Crestor 20mg Tablets
It is used to lower bad cholesterol (LDL).It is used to lower triglycerides.It is used to slow the progress of heart disease.It is used in some people to lower the chance of heart attack, stroke, and certain heart procedures.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antilipemic Agent, HMG-CoA Reductase Inhibitor
Pharmacologic Class
HMG-CoA Reductase Inhibitor (Statin)
Pregnancy Category
Category X
FDA Approved
Aug 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
Rosuvastatin is a medication used to lower high cholesterol and triglyceride levels in the blood. It works by blocking an enzyme in the liver that makes cholesterol. Lowering cholesterol helps prevent heart attacks, strokes, and other heart problems.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. Take your medication at the same time every day to establish a routine. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
You can take your medication with or without food. However, if you are taking an antacid that contains aluminum or magnesium, take it at least 2 hours after taking your medication. Swallow your medication whole with a glass of water or another drink.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications in a safe and secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses to make up for the missed dose.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. Take your medication at the same time every day to establish a routine. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
You can take your medication with or without food. However, if you are taking an antacid that contains aluminum or magnesium, take it at least 2 hours after taking your medication. Swallow your medication whole with a glass of water or another drink.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications in a safe and secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses to make up for the missed dose.
Lifestyle & Tips
- Continue a cholesterol-lowering diet (low in saturated fat and cholesterol) as recommended by your doctor.
- Engage in regular physical activity.
- Maintain a healthy weight.
- Avoid excessive alcohol consumption.
- Quit smoking.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
10 mg to 20 mg orally once daily
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
Primary Hypercholesterolemia and Mixed Dyslipidemia:
Initial 10-20 mg once daily; Max 40 mg once daily.
Homozygous Familial Hypercholesterolemia (HoFH):
Initial 20 mg once daily; Max 40 mg once daily.
Atherosclerotic Cardiovascular Disease (ASCVD) Prevention:
Initial 5-20 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH) in patients 8 to <10 years: 5 mg to 10 mg orally once daily. HeFH in patients 10 to <18 years: 5 mg to 20 mg orally once daily.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH) in patients 10 to <18 years: 5 mg to 20 mg orally once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed (CrCl ≥60 mL/min/1.73m²).
Moderate:
No dose adjustment needed (CrCl 30-59 mL/min/1.73m²).
Severe:
Initial 5 mg once daily; Max 10 mg once daily (CrCl <30 mL/min/1.73m² and not on hemodialysis).
Dialysis:
Contraindicated in patients with severe renal impairment not on hemodialysis. For patients on hemodialysis, initial 5 mg once daily; Max 10 mg once daily.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A).
Moderate:
No dose adjustment needed (Child-Pugh B).
Severe:
Contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases (Child-Pugh C).
Pharmacology
Mechanism of Action
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor for cholesterol. This inhibition leads to a decrease in hepatic cholesterol synthesis, which in turn upregulates the expression of LDL receptors on hepatocyte surfaces, increasing the uptake and catabolism of LDL. It also inhibits hepatic synthesis of VLDL, thereby reducing total cholesterol, LDL-C, ApoB, and triglycerides, and increasing HDL-C.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20%
Tmax:
3-5 hours
FoodEffect:
Food does not affect the bioavailability of rosuvastatin, but Cmax may be reduced by about 20%.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to plasma proteins)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available (primarily eliminated unchanged)
ExcretionRoute:
Fecal (approximately 90%), Renal (approximately 10%)
Unchanged:
Approximately 90% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
Typically 2-4 weeks for maximal lipid-lowering effect
DurationOfAction:
24 hours (due to once-daily dosing)
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Memory problems or loss
Feeling confused
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid droop
This medication may also cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. The risk of muscle problems may be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, and even death. If you experience abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell), contact your doctor immediately. If muscle problems persist after stopping the medication, seek medical attention right away.
Additionally, liver problems have been reported with similar medications, and in some cases, have been fatal. If you notice any signs of liver problems, such as:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
contact your doctor immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to report any concerns to your doctor. Common side effects include:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
If you experience any of these side effects or any other symptoms that bother you or do not go away, contact your doctor for advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Memory problems or loss
Feeling confused
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid droop
This medication may also cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. The risk of muscle problems may be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, and even death. If you experience abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell), contact your doctor immediately. If muscle problems persist after stopping the medication, seek medical attention right away.
Additionally, liver problems have been reported with similar medications, and in some cases, have been fatal. If you notice any signs of liver problems, such as:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
contact your doctor immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to report any concerns to your doctor. Common side effects include:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
If you experience any of these side effects or any other symptoms that bother you or do not go away, contact your doctor for advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine (could indicate a serious muscle problem called rhabdomyolysis).
- Yellowing of the skin or eyes (jaundice), dark urine, light-colored stools, or unusual fatigue (could indicate liver problems).
- Severe stomach pain, nausea, or vomiting.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes, as this may affect your ability to take this medication.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis, as these may interact with this drug.
If you are pregnant or think you may be pregnant. It is crucial to note that you should not take this medication if you are pregnant.
* If you are breastfeeding. You should not breastfeed while taking this medication.
This list is not exhaustive, and it is vital to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes, as this may affect your ability to take this medication.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis, as these may interact with this drug.
If you are pregnant or think you may be pregnant. It is crucial to note that you should not take this medication if you are pregnant.
* If you are breastfeeding. You should not breastfeed while taking this medication.
This list is not exhaustive, and it is vital to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
This drug may cause an increase in blood sugar levels, potentially leading to new-onset diabetes or worsening of existing diabetes. Therefore, it is crucial to monitor your blood sugar levels as directed by your doctor.
Regular blood tests, as advised by your doctor, are necessary to ensure safe use of this medication. Be sure to discuss any concerns or questions with your doctor.
To minimize the risk of severe side effects, do not exceed the prescribed dosage. Adhere to the diet and exercise plan recommended by your doctor to optimize the benefits of this medication.
Limit alcohol consumption to no more than 2 drinks per day, as excessive alcohol intake may increase the risk of liver disease.
If you are of Asian descent, exercise caution when using this drug, as you may be more susceptible to side effects. Similarly, individuals 65 years or older should use this medication with caution, as they may also be at a higher risk of experiencing side effects.
This medication may pose a risk to an unborn baby. If you are pregnant or plan to become pregnant, it is essential to use effective birth control while taking this drug. If you become pregnant, notify your doctor immediately.
This drug may cause an increase in blood sugar levels, potentially leading to new-onset diabetes or worsening of existing diabetes. Therefore, it is crucial to monitor your blood sugar levels as directed by your doctor.
Regular blood tests, as advised by your doctor, are necessary to ensure safe use of this medication. Be sure to discuss any concerns or questions with your doctor.
To minimize the risk of severe side effects, do not exceed the prescribed dosage. Adhere to the diet and exercise plan recommended by your doctor to optimize the benefits of this medication.
Limit alcohol consumption to no more than 2 drinks per day, as excessive alcohol intake may increase the risk of liver disease.
If you are of Asian descent, exercise caution when using this drug, as you may be more susceptible to side effects. Similarly, individuals 65 years or older should use this medication with caution, as they may also be at a higher risk of experiencing side effects.
This medication may pose a risk to an unborn baby. If you are pregnant or plan to become pregnant, it is essential to use effective birth control while taking this drug. If you become pregnant, notify your doctor immediately.
Overdose Information
Overdose Symptoms:
- No specific symptoms of overdose have been reported. The most likely effects would be an exaggeration of known side effects, such as muscle pain or liver enzyme elevations.
What to Do:
There is no specific antidote for rosuvastatin overdose. Treatment should be symptomatic and supportive. Hemodialysis is not expected to be beneficial due to high protein binding. Contact a poison control center immediately (e.g., call 1-800-222-1222 in the US).
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
- Gemfibrozil (increases rosuvastatin exposure and risk of myopathy/rhabdomyolysis)
Major Interactions
- Warfarin (enhances anticoagulant effect, monitor INR)
- Protease Inhibitors (e.g., atazanavir/ritonavir, lopinavir/ritonavir, tipranavir/ritonavir, simeprevir; significantly increase rosuvastatin exposure, dose limitation required)
- Regorafenib (increases rosuvastatin exposure)
- Fostamatinib (increases rosuvastatin exposure)
- Capmatinib (increases rosuvastatin exposure)
- Febuxostat (increases rosuvastatin exposure)
- Teriflunomide (increases rosuvastatin exposure)
Moderate Interactions
- Niacin (high doses, >1g/day; increased risk of myopathy/rhabdomyolysis)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
- Ezetimibe (increased risk of myopathy/rhabdomyolysis)
- Antacids (aluminum and magnesium hydroxide; decreases rosuvastatin plasma concentrations, administer antacid 2 hours after rosuvastatin)
- Erythromycin (decreases rosuvastatin exposure)
- Oral Contraceptives (increases ethinyl estradiol and norgestrel AUC)
- Fibrates (other than gemfibrozil, e.g., fenofibrate; increased risk of myopathy/rhabdomyolysis)
Minor Interactions
- Coumarin anticoagulants (monitor INR)
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess treatment efficacy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST)
Rationale: To establish baseline liver enzyme levels and monitor for drug-induced hepatotoxicity.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline CK levels, especially in patients at increased risk for myopathy (e.g., renal impairment, hypothyroidism, genetic muscle disorders, history of statin-associated myopathy).
Timing: Prior to initiation of therapy (if indicated).
Routine Monitoring
Lipid Panel
Frequency: 4-12 weeks after initiation or dose titration, then every 3-12 months or as clinically indicated.
Target: LDL-C reduction based on ASCVD risk (e.g., >50% reduction for high-intensity, 30-49% for moderate-intensity).
Action Threshold: If lipid goals not met, consider dose titration or combination therapy. If levels are excessively low, consider dose reduction.
Liver Function Tests (ALT, AST)
Frequency: As clinically indicated. Routine periodic monitoring is not recommended unless clinically indicated (e.g., symptoms suggestive of liver injury).
Target: Within normal limits or stable.
Action Threshold: If persistent elevations >3 times the upper limit of normal (ULN), discontinue rosuvastatin. If elevations are <3x ULN and asymptomatic, continue monitoring.
Creatine Kinase (CK)
Frequency: As clinically indicated (e.g., if patient reports muscle pain, tenderness, or weakness). Routine periodic monitoring is not recommended.
Target: Within normal limits.
Action Threshold: If CK levels are significantly elevated (>10 times ULN) or if muscle symptoms are severe, discontinue rosuvastatin. If CK elevations are 5-10 times ULN, consider temporary discontinuation and re-evaluation.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (myopathy/rhabdomyolysis)
- Dark urine (rhabdomyolysis)
- Unusual fatigue or weakness
- Loss of appetite
- Upper abdominal pain
- Nausea, vomiting
- Yellowing of skin or eyes (jaundice)
- Flu-like symptoms
Special Patient Groups
Pregnancy
Rosuvastatin is contraindicated in pregnancy (Pregnancy Category X). Cholesterol and its derivatives are essential for fetal development. Statins may cause fetal harm. Discontinue immediately if pregnancy occurs.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity due to interference with cholesterol synthesis, which is critical for cell membranes and steroid hormones.
Second Trimester:
Continued risk of fetal harm.
Third Trimester:
Continued risk of fetal harm.
Lactation
Rosuvastatin is contraindicated during breastfeeding. It is unknown if rosuvastatin is excreted in human milk, but other statins are. Due to the potential for serious adverse reactions in breastfed infants, women taking rosuvastatin should not breastfeed.
Infant Risk:
High risk (L5) - potential for serious adverse effects due to interference with infant lipid metabolism.
Pediatric Use
Approved for Heterozygous Familial Hypercholesterolemia (HeFH) in patients 8 years and older. Dosing varies by age group. Safety and efficacy in children younger than 8 years have not been established. Monitor for growth and pubertal development in pediatric patients.
Geriatric Use
No overall differences in efficacy or safety were observed between elderly (>65 years) and younger patients. However, due to increased prevalence of renal impairment and potential for drug interactions, careful dose selection and monitoring are advised. No specific dose adjustment is required based on age alone.
Clinical Information
Clinical Pearls
- Rosuvastatin can be taken at any time of day, with or without food, as its absorption is not significantly affected by food and its long half-life allows for flexible dosing.
- Patients of Asian descent may have higher plasma concentrations of rosuvastatin; consider starting at a lower dose (e.g., 5 mg) in these patients.
- Counsel patients to report any unexplained muscle pain, tenderness, or weakness immediately, especially if accompanied by fever or dark urine.
- Avoid grapefruit juice in large quantities, although the interaction with rosuvastatin is less significant than with some other statins (e.g., simvastatin).
- Ensure patients understand the importance of lifestyle modifications (diet, exercise) in conjunction with medication for optimal lipid management.
Alternative Therapies
- Other HMG-CoA Reductase Inhibitors (Statins): Atorvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin
- PCSK9 Inhibitors: Alirocumab, Evolocumab
- Cholesterol Absorption Inhibitors: Ezetimibe
- Fibrates: Fenofibrate, Gemfibrozil
- Niacin (Nicotinic Acid)
- Bile Acid Sequestrants: Cholestyramine, Colestipol, Colesevelam
- Adenosine Triphosphate-Citrate Lyase (ACL) Inhibitors: Bempedoic Acid
- Omega-3 Fatty Acid Esters: Icosapent ethyl, Omega-3-acid ethyl esters
Cost & Coverage
Average Cost:
$10 - $300+ per 30 tablets (generic vs. brand)
Generic Available:
Yes
Insurance Coverage:
Tier 1 (generic) or Tier 2-3 (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.