Rosuvastatin

Rosuvastatinis used along with a proper diet to help lower "bad"cholesteroland fats (such asLDL,triglycerides) and raise "good" cholesterol (HDL) in the blood. It belongs to a group of drugs known as "statins." It works by reducing the amount of cholesterol made by the liver. Lowering "bad" cholesterol and triglycerides and raising "good" cholesterol decreases the risk ofheart diseaseand helps to prevent strokes and heart attacks.

In addition to eating a proper diet (such as a low cholesterol/low-fat diet), other lifestyle changes that may help rosuvastatin work better include exercising, losing weight ifoverweight, and stopping smoking. Talk with your doctor for more details.

Rosuvastatin is available under the following different brand names:Crestor.

Adult and Pediatric Dosage Forms and Strengths

• 5 mg
• 10 mg
• 20 mg
• 40 mg

Dosage Considerations – Should be Given as Follows:

Hypercholesterolemia

• Hypertriglyceridemia,hyperlipidemia, mixeddyslipidemia, slowing progression ofatherosclerosis, primary dysbetalipoproteinemia
• 10-20 mg orally once/day initially; may titrate; not to exceed 40 mg/day
• Dosage range: 5-40 mg/day
• Homozygousfamilial hypercholesterolemia: Initiate with 20 mg orally once/day; may titrate; not to exceed 40 mg/day

HeterozygousFamilialHypercholesterolemia (HeFH)

Indicated to reduce total-C, LDL-C, and ApoB levels in children and adolescents aged 8-17 years if after an adequate trial of diet therapy the following findings are present: LDL-C greater than 190 mg/dL, or greater than 160 mg/dL along with a positive family history of prematurecardiovascular disease(CVD) or 2cardiovasculardisease or more risk factors

• Children under 8 years: Safety and efficacy not established
• Children 8 to under 10 years: 5-10 mg orally once/day
• Children 10-17 years: 5-20 mg orally once/day; may adjust dose at intervals of at least 4 weeks; not to exceed 20 mg/day

Homozygous Familial Hypercholesterolemia (HoFH)

Indicated to reduce LDL-C, Total-C, nonHDL-C and ApoB in children and adolescents aged 7 to 17 years with homozygous familial hypercholesterolemia, either alone or with otherlipid-lowering treatments (e.g., LDLapheresis)

• Children under 7 years: Safety and efficacy not established
• Children 7-17 years: 20 mg orally once/day

Primary Prevention

Primary prevention of cardiovascular disease in individuals with no clinically evident heart disease but who are at risk because of combined effect of risk factors listed below

• Approval based on JUPITER trial (Justification for the Use of statins in Prevention: an Intervention Trial Evaluation Rosuvastatin)
• Initial: 10-20 mg orally once/day
• Dosage range 5-40 mg/day
• 心血管病
  • Shown to reduce risk ofstroke,heart attack(myocardial infarction[MI]), and arterial revascularization procedures (including coronary arterybypassgraft [CABG], bypass grafting of peripheral artery orcarotidartery, andangioplastyor stent placement)
• Risk factors
  • 在男性年龄(超过50年。超过60年的女性), AND
  • Elevated high-sensitivity C-reactive protein level (greater than 2 mg/L), AND
  • Presence of at least 1 additional cardiovascularrisk factor(e.g.,high blood pressure, low HDL-C, smoking, family history of premature heart disease)

Dosing Considerations

• Patients of Asian descent: Initiate with 5 mg/day
• Coadministration with other lipid-lowering therapy: Consider dose reduction if combined withniacinorfenofibrate, because of increased risk forskeletal muscleeffects
• Coadministration withcyclosporine: Not to exceed 5 mg/day
• Coadministration withgemfibrozil: Avoid if possible; if used together, do not exceed 10 mg/day
• Coadministration with ritonavir, lopinavir/ritonavir, or atazanavir/ritonavir: Not to exceed 10 mg/day
• Overdose management
  • Adverse drug reactions from overdose may includeperipheral neuropathy, diarrhea, increased postassium,myopathy,rhabdomyolysis,acute renal failure, elevated liver function tests (LFTs), eyelensopacities
  • Treatment is supportive

Dosing Modifications

Renal impairment

• Severe (CrCl less than 30 mL/min/1.73m²) and not onhemodialysis: Decrease starting dose to 5 mg orally once/day; not to exceed 10 mg orally once/day
• CrCl greater than 30mL/min/1.73m²: Dose adjustment not necessary
• Activeliver disease: Use is contraindicated
• Chronic alcoholic liver disease is known to increase rosuvastatin exposure; caution advised

Common side effects of rosuvastatin include:

• Muscle pain
• Joint pain
• Diabetes mellitus, new onset
• Sore throat
• Headache
• Weakness/lack of energy
• Dizziness
• Creatinephosphokinase (CPK) increased
• Nausea
• Abdominal pain
• Alaninetransaminase (ALT) increased
• Constipation
• Flulike illness
• Urinary tract infection(UTI)
• Hypersensitivity reactions (including rash, itching, hives, and swelling)
• Pancreatitis

Less common side effects of rosuvastatin include:

• Yellowing skin and eyes (jaundice)
• Muscle disease
• Musclewasting(rhabdomyolysis)

Postmarketing side effects of rosuvastatin reported include:

• Joint pain
• Numbness/tingling/pain in extremities
• Depression and sleep disorders (including insomnia and nightmares)
• Fatal and nonfatal hepatic failure,hepatitis, jaundice
• Low bloodplatelet count(thrombocytopenia)
• Breast tissue enlargement in males

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe interactions of rosuvastatin include:

• gemfibrozil
• red yeast rice

Serious interactions of rosuvastatin include:

• atazanavir
• clarithromycin
• colchicine
• cyclosporine
• eltrombopag
• fenofibrate
• fenofibrate micronized
• fenofibric acid
• gemfibrozil
• indinavir
• ketoconazole
• ledipasvir/sofosbuvir
• lopinavir
• mifepristone
• nelfinavir
• niacin
• ombitasvir/paritaprevir/ritonavir and dasabuvir
• ritonavir
• saquinavir

Rosuvastatin has moderate interactions with at least 46 different drugs.

Mild interactions of rosuvastatin include:

• coenzyme Q10
• colestipol
• erythromycinbase
• erythromycin ethylsuccinate
• erythromycin lactobionate
• erythromycin stearate
• ethinylestradiol
• isradipine
• mestranol
• orlistat
• trazodone

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

This medication contains rosuvastatin. Do not take Crestor if you are allergic to rosuvastatin or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity
• Active liver disease, elevated liver function tests (LFTs)
• Pregnancy, lactation

Effects of Drug Abuse

• None

Short-Term Effects

• See "What Are Side Effects Associated with Using Rosuvastatin?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Rosuvastatin?"

Cautions

• Non-serious and reversiblecognitiveside effects may occur.
• Increased blood sugar andglycosylated hemoglobin(HbA1c) levels reported with statin intake; in some instances these increases may exceed the threshold for the diagnosis ofdiabetesmellitus.
• Chronic liver disease.
• Measure liver enzymes before initiating and if signs or symptoms of liver injury occur.
• Consider lower initial dose (5 mg once/day) in patients with risk of myopathy.
• Increased risk of rhabdomyolysis, especially at highest approved dose of 40 mg/day; reserve highest dose only for patients who fail to achieve desired cholesterol level at 20 mg/day.
• Use 5 mg/day starting dose in people of Asian ancestry, who may build up higher drug levels and be at higher risk of myopathy.
• 免疫介导性坏死性myopat的罕见报道hy (IMNM), characterized by increased serum creatine kinase that persists despite discontinuing statin.
• Discontinue if creatine kinase (CK) levels are markedly elevated.

Pregnancy and Lactation

• Rosuvastatin is contraindicated for use during pregnancy. Because HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol (e.g., cell membranes), rosuvastatin may cause fetal harm when administered to pregnant women.
• Rosuvastatin is contraindicated for use while breastfeeding. Limited data indicate that rosuvastatin is present in human milk; because statins have the potential for serious adverse reactions in nursing infants, women who require rosuvastatin treatment should not breastfeed their infants.