Ezallor 5mg 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
Apr 2018
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ezallor (rosuvastatin) is a medication used to lower high cholesterol and triglyceride levels in your blood. By lowering 'bad' cholesterol (LDL) and increasing 'good' cholesterol (HDL), it helps reduce your risk of heart disease, heart attacks, and strokes. It works best when combined with a healthy diet and regular exercise.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. Take your medication at the same time every day to establish a routine.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better. You can take your medication with or without food. However, if you are taking an antacid that contains aluminum or magnesium, take it at least 2 hours after taking your medication.
Administration Instructions
Swallow your medication whole, without chewing or crushing it. If you have difficulty swallowing the 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 by your healthcare provider. After administering the medication through the feeding tube, flush the tube to ensure it is clear.
Storage and Disposal
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.
Missing a Dose
If you miss a dose, skip it 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 your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. Take your medication at the same time every day to establish a routine.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better. You can take your medication with or without food. However, if you are taking an antacid that contains aluminum or magnesium, take it at least 2 hours after taking your medication.
Administration Instructions
Swallow your medication whole, without chewing or crushing it. If you have difficulty swallowing the 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 by your healthcare provider. After administering the medication through the feeding tube, flush the tube to ensure it is clear.
Storage and Disposal
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.
Missing a Dose
If you miss a dose, skip it 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 and trans fats, cholesterol).
- Engage in regular physical activity as recommended by your doctor.
- Maintain a healthy weight.
- Quit smoking.
- Limit alcohol intake.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose 5-20 mg once daily, depending on indication and patient characteristics. Ezallor 5mg is a starting dose for some indications or patients requiring lower doses.
Dose Range:
5 - 40 mg
Condition-Specific Dosing:
primaryHyperlipidemia:
Initial 10-20 mg once daily; dose range 5-40 mg once daily. Max 40 mg.
homozygousFamilialHypercholesterolemia:
20 mg once daily.
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 <18 years: 5-20 mg once daily. Dosing based on LDL-C response and tolerability. Max 20 mg/day for children.
Adolescent:
Heterozygous Familial Hypercholesterolemia (HeFH): 10 to <18 years: 5-20 mg once daily. Max 20 mg/day.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed (CrCl âĨ30 mL/min).
Moderate:
No dose adjustment needed (CrCl âĨ30 mL/min).
Severe:
Starting dose 5 mg once daily; maximum dose 10 mg once daily (CrCl <30 mL/min, not on hemodialysis).
Dialysis:
Contraindicated in patients on hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A).
Moderate:
No dose adjustment needed (Child-Pugh B).
Severe:
Contraindicated in active liver disease or unexplained persistent elevations of serum transaminases (Child-Pugh C).
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 cholesterol, LDL-C, VLDL-C, and triglycerides, and increasing HDL-C.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20%
Tmax:
3-5 hours
FoodEffect:
Food does not significantly affect absorption, can be taken with or without food.
Distribution:
Vd:
Approximately 134 L
ProteinBinding:
Approximately 90% (primarily to plasma proteins)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours
Clearance:
Not available (primarily hepatic uptake)
ExcretionRoute:
Primarily feces (approximately 90%), with a small portion excreted in urine (approximately 10%).
Unchanged:
Approximately 90% of absorbed rosuvastatin is excreted unchanged in the feces.
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
2-4 weeks
DurationOfAction:
Related to half-life, effects persist as long as drug is taken.
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
Muscle Problems
This medication may cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. Your risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, 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 Problems
Liver problems have been reported with medications like this one, and in some cases, have been fatal. Seek medical help right away if you notice:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Other Side Effects
Most people do not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
This is not a complete 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
Muscle Problems
This medication may cause muscle pain, tenderness, or weakness, especially if you have low thyroid function, kidney problems, or are taking certain other medications. Your risk may also be higher if you are 65 or older. In rare cases, severe muscle problems can lead to kidney problems, 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 Problems
Liver problems have been reported with medications like this one, and in some cases, have been fatal. Seek medical help right away if you notice:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Other Side Effects
Most people do not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Stomach pain
Upset stomach
Constipation
Joint pain
* Weakness
This is not a complete 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 fatigue or weakness
- Severe stomach pain
- 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:
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, adhere to the schedule recommended by your doctor for getting blood work done, and discuss the results with them.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. It is crucial to follow the diet and exercise plan outlined by your doctor to ensure safe and effective use of this medication.
Limit your alcohol consumption to no more than 2 drinks per day, as excessive alcohol intake may increase your risk of developing liver disease.
If you are of Asian descent, exercise caution when 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 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 recommended by your doctor for getting blood work done, and discuss the results with them.
To minimize the risk of severe side effects, do not exceed the dosage prescribed by your doctor. It is crucial to follow the diet and exercise plan outlined by your doctor to ensure safe and effective use of this medication.
Limit your alcohol consumption to no more than 2 drinks per day, as excessive alcohol intake may increase your risk of developing liver disease.
If you are of Asian descent, exercise caution when 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 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:
- Limited experience with overdose. Symptoms are generally non-specific and may include gastrointestinal upset, 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 due to high protein binding. Contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Contraindicated Interactions
- Cyclosporine (significantly increases rosuvastatin exposure)
- Co-administration with certain protease inhibitors (e.g., tipranavir/ritonavir, lopinavir/ritonavir, simeprevir, atazanavir/ritonavir) due to significant increases in rosuvastatin exposure.
Major Interactions
- Warfarin (may increase INR; monitor INR closely)
- Gemfibrozil (increases rosuvastatin exposure; co-administration not recommended, if necessary, limit rosuvastatin to 10 mg/day)
- Other fibrates (e.g., fenofibrate, may increase risk of myopathy/rhabdomyolysis)
- Niacin (lipid-lowering doses, may increase risk of myopathy/rhabdomyolysis)
- Colchicine (may increase risk of myopathy/rhabdomyolysis)
- Regorafenib (increases rosuvastatin exposure; limit rosuvastatin to 10 mg/day)
- Darolutamide (increases rosuvastatin exposure; limit rosuvastatin to 5 mg/day)
Moderate Interactions
- Antacids (aluminum and magnesium hydroxide-containing; decreases rosuvastatin plasma concentrations; administer antacid 2 hours after rosuvastatin)
- Erythromycin (decreases rosuvastatin plasma concentrations)
- Ezetimibe (increases rosuvastatin exposure; monitor for adverse effects)
- Oral contraceptives (increases plasma concentrations of ethinyl estradiol and norgestrel; consider this when selecting oral contraceptive)
- Fusidic acid (increased risk of myopathy/rhabdomyolysis; temporary discontinuation of rosuvastatin recommended)
- Capmatinib (increases rosuvastatin exposure; limit rosuvastatin to 10 mg/day)
Minor Interactions
- Not many specific minor interactions listed; general caution with drugs affecting CYP2C9/3A4 or OATP1B1.
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess the need for therapy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST)
Rationale: To establish baseline liver enzyme levels and rule out active liver disease.
Timing: Prior to initiation of therapy.
Creatine Kinase (CK)
Rationale: To establish baseline levels if patient has predisposing factors for myopathy (e.g., renal impairment, hypothyroidism, history of muscle toxicity with other statins or fibrates, genetic muscle disorders, alcohol abuse).
Timing: Prior to initiation of therapy, if indicated.
Routine Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Frequency: 4-12 weeks after initiation or dose titration, then every 3-12 months or as clinically indicated.
Target: Individualized based on patient risk factors and guideline recommendations (e.g., LDL-C <100 mg/dL, <70 mg/dL, or <55 mg/dL depending on risk).
Action Threshold: Failure to achieve target lipid levels may warrant dose titration or consideration of alternative/add-on therapy.
Liver Function Tests (ALT, AST)
Frequency: Periodically, if clinically indicated (e.g., symptoms suggestive of liver injury). Routine monitoring is generally not recommended unless symptoms occur.
Target: Within normal limits.
Action Threshold: If transaminase levels persist at >3 times the upper limit of normal (ULN), discontinue rosuvastatin.
Creatine Kinase (CK)
Frequency: Only if muscle symptoms (e.g., pain, tenderness, weakness) develop.
Target: Within normal limits.
Action Threshold: If CK levels are significantly elevated (>10 times ULN) or if myopathy/rhabdomyolysis is diagnosed, discontinue rosuvastatin immediately.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (especially if accompanied by malaise or fever)
- Dark-colored urine
- Unusual fatigue or weakness
- Yellowing of the 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 fetal harm due to interference with cholesterol synthesis, which is critical for fetal development.
Second Trimester:
Potential for fetal harm.
Third Trimester:
Potential for fetal harm.
Lactation
Rosuvastatin is contraindicated during breastfeeding (Lactation Risk L5). It is unknown if rosuvastatin is excreted in human milk, but other statins are. Due to the potential for serious adverse reactions in the breastfed infant and the potential for interference with infant lipid metabolism, breastfeeding is not recommended.
Infant Risk:
High risk of adverse effects, including interference with infant lipid metabolism.
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 safety or effectiveness were observed between geriatric and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Increased risk of myopathy in patients âĨ65 years, particularly with higher doses or concomitant medications. No specific dose adjustment is required based on age alone, but consider starting at lower doses.
Clinical Information
Clinical Pearls
- Ezallor is a sprinkle capsule formulation, which can be opened and sprinkled on soft food (e.g., applesauce, pudding) 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, especially if accompanied by fever or malaise.
- Lifestyle modifications (diet, exercise, weight management) are crucial and should be continued while on rosuvastatin therapy.
- Avoid excessive alcohol consumption while on rosuvastatin due to increased risk of liver effects.
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): For dyslipidemia.
- Bile Acid Sequestrants: Cholestyramine, Colestipol, Colesevelam.
- Omega-3 Fatty Acid Esters: Icosapent ethyl, Omega-3-acid ethyl esters (for severe hypertriglyceridemia).
Cost & Coverage
Average Cost:
Highly variable, typically $50-$200+ per 30 capsules (5mg)
Generic Available:
Yes
Insurance Coverage:
Generic rosuvastatin is typically covered as Tier 1 or Tier 2. Brand-name Ezallor may be Tier 3 or higher, or require prior authorization.
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it is a good idea to check with your pharmacist. If you have any questions or concerns about this medication, do not 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.