pitavastatin

REMS

Livalo and Zypitamag

Primary hyperlipidemia (adjunctive therapy to diet).

Livalo

Heterozygous familial hypercholesterolemia (adjunctive therapy to diet).

Action ⬆ ⬇

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

Therapeutic effects:

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

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

(effect on lipids)

ROUTE	ONSET	PEAK	DURATION
PO	within 4 wk	4 wk	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Active liver disease, including unexplained elevations in liver function tests;
Concurrent use of cyclosporine;
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);
OB: Use statin therapy during pregnancy only if potential maternal benefit justifies potential fetal risk (if needed, consider using a more water-soluble agent [pravastatin or rosuvastatin] that is less likely to cross the placenta);
Rep: Women of reproductive potential;
Pedi: Children 8 yr (safety and effectiveness not established);
Geri: risk of myopathy in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: pruritus, rash, urticaria

Endo: hyperglycemia

GI: constipation, diarrhea, ↑liver enzymes

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

Neuro: amnesia, confusion, memory loss

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

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.

Route/Dosage ⬆ ⬇

Primary Hyperlipidemia

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.

Renal Impairment

PO (Adults and Children ≥8 yr): CCr <60 mL/min: 1 mg once daily initially, may ↑ up to 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.

Renal Impairment

PO (Adults and Children ≥8 yr): CCr <60 mL/min: 1 mg once daily initially, may ↑ up to 2 mg once daily.

Availability ⬆ ⬇

(Generic available)

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

Assessment ⬆ ⬇

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

Lab Test Considerations:

Evaluate serum cholesterol, LDL-C, HDL-C, 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 occur, 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.

Implementation ⬆ ⬇

PO: May be administered once daily at the same time each 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.
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: Instruct females of reproductive potential to use effective contraception during therapy, to notify health care professional promptly if pregnancy is planned or suspected, and to avoid breastfeeding during therapy. Use statin therapy during pregnancy only if potential maternal benefit justifies potential fetal risk (if needed, consider using a more water-soluble agent [pravastatin or rosuvastatin] that is less likely to cross the placenta).
Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

Evaluation/Desired Outcomes ⬆ ⬇

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

US Brand Names ⬆ ⬇

Code ⬆

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)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇