rosuvastatin


Also found in: Dictionary, Wikipedia.

rosuvastatin

(roe-soo-va-sta-tin) ,

Crestor

(trade name)

Classification

Therapeutic: lipid lowering agents
Pharmacologic: hmg coa reductase inhibitors
Pregnancy Category: X

Indications

Adjunctive 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).

Action

Inhibits 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 effects

Lowering of total and LDL cholesterol and triglycerides. Slightly increases HDL cholesterol.
Slows the progression of coronary atherosclerosis.

Pharmacokinetics

Absorption: 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)

ROUTEONSETPEAKDURATION
POunknown2–4 wkunknown

Contraindications/Precautions

Contraindicated 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 Effects

Central nervous system

  • amnesia
  • confusion
  • memory loss
  • weakness

Gastrointestinal

  • abdominal pain
  • constipation
  • drug-induced hepatitis
  • ↑ liver function tests
  • nausea

Dermatologic

  • rash

Endocrinologic

  • hyperglycemia

Hematologic

  • thrombocytopenia

Metabolic

  • rhabdomyolysis (life-threatening)
  • immune-mediated necrotizing myopathy
  • myalgia

Interactions

Drug-Drug interaction

Antacids ↓ 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/Dosage

Oral (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 Impairment

Oral (Adults) CCr <30 mL/min—5 mg once daily intially, may be ↑ to 10 mg/day.

Availability

Tablets: 5 mg, 10 mg, 20 mg, 40 mg

Nursing implications

Nursing 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 Diagnoses

Noncompliance (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

an antilipemic.
indications This drug is used as an adjunct in primary hypercholesterolemia (types IIa and b), mixed dyslipidemia, elevated serum triglycerides, and homozygous low-density lipoprotein receptor disorder.
contraindications Pregnancy, lactation, active liver disease, and known hypersensitivity to this drug prohibit its use.
adverse effects Adverse effects of this drug include vomiting; leg, shoulder, or localized pain; insomnia; paresthesia; photosensitivity; rhinitis; sinusitis; bronchitis; and increased cough. Life-threatening side effects include liver dysfunction, myositis, rhabdomyolysis, thrombocytopenia, hemolytic anemia, and leukopenia. Common side effects include nausea, constipation, abdominal pain, flatus, diarrhea, dyspepsia, heartburn, asthenia, muscle cramps, arthritis, arthralgia, myalgia, headache, dizziness, rash, pruritus, and pharyngitis.

rosuvastatin

A long-acting statin drug (see STATINS). A brand name is Crestor.
References in periodicals archive ?
under the code name S-4522 at the end of 1980s, rosuvastatin (rosuvastatin calcium) along with its development, marketing and sales rights, was transferred to AstraZeneca in June 1998 under the code name of ZD-4522.
To address those questions, US researchers planned a trial to compare daily rosuvastatin with placebo (a dummy pill) in HIV-positive adults.
The panel was not asked specifically to vote on whether to approve rosuvastatin for the indication.
Patients who achieved very low LDL-C (< 50 mg/dL) with rosuvastatin 20 mg achieved a significant 63% reduction in CV events (p<0.
As part of the agreement, Actavis is permitted to launch its rosuvastatin zinc alternate salt product beginning May 2, 2016 or earlier under certain circumstances, however, at this time, the company has made no decision regarding a potential launch.
On the basis of the GISSI-HF results, 47 patients with moderate to severe heart failure would have to receive rosuvastatin for nearly 4 years to prevent one case of AF.
Michael Cressman, AstraZeneca's Global Medical Science Director for CRESTOR added, "These data provide confirmation that, in patients with coronary artery disease rosuvastatin 40 mg can achieve regression of coronary atherosclerosis, the underlying cause of heart disease.
b) ORION, a 24-month, randomised, double-blind study, used Morphology-Enhanced Probabilistic Plaque Segmentation (MEPPS) to segment and identify carotid plaque composition as depicted by high-resolution magnetic resonance imaging (MRI), in 43 subjects randomised to low or high dose rosuvastatin therapy.
Indeed, the estimated number of patients aged at least 70 years who would need to be treated with rosuvastatin (Crestor) for 5 years to prevent one primary composite end point--comprising nonfatal MI or stroke, hospitalization for unstable angina or arterial revascularization, or cardiovascular death--was 19, one-third less than the NNT of 29 in patients younger than 70, Robert J.
ii) ORION (Outcome of Rosuvastatin Treatment on Carotid Artery Atheroma: a Magnetic Resonance Imaging ObservatioN) was the first study to use advanced, high resolution MRI to investigate the effect of a statin - CRESTOR - on the change in the composition of plaques in the carotid artery wall.
In fact, statin medications, which include lovastatin (Mevacor), simvastatin (Zocor), pravastatin (Pravachol), rosuvastatin (Crestor), fluvastatin (Lescol) and atorvastatin (Lipitor), best known for their cholesterol-lowering benefits, work so well at preventing heart disease in people with diabetes, regardless of cholesterol level, that in June 2003 experts began recommending that all people with diabetes, even those with normal cholesterol levels, take a statin.
The study results, "Comparison of Lipid-Modifying Efficacy of Rosuvastatin Versus Atorvastatin in Patients with Acute Coronary Syndrome (from the LUNAR Study)," were published in the May 1 edition of the American Journal of Cardiology (AJC).