How can high cholesterol be controlled?
Atorvastatin (Lipitor) and simvastatin (Zocor) are parts of a group of drugs called statins that revolutionized cholesterol management and heart disease prevention.
Atorvastatin and simvastatin both target the same chemical in the body to reduce drastically the bloodstream levels of LDL (low-density lipoprotein, or "bad cholesterol"), which lowers the risk it will clog up arteries, a central cause of cardiovascular problems.
These drugs also modestly raise levels of "good cholesterol" (HDL or high-density lipoprotein).
Both Lipitor and Zocor are good for lowering LDL, but Zocor is better at increasing HDL and tends to have fewer gastrointestinal side effects, according to one study.
Both atorvastatin and simvastatin share some possible side effects, including:
liver damage,
muscle inflammation and damage, and
Lipitor and Zocor differ on a number of other less serious side effects.
A large number of drugs interact with both atorvastatin and simvastatin, so be sure to tell your doctor about all your other medications if they prescribe you either of these cholesterol drugs.
Atorvastatin and simvastatin are both chemicals that interfere with liver cells' cholesterol production. They are in a family of statins which also includes:
fluvastatin (Lescol), and
The molecules of the medications target an enzyme called HMG-CoA reductase, one step in the chemical process cells use to fabricate cholesterol from simpler types of molecules. Because of this, statins are called "HMG-CoA reductase inhibitors."
Cholesterol is essential for many body functions, including hormone production, cell structure, lining of nerve cells, digestion, and more. The body can make all the cholesterol it needs, but foods also contain cholesterol the body can use.
A healthy liver can balance cholesterol levels, but too much cholesterol in the bloodstream in LDL form leads to a host of cardiovascular diseases. The excess LDL forms plaques on artery walls, narrowing blood vessels to cause clots and blockages that can lead to coronary heart disease, stroke, heart attack, and other debilitating or fatal problems.
Lipitor and Zocor, as well as other statins, stop the cholesterol-making process in the liver cells by grabbing onto and binding up HMG-CoA reductase before it becomes cholesterol, sabotaging the cell's cholesterol factory.
When the liver cells can't make enough of their own cholesterol anymore because of the statin treatment, the body's cholesterol balancing impulse kicks into action, causing liver cells to suck up more LDL from the bloodstream. The cells break down the LDL into cholesterol to make up for the shortfall in production. As a consequence, less LDL is floating around in the bloodstream to add to arterial plaque deposits, thus substantially reducing cardiovascular disease risk.
Statins like atorvastatin and simvastatin also modestly increase HDL (high-density lipoproteins) in the bloodstream, which is the so-called "good cholesterol." Good levels of HDL molecules are healthy because they act as scavenger molecules, grabbing LDL from the bloodstream and taking it to the liver for processing and removal.
Researchers don't yet understand exactly how statins increase HDL.
Lipitor and Zocor are used for the treatment ofelevated total cholesterol, LDL, andtriglycerides and to elevate HDL cholesterol. Both atorvastatin and simvastatin can help prevent:
hospitalization for congestive heart failure, and
revascularization procedures in individuals with coronary artery disease.
Lipitor and Zocor reduce the risk of heart attack,stroke, angina and revascularization procedures in adults with multiple risk factors for coronary artery disease.Atorvastatin and simvastatin also preventheart attacks and strokes in patients withtype 2 diabetes with multiple risk factors for coronary artery disease.
Side effects common to both Lipitor and Zocor include:
Common side effects unique to atorvastatin include constipation, fatigue, gas, heartburn, common cold, urinary tract infection and joint pain.
Simvastatin, on the other hand, can cause nausea, vomiting, gas, and allergic reactions.
The most serious possible side effect of both Lipitor and Zocor is liver damage. Statins will usually affect the results of liver tests soon after treatment starts, but then return to normal. Doctors should stop administering atorvastatin or simvastatin if liver tests for certain chemical markers remain three times normal concentrations for an extended period.
Muscle inflammation caused by Lipitor and Zocor can cause serious damage if muscle protein (myoglobin) leeches into the bloodstream. This can cause rhabdomyolysis, a potentially fatal condition that can cause kidney failure because those organs cannot filter myoglobin.
Anonther concern with both atorvastatin and simvastatin is they can raise blood sugar and HbA1c levels, mimicking conditions seen in diabetes.
Lipitor is prescribed once daily. The usual starting dose for adults is 10-20 mg per day, and the maximum dose is 80 mg per day. Adults who need more than a 45% reduction in LDL cholesterol may be started at 40 mg daily.
Pediatric patients should receive 10 mg once daily up to a maximum dose of 20 mg daily. Lipitor may be taken with or without food and at any time of day.
The recommended dose range of simvastatin is 10 mg to 40 mg, and it is administered once daily in the evening with or without food. People usually start with 10 or 20 mg daily, but those with high heart disease risk can start with 40 mg daily.
Simvastatin 80 mg is restricted to patients who have been taking simvastatin 40 mg long-term (for example, for a year or more) without evidence of muscle toxicity. The 80 mg dose is associated with increased risk of muscle toxicity, including rhabdomyolysis. Patients who are currently tolerating the 40 mg dose of simvastatin who need to start an interacting drug that should not be taken with simvastatin or is associated with a dose cap for simvastatin should be switched to an alternative statin or statin-based regimen with less potential for the drug-drug interaction.
Patients that require more than the 80 mg dose should be switched to an alternative drug.
A number of drugs reduce the body's ability to get rid of both Lipitor and Zocor. They include, but aren't limited to:
erythromycin (E-Mycin),
nefazodone (Serzone), and
HIV protease inhibitors such asindinavir (Crixivan) andritonavir (Norvir).
Large quantities of grape fruit juice (more than 1.2 liters daily) also will increase blood levels of atorvastatin and simvastatin, so drink it sparingly.
The following drugs also may increase the risk of muscle toxicity when combined with Lipitor or Zocor.
cyclosporine (Sandimmune)
A number of other drugs have reactions with Liptor and Zocor. This is not a complete list of drugs dangerous to combine with these statins, so make sure to tell your doctor about all the medications you are taking if they prescribe you atorvastatin or simvastatin.
Because cholesterol is vital to the formation of the fetus and the growth of infants, pregnant and nursing mothers should never take atorvastatin, simvastatin, or any other statin. The risk is so great, doctors won't prescribe statins to women of childbearing age unless they are unlikely to become pregnant.
Lipitor and Zocor are passed on in breast milk, so either feed your infant with formula or don't take any statins.
Atorvastatin (Lipitor) and simvastatin (Zocor) are both statins that lower cholesterol levels in the bloodstream. These drugs, part of a family called statins, are prescribed to treat a large number of cardiovascular disease, including to prevent heart failure. Learn dosage, side effects, and pregnancy safety information before taking this drug.
Reviewed By: Robert J. Bryg, MD
Reviewed on 6/21/2016
How can high cholesterol be controlled?
Nearly 1/3 of all adults in the U.S. have high cholesterol levels, according to the Centers for Disease Control (CDC). High cholesterol can put people at risk for heart disease, heart attacks, and death.
Cholesterol levels can be lowered with regular exercise, weight loss, and a healthy diet that is low in cholesterol and saturated fats. But in some cases, diet and exercise are not enough and cholesterol-lowering medications may be needed.
This slideshow will discuss the basics of cholesterol and the types of drugs prescribed to treat high cholesterol.
Cholesterol is a waxy, fat-like substance in the blood that is made by the body's liver and helps your body produce hormones, vitamin D, and to digest fat. The other source of cholesterol is from the diet in foods like egg yolks, fatty meats, and cheeses. You only need a small amount to regulate the body processes, and when there is excess cholesterol in the blood, it can build up on the walls of the blood vessels, in deposits called plaque. Plaque can contribute to the narrowing and blockages of arteries that can lead to heart disease.
There are different types of cholesterol. Most of your body's cholesterol is low density lipoprotein (LDL) cholesterol, also referred to as "bad" cholesterol because it can lead to plaque buildup in the arteries, which leads to heart disease and stroke.
High-density lipoprotein (HDL) cholesterol is called the "good" cholesterol because it absorbs "bad" cholesterol and carries it back to the liver, which helps remove it from your body. This can reduce your risk of heart disease and stroke.
Triglycerides are a type of fat found in your blood. High triglycerides combines with low HDL cholesterol or high LDL cholesterol can increase your risk for heart attack and stroke.
Numerous types of cholesterol drugs are available in the U.S., including statins (HMG CoA reductase inhibitors), nicotinic acid (niacin), fibric acid derivatives (fibrates), bile acid sequestrants, cholesterol absorption inhibitors and omega-3 fatty acids. These medications can help lower LDL ("bad") cholesterol levels, and increase HDL ("good") cholesterol levels. Different medications may also be combined to do both at the same time.
Statins are a class of drugs that work by lowering blood cholesterol levels, and reducing the production of cholesterol by the liver by blocking an enzyme. Statins are used to reduce high cholesterol levels, and also to prevent and treat hardening of the arteries (atherosclerosis) that can cause chest pain, heart attacks, strokes, peripheral vascular disease and intermittent claudication (cramping leg pain) in at-risk patients.
Risk factors for atherosclerosis include:
high LDL ("bad") cholesterol levels or low HDL ("good") cholesterol levels
high blood pressure
a family history of early heart attacks
smoking
increasing age
diabetes
insulin resistance
obesity
lack of physical activity
unhealthy diet
The next several slides are examples of statins currently prescribed to lower cholesterol.
Drug Class: Statins
Prescription: Yes
Generic: No
Preparations: Tablets of 10, 20, 40, and 80 mg.
Prescribed for: Atorvastatin (Lipitor) lowers the LDL ("bad") cholesterol and triglycerides and can raise your HDL ("good") cholesterol. This can lower the risk for heart attack, stroke, certain types of heart surgery, and chest pain in patients who have heart disease or risk factors for heart disease such as age, smoking, high blood pressure, low HDL, or family history of early heart disease.
Side effects: Atorvastatin (Lipitor) is generally well-tolerated. Minor side effects include diarrhea, constipation, nausea, upset stomach, gas, fatigue, heartburn, headache, muscle and joint pain, and changes in some blood tests. Atorvastatin (Lipitor) may cause liver and muscle damage (rhabdomyolysis).
Drug Class: Statins
Prescription: Yes
Generic: No
Preparations: Tablets of 5, 10, 20, and 40 mg.
Prescribed for: Rosuvastatin (Crestor) is used for the reduction of blood total cholesterol, LDL cholesterol and triglyceride levels, and to increase HDL cholesterol levels, to reduce the chances of developing problems like heart disease and strokes.
Side effects: The most common side effects of rosuvastatin (Crestor) are headache, depression, nausea, vomiting, stomach pain, indigestion, diarrhea, constipation, muscle aches or pains, joint pain, and sleep problems (insomnia or nightmares). The most serious side effects are liver failure, muscle breakdown (rhabdomyolysis), and kidney failure.
Drug Class: Statins
Prescription: Yes
Generic: Yes
Preparations: Tablets of 5, 10, 20, 40, and 80 mg.
Prescribed for: Simvastatin (Zocor) is used for reducing total cholesterol, LDL cholesterol, and triglycerides, and for increasing HDL cholesterol in patients with coronary heart disease, diabetes, peripheral vessel disease, or history of stroke or other cerebrovascular disease.
Side effects: The most common side effects of simvastatin (Zocor) are headache, nausea, vomiting, diarrhea, abdominal pain, muscle pain, heartburn, gas, bloating, indigestion, constipation, headache, joint pain, skin rash, sleep problems (insomnia), cold symptoms (stuffy nose, sneezing, or sore throat), and abnormal liver tests. Hypersensitivity reactions have also been reported. The most serious potential side effects are liver damage and muscle inflammation or breakdown.
Drug Class: Statins
Prescription: Yes
Generic: Yes
Preparations: Tablets of 10, 20, 40, and 80 mg.
Prescribed for: Pravastatin (Pravachol) is used for the reduction of total and LDL cholesterol as well as triglycerides, and to increase HDL cholesterol. It has been suggested that pravastatin may reduce the occurrence of heart attacks, strokes, and death caused by coronary artery disease.
Side Effects: The most common side effects of pravastatin (Pravachol) are headache, nausea, vomiting, diarrhea, muscle pain, skin rash, dizziness, and abnormal liver tests. The most serious potential side effects are liver damage and muscle inflammation or breakdown.
Drug Class: Statins
Prescription: Yes
Generic: Yes
Preparations: Tablets of 10, 20, and 40 mg.
Prescribed for: Lovastatin (Mevacor) is used to treat high LDL cholesterol. Effectiveness of the medication in lowering cholesterol is dose-related. Blood cholesterol determinations are performed in regular intervals during treatment so that dosage adjustments can be made. A reduction in LDL cholesterol level can be seen two weeks after starting therapy.
Side Effects: Side effects of lovastatin (Mevacor) are rare. Minor side effects include constipation, diarrhea, gas, heartburn, indigestion, stomach pain, nausea, headache, muscle pain, joint pain, back pain,and sleep problems (insomnia). Major side effects include abdominal pain or cramps, blurred vision, dizziness, itching, chest pain, muscle pain or cramps, rash, or yellowing of the skin or eyes.
Drug Class: Statins
Prescription: Yes
Generic: Yes
Preparations: Tablets of 20 and 40 mg.
Prescribed for: Fluvastatin (Lescol) is used to treat high LDL cholesterol. Effectiveness of the medication in lowering cholesterol is dose-related. Blood cholesterol is checked at regular intervals during treatment so that dosage adjustments can be made.
Side effects: Side effects of fluvastatin (Lescol) are rare. Minor side effects include stomach upset, constipation, diarrhea, gas, heartburn, headache, and insomnia. Major side effects include abdominal pain or cramps, blurred vision, dizziness, itching, muscle pain or cramps, rash, or yellowing of the skin or eyes.
Fibrates aim to lower blood triglyceride levels by 35 to 50 percent and raise HDL ("good") cholesterol levels by 5 to 20 percent. Fibrates work by reducing the amount of triglycerides produced by the liver, and increasing the rate at which the triglycerides are removed from the bloodstream.
While they can increase HDL cholesterol, fibrates do not work to lower LDL ("bad") cholesterol and are often combined with statins to accomplish this. Fibrates are also prescribed to help prevent heart attacks in at-risk patients with high blood triglycerides and low HDL cholesterol.
Drug Class: Fibrates
Prescription: Yes
Generic: Yes
Preparations: Tablets of 54 and 145 mg.
Prescribed for: Fenofibrate (Tricor) is used along with a non-drug program (including diet changes) to treat elevated cholesterol and triglyceride levels.
Side effects: Common side effects of fenofibrate (Tricor) include stomach pain or upset, back pain, constipation, headache, dizziness, trouble sleeping, or runny or stuffy nose. Muscle damage may occur, and muscle pain, tenderness, weakness and fever should be reported promptly to your physician. Decreased sexual drive, yellowing of the eyes or skin (jaundice), and stomach pain may occur and also should be reported.
Drug Class: Fibrates
Prescription: Yes
Generic: Yes
Preparations: Tablet of 600 mg.
Prescribed for: Gemfibrozil (Lopid) is used for persons with either low HDL cholesterol and/or high triglyceride concentrations to reduce the risk of heart attacks. It also is used in persons with very high triglyceride levels that are at risk for pancreatitis (inflammation of the pancreas).
Side effects: Side effects of gemfibrozil (Lopid) include upset stomach, stomach/abdominal pain, diarrhea, tiredness, nausea, vomiting, headache, dizziness, drowsiness, joint pain, loss of interest in sex, impotence, difficulty having an orgasm, numbness or tingly feeling, unusual taste, cold symptoms (stuffy nose, sneezing, sore throat), depression, blurred vision. Less common side effects are muscle aches, pains, weakness, or tenderness.
The liver produces bile acids (a main component of your digestive enzymes secreted by the liver) using cholesterol. Bile acid sequestrants bind bile acids in the intestine causing bile acids to be excreted in the stool. This causes the liver to use more of the blood cholesterol to make more bile acids, and in turn, lower blood cholesterol levels.
Bile acid sequestrants used alone, mildly lower LDL cholesterol. They are commonly used in combination with other classes of cholesterol drugs to more effectively lower LDL cholesterol levels.
Nicotinic acid (vitamin B3 or niacin) is a B vitamin. Niacin is a common vitamin component of most balanced diets. However, the dose of niacin used to treat cholesterol is much higher than the average dietary intake. Nicotinic acid (niacin) is available in immediate release and sustained release preparations. Some nicotinic acid preparations are available over-the-counter but are not federally regulated.
Nicotinic acid is used to increase HDL ("good") cholesterol (sometimes by as much as 30%). It is only mildly effective at lowering LDL ("bad") cholesterol and triglyceride levels.
Cholesterol absorption inhibitors keep the body from absorbing cholesterol from the foods we eat. This class of drug blocks this absorption in the intestine as our foods are digested. Cholesterol absorption inhibitors are most effective at lowering LDL ("bad") cholesterol, but may also have a small effect on lowering triglycerides and raising HDL ("good") cholesterol levels.
Because some medications are good at lowering LD ("bad") cholesterol, some are helpful in lowering triglycerides, and others can aid in raising HDL ("good") cholesterol levels, doctors frequently prescribe two medications from two different drug classes to work together. This can more aggressively lower LDL cholesterol and increase HDL cholesterol at the same time, for greater benefit to the patient.
Omega-3 fatty acids (omega-3 acid ethyl esters) reduce the production of VLDL particles in the liver, and speed up the removal of triglycerides from the blood. It is unclear how omega-3's work, but they are often recommended for people with high cholesterol.
Omega-3 fatty acids can be found in foods such as fatty fish (salmon, tuna, mackerel), but some people require a prescription dose.
This chart provides an overview of the cholesterol drugs discussed in this slideshow. It lists each of the medication classes, examples within each class, and their areas of effectiveness.
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