Ezallor 10mg 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
Dec 2018
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ezallor Sprinkle Capsules contain rosuvastatin, a medicine that helps lower 'bad' cholesterol (LDL) and triglycerides, and can raise 'good' cholesterol (HDL). By doing this, it helps reduce your risk of heart attack and stroke. It works best when combined with a healthy diet and exercise.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription 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; 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 save it for later use.
If you have a feeding tube, you can use your medication as directed by your healthcare provider. 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 a 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 prescription 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; 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 save it for later use.
If you have a feeding tube, you can use your medication as directed by your healthcare provider. 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 a missed dose.
Lifestyle & Tips
- Follow a cholesterol-lowering diet as recommended by your doctor or dietitian.
- Engage in regular physical activity.
- Maintain a healthy weight.
- Quit smoking.
- Limit alcohol intake.
- Take the capsule whole or sprinkle the contents on a small amount of soft food (e.g., applesauce, pudding) and swallow immediately without chewing. Do not store for later use.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 10-20 mg orally once daily; maximum 40 mg once daily.
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
Primary Hyperlipidemia/Mixed Dyslipidemia:
Initial 10-20 mg once daily; dose range 5-40 mg once daily. For patients requiring aggressive LDL-C reduction, consider 20 mg initial dose.
Homozygous Familial Hypercholesterolemia (HoFH):
20 mg once daily.
Primary Prevention of Cardiovascular Disease:
20 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH): 6 to <10 years: 5-10 mg orally once daily. Max 10 mg/day. 10 to <18 years: 5-20 mg orally once daily. Max 20 mg/day.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10 to <18 years: 5-20 mg orally once daily. Max 20 mg/day. Homozygous Familial Hypercholesterolemia (HoFH): 20 mg orally once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed (CrCl 30-80 mL/min).
Moderate:
No dose adjustment needed (CrCl 30-80 mL/min).
Severe:
Initial 5 mg orally once daily; maximum 10 mg orally once daily (CrCl <30 mL/min/1.73 m2, not on hemodialysis).
Dialysis:
Maximum 10 mg orally once daily. Rosuvastatin is not removed by hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A).
Moderate:
No dose adjustment needed (Child-Pugh B).
Severe:
Contraindicated (Child-Pugh C).
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 VLDL and triglyceride levels.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20%
Tmax:
3-5 hours
FoodEffect:
Food decreases Cmax by 20%, but AUC is not significantly affected. Can be taken with or without food.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not readily available as a single rate, but primarily hepatic uptake and biliary excretion.
ExcretionRoute:
Fecal (approximately 90%), Renal (approximately 10%)
Unchanged:
Approximately 90% (feces), Approximately 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Sustained with daily dosing
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
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. The risk of muscle problems 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 serious side effects, and many have only minor or no side effects at all. However, 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 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 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. The risk of muscle problems 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 serious side effects, and many have only minor or no side effects at all. However, 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 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 feeling unwell)
- Dark-colored urine
- Yellowing of the skin or eyes (jaundice)
- Severe stomach pain
- Unusual tiredness or weakness
- Loss of appetite
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 conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes, as this may affect how your body processes the medication.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis, as these may interact with this drug.
If you are pregnant or think you might be pregnant. It is crucial to note that you should not take this medication if you are pregnant.
* If you are breastfeeding. You should not breastfeed while taking this medication, as it may pose risks to your baby.
This list is not exhaustive, and it is vital to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe for you to take this medication alongside your other treatments. 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 conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes, as this may affect how your body processes the medication.
If you are currently taking any of the following medications: Cyclosporine, gemfibrozil, ledipasvir/sofosbuvir, sofosbuvir/velpatasvir/voxilaprevir, or tafamidis, as these may interact with this drug.
If you are pregnant or think you might be pregnant. It is crucial to note that you should not take this medication if you are pregnant.
* If you are breastfeeding. You should not breastfeed while taking this medication, as it may pose risks to your baby.
This list is not exhaustive, and it is vital to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe for you to take this medication alongside your other treatments. 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 recommended 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 outlined 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 a potential increased risk of side effects.
This drug may pose a risk to an unborn baby. If you are of childbearing potential, 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 recommended 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 outlined 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 a potential increased risk of side effects.
This drug may pose a risk to an unborn baby. If you are of childbearing potential, 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 are known. The most likely effects would be an exaggeration of known side effects, such as muscle pain or liver enzyme elevations.
What to Do:
In case of suspected overdose, contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention. Treatment is supportive, as rosuvastatin is not significantly removed by hemodialysis.
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
- Gemfibrozil (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Lopinavir/Ritonavir (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
Major Interactions
- Warfarin (may increase INR; monitor INR closely)
- Other fibrates (e.g., fenofibrate, increased risk of myopathy/rhabdomyolysis)
- Niacin (lipid-lowering doses, increased risk of myopathy/rhabdomyolysis)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
- Certain protease inhibitors (e.g., atazanavir/ritonavir, tipranavir/ritonavir, fosamprenavir/ritonavir, darunavir/ritonavir - dose adjustments or avoidance may be necessary due to increased rosuvastatin exposure)
- Regorafenib (increases rosuvastatin exposure)
- Fostamatinib (increases rosuvastatin exposure)
Moderate Interactions
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases ethinyl estradiol and norgestrel AUC)
- Antacids containing aluminum and magnesium hydroxide (decreases rosuvastatin plasma concentrations; administer antacid 2 hours after rosuvastatin)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis; temporary discontinuation of rosuvastatin recommended)
- Capmatinib (increases rosuvastatin exposure)
- Elbasvir/Grazoprevir (increases rosuvastatin exposure)
Minor Interactions
- No clinically significant minor interactions commonly cited for rosuvastatin that require specific action.
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, excessive alcohol intake).
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 adjustment, then every 3-12 months.
Target: Individualized based on patient risk factors and guideline recommendations (e.g., LDL-C reduction goals).
Action Threshold: If lipid goals not met, consider dose adjustment or addition of other therapies. If levels are excessively low, consider dose reduction.
Liver Function Tests (ALT, AST)
Frequency: As clinically indicated (e.g., if symptoms suggestive of liver injury occur). Routine periodic monitoring is generally not recommended unless clinically indicated.
Target: Within normal limits.
Action Threshold: If persistent elevations of serum transaminases >3 times the upper limit of normal (ULN) occur, discontinue rosuvastatin.
Creatine Kinase (CK)
Frequency: As clinically indicated (e.g., if muscle pain, tenderness, or weakness occurs). Routine periodic monitoring is generally not recommended.
Target: Within normal limits.
Action Threshold: If CK levels are markedly elevated (>10 times ULN) or if myopathy is diagnosed or suspected, discontinue rosuvastatin. If muscle symptoms are severe and CK is elevated, consider rhabdomyolysis.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (especially if accompanied by malaise or fever)
- Dark-colored urine
- Yellowing of the skin or eyes (jaundice)
- Unusual fatigue or weakness
- Loss of appetite
- Upper right abdominal pain
- Nausea or vomiting
Special Patient Groups
Pregnancy
Rosuvastatin is contraindicated in pregnancy (Pregnancy Category X). It can cause fetal harm. Cholesterol and other products of cholesterol biosynthesis are essential for fetal development. Inhibition of HMG-CoA reductase may cause fetal harm.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm due to interference with essential cholesterol synthesis.
Second Trimester:
Potential for fetal harm due to interference with essential cholesterol synthesis.
Third Trimester:
Potential for fetal harm due to interference with essential cholesterol synthesis.
Lactation
Rosuvastatin is contraindicated during breastfeeding (Lactation Risk L5). It is unknown if rosuvastatin is excreted in human milk, but other statins are. Because of the potential for serious adverse reactions in breastfed infants, women taking rosuvastatin should not breastfeed.
Infant Risk:
High risk of serious adverse reactions due to potential for excretion in breast milk and interference with infant lipid metabolism.
Pediatric Use
Approved for use in pediatric patients aged 6 years and older with heterozygous familial hypercholesterolemia (HeFH) and homozygous familial hypercholesterolemia (HoFH). Dosing is age and condition-dependent. Safety and efficacy in patients younger than 6 years have not been established.
Geriatric Use
No overall differences in efficacy or safety have been observed between elderly (>65 years) and younger patients, but greater sensitivity of some older individuals cannot be ruled out. No specific dose adjustment is required based on age alone, but consider starting at the lower end of the dosing range due to potential for increased exposure and higher risk of myopathy in some elderly patients.
Clinical Information
Clinical Pearls
- Ezallor Sprinkle Capsules offer an alternative formulation for patients who have difficulty swallowing tablets.
- Rosuvastatin can be taken at any time of day, with or without food.
- Patients should be advised to report any unexplained muscle pain, tenderness, or weakness immediately, as this could be a sign of myopathy or rhabdomyolysis.
- Avoid excessive alcohol consumption while on rosuvastatin, as it can increase the risk of liver problems.
- Do not stop taking rosuvastatin without consulting your doctor, even if you feel well, as stopping can lead to a rebound in cholesterol levels and increased cardiovascular risk.
- 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.
Alternative Therapies
- Other HMG-CoA reductase inhibitors (statins): Atorvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin
- Cholesterol absorption inhibitors: Ezetimibe
- PCSK9 inhibitors: Alirocumab, Evolocumab
- Fibrates: Fenofibrate, Gemfibrozil (for hypertriglyceridemia)
- Niacin (Nicotinic Acid)
- Bile acid sequestrants: Cholestyramine, Colestipol, Colesevelam
- Adenosine triphosphate-citrate lyase (ACL) inhibitors: Bempedoic acid
- Angiopoietin-like 3 (ANGPTL3) inhibitors: Evinacumab
Cost & Coverage
Average Cost:
Variable, typically $30-$150 for 30 capsules (generic rosuvastatin); Ezallor may be higher. per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 for generic rosuvastatin; Ezallor may be Tier 2 or Tier 3 depending on formulary.
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.