Atorvastatin (Lipitor)

Lipitor is the brand name for 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.)

Lipitor is the single biggest selling (in terms of total dollars) prescription drug in the world today. Annual global sales exceed $12 billion. It is the single biggest moneymaker for the biggest pharmaceutical company (Pfizer), making up over a quarter of that company’s sales. In 2010 the company started closing plants and laying off workers in anticipation of the expiration of the patent. The plant at Loughberg in County Cork, Ireland, where Lipitor is made, was announced as one of the plants to close.

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.

The cost is pretty high. A 2010 check of an online pharmacy showed the price of 10 mg tablets was $96 for a 30-day supply. The price of 20 mg tablets was $136 for a 30-day supply.

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 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.

What happens after the patent expires?

Right now Lipitor is under patent in the major countries. The patent in the US will expire in November 2011; until then only Pfizer can legally sell atorvastatin in the United States. Pfizer has told its investors it is already planning to cut costs in anticipation of a decline in revenue when the patent expires.

After patent expiration other manufacturers besides Pfizer will be able to sell the drug. 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.

Pfizer is advertising a website at www.onlylipitor.com to try to maintain its brand strength. The domain redirects to the main lipitor.com site where the title of the page says "There Is No Generic Form of LIPITOR". This page is apparently directed at consumers, not health professionals.

Earlier there were hopes that generic atorvastatin could be available in the US by March 2010, sold by Ranbaxy Laboratories. Pfizer settled disputes with Ranbaxy and there won’t be generic atorvastatin in the drugstores until late 2011. Under the agreement between the two companies, Ranbaxy will be able to sell the generic product in Canada and some European countries before the patent expires in the United States. So Canadians will get the generic drug earlier than Americans. The Federal Trade Commission disapproves of deals in which pharmaceutical companies pay each other off to keep generic drugs off the market, but Pfizer says this agreement will pass FTC scrutiny.

After patent expiration, 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

Atorvastatin is sold in the US only under the name Lipitor. This will be true until the patent expires or unless Pfizer sells it under another name. Other brand names used around the world include Lipodar, Atovarol, Tahor, and Sortis.

Side effects of stain drugs