Pitavastatin

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[edit] BRAND NAMES

[edit] STRUCTURE

Pitavastatin.jpg

[edit] MECHANISM OF ACTION

Pitavastatin is a hypolipidemic belonging to the class of drugs called Statins.

Cholesterol is made mainly in the liver. Statins work by blocking a key liver enzyme involved in this process, thereby slowing down the production of cholesterol in the liver. This encourages the liver to take extra cholesterol, LDL cholesterol in particular, out of the bloodstream, by increasing the number of hepatic LDL receptors on the cell-surface and thus, causing the LDL cholesterol level to decrease .

Pitavastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, this results in a decrease in mevalonate, a precursor of cholesterol. Pitavastatin reduces total-cholesterol, LDL-cholesterol, VLDL-cholesterol and TG and increases HDL-cholesterol (good cholesterol).

[edit] INDICATIONS

  • Primary hypercholesterolemia or mixed dyslipidemia (elevated LDL-cholesterol and triglyceride) as an adjunctive therapy to diet

[edit] DOSAGE

The dose range is 1 to 4 mg orally once daily at any time of the day with or without food. The recommended starting dose is 2 mg and the maximum dose is 4 mg. The starting dose and maintenance doses should be individualized according to patient characteristics, such as goal of therapy and response.

After initiation or upon titration of Pitavastatin, lipid levels should be analyzed after 4 weeks and the dosage adjusted accordingly

Doses greater than 4 mg once daily were associated with an increased risk for severe myopathy in premarketing clinical studies. Do not exceed 4 mg once daily dosing

[edit] DOSAGE FORMS AND STRENGTHS

  • Tablets: 1 mg, 2 mg, and 4 mg

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Pitavastatin
  • Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels
  • Women who are pregnant or may become pregnant
  • Nursing mothers
  • Co-administration with cyclosporine

[edit] WARNINGS AND PRECAUTIONS

  • Skeletal Muscle Effects: Myalgia, myopathy and, rarely, rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with HMG-CoA reductase inhibitors, including Pitavastatin. These risks can occur at any dose level, but are increased at the highest dose.
    Pitavastatin should be prescribed with caution in patients with predisposing factors for myopathy (e.g., age ≥ 65 years, inadequately treated hypothyroidism, renal impairment, personal or family history of hereditary muscular disorders, alcohol abuse).
    Concomitant use of Fibrates, Niacin and Cyclosporine may increase the risk of myopathy. (see Interaction).
    Whilst on treatment, patients should be asked to report inexplicable muscle pain, weakness or cramps immediately, particularly if associated with malaise or fever. Creatine Kinase (CK) levels should be measured in these patients. Therapy should be discontinued if Creatine Kinase (CK) levels are markedly elevated.
  • Liver enzyme abnormalities: Persistent elevations in hepatic transaminases can occur. Check liver enzyme tests before initiating therapy and as clinically indicated thereafter

[edit] METABOLISM

Pitavastatin is marginally metabolized by CYP2C9 and to a lesser extent by CYP2C8

[edit] INTERACTIONS

Drug Interactions Associated with Increased Risk of 
Myopathy/Rhabdomyolysis
Interacting Agents 
Prescribing Recommendations 
Erythromycin Limit Pitavastatin to 1 mg once daily.
Rifampin Limit Pitavastatin to 2 mg once daily.
Cyclosporine Co-administration of cyclosporine with Pitavastatin is contraindicated
Colchicine The risk of myopathy/rhabdomyolysis is increased with concomitant administration of colchicine and HMG-CoA reductase inhibitors. Caution should be exercised when prescribing Pitavastatin with colchicine
Gemfibrozil concomitant administration of Pitavastatin with gemfibrozil should be avoided
Other Fibrates Pitavastatin should be administered with caution when used concomitantly with other fibrates
Niacin A reduction in Pitavastatin dosage should be considered

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Pitavastatin is contraindicated in women who are or may become pregnant.
  • Women who require Pitavastatin treatment should be advised not to nurse their infants or to discontinue the drug

[edit] SIDE EFFECTS

The most frequent adverse reactions (rate ≥2.0%) were myalgia, back pain, diarrhea, constipation and pain in extremity.

See also WARNINGS AND PRECAUTIONS section

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