Statin type medications are known for their powerful effect on lowering LDL. Fibrates are specifically effective in lowering triglycerides. But neither have much an effect on the HDL. Raising HDL is of benefit in lowering the risk of heart disease. The cholesterol lowering effect of niacin, actually vitamin B-3, was first reported in 1955. As a general cholesterol drug, niacin has it all. In doses well above the vitamin requirement (about 50 mg per day), niacin can lower LDL and lower TG, but in particular it increases the HDL more than any other drug. Given in combination with a statin, niacin can lower the LDL more than any other drug combination.
Thus, you may prescribe niacin specifically to help increase HDL as well as lower the LDL (“up with the good and down with the bad”). The mechanism of action for niacin is not well understood but it may inhibit the release of free fatty acids from adipose tissue and thus increase the production of an enzyme called lipoprotein lipase; this in turn likely increases the rate of TG removal from the blood. Niacin has also been shown to reduce the synthesis of LDL in the liver. Indirectly, by increasing the amount of HDL, its action in what is called “reverse cholesterol transport” actually enhances the return of LDL to the liver and out of the circulation.
1. Common Names: there are a number of niacin preparation – so called “slo-niacin” has been questioned to be of any value in lowering cholesterols; however, the other preparations do have the desired therapeutic effect. There is immediate release niacin, extended release niacin, and (in prescription form only and the most effective) sustained release niacin (Niaspan).
2. Effect on Cholesterols: decrease LDL 5%-25%, raise HDL 15%-35%, decrease TG 20%-50% - the effect on TG is enhanced on a low carbohydrate type, weight loss diet; however, be aware that since niacin (except for Niaspan) is available from many sources including the internet and the health food store (actually a “nutraceutical” rather than a “pharmaceutical” and thus not strictly regulated) you may not always get what you pay for – so choose wisely; Niaspan, made by KOS Pharmaceutical on the other hand is strictly regulated as required by law.
3. Side Effects: the most common is flushing (potentially relieved by taking an aspirin 30 minutes before the dose) and gastrointestinal upset (can be reduced by taking dose with a low-fat snack such as yogurt); studies do indicate that niacin may increase blood sugar, but on the other hand it is a very useful medication in diabetics; niacin can increase the potential for gout and has a small risk of causing increases in liver enzymes, especially when combined with statins.
4. Usage: the frequency of dosing depends on the preparation – the immediate release and extended release niacin are taken generally twice per day; Niaspan is taken once per day.
5. Contraindications: an absolute contraindication is chronic liver disease; relative contraindications are gout, diabetes, and ulcer disease; liver blood tests should be monitored especially if also taking statin type medications.
Monday, August 3, 2009
Red Yeast Rice Reduces LDL-Cholesterol Levels in Statin-Intolerant Patients
According to the results of a new study, the use of red yeast rice and a therapeutic lifestyle change significantly reduced LDL-cholesterol levels in statin-intolerant patients with dyslipidemia and may provide a future treatment alternative for these difficult-to-treat patients. The results of the study are published in the June 16, 2009 issue of the Annals of Internal Medicine. "If properly regulated, I would say it's time that we began using red yeast rice in these statin-intolerant patients," said lead investigator Dr David Becker (Chestnut Hill Hospital, Flourtown, PA).
Extracts of red yeast rice have been widely used in China for therapy in patients with circulatory and digestive disorders for centuries, and preparations of red yeast rice have been shown to lower plasma LDL levels. Lovastatin occurs naturally in certain forms of red yeast rice that are made when the rice is cultivated with the mold Monascus purpureus. Red yeast rice is readily available in health food stores and over the internet, with US sales of $17 million in 2006.
In this study, 62 patients with dyslipidemia and a history of stopping statin therapy due to myalgias were randomized to receive 1800 mg of red yeast rice or placebo twice daily for 24 weeks. All patients were concomitantly enrolled in a 12-week therapeutic lifestyle-change program that included eating a Mediterranean-based diet, an exercise program, and relaxation techniques. The mean number of statins tried before the intervention was two.
After 12 weeks of treatment, LDL- and total-cholesterol levels were significantly lower in the red-yeast-rice group when compared with the placebo-treated patients. HDL-cholesterol levels were unchanged with treatment, and triglyceride levels were not significantly different between treatment arms. LDL- and HDL-cholesterol levels increased slightly from weeks 12 to 24, likely because the lifestyle intervention program ended and adherence to therapy declined, note investigators.
"The traditional approach among cardiologists is to patiently, or not so patiently, try one statin after another until they find a drug they can tolerate, because we know that they have to take this medication." said Becker. In the study, just two patients developed persistent intolerable myalgias. Becker noted that when patients develop myalgias with one statin, 40% to 60% typically end up stopping a second or third statin. Pain scores, derived from a self-administered questionnaire, were similar in both treatment arms at 12 and 24 weeks.
Becker noted that the dose of red yeast rice used in the study is equivalent to a daily lovastatin dose of just 6 mg, much less than established therapeutic doses of 20 mg to 40 mg, and that the amount of LDL lowering observed in the trial is disproportionate to such a low dose. Asked why red yeast rice was so well tolerated and yet so effective, Becker said that red yeast rice contains monacolin K, which is the naturally occurring lovastatin, but also numerous other monacolins that might work to lower LDL-cholesterol levels without causing recurrent muscle pain.
Investigators urged caution about moving these results into clinical practice, however, specifically pointing out that while the chemical composition of red yeast rice was known and controlled in this study, there is a lack of consistency between different manufacturers and an ongoing need for the Food and Drug Administration to better regulate this popular dietary supplement.
Extracts of red yeast rice have been widely used in China for therapy in patients with circulatory and digestive disorders for centuries, and preparations of red yeast rice have been shown to lower plasma LDL levels. Lovastatin occurs naturally in certain forms of red yeast rice that are made when the rice is cultivated with the mold Monascus purpureus. Red yeast rice is readily available in health food stores and over the internet, with US sales of $17 million in 2006.
In this study, 62 patients with dyslipidemia and a history of stopping statin therapy due to myalgias were randomized to receive 1800 mg of red yeast rice or placebo twice daily for 24 weeks. All patients were concomitantly enrolled in a 12-week therapeutic lifestyle-change program that included eating a Mediterranean-based diet, an exercise program, and relaxation techniques. The mean number of statins tried before the intervention was two.
After 12 weeks of treatment, LDL- and total-cholesterol levels were significantly lower in the red-yeast-rice group when compared with the placebo-treated patients. HDL-cholesterol levels were unchanged with treatment, and triglyceride levels were not significantly different between treatment arms. LDL- and HDL-cholesterol levels increased slightly from weeks 12 to 24, likely because the lifestyle intervention program ended and adherence to therapy declined, note investigators.
"The traditional approach among cardiologists is to patiently, or not so patiently, try one statin after another until they find a drug they can tolerate, because we know that they have to take this medication." said Becker. In the study, just two patients developed persistent intolerable myalgias. Becker noted that when patients develop myalgias with one statin, 40% to 60% typically end up stopping a second or third statin. Pain scores, derived from a self-administered questionnaire, were similar in both treatment arms at 12 and 24 weeks.
Becker noted that the dose of red yeast rice used in the study is equivalent to a daily lovastatin dose of just 6 mg, much less than established therapeutic doses of 20 mg to 40 mg, and that the amount of LDL lowering observed in the trial is disproportionate to such a low dose. Asked why red yeast rice was so well tolerated and yet so effective, Becker said that red yeast rice contains monacolin K, which is the naturally occurring lovastatin, but also numerous other monacolins that might work to lower LDL-cholesterol levels without causing recurrent muscle pain.
Investigators urged caution about moving these results into clinical practice, however, specifically pointing out that while the chemical composition of red yeast rice was known and controlled in this study, there is a lack of consistency between different manufacturers and an ongoing need for the Food and Drug Administration to better regulate this popular dietary supplement.
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