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Pharmacologic class: HMG-CoA reductase inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category X


Increases rate at which body removes cholesterol from blood and reduces production of cholesterol by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis


Tablets: 1 mg, 2 mg, 4 mg

Indications and dosages

Primary hyperlipidemia, mixed dyslipidemia

Adults: 2 mg P.O. daily; may increase to maximum of 4 mg daily

Dosage adjustment

• Renal impairment

• Patient with end-stage renal disease on dialysis

• Concurrent use of erythromycin or rifampin


• Hypersensitivity to drug or its components

• Active liver disease, unexplained persistent transaminase elevations

• Concurrent use of cyclosporine

• Women of childbearing age

• Breastfeeding


Use cautiously in:

• patients with severe renal impairment not on dialysis (use not recommended)

• patients with predisposing factors for myopathy (such as untreated hypothyroidism)

• patients who consume substantial quantities of alcohol or have history of chronic liver disease

• concurrent use of protease inhibitors (such as lopinavir, ritonavir), erythromycin, fibric acids (such as fenofibrate, gemfibrozil), rifampin, or niacin

• elderly patients

• children (safety and efficacy not established).


• Check liver function tests before starting therapy.

• Administer with or without food.

Adverse reactions

CNS: headache

EENT: nasopharyngitis

GI: diarrhea, constipation

Hepatic: liver enzyme abnormalities

Musculoskeletal: arthralgia, myalgia, back pain, extremity pain, rhabdomyolysis

Skin: rash, pruritus, urticaria

Other: influenza, hypersensitivity


Drug-drug. Cyclosporine, erythromycin, fibric acids, niacin, protease inhibitors, rifampin: increased pitavastatin effect and risk of myopathy

Drug-diagnostic tests. Alanine aminotransferase (ALT), alkaline phosphatase, aspartate aminotransferase (AST), bilirubin, blood glucose, creatine kinase: increased levels

Drug-food. Grapefruit juice: increased drug area under the curve

Patient monitoring

Discontinue drug if markedly elevated creatine kinase level occurs or myopathy is diagnosed or suspected.

Temporarily withhold drug if an acute serious condition suggests myopathy or predisposes to development of renal failure secondary to rhabdomyolysis (such as sepsis, hypotension, dehydration, major surgery, trauma, uncontrolled seizures, or severe metabolic, endocrine, and electrolyte disorders).

• Analyze lipid levels 4 weeks after starting therapy and after dosage titration; monitor liver enzyme levels 12 weeks after starting therapy, after dosage titration, and periodically thereafter. Should an increase in ALT or AST level of more than three times the upper limit of normal persist, dosage reduction or drug withdrawal is recommended. Continue to monitor patient who develops increased transaminase levels until abnormalities resolve.

• In patient receiving warfarin concurrently, closely monitor prothrombin time and International Normalized Ratio.

Patient teaching

• Tell patient to take drug with or without food.

Instruct patient to immediately report to prescriber if unexplained muscle pain, tenderness, or weakness occurs, especially if accompanied by malaise or fever.

• Caution patient to avoid or decrease alcohol intake.

• Advise breastfeeding patient not to breastfeed while taking drug.

• Advise female patient of childbearing age to use an effective method of birth control to prevent pregnancy while using drug and if she becomes pregnant, advise her to stop taking drug and notify prescriber.

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

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


(pi-tava-sta-tin) ,


(trade name)


Therapeutic: lipid lowering agents
Pharmacologic: hmg coa reductase inhibitors
Pregnancy Category: X


Treatment of primary hyperlipidemia and mixed dyslipidemia (adjunctive therapy to diet); to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C).


Inhibits 3–hydroxy-3–methylglutaryl-coenzyme A (HMG-CoA) reductase, an enzyme which is responsible for catalyzing an early step in cholesterol synthesis.

Therapeutic effects

Lowering of TC, LDL-C, Apo B and TG; increasing HDL-C.
In conjuction with multiple risk factor interventions, lowering of cardiovascular risk.


Absorption: Well absorbed (51%) following oral administration.
Distribution: unknown.
Protein Binding: >99%.
Metabolism and Excretion: Mostly metabolized by the liver; 15% excreted in urine, 79% excreted in feces mostly as metabolites.
Half-life: 12 hr.

Time/action profile (effect on lipids)

POwithin 4 wk4 wkunknown


Contraindicated in: Hypersensitivity; Active liver disease, including unexplained elevations in liver function tests; Concurrent use of cyclosporine; Severe renal impairment (CCr <30 mL/min); Obstetric: Pregnancy or women who may become pregnant; Lactation: Lactation.
Use Cautiously in: Renal impairment (↑ risk of myopathy, dosage ↓ recommended for CCr <60 mL/min); Hypothyroidism, concurrent use of fibrates or lipid-lowering doses of niacin (↑ risk of myopathy); Geriatric: ↑ risk of myopathy; History of alcohol abuse or moderate alcohol consumption (↑ risk of liver damage) Pediatric: Safety and effectiveness not established.

Adverse Reactions/Side Effects

Central nervous system

  • amnesia
  • confusion
  • memory loss


  • constipation (most frequent)
  • diarrhea (most frequent)
  • ↑ liver enzymes


  • pruritus
  • rash
  • urticaria


  • hyperglycemia


  • rhabdomyolysis (life-threatening)
  • myositis (most frequent)
  • back pain (most frequent)
  • extremity pain (most frequent)
  • myalgia (most frequent)
  • arthralgia
  • immune-mediated necrotizing myopathy


  • hypersensitivity reactions


Drug-Drug interaction

Cyclosporine ↑ levels and the risk for myopathy; concurrent use contraindicated.Risk of myopathy is ↑ by concurrent use of erythromycin, rifampin, fibrates, colchicine or large doses of niacin ; use ↓ doses with erythromycin, rifampin, and niacin; concurrent use with gemfibrozil should be avoided.Alcohol may ↑ risk of liver toxicity.


Oral (Adults) 2 mg once daily initially, may be ↑ up to 4 mg depending on response.Concurrent erythromycin therapy—Dose should not exceed 1 mg/day; Concurrent rifampin therapy—Dose should not exceed 2 mg/day.

Renal Impairment

Oral (Adults) CCr <60 mL/min—1 mg once daily initially, may be ↑ up to 2 mg daily.


Tablets: 1 mg, 2 mg, 4 mg

Nursing implications

Nursing assessment

  • Obtain a diet history, especially with regard to fat consumption.
  • Lab Test Considerations: Evaluate serum cholesterol and triglyceride levels before initiating, after 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, discontinue pitavastatin and do not restart. May also cause ↑ alkaline phosphatase and bilirubin levels.
    • If patient develops muscle tenderness during therapy, CK levels should be monitored. If CK levels are markedly elevated or myopathy occurs, therapy should be discontinued.

Potential Nursing Diagnoses

Noncompliance (Patient/Family Teaching)


  • Oral: May be administered at any time of the day without regard to food.

Patient/Family Teaching

  • Instruct patient to take medication exactly as directed, not to skip doses or double up on missed doses. Medication helps control but does not cure elevated serum cholesterol levels.
  • Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
  • Instruct patient to notify health care professional if unexplained muscle pain, tenderness, or weakness occurs, especially if accompanied by fever or malaise.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
  • Advise women of child bearing age to use effective contraception during therapy and discuss plans to discontinue pitavastatin if trying to conceive. Instruct female patients to notify health care professional promptly if pregnancy is suspected. Advise patients to avoid breastfeeding during therapy.
  • Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

Evaluation/Desired Outcomes

  • Decrease in LDL, apolipoprotein, and total cholesterol levels.
    • Increase in HDL cholesterol levels.
    • Decrease in triglyceride levels.
Drug Guide, © 2015 Farlex and Partners
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MEET THE STATINS EXAMPLES DOSAGE LDL (in milligrams) REDUCED High-Intensity Atorvastatin 40-80 mg (Lipitor[R]) 50% or Rosuvastatin 20-40 mg more (Crestor[R]) Moderate-Intensity Atorvastatin 10-20 mg Rosuvastatin 5-10 mg Simvastatin 20-40 mg (Zocor[R]) Pravastatin 40-80 mg (Pravachol[R]) Lovastatin 40-80 mg 30%-49% (Altoprev[R], Mevacor[R]) Pitavastatin 1-4 mg (Levalo[R]) Fluvastatin 40 mg (Lescol[R]) (twice daily) Fluvastatin XL 80 mg (Lescol XL[R]) Low-Intensity Simvastatin 10 mg Pravastatin 10-20 mg Less Lovastatin 20 mg than 30% Fluvastatin 20-40 mg Source: 2018 ACC/AHA Guideline on the Management of Blood Cholesterol, Circulation, Nov.
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Statins are li pid-lowering drugs by c ompeti ti vely inhibiting 3-hydroxy-3-methyl-glutar yl-coenz yme A reductase enzyme (HMGCR) and thus limiting cholesterol biosynthesis.1 Statins are administered daily as standard therapy for primary and s eco ndar y prevention of coronary heart disease (CHD), stroke and peripheral ar terial disease (PAD).2 Commonly used statins are rosuvastatin, atorvastatin, fluvastatin, lovas tatin, simvastatin, pravastatin and pitavastatin. Despite their clinical benefits, several patients discontinue these drugs due to intolerance, increasing the risk of cardiovascular morbidity and mortality.
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Kowa's nationwide sales force will co-promote Bystolic to cardiologists and select primary care healthcare providers across the country along with the company's cholesterol-lowering drug Livalo (pitavastatin) tablets.
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(Grapefruit is unlikely to boost the effects of fluvastatin, pravastatin, pitavastatin, or rosuvastatin, which are not metabolized by CYP3A4.)
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New-onset diabetes may be increased in patients treated with statins, though seeming to be dose related and less common with pravastatin and possibly pitavastatin [53].
Modulation of celecoxib-and streptozotocin-induced experimental dementia of Alzheimer's disease by pitavastatin and donepezil.