Ezallor 20mg Sprinkle Capsules
It is used to lower bad cholesterol (LDL).It is used to lower triglycerides.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
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ezallor (rosuvastatin) is a medication used to 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 prevent heart disease, strokes, and heart attacks. It's a sprinkle capsule, meaning you can open it and sprinkle the contents on soft food or mix with liquid if you have trouble swallowing pills.
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 to you 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 feeling 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; do not chew or crush it.
If you have difficulty swallowing your medication whole, you can sprinkle the contents on a small amount (at least 5 mL) of soft food, such as applesauce or pudding. Stir the mixture for 10 to 15 seconds and swallow it within 60 minutes. Do not chew the mixture, and do not store it for future use.
If you have a feeding tube, you can use your medication as directed. Flush the feeding tube after administering the medication.
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 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 these steps:
Take your medication exactly as directed by your doctor. Read all the information provided to you 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 feeling 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; do not chew or crush it.
If you have difficulty swallowing your medication whole, you can sprinkle the contents on a small amount (at least 5 mL) of soft food, such as applesauce or pudding. Stir the mixture for 10 to 15 seconds and swallow it within 60 minutes. Do not chew the mixture, and do not store it for future use.
If you have a feeding tube, you can use your medication as directed. Flush the feeding tube after administering the medication.
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 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.
- Lose weight if you are overweight or obese.
- Quit smoking.
- Limit alcohol consumption.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Hyperlipidemia: Initial 10-20 mg once daily. Max 40 mg once daily. Primary Prevention: 20 mg once daily.
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
Homozygous Familial Hypercholesterolemia (HoFH):
20 mg once daily, may increase to 40 mg once daily.
Primary Dysbetalipoproteinemia:
10-20 mg once daily.
Hypertriglyceridemia:
10-20 mg once daily, may increase to 40 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.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10 to <17 years: 5-20 mg once daily. Max 20 mg/day.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed.
Moderate:
CrCl <30 mL/min/1.73m2 (non-dialysis): Initial 5 mg once daily, max 10 mg once daily.
Severe:
CrCl <30 mL/min/1.73m2 (non-dialysis): Initial 5 mg once daily, max 10 mg once daily.
Dialysis:
Contraindicated in patients on hemodialysis.
Hepatic Impairment:
Mild:
No adjustment needed.
Moderate:
Child-Pugh score 7-9: Consider lower starting dose and careful titration. Max 20 mg/day.
Severe:
Child-Pugh score >9: 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 hepatocyte surfaces, increasing the uptake and catabolism of LDL. It also inhibits hepatic synthesis of VLDL, thereby reducing total VLDL and LDL particle numbers.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20%
Tmax:
3-5 hours
FoodEffect:
Food does not affect the bioavailability of rosuvastatin, but may decrease the rate of absorption.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to plasma proteins)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not readily quantifiable due to extensive first-pass effect and biliary excretion.
ExcretionRoute:
Approximately 90% excreted unchanged in feces (primarily absorbed drug and metabolites), 5% in urine.
Unchanged:
Approximately 90% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Sustained with once-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 immediately or seek emergency medical attention:
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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Drowsiness
+ Increased thirst or hunger
+ Frequent urination
+ Flushing
+ Rapid breathing
+ Fruity-smelling breath
Memory problems or loss
Confusion
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid drooping
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. The risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney damage, 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 life-threatening. Seek medical help right away if you notice:
Dark urine
Fatigue
Decreased appetite
Nausea or stomach pain
Light-colored stools
Vomiting
Yellowing of the skin or eyes
Other Possible Side Effects
Most people taking this medication do not experience significant side effects, but some may occur. If you notice any of the following side effects, contact your doctor if they bother you or do not go away:
Headache
Stomach pain
Nausea
Constipation
Joint pain
* Weakness
This is not an exhaustive list of potential 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 immediately or seek emergency medical attention:
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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood sugar, including:
+ Confusion
+ Drowsiness
+ Increased thirst or hunger
+ Frequent urination
+ Flushing
+ Rapid breathing
+ Fruity-smelling breath
Memory problems or loss
Confusion
Blood in the urine
Difficulty urinating or changes in urine output
Blurred vision, double vision, or other changes in eyesight
Eyelid drooping
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. The risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney damage, 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 life-threatening. Seek medical help right away if you notice:
Dark urine
Fatigue
Decreased appetite
Nausea or stomach pain
Light-colored stools
Vomiting
Yellowing of the skin or eyes
Other Possible Side Effects
Most people taking this medication do not experience significant side effects, but some may occur. If you notice any of the following side effects, contact your doctor if they bother you or do not go away:
Headache
Stomach pain
Nausea
Constipation
Joint pain
* Weakness
This is not an exhaustive list of potential 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 (could be a sign of serious muscle damage).
- Yellowing of the skin or eyes (jaundice), dark urine, light-colored stools, severe stomach pain, nausea, or vomiting (could be signs of liver problems).
- Unusual tiredness or weakness.
- Swelling in your hands or feet.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis.
If you are pregnant or think you might be pregnant. Note that this medication should not be taken during pregnancy.
* If you are breastfeeding. You should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe for you to take this medication with your other drugs 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 drugs 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 blood work checks and discuss the results with them.
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 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 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 blood work checks and discuss the results with them.
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 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. Symptoms would likely 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 suspected overdose, contact a poison control center or emergency medical services immediately. Treatment should be symptomatic and supportive. Hemodialysis is unlikely to be beneficial due to high protein binding.
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
- Gemfibrozil (increases rosuvastatin exposure, risk of myopathy/rhabdomyolysis)
- Lopinavir/ritonavir and other protease inhibitor combinations (significantly increases rosuvastatin exposure)
Major Interactions
- Warfarin (enhances anticoagulant effect, increased INR)
- Niacin (high doses, >1g/day, increased risk of myopathy/rhabdomyolysis)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
- Fibrates (e.g., fenofibrate, increased risk of myopathy/rhabdomyolysis)
- Regorafenib (increases rosuvastatin exposure)
- Certain other protease inhibitors (e.g., atazanavir/ritonavir, darunavir/ritonavir, tipranavir/ritonavir, fosamprenavir/ritonavir)
Moderate Interactions
- Antacids (aluminum and magnesium hydroxide, decreases rosuvastatin plasma concentrations if given within 2 hours)
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases ethinyl estradiol and norgestrel AUC)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis, avoid co-administration)
- Coumarin anticoagulants (monitor INR)
Minor Interactions
- No significant minor interactions commonly cited that require specific dose adjustments or close monitoring beyond general caution.
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 and monitor for drug-induced hepatotoxicity.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline CK levels, especially in patients with predisposing factors for myopathy (e.g., renal impairment, hypothyroidism, history of muscle toxicity with other lipid-lowering agents, genetic muscle disorders, alcohol abuse).
Timing: Prior to initiation of therapy (optional, but recommended in high-risk patients).
Routine Monitoring
Lipid Panel
Frequency: 4-12 weeks after initiation or dose titration, then every 3-12 months or as clinically indicated.
Target: LDL-C reduction based on risk assessment and guideline recommendations (e.g., >50% reduction for high-intensity statin).
Action Threshold: Failure to achieve target LDL-C, or if lipid levels worsen; consider dose adjustment or alternative therapy.
Liver Function Tests (ALT, AST)
Frequency: At baseline, then if clinically indicated (e.g., symptoms of liver injury). Routine periodic monitoring is generally not recommended unless clinically indicated.
Target: ALT/AST <3 times upper limit of normal (ULN).
Action Threshold: If ALT/AST >3 times ULN, discontinue rosuvastatin. If symptoms of liver injury (e.g., jaundice, dark urine, fatigue), discontinue immediately.
Creatine Kinase (CK)
Frequency: Only if muscle symptoms (e.g., pain, tenderness, weakness) develop.
Target: CK <10 times ULN.
Action Threshold: If CK >10 times ULN, or if muscle symptoms are severe or persistent, discontinue rosuvastatin. If CK >5 times ULN without symptoms, recheck in 5-7 days. If CK >5 times ULN with symptoms, discontinue.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (myopathy/rhabdomyolysis)
- Dark urine (rhabdomyolysis)
- Unusual fatigue or weakness
- Loss of appetite
- Upper right abdominal pain
- Nausea, vomiting
- Yellowing of skin or eyes (jaundice)
- Flu-like symptoms
Special Patient Groups
Pregnancy
Rosuvastatin is contraindicated in pregnancy (Pregnancy Category X). Cholesterol and cholesterol derivatives are essential for fetal development. Statins may cause fetal harm. Discontinue immediately if pregnancy occurs.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity due to interference with cholesterol synthesis, which is critical for fetal development.
Second Trimester:
Continued risk of interference with fetal development.
Third Trimester:
Continued risk of interference with fetal development.
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, breastfeeding is not recommended.
Infant Risk:
High risk of serious adverse effects due to interference with infant lipid metabolism and development.
Pediatric Use
Approved for heterozygous familial hypercholesterolemia (HeFH) in children aged 8 years and older. Dosing is age and weight-dependent, with a maximum dose of 20 mg/day. Safety and efficacy in children younger than 8 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, elderly patients may be more susceptible to myopathy, and renal function should be monitored. No specific dose adjustment is required based on age alone, but consider starting at the lowest dose.
Clinical Information
Clinical Pearls
- Ezallor sprinkle capsules can be opened and sprinkled on soft food (e.g., applesauce, pudding) or mixed in liquid (e.g., water, orange juice) for patients who have difficulty swallowing whole capsules. Do not chew the pellets.
- Administer rosuvastatin at any time of day, with or without food. Consistency in timing is recommended.
- Patients should be advised to report any unexplained muscle pain, tenderness, or weakness immediately, especially if accompanied by malaise or fever.
- Rosuvastatin is generally well-tolerated, but adherence to lifestyle modifications (diet, exercise) is crucial for optimal lipid-lowering effects.
- Due to the risk of myopathy/rhabdomyolysis, avoid concomitant use with cyclosporine, gemfibrozil, and certain protease inhibitor combinations.
- For patients with severe renal impairment (CrCl <30 mL/min/1.73m2) not on dialysis, the starting dose is 5 mg once daily, and the maximum dose is 10 mg once daily.
- For patients of Asian descent, consider a starting dose of 5 mg due to increased systemic exposure.
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 (for hypertriglyceridemia)
- Niacin (Nicotinic Acid)
- Bile acid sequestrants: Cholestyramine, Colestipol, Colesevelam
- Omega-3 fatty acid ethyl esters (for severe hypertriglyceridemia)
Cost & Coverage
Average Cost:
Varies widely, typically $100-$300+ per 30 capsules (Ezallor 20mg)
Generic Available:
Yes
Insurance Coverage:
Generic rosuvastatin is typically Tier 1 or 2. Brand-name Ezallor may be Tier 2 or 3, requiring prior authorization or step therapy.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. 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 it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.