Lipitor: What You Need to Know

Name that drug.
Associated Press/Amy Sancetta

If you take Lipitor to lower your cholesterol, you're not alone. More than 29 million people have been prescribed Lipitor, making it the No. 1 prescribed cholesterol medication in the world [source: Lipitor]. And since high cholesterol is a concern for so many, it's the highest-selling drug in the world, with sales well over $10 billion a year [source: Loftus]. If you're not on Lipitor, you may wonder what all the fuss is about. After all, Lipitor isn't the only cholesterol-reducing medication on the market, and it's certainly not the cheapest. Is there really anything that special about it?

You'd be in good company if you had those questions -- even Lipitor's creators weren't sure their new drug would make much of a dent on the market. Created by Parke-Davis (a company owned by pharmaceutical Warner-Lambert), Lipitor was a late entry into the cholesterol management market. Its development was marked by setbacks, including an early formula that essentially contained 50 percent waste material (material that had no health benefits) and mediocre results in animal studies [source: Winslow]. In those early studies, the drug performed exactly the same as other medications on the market. Though Parke-Davis created a process for eliminating the excess from the compound, there were still questions of whether the drug should move forward in testing. Was it worth it?


As you might guess from the first paragraph, it certainly was worth it. While the animal studies provided disappointing results, Lipitor immediately showed great promise for humans. In a study of 24 people, just 10 milligrams of Lipitor lowered counts of LDL, or bad cholesterol, by 38 percent, and at 80 milligrams, LDL was decreased by 58 percent [source: Winslow]. In both instances, these were significantly higher results than any other drug in this class could provide, even at higher doses.

Even with incredible results, Warner-Lambert still wasn't sure the drug could successfully enter the cholesterol market. The company partnered with Pfizer for marketing purposes, and due to the success of Lipitor, Pfizer acquired Warner-Lambert in 2000. Pfizer is known for its aggressive marketing practices, particularly its direct campaigns to doctors [source: Simons]. So is the success of Lipitor due to a great ad campaign or actual results? We'll take a look at what Lipitor does in your body on the next page.


Lipitor at Work in Your Body

Lipitor's starting dose is just 10 milligrams.
Associated Press/Paul Sakuma

Lipitor is in a class of cholesterol-lowering drugs known as statins. Statins were created in Japan in the early 1970s, after research showed that an enzyme called hydroxyl-methylglutaryl-coenzyme A (HMG-CoA), located in the liver, produced as much as 80 percent of the cholesterol count in the body. While people can directly affect 20 percent of their cholesterol count by watching their diet, there was nothing on the market that directly went after that cholesterol-creating machine.

The first statin, mevastatin, was developed in Japan in 1971, and several others followed over the years. Lipitor is the marketing name for atorvastatin. Statins work by inhibiting HMG-CoA. Not only does that reduce the amount of cholesterol that's produced, it means that the liver pulls some of that extra cholesterol out of the blood stream. In this way, your overall cholesterol count is lowered.


What differentiates Lipitor from other statins is that it reduces more cholesterol at lower doses compared to the competition. The typical starting dose for Lipitor is 10 milligrams daily, and it can be prescribed at levels of up to 80 milligrams daily, whereas other statins are typically prescribed in amounts of 20 to 40 milligrams daily. When doctors first began prescribing statins, many were worried about long-term effects of high doses of statins, so some of Lipitor's early success is somewhat psychological: Doctors were able to rationalize that if 80 milligrams was safe, then 10 milligrams must be extremely safe [source: Simons]. Scientists who developed the compound attribute the potency of the low dose to a longer half-life of the drug, which means it works in the body longer [source: Winslow].

Currently, there is no generic version of Lipitor. If you want the patented formula that has been shown to reduce bad cholesterol by as much as 60 percent, then you have to pay more [source: Lipitor]. Much of Pfizer's current marketing campaign is meant to show you that no other statin will work in your system the way that Lipitor will, and that it's not worth switching to a cheaper generic prescription. As of now, studies show that atorvastatin is more potent than its generic rivals and may have additional benefits, such as a lowered risk of heart disease [source: Berenson].

Just who should be taking Lipitor? Find out on the next page.


Lipitor Indications

man with hamburger and soda
Lipitor should be combined with a healthy diet, unlike the one seen in this photograph.

Lipitor is a medication used to lower bad cholesterol, more formally known as low-density lipoprotein (LDL). The drug is meant to be used in addition to an exercise regime and a healthy diet; you can't, in other words, take Lipitor and eat whatever you want without any effect on cholesterol. For some people, though, diet and exercise may not be enough to control cholesterol, because so much of it is made by the body.

Maintaining healthy levels of cholesterol has an enormous impact on your heart health, and unlike risk factors such as age or family history, cholesterol counts are a manageable risk factor for heart disease. High cholesterol levels in the blood can clog arteries, leading to a heart attack. Lipitor could lower bad cholesterol by 39 to 60 percent, depending on the dosage [source: Lipitor].


Lipitor also works to a lesser extent to increase high-density lipoproteins (HDL), or the good cholesterol; the medication has been shown to raise HDL by 5 to 9 percent [source: Lipitor]. Lowered levels of this good cholesterol can also increase the risk of heart disease, because HDL carries away extra cholesterol to the liver, thus removing it from the bloodstream and lowering your cholesterol count.

Because Lipitor reduces the risk of heart disease, the U.S. Food and Drug Administration (FDA) has recognized Lipitor as a way to reduce the risk of heart attack, certain kinds of heart surgeries and chest pain. It's also an approved way to reduce the risk of strokes, which are like heart attacks in the brain. While Lipitor can help stave off that first stroke, it's also an effective way to prevent a possible second. In a 2006 study published in the New England Journal of Medicine, researchers found that patients taking Lipitor after their first stroke saw a 16 percent reduction in the risk of another stroke compared to subjects taking a placebo [source: Rosalind Franklin University of Medicine and Science].

On the next page, we'll explore some side effects commonly associated with Lipitor.


Lipitor Side Effects

woman with muscle pain
If you have unexplained muscle pain after starting Lipitor, see a doctor.

Common side effects of Lipitor include headache, constipation, diarrhea, gas, stomach pains, rash and muscle pain.

In some cases, those muscle pains may indicate a more serious side effect: A small percentage of patients had muscle problems so serious that developed rhabdomyolysis. This condition causes muscles to break down, emitting proteins in the process that lead to kidney failure. The chance of this side effect increases if you're taking certain other medications in addition to Lipitor, so, as with any prescription drug, you should tell your doctor about other medications you may be taking.


One other serious side effect is liver problems. If you already have liver problems, you shouldn't take Lipitor, and your doctor may perform blood tests during the time you're on Lipitor to monitor your liver. Signs of these serious side effects include extreme muscle weakness and tenderness, nausea and vomiting, dark-colored urine, unusual exhaustion, yellow eyes or skin, and stomach pain.

Pregnant and breastfeeding women shouldn't take Lipitor. However, a 2008 study raises the question of whether Lipitor has any benefit at all for women. The authors of the study, which was published in the Journal of Empirical Legal Studies, claimed that proof that Lipitor reduces the risk of heart attack in women is lacking [source: Wiley-Blackwell]. Rather, the authors asserted, Pfizer was marketing the drug as beneficial to both genders and not disclosing the portion of the FDA-sanctioned label that admitted the evidence for women was lacking [source: Wiley-Blackwell].

The question of whether women should take Lipitor becomes important when you consider the possibility that the drug might result in memory loss in women. In 2008, Dr. Orli Etingin, vice chairman of medicine at New York Presbyterian Hospital, said, "This drug makes women stupid" [sources: Cahoon, Beck]. The quote, which was picked up by several media outlets, spurred many doctors to speak in defense of Lipitor. These doctors claimed that any evidence of memory loss linked to Lipitor was purely anecdotal, and that its benefits far outweigh this potential side effect. Because more studies on statins and cognitive effects are needed, it's worth asking your doctor about the latest research if you're concerned.

You can avoid some of Lipitor's more dangerous side effects by staying away from one substance. Find out what it is on the next page.


Lipitor and Grapefruit

grapefruit with glass of juice
Sorry, grapefruit lovers. The fruit and its juice are off-limits when you're on certain medications.

If you like starting the day with a big glass of refreshing grapefruit juice, that morning tradition will have to be one of the dietary habits you change when you start taking Lipitor. Even though the habit sounds healthy enough, it could have life threatening consequences. Lipitor is one of many drugs that has adverse effects when combined with grapefruit juice.

­When grapefruit juice is consumed, it's metabolized by certain enzymes in the liver -- the same enzymes that break down Lipitor in your body. Essentially, if the enzymes are too busy metabolizing the grapefruit juice, then the medication can't be broken down, which results in an overabundance of it in your system. That can lead to some of the more serious side effects we mentioned on the previous page, such as rhabdomyolysis, in which muscle pain leads to kidney problems.


In 2006, researchers at UNC-Chapel Hill identified chemicals known as furanocoumarins as the substance in grapefruit juice that might be tying up those enzymes, which means there's a potential for furanocoumarin-free grapefruit juice in the future [source: University of North Carolina School of Medicine]. Until then, check the warning label on all of your prescription drugs carefully; grapefruit juice can have negative interactions with about 50 medications [source: University of Rochester Medical Center]. This is also the perfect time to find a new favorite juice, as grapefruit juice is the only fruit juice that reacts negatively with medications.

For more information on popular prescription drugs, see the links on the next page.



Lots More Information

Related HowStuffWorks Articles

  • "Atorvastatin." MedlinePlus. Aug. 1, 2008. (Feb. 10, 2009)
  • Beck, Melinda. "Can a Drug That Helps Hearts Be Harmful to the Brain?" Wall Street Journal. Feb. 12, 2008. (Feb. 9, 2009)
  • Berenson, Alex. "Lipitor or Generic? Billion-Dollar Battle Looms." New York Times. Oct. 15, 2005. (Feb. 10, 2008)
  • Cahoon, Lauren. "Doctors Discredit Lipitor's Link to Memory Loss." ABC News. Feb. 13, 2008. (Feb. 10, 2009)
  • Lipitor Web site. (Feb. 10, 2009)
  • Loftus, Peter. "Pfizer's Lipitor Patent Reissue Rejected." Wall Street Journal. Aug. 16, 2007. (Feb. 10, 2009)
  • Rosalind Franklin University of Medicine and Science. "Aggressive Reduction in Cholesterol Levels Can Reduce Risk For Stroke by 16 Percent." ScienceDaily. Aug. 10, 2006. (Feb. 10, 2009)­/releases/2006/08/060809235129.htm
  • Simons, John. "The $10 Billion Pill." Fortune. Jan. 20, 2003.
  • University of North Carolina School of Medicine. "Study Identifies Substances in Grapefruit Juice That Interact Dangerously With Some Drugs." ScienceDaily. May 9, 2006. (Feb. 9, 2009)­/releases/2006/05/060509094500.htm
  • University of Rochester Medical Center. "Grapefruit Juice and Medication Can Be a Dangerous Mix." ScienceDaily. Jan. 26, 2005. (Feb. 10, 2009)­/releases/2005/01/050124010803.htm
  • Wiley-Blackwell. "Top-selling Cholesterol Drug Does Little for Women, Study Suggests." ScienceDaily. Sept. 18, 2008. (Feb. 10, 2009)­/releases/2008/09/080917145147.htm
  • Winslow, Ron. "Birth of a Blockbuster: Lipitor's Unlikely Route out of the Lab." Wall Street Journal. Jan. 24, 2000.