Crestor 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
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 (Crestor) 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 the amount of 'good' cholesterol (HDL). This helps to 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 your doctor's instructions carefully. Read all the information provided with your prescription 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 feeling 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 with your prescription 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 feeling 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
- Maintain a healthy diet low in saturated and trans fats, and cholesterol.
- Engage in regular physical activity as recommended by your doctor.
- Achieve and maintain a healthy weight.
- Quit smoking if you smoke.
- Limit alcohol consumption.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg once daily
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
primaryHyperlipidemia:
Initial 10-20 mg once daily; range 5-40 mg once daily. Max 40 mg/day.
homozygousFamilialHypercholesterolemia:
20 mg once daily. Max 40 mg/day.
primaryPreventionOfCardiovascularDisease:
Initial 5-10 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 <17 years: 5-20 mg once daily. Max 20 mg/day. Homozygous Familial Hypercholesterolemia (HoFH): 7 to <17 years: 20 mg once daily. Max 20 mg/day.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10 to <17 years: 5-20 mg once daily. Max 20 mg/day. Homozygous Familial Hypercholesterolemia (HoFH): 7 to <17 years: 20 mg once daily. Max 20 mg/day.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
CrCl <30 mL/min (non-dialysis): Initial 5 mg once daily, max 10 mg once daily. Contraindicated in HoFH patients with severe renal impairment.
Dialysis:
Contraindicated in patients on hemodialysis.
Hepatic Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
Child-Pugh score >9 (severe hepatic impairment): 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 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-C. It also inhibits hepatic synthesis of VLDL, thereby reducing total VLDL and triglyceride levels.
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 plasma albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available
ExcretionRoute:
Primarily feces (approximately 90% as unchanged drug and metabolites), minor renal excretion (approximately 5% as unchanged drug).
Unchanged:
Approximately 90% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Sustained with continued daily dosing
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Memory problems or loss
Feeling confused
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid droop
Muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications, or are 65 or older
Severe muscle problems can lead to kidney problems, and in rare cases, 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, which can be life-threatening, may occur with this medication. Seek medical help right away if you experience:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:
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 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 pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications, or are 65 or older
Severe muscle problems can lead to kidney problems, and in rare cases, 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, which can be life-threatening, may occur with this medication. Seek medical help right away if you experience:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:
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 muscle damage).
- Yellowing of the skin or eyes (jaundice), dark urine, or unusual fatigue (could be signs of liver problems).
- Severe stomach pain.
- Allergic reactions such as rash, itching, swelling of the face/tongue/throat, severe dizziness, or trouble breathing.
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 worsen existing diabetes. To monitor this, follow your doctor's instructions for checking your blood sugar levels. Additionally, have your blood work checked as directed by your doctor and discuss the results with them.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. Adhere to the diet and exercise plan recommended by your doctor to ensure safe and effective use 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 crucial 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 worsen existing diabetes. To monitor this, follow your doctor's instructions for checking your blood sugar levels. Additionally, have your blood work checked as directed by your doctor and discuss the results with them.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. Adhere to the diet and exercise plan recommended by your doctor to ensure safe and effective use 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 crucial 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. Treatment should be symptomatic and supportive. Hemodialysis is unlikely to be of benefit due to high protein binding. Call 1-800-222-1222 (Poison Control Center) immediately for advice.
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
- Gemfibrozil (concomitant use with 40 mg rosuvastatin is contraindicated; increases rosuvastatin exposure and risk of myopathy/rhabdomyolysis)
- Regorafenib (increases rosuvastatin exposure)
Major Interactions
- Anticoagulants (e.g., Warfarin: increased INR/bleeding risk)
- Other fibrates (e.g., Fenofibrate: increased risk of myopathy/rhabdomyolysis)
- Niacin (lipid-lowering doses: increased risk of myopathy/rhabdomyolysis)
- Certain protease inhibitors (e.g., Atazanavir/Ritonavir, Lopinavir/Ritonavir, Tipranavir/Ritonavir, Glecaprevir/Pibrentasvir: significantly increase rosuvastatin exposure)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
Moderate Interactions
- Ezetimibe (increased rosuvastatin exposure and risk of myopathy)
- Antacids (aluminum and magnesium hydroxide: decrease rosuvastatin plasma concentrations; administer antacid 2 hours after rosuvastatin)
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases ethinyl estradiol and norgestrel AUCs)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis; temporary discontinuation of statin recommended)
Minor Interactions
- Not specifically categorized as minor for significant clinical impact, but general caution with other drugs metabolized by minor CYP pathways.
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess treatment efficacy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST)
Rationale: To establish baseline liver enzyme levels. Statins can cause elevations in transaminases.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline CK levels, especially in patients at increased risk 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 indicated.
Routine Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Frequency: 4-12 weeks after initiation or dose titration, then every 3-12 months or as clinically indicated.
Target: Individualized based on risk assessment and guideline recommendations (e.g., LDL-C reduction targets).
Action Threshold: If lipid goals not met, consider dose adjustment or combination therapy. If lipid levels are excessively low, consider dose reduction.
Liver Function Tests (ALT, AST)
Frequency: Generally not routinely recommended unless clinically indicated (e.g., symptoms suggestive of liver injury).
Target: Within normal limits.
Action Threshold: If persistent ALT/AST elevations >3 times the upper limit of normal (ULN), consider dose reduction or discontinuation. If symptoms of liver injury (e.g., jaundice, dark urine), discontinue immediately.
Creatine Kinase (CK)
Frequency: Not routinely recommended unless patient develops muscle symptoms (pain, tenderness, weakness).
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 5-10 times ULN without severe symptoms, monitor closely or consider dose reduction/discontinuation.
Symptom Monitoring
- Unexplained muscle pain
- Muscle tenderness
- Muscle weakness
- Dark urine (cola-colored)
- Unusual fatigue
- Yellowing of skin or eyes (jaundice)
- Abdominal pain
- Loss of appetite
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 may 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. It is unknown if rosuvastatin is excreted in human milk, but other statins are. Due to the potential for serious adverse reactions in breastfed infants, women taking rosuvastatin should not breastfeed.
Infant Risk:
High risk of serious adverse effects due to potential for interference with infant lipid metabolism and development.
Pediatric Use
Use is approved for specific indications (HeFH, HoFH) in children aged 7 years and older, with specific dosing guidelines and maximum doses lower than adults. Safety and efficacy in children younger than 7 years have not been established. Monitoring of growth and pubertal development should be considered.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. However, due to increased prevalence of renal impairment in the elderly, dose adjustments may be necessary based on renal function. Use with caution in patients >65 years due to increased risk of myopathy.
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.
- The 40 mg dose of rosuvastatin should be reserved for patients who have not achieved their LDL-C goal with the 20 mg dose and who will be closely monitored for adverse reactions.
- Patients of Asian descent may have higher plasma concentrations of rosuvastatin; consider initiating at 5 mg once daily.
- Educate patients to report any unexplained muscle pain, tenderness, or weakness immediately, especially if accompanied by fever or dark urine.
- Avoid concomitant use with cyclosporine due to significantly increased rosuvastatin exposure.
- Unlike some other statins, rosuvastatin is minimally metabolized by CYP450 enzymes, reducing the likelihood of drug interactions via this pathway, but transporter-mediated interactions (e.g., OATP1B1) are significant.
Alternative Therapies
- Other HMG-CoA Reductase Inhibitors (Statins): Atorvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin
- PCSK9 Inhibitors (e.g., Alirocumab, Evolocumab)
- Cholesterol Absorption Inhibitors (e.g., Ezetimibe)
- Fibrates (e.g., Fenofibrate, Gemfibrozil)
- Niacin (Nicotinic Acid)
- Bile Acid Sequestrants (e.g., Cholestyramine, Colesevelam, Colestipol)
- Adenosine Triphosphate-Citrate Lyase (ACL) Inhibitors (e.g., Bempedoic acid)
- Omega-3 Fatty Acid Esters (e.g., Icosapent ethyl)
Cost & Coverage
Average Cost:
$10 - $300+ per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic rosuvastatin); Tier 3 or higher (brand Crestor)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.