| 释义 |
rosuvastatin
ro·su·va·stat·in R5340100 (rŏ-so͞o′və-stăt′n)n. A statin drug, C22H28FN3O6S, used in the form of its calcium salt to lower cholesterol (especially LDL) levels and to reduce the risk of heart attack and stroke in individuals with elevated risk.
[Perhaps (fluo)ro- + su(lfonyl) + -vastatin, statin suffix; see pravastatin.]Translations
rosuvastatin
rosuvastatin (roe-soo-va-sta-tin) rosuvastatin, Crestor (trade name) Classification Therapeutic: lipid lowering agents
Pharmacologic: hmg coa reductase inhibitors
Pregnancy Category: X
IndicationsAdjunctive management of primary hypercholesterolemia and mixed dyslipidemias.Adjunctive management of hypertriglyceridemia.Adjunctive management of primary dysbetalipoproteinemia.Homozygous familial hypercholesterolemia.Slows the progression of atherosclerosis as adjunct to diet.Adjunctive therapy to diet and exercise for the reduction of LDL cholesterol in children 10–17 yrs with heterozygous familial hypercholesterolemia if diet therapy fails (LDL cholesterol remains ≥190 mg/dL or remains ≥160 mg/dL [with family history of premature cardiovascular disease or ≥2 risk factors for cardiovascular disease]); may be used alone or in combination with statin.Primary prevention of cardiovascular disease (reduces risk of stroke, myocardial infarction, and revascularization) in patients without clinically evident coronary heart disease but with an increased risk of cardiovascular disease because of age (≥50 yr for men; ≥60 yr for women), hsCRP ≥2 mg/L, and the presence of ≥1 risk factor for cardiovascular disease (hypertension, low HDL-C, smoking, or premature family history of coronary heart disease).ActionInhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, an enzyme which is responsible for catalyzing an early step in the synthesis of cholesterol.Therapeutic effectsLowering of total and LDL cholesterol and triglycerides. Slightly increases HDL cholesterol.Slows the progression of coronary atherosclerosis.PharmacokineticsAbsorption: 20% absorbed following oral administration.Distribution: Unknown.Metabolism and Excretion: 10% metabolized, 90% excreted unchanged in feces.Half-life: 19 hr.Time/action profile (effect on lipids)| ROUTE | ONSET | PEAK | DURATION |
|---|
| PO | unknown | 2–4 wk | unknown |
Contraindications/PrecautionsContraindicated in: Hypersensitivity; Active liver disease or unexplained persistent elevations in AST & ALT; Obstetric / Lactation: Pregnancy or lactation.Use Cautiously in: History of liver disease; Alcoholism; Renal impairment; genetic implication Patients with Asian ancestry (may have ↑ blood levels and ↑ risk of rhabdomyolysis); Concurrent use of gemfibrozil, azole antifungals, protease inhibitors, niacin, cyclosporine, amiodarone, or verapamil (higher risk of myopathy/rhabdomyolysis); Obstetric: Women of childbearing age; Pediatric: Safety not established.Adverse Reactions/Side EffectsCentral nervous system- amnesia
- confusion
- memory loss
- weakness
Gastrointestinal- abdominal pain
- constipation
- drug-induced hepatitis
- ↑ liver function tests
- nausea
DermatologicEndocrinologicHematologicMetabolic- rhabdomyolysis (life-threatening)
- immune-mediated necrotizing myopathy
- myalgia
InteractionsDrug-Drug interactionAntacids ↓ absorption (administer 2 hr after rosuvastatin).↑ risk of myopathy when used with cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, colchicine, fibrates or large doses of niacin ; concurrent use of gemfibrozil should be avoided, if possible; use ↓ doses with cyclosporine, lopinavir/ritonavir, and atazanavir/ritonavir.↑ levels of norgestrel and ethinyl estradiol.May ↑ risk of bleeding with warfarin ; monitor INR.Route/DosageOral (Adults) 10 mg once daily initially (range 5–20 mg initially) (20 mg initial dose may be considered for patients with LDL-C >190 mg/dL or homozygous familial hypercholesterolemia); dose may be adjusted at 2–4 wk intervals, some patients may require up to 40 mg/day, however this dose is associated with ↑ risk of rhabdomyolysis; genetic implicationPatients with Asian ancestry—initial dose should be 5 mg; Concurrent cyclosporine therapy—Dose should not exceed 5 mg/day; Concurrent lopinavir/ritonavir or atazanavir/ritonavir therapy—Dose should not exceed 10 mg/day; Concurrent gemfibrozil therapy—Dose should not exceed 10 mg/day (avoid if possible).Oral (Children 10–17 yr) 5–20 mg once daily.Renal ImpairmentOral (Adults) CCr <30 mL/min—5 mg once daily intially, may be ↑ to 10 mg/day.AvailabilityTablets: 5 mg, 10 mg, 20 mg, 40 mg Nursing implicationsNursing assessment- Obtain a diet history, especially with regard to fat consumption.
- Lab Test Considerations: Evaluate serum cholesterol and triglyceride levels before initiating, after 2–4 wk of therapy, and periodically thereafter.
- Monitor liver function tests before initiation of therapy and as clinically indicated. If symptoms of serious liver injury, hyperbilirubinemia, or jaundice occurs, discontinue rosuvastatin and do not restart. May also cause ↑ alkaline phosphatase, glutamyl transpeptidase, and bilirubin levels.
- If patient develops muscle tenderness during therapy, CK levels should be monitored. If CK levels are markedly ↑ or myopathy occurs, discontinue therapy.
- May cause proteinuria and microscopic hematuria; if persistent, may require dose reduction.
Potential Nursing DiagnosesNoncompliance (Patient/Family Teaching)
Implementation- Oral: Administer once daily without regard to food. Swallow tablets whole; do not crush, break, or chew.
- If magnesium or aluminum-containing antacids are used concurrently, administer antacid at least 2 hr after rosuvastatin.
- Avoid grapefruit and grapefruit juice during therapy; may increase risk of toxicity.
Patient/Family Teaching- Instruct patient to take medication as directed, not to skip doses or double up on missed doses. Take missed doses as soon as remembered but not within 12 hr of next dose. Medication helps control but does not cure elevated serum cholesterol levels.
- Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
- Instruct patient to notify health care professional if unexplained muscle pain, tenderness, or weakness occurs, especially if accompanied by fever or malaise.
- Advise patient to take magnesium or aluminum-containing antacids, if needed, at least 2 hr after rosuvastatin.
- Instruct female patients to notify health care professional promptly if pregnancy is planned or suspected.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Advise patient to notify health care professional of medication regimen before treatment or surgery.
- Instruct female patient to inform health care professional if pregnancy is planned or suspected or if she is breastfeeding.
- Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.
Evaluation/Desired Outcomes- Decrease in LDL and total cholesterol levels.
- Increase in HDL cholesterol levels.
- Decrease in triglyceride levels.
- Slowing of the progression of coronary artery disease.
rosuvastatin (rŏ-so͞o′və-stăt′n)n. A statin drug, C22H28FN3O6S, used in the form of its calcium salt to treat hyperlipidemia.rosuvastatin A long-acting statin drug (see STATINS). A brand name is Crestor. |