ROSUVASTATIN
| ROSUVASTATIN (ro-su-va-sta'ten) Crestor Classifications: antilipemic; hmg-coa reductase inhibitor (statin); Therapeutic: antihyperlipemic; statin Prototype: Lovastatin Pregnancy Category: X |
Availability
5 mg, 10 mg, 20 mg, 40 mg tablets
Action
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.
Therapeutic Effect
Reduces total cholesterol and LDL cholesterol; additionally, lowers plasma triglycerides and apolipoprotein B while increasing HDL.
Uses
Adjunct to diet for the reduction of LDL cholesterol and triglycerides in patients with primary hypercholesterolemia and mixed dyslipidemia.
Contraindications
Hypersensitivity to any component of the product, active liver disease, pregnancy (category X), women of child-bearing potential not using appropriate contraceptive measures, lactation.
Cautious Use
Concomitant use of cyclosporine and gemfibrozil; excessive alcohol use or history of liver disease; renal impairment; advanced age; hypothyroidism.
Route & Dosage
| Hyperlipidemia Adult: PO 10 mg once daily (5–40 mg/d), max dose 40 mg/d. If taking cyclosporine, start with 5 mg/d. Geriatric: Initial dose of 5 mg/d Renal Impairment Clcr <30 mL/min: 5 mg once daily (max: 10 mg/d) |
Administration
Oral- 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. Hematologic: Anemia, ecchymosis. Musculoskeletal: Myalgia, arthritis, arthralgia, rhabdomyolysis (especially with dose >40 mg). Respiratory: Pharyngitis, rhinitis, sinusitis, bronchitis, increased cough, dyspnea, pneumonia, asthma. Skin: Rash, pruritus. Urogenital: UTI.Interactions
Drug: Cyclosporine, gemfibrozil, niacin, may increase risk of rhabdomyolysis; ANTACIDS may decrease rosuvastatin absorption; may cause increase in INR with warfarin.Pharmacokinetics
Absorption: Well absorbed. Peak: 3–5 h. Metabolism: Limited metabolism in the liver (not CYP3A4). Elimination: Primarily in feces (90%). Half-Life: 20 h.Nursing Implications
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.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug