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Product Name
Chemical Name
Therapeutic Category
Cardiovascular drugs
Pharmacologic Category
Antilipemic Agent, HMG-CoA Reductase Inhibitor
Pharmaceutical Form
Rosuvastatin 5mg /10mg /20mg /40mg
Dosing: Adult
Note: Doses should be individualized according to the baseline LDL-cholesterol levels, the recommended goal of therapy, and patient response; adjustments should be made at intervals of 4 weeks or more.
Hyperlipidemia, mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia, slowing progression of atherosclerosis: Oral:
Initial dose:
General dosing: 10 mg once daily; 20 mg once daily may be used in patients with severe hyperlipidemia (LDL >190 mg/dL) and aggressive lipid targets
Conservative dosing: Patients requiring less aggressive treatment or predisposed to myopathy (including patients of Asian descent): 5 mg once daily
Titration: After 2 weeks, may be increased by 5-10 mg once daily; dosing range: 5-40 mg/day (maximum dose: 40 mg once daily)
Note: The 40 mg dose should be reserved for patients who have not achieved goal cholesterol levels on a dose of 20 mg/day, including patients switched from another HMG-CoA reductase inhibitor.
Homozygous familial hypercholesterolemia (FH): Oral: Initial: 20 mg once daily (maximum dose: 40 mg/day)
Dosage adjustment with concomitant medications: Oral:
U.S. labeling:
Gemfibrozil: Avoid concurrent use; if unable to avoid concurrent use, rosuvastatin dose should not exceed 10 mg/day
Canadian labeling:
Gemfibrozil: Rosuvastatin dose should not exceed 20 mg/day
Dosage adjustment for hematuria and/or persistent, unexplained proteinuria while on 40 mg/day: Reduce dose and evaluate causes.

Dosing: Pediatric

Note: Doses should be individualized according to the baseline LDL-cholesterol levels, the recommended goal of therapy, and patient response; adjustments should be made at intervals of 4 weeks or more.
Heterozygous familial hypercholesterolemia (HeFH):
U.S. labeling: Children 10-17 years (females >1 year postmenarche): Oral: 5-20 mg once daily; maximum: 20 mg/day
Dosage adjustment for rosuvastatin with concomitant cyclosporine, atazanavir/ritonavir or lopinavir/ritonavir: Refer to drug-specific dosing in adult dosing section.
Canadian labeling: Oral: 5-10 mg once daily; maximum: 10 mg/day

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

Mild-to-moderate impairment: No dosage adjustment required.
Clcr <30 mL/minute/1.73 m2: Initial: 5 mg/day; do not exceed 10 mg once daily

Dosing: Hepatic Impairment

U.S. labeling: Active hepatic disease, including unexplained persistent transaminase elevations: Use is contraindicated.
Canadian labeling:
Active hepatic disease or unexplained persistent transaminase >3 x ULN: Use is contraindicated.
Mild-to-moderate impairment: No dosage adjustment required.
Severe impairment: Initial: 5 mg/day; do not exceed 20 mg once daily.
May be administered with or without food. May be taken at any time of the day.
Treatment of dyslipidemias:
Used with dietary therapy for hyperlipidemias to reduce elevations in total cholesterol (TC), LDL-C, apolipoprotein B, nonHDL-C, and triglycerides (TG) in patients with primary hypercholesterolemia (elevations of 1 or more components are present in Fredrickson type IIa, IIb, and IV hyperlipidemias); increase HDL-C; treatment of primary dysbetalipoproteinemia (Fredrickson type III hyperlipidemia); treatment of homozygous familial hypercholesterolemia (FH); to slow progression of atherosclerosis as an adjunct to diet to lower TC and LDL-C
Heterozygous familial hypercholesterolemia (HeFH): In adolescent patients (10-17 years of age, females >1 year postmenarche) with HeFH having LDL-C >190 mg/dL or LDL >160 mg/dL with positive family history of premature cardiovascular disease (CVD), or ≥2 other CVD risk factors.

Primary prevention of cardiovascular disease:
To reduce the risk of stroke, myocardial infarction, or arterial revascularization procedures in patients without clinically evident coronary heart disease or lipid abnormalities but with all of the following: 1) an increased risk of cardiovascular disease based on age ≥50 years old in men and ≥60 years old in women, 2) hsCRP ≥2 mg/L, and 3) the presence of at least one additional cardiovascular disease risk factor such as hypertension, low HDL-C, smoking, or a family history of premature coronary heart disease.

Secondary prevention of cardiovascular disease:
To slow progression of atherosclerosis
Medication Safety Issues
Sound-alike/look-alike issues:
Rosuvastatin may be confused with atorvastatin, nystatin, pitavastatin.
Adverse Reactions
>10%: Neuromuscular & skeletal: Myalgia (3% to 13%)
2% to 10%:
Central nervous system: Headache (6%), dizziness (4%)
Gastrointestinal: Nausea (3%), abdominal pain (2%), constipation (2%)
Hepatic: ALT increased (2%; >3 times ULN)
Neuromuscular & skeletal: Arthralgia (4% to 10%), CPK increased (3%; >10 x ULN: Children 3%), weakness (3%)
<2%, postmarketing, and/or case reports: Alkaline phosphatase increased, AST increased, bilirubin increased, depression, GGT increased, gynecomastia, hematuria (microscopic), hepatic failure, hepatitis, hyperglycemia, hypersensitivity reactions (including angioedema, pruritus, rash, urticaria), insomnia, jaundice, memory deficits, myoglobinuria, myositis, myopathy, nightmares, pancreatitis, proteinuria (dose related), renal failure, rhabdomyolysis, thyroid function test abnormalities
Adverse reactions reported with other HMG-CoA reductase inhibitors (not necessarily reported with rosuvastatin therapy) include a hypersensitivity syndrome (symptoms may include anaphylaxis, angioedema, arthralgia, erythema multiforme, eosinophilia, hemolytic anemia, interstitial lung disease, lupus syndrome, photosensitivity, polymyalgia rheumatica, positive ANA, purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, vasculitis)
Hypersensitivity to rosuvastatin or any component of the formulation; active liver disease; unexplained persistent elevations of serum transaminases (>3 times ULN); pregnancy; breast-feeding
Canadian labeling: Additional Contraindications (not in U.S. labeling): Concomitant administration of cyclosporine; use of 40 mg dose in Asian patients, patients with predisposing risk factors for myopathy/rhabdomyolysis (eg, hereditary muscle disorders, history of myotoxicity with other HMC-CoA reductase inhibitors, concomitant use with fibrates or niacin, severe hepatic impairment, severe renal impairment [Clcr <30 mL/minute/1.73 m2], hypothyroidism, alcohol abuse)
Warnings / Precautions Drug
Concerns related to adverse effects:
• Hematuria/proteinuria: Hematuria (microscopic) and proteinuria have been observed; more commonly reported in patients receiving rosuvastatin 40 mg daily. Typically, transient and not associated with a decrease in renal function. Consider dosage reduction if unexplained hematuria and proteinuria persists.
• Myopathy/rhabdomyolysis: Patients receiving HMG-CoA reductase inhibitors have developed rhabdomyolysis with acute renal failure and/or myopathy; patients should be monitored closely. This risk is dose-related and is increased with concurrent use of other lipid lowering medications. The manufacturer recommends temporary discontinuation for elective major surgery, acute medical or surgical conditions, or in any patient experiencing an acute or serious condition predisposing to renal failure (eg, sepsis, hypotension, trauma, uncontrolled seizures). However, based upon current evidence, HMG-CoA reductase inhibitor therapy should be continued in the perioperative period unless risk outweighs cardioprotective benefit. Use caution in patients with renal impairment, inadequately treated hypothyroidism, and those taking other drugs associated with myopathy (eg, colchicine); these patients are predisposed to myopathy. Patients should be instructed to report unexplained muscle pain, tenderness, weakness, or brown urine.

Disease-related concerns:

• Diabetes: In the JUPITER study, small increases in hemoglobin (Hb) A1c (mean HbA1c increased by ~0.1%) and physician-reported diabetes was significantly higher in the rosuvastatin group compared to placebo (Ridker, 2008). Overall, evidence supporting an association with diabetes risk is lacking. Because the clear benefits on cardiovascular disease risk outweigh any potential detrimental effects on glucose metabolism, the use of HMG-CoA reductase inhibitors in patients with diabetes continues to be recommended (ADA, 2011).
• Hepatic impairment and/or ethanol use: Use with caution in patients who consume large amounts of ethanol or have a history of liver disease. Use is contraindicated with active liver disease or unexplained transaminase elevations. In all patients, liver function must be monitored by baseline and periodic laboratory assessment; may cause hepatic dysfunction.
• Renal impairment: Dosage adjustment required in patients with a Clcr <30 mL/minute/1.73 m2 (contraindicated in the Canadian labeling).

Concurrent drug therapy issues:

• Cyclosporine: Cyclosporine significantly increases levels of rosuvastatin. Dose of rosuvastatin should be limited to 5 mg/day (concomitant use is contraindicated in the Canadian labeling).
• Gemfibrozil: Gemfibrozil significantly increases levels of rosuvastatin. Concomitant use of gemfibrozil is not recommended. If use of gemfibrozil is warranted, dose of rosuvastatin should be limited to 10 mg/day. Use of gemfibrozil or other fibrates in patients receiving concomitant rosuvastatin 40 mg/day is contraindicated in the Canadian labeling.
• Niacin: Use of niacin may increase the risk of myopathy when used with rosuvastatin. A reduction in rosuvastatin dose should be considered. Use in patients receiving concomitant rosuvastatin 40 mg/day is contraindicated in the Canadian labeling.
• Protease inhibitor/ritonavir combinations: Use with caution with concurrent protease inhibitor/ritonavir combinations. Atazanavir/ritonavir and lopinavir/ritonavir significantly increase rosuvastatin serum concentration; limit dose of rosuvastatin to 10 mg/day.
• Warfarin: Rosuvastatin significantly increases INR in patients on warfarin. INR should be monitored before starting rosuvastatin and frequently during therapy.

Special Populations:

• Asian population: Increased risk of rosuvastatin-associated myopathy in certain subgroups; dosage adjustment should be considered for patients of Asian descent. Use of rosuvastatin at a dose of 40 mg/day in Asian patients is contraindicated in the Canadian labeling.
• Elderly: Use with caution in patients with advanced age, these patients are predisposed to myopathy.

Other warnings/precautions:

• Appropriate use: Secondary causes of hyperlipidemia should be ruled out prior to therapy. Rosuvastatin has not been studied when the primary lipid abnormality is chylomicron elevation (Fredrickson types I and V).
Metabolism/Transport Effects
Substrate (minor) of CYP2C9, CYP3A4, SLCO1B1.
Amiodarone: May decrease the metabolism of HMG-CoA Reductase Inhibitors. Management: Dose of HMG-CoA reductase inhibitor may need to be reduced (e.g., simvastatin prescribing information recommends limiting adult maximum dose to 10 mg/day). Avoid Simcor (simvastatin/niacin) as fixed simvastatin doses exceed recommended maximum doses. Risk D: Consider therapy modification
Antacids: May decrease the serum concentration of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Fenofibrate: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Fenofibric Acid: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Gemfibrozil: May enhance the myopathic (rhabdomyolysis) effect of Rosuvastatin. Gemfibrozil may increase the serum concentration of Rosuvastatin. Management: If possible, avoid concomitant use of rosuvastatin with gemfibrozil. If concomitant can not be avoided, limit rosuvastatin to 10 mg/day (US recommendation) or 20 mg/day (Canadian recommendation). Monitor for signs/symptoms of rhabdomyolysis. Risk D: Consider therapy modification
Niacin: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Management: This is of greatest concern with niacin doses of 1 g or greater daily. Avoid simvastatin 80 mg in combination with niacin 1 g or greater in Chinese patients. Canadian labeling contraindicates use of niacin with rosuvastatin 40 mg. Risk D: Consider therapy modification
Protease Inhibitors: May increase the serum concentration of HMG-CoA Reductase Inhibitors. Limited data suggest pravastatin may slightly decrease protease inhibitor concentrations. Management: Lovastatin and simvastatin are contraindicated with protease inhibitors; also, avoid rosuvastatin with indinavir. Use lowest possible HMG-CoA reductase inhibitor dose and monitor for signs of toxicity if these agents are used concomitantly. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): HMG-CoA Reductase Inhibitors may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Pregnancy Implications
Cholesterol biosynthesis may be important in fetal development. Contraindicated in pregnancy. Administer to women of childbearing potential only when conception is highly unlikely and patients have been informed of potential hazards.
Excretion in breast milk unknown/contraindicated
Monitoring Parameters
Total cholesterol, LDL, and HDL cholesterol within 2-4 weeks of treatment initiation or dose change; liver function tests should be determined at baseline (prior to initiation), 3 months following initiation, 3 months after any increase in dose, and periodically thereafter (eg, semiannually); baseline CPK (recheck CPK in any patient with symptoms suggestive of myopathy). Monitor LDL-C at intervals no less than 4 weeks.
Mechanism of Action
Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism
Pharmacodynamics / Kinetics
Onset of action: Within 1 week; maximal at 4 weeks
Distribution: Vd: 134 L
Protein binding: 88%
Metabolism: Hepatic (10%), via CYP2C9 (1 active metabolite identified: N-desmethyl rosuvastatin, one-sixth to one-half the HMG-CoA reductase activity of the parent compound)
Bioavailability: 20% (high first-pass extraction by liver)
Asian patients have been noted to have increased bioavailability.
Half-life elimination: 19 hours
Time to peak, plasma: 3-5 hours
Excretion: Feces (90%), primarily as unchanged drug
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