Crestor 10mg 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 triglyceride levels in your blood. It works by reducing the amount of 'bad' cholesterol (LDL) your liver makes and increasing the amount of 'good' cholesterol (HDL). Lowering cholesterol can help prevent heart disease, heart attacks, and strokes.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication at the same time every day. Continue taking it as directed by your doctor or healthcare provider, even if you're feeling well. You can take it with or without food.
If you're taking an antacid that contains aluminum or magnesium, wait at least 2 hours after taking this medication before taking the antacid. Swallow the 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, avoiding the bathroom. Keep all medications in a safe 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 once or take extra doses to make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication at the same time every day. Continue taking it as directed by your doctor or healthcare provider, even if you're feeling well. You can take it with or without food.
If you're taking an antacid that contains aluminum or magnesium, wait at least 2 hours after taking this medication before taking the antacid. Swallow the 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, avoiding the bathroom. Keep all medications in a safe 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 once or take extra doses to make up for the missed one.
Lifestyle & Tips
- Continue to follow a cholesterol-lowering diet (low in saturated fat and cholesterol) as recommended by your doctor.
- Engage in regular physical activity.
- Maintain a healthy weight.
- Limit alcohol consumption.
- Quit smoking.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
10 mg once daily
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
primary hyperlipidemia and mixed dyslipidemia:
Initial 10-20 mg once daily; dose can be adjusted after 2-4 weeks. Max 40 mg once daily.
homozygous familial hypercholesterolemia (HoFH):
20 mg once daily. Max 40 mg once daily.
severe renal impairment (CrCl <30 mL/min):
Initial 5 mg once daily; max 10 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH) in patients âĨ8 years: Initial 5-10 mg once daily, max 20 mg once daily. Homozygous Familial Hypercholesterolemia (HoFH) in patients âĨ7 years: 20 mg once daily, max 40 mg once daily.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH) in patients âĨ8 years: Initial 5-10 mg once daily, max 20 mg once daily. Homozygous Familial Hypercholesterolemia (HoFH) in patients âĨ7 years: 20 mg once daily, max 40 mg once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed (CrCl âĨ60 mL/min).
Moderate:
No dose adjustment needed (CrCl 30-60 mL/min).
Severe:
Initial 5 mg once daily, max 10 mg once daily (CrCl <30 mL/min, not on hemodialysis). Use is not recommended in patients with severe renal impairment not on hemodialysis.
Dialysis:
Initial 5 mg once daily, max 10 mg once daily. Rosuvastatin is not significantly removed by hemodialysis.
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.
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-C from the circulation. It also inhibits hepatic synthesis of VLDL, thereby reducing total cholesterol, LDL-C, VLDL-C, and triglycerides, and increasing HDL-C.
Pharmacokinetics
Absorption:
Bioavailability:
~20%
Tmax:
3-5 hours
FoodEffect:
Food does not significantly affect absorption.
Distribution:
Vd:
~134 L
ProteinBinding:
~90% (primarily to plasma albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
~19 hours
Clearance:
Not available
ExcretionRoute:
Primarily fecal (approximately 90%), with a small renal component (approximately 10%).
Unchanged:
Approximately 90% (fecal), approximately 5% (renal)
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects are evident within 1 week.
PeakEffect:
Maximum lipid-lowering effect is generally achieved within 2-4 weeks of starting therapy or dose titration.
DurationOfAction:
Effects persist as long as the drug is taken.
Safety & Warnings
Side Effects
Serious 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 Problems
This medication may cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. The risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, 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 Problems
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 Side Effects
Most people do not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
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 Problems
This medication may cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. The risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, 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 Problems
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 Side Effects
Most people do not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
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 dark urine)
- Yellowing of the skin or eyes (jaundice)
- Unusual fatigue or weakness
- Loss of appetite
- Upper right abdominal pain
- Nausea or vomiting
- Swelling in your hands or feet
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 might 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 might 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 worsening of existing diabetes. Therefore, it is crucial to monitor your blood sugar levels as directed by your doctor.
Regular blood tests are also necessary, as advised by your doctor, to ensure your safety while taking this medication. Be sure to discuss any concerns or questions you may have 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 maximize the benefits of this medication.
It is also important to limit your alcohol consumption to no more than 2 drinks per day, as excessive alcohol use may increase your risk of developing liver disease.
If you are of Asian descent, exercise caution when taking this drug, as you may be more susceptible to side effects. Similarly, if you are 65 years or older, use this medication with caution, as you may also be at a higher risk of experiencing side effects.
This drug may pose a risk to an unborn baby. If you are pregnant or plan to become pregnant, it is essential to use birth control while taking this medication. 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 worsening of existing diabetes. Therefore, it is crucial to monitor your blood sugar levels as directed by your doctor.
Regular blood tests are also necessary, as advised by your doctor, to ensure your safety while taking this medication. Be sure to discuss any concerns or questions you may have 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 maximize the benefits of this medication.
It is also important to limit your alcohol consumption to no more than 2 drinks per day, as excessive alcohol use may increase your risk of developing liver disease.
If you are of Asian descent, exercise caution when taking this drug, as you may be more susceptible to side effects. Similarly, if you are 65 years or older, use this medication with caution, as you may also be at a higher risk of experiencing side effects.
This drug may pose a risk to an unborn baby. If you are pregnant or plan to become pregnant, it is essential to use birth control while taking this medication. 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. In the event of an overdose, treatment should be symptomatic and supportive. Hemodialysis is not expected to be effective in removing rosuvastatin due to its high protein binding. Call 1-800-222-1222 (Poison Control Center) for advice.
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
Major Interactions
- Gemfibrozil (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Warfarin (may increase INR, monitor INR closely)
- Lopinavir/Ritonavir (increases rosuvastatin exposure)
- Atazanavir/Ritonavir (increases rosuvastatin exposure)
- Darunavir/Ritonavir (increases rosuvastatin exposure)
- Tipranavir/Ritonavir (increases rosuvastatin exposure)
- Fosamprenavir/Ritonavir (increases rosuvastatin exposure)
- Glecaprevir/Pibrentasvir (increases rosuvastatin exposure)
Moderate Interactions
- Antacids containing aluminum and magnesium hydroxide (decreases rosuvastatin plasma concentrations, administer antacid 2 hours after rosuvastatin)
- Erythromycin (decreases rosuvastatin exposure)
- Niacin (may increase risk of myopathy/rhabdomyolysis)
- Colchicine (may increase risk of myopathy/rhabdomyolysis)
- Other fibrates (e.g., fenofibrate, may increase risk of myopathy/rhabdomyolysis)
- Oral contraceptives (increases plasma concentrations of ethinyl estradiol and norgestrel)
Minor Interactions
- No specific minor interactions requiring dose adjustment or close monitoring are commonly cited beyond those listed.
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess the need for therapy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST)
Rationale: To establish baseline liver enzyme levels, as statins can cause transaminase elevations.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline CK levels, especially in patients with predisposing factors for myopathy (e.g., renal impairment, hypothyroidism, history of muscle toxicity with other lipid-lowering agents, genetic muscle disorders, alcohol abuse).
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 patient risk factors and guideline recommendations (e.g., LDL-C reduction targets).
Action Threshold: If lipid goals are not met, consider dose adjustment or addition of other therapies. If lipid levels are excessively low, consider dose reduction.
Liver Function Tests (ALT, AST)
Frequency: Routine periodic monitoring of LFTs is not generally recommended unless clinically indicated (e.g., symptoms suggestive of liver injury).
Target: ALT/AST <3 times the upper limit of normal (ULN).
Action Threshold: If persistent elevations of ALT/AST >3 times ULN occur, discontinue rosuvastatin. If elevations are less than 3 times ULN, continue monitoring and consider dose reduction or discontinuation if elevations persist or worsen.
Creatine Kinase (CK)
Frequency: Not routinely monitored unless muscle symptoms (pain, tenderness, weakness) develop.
Target: CK <10 times ULN.
Action Threshold: If CK levels are significantly elevated (>10 times ULN) or if muscle symptoms are severe, discontinue rosuvastatin. If muscle symptoms are mild and CK is <10 times ULN, monitor closely and consider dose reduction or temporary interruption.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (especially if accompanied by malaise or fever)
- Dark-colored urine
- Yellowing of the skin or eyes (jaundice)
- Unusual fatigue or weakness
- Loss of appetite
- Upper right abdominal pain
- Nausea or vomiting
Special Patient Groups
Pregnancy
Rosuvastatin is contraindicated in pregnancy. Cholesterol and its derivatives are essential for fetal development. Inhibition of HMG-CoA reductase may cause fetal harm. If a patient becomes pregnant while taking rosuvastatin, the drug should be discontinued immediately.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm due to interference with cholesterol synthesis, which is critical for organogenesis.
Second Trimester:
Continued risk of fetal harm.
Third Trimester:
Continued risk of fetal harm.
Lactation
Rosuvastatin is contraindicated during breastfeeding. It is unknown whether rosuvastatin is excreted in human milk, but other statins have been shown to pass into breast milk. Due to the potential for serious adverse reactions in nursing infants, women taking rosuvastatin should not breastfeed.
Infant Risk:
High risk (L5) due to potential for serious adverse effects on the infant, including interference with lipid metabolism.
Pediatric Use
Approved for use in pediatric patients aged âĨ7 years for homozygous familial hypercholesterolemia (HoFH) and âĨ8 years for heterozygous familial hypercholesterolemia (HeFH). Dosing is age and condition-dependent. Safety and efficacy have not been established in patients younger than 7 years for HoFH or younger than 8 years for HeFH.
Geriatric Use
No overall differences in efficacy or safety have been observed between elderly (>65 years) and younger patients, but greater sensitivity of some older individuals cannot be ruled out. No specific dose adjustment is required based on age alone, but careful consideration of renal function and potential for drug interactions is warranted.
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.
- It is one of the most potent statins in terms of LDL-C lowering, often achieving significant reductions at lower doses.
- Patients of Asian descent may have higher plasma concentrations of rosuvastatin and should be initiated on a lower dose (e.g., 5 mg) due to genetic polymorphisms in OATP1B1.
- Educate patients about the symptoms of myopathy (muscle pain, tenderness, weakness) and rhabdomyolysis (severe muscle pain, dark urine) and to report them immediately.
- Avoid concomitant use with cyclosporine. For other interacting drugs (e.g., gemfibrozil, certain protease inhibitors), dose adjustments or alternative therapies may be necessary.
- Regular follow-up for lipid panel and symptom monitoring is crucial to ensure efficacy and safety.
Alternative Therapies
- Other HMG-CoA reductase inhibitors (Statins): Atorvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin
- PCSK9 inhibitors: Alirocumab, Evolocumab
- Cholesterol absorption inhibitors: Ezetimibe
- Fibrates: Gemfibrozil, Fenofibrate
- Niacin (Nicotinic Acid)
- Bile acid sequestrants: Cholestyramine, Colestipol, Colesevelam
- Adenosine triphosphate-citrate lyase (ACL) inhibitors: Bempedoic acid
- Angiopoietin-like 3 (ANGPTL3) inhibitors: Evinacumab
Cost & Coverage
Average Cost:
$10 - $30 per 30 tablets (generic 10mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 (generic) or Tier 2/3 (brand) on most commercial and Medicare Part D plans.
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 taken, the amount, and the time it happened.