Generic Name: atorvastatin

Atorvastatin is in a group of drugs called HMG CoA reductase inhibitors, or “statins.” Atorvastatin reduces levels of “bad” cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood while increasing levels of “good” cholesterol (high-density lipoprotein, or HDL).

Atorvastatin is used to treat high cholesterol, and to lower the risk of heart disease (stroke, heart attack) and blood vessel disease (including heart disease and stroke) in people with type 2 diabetes or coronary heart disease.

You should not take atorvastatin if you are allergic to it, or if you have liver disease.

Do not take atorvastatin if you are pregnant or breastfeeding.

To make sure atorvastatin is safe for you, tell your doctor if you have ever had liver or kidney disease, diabetes, or a thyroid disorder.

Do not take atorvastatin with other medicines that contain niacin (Advicor, Niaspan, Niacor, Slo-Niacin, and others).

Atorvastatin can harm an unborn baby or cause birth defects. Do not use if you are pregnant. Stop taking this medicine and tell your doctor right away if you become pregnant. Use effective birth control to prevent pregnancy while you are taking this medicine.

If you are a woman of childbearing age, you should have a negative pregnancy test before starting this treatment. You will need to take a pregnancy test every month during your treatment.

You may need to stop taking atorvastatin for a short time before having surgery or blood tests.

Your liver function may need to be tested often. You may need blood tests to check your liver function for several months after you stop using this medicine.

If you have diabetes, atorvastatin may affect your blood sugar levels. Check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.

Drug Interactions

Fiber, certain antacids, and cholesterol-lowering medicines can make it harder for your body to absorb atorvastatin. Avoid eating foods that are high in fat or cholesterol. Atorvastatin should be taken at night because that’s when your liver makes most LDL cholesterol.

Taking atorvastatin with certain other medicines can cause serious side effects. Your doctor may need to change your dose or monitor you more carefully for side effects. These include:

* Niacin (Advicor, Niaspan, Niacor, Slo-Niacin, and others)

* Other medicines to treat high cholesterol or triglycerides

* Antibiotics

* HIV protease inhibitors such as ritonavir (Norvir), atazanavir (Reyataz), or find inavir (Crixivan)

* An antifungal medicine such as ketoconazole (Nizoral), itraconazole (Spor anox), posaconazole (Noxafil), voriconazole (Vfend), or fluconazole (Diflucan)

* A seizure medicine such as carbamazepine (Carbatrol, Epitol, Equetro, Tegretol), phenobarbital (Luminal), or phenytoin (Dilantin, Phenytek)

* The hepatitis C protease inhibitor boceprevir (Victrelis)

* A heart rhythm medicine such as amiodarone (Cordarone), diltiazem (Cartia, Cardizem), quinidine (Quin-G), procainamide (Procanbid), or verapamil (Calan, Covera, Isoptin, Verelan)

* A blood thinner such as warfarin (Coumadin, Jantoven)

Pharmacokinetics

Atorvastatin is rapidly absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. The bioavailability of atorvastatin is approximately 14%.

Peak plasma concentrations of atorvastatin are achieved within 1 to 2 hours following oral administration.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

In rats and mice given atorvastatin for 18 months or longer, there was an increased incidence of testicular tumors. The significance of this finding to humans is unknown. Atorvastatin was not mutagenic in the Ames bacterial mutation assay with or without metabolic activation. It was also negative in an in vitro assay using human lymphocytes and in two mouse micronucleus assays. Atorvastatin had no effect on fertility or reproductive performance in rats at oral doses up to 18 times the human exposure (based on AUC0-24).

Clinical Studies

Adults

The efficacy of atorvastatin was examined for up to 6 years in 5 large, well-controlled trials involving a total of 18,686 patients. The primary endpoint was the change from baseline in LDL-C. In each trial, atorvastatin reduced LDL-C by approximately 50%. HDL-C and triglyceride levels were also reduced.

The effect of atorvastatin on LDL-C was dose-related, with maximum reductions achieved at the highest dose studied.

Side Effects

The most common side effects of atorvastatin are:

* headache

* muscle aches and pain

* diarrhea

* constipation

* nausea or vomiting

* stomach pain or upset

* skin rash or itching

These side effects usually go away after a few days. If they don’t, or if you have any other side effects, check with your doctor.

Serious Side Effects

Call your doctor right away if you have any serious side effects, including:

* yellowing of the skin or eyes

* dark urine

* pain in the upper right part of the stomach

* flu-like symptoms

* unusual tiredness or weakness

* easy bruising or bleeding

* mental or mood changes

These could be signs of a rare but serious liver problem.

Dosage and Administration

The recommended dose of atorvastatin is 10 to 80 mg once daily. The starting dose should be 10 mg for patients who are likely to require a lower starting dose (e.g., patients already taking another statin, patients with renal impairment, and female patients). For all other patients, the starting dose should be 40 mg.

The dose of atorvastatin should be individualized to obtain the desired LDL-C reduction. The usual target LDL-C level is less than 100 mg/dL.

Atorvastatin may be taken at any time of day, with or without food. If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of atorvastatin at the same time.

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 999. Otherwise, call a poison control center right away.

Storage

Store atorvastatin at room temperature away from moisture and heat.