Rosuvastatin

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Rosuvastatin (Crestor) belongs to the statin class of drugs.

Rosuvastatin is used to treat high cholesterol and related conditions, and to prevent cardiovascular disease (risk of a heart attack, stroke or related health problems).

Heart attack, stroke and other problems can be caused by a disease called atherosclerosis. Atherosclerosis is due to build up of fatty deposits in the arteries.

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Rosuvastatin.jpg

[edit] MECHANISM OF ACTION

Rosuvastatin 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 .

Rosuvastatin 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. Rosuvastatin reduces total-cholesterol, LDL-cholesterol, VLDL-cholesterol and TG and increases HDL-cholesterol (good cholesterol).

[edit] INDICATIONS

  • Hyperlipidemia in:
    • Patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (elevated LDL-cholesterol and triglyceride) as an adjunct to diet.
    • Patients with hypertriglyceridemia as an adjunct to diet
    • Patients with primary dysbetalipoproteinemia (Type III hyperlipoproteinemia) as an adjunct to diet. Dysbetalipoproteinemia is a rare lipid disorder characterized by high levels of blood cholesterol and triglycerides
    • Patients with homozygous familial hypercholesterolemia (HoFH).
    • Pediatric Patients 10 to 17 years of age with Heterozygous Familial Hypercholesterolemia (HeFH) after failing an adequate trial of diet therapy


  • Prevention of Cardiovascular Disease: Cholesterol can cause coronary heart disease by narrowing the coronary arteries. This condition, called atherosclerosis, may lead to angina, a heart attack (myocardial infarction), or a stroke. Rosuvastatin is indicated to slow the progression of atherosclerosis and to reduce the risk of myocardial infarction, stroke and arterial revascularization procedures (e.g. heart bypass, angioplasty) in patients WITHOUT clinically evident coronary heart disease, but WITH multiple risk factors such as diabetes, high blood pressure, smoking, obesity, family history of early heart disease, and age.

[edit] DOSAGE

  • The recommended start dose is 5 or 10 mg orally once daily. Dose range: 5-40 mg once daily. The 40 mg dose of Rosuvastatin should be used only for those patients who have not achieved their LDL-C goal utilizing the 20 mg dose.
  • Homozygous familial hypercholesterolemia: Starting dose is 20 mg
  • In pediatric patients 10 to 17 years of age with heterozygous familial hypercholesterolemia (HeFH), the usual dose range is 5-20 mg/day.
  • Asian population: Consider 5 mg starting dose (Pharmacokinetic studies have demonstrated an approximate 2-fold increase in median exposure to rosuvastatin in Asian subjects when compared with Caucasian controls)

Rosuvastatin may be given at any time of day, with or without food

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 5 mg, 10 mg, 20 mg, and 40 mg

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Rosuvastatin
  • Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels
  • Women who may become pregnant, pregnancy and breastfeeding

[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 Rosuvastatin. These risks can occur at any dose level, but are increased at the highest dose (40 mg).
    Rosuvastatin 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 some other lipid-lowering therapies (fibrates or niacin), gemfibrozil, cyclosporine, lopinavir/ritonavir, Colchicine 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 and monitoring: As with other HMG-CoA reductase inhibitors, persistent elevations in hepatic transaminases can occur. Monitor liver enzymes before and, 3 months following the initiation of treatment. Rosuvastatin should be discontinued or the dose reduced if the level of serum transaminases is greater than 3 times the upper limit of normal.

[edit] INTERACTIONS

  • Cyclosporine: Combination increases rosuvastatin exposure. Limit Rosuvastatin dose to 5 mg once daily.
  • Gemfibrozil: Combination should be avoided. If used together, limitRosuvastatin dose to 10 mg once daily.
  • Lopinavir/Ritonavir or Atazanavir/Ritonavir: Combination increases rosuvastatin exposure. Limit Rosuvastatin dose to 10 mg once daily.
  • Coumarin anticoagulants (Warfarin and Acenocoumarol): Combination prolongs the International Normalised Ratio (INR). Discontinuation or downtitration of Rosuvastatin may result in a decrease in INR. In such situations, appropriate monitoring of INR is desirable.
  • Concomitant lipid-lowering therapies: Use with fibrates or niacin doses ≥1 g/day may increase the risk of skeletal muscle effects

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Rosuvastatin may cause fetal harm, therefore, it is contraindicated in women who are or may become pregnant
  • Nursing mothers who require Rosuvastatin treatment should be advised not to nurse their infants.

[edit] SIDE EFFECTS

Most frequent adverse reactions (rate ≥ 2%) are headache, myalgia, abdominal pain, asthenia, and nausea.

See also WARNINGS AND PRECAUTIONS section

[edit] RELATED LINKS

http://www.crestor.com

[edit] BIBLIOGRAPHY

[edit] REFERENCES