Atorvastatin

What is Atorvastatin?

• Atorvastatin (Lipitor) is an HMG-CoA reductase inhibitor used to lower cholesterol in your blood.

Atorvastatin

Atorvastatine Structural Formula V1

Atorvastatin-3D-animated

Atorvastatin-1HWK-3D-balls

What are the uses of this medicine?

Atorvastatin (Lipitor) is used as an adjunct therapy to diet to:

• Reduce the risk of MI, stroke, revascularization procedures, and angina in adult patients without CHD, but with multiple risk factors.
• Reduce the risk of MI and stroke in adult patients with type 2 diabetes without CHD, but with multiple risk factors.
• Reduce the risk of non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for CHF, and angina in adult patients with CHD.
• Reduce elevated total-C, LDL-C, apo B, and TG levels and increase HDL-C in adult patients with primary hyperlipidemia (heterozygous familial and nonfamilial) and mixed dyslipidemia.
• Reduce elevated TG in adult patients with hypertriglyceridemia and primary dysbetalipoproteinemia.
• Reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH).
• Reduce elevated total-C, LDL-C, and apo B levels in pediatric patients, 10 years to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH) after failing an adequate trial of diet therapy.

Atorvastatin calcium tablets can lower the risk for heart attack, stroke, certain types of heart surgery, and chest pain in patients who have heart disease or risk factors for heart disease such as:

• age, smoking, high blood pressure, low HDL-C, heart disease in the family.

Atorvastatin calcium tablets can lower the risk for heart attack or stroke in patients with diabetes and risk factors such as:

• eye problems, kidney problems, smoking, or high blood pressure.
• Atorvastatin calcium tablets start to work in about 2 weeks.

Limitations of Use:

• Atorvastatin calcium tablets have not been studied in Fredrickson Types I and V dyslipidemias.

How does this medicine work?

• Atorvastatin (a tor" va stat' in) is a potent, orally available inhibitor of hepatic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the major rate-limiting enzyme in cholesterol synthesis.
• Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis.
• This agent increases the number of LDL receptors on hepatic cell surfaces, enhancing the uptake and catabolism of LDL and reducing LDL production and the number of LDL particles, and lowers plasma cholesterol and lipoprotein levels.
• Like other statins, atorvastatin may also display direct antineoplastic activity, possibly by inhibiting farnesylation and geranylgeranylation of proteins such as small GTP-binding proteins, which may result in the arrest of cells in the G1 phase of the cell cycle.
• This agent may also sensitize tumor cells to cyctostatic drugs, possibly through the mTOR-dependent inhibition of Akt phosphorylation.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are pregnant or think you may be pregnant, or are planning to become pregnant.
• are breastfeeding. Atorvastatin can pass into your breast milk and may harm your baby.
• have liver problems.
• are allergic to atorvastatin calcium tablets or any of their ingredients.

• Atorvastatin calcium tablet dosing has not been established in children under 10 years of age.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• antifungal medications such as itraconazole (Sporanox) and ketoconazole (Nizoral)
• boceprevir (Victrelis)
• cimetidine (Tagamet)
• clarithromycin (Biaxin)
• cobicistat-containing medications (Stribild)
• colchicine (Colcrys)
• digoxin (Lanoxin)
• efavirenz (Sustiva, in Atripla)
• oral contraceptives (birth control pills)
• other cholesterol-lowering medications such as fenofibrate (Tricor), gemfibrozil (Lopid), and niacin (nicotinic acid, Niacor, Niaspan)
• certain HIV protease inhibitors such as darunavir (Prezista), fosamprenavir (Lexiva), lopinavir (in Kaletra), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra), saquinavir (Invirase), and tipranavir (Aptivus)
• medications that suppress the immune system such as cyclosporine (Neoral, Sandimmune)
• rifampin (Rifadin, Rimactane)
• spironolactone (Aldactone)
• telaprevir (Incivek)

Is this medicine FDA approved?

• Atorvastatin was approved for use in the United States in 1996 and has become one of the most commonly prescribed drugs in America, with more than 50 million prescriptions filled yearly.

How should this medicine be used?

Recommended dosage:

• Dose range: 10 to 80 mg once daily.
• Recommended start dose: 10 or 20 mg once daily.
• Patients requiring large LDL-C reduction (> 45%) may start at 40 mg once daily.
• Pediatric patients with HeFH: starting dose: 10 mg once daily; dose range: 10 to 20 mg/day for patients 10 years to 17 years of age

Administration:

• Atorvastatin comes as a tablet to take by mouth.
• It is usually taken once a day with or without food.
• Take atorvastatin at around the same time every day.
• Take atorvastatin calcium tablets exactly as prescribed by your doctor.
• Do not change your dose or stop atorvastatin calcium tablets without talking to your doctor.
• Your doctor may do blood tests to check your cholesterol levels during your treatment with atorvastatin calcium tablets.
• Your dose of atorvastatin calcium tablets may be changed based on these blood test results.
• Don't break atorvastatin calcium tablets before taking.
• Your doctor should start you on a low-fat diet before giving you atorvastatin calcium tablets.
• Stay on this low-fat diet when you take atorvastatin calcium tablets.
• If you miss a dose of atorvastatin calcium tablets, take it as soon as you remember.
• Do not take atorvastatin calcium tablets if it has been more than 12 hours since you missed your last dose.
• Wait and take the next dose at your regular time.
• Do not take 2 doses of atorvastatin calcium tablets at the same time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 10, 20, 40, and 80 mg of atorvastatin

This medicine is available in fallowing brand namesː

• Lipitor

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea, upset stomach, muscle and joint pain, and alterations in some laboratory blood tests.

The following additional side effects have been reported with atorvastatin calcium tablets:

• tiredness, tendon problems, memory loss, and confusion.

Atorvastatin calcium tablets can cause serious side effects which may include:

• Muscle problems
• Liver problems

What special precautions should I follow?

• Atorvastatin calcium tablets may cause myopathy (muscle pain, tenderness, or weakness with creatine kinase (CK) above ten times the upper limit of normal) and rhabdomyolysis (with or without acute renal failure secondary to myoglobinuria). Risks increase when higher doses are used concomitantly with cyclosporine and strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, human immunodeficiency virus (HIV) or hepatitis C virus (HCV) protease inhibitors). Predisposing factors include advanced age (> 65), uncontrolled hypothyroidism, and renal impairment. Rare cases of rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported. Advise patients to promptly report to their physician unexplained and/or persistent muscle pain, tenderness, or weakness. Atorvastatin calcium tablet therapy should be discontinued if myopathy is diagnosed or suspected.
• There have been rare reports of Immune-Mediated Necrotizing Myopathy (IMNM), an autoimmune myopathy, associated with statin use. IMNM is characterized by: proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; positive anti-HMG CoA reductase antibody; muscle biopsy showing necrotizing myopathy; and improvement with immunosuppressive agents.
• Statins, like some other lipid-lowering therapies, have been associated with biochemical abnormalities of liver function. Persistent elevations in hepatic transaminases can occur. Check liver enzyme tests before initiating therapy and as clinically indicated thereafter.
• A higher incidence of hemorrhagic stroke was seen in patients without CHD but with stroke or TIA within the previous 6 months in the atorvastatin calcium tablets 80 mg group vs. placebo.
• Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors, including atorvastatin calcium tablets. Caution should be exercised if a statin is administered concomitantly with drugs that may decrease the levels or activity of endogenous steroid hormones, such as ketoconazole, spironolactone, and cimetidine.
• Advise women not to breastfeed during treatment with atorvastatin calcium tablets.
• It is recommended that liver enzyme tests be performed before the initiation of atorvastatin calcium tablets and if signs or symptoms of liver injury occur. All patients treated with atorvastatin calcium tablets should be advised to report promptly any symptoms that may indicate liver injury, including fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice.
• Do not get pregnant. If you get pregnant, stop taking atorvastatin calcium tablets right away and call your doctor.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• There is no specific treatment for atorvastatin calcium tablet overdosage.
• In the event of an overdose, the patient should be treated symptomatically, and supportive measures instituted as required.
• Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance atorvastatin clearance.

Can this medicine be used in pregnancy?

• Atorvastatin calcium tablets are contraindicated for use in pregnant women since safety in pregnant women has not been established and there is no apparent benefit of lipid lowering drugs during pregnancy.

Can this medicine be used in children?

• The safety and effectiveness of atorvastatin calcium tablets have been established in pediatric patients,10 years to 17 years of age, with HeFH as an adjunct to diet to reduce total cholesterol, LDL-C, and apo B levels.
• The safety and efficacy of atorvastatin calcium tablets have not been established in pediatric patients younger than 10 years of age with HeFH.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: atorvastatin calcium

• Inactive Ingredients: anhydrous lactose, anhydrous sodium carbonate, colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, L-Arginine, magnesium stearate and microcrystalline cellulose. The film coating of the tablets contains polyvinyl alcohol, talc and titanium dioxide, and may contain polyethylene glycol or lecithin and xanthan gum.

Who manufactures and distributes this medicine?

Manufactured for: Mylan Pharmaceuticals Inc. Morgantown, WV U.S.A.

Manufactured by:

• Mylan Laboratories Limited
• Hyderabad , India

What should I know about storage and disposal of this medication?

• Store atorvastatin calcium tablets at room temperature, 20° to 25°C (68° to 77°F).
• Do not keep medicine that is out of date or that you no longer need.
• Keep atorvastatin calcium tablets and all medicines out of the reach of children. Be sure that if you throw medicine away, it is out of the reach of children.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Atorvastatin
• FDA Atorvastatin

Atorvastatin Resources
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