Ezallor 40mg 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
Pregnancy Category
Category X
FDA Approved
Aug 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ezallor Sprinkle contains rosuvastatin, a medicine that helps lower 'bad' cholesterol (LDL) and triglycerides, and raise 'good' cholesterol (HDL) in your blood. It works by blocking an enzyme in your liver that makes cholesterol. Lowering cholesterol can reduce your risk of heart disease and stroke. The sprinkle capsules are designed to be easier to take, as they can be opened and sprinkled on soft food or mixed with water.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow these instructions carefully:
Take your medication exactly as directed by your doctor. 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 prescribed by your doctor or healthcare provider, even if you start feeling well.
You can take your medication with or without food.
If you are taking an antacid that contains aluminum or magnesium, take it at least 2 hours after taking your medication.
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
To ensure the safety and effectiveness 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 of your medication:
Skip the missed dose and return to your regular schedule.
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 instructions carefully:
Take your medication exactly as directed by your doctor. 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 prescribed by your doctor or healthcare provider, even if you start feeling well.
You can take your medication with or without food.
If you are taking an antacid that contains aluminum or magnesium, take it at least 2 hours after taking your medication.
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
To ensure the safety and effectiveness 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 of your medication:
Skip the missed dose and return to your regular schedule.
Do not take two doses at the same time or take extra doses to make up for the missed dose.
Lifestyle & Tips
- Follow a cholesterol-lowering diet (low in saturated fat and cholesterol).
- Engage in regular physical activity as recommended by your doctor.
- Maintain a healthy weight.
- Limit alcohol intake.
- Avoid grapefruit juice or large amounts of grapefruit, as it may interact with some statins (though less significant for rosuvastatin).
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose typically 10-20 mg once daily; maximum 40 mg once daily. Ezallor 40mg is the maximum dose.
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
primaryHyperlipidemia:
Initial 10-20 mg once daily; max 40 mg once daily.
homozygousFamilialHypercholesterolemia:
20 mg once daily initially, up to 40 mg once daily.
atheroscleroticCardiovascularDiseasePrevention:
20 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Heterozygous Familial Hypercholesterolemia (HeFH) 8-10 years: 5-10 mg once daily; 10-17 years: 5-20 mg once daily. Homozygous Familial Hypercholesterolemia (HoFH) 7-17 years: 20 mg once daily.
Adolescent:
HeFH 10-17 years: 5-20 mg once daily. HoFH 7-17 years: 20 mg once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed.
Moderate:
No dose adjustment needed.
Severe:
CrCl < 30 mL/min (non-dialysis): Initiate at 5 mg once daily; max 10 mg once daily. Contraindicated in patients with severe renal impairment receiving 40 mg dose.
Dialysis:
Not removed by hemodialysis. Initiate at 5 mg once daily; max 10 mg once daily.
Hepatic Impairment:
Mild:
No dose adjustment needed.
Moderate:
No dose adjustment needed.
Severe:
Contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases.
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 reduction in hepatic cholesterol synthesis and an increase in the number of LDL receptors on the hepatocyte surface, enhancing the uptake and catabolism of LDL. It also reduces VLDL and triglyceride levels and increases HDL-C.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20%
Tmax:
3-5 hours
FoodEffect:
Food does not affect absorption, but Cmax and AUC may be slightly reduced.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available
ExcretionRoute:
Approximately 90% excreted unchanged in feces (primarily unabsorbed drug and biliary excretion); approximately 5% excreted in urine.
Unchanged:
Approximately 90% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Not available (sustained effect 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. Additionally, if muscle problems persist after your doctor has instructed you to stop taking this medication, seek medical attention right away.
Liver Problems
Drugs like this one have been associated with liver problems, which can be fatal. If you notice any of the following symptoms, contact your doctor immediately:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical attention if you notice any of the following:
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. Additionally, if muscle problems persist after your doctor has instructed you to stop taking this medication, seek medical attention right away.
Liver Problems
Drugs like this one have been associated with liver problems, which can be fatal. If you notice any of the following symptoms, contact your doctor immediately:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical attention if you notice any of the following:
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.
- Yellowing of the skin or eyes (jaundice).
- Unusual tiredness or weakness.
- Loss of appetite.
- Upper stomach pain.
- Nausea or vomiting.
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 may 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 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 may 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 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.
This drug may cause high blood sugar levels, including the development of new-onset diabetes or worsening of existing diabetes. Therefore, it is crucial to monitor your blood sugar levels as directed by your doctor.
Regular blood tests, as advised by your doctor, are necessary to ensure safe treatment. Be sure to discuss any concerns or questions with your doctor.
To minimize the risk of severe side effects, do not exceed the prescribed dosage. Adhere to the diet and exercise plan recommended by your doctor to optimize treatment outcomes.
Limit alcohol consumption to no more than 2 drinks per day, as excessive alcohol use may increase the risk of liver disease.
If you are of Asian descent, exercise caution when taking this medication, as you may be more susceptible to side effects. Similarly, individuals 65 years or older should use this drug with caution due to a potential increased risk of side effects.
This medication may pose a risk to an unborn baby. If you are of childbearing potential, it is essential to use effective birth control while taking this drug. If you become pregnant, notify your doctor immediately.
This drug may cause high blood sugar levels, including the development of new-onset diabetes or worsening of existing diabetes. Therefore, it is crucial to monitor your blood sugar levels as directed by your doctor.
Regular blood tests, as advised by your doctor, are necessary to ensure safe treatment. Be sure to discuss any concerns or questions with your doctor.
To minimize the risk of severe side effects, do not exceed the prescribed dosage. Adhere to the diet and exercise plan recommended by your doctor to optimize treatment outcomes.
Limit alcohol consumption to no more than 2 drinks per day, as excessive alcohol use may increase the risk of liver disease.
If you are of Asian descent, exercise caution when taking this medication, as you may be more susceptible to side effects. Similarly, individuals 65 years or older should use this drug with caution due to a potential increased risk of side effects.
This medication may pose a risk to an unborn baby. If you are of childbearing potential, it is essential to use effective birth control while taking this drug. If you become pregnant, notify your doctor immediately.
Overdose Information
Overdose Symptoms:
- No specific symptoms of overdose have been reported with rosuvastatin. The most likely effects would be an exaggeration of known side effects, such as muscle pain or liver enzyme elevations.
What to Do:
There is no specific antidote for rosuvastatin overdose. Treatment should be symptomatic and supportive. Hemodialysis is not expected to be effective. Call 1-800-222-1222 (Poison Control Center) immediately for advice.
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
Major Interactions
- Gemfibrozil (increases rosuvastatin exposure, increased risk of myopathy/rhabdomyolysis)
- Certain protease inhibitors (e.g., atazanavir/ritonavir, lopinavir/ritonavir, sofosbuvir/velpatasvir/voxilaprevir, glecaprevir/pibrentasvir) (significantly increase rosuvastatin exposure)
- Regorafenib (increases rosuvastatin exposure)
- Fostamatinib (increases rosuvastatin exposure)
Moderate Interactions
- Warfarin (may potentiate anticoagulant effect, monitor INR)
- Niacin (concomitant use with statins increases risk of myopathy/rhabdomyolysis)
- Other fibrates (e.g., fenofibrate) (increased risk of myopathy/rhabdomyolysis)
- Colchicine (increased risk of myopathy/rhabdomyolysis)
- Erythromycin (decreases rosuvastatin exposure)
- Oral contraceptives (increases ethinyl estradiol and norgestrel AUC)
- Antacids containing aluminum and magnesium hydroxide (decreases rosuvastatin plasma concentrations, administer rosuvastatin 2 hours after antacid)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis, avoid concomitant use)
Minor Interactions
- Not available (most clinically significant interactions are moderate or major)
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 function and monitor for drug-induced hepatotoxicity.
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).
Timing: Prior to initiation of therapy (if indicated).
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 typically 45-55% for high-intensity statin (40mg dose). Target levels vary based on patient risk.
Action Threshold: Failure to achieve target lipid levels, or if lipid levels worsen, consider dose adjustment or alternative therapy.
Liver Function Tests (ALT, AST)
Frequency: Periodically, as clinically indicated. Routine monitoring is no longer universally recommended unless symptoms suggest liver injury.
Target: Within normal limits (WNL).
Action Threshold: If ALT or AST > 3 times the upper limit of normal (ULN) on two consecutive measurements, consider dose reduction or discontinuation.
Creatine Kinase (CK)
Frequency: Only if muscle symptoms (pain, tenderness, weakness) develop.
Target: WNL.
Action Threshold: If CK > 10 times ULN, or if muscle symptoms are severe or accompanied by dark urine, discontinue therapy immediately and evaluate for rhabdomyolysis.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (myalgia, myopathy)
- Dark urine (suggestive of rhabdomyolysis)
- Unusual fatigue or weakness
- 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. 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 (potential for serious adverse effects due to interference with infant lipid metabolism).
Pediatric Use
Use is limited to specific conditions like heterozygous and homozygous familial hypercholesterolemia. Dosing is age and weight-dependent. Safety and efficacy have not been established in children younger than 7 years for HoFH or younger than 8 years for HeFH.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. No dose adjustment is generally needed based on age alone, but consider renal function.
Clinical Information
Clinical Pearls
- Ezallor Sprinkle capsules can be opened and the contents sprinkled on a spoonful of soft food (e.g., applesauce, pudding) or mixed with water, then consumed immediately. Do not chew the pellets.
- Take rosuvastatin at any time of day, with or without food.
- Patients should be advised to report any unexplained muscle pain, tenderness, or weakness immediately.
- The 40 mg dose of rosuvastatin should be reserved for patients who have not achieved their LDL-C goal with 20 mg and are at high cardiovascular risk, and who do not have predisposing factors for myopathy.
- Avoid concomitant use with fusidic acid due to increased risk of myopathy/rhabdomyolysis; if unavoidable, discontinue rosuvastatin during fusidic acid treatment.
- Patients of Asian descent may have increased rosuvastatin exposure; consider initiating at 5 mg.
Alternative Therapies
- Other HMG-CoA reductase inhibitors (statins): Atorvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin
- Cholesterol absorption inhibitors: Ezetimibe
- PCSK9 inhibitors: Alirocumab, Evolocumab
- Bile acid sequestrants: Cholestyramine, Colestipol, Colesevelam
- Fibrates: Gemfibrozil, Fenofibrate
- Niacin (Nicotinic Acid)
- Omega-3 fatty acid ethyl esters
Cost & Coverage
Average Cost:
Varies widely by pharmacy and formulation (brand vs. generic). Ezallor (brand) is typically more expensive than generic rosuvastatin. per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Generic rosuvastatin is typically Tier 1 or 2. Brand Ezallor Sprinkle may be Tier 2 or 3, requiring higher co-pays or prior authorization.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.