Lipitor Information

* What is Lipitor (atorvastatin calcium) ?
* How does Lipitor work?
* How does Lipitor improve the different types of cholesterol?
* What are the effects of Lipitor tablets?
* What would I need to know about taking Lipitor?
* How long does it take Lipitor to work?
* Who should not take Lipitor tablets?
* Does Lipitor interact with any other drugs?
* What about side effects?
* Are there any contraindicatons to taking Lipitor?

Lipitor is a prescription drug in one of the newest classes of cholesterol-lowering medications, called statins. These drugs have been used widely for the last 5 years. For people with high cholesterol, Lipitor, in combination with a low-fat diet, can reduce your LDL cholesterol and triglyceride levels.

How does Lipitor work?

 Lipitor works by blocking an enzyme in the liver that your body uses to make cholesterol. When less cholesterol is produced, the liver takes up more cholesterol from the bloodstream. This results in lower levels of cholesterol circulating in your blood. (Lipitor is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. Cholesterol andtriglycerides circulate in the bloodstream as part of lipoprotein complexes. With ultracentrifugation, these complexesseparate into HDL (high-density lipoprotein), IDL (intermediate-density lipoprotein), LDL (low-density lipoprotein),and VLDL (very-low-density lipoprotein) fractions. Triglycerides (TG) and cholesterol in the liver are incorporated intoVLDL and released into the plasma for delivery to peripheral tissues. LDL is formed from VLDL and is catabolized primarily through the high-affinity LDL receptor. Clinical and pathologic studies show that elevated plasma levels of total }cholesterol (total-C), LDL-cholesterol (LDL-C), and apolipoprotein B (apo B) promote human atherosclerosis and are risk factors for developing cardiovascular disease, while increased levels of HDL-C are associated with a decreased cardiovascular risk.

 

How does Lipitor improve the different types of cholesterol?

In medical studies of people with high cholesterol, Lipitor, taken once a day, had the following effects at doses of 10 to 80 mg:

• Lowered total cholesterol by 29%-45%.
• Lowered LDL cholesterol, the "bad" cholesterol, by 39%-60%.
• Increased HDL cholesterol the "good" cholesterol, by 5%-9%.
• Lowered triglyceride levels by 19%-37%.

What are the effects of Lipitor tablets?

Lipitor is a very effective medicine for lowering high LDL cholesterol—the main target of cholesterol-lowering therapy. Your doctor will determine how much your LDL cholesterol needs to be lowered, based on your overall risk of heart disease Lipitor also effectively lowers high blood-triglyceride levels.

What would I need to know about taking Lipitor?

Most people will require the starting dose, which is a 10 mg tablet once daily. Your doctor will prescribe the dose that is right for you, which may be 10 mg to 80 mg. Lipitor can be taken any time of the day, with or without food. To make it easier to remember to take Lipitor you can plan to take it at the same time each day, such as after you brush your teeth in the evening. The amount or how often Lipitor is taken should never be changed without consulting your healthcare professional

How long does it take Lipitor to work?

Generally, Lipitor works within 2 weeks. The full effect is usually seen within 4 weeks and lasts as long as you continue taking it. Always take LIPITOR® as directed by your healthcare professional.

Who should not take Lipitor tablets?

Some people should not take Lipitor. Those with active liver disease or possible liver problems; women who are pregnant, could possibly become pregnant, or are breast-feeding; and people who are allergic to any of the ingredients in Lipitor.

Does Lipitor interact with any other drugs?

If you take Lipitor with certain other medicines, they may affect one another. Lipitor may interact with certain other cholesterol-lowering drugs, some antibiotics, and antifungal medications. It may also interact with less-frequently prescribed medications such as immunosuppressives (given after transplants). Be sure to tell your doctor or pharmacist about all prescription and nonprescription drugs you are taking.

What about side effects?

 Lipitor is generally well tolerated and side effects are usually mild. In studies, the most common side effects associated with Lipitor were constipation, flatulence, indigestion, and abdominal pain. If you are prescribed Lipitor your healthcare professional may want to conduct routine blood tests to check your liver function before and after starting treatment.

Be sure to tell your healthcare professional if you have any allergies to food or medication. Also, report promptly any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by discomfort or fever, as these symptoms may be signs of serious side effects.

For additional information about taking Lipitor along with other medicines, see your doctor or pharmacist. If you experience side effects, be sure to tell your doctor or other healthcare professional.

Are there any contraindicatons to taking Lipitor?

 Individuals who have active liver disease or unexplained persistent elevations of serum transaminases should not take the medication. Concerning women of child bearing age, since the active ingredient in Lipitor, HMG-CoA reductase inhibitors, decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, they may cause fetal harm when administered to pregnant women.Therefore, HMG-CoA reductase inhibitors are contraindicated during pregnancy and in nursing mothers. ATORVASTATIN SHOULD BE ADMINISTERED TO WOMEN OF CHILDBEARING AGE ONLY WHEN SUCH PATIENTS ARE HIGHLY UNLIKELY TO CONCEIVE AND HAVE BEEN INFORMED OF THE POTENTIAL HAZARDS. If the patient becomes pregnant

while taking this drug, therapy should be discontinued and the patient apprised of the potential hazard to the fetus. In addition, individuals that have any know hypersensitivity to any component of the medication should also refrain from taking Lipitor.

Are there any medications that significantly react with Lipitor? 

The risk of myopathy during treatment with Lipitor is increased with concurrent administration of cyclosporine, fibric acid derivatives, niacin (nicotinic acid), erythromycin, azole antifungals.

Antacid: When atorvastatin and Maalox® TC suspension were coadministered, plasma concentrations of atorvastatin decreased approximately 35%. However, LDL-C reduction was not altered.

Antipyrine: Because Lipitor does not affect the pharmacokinetics of antipyrine, interactions with other drugs metabolized via the same cytochrome isozymes are not expected.

Colestipol: Plasma concentrations of Lipitor decreased approximately 25% when colestipol and atorvastatin were coadministered. However, LDL-C reduction was greater when Lipitor and colestipol were coadministered

than when either drug was given alone.

Cimetidine: Lipitor plasma concentrations and LDL-C reduction were not altered by coadministration of cimetidine.

Digoxin: When multiple doses of Lipitor and digoxin were coadministered, steady-state plasma digoxin concentrations increased by approximately 20%. Patients taking digoxin should be monitored appropriately.

Erythromycin: In healthy individuals, plasma concentrations of Lipitor increased approximately 40% with coadministration of Lipitor and erythromycin, a known inhibitor of cytochrome P450 3A4.

Oral Contraceptives: Coadministration of Lipitor and an oral contraceptive increased AUC values for norethindrone and ethinyl estradiol by approximately 30% and 20%. These increases should be considered when selecting an oral contraceptive for a woman taking atorvastatin.

Warfarin: Atorvastatin had no clinically significant effect on prothrombin time when administered to patients receiving chronic warfarin treatment.