Rosuvastatin 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
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 your blood. It works by reducing the amount of 'bad' cholesterol (LDL) your body makes and increasing 'good' cholesterol (HDL). This helps to reduce your risk of heart disease, heart attacks, and strokes.
How to Use This Medicine
Taking Your Medication
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 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 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 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
- Take this medication exactly as prescribed, usually once a day, with or without food.
- Do not stop taking rosuvastatin without talking to your doctor, even if you feel well.
- Continue to follow a cholesterol-lowering diet (low in saturated fat and cholesterol) as recommended by your doctor or dietitian.
- Engage in regular physical activity as advised by your healthcare provider.
- Limit alcohol consumption.
- Inform your doctor about all other medications, supplements, and herbal products you are taking, as some can interact with rosuvastatin.
- Avoid grapefruit juice in large quantities, although the interaction is less significant than with some other statins.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
10 mg orally 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 every 2-4 weeks. Max 40 mg once daily.
homozygous familial hypercholesterolemia (HoFH):
20 mg once daily initially, up to 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): 8 to <10 years: 5-10 mg once daily. 10 to <18 years: 5-20 mg once daily. Max 20 mg/day.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10 to <18 years: 5-20 mg once daily. Max 20 mg/day.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required.
Moderate:
No dose adjustment required.
Severe:
CrCl < 30 mL/min (not on hemodialysis): Initiate with 5 mg once daily. Do not exceed 10 mg once daily.
Dialysis:
Contraindicated in patients with severe renal impairment not on hemodialysis. For patients on hemodialysis, use with caution, consider 5 mg initial dose, max 10 mg.
Hepatic Impairment:
Mild:
Child-Pugh A: No dose adjustment required.
Moderate:
Child-Pugh B: No dose adjustment required.
Severe:
Child-Pugh C: Contraindicated.
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 the hepatocyte surface, increasing the uptake and catabolism of circulating LDL. It also inhibits hepatic synthesis of VLDL, thereby reducing total cholesterol, LDL-C, VLDL-C, 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 20% when taken with food.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not readily quantifiable as it is primarily eliminated unchanged via feces.
ExcretionRoute:
Primarily fecal (approximately 90% as unchanged drug), with a small renal component (approximately 10%).
Unchanged:
Approximately 90% (fecal)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
Maximum LDL-C reduction typically achieved within 2-4 weeks of starting therapy or dose titration.
DurationOfAction:
Sustained with once-daily dosing due to long half-life and irreversible binding to HMG-CoA reductase.
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 attention 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 or seek medical help:
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 attention 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 or seek medical help:
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 dark urine)
- Yellowing of the skin or eyes (jaundice)
- Unusual tiredness or weakness
- Loss of appetite
- Upper stomach 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 alongside your other treatments 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 alongside your other treatments 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 regular blood work to ensure your health is closely monitored. If you have any concerns or questions, discuss them with your doctor.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. It is crucial to follow the diet and exercise plan recommended by your doctor to maintain optimal health while taking 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 due to the potential for increased side effects.
This drug may pose a risk to an unborn baby. If you are pregnant or planning to become pregnant, it is crucial to use effective 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 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 regular blood work to ensure your health is closely monitored. If you have any concerns or questions, discuss them with your doctor.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. It is crucial to follow the diet and exercise plan recommended by your doctor to maintain optimal health while taking 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 due to the potential for increased side effects.
This drug may pose a risk to an unborn baby. If you are pregnant or planning to become pregnant, it is crucial to use effective 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. 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)
Major Interactions
- Gemfibrozil (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Warfarin (may increase INR, monitor closely)
- Protease inhibitors (e.g., atazanavir/ritonavir, lopinavir/ritonavir, simeprevir, sofosbuvir/velpatasvir/voxilaprevir, glecaprevir/pibrentasvir - significantly increase rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Regorafenib (increases rosuvastatin exposure)
- Fostamatinib (increases rosuvastatin exposure)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
- Niacin (high doses, increased risk of myopathy/rhabdomyolysis)
Moderate Interactions
- Antacids (containing aluminum and magnesium hydroxide, decrease rosuvastatin plasma concentrations if taken within 2 hours of rosuvastatin)
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases plasma concentrations of ethinyl estradiol and norgestrel)
- Ezetimibe (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis, concurrent use generally not recommended)
- Fenofibrate (increased risk of myopathy/rhabdomyolysis)
Minor Interactions
- Not specifically listed as minor, most interactions are clinically significant due to myopathy risk.
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 pre-existing liver disease, as statins can cause transaminase elevations.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline 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, alcoholism).
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: Individualized based on patient risk factors and guidelines (e.g., LDL-C reduction targets).
Action Threshold: If lipid goals are not met, consider dose adjustment or combination therapy. If lipid levels are excessively low, consider dose reduction.
Liver Function Tests (ALT, AST)
Frequency: Periodically, if clinically indicated (e.g., symptoms suggestive of liver injury). Routine periodic monitoring is no longer universally recommended unless symptoms occur.
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 or consider dose reduction.
Creatine Kinase (CK)
Frequency: Only if muscle symptoms (pain, tenderness, weakness) develop.
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 levels are elevated but <10x ULN and symptoms are mild, monitor closely or consider dose reduction.
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
- Loss of appetite
- Abdominal pain
Special Patient Groups
Pregnancy
Rosuvastatin is contraindicated in pregnancy. Cholesterol and its derivatives are essential for fetal development. Inhibition of HMG-CoA reductase during pregnancy may cause fetal harm. If a patient becomes pregnant while taking this drug, therapy 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 if rosuvastatin is excreted in human milk, but other statins are known to be. Due to the potential for serious adverse reactions in breastfed infants, women taking rosuvastatin should not breastfeed.
Infant Risk:
L5 (Contraindicated) - Potential for serious adverse effects in the infant, including interference with lipid metabolism.
Pediatric Use
Approved for heterozygous familial hypercholesterolemia (HeFH) in children β₯8 years of age and homozygous familial hypercholesterolemia (HoFH) in children β₯7 years of age. Dosing is age and weight-dependent, and lower maximum doses apply compared to adults. Safety and efficacy in children younger than 7 years have not been established.
Geriatric Use
No overall differences in efficacy or safety have been observed between elderly (>65 years) and younger patients. However, increased systemic exposure has been observed in Asian subjects and in patients with severe renal impairment. Use with caution in elderly patients due to potential for increased susceptibility to myopathy and other adverse effects, especially if other risk factors are present.
Clinical Information
Clinical Pearls
- Rosuvastatin is considered one of the most potent statins for LDL-C reduction.
- Unlike some other statins, rosuvastatin can be taken at any time of day, with or without food, as its absorption is not significantly affected.
- Patients of Asian descent may have higher plasma concentrations of rosuvastatin and should be considered for a lower starting dose (e.g., 5 mg) and careful titration.
- It is crucial to educate patients about the symptoms of myopathy/rhabdomyolysis and to report them immediately.
- Rosuvastatin is primarily eliminated unchanged in the feces, with minimal hepatic metabolism, which may be advantageous in patients with significant liver disease (though contraindicated in severe hepatic impairment).
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
- Selective peroxisome proliferator-activated receptor alpha (PPARΞ±) modulators: Pemafibrate (not FDA approved in US)
- Omega-3 fatty acid ethyl esters
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 for generic 30 tablets per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic), Tier 3 or higher (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 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.