Lipitor

Action

Inhibits HMG-CoA reductase, which catalyzes first step in cholesterol synthesis; this action reduces concentrations of serum cholesterol and low-density lipoproteins (LDLs), linked to increased risk of coronary artery disease (CAD). Also moderately increases concentration of high-density lipoproteins (HDLs), associated with decreased risk of CAD.

Availability

Tablets: 10 mg, 20 mg, 40 mg, 80 mg

Indications and dosages

➣ Adjunct to diet for controlling LDL, total cholesterol, apo-lipoprotein B, and triglyceride levels and to increase HDL levels in patients with primary hypercholesterolemia and mixed dyslipidemia; primary dysbetalipoproteinemia in patients unresponsive to diet alone; adjunct to diet to reduce elevated triglyceride levels

Adults: Initially, 10 mg P.O. daily; increase to 80 mg P.O. daily if needed. Adjust dosage according to patient's cholesterol level.

➣ Adjunct to other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia

Adults: 10 to 80 mg P.O. daily

➣ Adjunct to diet to decrease total cholesterol, LDL, and apo-lipoprotein B levels in boys and postmenarchal girls ages 10 to 17 with familial and nonfamilial heterozygous hypercholesterolemia

Boys and girls: Initially, 10 mg P.O. daily; adjust dosage upward or downward based on lipid levels. Maximum dosage is 20 mg daily.

➣ Prevention of cardiovascular disease in patients without clinically evident coronary heart disease (CHD) but with multiple CHD risk factors

Adults: 10 mg P.O. daily

➣ Prevention of stroke and myocardial infarction in patients with type 2 diabetes who have multiple risk factors for CHD but without clinically evident CHD

Adults: Dosage individualized according to patient characteristics, such as goal of therapy and response according to National Cholesterol Education Program guidelines

Contraindications

• Hypersensitivity to drug or its components

• Active hepatic disease or unexplained, persistent serum transaminase elevations

• Pregnancy or breastfeeding

Precautions

Use cautiously in:

• hypotension, uncontrolled seizures, myopathy, alcoholism

• severe metabolic, endocrine, or electrolyte disorders

• concurrent use of cyclosporine, HIV protease inhibitors tipranavir or lopinavir plus ritonavir, hepatitis C protease inhibitor telaprevir, HMG-CoA reductase inhibitor gemfibrozil (avoid use)

• concurrent use of colchicine, fibric acid products, lipid-modifying doses (1 g/day or more) of niacin, clarithromycin and itraconazole (with atorvastatin dose above 20 mg), or grapefruit juice (more than 1.2 L/day)

• women of childbearing age

• children younger than age 18.

Administration

• Give with or without food.

• Don't give with grapefruit juice or antacids.

• If patient is also taking a CYP450 3A4 inducer (such as efavirenz or rifampin), give simultaneously with atorvastatin because delayed atorvastatin administration after rifampin administration has been associated with a significant reduction in atorvastatin plasma concentration.

Adverse reactions

CNS: amnesia, abnormal dreams, emotional lability, headache, hyperactivity, poor coordination, malaise, paresthesia, peripheral neuropathy, drowsiness, syncope, weakness

CV: orthostatic hypotension, palpitations, phlebitis, vasodilation, arrhythmias

EENT: amblyopia, altered refraction, glaucoma, eye hemorrhage, dry eyes, hearing loss, tinnitus, epistaxis, sinusitis, pharyngitis

GI: nausea, vomiting, diarrhea, constipation, abdominal cramps, abdominal or biliary pain, colitis, indigestion, dyspepsia, flatulence, stomach ulcers, gastroenteritis, melena, tenesmus, glossitis, mouth sores, dry mouth, dysphagia, esophagitis, pancreatitis, rectal hemorrhage

GU: hematuria, nocturia, dysuria, urinary frequency or urgency, urinary retention, cystitis, nephritis, renal calculi, abnormal ejaculation, decreased libido, erectile dysfunction, epididymitis

Hematologic: anemia, thrombocytopenia

Hepatic: jaundice, hepatic failure, hepatitis

Metabolic: hyperglycemia, hypoglycemia

Musculoskeletal: bursitis, joint pain, back pain, leg cramps, gout, muscle pain or aches, myositis, myasthenia gravis, neck rigidity, torticollis, rhabdomyolysis

Respiratory: dyspnea, pneumonia, bronchitis

Skin: alopecia, acne, contact dermatitis, eczema, dry skin, pruritus, rash, urticaria, skin ulcers, seborrhea, photo-sensitivity, diaphoresis, toxic epidermal necrolysis

Other: taste loss, gingival bleeding, fever, facial paralysis, facial or generalized edema, flulike symptoms, infection, appetite changes, weight gain, allergic reaction, Stevens-Johnson syndrome

Interactions

Drug-drug. Antacids, colestipol, CYP450 3A4 (such as efavirenz, rifampin): decreased atorvastatin blood level

Azole antifungals, colchicine, cyclosporine, erythromycin, fibric acid derivatives, HIV protease inhibitors, lipid-modifying doses of niacin, other HMG-CoA reductase inhibitors, strong CYP3A4 inhibitors (such as clarithromycin, itraconazole): protease inhibitors: increased risk of myopathy or rhabdomyolysis

Digoxin: increased digoxin level, greater risk of toxicity

Hormonal contraceptives: increased levels of these drugs

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, creatine kinase: increased levels

Drug-food. Grapefruit juice: increased drug blood level, greater risk of adverse effects

Patient monitoring

• Monitor patient for signs and symptoms of allergic response.

☞ Evaluate for muscle weakness (a symptom of myositis and possibly rhabdomyolysis).

• Be aware that reduction in dosage and periodic monitoring of creatine kinase level may be considered for patients taking drugs that may increase atorvastatin level.

• Monitor liver function test results and blood lipid levels.

Patient teaching

• Tell patient he may take drug with or without food.

☞ Advise patient to immediately report allergic response, irregular heart beats, unusual bruising or bleeding, unusual tiredness, yellowing of skin or eyes, or muscle weakness.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, alertness, and vision.

• Inform patient taking hormonal contraceptives that drug increases estrogen levels. Instruct her to tell all prescribers she's taking drug.

• Tell men that drug may cause erectile dysfunction and abnormal ejaculation. Encourage them to discuss these issues with prescriber.

• Tell patient he'll undergo regular blood testing during therapy.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.