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. Today it is the newest medicine among all cholesterol pills. It belongs to the statins of the last IV generation.

The drug has 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 intestines, from 5 to 10% excreted naturally by the kidneys in the urine. The half-life of rosuvastatin is from 12 to 16 hours, depending on the dosage, and the therapeutic effect lasts for about 30 hours. The 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

You can buy by prescription.

Price

How much does rosuvastatin in pharmacies? The average price is at 350 rubles.

Composition and release form

The drug Rosuvastatin is made in the dosage form of a film-coated tablet 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 is Rosuvastatin.

Excipients:

  • corn starch;
  • magnesium stearate;
  • microcrystalline cellulose;
  • Povidone;
  • calcium hydrophosphate dihydrate.

The composition of the film shell:

  • selekoat 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 hypolipidemic agent, a selective competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, which is an enzyme that converts 3-hydroxy-3-methylglutarylCoA to its precursor XC (cholesterol) -mevalonate. The drug increases the number of LDL receptors (low density lipoproteins) on the surface of liver cells, resulting in increased catabolism and LDL uptake and inhibits the synthesis of VLDL (very low density lipoproteins). Ultimately, the total number of VLDL and LDL decreases.

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

The therapeutic effect of the drug develops during the first week after the start 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 is about 20%.

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

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

The pharmacokinetics of rozuvastatin is independent of the gender and age of the patient.

In people of the Mongoloid race, there is a twofold increase in the maximum plasma concentration of rosuvastatin and the AUC median (area under the concentration-time curve) compared with European patients; In Indians, the maximum plasma concentration and the median AUC increase 1.3 times; in representatives of the Negroid race, pharmacokinetic parameters are similar to those in Caucasians.

Mild or moderate renal failure does not significantly affect the concentration of rosuvastatin and its metabolite N-desmethylrozuvastatin. In severe renal insufficiency, the plasma concentration of rosuvastatin increases about three times, and N-desmethylrozuvastatin increases nine times. In patients with hemodialysis, the concentration of the active substance is about 50% higher.

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

Indications for use

For taking rozuvastatin tablets, there are several medical indications, which include:

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

Also, the drug is used to slow the development of atherosclerosis as a supplement to dietary recommendations.

Contraindications

Absolute:

  • lactase deficiency, lactose intolerance, or glucose-galactose malabsorption;
  • pregnancy, lactation, lack of adequate methods of contraception in women of reproductive age;
  • age up to 18 years;
  • liver diseases occurring in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity ≥ 3 times as compared with VGN (upper limit of normal);
  • myopathy and predisposition to the occurrence of myotoxic complications;
  • renal 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);
  • combination therapy with cyclosporine;
  • individual hypersensitivity to rosuvastatin or any auxiliary component of the drug.

Additional absolute contraindications for the use of Rosuvastatin at a dose of 40 mg are the following risk factors for the development of rhabdomyolysis and / or myopathy:

  • conditions in which the plasma concentration of rosuvastatin may increase;
  • history of muscular diseases (including family);
  • hypothyroidism;
  • myotoxicity in the presence of other fibrates or HMG-CoA reductase inhibitors in history;
  • alcohol abuse;
  • simultaneous use of fibrates;
  • belonging to the Mongoloid race.

Relative (diseases / conditions whose presence requires caution when using Rosuvastatin):

  • history of liver disease;
  • hypotension;
  • sepsis;
  • metabolic, water-electrolyte or endocrine disorders in severe form or uncontrolled seizures;
  • extensive surgical interventions;
  • injuries;
  • age over 65 years;
  • the presence of risk factors for rhabdomyolysis / myopathy: hypothyroidism, impaired renal function, personal / family history of muscular diseases, previous history of muscular toxicity with the use of other fibrates or statins;
  • conditions in which increased plasma concentrations of rosuvastatin are possible;
  • mild renal failure (creatinine clearance more than 60 ml / min);
  • excessive drinking;
  • simultaneous use with fibrates;
  • belonging to the Mongoloid race.

Appointment during pregnancy and lactation

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

If an unplanned pregnancy occurs, then cholesterol pills should be stopped immediately. It is not recommended to breastfeed during the period of treatment with this drug.

Dosage and method of use

As indicated in the instructions for use Rosuvastatin is taken orally, do not chew or crush the pill, swallow whole, washed down with water. The drug can be administered at any time of the day, regardless of the meal time.

Before initiating rozuvastatin therapy, the patient should begin to follow the standard cholesterol-lowering diet and continue to follow it during treatment. The dose of the drug should be chosen individually depending on the goals of therapy and the therapeutic response to treatment, taking into account the current recommendations on target lipid concentrations.

  • The recommended initial dose for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, should be 5 or 10 mg of Rosuvastatin 1 time per day. When choosing the initial dose, one should be guided by the individual cholesterol content and take into account the possible risk of cardiovascular complications, and the potential risk of side effects should be evaluated. If necessary, the dose can be increased to a maximum 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 Effects”), increasing the dose to 40 mg, after an additional dose of the dose above the recommended initial dose within 4 weeks treatment can only be carried out in patients with severe hypercholesterolemia and at high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired result of therapy when taking a dose of 20 mg t be under the supervision of a specialist (see. section "Special instructions"). Especially careful monitoring of patients receiving the drug at a dose of 40 mg is recommended.

It is not recommended to prescribe a dose of 40 mg to patients who have not previously visited a doctor. After 2-4 weeks of therapy and / or with an increase in the dose of the drug Rosuvastatin, control of lipid metabolism indices is necessary (dose adjustment is necessary if necessary). The use of the drug in a higher dose than 40 mg is not justified due to increased side effects and in most cases is not recommended.

  1. When creatinine clearance is 30-60 ml / min, Rosuvastatin is prescribed 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 the presence of liver disease in the active phase of the drug is not appointed.
  2. The recommended starting dose for patients with a Mongoloid race is 5 mg. At a dose of 40 mg, the drug is not prescribed to this group of patients.
  3. For patients with genotypes p.521CC 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 a combination therapy, it is necessary to assess the likelihood of myopathy.

Side effect

Violations observed during therapy are usually dose-dependent and unexpressed and pass independently.

Possible side reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely; if it is impossible to estimate the frequency of occurrence of violations - with Unknown frequency):

  • urinary system: proteinuria (usually decreases / passes during treatment and is not a sign of acute or progression of existing kidney disease);
  • laboratory indicators: an increase in the concentration of bilirubin, glucose, the activity of gamma-glutamyl transpeptidase, alkaline phosphatase, functional disorders of the thyroid gland;
  • endocrine system: often - type 2 diabetes;
  • immune system: rarely - angioedema and other hypersensitivity reactions;
  • central nervous system: often - dizziness, headache;
  • musculoskeletal system: often - myalgia; rarely - rhabdomyolysis, myopathy, including myositis (with an increase in the activity of creatine phosphokinase more than 5 times, the use of Rosuvastatin is suspended);
  • digestive system: often - nausea, constipation, pain in the abdomen; rarely - pancreatitis;
  • skin: infrequently - rash, pruritus, urticaria;
  • liver: increased activity of hepatic transaminases (usually dose-dependent, minor, asymptomatic and temporary);
  • other reactions: often - asthenic syndrome.

Violations identified during post-registration studies:

  • reproductive system and mammary gland: with unknown frequency - gynecomastia;
  • respiratory system: with an unspecified frequency - shortness of breath, cough;
  • hematopoietic system: with unknown frequency - thrombocytopenia;
  • digestive system: very rarely - hepatitis, jaundice; rarely, increased liver transaminase activity; with an unknown frequency - diarrhea;
  • musculoskeletal system: very rarely - arthralgia; with unknown frequency, immuno-mediated necrotizing myopathy;
  • urinary system: very rarely - hematuria;
  • central nervous system: very rarely - decrease / loss of memory; with unknown frequency - peripheral neuropathy;
  • integuments and subcutaneous fat: with an unknown frequency - Stevens-Johnson syndrome;
  • others: with unknown frequency - peripheral edema.

The following adverse reactions have been reported with some statins: sexual dysfunction, depression, hyperglycemia, sleep disturbances, including nightmares and insomnia, increased glycated hemoglobin concentration. There is isolated information about the development of interstitial lung disease, especially during long-term treatment.

Overdose

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

In such cases, gastric lavage, intestinal sorbents are taken, as well as symptomatic therapy. There is no specific antidote.

Special instructions

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

When determining the activity of CPK, in order to avoid misinterpretation of the results, analysis should not be carried out after considerable physical exertion, and other possible reasons for increasing the level of CPK should be taken into account. If the initial concentration is significantly increased (5 times or more in comparison with the upper limit of the norm), the repeated analysis should be carried out in 5-7 days. When confirming the initial elevated level of CPK concentration as a result of repeated measurement, Rosuvastatin should not be started on therapy.

In the case of the likelihood factors for the development of rhabdomyolysis, it is necessary to take into account the ratio of benefits and possible risks and to conduct clinical monitoring of the patient's condition throughout the entire course of therapy.

The patient should immediately inform the doctor about the unexpected appearance of muscle pain, spasms or muscle weakness. In such patients it is necessary to check the activity of CPK. If the level of CPK concentration is significantly elevated (5 times or more compared to the upper limit of the norm) or if the muscle symptoms are pronounced even with a slight deviation from the norm, the therapy should be stopped. After the disappearance of the symptoms and the return of the activity of CPK to normal, it is possible to reappoint Rosuvastatin or other HMG-CoA reductase inhibitors, but in smaller doses and under close medical supervision. In the absence of symptoms, it is impractical to measure CPK activity.

When taking Rosuvastatin and concomitant treatment, there were no signs of increased effects on skeletal muscles. However, there have been reports of an increase in cases of myopathy and myositis in patients who took other HMG-CoA reductase inhibitors simultaneously with fibrin acid derivatives, including nicotinic acid in lipid-lowering doses, cyclosporine, gemfibrozil, macrolide antibiotics, protease inhibitors and azole anti-fungi.

The combined use of gemfibrozil and rosuvastatin is not recommended, because gemfibrozil increases the likelihood of myopathy in combination therapy with some HMG-CoA reductase inhibitors. It is necessary to take into account the risk / benefit ratio with the simultaneous use of nicotinic acid or fibrate in lipid-lowering doses and Rosuvastatin.

Monitoring of liver function indicators is recommended before starting treatment and after 3 months of drug treatment.

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

In patients with hypercholesterolemia due to nephrotic syndrome or hypothyroidism, treatment of major diseases should be carried out before the start of Rosuvastatin.

If you suspect the occurrence of an ISL, which manifests itself in the form of unproductive cough, shortness of breath, weight loss, weakness, deterioration of general well-being and fever, taking the drug should be canceled.

Due to the possible likelihood of convulsions while taking rozuvastatin tablets, you should avoid eating green tea.

With abnormal liver function

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

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

In case of impaired renal function

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

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

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

To use the drug with caution in a daily dose of 40 mg in patients with low-grade renal insufficiency (CC more than 60 ml / min).

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

Interaction with other drugs

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

But most of the cases of negative drug interactions with the advent of statins IV generation did not disappear. There may be problems with some pills for pressure, cardiac arrhythmias, antibiotics, immunosuppressants, and many other medications. This can cause severe side effects - liver and kidney problems.

Carefully read the instructions for use of the drug that you have been prescribed. Talk with your doctor! Tell your doctor about all the medicines, dietary supplements and herbs that you take.

Reviews

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

  1. Sasha. I was prescribed by the therapist rosuvastatin 1 tab once a night. I began to drink and my heart began to beat very strangely. Somehow with heavy overloads as if the motor is working with difficulty. I stopped drinking and these strange heartbeats stopped. I read the instructions where it says. that m b. cardiovascular reactions. I had to drink for now. And how do you lower your cholesterol now?
  2. Elizabeth. As far as I know, rosuvastatin analogues, even not very expensive, have the same effect, so I buy rosuvastatin-sz. It may take a very long time, so the price is very important. and the result after applying is excellent - cholesterol dropped to 3.9.
  3. Novel. I accept an analogue of this drug, it is called Rosuvastatin-SZ. A cardiologist wrote him out a long time ago, to prevent a heart attack, he coped well with the task of lowering cholesterol, for six months he reduced from 7.9 to 5.5. Often they write about side effects, but personally I didn’t have anything like that, my state of health is normal.

Analogs

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

These alternatives include:

  • Merten;
  • Roscard;
  • Rosart;
  • Rosulip;
  • Roxera;
  • Tevastor;
  • Acorta;
  • Crestor;
  • Rosistark.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Store in a dark place at a temperature up to 25 ° C. Keep out of the reach of children.

Shelf life - 2 years.

Watch the video: The Side Effects of Statins (November 2019).

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