Classifications: antilipemic agent; hmg-coa; reductase inhibitor (statin); Therapeutic: antilipemic; statin
Pregnancy Category: X
10 mg, 20 mg, 40 mg tablets
Atorvastatin is an inhibitor of reductase 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA), which is essential to hepatic
production of cholesterol. Lipitor increases the number of hepatic low-density-lipid (LDL) receptors, thus increasing LDL
uptake and catabolism of LDL. HDL cholesterol blood level increases with use of atorvastatin.
Atorvastatin reduces LDL and total triglyceride (TG) production as well as increases the plasma level of high-density lipids
Adjunct to diet for the reduction of LDL cholesterol and triglycerides in patients with primary hypercholesterolemia and
mixed dyslipidemia, prevention of cardiovascular disease in patients with multiple risk factors.
Hypersensitivity to atorvastatin, myopathy, active liver disease, unexplained persistent transaminase elevations, renal
failure, renal impairment, hepatic encephalopathy, hepatitis, hepatic disease; jaundice, rhabdomyolysis; uncontrolled seizure
disorders; pregnancy (category X), lactation.
Hypersensitivity to other HMG-CoA reductase inhibitors, history of liver disease, patients who consume substantial quantities
of alcohol. Safety and efficacy in children <10 y have not been established.
Route & Dosage
|Hypercholesterolemia/Prevention of Cardiovascular Disease
Adult: PO Start with 1040 mg q.d., may increase up to 80 mg/d
Child/Adolescent (1017 y): PO Start with 10 mg q.d., may increase up to 20 mg/d
- May be given at any time of day.
- Store at 20°25° C (68°77° F).
Adverse Effects (≥1%)Body as a Whole:
Back pain, asthenia, hypersensitivity reaction, myalgia, rhabdomyolysis. CNS:
Abdominal pain, constipation
, diarrhea, dyspepsia, flatulence, increased liver function tests. Respiratory: Sinusitis
, pharyngitis. Skin:
May increase digoxin
levels 20%, increases levels of norethindrone
and ethinyl estradiol
oral contraceptives; erythromycin
may increase atorvastatin levels 40%; macrolide antibiotics
, cyclosporine, delaviradine, gemfibrozil, niacin, clofibrate, azole antifungals
) may increase risk of rhabdomyolysis; nelfinavir
may increase atorvastatin levels. Food: Grapefruit juice
(>1 qt/d) may increase risk of myopathy and rhabdomyolysis.
Rapidly from GI tract. 30% reaches the systemic circulation. Onset:
Cholesterol reduction2 wk. Peak: Plasma
concentration, 12 h; effect 24 wk. Distribution:
≥98% protein bound. Crosses placenta, distributed into breast milk of
In the liver by CYP3A4 to active metabolites. Elimination:
Primarily in bile; <2% in urine. Half-Life:
14 h; 2030 h for active metabolites.
Assessment & Drug Effects
- Monitor for therapeutic effectiveness which is indicated by reduction in the level of LDL-C.
- Lab tests: Monitor lipid levels within 24 wk after initiation of therapy or upon change in dosage; monitor liver functions
at 6 and 12 wk after initiation or elevation of dose, and periodically thereafter.
- Assess for muscle pain, tenderness, or weakness; and, if present, monitor CPK level (discontinue drug with marked elevations
of CPK or if myopathy is suspected).
- Monitor carefully for digoxin toxicity with concurrent digoxin use.
Patient & Family Education
- Report promptly any of the following: Unexplained muscle pain, tenderness, or weakness, especially with fever or malaise;
yellowing of skin or eyes; stomach pain with nausea, vomiting, or loss of appetite; skin rash or hives.
- Do not take drug during pregnancy because it may cause birth defects. Immediately inform physician of a suspected or known
- Inform physician regarding concurrent use of any of the following drugs: erythromycin, niacin, antifungals, or birth control
- Minimize alcohol intake while taking this drug.