Rosuvastatin

Rosuvastatin is a drug that reduces the production of "bad" LDL cholesterol in the liver.

It also increases the concentration of "good" HDL cholesterol. Rosuvastatin inhibits the development of atherosclerosis and even reduces the size of atherosclerotic plaques that have already formed. For today it is the newest medicine among all tablets from cholesterol. It refers to the statins of the last IV generation.

The drug is characterized by a low load on the liver, since the metabolism of rosuvastatin in the liver is minimal. Over 80% of the drug is excreted naturally through the intestine, from 5 to 10% is excreted naturally by kidneys with urine. The half-life of rosuvastatin ranges from 12 to 16 hours, depending on the dosage, and the therapeutic effect persists for approximately 30 hours. Cumulation of the drug in the body does not exceed 2 - 5%, depending on the individual characteristics of the patient.

Clinical and pharmacological group

Lipid-lowering drug.

Terms of sale from pharmacies

It is possible to buy under the prescription of the doctor.

Price

How much does rosuvastatin cost in pharmacies? The average price is at the level of350 rubles.

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Composition and form of release

The drug Rosuvastatin is manufactured in the form of a tablet coated with a film coating for oral (oral) administration. They have a light pink or pink color, a round shape and a biconvex surface.

Each tablet is film-coated. The main substance -rosuvastatin.

Excipients:

• corn starch;
• magnesium stearate;
• microcrystalline cellulose;
• povidone;
• calcium hydrogen phosphate dihydrate.

Composition of the film shell:

• seleicate AQ-01032 red;
• titanium dioxide;
• hypromellose;
• macrogol-400;
• macrogol-6000.

Depending on the dosage (10 mg, 20 mg, 40 mg), the composition of the tablet varies.

pharmachologic effect

Rosuvastatin is a lipid-lowering drug, a selective competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) -reductase, which is an enzyme that converts 3-hydroxy-3-methylglutaryl Coo into the precursor of cholesterol (cholesterol) - mevalonate. The drug increases the number of LDL receptors (low-density lipoproteins) on the surface of liver cells, as a result, catabolism and the uptake of LDL are increased and the VLDLP synthesis is inhibited (very low lipoproteins density). Eventually, the total number of VLDL and LDL is reduced.

Under the influence of rosuvastatin reduced elevated concentrations of OXC (total cholesterol), LDL-C (low-density lipoprotein cholesterol), TG (triglycerides), ApoB (apolipoprotein B), TG-VLDL and HS-VLDL. The drug increases the concentration of HDL cholesterol (high-density lipoprotein cholesterol) and ApoA-I (apolipoprotein A-I). Rosuvastatin reduces the atherogenic index, improving the lipid profile in patients with hypercholesterolemia.

The therapeutic effect of the drug develops within the first week after the initiation of its administration, reaching a maximum by the fourth week of the course.

Pharmacokinetics

The maximum plasma concentration of the active substance is reached 5 hours after taking Rosuvastatin. Absolute bioavailability of about 20%.

The main metabolism is carried out by the liver. The volume of distribution is 134 liters. About 90% of the substance binds to plasma proteins (mainly with albumins). The main metabolites are lactone metabolites (do not have pharmacological activity) and N-desmethylrozuvastatin (50% less active than rosuvastatin).

Approximately 90% of the accepted dose of the drug is excreted through the intestine in unchanged form, the rest - by the kidneys. The half-life of the plasma is 19 hours.

The pharmacokinetics of rosuvastatin does not depend on the sex and age of the patient.

In persons of the Mongoloid race, a double increase in the maximum plasma concentration of rosuvastatin and the median AUC (area under the "concentration-time" curve) is observed in comparison with patients-Caucasians; In Indians, the maximum plasma concentration and the median AUC increase by a factor of; in representatives of the Negroid race, the pharmacokinetic indices are similar to the similar ones indicators of Caucasians.

Mild or moderate renal failure does not significantly affect the concentration of rosuvastatin and its metabolite N-desmethyl-rosuvastatin. In severe renal failure, the plasma concentration of rosuvastatin increases approximately three-fold, and N-desmethyl-rosvastatin is increased nine-fold. In patients on hemodialysis, the concentration of the active ingredient is higher by approximately 50%.

In patients with severe hepatic insufficiency, the half-life of rosuvastatin may increase at least twice.

Indications for use

For taking rosuvastatin tablets, several medical indications are distinguished, which include:

1. Family (hereditary) homozygous hypercholesterolemia.
2. Primary hypercholesterolemia is a condition accompanied by an increase in the level of cholesterol in the blood.
3. Hypertriglyceridemia is an increased concentration of free fats (triglycerides) in the blood.
4. Prevention of complications of atherosclerosis (deposition of cholesterol in the walls of arterial vessels with a narrowing of their lumen), in particular angina pectoris, myocardial infarction, hypertension, cerebral stroke in persons over the age of 50 years.

Also, the drug is used to slow the development of atherosclerosis as an adjunct to dietary recommendations.

Contraindications

Absolute:

• deficiency of lactase, lactose intolerance or malabsorption of glucose-galactose;
• pregnancy, lactation, lack of adequate methods of contraception in women of reproductive age;
• age to 18 years;
• liver diseases that occur in the active phase, including a persistent increase in the activity of transaminases in serum and any increase in the serum activity of transaminases ≥ 3 times compared with IGN (upper boundary of the norm);
• Myopathy and predisposition to the occurrence of myotoxic complications;
• kidney failure: for a dose of 5, 10, 15 or 20 mg per day - in severe form (creatinine clearance less than 30 ml / min); for a dose of 40 mg per day - moderate severity (creatinine clearance less than 60 ml / moment);
• combined therapy with cyclosporine;
• individual hypersensitivity to rosuvastatin or any auxiliary component of the drug.

Additional absolute contraindications for the use of rosuvastatin in a dose of 40 mg are the following risk factors in which rhabdomyolysis and / or myopathy is possible:

• conditions in which the plasma concentration of rosuvastatin may increase;
• anamnesis of muscular diseases (familial including);
• hypothyroidism;
• myotoxicity on the background of taking other fibrates or inhibitors of HMG-CoA reductase in anamnesis;
• alcohol abuse;
• simultaneous application of fibrates;
• belonging to the Mongoloid race.

Relative (diseases / conditions, the presence of which requires caution when applying Rosuvastatin):

• liver disease in history;
• arterial hypotension;
• sepsis;
• metabolic, water-electrolyte or endocrine disorders in severe form or uncontrolled convulsive seizures;
• extensive surgical interventions;
• injuries;
• age over 65 years;
• presence of risk factors for rhabdomyolysis / myopathy: hypothyroidism, renal dysfunction, personal / family history of muscle disease, a previous history of muscle toxicity with other fibrates or statins;
• conditions in which an increase in the concentration of rosuvastatin in the blood plasma is possible;
• renal failure of mild severity (creatinine clearance more than 60 ml / min);
• excessive use of alcohol;
• simultaneous application with fibrates;
• belonging to the Mongoloid race.

Intended use for pregnancy and lactation

Rosuvastatin and other statins are contraindicated in pregnancy. There is evidence that this medicine negatively affects the development of the fetus, increases the risk of deviations in newborns. Women of reproductive age who take statins should carefully use effective methods of contraception.

If there was an unplanned pregnancy, the taking of tablets from cholesterol is immediately stopped. It is not recommended to breast-feed during the treatment with this medication.

Dosage and route of administration

As indicated in the instructions for use Rosewastatin taken inside, do not chew and do not grind the tablet, swallow whole, squeezed with water. The drug can be administered at any time of the day, regardless of the time of meal.

Before starting therapy with Rosuvastatin, the patient should begin to follow the standard hypocholesterolemic diet and continue to observe it during treatment. The dose of the drug should be selected individually, depending on the purpose of therapy and the therapeutic response to treatment, taking into account current recommendations for target lipid concentrations.

• The recommended initial dose for patients starting to take the drug, or for patients transferred with the administration of other inhibitors of HMG-CoA reductase, should be 5 or 10 mg of the drug Rosuvastatin 1 once / day. When choosing the initial dose should be guided by the individual content of cholesterol and take into account possible risk of cardiovascular complications, and it is also necessary to assess the potential risk of adverse effects. If necessary, the dose may be increased to greater after 4 weeks (see. section "Pharmacodynamics").
• In connection with the possible development of side effects when taking a dose of 40 mg, compared with lower doses of the drug (see. section "Side effect"), increasing the dose to 40 mg, after additional dose intake above the recommended initial dose for 4 weeks of therapy, can be performed only in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) who did not achieve the desired result of therapy with a 20 mg dose and who will be monitored specialist (see section "Special instructions"). It is recommended especially careful monitoring of patients receiving the drug in a dose of 40 mg.

Do not administer a dose of 40 mg to patients who have not previously consulted a doctor. After 2-4 weeks of therapy and / or with an increase in the dose of the drug, rosuvastatin requires monitoring of lipid metabolism (if necessary, dose adjustment is required). The use of the drug in a higher dose than 40 mg is not justified due to the increased side effects and in most cases is not recommended.

1. In the case of creatinine clearance of 30-60 ml / min, rosuvastatin is given in an initial dose of 5 mg. The use of the drug in a daily dose of 40 mg is contraindicated. Patients with creatinine clearance less than 30 ml / min, as well as in cases of liver disease in the active phase, the drug is not prescribed.
2. The recommended initial dose for patients of the Mongoloid race is 5 mg. In a dose of 40 mg the drug is not prescribed for this group of patients.
3. Patients with carriers of genotypes p.521SS or p.421AA the recommended maximum daily dose of rosuvastatin is 20 mg.
4. In cases of predisposition to the development of myopathy, the recommended initial dose is 5 mg, the maximum - 20 mg.
5. When prescribing combination therapy, it is necessary to evaluate the likelihood of myopathy.

Side effect

Disturbances observed during therapy are usually dose-dependent and not expressed and pass independently.

Possible side reactions (> 10% - very often;> 1% and <10% - often;>,% and <1% - infrequently;>, 1% and

• urinary system: proteinuria (usually decreases / passes during treatment and is not a sign of the onset or progression of existing kidney disease);
• laboratory indicators: increased concentrations of bilirubin, glucose, activity of gamma-glutamyltranspeptidase, alkaline phosphatase, functional thyroid disorders;
• endocrine system: often - type 2 diabetes mellitus;
• immune system: rarely - angioedema and other hypersensitivity reactions;
• central nervous system: often - dizziness, headache;
• musculoskeletal system: often - myalgia; rarely - rhabdomyolysis, myopathy, incl. myositis (when the activity of creatine phosphokinase increases more than 5-fold, the use of rosuvastatin is suspended);
• system of digestion: often - nausea, constipation, pain in the abdomen; rarely - pancreatitis;
• skin: infrequent - rash, itching, hives;
• liver: increased activity of hepatic transaminases (usually is dose-dependent, minor, asymptomatic and temporary);
• other reactions: often - asthenic syndrome.

Violations revealed during post-registration studies:

• reproductive system and mammary gland: with an unidentified frequency - gynecomastia;
• respiratory system: with an unidentified frequency - dyspnea, cough;
• hematopoiesis system: with an unidentified frequency - thrombocytopenia;
• digestive system: very rarely - hepatitis, jaundice; rarely - increased activity of hepatic transaminases; with an unidentified frequency - diarrhea;
• musculoskeletal system: very rarely - arthralgia; with an unidentified frequency - immuno-mediated necrotizing myopathy;
• urinary system: very rarely - hematuria;
• central nervous system: very rarely - decrease / loss of memory; with an unidentified frequency - peripheral neuropathy;
• skin and subcutaneous fat: at an unidentified frequency - Stevens-Johnson syndrome;
• others: with an unidentified frequency - peripheral edema.

Some statins reported the following adverse reactions: sexual dysfunction, depression, hyperglycemia, sleep disturbance, including nightmares and insomnia, increased concentrations of glycosylated hemoglobin. There is a single information on the development of interstitial lung disease, especially when carrying out prolonged treatment.

Overdose

With the simultaneous administration of several daily doses, the symptoms of overdose do not develop, as the pharmacokinetics of the active component of the rosuvastatin tablets remains at the same level. With a more severe overdose, symptoms of side effects appear or increase.

In such cases, gastric lavage, intestinal sorbents, and symptomatic therapy are performed. There is no specific antidote.

special instructions

Patients taking Rosuvastatin at a dose of 40 mg should be monitored for indicators of kidney function.

When determining the activity of CKK, in order to avoid misinterpretation of the results, an analysis after significant physical exertion, and also consider other possible causes of increase in the level of CK. If the initial concentration is significantly increased (5 times or more in comparison with the upper limit of the norm), repeat analysis should be carried out after 5-7 days. When confirming the initial elevated level of concentration of CK as a result of repeated measurement, therapy with rosuvastatin should not be started.

In case of presence of factors of probability of development of rhabdomyolysis, it is necessary to take into account the ratio of benefit and possible risk and during the whole course of therapy to carry out clinical monitoring of the condition patient.

The patient should immediately inform the doctor of the unexpected appearance of muscle pains, spasms or muscle weakness. In such patients, it is necessary to check the activity of CK. If the level of concentration of CK is significantly increased (5 times or more in comparison with the upper limit of the norm) or if muscular symptoms are pronounced even with a slight deviation of CPK activity from normal, therapy is necessary to cease. After the disappearance of the symptoms and the return of the activity of CPK to normal, a reappointment is possible Rosuvastatin or other inhibitors of HMG-CoA reductase, but in smaller doses and under careful medical observation. In the absence of symptoms, it is not practical to measure the activity of CK.

When taking rosuvastatin and concomitant treatment, signs of increased effects on skeletal muscle were not detected. However, there have been reports of an increase in the incidence of myopathy and myositis in patients taking other HMG-CoA reductase inhibitors concomitantly with fibrin acid derivatives, including nicotinic acid in lipid-lowering doses, cyclosporine, gemfibrozil, macrolide antibiotics, protease inhibitors and azole antifungal means.

Combined use of gemfibrozil and rosuvastatin is not recommended, as gemfibrozil increases the likelihood of myopathy in combination therapy with certain HMG-CoA reductase inhibitors. It is necessary to take into account the risk / benefit ratio when using nicotinic acid or fibrates at the same time in lipid lowering doses and Rosuvastatin.

It is recommended to monitor the liver function before starting therapy and after 3 months of treatment with the drug.

If the serum level of transaminase activity exceeds 3 times the VGN, the drug should be discontinued.

In patients with hypercholesterolemia due to nephrotic syndrome or hypothyroidism, treatment of major diseases should be performed prior to the initiation of Rosuvastatin.

If there is a suspicion of LLE, which manifests itself in the form of an unproductive cough, shortness of breath, weight loss, weakness, deterioration in overall well-being and fever, taking the drug should be discarded.

Because of the possible likelihood of developing seizures during taking Rosuvastatin tablets, you should avoid eating green tea.

With violations of liver function

The use of the drug in a daily dose of 5 mg, 10 mg, 20 mg and 40 mg to patients with liver diseases in the active phase, including a persistent increase in serum the activity of transaminases and any increase in the activity of transaminases in the blood serum (more than 3 times compared with the upper limit of the norm) it is contraindicated.

With caution apply the drug in a daily dose of 5 mg, 10 mg, 20 mg and 40 mg to patients with liver disease in the history.

In case of violations of kidney function

The use of the drug in a daily dose of 5 mg, 10 mg and 20 mg in patients with severe renal dysfunction (CC less than 30 ml / min) is contraindicated.

The use of the drug in a daily dose of 40 mg to patients with moderate-level renal insufficiency (CC less than 60 ml / min) is contraindicated

With caution apply the drug in a daily dose of 5 mg, 10 mg and 20 mg in patients with renal insufficiency.

With caution apply the drug in a daily dose of 40 mg to patients with renal insufficiency of low severity (CC greater than 60 ml / min).

Patients with moderate impairment of renal function are recommended an initial dose of 5 mg.

Interaction with other drugs

Rosuvastatin can be taken along with certain medications with which other statins can not be taken.

But still, most cases of negative drug interactions with the appearance of IV IV statins have not disappeared. Possible problems with certain pills from pressure, cardiac arrhythmia, antibiotics, immunosuppressants and many other medicines. This can cause severe side effects - violations of the liver and kidneys.

Carefully study the instructions for use of the drug that you have been prescribed. Discuss with the doctor! Inform the doctor about all medicines, dietary supplements and herbs that you take.

Reviews

We offer you to read reviews of people who used the drug Rosuvastatin:

1. Sasha. I prescribed a therapist rosuvastatin 1 tab once a night. Began to drink and very strange heart began to beat. Somehow, with heavy overloads, it seems like the motor is working with difficulty. She stopped drinking and those strange palpitations stopped. read the instructions where it says. that m b. reactions of the cardiovascular system. It was necessary to not drink yet And how now to lower a level of a cholesterin at itself?
2. Elizabeth. As far as I know, rosuvastatin analogues, even if not very expensive, have the same effect, so I buy rosuvastatin-cz. It may take a very long time, so the price is of great importance. and the result after the application is excellent - cholesterol decreased to,.
3. Novel. I take an analogue of this drug, it is called Rosuvastatin-SZ. The cardiologist has long since written it out, to prevent a heart attack, with the task of lowering cholesterol, he coped well, for six months reduced from, to,. Often they write about side effects, but personally I did not have anything like that, I feel normal.

Analogues

There are a number of drugs that have exactly the same active substance as rosuvastatin, and therefore can be used as alternatives. However, before using them, it is absolutely recommended that you consult your doctor.

These alternatives include:

• Mertenil;
• Rosewood;
• Rosart;
• Rosulip;
• Roxer;
• Tevastor;
• Akorta;
• The Cross;
• Rosistark.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Store in a dark place at a temperature of up to 25 ° C. Keep away from children.

Shelf life - 2 years.

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