Taxonomic class

Monascaceae

Common Trade Names

Cholestin

Common Forms

Available as a 600-mg capsule in the United States. In China, dried red yeast rice is either powdered (ZhiTai) or extracted with alcohol (XueZhiKang) .

Source

Red yeast rice is a traditional Chinese substance made by fermenting a particular strain of yeast, called Monascus purpureus, over rice. The red yeast rice is produced in China and imported by Pharmanex, Inc., for packaging into gelatin capsules in the United States.

Chemical Components

Red yeast rice contains 0.4% naturally occurring HMG-CoA reductase inhibitors. The most abundant HMG-CoA reductase inhibitor is mevinolin, or lovastatin. It also contains unsaturated fatty acids, including monounsaturated fatty acids, diene-, triene-, tetraene-, and pentaenefatty acids. Other components include amino acids, protein, saccharides, beta-sitosterol, campesterol, stignasterol, isoflavone, saponin, and other trace elements.

Actions

Red yeast rice has cholesterol-reducing properties. It contains lovastatin and related mevinic acid compounds that competitively inhibit 3­hydroA)-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase. This blocks the synthesis of cholesterol in the liver and results in decreased LDL, VLDL, and triglyceride levels. It also increases HDL levels.

Reported Uses

Red yeast rice has been used to maintain desirable cholesterol levels in healthy people and to reduce cholesterol levels in people with hypercholesterolemia. Chinese medicine uses this product for diarrhea and indigestion, for improving blood circulation, and for spleen and stomach health.

Animal and human studies to evaluate the effectiveness of red yeast rice in hypercholesterolemia have been performed primarily in China. Studies in rabbits and quail have demonstrated cholesterol lowering and decreased lipid accumulation in the liver with XueZhiKang . Clinical studies performed with several formulations of M. purpurpeus have also shown cholesterol-lowering effects. Studies conducted in the United States included appropriate diet instructions or surveys for the patients.

Dosage

Capsules: Two 600-mg capsules P.O. b.i.d.

Extract: 0.6 g P.O. b.i.d.

Each gram of Cholestin contains 4 mg of HMG-CoA reductase inhibitors: 2 mg as lovastatin, 1 mg as lovastatin acid, and 1 mg as a mixture of seven other statins. Therefore, the recommended dose of 1,200 mg b.i.d. would provide 7.2 mg oflovastatin and 2.4 mg of other statins . The product is standardized to contain 0.4% (9.6 mg) HMG-CoA reductase inhibitors and greater than or equal to ISO mg of unsaturated fatty acids per daily dosage.

Adverse Reactions

CNS: dizziness.

GI: bloating, flatulence, heartburn.

Other: anaphylaxis .

Interactions

Cytochrome P-450 inhibiting drugs: Increased serum lovastatin level and risk of adverse effects. Avoid administration with red yeast rice.

Food: Increased bioavailability of lovastatin. Red yeast rice may be taken with food.

Grapefruit juice: 15-fold increase in serum lovastatin levels; increased risk of adverse effects. Do not administer red yeast rice with grapefruit juice.

Levothyroxine: Concomitant use with lovastatin can cause thyroid function abnormalities. Avoid using together.

Other cholesterol-lowering drugs: Increased risk of adverse effects and

toxicity. Avoid administration with red yeast rice.

Contraindications and Precautions

Red yeast rice should be avoided in patients who are at risk for or who have active hepatic disease and in those with a history of hepatic disease. It is also contraindicated in people who consume more than two alcoholic beverages daily; in patients with a serious infection, disease, or physical disorder or who have had an organ transplant; and in anyone younger than age 20. Avoid use in female patients who are breast­feeding, pregnant, or planning to become pregnant.

Special Considerations

• Red yeast rice may be taken with food to minimize adverse GI effects.

Alert Anaphylaxis to red yeast rice has been reported.

• Natural constituents in red yeast rice (HMG-CoA reductase inhibitors) in much higher doses have been associated with some rare but serious adverse effects, including hepatic and skeletal muscle disease.

Elevated liver enzyme and creatine kinase levels can occur.

Points of Interest

• Cholestin is considered a dietary supplement.
• Red yeast rice has been used in China since A.D. 800 to make red rice wine, to preserve and enhance food, and as a medicinal substance.
• Written records from the Ming dynasty show that red yeast rice was believed to improve blood circulation and reduce clotting.

Commentary

Red yeast rice appears to be well tolerated and effective in lowering cholesterollevels. It is sold in the United States as a dietary supplement.

Until more clinical studies are performed, red yeast rice should be treated as an HMG-CoA reductase inhibitor. This includes potential adverse effects, drug interactions, and precautions associated with this drug class. Studies to evaluate the long-term safety and efficacy of this supplement in larger populations are needed.