Pronunciation: a-TOR-va-STAT-in KAL-see-um
Class: HMG-CoA reductase inhibitor
- Tablets, oral 10 mg
- Tablets, oral 20 mg
- Tablets, oral 40 mg
- Tablets, oral 80 mg
Increases the rate at which the body removes cholesterol from the blood and reduces production of cholesterol by inhibiting the enzyme that catalyzes early rate-limiting step in cholesterol synthesis; increases HDL; reduces LDL, VLDL, and triglycerides.
Rapidly absorbed; T max is 1 to 2 h. Bioavailability is approximately 14%; low bioavailability is because of presystemic Cl in GI mucosa and/or hepatic first-pass metabolism. Food decreases rate and extent of absorption approximately 25% and 9%, respectively, but does not alter efficacy.
Vd is approximately 381 L. At least 98% is protein bound.
Undergoes hepatic and extrahepatic metabolism, including first-pass metabolism and CYP3A4. Extensively metabolized to active metabolites, which produce approximately 70% of circulating inhibitory activity for HMG-CoA reductase.
Atorvastatin and metabolites are eliminated primarily in bile. Less than 2% of the dose is recovered in the urine. Plasma half-life is approximately 14 h.
The half-life of HMG-CoA reductase inhibition is 20 to 30 h.
Special PopulationsHepatic Function Impairment
Plasma levels are markedly increased in patients with chronic alcoholic liver disease.
Indications and UsageCV disease
Reduce risk of MI or stroke and reduce risk for revascularization procedures and angina in patients with multiple risk factors for coronary heart disease (CHD), such as age, smoking, hypertension, low HDL cholesterol (HDL-C), or family history of early CHD. Reduce risk of nonfatal MI and fatal and nonfatal stroke in patients with type 2 diabetes, and without clinically evident CHD, but with multiple risk factors for CHD, such as albuminuria, hypertension, retinopathy, or smoking. Reduce risk of angina, nonfatal MI, fatal and nonfatal stroke, or hospitalization for CHD, and reduce risk for revascularization procedures in patients with clinically evident CHD.Hypercholesterolemia
Adjunct to diet to reduce elevated total-C, LDL-C, apolipoprotein B (apo B), and triglyceride levels, and increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (Fredrickson types IIa and IIb). Adjunct to diet for treatment of patients with elevated serum triglyceride levels (Fredrickson type IV). Treatment of primary dysbetalipoprotein (Fredrickson type III) in patients who do not respond adequately to diet. Reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatment (LDL apheresis), or if such treatments are unavailable. Adjunct to diet to reduce total-C, LDL-C, and apo B levels in boys and postmenarchal girls, 10 to 17 y of age, with heterozygous familial hypercholesterolemia if, after an adequate trial of diet therapy, the following are present: LDL-C remains at a level of at least 190 mg/dL; LDC-C remains at a level of least 160 mg/dL and there is a positive family history of premature CV disease; 2 or more other CV disease risk factors are present in children.
Active liver disease or unexplained persistent elevation of serum transaminases; pregnancy; lactation; hypersensitivity to any component of the product.
Dosage and AdministrationAdults
PO 10 to 80 mg/day.Heterozygous Familial Hypercholesterolemia
Children 10 to 17 y of age
PO Start with 10 mg/day (max, 20 mg/day).
Store tablets at controlled room temperature (68° to 77°F).
Consumption of substantial quantities of alcohol should be avoided because of the potential hepatic effects.Amiodarone, azole antifungal agents (eg, itraconazole), colchicine, cyclosporine, diltiazem, gemfibrozil, grapefruit juice, macrolide antibiotics (eg, clarithromycin, erythromycin), nefazodone, niacin, NNRTIs, (eg, delavirdine, efavirenz, nevirapine), protease inhibitors (eg, fosamprenavir, nelfinavir, ritonavir, saquinavir, telaprevir, tipranavir), tacrolimus, verapamil
Severe myopathy or rhabdomyolysis may occur. Avoid coadministration of atorvastatin with cyclosporine, gemfibrozil, telaprevir, or tipranavir plus ritonavir. Do not exceed an atorvastatin dosage of 20 mg/day when given with clarithromycin, darunavir plus ritonavir, fosamprenavir with or without ritonavir, itraconazole, or saquinavir plus ritonavir. Do not exceed an atorvastatin dosage of 40 mg/day when given with nelfinavir.Antacids, bile acid sequestrants (eg, cholestyramine, colestipol), carbamazepine, rifampin
Coadministration may decrease atorvastatin levels. Administer bile acid sequestrants at least 4 h before atorvastatin.Contraceptives, oral
May increase AUC for norethindrone and ethinyl estradiol.Digoxin
Elevated digoxin levels may occur.Fiber
Coadministration may decrease GI absorption of atorvastatin. Separate fiber ingestion and atorvastatin administration by as much time as possible.Midazolam
The effects of midazolam may be increased or prolonged.
Headache (17%); asthenia (4%); dizziness, insomnia (at least 2%).
Rash (4%); bullous rashes, including erythema multiforme, Stevens-Johnson syndrome, and TEN (postmarketing).
Sinusitis (6%); pharyngitis (3%); rhinitis (at least 2%).
Diarrhea (5%); abdominal pain (4%); constipation, dyspepsia, flatulence (3%); nausea (at least 2%).
Albuminuria, hematuria, UTI (at least 2%).
Fatal and nonfatal hepatic failure (postmarketing).
Peripheral edema (at least 2%).
Myalgia (6%); arthralgia (5%); back pain (4%); arthritis (at least 2%); rhabdomyolysis (postmarketing).
Bronchitis (at least 2%).
Accidental injury (4%); flu-like symptoms (3%); chest pain (at least 2%); anaphylaxis, angioneurotic edema (postmarketing).
Perform LFTs prior to the initiation of therapy and repeat as clinically indicated. Monitor lipid levels 2 to 4 wk after initiation and/or upon dosage titration. Consider monitoring of CPK in patients who present with muscle pain, tenderness, or weakness during therapy or when coadministering fibric acid derivatives, erythromycin, cyclosporine, azole antifungals, combinations of HIV protease inhibitors, or niacin.
Category X .
Contraindicated in breast-feeding women.
Safety and efficacy not established, except in children 10 to 17 y of age with heterozygous familial hypercholesterolemia.
Use with caution in patients who consume substantial quantities of alcohol or have a history of liver disease. Contraindicated in patients with active liver disease, including unexplained persistent transaminase elevations.
Increases in HbA 1c and fasting serum glucose levels have been reported.
Elevations in serum transaminases may occur. Fatal and nonfatal hepatic failure has been reported rarely. Interrupt therapy if serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs. If no alternate etiology is found, do not restart atorvastatin.
Ensure secondary causes of hypercholesterolemia (eg, poorly controlled diabetes, hypothyroidism, drugs that increase LDL-C and decrease HDL-C) are excluded, or, if appropriate, treated, before starting therapy.
Recent stroke or transient ischemic attack
Increased incidence of hemorrhagic stroke was observed in patients treated with atorvastatin who had a history of stroke or transient ischemic attack in the past 6 mo.
Skeletal muscle effects
Rhabdomyolysis with renal impairment secondary to myoglobinuria has occurred with this class of drugs. Consider myopathy in any patient with diffuse myalgia, muscle tenderness or weakness, or marked elevation of CPK. Ensure therapy is temporarily withheld in patients with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, hypotension, major surgery, sepsis, trauma).
- Explain the name, dose, action, potential adverse effects of medication, and cholesterol goals.
- Advise patients that the dose of the medication may change, based on results of cholesterol blood tests, in an effort to reach cholesterol goals.
- Advise patients to take prescribed dose once daily without regard to meals, but to take with food if stomach upset occurs.
- Advise patients to try to take each dose at about the same time each day.
- Caution patients not to take atorvastatin with grapefruit juice.
- Advise patients that if a dose is missed to take as soon as remembered but to never take more than 1 dose of atorvastatin per day.
- Advise patients that atorvastatin helps control, but does not cure, cholesterol abnormality and to continue taking as prescribed when cholesterol goal has been reached.
- Emphasize to patients the importance of other modalities for cholesterol control: dietary changes (eg, reduced saturated fat intake, increased soluble fiber intake), weight control, regular exercise, and smoking cessation.
- Instruct patients to continue taking other cholesterol-lowering medications as prescribed by their health care provider.
- Instruct patients to immediately notify their health care provider if they experience dark urine; fatigue; flu-like symptoms; pain under the right rib cage; persistent nausea; unexplained muscle pain, tenderness, and/or weakness; yellowing of skin or eyes; or any other unusual feelings.
- Advise women of childbearing potential to use effective contraception during treatment with atorvastatin.
Copyright © 2009 Wolters Kluwer Health.
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