pi-TAVa-sta-tin

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: hmg coa reductase inhibitors (statins)

Livalo and Zypitamag:

• Primary hyperlipidemia and mixed dyslipidemia (adjunctive therapy to diet).

Livalo:

• Heterozygous familial hypercholesterolemia (adjunctive therapy to diet).

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

• Lowers of total cholesterol, low-density lipoprotein cholesterol (LDL-C), apolipoprotein B, and triglycerides;
• Increases high-density lipoprotein cholesterol (HDL-C).

Absorption: Well absorbed (51%) following oral administration.

Distribution: unknown.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized by the liver; 15% excreted in urine, 79% excreted in feces mostly as metabolites.

Half-life: 12 hr.

(effect on lipids)

Contraindicated in:

• Hypersensitivity
• Active liver disease, including unexplained elevations in liver function tests
• Concurrent use of cyclosporine
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Renal impairment (↑ risk of myopathy; ↓ dose if CCr <60 mL/min)
• Hypothyroidism, concurrent use of fibrates or lipid-lowering doses of niacin (↑ risk of myopathy)
• History of alcohol abuse or moderate alcohol consumption (↑ risk of liver damage)
• Rep: Women of reproductive potential
• Pedi: Children <8 yr (safety and effectiveness not established)
• Geri: ↑risk of myopathy in older adults.

CNS: amnesia, confusion, memory loss.

Derm: pruritus, rash, urticaria.

Endo: hyperglycemia.

GI: constipation, diarrhea, ↑ liver enzymes.

MS: myositis, back pain, extremity pain, myalgia, arthralgia, immune-mediated necrotizing myopathy, RHABDOMYOLYSIS.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA).

Drug-Drug:

• 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.

Primary Hyperlipidemia and Mixed Dyslipidemia

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

Heterozygous Familial Hypercholesterolemia

• PO (Children 8 yr): 2 mg once daily initially, may ↑ up to 4 mg once daily depending on response.Concurrent erythromycin therapy — Dose should not exceed 1 mg once daily; Concurrent rifampin therapy — Dose should not exceed 2 mg once daily.

(Generic available)

• Tablets (Livalo): 1 mg; 2 mg; 4 mg;
• Tablets (Zypitamag): 2 mg; 4 mg;

• Obtain a diet history, especially with regard to fat consumption.

• Evaluate serum cholesterol and triglyceride levels before starting, 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 pain, tenderness, or weakness during therapy, monitor creatine kinase levels. If creatine kinase levels are markedly elevated or myopathy occurs, therapy should be discontinued.
  • May cause ↑ in hemoglobin A1c.

• PO: May be administered once daily at the same time each day without regard to food.

• 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.
• Inform patient that pitavastatin may cause increases in hemoglobin A1c. Advise patient to maintain lifestyle measures (regular exercise, maintaining healthy body weight, making healthy food choices).
• Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
• Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during therapy and discuss plans to discontinue pitavastatin if trying to conceive. Instruct patient 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.

• Decrease in LDL, apolipoprotein, and total cholesterol levels.
  • Increase in HDL cholesterol levels.
  • Decrease in triglyceride levels.

Livalo, Zypitamag

NDC Code^*

• 66869- Kowa Pharmaceuticals America, Inc.
  • 66869-104- Livalo
    • 66869-104-90- 90 TABLET, FILM COATED in 1 BOTTLE, DISPENSING (66869-104-90)

• 66869- Kowa Pharmaceuticals America, Inc.
  • 66869-204- Livalo
    • 66869-204-07- 7 TABLET, FILM COATED in 1 CARTON (66869-204-07)

• 66869- Kowa Pharmaceuticals America, Inc.
  • 66869-204- Livalo
    • 66869-204-90- 90 TABLET, FILM COATED in 1 BOTTLE, DISPENSING (66869-204-90)

• 66869- Kowa Pharmaceuticals America, Inc.
  • 66869-404- Livalo
    • 66869-404-07- 7 TABLET, FILM COATED in 1 CARTON (66869-404-07)

• 66869- Kowa Pharmaceuticals America, Inc.
  • 66869-404- Livalo
    • 66869-404-90- 90 TABLET, FILM COATED in 1 BOTTLE, DISPENSING (66869-404-90)