Dataset Information

Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin.

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.

SUBMITTER: Chen CH

PROVIDER: S-EPMC3513969 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature

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Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin.

Chen Chia-Hao CH Uang Yow-Shieng YS Wang Shang-Ta ST Yang Jyh-Chin JC Lin Chun-Jung CJ

Evidence-based complementary and alternative medicine : eCAM 20121114

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 ...[more]

PMID: 23227093

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Project description:While several studies have demonstrated the preventive and therapeutic effects of red yeast rice (RYR), a traditional Chinese medicine, on carotid atherosclerosis through the reduction of low-density lipoprotein cholesterol (LDL-C) level and other risk factors, the evidence remains inconsistent. This study aimed to further evaluate the effects of RYR in carotid atherosclerosis. Several databases were searched for original trials of RYR for the treatment of carotid atherosclerosis that reported plaque indicators. Carotid plaque area (AREA), carotid plaque score (SCORE), and intima-media thickness (IMT) were set as the primary outcomes, while lipid profile and safety indicators were set as the secondary outcomes. Meta-analyses were performed on the randomized controlled trials (RCTs) using Comprehensive Meta-analysis software. Heterogeneity was evaluated using the I 2 index and Q statistic. Subgroup, sensitivity, and dose-effect analyses were conducted. Twenty RCTs with 2217 patients were included. Compared to the control group, AREA (SMD = -0.855, 95%CI: -1.259 to -0.451, p < 0.001), IMT (SMD = -0.588, 95%CI: -0.792 to -0.384, p < 0.001), SCORE (SMD = -0.708, 95%CI: -1.135 to -0.282, p = 0.001), LDL-C (SMD = -0.938, 95%CI: -1.375 to -0.502, p < 0.001), triglyceride (SMD = -0.766, 95%CI: -0.980 to -0.551, p < 0.001), and total cholesterol (SMD = -0.858, 95%CI: -1.254 to -0.462, p < 0.001) were significantly decreased and HDL-C (SMD = 0.389, 95%CI: 0.044-0.733, p = 0.027) was significantly increased following RYR therapy. The indicators for safety were not significant and did not differ between the two groups (p > 0.050). Heterogeneities mainly existed for the treatment time or control group setting. Most results showed no changes in the sensitivity analysis. Dose-effect relationships were observed for all indicators except for TC and HDL-C. We concluded that RYR therapy showed considerable efficacy and an acceptable safety profile for the treatment of carotid atherosclerosis in the Chinese population.

Project description:Background: RYR is a commonly used lipid-lowering dietary supplements in Asian and European countries, showing considerable benefits and low toxicity. This quantitative study aims to present high-quality evidence regarding the efficacy and safety of RYR in treating hyperlipidemia, in order to promote its clinical application. Methods: PubMed, embase, and Cochrane Central Register of Controlled Trials databases were systematically searched, and high-quality randomized controlled trials comparing RYR with non-RYR interventions were included. RevMan5.3 software was used to conduct the meta-analysis. Results: A total of 1,012 individuals participated in this study (481 in the experimental and 531 in the control group). In comparison to statins, RYR was more effective in lowering TG (MD, -19.90; 95% CI, -32.22 to -7.58; p = 0.002), comparable in lowering LDL-C and elevating HDL-C, and less effective in lowering TC (MD, 12.24; 95% CI, 2.19 to 22.29; p = 0.02). Compared with nutraceutical, RYR significantly reduced TC (MD, -17.80; 95% CI, -27.12 to -8.48; p = 0.0002) and LDL-C (MD, -14.40; 95% CI, -22.71 to -6.09; p = 0.0007), and elevated HDL-C (MD, 7.60; 95% CI, 4.33 to 10.87; p < 0.00001). Moreover, RYR effectively synergized nutraceutical to further reduce TC (MD, -31.10; 95% CI, -38.83 to -23.36; p < 0.00001), LDL-C (MD, -27.91; 95% CI, -36.58 to -19.24; p < 0.00001), and TG (MD, -26.32; 95% CI, -34.05 to -18.59; p < 0.00001). Additionally, RYR significantly reduced apoB (MD, -27.98; 95% CI, -35.51 to -20.45; p < 0.00001) and, whether alone or in combination, did not increase the risk of adverse events in patients with hyperlipidemia. Conclusion: RYR at 200-4800 mg daily appears to be a safe and effective treatment for hyperlipidemia, effectively regulating blood lipid levels with an exceptional impact on TG. Looking forward, high-quality clinical trials with longer observation periods are required to evaluate the efficacy and safety of RYR as a long-term medication. Systematic Review Registration: (https://www.crd.york.ac.uk/PROSPERO/), identifier (CRD4202128450).

Dataset Information

Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin.

Publications

Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin.

Similar Datasets

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