Statin Drugs
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Statin Drugs


The statin drugs, also known as HMG-CoA reductase inhibitors, are the most popular and powerful medications for improving cholesterol profile. They work by interfering with HMG-CoA reductase, an enzyme necessary for the body's manufacture of cholesterol. Drugs in this family include:

  • Atorvastatin calcium (Lipitor),
  • Fluvastatin (Lescol),
  • Lovastatin (Mevacor),
  • Pravastatin (Pravachol),
  • Simvastatin (Zocor),
  • Rosuvastatin (Crestor),
  • and others.

Chaparral, Comfrey, and Coltsfoot

Possible Harmful Interaction

The herb chaparral (Larrea tridentate or L. mexicana) has been promoted for use in arthritis, cancer, and various other conditions, but there is insufficient evidence supporting its effectiveness. There are, however, concerns about its apparent liver toxicity.

Several cases of chaparral-induced liver damage have been reported, some of them severe enough to require liver transplantation.1-6

Based on these reports, combining chaparral with other agents that are hard on the liver, such as statin drugs, may amplify the risk of potential liver problems.7 Other herbs that are toxic to the liver include comfrey (Symphytum officinale) and coltsfoot (Tussilago farfara).

Chinese Skullcap (Scutellaria baicalensis)

Possible Harmful Interaction

The herb Chinese skullcap contains the substance baicalin as one of its presumed major active ingredients. One study found evidence that consumption of baicalin might lower blood levels of statin drugs.34

St. John's Wort

Possible Harmful Interaction

The herb St. John’s wort, used to treat depression, may decrease blood levels of various drugs in the statin family, including simvastatin, lovastatin, and atorvastatin (but possibly not pravastatin).22 One study documented that when people taking atorvastatin for high cholesterol additionally took St. John’s wort, cholesterol levels promptly rose.33

Grapefruit Juice

Possible Harmful Interaction

Grapefruit juice impairs the body's normal breakdown of several drugs, including statins, allowing them to build up to potentially excessive levels in the blood.8 A recent study indicates that this effect can last for 3 days or more following the last glass of juice.9

Because this could increase the risk of serious drug side effects, if you take interacting statins, the safest approach is to avoid grapefruit juice altogether. Grapefruit juice may not affect fluvastatin or pravastatin because these drugs are broken down differently than other statins.10

Vitamin B3

Possible Benefits and Risks

Niacin (nicotinic acid) is vitamin B3. In high doses (often 1,500 mg daily or more), niacin is effective in lowering cholesterol levels. Its other form, niacinamide (nicotinamide), does not affect cholesterol.

Combining high-dose niacin with statin drugs further improves cholesterol profile by raising HDL (“good”) cholesterol.23,24,25 Unfortunately, there are real concerns that this combination therapy could cause a potentially fatal condition of muscle breakdown called rhabdomyolysis.

A growing body of evidence, however, suggests that the risk is relatively slight in individuals with healthy kidneys. Furthermore, even much lower doses of niacin than the usual dose given to improve cholesterol levels (100 mg versus 1,000 mg or more) may provide a similar benefit.26 At this dose, the risk of rhabdomyolysis should be decreased. Nonetheless, it is not safe to try this combination except under close physician supervision.

Pomegranate

Possible Harmful Interaction

One case report suggests that consumption of pomegranate juice might increase the risk of rhabdomyolosis with rosuvastatin (Crestor).28

Red Yeast Rice

Possible Harmful Interaction

Red yeast rice is an herbal cholesterol-lowering therapy. It contains a mixture of statins; its primary statin ingredient is lovastatin, making it most closely resemble the prescription drug Mevacor.

Based on the similarity of red yeast rice to statin drugs, the two should not be combined without medical supervision.

Coenzyme Q10 (CoQ10)

Supplementation Possibly Helpful

Coenzyme Q10 (CoQ10) is a vitamin-like substance that plays a fundamental role in the body's energy production13,14 and appears to be important for normal heart function.15

Statin drugs inhibit the enzyme necessary for the body's synthesis of both cholesterol and CoQ10, and as an inevitable part of their mechanism of action, reduce CoQ10 levels in the body.16-18 Since these drugs are used to protect the heart, and since CoQ10 deficiency could in theory impair heart function, it has been suggested that this side effect may work against the intended purpose of taking statins. Furthermore, one might naturally hypothesize that some of the side effects of statins could be caused by this induced CoQ10 deficiency. Taking CoQ10 supplements does prevent the lowering of CoQ10 levels caused by statin drugs and accomplishes this without interfering with their therapeutic effects.20 However, studies designed to determine whether the use of CoQ10 supplements actually offers any benefit to people taking statins have returned inconsistent results at best.27,30-32,36 The most recent of these studies, for example, a relatively large double-blind, placebo-controlled trial of 44 people, failed to find that use of CoQ10 at a dose of 200 mg daily reduced the side effects of simvastatin.36

Fish Oil

Supplementation Probably Helpful

Three double-blind, placebo-controlled studies suggest that combining adding fish oil (or its constituent DHA) with statin drugs may result in additional improvement in lipid profile.21,29,35

References

1.   Alderman S, Kailas S, Goldfarb S, et al. Cholestatic hepatitis after ingestion of chaparral leaf: confirmation by endoscopic retrograde cholangiopancreatography and liver biopsy. J Clin Gastroenterol. 1994;19:242-247.

2.   [No authors listed]. From the Centers for Disease Control and Prevention. Chaparral-induced toxic hepatitis—California and Texas, 1992. JAMA. 1992;268:3295,3298.

3.   Gordon DW, Rosenthal G, Hart J, et al. Chaparral ingestion. The broadening spectrum of liver injury caused by herbal medications. JAMA. 1995;273:489-490.

4.   Katz M, Saibil F. Herbal hepatitis: subacute hepatic necrosis secondary to chaparral leaf. J Clin Gastroenterol. 1990;12:203-206.

5.   Smith BC, Desmond PV. Acute hepatitis induced by ingestion of the herbal medication chaparral [letter]. Aust N Z J Med. 1993;23:526.

6.   Sheikh NM, Philen RM, Love LA. Chaparral-associated hepatotoxicity. Arch Intern Med. 1997;157:913-919.

7.   Jim LK, Gee JP. Adverse effects of drugs on the liver. In: Young LY, Koda-Kimble MA, eds. Applied Therapeutics: The Clinical Use of Drugs. Vancouver, WA: Applied Therapeutics, Inc; 1995:26:1-26.

8.   A to Z Drug Facts [book on CD-ROM]. 2nd ed. St. Louis, MO: Facts and Comparisons; 2000.

9.   Takanaga H, Ohnishi A, Murakami H, et al. Relationship between time after intake of grapefruit juice and the effect on pharmacokinetics and pharmacodynamics of nisoldipine in healthy subjects. Clin Pharmacol Ther. 2000;67:201-214.

10.   A to Z Drug Facts [book on CD-ROM]. 2nd ed. St. Louis, MO: Facts and Comparisons; 2000.

11.   Jacobson TA, Amorosa LF. Combination therapy with fluvastatin and niacin in hypercholesterolemia: a preliminary report on safety. Am J Cardiol. 1994;73:25D-29D.

12.   Kashyap ML, Evans R, Simmons PD, et al. New combination niacin/statin formulation shows pronounced effects on major lipoproteins and is well tolerated [abstract]. J Am Coll Cardiol. 2000;35(2 suppl A):A326.

13.   Mortensen SA, Leth A, Agner E, et al. Dose-related decrease of serum coenzyme Q10 during treatment with HMG-CoA reductase inhibitors. Mol Aspects Med. 1997;18(suppl):S137-S144.

14.   Ghirlanda G, Oradei A, Manto A, et al. Evidence of plasma CoQ10-lowering effect by HMG-CoA reductase inhibitors: a double-blind, placebo-controlled study. J Clin Pharmacol. 1993;33:226-229.

15.   Mortensen SA, Vadhanavikit S, Muratsu K, et al. Coenzyme Q10: clinical benefits with biochemical correlates suggesting a scientific breakthrough in the management of chronic heart failure. Int J Tissue React. 1990;12:155-162.

16.   Mortensen SA, Leth A, Agner E, et al. Dose-related decrease of serum coenzyme Q10 during treatment with HMG-CoA reductase inhibitors. Mol Aspects Med. 1997;18(suppl):S137-S144.

17.   Ghirlanda G, Oradei A, Manto A, et al. Evidence of plasma CoQ10 -lowering effect by HMG-CoA reductase inhibitors: a double-blind, placebo-controlled study. J Clin Pharmacol. 1993;33:226-229.

18.   Folkers K, Langsjoen P, Willis R, et al. Lovastatin decreases coenzyme Q levels in humans. Proc Natl Acad Sci USA. 1990;87:8931-8934.

19.   Folkers K, Langsjoen P, Willis R, et al. Lovastatin decreases coenzyme Q levels in humans. Proc Natl Acad Sci USA. 1990;87:8931-8934.

20.   Bargossi AM, Battino M, Gaddi A, et al. Exogenous CoQ10 preserves plasma ubiquinone levels in patients treated with 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Int J Clin Lab Res. 1994;24:171-176.

21.   Durrington PN, Bhatnagar D, Mackness MI, et al. An omega-3 polyunsaturated fatty acid concentrate administered for one year decreased triglycerides in simvastatin treated patients with coronary heart disease and persisting hypertriglyceridaemia. Heart. 2001;85:544-548.

22.   Sugimoto Ki K, Ohmori M, Tsuruoka S, et al. Different effects of St John's Wort on the pharmacokinetics of simvastatin and pravastatin. Clin Pharmacol Ther. 2001;70:518-524.

23.   Jacobson TA, Amorosa LF. Combination therapy with fluvastatin and niacin in hypercholesterolemia: a preliminary report on safety. Am J Cardiol. 1994;73:25D-29D.

24.   Kashyap ML, Evans R, Simmons PD, et al. New combination niacin/statin formulation shows pronounced effects on major lipoproteins and is well tolerated. J Am Coll Cardiol. 2000;35(suppl A):326.

25.   Wolfe ML, Vartanian SF, Ross JL, et al. Safety and effectiveness of Niaspan when added sequentially to a statin for treatment of dyslipidemia. Am J Cardiol. 2001;87:476-479.

26.   Wink J, Giacoppe G, King J. Effect of very-low-dose niacin on high-density lipoprotein in patients undergoing long-term statin therapy. Am Heart J. 2002;143:514-518.

27.   Stocker R, Pollicino C, Gay CA et al. Neither plasma coenzyme Q(10) concentration, nor its decline during pravastatin therapy, is linked to recurrent cardiovascular disease events: A prospective case-control study from the LIPID study. Atherosclerosis. 2005 Oct 8. [Epub ahead of print]

28.   Sorokin AV, Duncan B, Panetta R, Thompson PD. Rhabdomyolysis associated with pomegranate juice consumption. Am J Cardiol. 2006;98:705-706.

29.   Meyer BJ, Hammervold T, Rustan AC, et al. Dose-dependent effects of docosahexaenoic acid supplementation on blood lipids in statin-treated hyperlipidaemic subjects. Lipids. 2007;42:109-115.

30.   Marcoff L, Thompson PD. The role of coenzyme Q10 in statin-associated myopathy: a systematic review. J Am Coll Cardiol. 2007;49:2231-2237.

31.   Mabuchi H, Nohara A, Kobayashi J, et al. Effects of CoQ10 supplementation on plasma lipoprotein lipid, CoQ10 and liver and muscle enzyme levels in hypercholesterolemic patients treated with atorvastatin: A randomized double-blind study. Atherosclerosis. 2007 Aug 4. [Epub ahead of print]

32.   Strey CH, Young JM, Molyneux SL, et al. Endothelium-ameliorating effects of statin therapy and coenzyme Q(10) reductions in chronic heart failure. Atherosclerosis. 2005;179:201-206.

33.   Andren L, Andreasson A, Eggertsen R. Interaction between a commercially available St. John's wort product (Movina) and atorvastatin in patients with hypercholesterolemia. Eur J Clin Pharmacol. 2007 Aug 15. [Epub ahead of print]

34.   Fan L, Zhang W, Guo D, et al. The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1. Clin Pharmacol Ther. 2007 Sep 12. [Epub ahead of print]

35.   Davidson MH, Stein EA, Bays HE, et al. Efficacy and tolerability of adding prescription omega-3 fatty acids 4 g/d to simvastatin 40 mg/d in hypertriglyceridemic patients: an 8-week, randomized, double-blind, placebo-controlled study. Clin Ther. 2007;29:1354-1367.

36.   Young JM, Florkowski CM, Molyneux SL, et al. Effect of coenzyme q(10) supplementation on simvastatin-induced myalgia. Am J Cardiol. 2007;100:1400-1403.



Last reviewed November 2007 by EBSCO CAM Review Board

Please be aware that this information is provided to supplement the care provided by your physician. It is neither intended nor implied to be a substitute for professional medical advice. CALL YOUR HEALTHCARE PROVIDER IMMEDIATELY IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY. Always seek the advice of your physician or other qualified health provider prior to starting any new treatment or with any questions you may have regarding a medical condition.


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