ROSUVASTATIN
(ro-su-va-sta'ten)
Crestor
Classifications: cardiovascular agent; antilipemic; hmg-coa reductase inhibitor (statin)
Prototype: Lovastatin
Pregnancy Category: X

Availability

5 mg, 10 mg, 20 mg, 40 mg tablets

Actions

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's activity reduces the quantity of mevalonic acid, a precursor of cholesterol.

Therapeutic Effects

Reduces total cholesterol and LDL cholesterol, and also 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

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 CYP 3A4). Elimination: Eliminated primarily in feces (90%). Half-Life: 20 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug