pitavastatin

Action

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

Availability

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

Contraindications

• Hypersensitivity to drug or its components

• Active liver disease, unexplained persistent transaminase elevations

• Concurrent use of cyclosporine

• Women of childbearing age

• Breastfeeding

Precautions

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).

Administration

• 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

Interactions

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

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

See 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.

See 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.