Classifications: antilipemic; hmg-coa reductase inhibitor (statin); Therapeutic: antihyperlipemic; statin
Pregnancy Category: X
5 mg, 10 mg, 20 mg, 40 mg tablets
Rosuvastatin is a potent inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonic
acid, an early and rate-limiting step in cholesterol biosynthesis. Interference with this enzyme reduces the quantity of
mevalonic acid, a precursor of cholesterol.
Reduces total cholesterol and LDL cholesterol; additionally, lowers plasma triglycerides and apolipoprotein B while increasing
Adjunct to diet for the reduction of LDL cholesterol and triglycerides in patients with primary hypercholesterolemia and
Hypersensitivity to any component of the product, active liver disease, pregnancy (category X), women of child-bearing potential
not using appropriate contraceptive measures, lactation.
Concomitant use of cyclosporine and gemfibrozil; excessive alcohol use or history of liver disease; renal impairment; advanced
Route & Dosage
Adult: PO 10 mg once daily (540 mg/d), max dose 40 mg/d. If taking cyclosporine, start with 5 mg/d.
Geriatric: Initial dose of 5 mg/d
Clcr <30 mL/min: 5 mg once daily (max: 10 mg/d)
- Persons of Asian descent may be slow metabolizers and may require half the normal dose.
- May give any time of day without regard to food.
- Store at or below 30° C (86° F).
Adverse Effects (≥1%)Body as a Whole:
Asthenia, back pain, flu syndrome, chest pain, infection, pain, peripheral edema. CNS:
Headache, dizziness, insomnia
, hypertonia, paresthesia, depression
, anxiety, vertigo, neuralgia. CV:
Hypertension, angina, vasodilatation, palpitations. GI:
Diarrhea, dyspepsia, nausea, abdominal pain, constipation
, gastroenteritis, vomiting, flatulence, gastritis
. Endocrine: Diabetes
Anemia, ecchymosis. Musculoskeletal:
, arthralgia, rhabdomyolysis (especially with dose >40 mg). Respiratory:
Pharyngitis, rhinitis, sinusitis
, increased cough, dyspnea
Rash, pruritus. Urogenital:
InteractionsDrug: Cyclosporine, gemfibrozil, niacin,
may increase risk of rhabdomyolysis; ANTACIDS
may decrease rosuvastatin absorption; may cause increase in INR with warfarin.
Well absorbed. Peak:
35 h. Metabolism:
in the liver (not CYP3A4). Elimination:
Primarily in feces (90%). Half-Life:
Assessment & Drug Effects
- Monitor for and report promptly S&S of myopathy (e.g., skeletal muscle pain, tenderness or weakness).
- Withhold drug and notify physician if CPK levels are markedly elevated (≥10
x ULN) or if myopathy is diagnosed or suspected.
- Lab tests: CPK levels for S&S of myopathy; periodic LFTs; more frequent INR values with concomitant warfarin therapy.
- Monitor CV status, especially with a known history of hypertension or heart disease.
- Monitor diabetics for loss of glycemic control.
Patient & Family Education
- Do not take antacids within 2 h of taking this drug.
- Females should use reliable means of contraception while taking this drug to prevent pregnancy.