Rosuvastatin

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Pregnancy

Contraindicated

Because HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol (eg, cell membranes), rosuvastatin may cause fetal harm when administered to pregnant women

Lactation

Contraindicated

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

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Common side effects of Crestor include:

• Muscle and joint pain
• Headache
• Weakness
• Abdominal pain and nausea
• Elevated sugar levels
• Memory loss
• Confusion

Let your doctor know immediately if you have muscle pain or weakness, especially if it’s accompanied by fever, and if muscle problems continue after you quit taking Crestor.

Unexplained muscle pain, weakness, or tenderness, especially when it occurs with a fever, could be a sign of a rare muscle problem that might result in serious kidney problems.

If you are 65 or older or have thyroid or kidney problems, your risk of muscle problems will be greater.

Before you start using Crestor, your doctor should test your liver function.

Once you start taking this drug, contact your doctor immediately if you notice any sign of liver problems, including:

• Feeling excessively tired
• Loss of appetite
• Dark urine
• Pain in your upper belly
• Yellowing of the skin or eyes (jaundice)

Rosuvastatin is a prescription medication used to treat high cholesterol levels and to prevent heart disease. Rosuvastatin belongs to a group of drugs called HMG-CoA reductase inhibitors, also known as statins. Statins help to lower cholesterol levels in the body.

This medication comes in tablet form and is taken by mouth once a day, with or without food.

Common side effects are headache, muscle ache, abdominal pain, weakness, and nausea.

Rosuvastatin is in a group of drugs called HMG CoA reductase inhibitors, or "statins." Rosuvastatin reduces levels of "bad" cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL).

Rosuvastatin is used in adults and children who are at least 8 years old, to lower cholesterol and triglycerides (types of fat) in the blood and to slow the build-up of plaque (fatty deposits) in blood vessels.

Rosuvastatin is also used to lower the risk of stroke, heart attack, and other heart complications in certain people with diabetes, coronary heart disease, or other risk factors.

Rosuvastatin is also used to treat hereditary forms of high cholesterol, including the heterozygous type (inherited from one parent) and the homozygous type (inherited from both parents). For the heterozygous type, rosuvastatin can be used in children who are at least 8 years old. For the homozygous type, rosuvastatin can be used in children as young as 7 years old.

Rosuvastatin may also be used for purposes not listed in this medication guide.

Take the missed dose as soon as you remember. If you are more than 12 hours late, skip the missed dose. Do not take extra medicine to make up the missed dose.

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

In rare cases, rosuvastatin can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.

Also call your doctor at once if you have:

• confusion, memory problems;

• liver problems--nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or

• signs of a kidney problem--little or no urinating; painful or difficult urination; swelling in your feet or ankles; feeling tired or short of breath.

Common side effects may include:

• liver symptoms (stomach pain, dark urine, jaundice);

• unusual weakness or tired feeling;

• headache, muscle aches; or

• nausea, upset stomach.

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

Rosuvastatin is used together with a proper diet to lower cholesterol and triglycerides (fats) in the blood. rosuvastatin may help prevent or slow down medical problems, like atherosclerosis (hardening of the arteries), that are caused by fats clogging the blood vessels. It may also be used to prevent certain types of heart and blood vessel problems in patients with risk factors for heart problems.

Rosuvastatin belongs to a group of medicines called HMG-CoA reductase inhibitors, or statins. It works by blocking an enzyme that is needed by the body to make cholesterol, so this reduces the amount of cholesterol in the blood.

rosuvastatin is available only with your doctor's prescription.

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly to lower your cholesterol and triglyceride levels and to decide if you should continue to take it. Blood tests may be needed to check for unwanted effects.

Using rosuvastatin while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away.

Make sure any doctor or dentist who treats you knows that you are using rosuvastatin. You may need to stop using rosuvastatin if you have a major surgery, major injury, or you develop other serious health problems.

Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness. These could be symptoms of serious muscle problems such as myopathy or immune-mediated necrotizing myopathy (IMNM).

Call your doctor right away if you have dark-colored urine, fever, muscle cramps or spasms, muscle pain or stiffness, or unusual tiredness or weakness. These could be symptoms of a serious muscle problem called rhabdomyolysis, which can cause kidney problems.

Call your doctor right away if you get a headache, stomach pain, vomiting, dark-colored urine, loss of appetite, weight loss, general feeling of tiredness or weakness, light-colored stools, upper right stomach pain, or yellow eyes or skin. These could be symptoms of liver damage.

Do not stop or change your dose without checking first with your doctor, even if you are feeling well.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Crestor: 5 mg, 10 mg, 20 mg, 40 mg

Generic: 5 mg, 10 mg, 20 mg, 40 mg

Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism. In addition to the ability of HMG-CoA reductase inhibitors to decrease levels of high-sensitivity C-reactive protein (hsCRP), they also possess pleiotropic properties including improved endothelial function, reduced inflammation at the site of the coronary plaque, inhibition of platelet aggregation, and anticoagulant effects (de Denus 2002; Ray 2005).

Distribution

Vd: 134 L

Metabolism

Hepatic (10%), via CYP2C9 (1 active metabolite identified: N-desmethyl rosuvastatin, one-sixth to one-half the HMG-CoA reductase activity of the parent compound)

Excretion

Feces (90%), primarily as unchanged drug

Hypersensitivity to rosuvastatin or any component of the formulation; active liver disease or unexplained persistent elevations of serum transaminases; pregnancy; breast-feeding.

Canadian labeling: Additional contraindications (not in US labeling): Concomitant administration of cyclosporine; use of 40 mg dose in Asian patients, patients with predisposing risk factors for myopathy/rhabdomyolysis (eg, hereditary muscle disorders, history of myotoxicity with other HMG-CoA reductase inhibitors, concomitant use with fibrates or niacin, severe hepatic impairment, severe renal impairment [CrCl <30 mL/minute/1.73 m2], hypothyroidism, alcohol abuse, situations where an increase in rosuvastatin plasma levels may occur)

CrCl ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.

CrCl <30 mL/minute/1.73 m2: Initial: 5 mg once daily (maximum: 10 mg/day).

>10%: Neuromuscular & skeletal: Myalgia (2% to 13%)

1% to 10%:

Central nervous system: Headache (6% to 9%), dizziness (4%)

Endocrine & metabolic: Diabetes mellitus (new onset: 3%)

Gastrointestinal: Nausea (4% to 6%), constipation (3% to 5%)

Genitourinary: Cystitis (interstitial; Huang 2015)

Hepatic: Increased serum ALT (2%; >3 times ULN)

Neuromuscular & skeletal: Arthralgia (4% to 10%), increased creatine phosphokinase (3%; >10 x ULN: Children 3%), weakness (5%)

<1% (Limited to important or life-threatening): Abnormal thyroid function test, cognitive dysfunction (reversible; includes amnesia, confusion, memory impairment), depression, elevated glycosylated hemoglobin (HbA1c), gynecomastia, hematuria (microscopic), hepatic failure, hepatitis, hypersensitivity reaction (including angioedema, pruritus, skin rash, urticaria), immune-mediated necrotizing myopathy, increased gamma-glutamyl transferase, increased serum alkaline phosphatase, increased serum bilirubin, increased serum glucose, increased serum transaminases, jaundice, myoglobinuria, myopathy, myositis, pancreatitis, peripheral neuropathy, proteinuria (dose related), renal failure, rhabdomyolysis, sleep disorder (including insomnia and nightmares), thrombocytopenia

Initial dose: 20 mg orally once a day
Maintenance dose: 5 mg to 40 mg orally once a day

Comments:
-Response to therapy should be estimated from preapheresis LDL-C levels.

Use: For the reduction of LDL-C, Total-C, and ApoB in patients with homozygous familial hypercholesterolemia

Initial dose: 10 mg to 20 mg orally once a day
Maintenance dose: 5 mg to 40 mg orally once a day

Use: For individuals without clinically evident coronary heart disease but with an increased risk of cardiovascular disease (CVD) based on age 50 years or older in men and 60 years or older in women, high-sensitivity C-reactive protein test of 2 mg/L or higher, and presence of at least 1 additional CVD risk factor (e.g., hypertension, low HDL-C, smoking, or family history of premature coronary heart disease) to reduce the risk of stroke and myocardial infarction, and reduce the risk of arterial revascularization procedures