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Member Forum >> Heart Health Forum >> Berberine
 Berberine
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Posted: 12/9/2010 5:57:14 PM
 
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I thought I would start Building a thread on Berberine.  

There are some negative effects but their are also postive reports of Berberine.

I thought I would take a look at this HB

Feedback Welcomed

Abstract

OBJECTIVE: To study the effects of berberine (BBR) on the blood concentration and pharmacokinetics of cyclosporin A (CsA) in renal-transplant recipients.

METHODS: In a randomized and controlled clinical trial, 52 renal-transplant recipients were treated with CsA and 0.2 g BBR three times daily for 3 months, while another 52 subjects received CsA without BBR co-administration. Blood trough concentration of CsA and biochemistry indexes for hepatic and renal functions were determined. For the pharmacokinetic study, six renal-transplant recipients were included with a 3-mg/kg dosage of CsA twice daily before and after oral co-administration of 0.2 g BBR three times daily for 12 days.

RESULTS: The trough blood concentrations and the ratios of concentration/dose of CsA in the BBR-treated group increased by 88.9% and 98.4%, respectively, compared with those at baseline (P < 0.05). As for the BBR-free group, they rose by 64.5% and 69.4%, respectively, relative to those at baseline (P < 0.01). Nevertheless, the final blood concentrations and the ratios of concentration/dose of CsA in BBR-treated patients were still 29.3% and 27.8%, respectively, higher than those in BBR-free patients (P < 0.05). No significant effects on liver or renal functions were observed under coadministration of BBR. After co-administration of BBR in six patients for 12 days, the mean AUC of CsA was increased by 34.5% (P < 0.05). The mean time taken to reach the peak blood concentration (t(max)) and the mean half-life (t(1/2)) of CsA were increased by 1.7 h and 2.7 h, respectively (P < 0.05). The average percentage increases in the steady-state drug concentration (Css) and minimum blood concentration (Cmin) were 34.5% and 88.3%, respectively (P < 0.05). In addition, the average percentage decrease in CL/F was 40.4% (P < 0.05) and the peak-to-through fluctuation index was significantly reduced (P < 0.01).

CONCLUSION: The BBR can markedly elevate the blood concentration of CsA in renal-transplant recipients in both clinical and pharmacokinetic studies. This combination may allow a reduction of the CsA dosage. The mechanism for this interaction is most likely explained by inhibition of CYP3A4 by BBR in the liver and/or sm
http://www.ncbi.nlm.nih.gov/pubmed/16133554?dopt=Abstract


Methods Find Exp Clin Pharmacol. 2006 Jan-Feb;28(1):25-9.

The effects of berberine on the pharmacokinetics of cyclosporin A in healthy volunteers.

Xin HW, Wu XC, Li Q, Yu AR, Zhong MY, Liu YY.

Department of Clinical Pharmacology, Wuhan General Hospital, Wuhan, People's Republic of China.

Abstract

The effects of berberine (BBR) on the pharmacokinetics of ciclosporin A (CsA) were examined in healthy volunteers. Six healthy male volunteers were orally treated with 0.3 g BBR, twice daily for 10 days. Pharmacokinetic investigations on CsA at 6 mg/kg were done both before and at the end of the BBR treatment period. Another six healthy male volunteers were involved in the pharmacokinetic study with 3 mg CsA/kg, in which the subjects orally received the second single dose of 3 mg CsA/kg, followed by a single oral dose of 0.3 g BBR. The blood CsA concentrations were determined by fluorescence polarization immunoassay. In the pharmacokinetic study with 6 mg CsA/kg, BBR caused no significant changes in the pharmacokinetic parameters of CsA. However, in the trial with 3 mg CsA/kg, the average percentage increase in area under the blood concentration-time curve of CsA was 19.2% (P < 0.05) and the mean C12 increased to 123 microg/l from 104 microg/l (P < 0.05), without altering elimination half-life (t(1/2)), maximum blood drug concentration (Cmax), time to Cmax (tmax), apparent oral clearance (CL/F). The present results suggest that BBR can increase the oral bioavailability of CsA at the dosage of 3 mg/kg. The BBR-mediated increase in CsA bioavailability may be partly attributed to a decrease in liver and/or intestinal metabolism through the inhibition of CYP3A4 in the liver and/or gut wall. The BBR-induced increase in emptying time of stomach and small intestine might be another reason for the increase in CsA bioavailability. However, the speculation should be proved by further investigation.

2006 Prous Science.

http://www.ncbi.nlm.nih.gov/pubmed/16541194


Phytother Res. 2009 Nov;23(11):1553-8.

Effect of berberine on the pharmacokinetics of substrates of CYP3A and P-gp.

Qiu W, Jiang XH, Liu CX, Ju Y, Jin JX.

Department of Clinical Pharmacy, West China School of Pharmacy, Sichuan University, No. 17, Section 3, Renmin South Road, Chengdu 610041, China.

Abstract

The in vivo effects of berberine (BBR), the widely used bioactive herbal ingredient from many traditional Chinese medicinal herbs, on the pharmacokinetics of carbamazepine (CBZ, a substrate of CYP3A) and its metabolite carbamazepine 10,11-epoxide (ECBZ), digoxin (DIG, a substrate of P-gp) and cyclosporine A (CsA, a dual substrate of CYP3A and P-gp) were evaluated in rats. After a 2-week pretreatment with BBR, the pharmacokinetic parameters of i.g. administered CBZ and ECBZ were not significantly altered. The pharmacokinetics of i.v. administered DIG was not modified by single and 2-week pretreatments with BBR, but a dose-dependent increase in AUC and C(max) was observed in the i.g. administered DIG parameters in rats. The AUCs of DIG with BBR (30 mg/kg, 100 mg/kg) were 133%, 170% (single) and 123%, 169% (2-week) of control, respectively. The AUC and C(max) of i.g. administered CsA with a 2-week pretreatment with BBR increased by 62% and 43% (BBR 30 mg/kg, p < 0.05), 96% and 60% (BBR 100 mg/kg, p < 0.01), compared with the control. In conclusion, berberine produced a dose-dependent increased bioavailability of digoxin and cyclosporine A by inhibition of intestinal P-gp. No significant changes in CYP3A activity by berberine were observed.

PMID: 19370549 [PubMed - indexed for MEDLINE]


http://www.ncbi.nlm.nih.gov/pubmed/19370549

Berberine benefit, side effects, by Ray Sahelian, M.D. Benefit of berberine supplement hydrochloride sulfate hcl
Role in diabetes, cholesterol and other medical conditions

Berberine is a plant alkaloid isolated from the roots and bark of several herbs. Some of these herbs include:

Barberry (Berberis vulgaris), Berberis integerrima. Berbamine and berberine are found in the plant barberry.
Coptis chinensis or Berberis aristata
Goldenseal (Hydrastis canadensis)
Oregon Grape (Berberis aquifolium)
Phellodendron Amurense
Yerba mansa (Anemopsis californica). 

The berberine alkaloid can be found in the roots, rhizomes, stem, and bark of the plants. Berberine-containing plants are used medicinally in many traditional medical systems, including Ayurvedic herbal and Chinese herbal medicine.

Coptis chinensis rhizome -- Golden Thread -- Huang Lian -- Intense yellow color most likely due to high content of berberine, which is very bitter in taste.

Berberine potential benefits
Some people claim berberine is useful for fungal, candida, yeast, parasites, bacterial and viral infections. Berberine extracts and decoctions have demonstrated antimicrobial activity against a variety of organisms including bacteria, viruses, fungi, protozoans, helminths, and chlamydia. Currently, the predominant clinical uses of berberine include bacterial diarrhea, intestinal parasite infections, and ocular trachoma infections.
   Berberine has been tested in diabetes, prostate cancer, cardiac arrhythmia and leukemia.

Berberine and Diabetes
A collaboration between Chinese, Korean, and Australian scientists at Sydney's Garvan Institute indicates berberine could be helpful. They say "Our studies in animal models of diabetes show that berberine acts in part by activating an enzyme in the muscle and liver that is involved in improving sensitivity of the tissue to insulin. This in turn helps lower blood sugar levels. In addition, it seems berberine can help reduce body weight". "Berberine has been used for decades, if not centuries, with few reported side effects. Given the limitations of existing medicines we are excited to have evidence that berberine may be a helpful new treatment for type 2 diabetes; however, despite its widespread use in traditional medicine practices, it will still have to be evaluated properly following the defined clinical trials process", said Professor James, head of the Garvan's Diabetes & Obesity Research Program and co-author of the Diabetes paper.

Berberine, blood sugar, cholesterol, and blood pressure
Berberine may be helpful in maintaining healthy blood sugar and cholesterol levels in those with type 2 diabetes. Dr. Guang Ning, of Shanghai Jiao Tong University School of Medicine in Shanghai and colleagues randomized 116 diabetes patients to receive one gram of berberine daily or placebo for 3 months. Average hemoglobin A1C -- a measure of long-term blood sugar control -- dropped from 7.5 percent to 6.6 percent in those taking berberine supplements. Patients taking berberine also showed significant reductions in total and "bad" LDL cholesterol. Blood pressure also fell in patients taking berberine. Patients on berberine lost 2.3 kilograms (5.1 pounds), on average, compared to 1.3 kilograms (2.9 pounds) for the placebo group. Patients taking berberine were more likely to have a side effect of constipation, and two patients in the berberine group had their dosage reduced for this reason. Journal of Clinical Endocrinology and Metabolism, July 2008.

Berberine Research study
Berberine, a natural product, induces G1-phase cell cycle arrest and caspase-3-dependent apoptosis in human prostate carcinoma cells.
Mol Cancer Ther. 2006 Feb;5(2):296-308. Department of Dermatology, University of Alabama at Birmingham, Volker Hall 557, 1670 University Boulevard, Birmingham, AL
Berberine, a naturally occurring isoquinoline alkaloid, has been shown to possess anti-inflammatory and antitumor properties in some in vitro systems. Here, we report that in vitro treatment of androgen-insensitive (DU145 and PC-3) and androgen-sensitive (LNCaP) prostate cancer cells with berberine inhibited cell proliferation and induced cell death in a dose-dependent and time-dependent manner. The effectiveness of berberine in checking the growth of androgen-insensitive, as well as androgen-sensitive, prostate cancer cells without affecting the growth of normal prostate epithelial cells indicates that it may be a promising candidate for prostate cancer therapy.

Antimicrobial activity of berberine alone and in combination with ampicillin or oxacillin against methicillin-resistant Staphylococcus aureus.
J Med Food. 2005 Winter;8(4):454-61. Department of Food and Nutrition, Kunsan National University, Kunsan.
Methicillin-resistant Staphylococcus aureus (MRSA) bacteria have been responsible for substantial morbidity and mortality in hospitals because they usually have multidrug resistance. Some natural products are candidates as new antibiotic substances. In the present study, we investigated the antimicrobial activity of berberine, the main antibacterial substance of Coptidis rhizoma (Coptis chinensis Franch) and Phellodendri cortex (Phellodendron amurense Ruprecht), against clinical isolates of MRSA, and the effects of berberine on the adhesion to MRSA and intracellular invasion into human gingival fibroblasts (HGFs). Berberine showed antimicrobial activity against all tested strains of MRSA. These results suggest that berberine may have antimicrobial activity and the potential to restore the effectiveness of beta-lactam antibiotics against MRSA, and inhibit the MRSA adhesion and intracellular invasion in HGFs.

Hepatobiliary excretion of berberine.
Drug Metab Dispos. 2004 Apr;32(4):405-12.
To investigate the detailed pharmacokinetics of berberine and its mechanisms of hepatobiliary excretion, an in vivo microdialysis coupled with high-performance liquid chromatography was performed. In the control group, rats received berberine alone; in the drug-treated group, 10 min before berberine administration, the rats were injected with cyclosporin A (CsA), a P-glycoprotein (P-gp) inhibitor; quinidine, both organic cation transport (OCT) and P-gp inhibitors; SKF-525A (proadifen), a cytochrome P450 inhibitor; and probenecid to inhibit the glucuronidation. The results indicate that berberine displays a linear pharmacokinetic phenomenon in the dosage range from 10 to 20 mg kg(-1), since a proportional increase in the area under the concentration-time curve (AUC) of berberine was observed in this dosage range. Moreover, berberine was processed through hepatobiliary excretion against a concentration gradient based on the bile-to-blood distribution ratio (AUC(bile)/AUC(blood)); the active berberine efflux might be affected by P-gp and OCT since coadministration of berberine and CsA or quinidine at the same dosage of 10 mg kg(-1) significantly decreased the berberine amount in bile. In addition, berberine was metabolized in the liver with phase I demethylation and phase II glucuronidation, as identified by liquid chromatography/tandem mass spectrometry. Also, the phase I metabolism of berberine was partially reduced by SKF-525A treatment, but the phase II glucuronidation of berberine was not obviously affected by probenecid under the present study design.

Cytotoxic effects of Coptis chinensis and Epimedium sagittatum extracts and their major constituents (berberine, coptisine and icariin) on hepatoma and leukemia cell growth.
Clin Exp Pharmacol Physiol. 2004 Jan-Feb;31(1-2):65-9.
The present study was conducted to evaluate the cytotoxic effects of Coptis chinensis and Epimedium sagittatum extracts and their major constituents on hepatoma and leukemia cells in vitro. Four human liver cancer cell lines, namely HepG2, Hep3B, SK-Hep1 and PLC/PRF/5, and four leukemia cell lines, namely K562, U937, P3H1 and Raji, were used in the present study. Of the two crude drugs, Coptis chinensis exhibited the strongest activity against SK-Hep1  and Raji cell lines. Icariin (the major compound of E. sagittatum) showed no inhibition of either the hepatoma or leukemia cell lines. The results of the present study suggest that the Coptis chinensis extract and its major constituents berberine and coptisine possess active antihepatoma and anti leukemia activities.

Effect of berberine on regression of pressure-overload induced cardiac hypertrophy in rats.
Am J Chin Med. 2002;30(4):589-99.
Berberine is the basic chemical component of a Chinese herb, Coptis chinensis Franch (coptis), considered to be useful in treating some diseases of the cardiovascular system, such as hypertension and chronic heart failure (CHF). In this study, we investigate the inhibitory effect of berberine on experimental cardiac hypertrophy, which is regarded as a risk factor of CHF and other heart diseases. Forty-two male SD rats were divided into four groups: age-matched control, aortic banding model, berberine-treated group and captopril-treated group. Cardiac hypertrophy was induced by suprarenal abdominal aorta constriction (banding). The drugs were orally administered for 8 weeks starting from 4 weeks after surgery at dosage of berberine 10 mg/kg and captopril 50 mg/kg. Blood pressure (BP) was measured four times during the period of the experiment, and hemodynamic parameters, cardiac index, cell size of left ventricular myocardium and total protein of left ventricular tissue were detected 8 weeks after treatment with drugs. The data from the present study showed that: The BP of the aorta banded rats was increased compared with those of the normal and the age-matched control rats, and berberine showed no significant effect on it. After 8 weeks of treatment with berberine, the elevated left ventricular end diastolic pressure (LVEDP) was slightly decreased compared with the aortic banded rats. Meanwhile, the maximum rates of contraction and relaxation (+/- dp/dtmax) was increased and the time to reach the point of maximum rate from beginning of contraction (t-dp/dt) was shortened, indicating that the functions of heart, both contraction and relaxation, were improved. Cardiac growth was inhibited by treatment with berberine. Both whole heart and left ventricular weight were notably decreased compared with the banded rats. The cell size of left ventricular myocardium was significantly reduced and the total protein of left ventricular tissue was slightly down-regulated by treatment with berberine. These data suggest that berberine can improve abnormal cardiac function and can prevent the development of left ventricular hypertrophy induced by pressure-overload. This indicates that it may have therapeutic potential in the treatment of CHF.

Efficacy and safety of berberine for congestive heart failure secondary to ischemic or idiopathic dilated cardiomyopathy.
Am J Cardiol. 2003 Jul 15;92(2):173-6.
This study was designed to assess the efficacy and safety of berberine for chronic congestive heart failure. One hundred fifty-six patients with CHF and >90 ventricular premature complexes (VPCs) and/or nonsustained ventricular tachycardia (VT) on 24-hour Holter monitoring were randomly divided into 2 groups. All patients were given conventional therapy for congestive heart failure, consisting of angiotensin-converting enzyme inhibitors, digoxin, diuretics, and nitrates. Patients in the treatment group (n = 79) were also given berberine 1.2 to 2.0 g/day. The remaining 77 patients were given placebo. Symptoms, a 6-minute walk test, left ventricular (LV) ejection fraction (EF), frequency and complexity of VPCs, and quality of life were assessed after 8 weeks of treatment and during a mean 24-month follow-up. After treatment with berberine, there was a significantly greater increase in LVEF, exercise capacity, improvement of the dyspnea-fatigue index, and a decrease of frequency and complexity of VPCs compared with the control group. There was a significant decrease in mortality in the berberine -treated patients during long-term follow-up (7 patients receiving treatment died vs 13 on placebo). Proarrhythmia was not observed, and there were no apparent side effects. Thus, berberine improved quality of life and decreased VPCs and mortality in patients with congestive heart failure.

Effect of berberine on bone mineral density in SAMP6 as a senile osteoporosis model.
Biol Pharm Bull. 2003 Jan;26(1):110-1.
The effects of berberine in senescence accelerated mice P6 (SAMP6) were investigated to learn whether the alkaloid affects bone mineral density (BMD). Oral administration of berberine (10 mg/kg/d) to male and female mice for 22 weeks resulted in an increase in BMD in both sexes. A decreased concentration of deoxypyridinoline (Dpd) in urine was only observed in female mice. There was no effect on body or tibia weight or on the concentration of procollagen type I carboxyterminal extension peptide (PICP) in serum.

A comparative study on the anti-inflammatory, antinociceptive and antipyretic effects of isoquinoline alkaloids from the roots of Turkish Berberis species.
Life Sci. 2002 Dec 27;72(6):645-57.
Roots and barks of various Berberis species are used as folk remedy for the treatment of various inflammatory diseases such as lumbago, rheumatism and to reduce fever. Six isoquinoline alkaloids namely berberine, berbamine, palmatine, oxyacanthine, magnoflorine, and columbamine were isolated as the main components of alkaloidal fraction from the roots of Turkish Berberis species and effects were studied using various in vivo models in mice. All alkaloids inhibited inflammations in varying degrees, among them berberine, berbamine and palmatine were shown to possess significant and dose-dependent inhibitory activity against serotonin-induced hind paw oedema both on oral and topical applications and acetic acid-induced increase in vascular permeability on oral administration. Moreover, these three alkaloids were also shown to possess dose-dependent antinociceptive activity, which assessed by using the model based on the inhibition of p-benzoquinone-induced writhing movements as well as antipyretic activity on FCA-induced increased rectal temperature on subacute administration. However, all alkaloids induced gastric lesions in varying degrees.

Inhibitory effects of berberine on IK1, IK, and HERG channels of cardiac myocytes.
Acta Pharmacol Sin. 2001 Feb;22(2):125-31.
To study the effects of berberine on inward rectifier potassium current (IK1) and outward delayed rectifier potassium current (IK) of guinea pig ventricular myocytes, and on human ether-a-go-go related gene (HERG) channel expressed in Xenopus oocytes. Berberine prolonged action potential duration (APD) and inhibited IK1 and IK in a concentration-dependent manner. Berberine 100 micromol/L increased APD90 from (450 +\- 48) ms to (888 +\- 90) ms, and inhibited IK1 by 65 %. Berberine 50 micromol/L inhibited IK by 57 %, IKtail by 53 %. Berberine produced a voltage-dependent block on IK that increased with stronger depolarization, and once all channels were activated, there was no further block at positive potentials. Berberine blocked the HERG channels potently with an IC50 value of approximately 75 micromol/L. This block was voltage-dependent, suggesting that it probably bind to either open or inactivated HERG channels. Berberine prolonged APD and possessed blocking effect on IK1, IK, and HERG channel expressed in Xenopus oocytes. The antiarrhythmic mechanism of berberine is related to its inhibitory effects on IK1, IK, and HERG channel.

Cardiovascular actions of berberine.
Cardiovasc Drug Rev. 2001 Fall;19(3):234-44.
Berberine, is an alkaloid from Hydrastis canadensis L., Chinese herb Huanglian, and many other plants. It is widely used in traditional Chinese medicine as an antimicrobial in the treatment of dysentery and infectious diarrhea. This manuscript describes cardiovascular effects of berberine and its derivatives, tetrahydroberberine and 8-oxoberberine. Berberine has positive inotropic, negative chronotropic, antiarrhythmic, and vasodilator properties. Both derivatives of berberine have antiarrhythmic activity. Some cardiovascular effects of berberine and its derivatives are attributed to the blockade of K+ channels (delayed rectifier and K(ATP)) and stimulation of Na+ -Ca(2+) exchanger. Berberine has been shown to prolong the duration of ventricular action potential. Its vasodilator activity has been attributed to multiple cellular mechanisms. The cardiovascular effects of berberine suggest its possible clinical usefulness in the treatment of arrhythmias and/or heart failure.

Effects of berberine of L- and T-type calcium channels in guinea pig ventricular myocytes.
Zhongguo Yao Li Xue Bao. 1997 Nov;18(6):515-8.
To study the effects of berberine on L and T-type channels in isolated guinea pig ventricular myocytes. Berberine possessed blocking effects on both L- and T-type calcium channels.


http://www.raysahelian.com/berberine.html

Decreased oral absorption of cyclosporine A after liver ischemia-reperfusion injury in rats: the contribution of CYP3A and P-glycoprotein to the first-pass metabolism in intestinal epithelial cells.

Ikemura K, Urano K, Matsuda H, Mizutani H, Iwamoto T, Okuda M.

Department of Clinical Pharmacy and Biopharmaceutics, Mie University Graduate School of Medicine, Mie, Japan.

Abstract

The bioavailability of orally administrated cyclosporine A (CsA) is poor and variable in liver transplantation recipients. Little information is available about the effect of liver ischemia-reperfusion (I/R) injury, which is associated with liver transplantation, on the intestinal first-pass metabolism of CsA. In the present study, we investigated the pharmacokinetics of CsA after liver I/R and assessed the effect of liver I/R via CYP3A and P-glycoprotein (P-gp) on its intestinal first-pass metabolism. When CsA alone was administrated orally, the area under the concentration-time curve (AUC) in the I/R rats was significantly decreased compared with that in the sham rats. On the other hand, there were no significant differences in the AUC between I/R and sham rats when CsA was administrated intravenously or orally with ketoconazole. After intraloop administration of CsA to the small intestine (upper, middle, and lower portions) of the I/R and sham rats, the AUC(0-15 min) in the upper intestine was significantly lower in the I/R rats than in the sham rats. CYP3A activity and the expression levels of P-gp in the upper intestine of the I/R rats were significantly higher than those of the sham rats. Our study clearly demonstrates for the first time that liver I/R decreases the oral bioavailability of CsA and that this is attributable principally to increased first-pass metabolism mediated by CYP3A and P-gp in the upper small intestine. The present findings provide useful information for the etiology of liver I/R injury and appropriate use of CsA after liver transplantation.

PMID: 18842703 [PubMed - indexed for MEDLINE]Free Article


http://www.ncbi.nlm.nih.gov/pubmed/18842703


TYP threads on berberine

www.trackyourplaque.com/forum/topics.aspx

http://www.trackyourplaque.com/forum/topics.aspx?ID=1094






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Posted: 12/10/2010 8:36:47 AM
 
I posted a comment in the general discussion diabetes/berberine thread.


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Posted: 12/10/2010 5:03:56 PM
 
Thank You Dr Jgoldstrich.
HB




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Posted: 11/19/2011 7:34:34 PM
 
General survey of postive effects of berberine.HB


http://www.life-enhancement.com/article_template.asp?ID=2484




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Posted: 11/27/2011 1:20:46 AM
 
Hmm sounds like something here might help me. Anyone here tried it or bought it even.HB did u ever use it?




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Posted: 11/27/2011 11:34:35 PM
 
So I am on crestor, bP meds, elavil 25 for sleep. Then Typ supplements so should be ok from what I read here.thanks for all the research you do and posting of articles, mucho gracious:)




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Posted: 2/25/2012 9:05:23 PM
 
In Canada anytime a supplement becomes meaningful and Joe Public uses it our gov interfers and soon it is Rx!




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Tags: Berberine,Imodium,Loperamide

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Posted: 5/18/2018 6:02:26 PM
 
What is the berberine for?


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Posted: 5/18/2018 8:53:06 PM
 
Thanks for the info..  A link would have been fine.. 

Is there any specific reason a Dr Is recommending it for your husband?


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