roe-SOO-va-sta-tin

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: hmg coa reductase inhibitors (statins)

• • Adjunctive management of primary hypercholesterolemia and mixed dyslipidemias,
  • Adjunctive management of hypertriglyceridemia,
  • Homozygous familial hypercholesterolemia.
• • Adjunctive management of hypertriglyceridemia,
  • Slows the progression of atherosclerosis as adjunct to diet.
  • Adjunctive therapy to diet and exercise for the reduction of LDL cholesterol (LDL-C) in children 8–17 yr with heterozygous familial hypercholesterolemia if after diet therapy fails the following still exist: LDL-C remains >190 mg/dL or remains >160 mg/dL (with family history of premature cardiovascular disease or 2 risk factors for cardiovascular disease),
  • 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 cholesterol [HDL-C], smoking, or premature family history of coronary heart disease).

• Inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, an enzyme that is responsible for catalyzing an early step in the synthesis of cholesterol.

• Lowering of total and LDL-C and triglycerides. Slightly increases HDL-C.
• Slows the progression of coronary atherosclerosis.

Absorption: 20% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: 10% metabolized, 90% excreted unchanged in feces.

Half-life: 19 hr.

(effect on lipids)

Contraindicated in:

• Hypersensitivity
• Active liver disease or unexplained persistent elevations in AST and ALT
• Lactation: Lactation.

Use Cautiously in:

• History of liver disease
• Alcoholism
• Renal impairment
• Patients with Asian ancestry (may have ↑ levels and ↑ risk of rhabdomyolysis)
• Women of reproductive potential
• OB: Use statin therapy during pregnancy only if potential maternal benefit justifies potential fetal risk (if needed, consider using a more water-soluble agent [pravastatin or rosuvastatin] that is less likely to cross the placenta)
• Pedi: Children <7 yr (safety and effectiveness not established in children).

Derm: rash.

Endo: hyperglycemia.

GI: abdominal pain, constipation, drug-induced hepatitis, ↑ liver enzymes, nausea.

Hemat: thrombocytopenia.

MS: immune-mediated necrotizing myopathy, myalgia, RHABDOMYOLYSIS.

Neuro: amnesia, confusion, memory loss, weakness.

Drug-Drug:

• Aluminum- and magnesium-containing antacids↓ absorption (administer 2 hr after rosuvastatin).
• Ledipasvir/sofosbuvir and sofosbuvir/velpatasvir/voxilaprevir may ↑ levels and risk of myopathy; concurrent use not recommended.
• Atazanavir/ritonavir, capmatinib, colchicine, cyclosporine, darolutamide, dasabuvir/ombitasvir/paritaprevir/ritonavir, elbasvir/grazoprevir, enasidenib, febuxostat, fibrates, fostamatinib, glecaprevir/pibrentasvir,lopinavir/ritonavir, niacin (large doses), regorafenib, sofosbuvir/velpatasvir, tafamidis, and teriflunomide may ↑ levels and risk of myopathy; avoid concurrent use with gemfibrozil; use ↓ doses with atazanavir/ritonavir, capmatinib, cyclosporine, darolutamide, dasabuvir/ombitasvir/paritaprevir/ritonavir, elbasvir/grazoprevir, enasidenib, fostamatinib, glecaprevir/pibrentasvir, lopinavir/ritonavir, regorafenib, sofosbuvir/velpatasvir, tafamidis, and teriflunomide.
• ↑levels of norgestrel and ethinyl estradiol.
• May ↑ risk of bleeding with warfarin; monitor INR.

• PO (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. Patients with Asian ancestry: Initial dose should be 5 mg once daily. Concurrent use of cyclosporine or darolutamide: Dose should not exceed 5 mg/day. Concurrent use of capmatinib, enasidenib, regorafenib, or teriflunomide: Dose should not exceed 10 mg/day. Concurrent use of gemfibrozil: Initial dose should be 5 mg once daily; dose should not exceed 10 mg/day (avoid if possible). Concurrent use of atazanavir/ritonavir, dasabuvir/ombitasvir/paritaprevir/ritonavir, elbasvir/grazoprevir, glecaprevir/pibrentasvir, lopinavir/ritonavir, or sofosbuvir/velpatasvir:Initial dose should be 5 mg once daily; dose should not exceed 10 mg/day. Concurrent use of tafamidis: Initial dose should be 5 mg once daily; dose should not exceed 20 mg/day (avoid if possible). Concurrent use of febuxostat or fostamatinib: Dose should not exceed 20 mg/day.
• PO (Children 10–17 yr): Heterozygous familial hypercholesterolemia: 5–20 mg once daily. Patients with Asian ancestry: Initial dose should be 5 mg. Concurrent use of cyclosporine: Dose should not exceed 5 mg/day. Concurrent use of atazanavir/ritonavir, glecaprevir/pibrentasvir, lopinavir/ritonavir, or sofosbuvir/velpatasvir: Dose should not exceed 10 mg/day.
• PO (Children 8–<10 yr): Heterozygous familial hypercholesterolemia: 5–10 mg once daily. Patients with Asian ancestry: Initial dose should be 5 mg. Concurrent use of cyclosporine: Dose should not exceed 5 mg/day. Concurrent use of atazanavir/ritonavir, lopinavir/ritonavir, or sofosbuvir/velpatasvir: Dose should not exceed 10 mg/day.
• PO (Children 7–17 yr): Homozygous familial hypercholesterolemia: 20 mg once daily. Patients with Asian ancestry: Initial dose should be 5 mg. Concurrent use of cyclosporine: Dose should not exceed 5 mg/day. Concurrent use of atazanavir/ritonavir, lopinavir/ritonavir, or sofosbuvir/velpatasvir: Dose should not exceed 10 mg/day.

(Generic available)

• Tablets: 5 mg; 10 mg; 20 mg; 40 mg;

• Obtain a diet history, especially with regard to fat consumption.

• Evaluate serum cholesterol and triglyceride levels before starting therapy, after 2–4 wk of therapy, and periodically thereafter.
  • Monitor liver function tests before starting 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, monitor CK levels. If CK levels are markedly ↑ or myopathy occurs, discontinue therapy.
  • May cause proteinuria and microscopic hematuria; if persistent, may require dose reduction.

• PO: Administer once daily without regard to food. DNC: 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.

• 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 to avoid grapefruit or grapefruit juice during therapy.
• 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.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications during therapy.
• Advise patient to notify health care professional if signs and symptoms of liver injury (fatigue, anorexia, right upper abdominal discomfort, dark urine, jaundice) occur.
• 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 females of reproductive potential to use effective contraception during therapy, to notify health care professional promptly if pregnancy is planned or suspected, and to avoid breastfeeding during therapy. Use statin therapy during pregnancy only if potential maternal benefit justifies potential fetal risk (if needed, consider using a more water-soluble agent [pravastatin or rosuvastatin] that is less likely to cross the placenta).
• Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

• Decrease in total cholesterol and LDL-C levels.
  • Increase in HDL-C levels.
  • Decrease in triglyceride levels.
• Slowing of the progression of coronary artery disease.

Crestor