Rosuvastatin 5mg 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 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 body 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, 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
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, 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
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
- Take this medication exactly as prescribed, usually once daily, with or without food. Consistency in timing is more important than taking it at a specific time of day.
- 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 intake.
- Quit smoking.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg to 20 mg orally once daily, typically in the evening.
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
hyperlipidemia:
Initial dose 5-10 mg once daily. Max dose 40 mg once daily.
homozygousFamilialHypercholesterolemia:
20 mg once daily.
severeRenalImpairment:
Initial dose 5 mg once daily, max 10 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH) in patients 8 to <10 years: 5-10 mg once daily. HeFH in patients 10 to <17 years: 5-20 mg once daily. Homozygous Familial Hypercholesterolemia (HoFH) in patients 7 to <17 years: 20 mg once daily.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH) in patients 10 to <17 years: 5-20 mg once daily. Homozygous Familial Hypercholesterolemia (HoFH) in patients 7 to <17 years: 20 mg once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary.
Severe:
CrCl <30 mL/min/1.73m² (not on hemodialysis): Initiate with 5 mg once daily, do not exceed 10 mg once daily.
Dialysis:
No dose adjustment necessary for patients on hemodialysis, but use with caution. Contraindicated in severe renal impairment not on dialysis.
Hepatic Impairment:
Mild:
No dose adjustment necessary (Child-Pugh A).
Moderate:
No dose adjustment necessary (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, 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 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 about 20%.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to plasma proteins, mainly albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available
ExcretionRoute:
Primarily fecal (approximately 90%), with a minor renal component (approximately 10%)
Unchanged:
Approximately 90% (feces), approximately 5% (urine)
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects are evident within 1 week of therapy.
PeakEffect:
Maximum therapeutic response is generally achieved within 2-4 weeks.
DurationOfAction:
Sustained with once-daily dosing due to long half-life and irreversible binding to the enzyme.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention 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 help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Memory problems or loss
Feeling confused
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid droop
This medication may also cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. Your risk may be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, and even death. If you experience abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell), contact your doctor immediately. If muscle problems persist after stopping the medication, seek medical attention right away.
Additionally, liver problems have been reported with similar medications, and in some cases, have been fatal. If you notice any signs of liver problems, such as:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
contact your doctor immediately.
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you notice any of the following side effects, or if they bother you or 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 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 help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Memory problems or loss
Feeling confused
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid droop
This medication may also cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. Your risk may be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, and even death. If you experience abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell), contact your doctor immediately. If muscle problems persist after stopping the medication, seek medical attention right away.
Additionally, liver problems have been reported with similar medications, and in some cases, have been fatal. If you notice any signs of liver problems, such as:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
contact your doctor immediately.
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you notice any of the following side effects, or if they bother you or 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 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 (could be signs of rhabdomyolysis, a serious muscle condition).
- Yellowing of the skin or eyes (jaundice), dark urine, or unusual fatigue (could be signs of liver problems).
- Severe stomach pain.
- Swelling of the face, lips, tongue, or throat (signs of an allergic reaction).
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. To monitor this, follow your doctor's instructions for checking your blood sugar levels. Additionally, adhere to the schedule recommended by your doctor for getting blood work done, and discuss the results with them.
To minimize the risk of severe side effects, do not exceed the prescribed dosage. It is crucial to follow the diet and exercise plan outlined 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 due to the potential for increased 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 recommended by your doctor for getting blood work done, and discuss the results with them.
To minimize the risk of severe side effects, do not exceed the prescribed dosage. It is crucial to follow the diet and exercise plan outlined 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 due to the potential for increased 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 adverse 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. 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, risk of myopathy/rhabdomyolysis)
- Lopinavir/Ritonavir, Atazanavir/Ritonavir, Darunavir/Ritonavir, Tipranavir/Ritonavir, Fosamprenavir/Ritonavir (and other protease inhibitor combinations: significantly increase rosuvastatin exposure, risk of myopathy/rhabdomyolysis)
- Regorafenib (increases rosuvastatin exposure)
- Warfarin (may increase INR, monitor closely)
Moderate Interactions
- Niacin (lipid-lowering doses, risk of myopathy/rhabdomyolysis)
- Colchicine (risk of myopathy/rhabdomyolysis)
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases plasma concentrations of ethinyl estradiol and norgestrel)
- Antacids containing aluminum and magnesium hydroxide (decreases rosuvastatin absorption, administer rosuvastatin 2 hours after antacid)
- Fostamatinib (increases rosuvastatin exposure)
- Capmatinib (increases rosuvastatin exposure)
- Febuxostat (increases rosuvastatin exposure)
Minor Interactions
- No specific minor interactions requiring dose adjustment or close monitoring are commonly cited beyond general caution.
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, which is a contraindication.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish a baseline in patients at increased risk for myopathy (e.g., renal impairment, hypothyroidism, genetic muscle disorders, prior statin-associated myopathy).
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 goals).
Action Threshold: If lipid goals are not met, consider dose adjustment or alternative 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 but persistent, monitor closely or consider dose reduction/discontinuation.
Creatine Kinase (CK)
Frequency: Not routinely recommended unless 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 immediately. If CK levels are elevated but <10x ULN and symptoms are mild, monitor closely or consider temporary discontinuation.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (especially if accompanied by malaise or fever)
- Dark-colored 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 (Pregnancy Category X). Cholesterol and its derivatives are essential for fetal development. Inhibition of HMG-CoA reductase could cause fetal harm. Discontinue immediately if pregnancy occurs.
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 (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, breastfeeding is not recommended.
Infant Risk:
High risk. Potential for serious adverse effects in the infant, including interference with lipid metabolism.
Pediatric Use
Approved for heterozygous familial hypercholesterolemia (HeFH) in children ≥8 years and homozygous familial hypercholesterolemia (HoFH) in children ≥7 years. Dosing is age and condition-specific. Safety and efficacy have not been established in patients younger than 7 years of age.
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 patients with severe renal impairment, which may be more prevalent in the elderly. Dose adjustments may be necessary based on renal function and individual patient response.
Clinical Information
Clinical Pearls
- Rosuvastatin has a relatively long half-life, allowing for once-daily dosing at any time of day, though consistency is recommended.
- It has a lower potential for CYP450-mediated drug interactions compared to some other statins (e.g., simvastatin, atorvastatin) due to its limited metabolism by these enzymes.
- The 40 mg dose should be reserved for patients who have not achieved their LDL-C goal with 20 mg and are at high cardiovascular risk, and should be used with caution due to increased risk of myopathy.
- Patients of Asian descent may have increased systemic exposure to rosuvastatin; consider initiating at 5 mg and titrating cautiously.
- Educate patients on the importance of reporting any muscle pain, tenderness, or weakness immediately.
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
- Bile acid sequestrants: Cholestyramine, Colestipol, Colesevelam
- Niacin (Nicotinic acid)
- Adenosine triphosphate-citrate lyase (ACL) inhibitors: Bempedoic acid
Cost & Coverage
Average Cost:
$10 - $50 per 30 tablets (generic 5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.