Red yeast rice for dyslipidemia in statin-intolerant patients: a randomized trial

Chestnut Hill Hospital, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania, USA.
Annals of internal medicine (Impact Factor: 16.1). 07/2009; 150(12):830-9, W147-9.
Source: PubMed

ABSTRACT Red yeast rice is an herbal supplement that decreases low-density lipoprotein (LDL) cholesterol level.
To evaluate the effectiveness and tolerability of red yeast rice and therapeutic lifestyle change to treat dyslipidemia in patients who cannot tolerate statin therapy.
Randomized, controlled trial.
Community-based cardiology practice.
62 patients with dyslipidemia and history of discontinuation of statin therapy due to myalgias.
Patients were assigned by random allocation software to receive red yeast rice, 1800 mg (31 patients), or placebo (31 patients) twice daily for 24 weeks. All patients were concomitantly enrolled in a 12-week therapeutic lifestyle change program.
Primary outcome was LDL cholesterol level, measured at baseline, week 12, and week 24. Secondary outcomes included total cholesterol, high-density lipoprotein (HDL) cholesterol, triglyceride, liver enzyme, and creatinine phosphokinase (CPK) levels; weight; and Brief Pain Inventory score.
In the red yeast rice group, LDL cholesterol decreased by 1.11 mmol/L (43 mg/dL) from baseline at week 12 and by 0.90 mmol/L (35 mg/dL) at week 24. In the placebo group, LDL cholesterol decreased by 0.28 mmol/L (11 mg/dL) at week 12 and by 0.39 mmol/L (15 mg/dL) at week 24. Low-density lipoprotein cholesterol level was significantly lower in the red yeast rice group than in the placebo group at both weeks 12 (P < 0.001) and 24 (P = 0.011). Significant treatment effects were also observed for total cholesterol level at weeks 12 (P < 0.001) and 24 (P = 0.016). Levels of HDL cholesterol, triglyceride, liver enzyme, or CPK; weight loss; and pain severity scores did not significantly differ between groups at either week 12 or week 24.
The study was small, was single-site, was of short duration, and focused on laboratory measures.
Red yeast rice and therapeutic lifestyle change decrease LDL cholesterol level without increasing CPK or pain levels and may be a treatment option for dyslipidemic patients who cannot tolerate statin therapy.

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    • "Several clinical trials have found that 5–6 mg/day of lovastatin in RYR has a comparable efficacy to 20–40 mg/day of pure lovastatin in lowering blood cholesterol (Heber et al., 1999; Becker et al., 2008, 2009) suggesting additive and/or synergistic pharmacological effects of RYR components. However, it is not clear whether, or how, RYR components increase the bioavailability of lovastatin, which, in turn, partly contributes to the cholesterol lowering effects of RYR. "
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    ABSTRACT: Lovastatin, categorized as a class II compound according to the Biopharmaceutics Classification System, is mainly responsible for the blood cholesterol lowering effect of red yeast rice (RYR). The aim of this study was to compare the dissolution rate, physical state, and oral bioavailability of lovastatin in three RYR products (LipoCol Forte, Cholestin, or Xuezhikang) to those of two lovastatin tablets (Mevacor or Lovasta). The results showed that the dissolution rate of lovastatin in various dissolution media in the registered RYR products was faster and higher than that of lovastatin in lovastatin tablets. Powder X-ray diffraction and differential scanning calorimetry patterns showed that the crystallinity of lovastatin was reduced in RYR products. In human studies, the AUC and C(max) values for both lovastatin and its active metabolite, lovastatin acid, were significant higher in volunteers receiving LipoCol Forte capsules or powder than in those receiving lovastatin tablets or powder. In addition, shorter and less variable T(max) values were observed in volunteers taking LipoCol Forte than in those taking lovastatin tablets. These findings suggest that the oral bioavailability of lovastatin is significantly improved in RYR products as a result of a higher dissolution rate and reduced crystallinity.
    International Journal of Pharmaceutics 01/2013; 444(1-2). DOI:10.1016/j.ijpharm.2013.01.028 · 3.79 Impact Factor
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    • "In addition, LipoCol Forte, with similar constituents to Xuezhikang , is a newly developed RYR product that is approved as a drug in Taiwan. Although RYR products have been demonstrated to be well tolerated [10] [11] [16] [17], consumption of RYR products has been associated with occurrence of myopathy, rhabdomyolysis , or hepatitis in several case reports [18] [19] [20] [21]. Nonetheless , it is noted that the occurrence of RYR-associated adverse reaction has usually been reported in patients with concomitant comedication [18] [19] [20]. "
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    ABSTRACT: Red yeast rice (RYR) can reduce cholesterol through its active component, lovastatin. This study was to investigate the pharmacokinetic properties of lovastatin in RYR products and potential RYR-drug interactions. Extracts of three registered RYR products (LipoCol Forte, Cholestin, and Xuezhikang) were more effective than pure lovastatin in inhibiting the activities of cytochrome P450 enzymes and P-glycoprotein. Among CYP450 enzymes, RYR showed the highest inhibition on CYP1A2 and CYP2C19, with comparable inhibitory potencies to the corresponding typical inhibitors. In healthy volunteers taking the RYR product LipoCol Forte, the pharmacokinetic properties of lovastatin and lovastatin acid were linear in the dose range of 1 to 4 capsules taken as a single dose and no significant accumulation was observed after multiple dosing. Concomitant use of one LipoCol Forte capsule with nifedipine did not change the pharmacokinetics of nifedipine. Yet, concomitant use of gemfibrozil with LipoCol Forte resulted in a significant increase in the plasma concentration of lovastatin acid. These findings suggest that the use of RYR products may not have effects on the pharmacokinetics of concomitant comedications despite their effects to inhibit the activities of CYP450 enzymes and P-gp, whereas gemfibrozil affects the pharmacokinetics of lovastatin acid when used concomitantly with RYR products.
    Evidence-based Complementary and Alternative Medicine 11/2012; 2012:127043. DOI:10.1155/2012/127043 · 1.88 Impact Factor
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    • "of 40 mg pravastatin and 4800 mg red yeast rice (equivalent to 10 mg monacolin K) in this group of patients [10]. Therefore, this " statin-intolerance " seems to be an effect of inadequate dosing. "
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    ABSTRACT: Red yeast rice (i.e., rice fermented with Monascus spp.) is currently sold via the Internet as a dietary supplement. Claims state that red yeast rice has the ability to lower blood cholesterol concentrations. The mechanism of action is well characterised because the red yeast rice constituent monacolin K is identical with lovastatin, an inhibitor of the hydroxymethylglutaryl-CoA (HMG-CoA) reductase that is used in many cholesterol-lowering medicinal products. The aim of this article is to evaluate the properties of red yeast rice products that are marketed via the Internet. Three out of five analyzed products may reach the daily dosage of 10 mg lovastatin, which is necessary for the substantiation of health claims on the maintenance of normal blood LDL-cholesterol levels as suggested by the Scientific Opinion of the European Food Safety Authority. 10 mg is also the starting dosage of medicinal lovastatin products on the German market. From a regulatory standpoint, red yeast rice products would rather have to be sold as medicinal products than as food supplements as they clearly exhibit a pharmacological action that is comparable to approved statin-containing medicinal products. This also implies potential adverse effects and interactions, about which the consumer is insufficiently informed in the case of food supplements. The lack of control over the Internet market is evidenced by the fact that four of the tested products were not marketable in conventional trade in Germany due to violations of labelling rules.
    Deutsche Lebensmittel-Rundschau: Zeitschrift für Lebensmittelkunde und Lebensmittelrecht 07/2012; 108(7):357-360. · 0.06 Impact Factor
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