Atorvastatin (Lipitor)

Atorvastatin is the most widely used statin drug. Is it different from other statins? A little.

The commercial preparation is atorvastatin calcium. (The calcium is the anion part of the salt. Prescription drugs are frequently sold as salts. This drug is not a major source of dietary calcium.)

Atorvastatin is available in 10, 20, 40, and 80 mg tablets. Most patients take 10 or 20 mg per day. Your doctor will prescribe a dosage based on many factors. Some patients need 40 mg/day and 80 mg daily is given to patients with acute coronary syndrome.

Atorvastatin interacts with many other drugs. Be sure to tell your doctor about ALL prescription drugs and over-the-counter drugs that you take. Patients with a history of hemorrhagic stroke may be at increased risk for another stroke.

Like all statins, atorvastatin works in the liver, by inhibiting enzymes that make cholesterol. It is taken as a pill, and the concentration of the drug in the bloodstream peaks an hour or two after the pill is ingested. Guidelines suggest you eat a little food with the pill as this tends to slow the absorption from the digestive system. Almost all the atovastatin in the blood is bound to plasma proteins. In this way, the medicine and cholesterol are similar in the way they travel in the bloodstream.

Atorvastatin in the Body

The medicine is absorbed in the instestine and once in the bloodstream, most is metabolized. Less than 2% is removed by the kidneys. After ingestion, peak bloodstream concentration is in 60 to 120 minutes. The half-life is 14 hours for atorvastatin. Equipotent metabolites have a half-life of 20-30 hours. The half-life is longer than the half-life of simvastatin. Unlike that drug, atorvastatin can be taken in the morning because of its long half-life, but most doctors recommend it be swallowed in the evening.

The drug starts to work several days after the patient starts taking it and achieves peaks in about 2 weeks, leveling off if a constant dosaging is maintained.

Atorvastatin is not approved for pregnant women, and is not considered safe for fetuses. Like other statins, atorvastatin can be taken with meals.

Patients who drink large amounts of alcohol or have a history of liver disease are sometimes not prescribed atorvastatin because of concerns about the drug's effect on the liver.

Like other statins, the side effects that are of most concern involve the liver (requiring periodic check of transaminase levels in the blood) and muscle damage. Other common atorvastatin side effects are diarrhea, arthralgia, and inflammation and pain in the pharynx and larynx.

Other Resources

Pfizer's Lipitor site

Mayo Clinic

Medline

PubMed

Patent expiration

The pharmaceutical company Pfizer held the US patent on atorvastatin for years and sold it undetrthe brand name Lipitor. The sold billions of dollars of Lipitor. It was Pfizer's biggest selling product and indeed the single biggest selling drug (in terms of revenues) during the 2000s. Pfizer reportedly sold $10.7 billion worth of Lipitor in 2010. $7 billon was from the U.S. alone, where 3.5 million people take the drug.

In November 2011 the patent expired and the drug companies Watson and Ranbaxy now sell atorvastatin in the US. In 2012 other companies will be able to do the same.

Other sellers must still meet government standards for safety and efficacy. The price of the generic atorvastatin should be substantially lower. In the case of Zocor/simvastatin, the generic version is about one-fourth the price of the brand name. The price of the brand name drug might fall, but that depends on Pfizer's marketing strategy.

Now that the patent has expired, will the price decline? Maybe. History shows that the price of Zocor (simvastatin) declined once a generic product hit the market, but not as much as observers had predicted. The brand name seems to command some premium, as Zocor costs most than the generic equivalent.

Brand Names for Atorvastatin

Pfizer sells atorvastatin in the US under the name Lipitor. Other brand names used around the world include Lipodar, Atovarol, Tahor, and Sortis. A combination of atorvastatin and the calcium channel blocker high blood pressure drug amlodipine is sold under the name Caduet.

Acute effects of atorvastatin on glomerular filtration rate, tubular function, blood pressure, and vasoactive hormones in patients with type 2 diabetes.

Sympathoinhibition by atorvastatin in hypertensive patients.

Side effects of stain drugs