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Antihyperlipidemic

Antihyperlipidemic

Generic Trade Name
Atorvastatin Lipitor
Cerivastatin Baycol
Chlolestyramine  Cholybar, Questran, Questran Light
Clofibrate  Atromid-S
Colestipol  Colestid
Dextrothyroxine  Choloxin
Fluvastatin  Lescol
Gemfibrozil  Lopid
Lovastatin  Mevacor
Nicotinic Acid  Niacin, Nicobid, Nicolar
Pravastatin  Pravachol
Probucol  Lorelco
Simvastatin  Zocor

Description:

There are several drugs classified as antihyperlipidemic agents. There are subcategories under this heading based on how these drugs prinicipally lower cholesterol. Drugs considered as bile acid sequestrants are: Cholestyramine (Questran) and Colestipol (Colestid).
These agents are used to reduce cholesterol and triglycerides in the blood by preventing the formation of bile acids.

Cholestyramine reduces high bile acids levels, which occur with some liver problems, and lowers cholesterol levels.

Gemfibrozil (Lopid), Clofibrate(Atromid-S) and Fenofibrate(Tricor), are examples of lipid lowering formulations that primarily lower serum triglyceride levels and very low density lipoprotein (VLDL).

Nicotinic acid is a vitamin and prescription drug classified as a vitamin supplement, antihyperlipidemic, and vasodilator. It is used to reduce cholesterol and triglyceride levels in the blood. Nicotinic acid dilates blood vessels and, with large doses, decreases cholesterol production. This often gives rise to a "flush", which may be considered by some, to be an undesirable side-effect. Related forms include: niacinamide and nicotinamide.

Dextrothyroxine sodium is a prescription drug classified as a cardiovascular agent. It is used to reduce serum cholesterol in patients with excessive quantities of fat in their blood. Dextrothyroxine is reported to stimulate the liver to increase catabolism and excretion of cholesterol.

"Statins" include: Atorvastatin (Lipitor) and Lovastatin (Mevacor), Pravastatin (Pravachol), Fluvastatin (Lescol). The principal action appears to be the inhibition of HMG-CoA reductase. This affects both cholesterol and CoQ10 plasma levels, however, possibly reducing both by as much as 40%. (Facts and Comparisons 1999)

Nutritional Considerations:

Limit alcohol.

The inhibition of HMG-CoA reductase also affects the biosynthesis of ubiquinone (Coenzyme Q10). Hence supplementation has been recommended (Bargossi, Ghirlanda, Mortensen).

Avoid taking the statin class of medications with grapefruit juice, except Pravastatin, it does not seem to be effected. (Lilja 1999)(Pronsky 1999)

Do not take "statins" with niacin due to possible myopathy. (Pronsky 1999)

Supplementation of fat soluble vitamins, (A, D, E and K) vitamin B-12 and folic acid may be necessary with long term use of some antihyperlipidemics. (Facts 1999) (Brinker 1998) Selected fatty acids may also help fat metabolism.

Fiber will reduce absorption of lovastatin and if taken should be separated from the drug by several hours (Richter)(Pronsky 1999).

Bile acid sequestrants - Cholestyramine (Questran) and Colestipol (Colestid) - have also been asssociated with an increased risk for folate deficiency, so supplements of folic acid and vitamin B12 have been recommended; together with minerals: iron and zinc. (Pronsky 1999).

Iron and zinc absorption may also be impaired with some antihyperlipidemics. (Brinker 1998)

Herbal Considerations:

Newall has compiled the following list of herbs with hyperlipidemic effect. It would appear that their use is contra-indicated in people suffering from hyperlipidemia.

Hypercholesterolemic Herbal Ingredients

Herb        
                                
Hydrocotyle (Gotu Kola)        
Plantain                                
Skullcap                                
Tansy                                

Similarly, Newall has compiled the following list of herbs with hypocholesterolemic effect.

Herb                                        

Alfalfa                                
Artichoke Plant                        
Black Cohosh,                        
Fenugreek                                
Garlic Plant                        
Ginger                                

These herbs have approval status by the German Commission E regarding this specific action (cholesterol lowering):

Psyllium seed, blonde
Psyllium seed husk, blonde

The weak antithrombotic effect of garlic plant, ginger and onion plant, may be increased by concomitant administration of clofibrate.

Note:

Cholestin has been a dietary supplement. Officials at the Food and Drug Administration call it: an illegal, unapproved drug.

Cholestin is composed of a pulverized strain of rice fermented with red yeast and is imported from China, where it has been consumed for 2,000 years, as an herbal remedy (it is thought to improve blood flow) and a food (it spices up tofu and makes a tasty marinade for duck and pork.).

At issue is not whether Cholestin is dangerous; no one argues that it is. Rather, the agency contends that Cholestin has crossed the increasingly murky boundary that separates dietary supplements from drugs, because it contains an ingredient, lovastatin that is the key component of a cholesterol-lowering drug.

Pharmanex says the lovastatin occurs naturally in the rice and that Cholestin is more akin to a food than to a drug.

References

Bargossi Am, Grossi G, Fiorella PL, et al: Exogenous CoQ10 supplementation prevents plasma ubiquinone reduction induced by HMG-CoA reductase inhibitors, Mol Aspects Med, 1994, 15 (suppl): 187-93

Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.

Basu, T.K. : Drug-Nutrient Interactions. Helm, London. 1988.

Brinker, Francis N.D. Herb Contraindications and Drug Interactions. Eclectic Medical Publications. 1998.

Courtney SP & Wightman JAK: Urethral calculi caused by cholestyramine. Br J Urology 1991; 68:654-661.

Curtis DM, Driscoll DJ, Goldman DH et al: Case report: loss of dental enamel in a patient taking cholestyramine. Mayo Clin Proc 1991; 66:1131.

De Pinieux G et al., Lipid-lowering drugs and mitochondrial function: effects of HMG-CoA reductase inhibitors on serum ubiquinone and blood lactate/pyruvate ratio. Br J Clin Pharmacol, 1996 Sep, 42:3, 333-7.

Facts and Comparisons, Clinisphere 2.0. A Wolters Kluwer Company. 1999.

Ghirlanda, G et al., Evidence of plasma CoQ10-lowering effect by HMG-CoA reductase inhibitors. J of Clin. Pharm. 1993, 33(3):226-229.

Griffith, H. W. 1983. Complete Guide to Prescription and Non-Prescription. Fisher Publishing, Inc., Tucson.

Human JA et al., The effect of Simvastatin on the plasma antioxidant concentrations in patients with hypercholesterolaemia. Clin Chim Acta, 1997 Jul, 263:1, 67-77.

Kantola T, Kivisto KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998;63:396-402.

Kontush A et al., Plasma ubiquinol-10 is decreased in patients with hyperlipidaemia. Atherosclerosis, 1997 Feb, 129:1, 119-26.

Kniffen, J.C. et al: Clin. Res. 1970, 18: 38. Anon: Cholestyramine for elevated serum cholesterol. Med Lett Drugs Ther 1974; 16:33.

Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin. Clin Pharmacol Ther 1999; 66:118-27.

Merten DF & Grossman H: Intestinal obstruction associated with cholestyramine therapy. Am J Roentgenol 1980; 134:827-828.

Mortensen SA, Leth A, Agner E, Rohde M. Dose-related decrease of serum coenzyme Q10 during treatment with HMG-CoA reductase inhibitors. Mol Aspects Med 1997;18(suppl):S137-44.

Osol, Arthur. 1980. Remington's Pharmaceutical Sciences. Mack Publishing Company, Pennsylvania.

Newall CA, Anderson LA, Phillipson JD. Herbal Medicines A Guide for Health-care Professionals. London: The Pharmaceutical Press, 1996.

Product Information: Cholybar(R), cholestyramine. Parke-Davis, Morris Plains, NJ, 1992.

Product Information: Questran(R), cholestyramine. Bristol Laboratories, Evansville, IN, 1995.

Product Information: Questran Light(R), cholestyramine. Bristol Laboratories, Evansville, IN, 1995.

Pronsky, Zaneta M. Food Medication Interactions. 11th edition. 1999

Richter W, Jacob B, Schwandt P. Interaction between fiber and lovastatin. Lancet 1991;338:706 [letter].

Thomas FB, McCullough FS & Greenberger NJ: Inhibition of the intestinal absorption of inorganic and hemoglobin iron by cholestyramine. J Lab Clin Med 1971; 78:70-80.

Ubbink JB: The role of vitamins in the pathogenesis and treatment of hyperhomocyst(e)inaemia. J Inherit Metab Dis, 1997 Jun, 20:2, 316-25.