Medication adjustments may be necessary. Berberine may decrease total and
LDL cholesterol, as well as
triglycerides. Caution is advised in patients taking any cholesterol-lowering agents.
There may be additive hypotensive (
blood pressure
lowering) effects and bradycardia (slowed heart rate) when combining
berberine with agents that lower blood pressure. Caution is advised.
Berberine may modulate the expression and function of PGP-170 in
hepatoma cells. In theory, berberine may interact with
antineoplastic agents.
Berberine and berberine
sulfate have anti-inflammatory effects and may interact with COX-2 inhibitors. COX-2 inhibitor drugs include
celecoxib (Celebrex®) and rofecoxib (Vioxx®).
Berberine may elevate the blood concentration of
cyclosporin A. Caution is advised.
Berberine may interfere with the way the body processes certain drugs
using the liver's "cytochrome P450" enzyme system. As a result, the
levels of these drugs may be increased in the blood, and may cause
increased effects or potentially serious adverse reactions. Patients
using any medications should check the package insert, and speak with a
qualified healthcare professional, including a pharmacist, about
possible interactions.
Although not well studied in humans, there may be a potential for synergism between berberine
chloride and
fluconazole.
Berberine and L-phenylephrine may have additive effects when
administered concurrently. Furthermore, berberine may reverse the
secretory properties of
neostigmine (Prostigmin®).
Berberine and 1,3-bis (2-chloroethyl)-1-nitosurea (BCNU) may have additive effects.
Berberine may increase sensitization to acetylcholine's hypotensive (blood pressure lowering) effects.
P-glycoprotein may contribute to the poor intestinal absorption of berberine.
It is been purported that berberine may have
sedative effects. Although human study is lacking, caution is advised.
Berberine may competitively inhibit the binding of
yohimbine
to platelets. Patients taking yohimbine should consult with a qualified
healthcare professional, including a pharmacist, to check for
interactions.
Interactions with Herbs and Dietary Supplements
Berberine may counter or prevent irregular heartbeat. Caution is advised when taking berberine with other
herbs that alter heart rate. Berberine may decrease the efficacy of tetracycline; thus, in theory,
berberine may decrease the efficacy of herbs with antibacterial
activity.
Berberine bisulfate may stimulate platelet formation, and berberine
may have an antiheparin action. Thus, berberine may interact with
certain herbs that increase the risk of bleeding and reduce their
effectiveness. Multiple cases of bleeding have been reported with the
use of
Ginkgo biloba, and fewer cases with
garlic and
saw palmetto. Numerous other agents may theoretically increase the risk of bleeding, although this has not been proven in most cases.
There may be additive hypotensive (blood pressure lowering) effects
and bradycardia (slowed heart rate) when combining berberine with herbs
that lower blood pressure. Caution is advised.
Berberine may lower blood sugar levels. Caution is advised when using herbs or supplements that may also lower blood sugar.
Blood glucose levels may require monitoring, and doses may need adjustment.
Berberine may decrease total and LDL cholesterol, as well as
triglycerides. Caution is advised in patients taking herbs or
supplements with cholesterol-lowering effects, such as
red yeast rice.
Concomitant use of berberine-containing herbs may increase the risk of berberine toxicity. Berberine-containing herbs include:
bloodroot,
goldenseal, celandine, Chinese
goldthread, goldthread, Oregon grape (
Mahonia species), amur cork tree, and Chinese corktree.
Berberine may interfere with the way the body processes certain herbs
or supplements using the liver's "cytochrome P450" enzyme system. As a
result, the levels of other herbs or supplements may become too high in
the blood. It may also alter the effects that other herbs or supplements
possibly have on the P450 system.
Although not well studied in humans, berberine may have sedative effects.
Based on clinical study, tyramine-containing foods, such as wine,
cheese, and chocolate, may have an interaction with berberine due to
berberine's effect on decreasing levels of tyramine.
Berberine may competitively inhibit the binding of yohimbine to
platelets. In addition, due to the antifertililty properties of
berberine, use of
yohimbe for
fertility may not be effective.
Berberine may decrease the metabolism of
vitamin B; therefore, the concomitant use of berberine with vitamin B should be avoided.
Source:
http://www.healthline.com/natstandardcontent/berberine#4