ATORVASTATIN CALCIUM
| ATORVASTATIN CALCIUM (a-tor-va'sta-tin) Lipitor Classifications: antilipemic agent; hmg-coa; reductase inhibitor (statin); Therapeutic: antilipemic; statin Prototype: Lovastatin Pregnancy Category: X |
Availability
10 mg, 20 mg, 40 mg tablets
Action
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.
Therapeutic Effect
Atorvastatin reduces LDL and total triglyceride (TG) production as well as increases the plasma level of high-density lipids (HDL).
Uses
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.
Contraindications
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.
Cautious Use
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 10–40 mg q.d., may increase up to 80 mg/d Child/Adolescent (10–17 y): PO Start with 10 mg q.d., may increase up to 20 mg/d |
Administration
Oral- 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: Headache. GI: Abdominal pain, constipation, diarrhea, dyspepsia, flatulence, increased liver function tests. Respiratory: Sinusitis, pharyngitis. Skin: Rash.Interactions
Drug: 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 (ketoconazole, itraconazole) may increase risk of rhabdomyolysis; nelfinavir may increase atorvastatin levels. Food: Grapefruit juice (>1 qt/d) may increase risk of myopathy and rhabdomyolysis.Pharmacokinetics
Absorption: Rapidly from GI tract. 30% reaches the systemic circulation. Onset: Cholesterol reduction—2 wk. Peak: Plasma concentration, 1–2 h; effect 2–4 wk. Distribution: ≥98% protein bound. Crosses placenta, distributed into breast milk of animals. Metabolism: In the liver by CYP3A4 to active metabolites. Elimination: Primarily in bile; <2% in urine. Half-Life: 14 h; 20–30 h for active metabolites.Nursing Implications
Assessment & Drug Effects
- Monitor for therapeutic effectiveness which is indicated by reduction in the level of LDL-C.
- Lab tests: Monitor lipid levels within 2–4 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 pregnancy.
- Inform physician regarding concurrent use of any of the following drugs: erythromycin, niacin, antifungals, or birth control pills.
- Minimize alcohol intake while taking this drug.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug