Rosuvastatin 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, 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 called a 'statin' that helps lower high cholesterol and triglycerides in your blood. It works by reducing the amount of 'bad' cholesterol (LDL) your body makes and increasing the amount of 'good' cholesterol (HDL). This helps reduce your risk of heart disease, heart attacks, and strokes.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
You can take your medication with or without food.
If you are taking an antacid that contains aluminum or magnesium, wait at least 2 hours after taking your medication before taking the antacid.
Swallow your medication whole with a glass of water or another drink.
Storing and Disposing of Your Medication
To ensure your medication remains effective and safe:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Skip the missed dose and resume your regular dosing schedule.
* 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 these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
You can take your medication with or without food.
If you are taking an antacid that contains aluminum or magnesium, wait at least 2 hours after taking your medication before taking the antacid.
Swallow your medication whole with a glass of water or another drink.
Storing and Disposing of Your Medication
To ensure your medication remains effective and safe:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Skip the missed dose and resume your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for the missed dose.
Lifestyle & Tips
- Take this medication exactly as prescribed, usually once a day, with or without food.
- Continue to follow a cholesterol-lowering diet (low in saturated fat and cholesterol) as recommended by your doctor.
- Engage in regular physical activity as advised by your healthcare provider.
- Maintain a healthy weight.
- Limit alcohol intake.
- Do not stop taking rosuvastatin without talking to your doctor, even if you feel well, as cholesterol levels can rise again.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose 10-20 mg orally once daily; maximum 40 mg orally once daily.
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
Hypercholesterolemia:
Initial 10-20 mg once daily; max 40 mg once daily. For severe hypercholesterolemia or aggressive lipid targets, 20 mg initial dose may be considered.
Homozygous Familial Hypercholesterolemia (HoFH):
20 mg once daily. Max 40 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH): 8 to <10 years: 5-10 mg orally once daily. 10 to <17 years: 5-20 mg orally once daily.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10 to <17 years: 5-20 mg orally once daily. Homozygous Familial Hypercholesterolemia (HoFH): 7 to <17 years: 20 mg orally once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed (CrCl âĨ60 mL/min).
Moderate:
No dose adjustment needed (CrCl 30-59 mL/min).
Severe:
Initial dose 5 mg once daily; maximum 10 mg once daily (CrCl <30 mL/min, not on hemodialysis).
Dialysis:
Contraindicated in patients on 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.
Note:
Exposure is increased in patients with chronic alcohol liver disease.
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 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 reduces hepatic production of VLDL and LDL.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20%
Tmax:
3-5 hours
FoodEffect:
Food decreases the rate but not the extent of absorption.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available
ExcretionRoute:
Approximately 90% excreted unchanged in feces (primarily unabsorbed drug and biliary excretion); approximately 5% excreted in urine.
Unchanged:
Approximately 90% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Not available (effects persist as long as therapy continues)
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
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 Side Effects
Most people do not experience significant side effects, but some may occur. If you are bothered by any of the following side effects or if they do not go away, contact your doctor:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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 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
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 Side Effects
Most people do not experience significant side effects, but some may occur. If you are bothered by any of the following side effects or if they do not go away, contact your doctor:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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). This could be a sign of a serious muscle problem.
- Dark-colored urine.
- Yellowing of your skin or the whites of your eyes (jaundice).
- Unusual tiredness or weakness.
- Loss of appetite.
- Pain in your upper stomach.
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 medication.
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 conditions 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 medication.
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 conditions 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.
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. 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 them.
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 to ensure safe and effective use of this medication.
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 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. 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 them.
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 to ensure safe and effective use of this medication.
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 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 adverse 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 case of overdose, treatment should be symptomatic and supportive. Hemodialysis is unlikely to be of benefit due to high protein binding. Contact a poison control center immediately (e.g., 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)
- Lopinavir/ritonavir, Atazanavir/ritonavir, Simeprevir, Sofosbuvir/velpatasvir/voxilaprevir (significantly increase rosuvastatin exposure, dose limitation required)
- Regorafenib (increases rosuvastatin exposure)
- Fibrates (e.g., fenofibrate, increased risk of myopathy/rhabdomyolysis)
- Niacin (lipid-lowering doses, increased risk of myopathy/rhabdomyolysis)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
Moderate Interactions
- Antacids (aluminum and magnesium hydroxide, decreases rosuvastatin plasma concentrations if given simultaneously; administer rosuvastatin 2 hours after antacid)
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases ethinyl estradiol and norgestrel concentrations)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis, temporary discontinuation of statin recommended)
- Darolutamide (increases rosuvastatin exposure)
Minor Interactions
- Not available (most clinically significant interactions are moderate to major)
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 and rule out active liver disease.
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).
Timing: Prior to initiation of therapy, if clinically 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: LDL-C reduction based on patient risk category (e.g., <100 mg/dL, <70 mg/dL, or 30-50% reduction).
Action Threshold: If lipid goals are not met, consider dose titration or combination therapy. If lipid levels are excessively low, consider dose reduction.
Liver Function Tests (ALT, AST)
Frequency: Not routinely recommended unless clinically indicated (e.g., symptoms suggestive of liver injury).
Target: Within normal limits.
Action Threshold: If persistent elevations >3 times the upper limit of normal (ULN) occur, discontinue rosuvastatin. If elevations are <3x ULN, monitor closely.
Creatine Kinase (CK)
Frequency: Not routinely recommended unless symptoms of myopathy (e.g., muscle pain, tenderness, weakness) occur.
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 moderate and symptoms are mild, 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 urine
- Yellowing of skin or eyes (jaundice)
- Unusual fatigue or weakness
- Loss of appetite
- Upper right abdominal pain
Special Patient Groups
Pregnancy
Rosuvastatin is contraindicated in pregnancy. Cholesterol and its derivatives are essential for fetal development. Statins may cause fetal harm when administered to pregnant women. If a patient becomes pregnant while taking this drug, the drug should be discontinued immediately and the patient apprised of the potential hazard to the fetus.
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:
Potential for fetal harm.
Third Trimester:
Potential for fetal harm.
Lactation
Rosuvastatin is contraindicated during breastfeeding. It is unknown whether rosuvastatin is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants, women taking rosuvastatin should not breastfeed.
Infant Risk:
L5 (Contraindicated - high risk of adverse effects to infant or milk production)
Pediatric Use
Rosuvastatin is indicated for pediatric patients 8 years and older with heterozygous familial hypercholesterolemia (HeFH) and for pediatric patients 7 years and older with homozygous familial hypercholesterolemia (HoFH). Dosing is age and condition-specific. Safety and efficacy have not been established in patients younger than 7 years.
Geriatric Use
No overall differences in effectiveness or safety were observed between patients âĨ65 years of age and younger patients. However, due to increased susceptibility to myopathy and other adverse effects in the elderly, caution should be exercised, and the lowest effective dose should be considered. Renal function should be monitored.
Clinical Information
Clinical Pearls
- Rosuvastatin is one of the most potent statins for LDL-C reduction.
- The 40 mg dose should be reserved for patients who have not achieved their LDL-C goal with 20 mg and who are at high cardiovascular risk, or for patients with severe hypercholesterolemia, and should be used with caution due to increased risk of myopathy.
- Patients of Asian descent may have higher plasma concentrations of rosuvastatin; consider starting at 5 mg once daily.
- Educate patients on the importance of reporting any muscle pain, tenderness, or weakness immediately.
- Administer rosuvastatin at least 2 hours after aluminum and magnesium hydroxide antacids to avoid decreased absorption.
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
- Niacin (Nicotinic Acid)
- 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
Cost & Coverage
Average Cost:
$10 - $50 per 30 tablets (generic 40mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.