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 Cholesterol Medications

Many physicians will use medications as a last resort when proper diet and exercise does not lower your risk of developing heart disease to a satisfactory level. It must be noted that these medications are not a free license to stop proper diet and exercise.

Medications should be thought of as additional components in conjunction with proper diet and exercise that can help reduce the risk of heart disease.

Cholesterol Medications

HMG-CoA Reductase Inhibitors (Statins). One of the essential rate limiting steps in the production of cholesterol in the body involves the enzyme HMG-CoA reductase. By inhibiting this enzyme, the production of cholesterol by the liver is reduced, and concomitantly, cholesterol in the blood is removed as well. Due to their effectiveness and their general well tolerance, statins have become the first line of medication favored by many physicians in treating high cholesterol. Patients taking statins often show markedly improved cholesterol levels in about a month’s time. Side effects usually involve drug-drug interactions. If you have generalized aches, pain and dark urine; stop your medications and consult your physician right away. Some examples of statins are: Lovastatin (Mevacor, Altocor, Advicor, Altoprev), Pravastatin (Pravachol), Simvastatin (Zocor), Fluvastatin (Lescol), Atorvastatin (Lipitor) and Rosuvastatin (Crestor).

Bile Acid Sequestrants (Resins). Bile acids play a key role in emulsification and absorption of fats in the intestines. Resins bind to these cholesterol laden bile acids, effectively lowering the body’s supply of recyclable cholesterol. Sequestered bile acids are eliminated in the stool. Resins are often co-prescribed with other cholesterol lowering medications to produce a synergistic effect. Examples of resins include: Cholestyramine (Questran, Questran Light), Colestipol (Colestid) and Colesevelam (WelChol).

Nicotinic Acids (Niacin). Also known as Vitamin B3, Niacin in high doses lowers all the bad cholesterol while raising the good cholesterol. In fact, Niacin is the drug of choice in raising HDL levels. Due to the side effects that may be subtle yet dangerous, niacin should not be taken without careful monitoring by a physician. Some available niacins include: Immediate-release nicotinic acid, extended-release nicotinic acid (Niaspan, Nicolar, Niacor) and sustained-release nicotinic acid.

Fibric Acids (Fibrates). Fibrates facilitate transcription of genes that affect lipid metabolism. This mechanism is mostly effective in lowering trigylceride production. To a much lesser extent, fibrates can lower LDL levels and elevate HDL levels. Examples of fibric acids include: Gemfibrozil (Lopid), Fenofibrate (Tricor), Clofibrate (Atromid), Bezafibrate (Bezalip) and Ciprofibrate (Modalim).

Cholesterol Absorption Blockers. A relatively new class of anti-hyperlipidemic drug, cholesterol absorption blockers are often used to augment statins. Ezetimibe (Zetia) is the first drug in this class that lowers LDL levels by inhibiting the Niemann-Pick C1 Like 1 Protein (a necessary component for cholesterol absorption). Side effects are rare but liver function tests should be taken by your physician as a precaution.

Vytorin is a prescription medication that is comprised of a cholesterol absorption blocker (Ezetimibe) and a statin (Simvastatin). Vytorin is marketed as being the only current cholesterol medication proven to address both main causes of high cholesterol levels: hereditary and dietary. It reduces the cholesterol made naturally by the body, as well as helps block the absorption of cholesterol that comes from food. This results as lower LDL (bad) cholesterol, lower total cholesterol, lower triglycerides (fatty substances in your blood), and higher HDL (good) cholesterol. Side effects of vytorin include – Rare: muscle pain, tenderness, or weakness; Serious: decreased urine or rust-colored urine, blurred vision, allergic reactions; Less Serious: gas, bloating, nausea, stomach upset, heartburn, abdominal pain, constipation, or diarrhea.

Drug Class Agents and Daily Doses Lipid/Lipoprotein Effects Side Effects Contraindications
HMG CoA reductase inhibitors (statins) Lovastatin (20-80 mg), Pravastatin (20-40 mg), Simvastatin (20-80 mg), Fluvastatin (20-80 mg), Atorvastatin (10-80 mg) LDL-C 18-55%
HDL-C 5-15%
TG 7-30%
Increased liver enzymes
· Active or chronic liver disease
· Concomitant use of certain drugs*
Bile acid Sequestrants Cholestyramine (4-16 g) Colestipol (5-20 g) Colesevelam (2.6-3.8 g) LDL-C 15-30%
HDL-C 3-5%
TG No change or increase
Gastrointestinal distress
Decreased absorption of other drugs
· dysbeta-lipoproteinemia
· TG >400 mg/dL
· TG >200 mg/dL
Nicotinic acid Immediate release (crystalline) nicotinic acid (1.5-3 gm), extended release nicotinic acid (Niaspan ®) (1-2 g), sustained release nicotinic acid (1-2 g) LDL-C 5-25%
HDL-C 15-35%
TG 20-50%
Hyperuricemia (or gout)
Upper GI distress
· Chronic liver disease
· Severe gout
· Diabetes
· Hyperuricemia
· Peptic ulcer disease
Fibric acids Gemfibrozil (600 mg BID)
Fenofibrate (200 mg)
Clofibrate (1000 mg BID)
LDL-C 5-20% (may be increased in patients with high TG)
HDL-C 10-20%
TG 20-50%
· Severe renal disease
· Severe hepatic disease