Crestor 40mg 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
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 medicine called a 'statin' that helps lower high cholesterol and triglycerides in your blood. It works by reducing the amount of 'bad' cholesterol (LDL) your liver makes and increasing the amount of 'good' cholesterol (HDL). This helps reduce your risk of heart disease and stroke.
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
- Maintain a heart-healthy diet low in saturated and trans fats, and cholesterol.
- Engage in regular physical activity as recommended by your doctor.
- Achieve and maintain a healthy weight.
- Quit smoking.
- Limit alcohol intake.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
5 to 40 mg orally once daily
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
primaryHyperlipidemia:
10-20 mg once daily, may increase to 40 mg
homozygousFamilialHypercholesterolemia:
20 mg once daily, may increase to 40 mg
severeHypercholesterolemia:
Initial 20 mg once daily, maximum 40 mg once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH): 8-10 years: 5-20 mg once daily; 10-17 years: 5-20 mg once daily (max 20 mg for most patients, 40 mg for severe cases under specialist supervision)
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10-17 years: 5-20 mg once daily (max 20 mg for most patients, 40 mg for severe cases under specialist supervision)
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed (CrCl âĨ 60 mL/min)
Moderate:
Initial 5 mg once daily, max 20 mg once daily (CrCl 30-59 mL/min)
Severe:
Initial 5 mg once daily, max 10 mg once daily (CrCl < 30 mL/min, not on hemodialysis)
Dialysis:
Initial 5 mg once daily, max 10 mg once daily. Not removed by hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A)
Moderate:
No dose adjustment needed (Child-Pugh B), but caution advised. Monitor LFTs.
Severe:
Contraindicated in active liver disease or unexplained persistent elevations of serum transaminases.
Pharmacology
Mechanism of Action
Rosuvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of 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 bioavailability, but Tmax may be delayed.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to plasma albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available (systemic clearance is approximately 31 L/hr)
ExcretionRoute:
Approximately 90% excreted unchanged in feces (primarily unabsorbed drug and biliary excretion), approximately 5% in urine.
Unchanged:
Approximately 90% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Maintained with continued dosing
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
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 immediately:
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
Muscle-Related Side Effects
This medication may cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. Your risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney issues, and even death. Contact your doctor immediately if you experience:
Abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell)
Muscle problems that persist after stopping the medication
Liver-Related Side Effects
Drugs like this one have been associated with liver problems, which can be fatal. Seek medical help right away if you notice:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. 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 immediately:
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
Muscle-Related Side Effects
This medication may cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. Your risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney issues, and even death. Contact your doctor immediately if you experience:
Abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell)
Muscle problems that persist after stopping the medication
Liver-Related Side Effects
Drugs like this one have been associated with liver problems, which can be fatal. Seek medical help right away if you notice:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. 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 feeling unwell)
- Dark-colored urine
- Yellowing of your skin or the whites of your eyes (jaundice)
- Unusual tiredness or weakness
- Loss of appetite
- Upper 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.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis.
If you are pregnant or think you may be pregnant. Note that this medication should not be taken during pregnancy.
* If you are breastfeeding. You should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial 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 adjust the dosage 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.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis.
If you are pregnant or think you may be pregnant. Note that this medication should not be taken during pregnancy.
* If you are breastfeeding. You should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial 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 adjust the dosage 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.
One of the potential side effects of this drug is high blood sugar, which may lead to the development of new-onset diabetes or worsen existing diabetes. To monitor this, follow your doctor's instructions for checking your blood sugar levels. Additionally, adhere to the schedule set by your doctor for blood work checks, and discuss any concerns or questions with your doctor.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. It is also crucial to follow the diet and exercise plan recommended by your doctor.
Limit your alcohol consumption to no more than 2 drinks per day, as excessive alcohol intake may increase your risk of developing liver disease.
If you are of Asian descent, exercise caution when using this medication, as you may be more susceptible to side effects. Similarly, if you are 65 years or older, use this drug with caution due to the potential for increased side effects.
This medication may pose a risk to an unborn baby. If you are of childbearing potential, it is essential to use birth control while taking this drug. If you become pregnant, notify your doctor immediately.
One of the potential side effects of this drug is high blood sugar, which may lead to the development of new-onset diabetes or worsen existing diabetes. To monitor this, follow your doctor's instructions for checking your blood sugar levels. Additionally, adhere to the schedule set by your doctor for blood work checks, and discuss any concerns or questions with your doctor.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. It is also crucial to follow the diet and exercise plan recommended by your doctor.
Limit your alcohol consumption to no more than 2 drinks per day, as excessive alcohol intake may increase your risk of developing liver disease.
If you are of Asian descent, exercise caution when using this medication, as you may be more susceptible to side effects. Similarly, if you are 65 years or older, use this drug with caution due to the potential for increased side effects.
This medication may pose a risk to an unborn baby. If you are of childbearing potential, it is essential to use 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 effective. Contact a poison control center immediately (1-800-222-1222).
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
- Co-administration with gemfibrozil (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Active liver disease
Major Interactions
- Warfarin (increased INR/bleeding risk)
- Protease inhibitors (e.g., atazanavir/ritonavir, lopinavir/ritonavir, tipranavir/ritonavir, fosamprenavir/ritonavir, darunavir/ritonavir, simeprevir, sofosbuvir/velpatasvir/voxilaprevir) - significantly increase rosuvastatin exposure, max rosuvastatin dose 10-20 mg depending on specific regimen
- Fibrates (e.g., fenofibrate) - increased risk of myopathy/rhabdomyolysis
- Niacin (lipid-lowering doses, âĨ1 g/day) - increased risk of myopathy/rhabdomyolysis
- Colchicine - increased risk of myopathy/rhabdomyolysis
Moderate Interactions
- Antacids (aluminum and magnesium hydroxide) - decreases rosuvastatin plasma concentrations (administer antacids 2 hours after rosuvastatin)
- Erythromycin - decreases rosuvastatin plasma concentrations
- Oral contraceptives - increases ethinyl estradiol and norgestrel plasma concentrations
- Fusidic acid (systemic) - increased risk of myopathy/rhabdomyolysis (avoid co-administration)
Minor Interactions
- Not specifically listed as minor for rosuvastatin, but general caution with other drugs metabolized by minor CYP pathways.
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 assess baseline liver function and identify pre-existing liver disease. Statins can cause transaminase elevations.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline in patients at increased risk for myopathy (e.g., renal impairment, hypothyroidism, genetic muscle disorders, prior statin-associated muscle toxicity).
Timing: Prior to initiation of therapy (if indicated).
Routine Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Frequency: 4-12 weeks after initiation or dose titration, then every 3-12 months or as clinically indicated.
Target: Individualized based on risk assessment and guideline recommendations (e.g., LDL-C reduction goals).
Action Threshold: Failure to meet lipid goals, or if lipid levels worsen.
Liver Function Tests (ALT, AST)
Frequency: Generally not routinely recommended unless clinically indicated (e.g., symptoms of liver injury, dose increase to 40 mg).
Target: ALT/AST < 3 times upper limit of normal (ULN).
Action Threshold: Persistent elevations > 3 times ULN; discontinue or reduce dose.
Creatine Kinase (CK)
Frequency: Not routinely recommended unless muscle symptoms (pain, tenderness, weakness) develop.
Target: CK < 10 times ULN.
Action Threshold: CK > 10 times ULN or if muscle symptoms are severe; discontinue rosuvastatin. If CK < 10 times ULN but symptoms are bothersome, consider dose reduction or temporary discontinuation.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (especially if accompanied by malaise or fever)
- Dark urine
- Yellowing of skin or eyes (jaundice)
- Unusual fatigue or weakness
- Loss of appetite
- Abdominal pain
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 rosuvastatin as soon as pregnancy is detected.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm due to interference with cholesterol synthesis, which is critical for cell membranes and steroid hormone synthesis.
Second Trimester:
Continued risk of fetal harm.
Third Trimester:
Continued risk of fetal harm.
Lactation
Rosuvastatin is contraindicated during breastfeeding (Lactation Risk L5). 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 of serious adverse effects due to potential for interference with infant lipid metabolism and development.
Pediatric Use
Rosuvastatin is indicated for heterozygous familial hypercholesterolemia (HeFH) in pediatric patients aged 8 years and older, and for homozygous familial hypercholesterolemia (HoFH) in pediatric patients aged 7 years and older. Dosing should be individualized and initiated at lower doses (e.g., 5 mg) with careful titration. Max dose for most pediatric patients with HeFH is 20 mg/day, but 40 mg/day may be used for severe cases under specialist supervision.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. However, due to increased susceptibility to myopathy in the elderly, caution is advised, and the lowest effective dose should be used. 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 long half-life (19 hours) makes timing less critical than for some other statins.
- For patients of Asian descent, a lower starting dose (e.g., 5 mg) is recommended due to higher systemic exposure to rosuvastatin.
- The 40 mg dose of rosuvastatin should be reserved for patients who have not achieved their LDL-C goal with 20 mg and are under specialist supervision, as it carries a higher risk of muscle-related adverse events.
- Patients should be advised to report any unexplained muscle pain, tenderness, or weakness immediately, especially if accompanied by fever or malaise.
- Rosuvastatin is a substrate for the OATP1B1 transporter; co-administration with inhibitors of this transporter (e.g., cyclosporine, some protease inhibitors) can significantly increase rosuvastatin exposure and risk of myopathy.
Alternative Therapies
- Other HMG-CoA reductase inhibitors (statins): Atorvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin
- Cholesterol absorption inhibitors: Ezetimibe
- PCSK9 inhibitors: Alirocumab, Evolocumab
- Fibrates: Gemfibrozil, Fenofibrate (primarily for triglycerides)
- Niacin (Nicotinic Acid): (primarily for triglycerides and HDL-C)
- Bile acid sequestrants: Cholestyramine, Colestipol, Colesevelam
- Adenosine triphosphate-citrate lyase (ACL) inhibitors: Bempedoic acid
- Omega-3 fatty acid ethyl esters: Icosapent ethyl, Omega-3-acid ethyl esters (primarily for triglycerides)
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 for generic rosuvastatin 40mg, $200-$400+ for brand Crestor 40mg per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Generic rosuvastatin is typically covered as a Tier 1 or Tier 2 medication. Brand-name Crestor may be Tier 2 or Tier 3, or require prior authorization.
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 your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.