Crestor

What is Crestor?

• Crestor (rosuvastatin calcium) is an HMG Co-A reductase inhibitor used lower the amount of cholesterol and other harmful substances, such as triglycerides, in the blood.

Error creating thumbnail:

Rosuvastatin

Rosuvastatin 3D Ball and Stick

Rosuvastatin3D

What are the uses of this medicine?

• Crestor is a prescription medicine that contains a cholesterol-lowering medicine called rosuvastatin calcium.

Crestor is used along with diet to:

• lower the level of your “bad” cholesterol (LDL)
• increase the level of your “good” cholesterol (HDL)
• lower the level of fat in your blood (triglycerides)
• slow the buildup of fatty deposits (plaque) in the walls of blood vessels

Crestor is used to treat:

• adults who cannot control their cholesterol levels by diet and exercise alone
• children 8 to 17 years of age with heterozygous familial hypercholesterolemia (an inherited condition that causes high levels of LDL)
• children 7 to 17 years of age with homozygous familial hypercholesterolemia (an inherited condition that causes high levels of LDL).

• Crestor is used to reduce the risk of heart attacks and strokes in men 50 years of age and older and women 60 years of age and older who do not have known heart disease but do have certain additional risk factors.

Limitations of use:

• Crestor is not approved for use in children with heterozygous familial hypercholesterolemia younger than 8 years of age or for use in children with homozygous familial hypercholesterolemia younger than 7 years of age.
• It is not known if Crestor is safe and effective in people who have Fredrickson Type I and V dyslipidemias.

How does this medicine work?

• Rosuvastatin (roe soo" va stat' in) is a potent, orally available inhibitor of hepatic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase the major rate-limiting enzyme in cholesterol synthesis.
• First, it increases the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL.
• Second, rosuvastatin inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to rosuvastatin calcium or any of the ingredients in Crestor.
• have liver problems.
• are pregnant or think you may be pregnant, or are planning to become pregnant.
• are breastfeeding.

What drug interactions can this medicine cause?

• Combination of sofosbuvir/velpatasvir/voxilaprevir or ledipasvir/sofosbuvir increases rosuvastatin exposure. Use with Crestor is not recommended.
• Cyclosporine and darolutamide combination increases rosuvastatin exposure. Limit Crestor dose to 5 mg once daily.
• Gemfibrozil should be avoided. If used together, limit Crestor dose to 10 mg once daily.
• Atazanavir/ritonavir, lopinavir/ritonavir, simeprevir or combination of dasabuvir/ombitasvir/paritaprevir/ritonavir, elbasvir/grazoprevir, sofosbuvir/velpatasvir and glecaprevir/pibrentasvir combination increases rosuvastatin exposure. Limit Crestor dose to 10 mg once daily.
• Regorafenib combination increases rosuvastatin exposure. Limit Crestor dose to 10 mg once daily.
• Coumarin anticoagulants combination prolongs INR. Achieve stable INR prior to starting Crestor. Monitor INR frequently until stable upon initiation or alteration of Crestor therapy.
• Use with fibrates or lipid-modifying doses (≥1 g/day) of niacin increases the risk of adverse skeletal muscle effects. Caution should be used when prescribing with Crestor.

Is this medicine FDA approved?

• Rosuvastatin was patented in 1991, and approved for medical use in the United States in 2003.
• In 2019, it was the 21st most commonly prescribed medication in the United States, with more than 27 million prescriptions.

How should this medicine be used?

Recommended dosage:

• The dose range for Crestor in adults is 5 to 40 mg orally once daily. The usual starting dose is 10 to 20 mg once daily.

Adult with homozygous familial hypercholesterolemia (HoFH):

• Starting dose 20 mg/day.

Pediatric patients with heterozygous familial hypercholesterolemia (HeFH):

• 5 to 10 mg/day for patients 8 to less than 10 years of age, and 5 to 20 mg/day for patients 10 to 17 years of age. (2.2)

Pediatric patients with HoFH:

• 20 mg/day for patients 7 to 17 years of age.

Administration:

• Take Crestor exactly as your doctor tells you to take it.
• Take Crestor, by mouth, 1 time each day. Swallow the tablet whole.
• Crestor can be taken at any time of day, with or without food.
• Do not change your dose or stop Crestor without talking to your doctor, even if you are feeling well.
• Your doctor may do blood tests to check your cholesterol levels before and during your treatment with Crestor. Your doctor may change your dose of Crestor if needed.•
• Your doctor may start you on a cholesterol lowering diet before giving you Crestor. Stay on this diet when you take Crestor.
• Wait at least 2 hours after taking Crestor to take an antacid that contains a combination of aluminum and magnesium hydroxide.
• If you miss a dose of Crestor, take it as soon as you remember. However, do not take 2 doses of Crestor within 12 hours of each other.
• If you take too much Crestor or overdose, call your doctor or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 5 mg, 10 mg, 20 mg, and 40 mg

This medicine is available in fallowing brand namesː

• Crestor

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache, muscle aches and pains, abdominal pain, weakness, and nausea.

• Additional side effects that have been reported with Crestor include memory loss and confusion.

Crestor may cause serious side effects, including:

• Muscle pain, tenderness and weakness (myopathy)
• Liver problems

What special precautions should I follow?

• The risk of myopathy during treatment with Crestor may be increased. Risks increase with use of 40 mg dose, advanced age (≥65), hypothyroidism, renal impairment, and combination use with cyclosporine, darolutamide, regorafenib, certain anti-viral medicines or their combinations. Cases of myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported. Advise patients to promptly report to their physician unexplained and/or persistent muscle pain, tenderness, or weakness and discontinue Crestor if signs or symptoms appear.
• There have been rare reports of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, associated with statin use. IMNM is characterized by: proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; positive anti-HMG CoA reductase antibody; muscle biopsy showing necrotizing myopathy; and improvement with immunosuppressive agents.
• Increases in serum transaminases [AST (SGOT) or ALT (SGPT)] have been reported with HMG‑CoA reductase inhibitors, including Crestor. Perform liver enzyme tests before initiating therapy and as clinically indicated thereafter.
• In the Crestor clinical trial program, dipstick-positive proteinuria and microscopic hematuria were observed among Crestor treated patients

What to do in case of emergency/overdose?

Treatment of overdosage:

• There is no specific treatment in the event of overdose.
• In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required.
• Hemodialysis does not significantly enhance clearance of rosuvastatin.

Can this medicine be used in pregnancy?

• Crestor is contraindicated for use in pregnant women since safety in pregnant women has not been established and there is no apparent benefit to therapy with Crestor during pregnancy.

Can this medicine be used in children?

• Crestor is not approved for use in children with heterozygous familial hypercholesterolemia younger than 8 years of age or for use in children with homozygous familial hypercholesterolemia younger than 7 years of age.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: rosuvastatin as rosuvastatin calcium
• Inactive Ingredients: microcrystalline cellulose NF, lactose monohydrate NF, tribasic calcium phosphate NF, crospovidone NF, magnesium stearate NF, hypromellose NF, triacetin NF, titanium dioxide USP, yellow ferric oxide, and red ferric oxide NF.

Who manufactures and distributes this medicine?

• Distributed by:

AstraZeneca Pharmaceuticals LP Wilmington, DE

What should I know about storage and disposal of this medication?

• Store Crestor at room temperature, between 68°F to 77°F (20°C to 25°C) and in a dry place.
• Safely throw away medicine that is out of date or no longer needed.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Crestor
• FDA Crestor

Crestor Resources
Latest articles Most recent articles Ongoing trials	Wikipedia