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Atorvastatin (Lipitor)

Atorvastatin is the second-most widely used statin drug with 21% of the US market. Sold under the brand name Lipitor it was the biggest of the blockbuster drugs of the 21st Century. The patent recently expired and the pharmaceutical industry is in the process of rolling out generic forms.

The long-term benefits of atorvastatin have been demonstrated in scientific study after study. In one European study, patients who had been given low (10 mg/day) doses of atoravastain were revisited by researchers long after the study was finished. Compared to untreated patients, the statin patients had lower death rates from even non-cardiovascular causes. These include respiratory problems and other common causes of death which the antiinflammatory effects of atorvastatin may help.

atorvastatin structure Many studies have established the effectiveness and safety of atorvastatin. Scientists have followed the health of tens of thousands of people on this medicine, in different countries. It lowers the mortality and risk of heart disease in patients with a history of cardiovascular problems. Whether it should be prescribed for patients with no history of problems or certain risk factors is a matter of debate within the medical community.

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 also have anti-inflammatory effects. 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 atorvastatin in the blood becomes bound to plasma proteins. In this way, the medicine and cholesterol are similar in the way they travel in the bloodstream.

Atorvastatin Regimen

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 in the Body

The medicine is absorbed in the intestine 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. 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 peak blood concentrations in about 2 weeks, leveling off if a constant dose 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.

Side effects

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, joint pain, and inflammation and pain in the pharynx and larynx.

Atorvastatin for Stroke Prevention

Statin medications reduce the risk of stroke in people with vascular disease. Incidences of ischaemic stroke decline, but probably not those of hemorrhagic stroke. Further, even after people have had a stroke or transitory ischemic attack, using statins reduces the risk of a second stroke.

Note that epidemiological studies have not shown a definitive association between cholesterol levels and stroke. It is possible that however statins stop strokes is through a different mechanism than how they reduce heart disease risk.

Patent expiration

The pharmaceutical company Pfizer held the US patent on atorvastatin for years and sold the medicine under the brand name Lipitor. They 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 billion was from the U.S. alone, where 3.5 million people took the drug.

In November 2011 the patent expired and the drug companies Watson and Ranbaxy now sell atorvastatin in the US. Ranbaxy now sells more atorvastatin pills than Pfizer does. The Israeli generic pharmaceutical company Teva Pharmaceutical announced announced it would not move into the atorvastatin market.

Other sellers must still meet government standards for safety and efficacy. The price of the generic atorvastatin is substantially lower than the price of branded Lipitor. If you still take branded Lipitor, ask your doctor or insurance company about switching to the generic version. Also be sure to check different retail pharmacies in your area because the price of even the generic form can vary considerably.

Facts

Formula: C33H35FN2O5
Category: synthetic, Type I
Manufacture: chemical synthesis
Solubility: water
Introduction: 1996
Brands: Lipitor, Atovarol, Tahor, and Sortis

A combination of atorvastatin and the calcium channel blocker high blood pressure drug amlodipine is sold under the name Caduet.

 

Comparative Effectiveness of Generic Atorvastatin and LipitorĀ® in Patients Hospitalized With an Acute Coronary Syndrome.

Sympathoinhibition by atorvastatin in hypertensive patientsAtorvastatin Ameliorates Cardiac Injury and Inflammation via Adiponectin-independent Activation of AMP-activated Protein Kinase and Inhibition of the Nf-?B Pathway in Rats With Metabolic Syndrome.

Medline

 

 

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