What are the common and serious side effects of taking Crestor (rosuvastatin) for cholesterol management? How can you manage or prevent these side effects?

Understanding Crestor and Its Side Effects

Crestor, also known as rosuvastatin, is a statin medication used to lower low-density lipoprotein (LDL) or “bad” cholesterol. It works by blocking a substance in the liver needed to make cholesterol, while also helping the liver break down the cholesterol in the blood. Crestor can help increase high-density lipoprotein (HDL) or “good” cholesterol, lower triglycerides, and slow the buildup of plaque in blood vessels, reducing the risk of heart disease, heart attack, and stroke.

While Crestor can be effective in managing cholesterol, it may also cause some side effects, ranging from mild to more serious. It’s important to understand these potential side effects and know how to manage them.

Common Side Effects of Crestor

The most common side effects associated with Crestor include:

• Headache
• Muscle pain
• Stomach pain
• Feeling weak
• Nausea

These side effects are generally mild and may subside as your body adjusts to the medication. If they persist or worsen, be sure to consult your healthcare provider.

Serious Side Effects of Crestor

In some cases, Crestor can cause more serious side effects that require immediate medical attention. These include:

Muscle Breakdown (Rhabdomyolysis)

Rhabdomyolysis is a condition where the skeletal muscles break down, releasing proteins into the bloodstream that can damage the kidneys. This is a potentially serious side effect that is more likely to occur if you are older, have uncontrolled hypothyroidism, kidney problems, or are taking certain other medications. Signs to watch for include unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or unusual fatigue. If you experience these symptoms, contact your doctor right away, as they may need to stop your Crestor treatment.

Liver Disease

Crestor can also cause liver disease in some individuals. Your doctor will likely order blood tests to check your liver function before you start taking Crestor, and may continue to monitor it while you are on the medication. Symptoms of liver disease can include unusual tiredness, loss of appetite, upper abdominal pain, dark urine, and yellowing of the skin or eyes. Contact your doctor immediately if you experience any of these signs.

Rare Side Effects of Crestor

In rare cases, Crestor may also cause the following side effects:

• Immune-mediated necrotizing myositis (IMNM): A type of muscle inflammation that can lead to muscle cell death
• Kidney injury, which can develop from statin-associated rhabdomyolysis
• Rise in blood sugar, potentially leading to type 2 diabetes
• Memory loss or confusion

While these side effects are uncommon, it’s still important to be aware of them and report any concerning symptoms to your healthcare provider.

Managing Crestor Side Effects

If you do experience side effects from Crestor, there are several steps you can take to help manage or prevent them:

Consult Your Doctor

The first step is to make sure your doctor believes Crestor is the best medication for your specific situation and health history. They can help determine if the benefits of the drug outweigh the risks for you.

Adjust Your Exercise Routine

If you experience muscle pain or weakness, try adjusting your exercise routine. Avoid high-intensity workouts until the side effects subside, as strenuous exercise can increase the risk of muscle injury while taking Crestor.

Consider a Temporary Break

Taking a short break from Crestor can help you determine whether your aches and pains are due to the medication or something else. However, do not stop taking the drug without first consulting your doctor.

Adjust Your Dosage

Your doctor may be able to lower your Crestor dose or have you take it every other day, which could reduce some side effects while still providing cholesterol-lowering benefits.

Switch to Another Statin

If other management strategies don’t work, your doctor may recommend switching you to a different statin medication, as your body may tolerate a different drug better.

Dietary Considerations with Crestor

While taking Crestor, it’s important to follow a low-fat, low-cholesterol diet to maximize the drug’s effectiveness. Avoid grapefruit, as it can increase the absorption of Crestor and potentially lead to toxicity. Eggs, which can raise cholesterol, should be limited to no more than four yolks per week, but you can enjoy egg whites as desired.

By understanding the potential side effects of Crestor and working closely with your healthcare provider to manage them, you can help ensure that this medication effectively lowers your cholesterol while minimizing any unwanted consequences.

Nausea, Liver Disease, and More

Crestor is used along with dietary changes to lower your low-density lipoprotein (LDL), or “bad” cholesterol. Its common side effects tend to be mild, but some more serious complications may rarely occur.

Crestor is an HMG-CoA inhibitor, also known as a statin. Drugs in this class help treat high cholesterol by blocking a substance your liver needs to make cholesterol. They also work with your liver to break down the cholesterol in your blood.

Crestor helps increase your high-density lipoprotein (HDL), or “good” cholesterol. Additionally, the drug helps lower triglyceride (fat in your blood) and slow plaque buildup in the walls of blood vessels.

Crestor can help prevent heart disease, heart attack, and stroke in some people. However, sometimes it causes unwanted side effects. Learn what they are and tips to ease or stop them.

Crestor may create some mild or serious side effects, though you may not experience any. Serious side effects may also be possible, but they are less common. Other side effects are rare.

Common side effects

Common side effects can include:

• headache
• muscle pain
• stomach pain
• feeling weak
• nausea

Serious side effects

The following side effects are serious and require immediate medical attention:

Muscle breakdown (rhabdomyolysis)

Rhabdomyolysis is a breakdown of the muscles attached to your bones (skeletal muscles). It can be serious and can lead to severe kidney damage from the buildup of protein from the muscle tissue that is processed through your kidneys.

Your chance of muscle breakdown is higher if you:

• take certain other medicines while you take Crestor
• are 65 years old or older
• have hypothyroidism that isn’t controlled
• have kidney problems
• are taking a higher dose of Crestor than is typically prescribed

Talk with your doctor right away if you have unexplained muscle pains, tenderness, or weakness, especially if you have a fever or feel more tired than usual while you take Crestor. Your doctor may have you stop taking Crestor. If you have muscle problems that don’t go away even after you stop taking Crestor, let your doctor know.

Liver disease

Liver disease can also be a severe side effect of Crestor. Your doctor should do blood tests to check your liver before you start taking Crestor.

They should also do these tests if you have symptoms of liver disease while you take the drug. Call your doctor right away if you have any of the following symptoms of liver disease:

• unusual tiredness or weakness
• loss of appetite
• pain in your upper abdomen
• dark urine
• yellowing of your skin or the whites of your eyes

Rare side effects

In rare cases, you could develop the following:

• Immune-mediated necrotizing myositis (IMNM): A type of myositis that causes necrosis and cell death.
• Kidney injury: This can develop from statin-associated rhabdomyolysis.
• Rise in blood sugar, which can lead to type 2 diabetes.
• Memory loss or confusion

If you do have side effects, you can take steps to help relieve them or even make them go away. Talk with your doctor about the following actions:

• Consult with your doctor: Make sure that your doctor believes Crestor is the best medication for you, given your symptoms and health history.
• Slow down when you exercise: If you exercise more vigorously than usual while taking Crestor, your risk of muscle injury may be higher. It is best to change your exercise routine gradually. Exercise may cause muscle pain, so it may sometimes be hard to know if your pain is from heavy exercise or from taking Crestor.
• Take a short break: Stopping Crestor for a short time can help you decide whether your aches and pains are due to the medication or something else. Talk with your doctor before you stop taking your medication, however.
• Change your dose: Lowering your dose may reduce some of your side effects. But it may also reduce some of the cholesterol-lowering benefits. Another option may be to take Crestor every other day. Your doctor needs to approve these dosage changes before you try them.
• Switch to another statin drug: It’s possible that switching statins may reduce your side effects. If nothing else has worked, talk with your doctor about trying a different cholesterol drug.

What foods should be avoided when taking Crestor?

While taking Crestor, you should eat foods low in fat and low in cholesterol. Otherwise, the drug may not be as effective. In addition, avoid eating grapefruit, which can cause higher absorption of the drug and can lead to toxicity.

What fruit to avoid when taking Crestor?

A low cholesterol diet can include many fruits and vegetables. Here are some low cholesterol foods and food groups you can choose from.

Can I eat eggs while taking Crestor?

Eggs are very nutritious. However, they can raise your cholesterol and interfere with the effect of Crestor. Limit your egg yolk consumption to four times a week. You may eat egg whites as much as you like.

Crestor is a statin medication used to treat high cholesterol. You may experience some mild side effects while taking Crestor. In less common cases, serious side effects have been known to occur.

That said, in most cases taking this medication while making sure to eat a balanced, low cholesterol diet is safe. If you have other underlying medical conditions, your chance of serious consequences is greater. Speak with your doctor to make sure Crestor is right for you.

Common and Rare Side Effects for Crestor

COMMON side effects

If experienced, these tend to have a Severe expression i

If experienced, these tend to have a Less Severe expression i

INFREQUENT side effects

If experienced, these tend to have a Severe expression i

If experienced, these tend to have a Less Severe expression i

RARE side effects

If experienced, these tend to have a Severe expression i

If experienced, these tend to have a Less Severe expression i

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CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

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Crestor :: Instructions :: Price :: Description of the drug

Inactive ingredients: lactose monohydrate, microcrystalline cellulose, calcium phosphate, magnesium stearate, crospovidone, glycerol triacetate, hypromellose, red iron oxide (E 172), titanium dioxide, purified water.

Crestor 20 mg
Active substance: rosuvastatin 20 mg.
Inactive ingredients: lactose monohydrate, microcrystalline cellulose, calcium phosphate, magnesium stearate, crospovidone, glycerol triacetate, hypromellose, red iron oxide (E 172), titanium dioxide, purified water.

Crestor 40 mg
Active substance: rosuvastatin 40 mg.
Inactive ingredients: lactose monohydrate, microcrystalline cellulose, calcium phosphate, magnesium stearate, crospovidone, glycerol triacetate, hypromellose, red iron oxide (E 172), titanium dioxide, purified water.

Crestor is a lipid-lowering agent. The active substance of the drug is rosuvastatin – a competitive selective inhibitor of HMG-CoA reductase, an enzyme that transforms 3-hydroxy 3-methylglutarylcoenzyme A into a cholesterol precursor – mevalonate. The site of action of rosuvastatin is the liver, where low-density lipoprotein (LDL) catabolism and the formation of cholesterol (Cholesterol) occur. Rosuvastatin increases the number of hepatic receptors for low density lipoproteins on cell membranes, which leads to increased catabolism and uptake of low density lipoproteins and suppression of the formation of very low density lipoproteins (VLDL). As a result, there is a decrease in the content of low and very low density lipoproteins in the blood serum.

Rosuvastatin reduces elevated levels of total cholesterol, triglycerides and LDL cholesterol, apolipoprotein B (ApoB), VLDL-C, non-HDL-C, VLDL-C, LDL-C/HDL-C ratio, total-C/HDL-C, non-LDL/HDL-C and ApoB/ ApoA-I. Rosuvastatin slightly increases the content of HDL cholesterol and ApoA-I (apolipoprotein A-I).
The maximum effect of Crestor develops after 21 days of administration and remains constant. Already after 7 days of taking the drug, the therapeutic effect of Crestor is observed, and after 14 days of taking the drug, the effectiveness of the drug is 90% of the maximum possible.

The drug is indicated for adults with or without hypertriglyceridemia and hypercholesterolemia, regardless of age, sex or race. The drug can also be used in patients with familial hypercholesterolemia or diabetes mellitus.
While taking Crestor at a dosage of 10 mg, 80% of patients with an average baseline LDL cholesterol level of 4.8 mmol / l (hypercholesterolemia IIa and types) have a decrease in LDL cholesterol to ≤3 mmol / l. In patients with familial hypercholesterolemia who receive the drug at a dosage of 20–80 mg, a positive change in lipid profile is observed (a clinical study was conducted with the participation of 435 patients).

A 53% reduction in LDL-C was observed with 12 weeks of Crestor therapy after 40 mg/day dose titration, with LDL-C ≤3 mmol/L achieved in 33% of patients. Patients with familial homozygous hypercholesterolemia were prescribed the drug at a dosage of 20 and 40 mg, and during treatment with Crestor, the decrease in LDL cholesterol was 22%.
When combined with fenofibrate, an additive effect (triglyceride level) was registered, which was also observed when combined with nicotinic acid (in relation to HDL cholesterol).
While there is no evidence to estimate the reduction in the number of complications that are associated with lipid profile disorders (eg, coronary heart disease) – clinical studies are currently ongoing.

The maximum concentration of the active substance in the blood plasma is observed approximately 5 hours after the internal use of Crestor. Bioavailability – approximately 20%. Accumulates in the liver. The volume of distribution of rosuvastatin is 134 liters. Approximately 90% of the administered dose is bound by plasma proteins (albumin).

Approximately 10% of a dose of rosuvastatin undergoes limited metabolism. Rosuvastatin is a non-core substance for metabolism carried out by the cytochrome P450 system. The main enzyme that metabolizes rosuvastatin is CYP 2C9. To a lesser extent, CYP 3A4, CYP 2C19 and CYP 2D6 enzymes are involved in the metabolism of rosuvastatin. The main metabolites of the active substance are lactone metabolites and N-dismethyl. When comparing them, it turned out that N-dismethyl is about half (50%) less active than rosuvastatin. It was determined that lactone metabolites are pharmacologically inactive.

Geometric mean clearance of rosuvastatin is about 50 l/h with a coefficient of variation of 21.7%. 10% of the substance is eliminated by the kidneys. The half-life is approximately 19 hours, which is unchanged with increasing dosage. In the process of hepatic uptake of the active substance molecule (as with other HMG-CoA reductase inhibitors), a cholesterol transporter is involved, which plays an important role in the elimination of rosuvastatin by the liver.
The systemic exposure of rosuvastatin increases in proportion to the administered dose. In the case of taking several daily doses of the drug, the pharmacokinetic parameters of the active substance Crestor do not change.

A comparative study in patients living in Asia (Asian race) showed an increase in AUC and a 2-fold increase in the maximum concentration of rosuvastatin, compared with those living in Europe and Asia of Europeans. The influence of environmental factors and genetic factors on the obtained difference in pharmacokinetic parameters was not revealed. There were no clinically significant differences in the pharmacokinetics of rosuvastatin between patients of the Negroid and Caucasian races.

In case of impaired renal function (mild or moderate), the plasma content of rosuvastatin and its active metabolite (N-dismethyl) does not change significantly. In severe renal failure with a creatinine clearance level of ≤30 ml / min, the plasma concentration of the active substance increases by 3 times (moreover, the active metabolite, N-dismethyl, increases by 9 times). The plasma concentration of rosuvastatin in patients receiving chronic hemodialysis is approximately 50% higher. A study to study the pharmacokinetic parameters of rosuvastatin in patients with kidney disease was compared with a group of healthy volunteers.

There was no increase in the parameters of the half-life of the active substance in patients with different degrees of hepatic insufficiency, which were assessed on the Child-Pugh scale of 7 or less points. In patients rated at 8 and 9 points on the Child-Pugh scale, an increase in the half-life of at least 2 times was observed. So far, there is no experience with the use of rosuvastatin in patients with hepatic insufficiency with a Child-Pugh score of 9 or more.

Therapy for atherosclerosis to slow the progression of the disease in patients in whom lipid-lowering treatment is indicated;
in homozygous familial hypercholesterolemia as an adjunct to other cholesterol-lowering treatment (eg, LDL apheresis) or diet, as well as in cases where such treatment is ineffective;
as an adjunct to diet – in mixed hypercholesterolemia (type IIc) when non-pharmacological methods (weight loss, physical activity) and dietary changes are ineffective;
Primary hypercholesterolemia type IIa (including familial heterozygous hypercholesterolemia).

The drug is taken orally with water at any time of the day, regardless of food intake. Do not chew.
The dose of Crestor is titrated according to the response to treatment and the purpose of rosuvstatin use, taking into account recommendations for target lipoprotein levels. During treatment with the drug, the patient is prescribed a lipid-lowering diet (standard) for continuous use.

In the case of replacement of other HMG-CoA reductases or the first appointment of Crestor, a starting dosage of 5-10 mg / day is recommended. The choice of dose depends on individual cholesterol levels, the risk of side effects and risk factors for future complications from the cardiovascular system. With insufficient effect, you can increase the dosage of Crestor no earlier than 21 days after the start of taking the drug (since the maximum therapeutic effect develops precisely by this time). Reception of Crestor at a dose of 40 mg causes an increased risk of side effects of the drug compared to lower dosages, therefore, an increase in the dose of Crestor to 40 mg / day is allowed only at a high risk of developing cardiovascular complications (including patients with familial hypercholesterolemia) and in severe hypercholesterolemia. An increase in dosage to 40 mg / day is carried out only if the desired effect from the use of Crestor 20 mg / day has not been achieved, while the patient should be under close medical supervision. Particular attention to such a patient is necessary during the first days of taking Crestor at a dose of 40 mg / day.

Dosage escalation is appropriate if the desired result is not achieved with the 20 mg dosage and if patients are closely monitored by a specialist. Special control is recommended at the beginning of taking 40 mg of the drug.
Patients with a geriatric profile do not need to adjust the dosage of the drug.

In renal failure
Patients with mild dose adjustment is not required. In patients with moderate renal insufficiency, the starting dose of rosuvastatin should be 5 mg / day.
The maximum daily dosage for mild renal failure is 40 mg / day, for moderate renal failure (with creatinine clearance ≤60 ml / min) – 20 mg / day.
Crestor is contraindicated in patients with severe renal impairment.

In hepatic insufficiency
There is no experience with Crestor in patients with hepatic insufficiency who have a Child-Pugh score of 9 or more. The appointment of Crestor is contraindicated in patients with liver disease in the active phase.

Ethnic groups
An increase in the systemic concentration of rosuvastatin has been observed in patients of the Mongoloid race. Such patients should begin therapy with a dosage of 5 mg / day, with a maximum dose of 20 mg / day. The appointment of Crestor for patients of the Mongoloid race at a dosage of 40 mg / day is contraindicated.

With a tendency to develop myopathy
In patients with a tendency to develop myopathy, the starting dose of rosuvastatin should be 5 mg / day, the maximum dose – 20 mg / day. Such patients are contraindicated in the appointment of a dose of Crestor 40 mg / day.

The frequency of side effects, as with other HMG-CoA reductase inhibitors, depends on the dose used.
The incidence of side effects was estimated as follows: common side effects (≥1/100, ≤1/10), infrequent side effects (≥1/1000, ≤1/100), rare side effects (≥1/10,000, ≤ 1/1000), very rare side effects (≤1/10,000). Side effects in the application of Crestor are rated as moderately pronounced and stop on their own. Discontinuation of Crestor therapy during clinical trials due to side effects was 4% or less.

From the nervous system: dizziness, headache (often).
From the immune system: allergic reactions (including angioedema) – rarely.
From the skin and its appendages: rash, itching, urticaria (infrequent side effects).
From the musculoskeletal system: rhabdomyolysis and myopathy (rarely), muscle pain (often). Myopathy, muscle pain, and (rarely) rhabdomyolysis have been reported in patients taking any dose of Crestor, but especially in those using the 20 mg/day dose. The dose-dependent increase in the level of creatine phosphokinase (CPK), observed in patients who took Crestor, in most cases was not pronounced, transient and without symptoms. In the case of an increase in the level of CPK by 5 or more times, rosuvastatin is stopped.
From the gastrointestinal tract: constipation, abdominal pain, nausea (often), pancreatitis (rare).

From the urinary system: tubular proteinuria. There was a change in the amount of protein in the urine in gradation from no to traces of protein or up to two pluses or more in ≤1% of patients who were prescribed a dose of Crestor 10-20 mg / day. When taking a dose of 40 mg / day, the number of such patients was approximately 3% of patients. When using a dosage of Crestor at 20 mg / day, slight increases in the amount of protein in the urine were observed. Proteinuria in most cases decreased or disappeared with continued use and was not a symptom of the development of acute kidney disease or the progression of an existing one.
From the side of the liver: in a small number of patients, a dose-dependent increase in the content of transaminases was noted, as with other HMG-CoA reductase inhibitors. The increase in transaminases in most cases was transient, without symptoms and insignificant.
Other: asthenia (often).

After the widespread introduction of Crestor into medical practice, the following side effects have also been reported:
From the musculoskeletal system: joint pain (rare).
From the nervous system: polyneuropathy (very rare).
From the hepatobiliary system: hepatitis and jaundice (very rare).

· Liver disease in the active stage, including a persistent increase in the level of unexplained transaminases, as well as any increase in transaminases with a level of 3 or more times the upper limit of normal;
severe impairment of renal function with creatinine clearance ≤30 ml/min;
simultaneous use of cyclosporine;
during pregnancy and lactation;
hypersensitivity of the immune system to rosuvastatin or any other component of Crestor;
the drug is not prescribed to patients who do not use highly effective and effective methods of contraception;
myopathy;
The dose of Crestor 40 mg/day is contraindicated in patients with an increased risk of developing rhabdomyolysis or myopathy;
Age up to 18 years.

Crestor is contraindicated for use in pregnant women. In the case of the appointment of a nursing mother, breastfeeding is stopped. Before treatment with Crestor in women of reproductive age, a pregnancy test should be performed. While taking the drug, you must use adequate methods of contraception.

With the simultaneous use of cyclosporine and rosuvastatin, the AUC of the latter was approximately 7 times greater than the same parameter in healthy volunteers. The simultaneous use of these drugs does not change the plasma concentration of cyclosporine.

At the beginning of treatment and during an increase in the dose of Crestor in patients who simultaneously receive warfarin and other vitamin K antagonists, as in the case of other HMG-Co-A reductase inhibitors, an increase in INR – International Normalized Ratio – prothrombin time may be observed . Withdrawing Crestor or reducing its dosage causes a decrease in INR. When combining Crestor with vitamin K antagonists, monitoring of INR (prothrombin time) is recommended.

Simultaneous use of lipid-lowering drugs (eg gemifibrozil) and rosuvastatin causes an increase in the maximum plasma concentration of rosuvastatin and increase its AUC by 2 times.
The simultaneous use of ezetimibe and Crestor did not cause changes in the maximum plasma concentration of both drugs, as well as AUC. However, it is not recommended to exclude their pharmacological interaction with the development of side effects.

No pharmacokinetic interaction expected with fibrates, but pharmacodynamic interaction possible. Hemofibrates, gemfibrozil, other fibrates and lipid-lowering dosages of nicotinic acid (at a dose equivalent to 1 g / day or more) potentiate the risk of developing myopathy while taking HMG-CoA reductase inhibitors. This is probably due to the fact that these drugs cause the occurrence of myopathy when they are prescribed as monotherapy. Therefore, with this combination, patients are advised to initially prescribe a dose of Crestor 5 mg / day.

In a pharmacokinetic study in healthy volunteers, the combination of Crestor and a combination agent containing two protease inhibitors (100 mg ritonavor and 400 mg lopinavir) was associated with an approximately 2-fold increase in Crestor AUC. At the same time, the maximum concentration of rosuvastatin increased by about 5 times. Interactions with other protease inhibitors have not been studied. When prescribing Crestor to HIV-infected patients who are taking ritonavir/lopinavir while taking Crestor, the risk/benefit ratio should be considered, especially when increasing the dose or at the beginning of treatment.

Simultaneous administration of erythromycin and rosuvastatin causes a decrease in the AUC of rosuvastatin by 20% and its maximum plasma concentration by 30%. Such an interaction develops due to an increase in intestinal motility due to the administration of erythromycin.
The clinical significance of the interaction of antacids and Crestor has not been studied. The simultaneous use of antacids with the inclusion of magnesium hydroxide or aluminum and rosuvastatin causes a decrease in the concentration of the latter in the blood plasma by 50%. If antacids are taken 2 hours after rosuvastatin, then this effect is less pronounced.
No clinically significant interaction expected with digoxin.

The simultaneous use of rosuvastatin and oral contraceptives increases the AUC of norgestrel and the AUC of ethinyl estradiol by 34% and 26%, respectively. Therefore, an increase in plasma concentration should be considered when taking contraceptives. Pharmacokinetic parameters have not been studied with the combination of Crestor and drugs for hormone replacement therapy, but such an interaction cannot be ruled out. A similar combination of drugs was widely used during clinical trials – all patients tolerated it well.

The results of an in vivo and in vitro interaction study indicate that the active substance of Crestor is neither an inducer nor an inhibitor of enzymes of the cytochrome P450 system. Rosuvastatin is only a weak substrate for the action of these enzymes. No clinically significant interactions have been identified between ketoconazole (an inhibitor of CYP 3A4 and CYP 2A6) or fluconazole (an inhibitor of CYP 3A4 and CYP 2A9) and rosuvastatin. Simultaneous administration of itraconazole (an inhibitor of CY P3A4) and rosuvastatin increases the AUC of the latter by 28%, which has no clinical significance. Therefore, no interaction associated with the metabolism of cytochrome P450 is expected.

No specific treatment has been developed for overdose. Apply symptomatic agents and supportive therapy. If the dose is exceeded, it is necessary to monitor hepatic functions and the content of creatine phosphokinase (CPK). The effectiveness of hemodialysis is unlikely.

Tablets of 10; 20; 40 mg. There are 28 tablets in a blister.

Store below 30°C. Keep away from children. Released by prescription.

If there is an increased risk of developing myopathy or rhabdomyolysis, consider the benefit of treatment against the potential risk; such patients are subject to close medical supervision. If the level of CK increases significantly (5 times or more) even before the start of treatment, rosuvastatin should not be taken. The determination of cretinphosphokinase to control the possible development of rhabdomyolysis or myopathy is inappropriate to carry out in the presence of other likely factors for an increase in CPK or after intense physical exertion, since this may contribute to the incorrect interpretation of the results. In the event that the initial content of creatine phosphokinase is increased by 5 times or more, the next determination of the enzyme in the blood serum must be carried out no less than 5 (maximum – 7) days. Treatment with Crestor should not be started if a repeat determination shows a high baseline creatine phosphokinase level (5 times the upper limit of normal).

Crestor, like other HMG-CoA reductase inhibitors, should be used with caution in patients with a tendency to develop myopathy/rhabdomyolysis. Risk factors for rhabdomyolysis or myopathy may include: hypothyroidism; kidney failure; conditions that cause an increase in the plasma concentration of rosuvastatin; alcohol abuse; age over 70; the presence of hereditary muscle diseases in a family or individual history; myotoxicity provoked by the use of other fibrates or inhibitors of GMC-CoA reductase in history; simultaneous use of fibrates.

If the patient is prescribed Crestor, he must be informed of the obligation to immediately report to the attending physician about all cases of unexpected muscle weakness, muscle pain or spasms, especially if they are accompanied by fever and malaise. In such patients, determination of the level of creatine phosphokinase (CPK) is required. Reception of Crestor should be discontinued if the content of CPK is significantly increased (by 5 times or more), or with a sharp severity of muscle symptoms that cause constant daily discomfort even if the content of creatine phosphokinase has not reached a 5-fold increase. If the signs disappear and the content of CPK returns to its original physiological value, the possibility of re-administration of other inhibitors of HMG-CoA reductase or Crestor at doses lower than the previous ones is considered. Such a patient needs careful medical supervision. Routine monitoring of CPK in the absence of signs of rhabdomyolysis or myopathy is not advisable.

There was no evidence of an increase in the effect of Crestor on skeletal muscle during clinical studies with concomitant therapy. However, there are reports of an increase in the number of cases of myopathy and myositis in patients who took other HMG-CoA reductase inhibitors against the background of the use of fibric acid derivatives (including when prescribing drugs such as nicotinic acid, gemfibrozil, cyclosporine, inhibitors proteases, azole antifungals and macrolide antibiotics). Gemfibrozil increases the risk of myopathy when Crestor is combined with certain HMG-CoA reductase inhibitors. It is not recommended to prescribe Crestor and gemfibrozil at the same time. It is necessary to carefully evaluate the ratio of possible benefits and potential risks when prescribing a combination of niacin, fibrates and Crestor.
Co-administration with Crestor fibrates at a dose of 40 mg is contraindicated.

Crestor is not recommended for patients with acute severe conditions (eg, hypotension, trauma, sepsis, major surgery, marked endocrine, metabolic, or electrolyte disturbances, or uncontrolled epilepsy, as these conditions may be contributing factors) risk of rhabdomyolysis/myopathy).

Cases of tubular proteinuria have been observed in patients taking high doses of rosuvastatin (mainly 40 mg/day). Tubular proteinuria was short-term or transient in most cases. This proteinuria was not evidence of the development of acute kidney disease or the progression of an existing one. Patients receiving Crestor at a dosage of 40 mg / day are recommended to periodically monitor the functional parameters of the kidneys during the administration of Crestor (the entire course of therapy).
When taking rosuvastatin, especially at doses of approximately 20 mg / day, there have been reports of skeletal muscle effects, such as muscle pain, rhabdomyolysis or myopathy. However, with the combination of ezetimibe and HMG-CoA reductase inhibitors, rhabdomyolysis developed in very rare cases.

The safety and efficacy of Crestor in children have not been established. In pediatric practice, the experience of using rosulostatin is limited to a small number of observations (children under 8 years of age and older with homozygous familial hypercholesterolemia). Therefore, it is not recommended to use Crestor for treatment in pediatric practice.

The instruction was compiled by a team of authors and editors of the Piluli website. The list of authors of the drug reference book is presented on the site editorial page: Site editors.

References to used sources of information.

Attention!
Description of the drug “ Crestor ” on this page is a simplified and supplemented version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the annotation approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide on the appointment of the drug, as well as determine the dose and methods of its use.

The choice of drugs to lower cholesterol and prevent the risk of cardiovascular disease

Currently, this is probably the only group of drugs that causes a huge amount of controversy and misunderstanding among patients.

Why?

Cholesterol level is not felt by the body. The effectiveness of the use of statins can only be monitored using laboratory tests.

There is a whole campaign on the Internet and in the media about the side effects of using statins, especially their harmful effects on the liver, which in fact have nothing to do with the real situation. This is a separate study (https://pubmed.ncbi.nlm.nih.gov/32557172/)

You need to take statins for life. This is not an emergency medicine. Even if the cholesterol level has returned to normal, you can stop taking the drug only in extreme cases.

According to the study In Russia, after 1 year, 69.9% of patients refuse to take statins, and within 5 years – 93.1%.

Causes:

• Fear of adverse effects that they read about in the instructions for the drug or in the media (46%)
• Lack of faith that the drug prolongs life (29.4%)
• Taking a large number of concomitant tablets (27.6%)
• Forgetfulness (26.5%)
• Weak effect on blood cholesterol levels while taking medication (18.8%)
• Physician withdrawal (13.5%).

At the same time, the real development of adverse events on statin therapy was observed only in 11.7% of patients, and their manifestations were mild to moderate.
It turns out that fear and “lack of faith” lead to 6 times more drug withdrawal than actual side effects.

The following groups of drugs are used to lower blood cholesterol levels and prevent cardiovascular diseases:

statins

bile acid sequestrants

fibrates

nicotinic acid

cholesterol reabsorption blockers

CETP inhibitors

Detailed description of each group of drugs, assessment of their action, possible side effects, contraindications and impact on the forecast are presented in the table.

As can be seen from the table, statins and bile acid sequestrants have mainly a cholesterol-lowering effect, fibrates predominantly reduce hypertriglyceridemia, and nicotinic acid reduces both cholesterol and triglycerides. Bile acid sequestrants, which not only do not reduce the level of TG, but can even significantly increase it, are not prescribed when the upper limit of the normal TG (200 mg / dL) is exceeded. Nicotinic acid lowers both cholesterol and TG levels. Fibrates have the most pronounced ability to correct hypertriglyceridemia, but their cholesterol-lowering effect is inferior to that of other classes of lipid-lowering drugs.

Thus, the main drug of choice in the selection of cholesterol-lowering therapy are statins.

The main representatives of the group of statins that are prescribed and used today are rosuvastatin and atorvastatin. They are the safest and most effective.

A few examples from my own practice:

1. Woman, 64 years old, suffering from compensated type 2 diabetes since the age of 49. BMI (body mass index) 30.4, heredity is aggravated – the father had diabetes, was overweight, arterial hypertension, died at 56 from a heart attack.

On examination: according to the ultrasound examination of the carotid arteries, thickening of the intima-media complex up to 1. 1 mm, no plaques.

Blood creatinine is normal, but microalbuminuria is increased by 2.5 times, the initial decrease in glomerular filtration rate is a sign of diabetic nephropathy. The level of low-density lipoprotein cholesterol (LDL cholesterol) increased to 4.4 mmol/l.

There are no clinical signs of atherosclerosis, however, the presence and duration of type 2 diabetes is characterized by damage to target organs (kidneys, endothelium), and, in addition, according to the latest recommendations, diabetes is equated to coronary artery disease in terms of the risk of developing cardiovascular complications.

Therefore, it is advisable for the patient to prescribe statins – atorvastatin at a dose of 40 mg / day is indicated due to the significant height of cardiovascular risk.

A year later, compensation for type 2 diabetes is maintained, there are no clinical manifestations of atherosclerosis, kidney and liver function are normal, microalbuminuria does not exceed 2 times the norm, the target LDL cholesterol level of 1. 9 mmol/l has been reached.

It is recommended to continue ongoing therapy, including taking Liprimar at a dose of 20 mg/day.

2. Man, 57 years old, arterial hypertension of the 2nd degree, metabolic syndrome, BMI 32, heredity is not burdened.

On examination: the level of microalbuminuria increased by 3.5 times, LDL cholesterol increased to 5.2 mmol/l. Receives treatment: angiotensin-converting enzyme inhibitor, thiazide diuretic, calcium channel antagonist, aspirin. Blood pressure at the target level. Should I prescribe statins?

For a patient with arterial hypertension and three risk factors, it is advisable to prescribe atorvastatin at a dose of 20 mg / day for the purpose of primary prevention of cardiovascular complications.

At the examination after 4 months: the level of microalbuminuria is reduced to 1.5-fold, LDL – 2.9 mmol / l, AST, ALT, CPK are normal. diet for weight loss: “plate rule”, physical activity – 10,000 steps a day

Despite the apparent positive effect of statins, these drugs are far from safe. And I, as a doctor, always warn patients about the possible complications that may arise when taking them.

Main side effects of statins

1. Muscle pain is one of the most common complaints of patients taking statins. It can be felt as mild discomfort (soreness, fatigue, muscle weakness), or it can be difficult to bear. A 2016 study published in the Journal of the American College of Cardiology found that this symptom usually occurs in people who: have low muscle mass have hypothyroidism are vitamin D deficient drink alcohol regularly take tricyclic antidepressants, azole antifungals, or mycin antibiotics often drink grapefruit or pomegranate juice. Moreover, in some cases, patients develop rhabdomyolysis, an extreme degree of muscle damage in which a large number of muscle cells are destroyed at the same time. The breakdown products enter the systemic circulation and cause muscle pain, nausea, vomiting, disorientation, heart rhythm disturbances, and even acute renal failure. The risk of a life-threatening condition is very low – only a few cases per million people taking statins. Rhabdomyolysis can occur if you are taking statins in combination with certain medications or if you are taking high doses of statins.

2. Liver damage. According to a study published in the Journal of the American College of Cardiology, abnormal liver function tests are sometimes observed with statins, and this is especially true for patients taking lipid-lowering drugs for the first time. As you know, an increase in ALT and AST enzymes may indicate an inflammatory process in the liver. If the indicators are slightly increased, the course of treatment with statins, as a rule, is not interrupted. With a strong increase in the level of enzymes, the statin drug can be replaced. To prevent liver damage, patients are advised to take a biochemical blood test for liver enzymes before the course of statins and some time after the start of therapy. In addition, doctors advise combining statins with ursodeoxycholic acid preparations. UDCA simultaneously protects liver cells and improves the anti-cholesterol effect. Be sure to tell your doctor if you experience unusual fatigue or weakness while taking statins, notice a lack of appetite, pain in the upper abdomen, dark urine and / or yellowing of the skin and mucous membranes.

3. High blood sugar or type 2 diabetes. A 2017 meta-analysis published in Nutrition, Metabolism and Cardiovascular Diseases found an association between statin use and type 2 diabetes. The authors of the study stated that patients treated with statins had a 44% increased risk of developing diabetes. People without a predisposition to diabetes are advised to keep their blood sugar under control and, if they worsen, talk to their doctor about changing their treatment strategy. Patients with an inherently high risk of diabetes may be better off looking for other approaches to lower cholesterol levels (through diet, exercise, and other medications).

4. Very rare, but possible neurological side effects in the form of memory loss and confusion . These side effects disappear as soon as you stop taking the medicine.

Who is at high risk for the side effects of statins.

Not everyone who takes a statin has side effects. Here are the categories of patients at increased risk of unpleasant symptoms:

Patients taking multiple cholesterol-lowering drugs at the same time

Patients with kidney or liver disease

Alcohol abusers

Patients with hypothyroidism or neuromuscular disorders such as amyotrophic lateral sclerosis (ALS) 90 005

Patients aged 80 and over

Women

Drugs that increase the risk of side effects when taking statins:

1. Amiodarone – for the treatment of arrhythmia

2.