CholesterolRoszet (Generic)
Generic drugs, marketed without brand names, contain the exact same active ingredients used in their brand-name counterparts, but cost significantly less. The drugs are required to meet US Food and Drug Administration (FDA) standards for safety, purity and effectiveness.
Roszet
Both rosuvastatin and ezetimibe are the active ingredients of the cholesterol-lowering medication known as Roszet. Roszet is prescribed to persons with high blood cholesterol levels in conjunction with dietary changes in order to lower low density lipoprotein cholesterol (LDL-C), often known as "bad cholesterol." To lower LDL-C levels in individuals who have a form of high cholesterol known as homozygous familial hypercholesterolemia (HoFH), it is also used either by alone or in combination with other medications that lower LDL.
Generic Roszet (Rosuvastatin and Ezetimibe): A Comprehensive Overview
Introduction
Generic Roszet is a combination medication that includes two active ingredients: Rosuvastatin and Ezetimibe. It is used to manage high cholesterol and reduce the risk of cardiovascular diseases. Rosuvastatin is a statin that works by inhibiting cholesterol production in the liver, while Ezetimibe is a cholesterol absorption inhibitor that reduces the amount of cholesterol absorbed from the diet. Together, these two agents provide a dual mechanism of action to lower LDL cholesterol (bad cholesterol), increase HDL cholesterol (good cholesterol), and improve overall lipid profiles. This article provides an in-depth exploration of the pharmacology, therapeutic uses, mechanism of action, side effects, and other important aspects of Generic Roszet (Rosuvastatin and Ezetimibe).
Pharmacology
Chemical Structure and Properties
Rosuvastatin:
Chemical Name: (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamido)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid.
Molecular Formula: C22H28FN3O6S.
Molecular Weight: 481.54 g/mol.
Rosuvastatin is a white to off-white powder that is sparingly soluble in water and methanol.
Ezetimibe:
Chemical Name: 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-3-hydroxypropyl]-4S-(4-hydroxyphenyl)-2-azetidinone.
Molecular Formula: C24H21F2NO3.
Molecular Weight: 409.43 g/mol.
Ezetimibe is a white, crystalline powder that is insoluble in water but soluble in ethanol and methanol.
Mechanism of Action
1. Rosuvastatin:
HMG-CoA Reductase Inhibition: Rosuvastatin is a competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme responsible for converting HMG-CoA to mevalonate, a precursor of cholesterol. By inhibiting this enzyme, Rosuvastatin reduces the production of cholesterol in the liver.
LDL Receptor Upregulation: Rosuvastatin increases the expression of LDL receptors on the surface of liver cells, enhancing the clearance of LDL cholesterol from the bloodstream.
Triglyceride Reduction: Rosuvastatin also reduces triglyceride levels by inhibiting their synthesis and increasing their clearance.
HDL Cholesterol Increase: Rosuvastatin modestly increases HDL cholesterol levels, which is beneficial for cardiovascular health.
2. Ezetimibe:
Cholesterol Absorption Inhibition: Ezetimibe works in the small intestine by selectively inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) protein, which is responsible for the absorption of dietary and biliary cholesterol. This action reduces the amount of cholesterol entering the bloodstream.
Complementary Mechanism: When combined with Rosuvastatin, Ezetimibe provides an additional mechanism to lower LDL cholesterol by targeting cholesterol absorption, while Rosuvastatin targets cholesterol production.
Pharmacokinetics
1. Rosuvastatin:
Absorption: Rosuvastatin is well absorbed after oral administration, with peak plasma concentrations occurring within 3-5 hours. Its bioavailability is approximately 20%.
Distribution: Rosuvastatin is highly bound to plasma proteins (88%) and is distributed primarily to the liver, the target site of its action.
Metabolism: Rosuvastatin undergoes limited metabolism in the liver, primarily via cytochrome P450 2C9 (CYP2C9) and 2C19 (CYP2C19). It is not significantly metabolized by CYP3A4, reducing the risk of drug interactions.
Excretion: Rosuvastatin is primarily excreted unchanged in the feces (90%), with a small portion excreted in the urine (10%). Its elimination half-life is approximately 19 hours.
2. Ezetimibe:
Absorption: Ezetimibe is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 4-12 hours. Its bioavailability is approximately 35%.
Distribution: Ezetimibe is highly bound to plasma proteins (99.7%) and is distributed extensively throughout the body.
Metabolism: Ezetimibe is metabolized in the liver and small intestine to its active glucuronide metabolite, which is also effective in inhibiting cholesterol absorption.
Excretion: Ezetimibe and its metabolite are primarily excreted in the feces (78%) and urine (11%). The elimination half-life of Ezetimibe is approximately 22 hours.
Therapeutic Uses
1. Primary Hyperlipidemia:
Generic Roszet is used to treat primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH), a genetic condition characterized by high LDL cholesterol levels. It is particularly effective in patients who require additional LDL cholesterol lowering beyond what can be achieved with statin monotherapy.
Roszet is also used to treat HoFH, a rare genetic disorder characterized by extremely high LDL cholesterol levels. The combination of Rosuvastatin and Ezetimibe provides significant LDL cholesterol reduction in these patients.
3. Atherosclerosis Prevention:
By lowering LDL cholesterol and improving lipid profiles, Roszet helps reduce the risk of atherosclerosis (plaque buildup in arteries), which can lead to cardiovascular events such as heart attacks and strokes.
4. Adjunct to Diet and Lifestyle Modifications:
Roszet is used as an adjunct to diet, exercise, and other lifestyle modifications to manage high cholesterol in patients who have not achieved their target lipid levels with statin monotherapy.
Dosage and Administration
Generic Roszet is available in fixed-dose combinations of Rosuvastatin and Ezetimibe. Common dosages include:
Rosuvastatin 10 mg + Ezetimibe 10 mg.
Rosuvastatin 20 mg + Ezetimibe 10 mg.
Rosuvastatin 40 mg + Ezetimibe 10 mg.
Administration Guidelines:
Taken orally once daily, with or without food.
Should be taken in the evening for optimal efficacy, as cholesterol synthesis is highest at night.
Dosage adjustments may be necessary based on patient response, tolerance, and underlying conditions.
Side Effects and Adverse Reactions
Common Side Effects:
Muscle Pain (Myalgia): A common side effect of statins, including Rosuvastatin.
Headache: Mild to moderate headaches may occur.
Gastrointestinal Disturbances: Nausea, diarrhea, and abdominal pain are possible, particularly with Ezetimibe.
Fatigue: Some patients may experience tiredness or weakness.
Serious Side Effects:
Myopathy and Rhabdomyolysis: Rare but serious conditions involving muscle breakdown, which can lead to kidney damage.
Hepatotoxicity: Elevated liver enzymes and, in rare cases, liver damage.
Allergic Reactions: Rash, itching, and swelling of the face, lips, or tongue.
Increased Blood Sugar Levels: Statins may increase the risk of developing type 2 diabetes.
Drug Interactions
Cyclosporine: Increases the risk of myopathy and rhabdomyolysis when used with Rosuvastatin.
Gemfibrozil and Other Fibrates: May increase the risk of muscle-related side effects.
Warfarin: Rosuvastatin may enhance the anticoagulant effect of warfarin, requiring close monitoring of INR levels.
Bile Acid Sequestrants: May reduce the absorption of Ezetimibe if taken simultaneously. Ezetimibe should be taken at least 2 hours before or 4 hours after bile acid sequestrants.
Contraindications and Precautions
Contraindications:
Hypersensitivity to Rosuvastatin, Ezetimibe, or any component of the formulation.
Active liver disease or unexplained persistent elevations in liver enzymes.
Pregnancy and lactation (statins are contraindicated during pregnancy due to the risk of fetal harm).
Precautions:
Liver Function: Monitor liver enzymes before and during treatment.
Muscle Symptoms: Monitor for signs of myopathy, particularly in patients at higher risk (e.g., elderly, renal impairment).
Renal Impairment: Dose adjustments may be necessary for patients with severe renal impairment.
Special Populations
Elderly Patients:
Older adults may be at higher risk for muscle-related side effects and should be monitored closely.
Pediatric Patients:
The safety and efficacy of Roszet in children have not been established.
Patients with Renal or Hepatic Impairment:
Use with caution in patients with severe renal or hepatic impairment. Dose adjustments may be necessary.
Conclusion
Generic Roszet (Rosuvastatin and Ezetimibe) is a powerful combination medication for managing high cholesterol and reducing the risk of cardiovascular diseases. By targeting both cholesterol production and absorption, it provides a comprehensive approach to lipid management. While generally well-tolerated, it requires careful monitoring for potential side effects, particularly muscle-related and liver-related complications. With appropriate use and monitoring, Roszet offers significant benefits for patients with hyperlipidemia, helping them achieve their cholesterol goals and improve their overall cardiovascular health.
What is Roszet tablet?
What kind of medication is this?
Both rosuvastatin and ezetimibe are the active ingredients of the cholesterol-lowering medication known as Roszet. Together with dietary changes, Roszet is prescribed to persons who already have high blood cholesterol levels in order to lower low density lipoprotein cholesterol (LDL-C), often known as "bad cholesterol."
LDL-C levels can be lowered in people with homozygous familial hypercholesterolemia (HoFH), a kind of high cholesterol that can be treated either on its own or in conjunction with other medications that lower LDL levels.
It is unknown at this time whether or not this medication is both safe and effective when administered to youngsters.
Who shouldn't use the Roszet medication?
Do not use Roszet if you have any condition that affects your liver, including recurring blood tests that reveal probable liver damage.
are hypersensitive to ezetimibe, rosuvastatin, or any of the other components of this medication. A comprehensive list of the components may be found at the bottom of this page.
Before I start using this medication, what information is important for my physician to have?
Inform your healthcare practitioner about all of your medical issues before beginning therapy. This is especially important if you have any symptoms that cannot be explained, such as muscular pains or weakness.
having issues with their thyroid.
have renal troubles.
drink more than two glasses of alcohol every day or have previously struggled with liver issues.
have diabetes.
are pregnant or intend to get pregnant. There is a risk that Roszet will damage your unborn child. If you get pregnant while undergoing therapy, you should immediately contact your healthcare professional and cease the treatment.
are still nursing their infants. Roszet has been shown to enter breast milk, where it might potentially affect a nursing infant. If you are taking Roszet, you should consult your healthcare professional about the safest and most effective approach to feed your child. While you are on Roszet, you should not breastfeed.
are at least 65 years old if not older.
are descended from people in Asia.
Inform your doctor about any and all of the medications you use, whether they are prescribed to you or purchased over the counter, as well as any vitamins or herbal supplements you take. Have a conversation with your primary care physician before beginning treatment with any new medication.
Using Roszet with other medications may increase the likelihood that you will experience muscular difficulties or other adverse effects.
In particular, make sure your doctor knows if you take any medications for: acid reflux or heartburn (such as antacids that contain aluminum and magnesium hydroxide)
cholesterol, medications for your immune system (like cyclosporine), and your immune system (such as niacin or nicotinic acid, gemfibrozil, fibrates)
anti-fungal medications or illnesses (such as itraconazole, ketoconazole, and fluconazole)
heart failure, including the use of anticoagulants containing coumarin (such as warfarin)
gout (such as colchicine) (such as colchicine)
darolutamide (a medication for the treatment of prostate cancer) (a medicine for the treatment of prostate cancer)
regorafenib (a medication used to treat cancer of the colon and rectum) (a medicine used to treat cancer of the colon and rectum)
anti-viral medications, such as some HIV or hepatitis C virus drugs, such as: lopinavir, ritonavir, fosamprenavir, tipranavir, atazanavir, simeprevir combo of sofosbuvir/velpatasvir/voxilaprevir; atazanavir; simeprevir; atazanavir; simeprevir; simeprevir; atazanavir; si
dasabuvir/ombitasvir/paritaprevir/ritonavir\selbasvir/grazoprevir
sofosbuvir/velpatasvir
glecaprevir/pibrentasvir in addition to all other possible combinations with ledipasvir, including ledipasvir/sofosbuvir
If you are unsure, you should inquire with your healthcare practitioner or pharmacist about obtaining a list of these medications. You should be aware of every medication you take. Make sure to keep a list of them to show your healthcare professional and the pharmacy if you obtain a new medication.
What is the correct way to take this medication?
Take Roszet precisely as directed by your primary care physician or other healthcare professional.
Take one dose of Roszet once day, either with or without meals. It is possible that if you take your medication at the same time each day, such as when you eat breakfast, dinner, or before bed, it will be simpler for you to remember to take it.
Tablets should be ingested in their whole. Tablets should not be chewed, crushed, or dissolved in liquid.
You should continue to take Roszet until your healthcare practitioner instructs you otherwise. If you stop taking the medication, your cholesterol levels may start to climb again.
If you miss a dosage, do not take an additional dose. Take the following dosage at the regular interval. If it has been less than 12 hours since your previous dosage of Roszet, do not take another dose.
In the event that you take too much or overdose, immediately contact the Poison Control Center at 1-800-222-1222 or go to the emergency department of the hospital that is closest to you.
See your primary care physician on a regular basis to have your cholesterol level monitored and to screen for any potential adverse effects. Before beginning therapy and periodically thereafter, your doctor may order blood tests to evaluate the function of your liver.
Which additional substances will have an effect on Roszet?
If you are also taking cholestyramine, colesevelam, or colestipol, you should take your dose of ezetimibe and rosuvastatin either two hours before or four hours after you take the other medication.
Talk to your primary care physician about any other medications you are taking. When taken together, ezetimibe and rosuvastatin can increase the risk of serious muscle problems, particularly in patients taking the following medications: colchicine, cyclosporine; antifungal medication fluconazole, itraconazole, ketoconazole; a blood thinner warfarin, Coumadin, Jantoven; cancer medicine darolutamide, regoragenib; other cholesterol medications fenofibrate, fenofibric acid
This list is not exhaustive, and the effects of ezetimibe and rosuvastatin may also be influenced by a wide variety of other medications. This include both prescription and over-the-counter medications, in addition to herbal and vitamin supplements. This page does not provide a complete listing of all possible medication interactions.
What potential negative reactions may I have to this medication?
Roszet has the potential to induce certain major adverse effects, including:
Reactions caused by allergies, include the life-threatening condition known as anaphylaxis. If you have any of the following symptoms, you should contact your healthcare professional as soon as possible:
symptoms may include: puffiness of the face, lips, tongue, and/or throat, which makes it difficult to swallow or breathe; breathing difficulties or wheezing; feeling dizzy or fainting; rash or hives; itching; and/or
Pain, sensitivity, and weakening in the muscles (myopathy). Problems with the muscles, particularly muscular breakdown, can be significant in certain people and, although it happens seldom, can cause damage to the kidneys that can ultimately result in death. If you take certain other medications along with Roszet, your risk of experiencing muscular difficulties will be significantly increased. When you are using Roszet, you should immediately contact your healthcare practitioner if you experience any of the following symptoms: muscular discomfort, soreness, or weakness for no apparent reason, particularly if you have a fever or feel more fatigued than usual.
Even after following the advice of your healthcare physician to discontinue use of Roszet, you continue to experience muscular issues that do not go away. In order to determine the root cause of your muscular issues, your doctor may order some more diagnostic procedures.
The following are the most often experienced adverse effects:
headache
weakness
diarrhea
dizziness
aches and pains (in the back, hands, and legs), nausea, constipation, and painful joints
aches and pains in the muscles as well as the stomach
The flu and the common cold
a scratchy throat and runny nose are symptoms of fatigue.
Talk to your doctor if you have any side effects that make you uncomfortable or that do not go away after a reasonable amount of time.
What is the best way to store Roszet?
Keep Roszet at a temperature between 20 and 68 degrees Celsius (68 and 77 degrees Fahrenheit) at room temperature.
Keep the bottle of Roszet away from any sources of moisture or humidity.
You should never take a pill out of its bottle until you are ready to consume it.
After taking the pill out of the container, put the top back on and make sure it's on very securely.
When the container has been opened, the pills should be used within the following month.
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selection of products. I wasn’t happy with my current ED product was using, so I was able to
try out a different kind and see if it was a better fit for my needs. Which it was!
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crossed my mind how much cheaper the generic versions were. When I started browsing the
items I couldn’t believe the price difference! This is my go to shop right now.
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always bought it in store. I spoke to one of their support reps and they were really nice
and helped to explain how it works and made me feel much more comfortable with my order!
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and it definitely won’t be my last! They had all the items I needed in one place and the
prices are the best I could find online.
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for shipping. When I found this site I was thrilled to see they offer free discreet
shipping. I am saving significantly more money.
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