Drug for Lipid Disorders
Lipid
Disorder
Drugs
Hypolipidemic agents, or antihyperlipidemic
agents, are a diverse group
of pharmaceuticals that are used in the treatment
of high levels of fats (lipids), such as cholesterol,
Atorvastatin
in the blood (hyperlipidemia). They are
called lipid-lowering drugs.
BRAND NAME Atorvastatin (a-tore-va-stat-in)
GENERIC NAME: Lipitor
CLASSIFICATIONS:
Therapeutic: lipid-lowering agents
Pharmacologic: HMG-CoA reductase inhibitors
PREGNANCY CATERGORY: X
INDICATIONS: Adjunctive management of primary hypercholesterolemia
and mixed dyslipidemia. Primary prevention of coronary
heart disease (myocardial infarction, stroke, angina, and
coronary revascularization) in asymptomatic patients with
increased total and low-density lipoprotein (LDL) cholesterol
and decreased high-density lipoprotein (HDL) cholesterol.
ACTION: Inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-
CoA) reductase, an enzyme which is responsible for
catalyzing an early step in the synthesis of cholesterol.
THERAPEUTIC EFFECTS: Lowering of total and LDL cholesterol and triglycerides.
Slightly increases HDL cholesterol. Reduction of
lipids/cholesterol reduces the risk of myo-cardial infarction
and stroke sequelae. Slows the progression of coronary
atheroscle-rosis with resultant decrease in coronary heart
disease– related events.
PHARMACOKINETICS:
Absorption: Rapidly absorbed but undergoes extensive gastrointestinal
and he-patic metabolism resulting in 14% bioavailability
(30% for lipid-lowering activity).
Distribution: Probably enters breast milk.
Protein Binding: 98%.
Metabolism and Excretion: Extensively metabolized by the liver, most during first pass;
excreted in bile and feces. 2% excreted unchanged by the kidneys.
2 me-tabolites have lipid-lowering activity.
TIME/ACTION PROFILE (cholesterol-lowering effect)
ROUTE ONSET PEAK DURATION
PO unknown unknown 20 – 30 hr†
†Following discontinuation
CONTRAINDICATIONS/PRECAUTIONS:
Contraindicated in: Hypersensitivity; Active liver disease or unexplained
persistent elevations in AST and ALT; OB: Potential for
fetal anomalies; Lactation: May ap-pear in breast milk.
Use Cautiously in: History of liver disease; Alcoholism; Renal impairment;
Con- current use of gemfibrozil, azole antifungals, erythromycin,
clarithromycin, protease inhibitors, niacin, or cyclosporine
(higher risk of myopathy/rhabdomyolysis); OB: Women of
childbearing age; Pedi: Children 10 yr (safety not
established).
ADVERSE REACTIONS/SIDE EFFECTS:
CNS: amnesia, confusion, dizziness, headache, insomnia,
memory loss, weakness.
EENT: rhinitis. Resp: bronchitis.
CV: chest pain, peripheral edema.
GI: abdomi-nal cramps, constipation, diarrhea, flatus,
heartburn, altered taste, drug-induced hepatitis,
dyspepsia,qliver enzymes, nausea, pancreatitis.
Endo: hyperglycemia.
GU: erectile dysfunction.
Derm: rashes, pruritus.
MS: RHABDOMYOLYSIS, arthralgia, arthritis, immune-
mediated necrotizing myopathy, myalgia, myositis.
Misc: hyper-sensitivity reactions including
ANGIONEUROTIC EDEMA.
INTERACTIONS:
Drug-Drug: Metabolized by the hepatic CYP3A4 enzyme system. Cholesterol-
lowering effect may be additive with bile acid sequestrants (cholestyramine,
colestipol). Bioavailability may bepby bile acid sequestrants.qrisk
of myopathy with concurrent use ofcyclosporine, gemfibrozil,
itraconazole, colchicine, erythromycin, clarithromycin, nelfinavir,
ritonavir/saquinavir, lopinavir/ ritonavir, tipranavir/ritonavir,
saquinavir/ritonavir, darunavir/ritonavir, fosamprenavir,
fosamprenavir/ritonavir, telaprevir, and large doses of niacin (concurrent use with
gemfibrozil, cyclosporine, tipranavir/ritonavir, or tela-previr should
be avoided; use lowest dose with lopinavir/ritonavir; usepdoses with
nelfinavir, clarithromycin, itraconazole, saquinavir/ritonavir, daruna-vir/ritonavir,
fosamprenavir, or fosamprenavir/ritonavir). May
slightlyqse-rum digoxin levels. Mayqlevels of oral contraceptives.
Mayqeffects of warfarin.
Drug-Food: Grapefruit juice levels and risk of rhabdomyolysis.
ROUTE/DOSAGE: PO (Adults): 10– 20 mg once daily initially; (may start with 40 mg/day if
LDL-C needs to bepby 45%); may beqevery 2– 4 wk up to 80 mg/day;
Concurrent nelfi-navir therapy — Dose should not exceed 40 mg/day;
Concurrent clarithromycin, itraconazole, saquinavir/ritonavir,
darunavir/ritonavir, fosamprenavir, or fos-amprenavir/ritonavir therapy
— Dose should not exceed 20 mg/day.
PO (Children 10– 17 yr): 10 mg/day initially, may beqevery 4 wk up to
20 mg/ day; Concurrent nelfinavir therapy — Dose should not exceed 40
mg/day; Concur-rent clarithromycin, itraconazole, saquinavir/ritonavir,
darunavir/ritonavir, fosamprenavir, or fosamprenavir/ritonavir therapy —
Dose should not exceed 20 mg/day.
NURSING IMPLICATIONS:
Assessment
Obtain a diet history, especially with regard to fat consumption.
Lab Test Considerations: Evaluate serum cholesterol and triglyceride levels before
initiating, after 2– 4 wk of therapy, and periodically thereafter.
Monitor liver function tests prior to initiation of therapy and as clinically indicated.
If symptoms of serious liver injury, hyperbilirubinemia, or jaundice occurs dis-
continue atorvastatin and do not restart. May also causeqalkaline phosphatase and
bilirubin levels.
If patient develops muscle tenderness during therapy, CPK levels should be
monitored. If CPK levels are 10 times the upper limit of normal or myopathy
occurs, therapy should be discontinued. Monitor for signs and symptoms of
immune-mediated necrotizing myopathy (IMNM) (proxi-mal muscle weakness
andqserum creatine kinase), persisting despite discontinuation of statin therapy.
Perform muscle biopsy to diagnose; shows necrotizing myopathy without
significant inflammation. Treat with immunosuppressive agents.
Potential Nursing Diagnoses
Noncompliance (Patient/Family Teaching)
Implementation
Do not confuse Lipitor with Loniten or Zyrtec.
PO: May be administered without regard to food.
Avoid grapefruit and grapefruit juice during therapy; may increase risk of toxicity.
Patient/Family Teaching
Instruct patient to take medication as directed. Take missed doses as soon as re-
membered more than 12 hrs since missed dose; omit and take next scheduled dose.
Do not double up on missed doses. Advise patient to avoid drinking more than one
quart of grapefruit juice per day during therapy. Medication helps con-trol but does
not cure elevated serum cholesterol levels.
Advise patient that this medication should be used in conjunction with diet restric-
tions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smok-ing.
Instruct patient to notify health care professional if unexplained muscle pain,
tenderness, or weakness occurs, especially if accompanied by fe-ver or malaise.
Instruct patient to notify health care professional of all Rx or OTC medications, vi-
tamins, or herbal products being taken and consult health care professional be-fore
taking any new medications.
Advise patient to notify health care professional of medication regimen prior to
treatment or surgery.
Instruct female patients to notify health care professional promptly if
pregnancy is planned or suspected, or if breast feeding.
Emphasize the importance of follow-up exams to determine effectiveness and to
monitor for side effects.
Evaluation/Desired Outcomes
Decrease in LDL and total cholesterol levels.
Increase in HDL cholesterol levels.
Decrease in triglyceride levels.
Slowing of the progression of coronary artery disease.
