What is Lipitor?
Lipitor is a prescription drug manufactured by pharmaceutical giant Pfizer and used to control high cholesterol levels. By lowering cholesterol, the drug aims to prevent dangerous blockages in blood flow and thereby reduce the risk of heart attack and stroke.
The U.S. Food and Drug Administration (FDA) approved Lipitor in 1996. The drug’s active ingredient is atorvastatin calcium.
This class of medications is generally well-tolerated; however, it has been associated with multiple risks, including:
- Type 2 diabetes
- Muscle disease
Lipitor belongs to a popular class of cholesterol-lowering drugs called statins, which represent the most widely prescribed class of drugs in the U.S. Lipitor is the most popular of all statins.
Patients take statins to lower levels of cholesterol and other fatty substances in the blood that, if left unchecked, can increase the risk for heart attack, stroke and other related health complications.
The liver makes most of the cholesterol found in blood. Statins reduce the amount of cholesterol made by the liver and help the liver remove cholesterol that’s already in the blood.
How Lipitor Works
Cholesterol plays a crucial role in several bodily processes that are essential to our health, but unhealthy levels of cholesterol can lead to buildup (plaque) on the walls of arteries. This can block blood flow to the brain and heart and put people at higher risk for stroke and heart disease. According to the Centers for Disease Control and Prevention, heart disease is the leading cause of death for both men and women in the U.S.
Lipitor prevents heart attack and stroke by lowering cholesterol in the blood. It slows the production of cholesterol in the body therefore decreasing the amount of plaque buildup that may block the flow of blood to the heart and brain.
Lipitor and Bad Cholesterol
Statins like Lipitor block HMG-CoA reductase, a liver enzyme needed to produce low-density lipoproteins (LDL), or “bad” cholesterol. By lowering the amount of LDL in the blood, Lipitor prevents atherosclerosis, a condition where plaque deposits accumulate on the inner walls of arteries, causing them to stiffen and narrow. In turn, this reduces the risk of atherosclerosis complications like heart attack, stroke, chest pain and aneurysms.
Lipitor and Good Cholesterol
Lipitor can also raise levels of high-density lipoproteins (HDL), or “good” cholesterol, which protect against heart attack. Some experts believe that HDL can carry plaque away from arteries to the liver, which helps to slow its buildup and prevent dangerous blockages in blood flow.
The FDA approved Lipitor for use in patients who may develop heart disease or who were already diagnosed with heart disease. The agency also approved the drug for use in certain teens and children.
Doctors commonly prescribe Lipitor together with diet, weight loss and exercise to help stave off cardiovascular disease in patients who may develop heart conditions. The drug can be used to reduce the risk of heart attack, stroke and chest pain for patients with multiple heart disease risk factors.
Heart disease risk factors include:
- Advanced age
- A family history of cardiovascular disease
- Low levels of good cholesterol (HDL)
- A history of smoking or hypertension
The FDA approved Lipitor for this use based on clinical trials. In one clinical trial called the Anglo-Scandinavian Cardiac Outcomes Trial (ASCOT), researchers investigated Lipitor’s ability to prevent heart disease in more than 10,000 at-risk patients. The drug was found to reduce the risk of fatal or nonfatal cardiac events by 36 percent when compared with patients taking a placebo.
Lipitor is also a preventative treatment option for patients with type 2 diabetes and several risk factors for heart disease and stroke, such as hypertension, a history of smoking and two diabetes-related conditions called retinopathy and albuminuria.
Patients already diagnosed with heart disease also take the drug to lower their risk of having a cardiac event. For patients diagnosed with coronary heart disease, the drug can reduce the risk of heart attack, stroke and chest pain while also lowering the risk for heart failure surgeries and hospitalization from congestive heart failure.
Lipitor is also indicated for use in children and teenagers who are 10 to 17 years of age and have familial heterozygous hypercholesterolemia, an inherited condition in which cholesterol cannot be removed from the body normally. If diet therapy fails, Lipitor may be used in these patients to decrease the amount of cholesterol and other fatty substances in the blood.
What Lipitor Looks Like and How to Take It
Lipitor comes in 10, 20, 40 and 80 mg tablets to be taken by mouth. The tablets are white, oval-shaped and film-coated. The medication is usually taken once a day with or without food. It’s recommended to take Lipitor around the same time each day.
Doctors may start patients on a low dose and then slowly up the dose, not more than once every two to four weeks. The recommended starting dose is 10 to 20 mg once daily.
Dietary Dos and Don’ts for Lipitor Users
When taking Lipitor, it’s important to follow the exercise and dietary recommendations made by your doctor or dietitian. Typically, Lipitor users are instructed to eat a low-fat, low-cholesterol diet.
The U.S. Department of Health and Human Services recommends that people looking to lower their cholesterol have:
- Less than 7 percent of daily calories from saturated fat
- Less than 200 mg a day of cholesterol
- 25 to 35 percent of daily calories from total fat
Lipitor’s drug label warns users to avoid of drinking large amounts of grapefruit juice while taking the drug. This means users should not drink more than 1.2 liters — or 1 quart — of grapefruit juice per day. Grapefruit juice contains one or more components that inhibit CYP34A, an important enzyme found in the liver, and it can increase plasma concentrations of atorvastatin.
Experts also recommend at least 30 minutes a day of moderate intensity physical activity such as brisk walking.
Common Side Effects and Serious Risks of Lipitor
The vast majority of patients taking Lipitor tolerate the drug well. In premarket clinical studies, less than 2 percent of patients chose to discontinue treatment because of adverse health effects.
|In placebo-controlled studies, the most commonly reported adverse reactions include:|
|Urinary tract infection||Joint pain||pain in extremities|
|Other Lipitor side effects reported in clinical trials or by patients include:|
|Abdominal discomfort||Musculoskeletal pain||Blurred vision|
|Memory loss||Malaise (general feeling of discomfort, illness or uneasiness)||Cognitive impairment|
|Tinnitus (ringing in the ears}|
Although occurrences are rare, Lipitor patients have reported serious complications to their doctors and the FDA. Many of these complications can occur with all statins, which raises serious safety concerns about the drug class as a whole.
Numerous clinical studies are investigating the increased risk that Lipitor and other statins pose for diabetes, as well as damage to the kidneys, liver and muscles. The FDA also warns against use of Lipitor during pregnancy as the drug may cause harm to a fetus when administered to expectant mothers.
Patients have reported damage to liver function and fatal and non-fatal liver failure after taking Lipitor. Women have filed thousands of lawsuits against Pfizer alleging Lipitor caused their type 2 diabetes. And researchers have linked Lipitor use with muscle and joint problems, myopathy and rhabdomyolysis.
Lipitor and Diabetes
Nearly two decades after the FDA approved Lipitor, evidence of a minimal diabetes risk from statins first emerged. Data collected from 91,000 patients treated with either a statin or a placebo revealed that 0.4 percent of statin users went on to develop diabetes. However, researchers later found this figure to be inaccurate. Further studies revealed that some statins pose a higher risk for new-onset diabetes, particularly those commonly prescribed in higher potencies like Lipitor, Zocor and Crestor.
In a February 2012 consumer update, the FDA communicated several new health complications associated with Lipitor use, including an increased risk for high blood sugar (hyperglycemia) and the development of type 2 diabetes.
That year, the FDA updated the safety labels for all statins to warn consumers that the drugs may be linked to diabetes. The FDA’s label revisions also indicated that Lipitor and other statins can cause damage to the livers, muscles and cognitive function of some patients, though reports of these injuries are rare.
Type 2 diabetes occurs when the body fails to properly use or produce insulin, a crucial hormone the body uses to convert food into energy. Researchers suspect that taking statins, including Lipitor, impairs the function of special cells in the pancreas that store and release insulin. There is also evidence that statins, like Lipitor, can decrease the body’s sensitivity to insulin.
People Most at Risk for Diabetes from Statin Use
Studies indicate that diabetes risk is higher for certain groups, including the elderly, women and Asians. Researchers have concluded that those most at risk for diabetes from statin use are:
Lipitor and Crestor Users
In a 2013 clinical study published in the British Medical Journal, Canadian researchers investigated the diabetes risk of six statins: Pravachol, Lipitor, Crestor, Zocor, Lescol (fluvastatin) and Mevacor (lovastatin). Among more than 470,000 patients newly treated with a statin, researchers found that the drug class is associated with a 10 to 22 percent increased risk for type 2 diabetes. Lipitor and Crestor presented the highest diabetes risk at 22 and 18 percent, respectively. Both drugs are routinely prescribed in higher potencies than other statins. There is some evidence that the diabetes risk increases with dosage.
he results of a 2012 study published in the Archives of Internal Medicine found that the diabetes risk of Lipitor and other statins is greater among post-menopausal women. Researchers drew from 12 years of clinical data that followed more than 150,000 women between the ages of 50 and 79 and determined that post-menopausal woman who took Lipitor or other statins face a 48 percent increased risk for developing type 2 diabetes compared to those who did not. The study considered several other factors also known to increase the risk for diabetes, including advanced age, obesity and lack of physical activity.
Researchers found that the risk for diabetes from statins varied among ethnicities. Asian women carried the highest risk followed by white women and Latinas. African American women experienced the lowest risk.
Women and Lipitor Diabetes Risk
Because women are less likely to suffer a heart attack than men, their statin use has historically been lower. That trend changed in recent years, however. According to the Centers for Disease Control, 36 percent of women between the ages of 64 and 74 and 39 percent of those 75 and older take statins to prevent their first heart attack or a repeat cardiac event. For those age ranges, nearly 50 percent of men are taking statins.
Medical experts affirm that the benefits of Lipitor and other statins still outweigh the potential health risks for women at high risk for heart disease. However, researchers are unsure if the drug class’s benefits measure up to the diabetes risk for women taking statins who have no previous diagnosis of heart disease.
Lipitor and Muscle Disease
Some Lipitor patients report various types of muscle injuries after taking the drug. While the risk is minimal, researchers determined that the likelihood for muscle disease is substantially elevated among patients taking other medications in addition to Lipitor, including certain antibiotics, antifungals and treatments for HIV and hepatitis C.
Muscle and Joint Problems
The results of a 2013 study indicated that patients may face an increased risk for musculoskeletal injuries and diseases. Researchers followed nearly 14,000 U.S. soldiers and veterans taking statins and found a 19 percent greater risk for muscle and joint problems compared with nonusers. Statin users in the study were 13 percent more likely to experience strains, sprains or dislocations.
Another muscular side effect associated with Lipitor use is myopathy, a general condition where muscle tissue fibers do not function as they should. Early symptoms of myopathy include pain, weakness or tenderness of the muscles, and dark urine. These signs typically appear within the first few months of therapy.
Researchers linked a particularly severe form of myopathy called rhabdomyolysis to the use of Lipitor and other statins. In this potentially life-threatening complication, muscle tissue dies, and products of the damaged cells can enter the bloodstream. Some of these products are toxic to the kidneys and may lead to kidney failure. While rhabdomyolysis only occurs in about 0.1 percent of patients taking statins, the risk increases for patients taking certain drugs, such as macrolides.
Lipitor and Liver Disease
Doctors advise against statin therapy for patients with liver problems. Clinical studies revealed that Lipitor can damage liver function, and there have been rare postmarketing reports of both fatal and nonfatal liver failure. The FDA recommends that doctors perform liver enzyme tests before statin therapy to determine whether the patient can tolerate treatment.
Complications related to Lipitor liver injury:
- Fatty changes to the liver
Symptoms related to Lipitor liver injury:
- Loss of appetite
- Pain in the right upper abdomen
- Dark urine
- Yellowing of the skin or eyes
Pregnancy Category X
Before the FDA replaced its pregnancy risk letter categories in 2015, it had deemed Lipitor as Pregnancy Category X, indicating that the risks involved with use of the drug in pregnant women clearly outweigh the potential benefits. Pregnancy Category X means studies in animals or humans have demonstrated fetal abnormalities and/ or there is evidence of fetal risk based on human experience.
According to Lipitor’s label, the drug may cause fetal harm when administered to a pregnant woman.
“Lipitor should be administered to women of childbearing potential only when such patients are highly unlikely to conceive and have been informed of the potential hazards,” the drug label states. “If the woman becomes pregnant while taking LIPITOR, it should be discontinued immediately and the patient advised again as to the potential hazards to the fetus and the lack of known clinical benefit with continued use during pregnancy.”
Emily Miller is an award-winning journalist who has held writing and editorial positions with numerous print and online publications around the U.S. She draws on her background as both a patient and a journalist to help readers understand complex health topics. Her most recent experience is in writing about litigation involving medicines that cause life-altering side effects.
- Reinberg, S. (2013, June 3). Cholesterol Drugs Linked to Muscle, Joint Problems: Study. Health Day. Retrieved from http://health.usnews.com/health-news/news/articles/2013/06/03/cholesterol-drugs-linked-to-muscle-joint-problems-study
- American Heart Association. (2013, May 1). Good vs. Bad Cholesterol. Retrieved from http://www.heart.org/HEARTORG/Conditions/Cholesterol/AboutCholesterol/Good-vs-Bad-Cholesterol_UCM_305561_Article.jsp
- National Library of Medicine. (2012, October). Lipitor Prescription Drug Label. Daily Med. Retrieved from http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c6e131fe-e7df-4876-83f7-9156fc4e8228
- Fallah, A., Deep, M., Smallwood, D. and Hughes, P. (2013, March 31). Life-threatening Rhabdomyolysis Following the Interaction of Two Commonly Prescribed Medications. Australian Medical Journal. Retrieved from http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3626026/
- Pfizer. (2012, October). Lipitor Prescribing Information. Retrieved from http://labeling.pfizer.com/ShowLabeling.aspx?id=587#page=23
- Carter, A., Gomes, T., Camacho, X., Juurlink, D., Shah, B. and Mamdani, M. (2013, March 28). BMJ. Retrieved from http://www.bmj.com/content/346/bmj.f2610
- Topol. E. (2012, March 4). The Diabetes Dilemma for Statin Users. The New York Times. Retrieved from http://www.nytimes.com/2012/03/05/opinion/the-diabetes-dilemma-for-statin-users.html?_r=1&
- Goldstein, MR and Mascitelli, L. (2013, June). Do Statins Cause Diabetes? Current Diabetes Reports. Retrieved from http://www.ncbi.nlm.nih.gov/pubmed/23456437
- U.S. Food and Drug Administration. (2012, February). FDA Expands Advice on Statin Risks. Retrieved from http://www.fda.gov/
- Carter, A. et al. (2013, March 28). Risk of Incident Diabetes Among Patients Treated with Statins: Population Based Study. British Medical Journal. Retrieved from http://www.bmj.com/content/346/bmj.f2610
- Goldstein, M.R. and Mascitelli, L. (2013, June ). Do Statins Cause Diabetes? Current Diabetes Reports. Retrieved from http://www.ncbi.nlm.nih.gov/pubmed/23456437
- U.S. Food and Drug Administration. (2012, February). FDA Expands Advice on Statin Risks. Retrieved from http://www.fda.gov/
- Healy, M. (2012, January 10). Statins Raise Risk of Type 2 Diabetes in Older Women, Study Finds. Los Angeles Times. Retrieved from http://articles.latimes.com/2012/jan/10/health/la-he-statins-diabetes-20120110
- Rajpathak, S., Kumbhani, D., Crandall, J., Barzilai, N., Alderman, M. and Ridker, P. (2009, October). Statin Therapy and Risk of Developing Type 2 Diabetes: A Meta-Analysis. Diabetes Care. Retrieved from http://care.diabetesjournals.org/content/32/10/1924?ijkey=bb84477ea9e9e751c274d490054c566f6f385aa0&keytype2=tf_ipsecsha&linkType=ABST&journalCode=diacare&resid=32/10/1924&atom=/bmj/346/bmj.f2610.atom
- Simons, J. (2003, January 20). The $10 Billion Pill. Fortune Magazine. Retrieved from http://cnn.com/
- Boyles, S. (2012, January 10). Statins May Raise Diabetes Risk in Older Women. WebMD. Retrieved from http://www.cbsnews.com/news/statins-may-raise-diabetes-risk-in-older-wohealth/men/
- Nisen, M. (2012, June 28). The 10 Best Selling Prescription Drugs in the United States. Business Insider. Retrieved from http://www.businessinsider.com/10-best-selling-blockbuster-drugs-2012-6?op=1
- Kuepper, J. (2013, May 16). Finding the Next Big Blockbuster Drug. Retrieved from http://secfilings.com/News.aspx?title=finding_the_next_big_blockbuster_drug&naid=386
- Freeman, D et al. (2001). Pravastatin and the Development of Diabetes Mellitus. Circulation. Retrieved from http://circ.ahajournals.org/content/103/3/357.full
- American Diabetes Association. (n.d.). Facts About Type 2. Retrieved from http://www.diabetes.org/diabetes-basics/type-2/facts-about-type-2.html
- Topol, E. (2012, March 4). The Diabetes Dilemma for Statin Users. The New York Times. Retrieved from http://www.nytimes.com/2012/03/05/opinion/the-diabetes-dilemma-for-statin-users.html?_r=1&
- U.S. National Library of Medicine. (20105, August 15). Atorvastatin. Retrieved from https://medlineplus.gov/druginfo/meds/a600045.html
- Pfizer. (2010, December). Pfizer to Recall One Additional Lot of Lipitor in the U.S. Retrieved from http://www.pfizer.com/files/news/lipitor_recall_122010.pdf
- Gever, J. (2010, December 22). Pfizer Expands Lipitor Recall. Retrieved from http://abcnews.go.com/Health/Cholesterol/recall-cholesterol-drug-lipitor-expands/story?id=12459069
- U.S. Food & Drug Administration. (2017, February 16). Controlling Cholesterol with Statins. Retrieved from https://www.fda.gov/ForConsumers/ConsumerUpdates/ucm293330.htm
- U.S. Department of Health and Human Services. (2005, December). Your Guide to Lowering Cholesterol with TLC. Retrieved from https://www.nhlbi.nih.gov/files/docs/public/heart/chol_tlc.pdf
- U.S. Food & Drug Administration. (n.d.). Highlights of Prescribing Information. Retrieved from https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020702s065lbl.pdf