Description
Latin name
MERTENIL
Release form
Coated tablets.
Packaging
In a blister pack of 10 tablets. There are 3 blisters in the package.
Pharmacological action of
Mertenil is a selective and competitive inhibitor of HMG-CoA reductase, an enzyme, converting 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, which is a precursor of cholesterol. The main target of the action of rosuvastatin is the liver, where the synthesis of cholesterol (cholesterol) and the catabolism of low density lipoproteins (LDL) are carried out.
Rosuvastatin increases the number of liver LDL receptors on the cell surface, increasing the uptake and catabolism of LDL. It also inhibits the synthesis of very low density lipoprotein cholesterol (VLDL) in the liver cells, thereby reducing the total content of LDL and VLDL. Rosuvastatin reduces high cholesterol – LDL (cholesterol-LDL), total cholesterol and triglycerides (TG), increases high-density lipoprotein cholesterol (cholesterol-HDL), and also lowers apolipoprotein B (ApoV), non-HDL cholesterol minus HDL cholesterol, CS-VLDLP, TG-VLDLP and increases the level of apolipoprotein A-1 (ApoA-1). Rosuvastatin reduces the ratio of LDL-C / HDL-C, total HDL-HDL, HDL-HDL / HDL and ApoV / ApoA-1.
The therapeutic effect can be achieved and within one week after the start of treatment, after 2 weeks 90% of the maximum possible effect is achieved. Usually, the maximum possible therapeutic effect is achieved after 4 weeks and is maintained with further administration of the drug.
Rosuvastatin is effective in baking adult patients with hypercholesterolemia with or without symptoms of hypertriglyceridemia, regardless of race, gender or age, as well as in the treatment of a special category of patients with diabetes mellitus or a hereditary form of familial hypercholesterolemia. Rosuvastatin is effective for the treatment of patients with type IIa and IIb hypercholesterolemia according to Frederickson (average baseline LDL-C level okopo 4.8 mmol / l).
In 80% of patients receiving 10 mg of rosuvastatin, the target levels of LDL-C established by the European Society for the Study of Atherosclerosis (less than 3 mmol / l) were achieved. In patients with heterozygous familial hypercholesterolemia who took rosuvastatin in doses of 20 to 80 mg according to the forced dose titration scheme, all doses taken had a significant effect on changing the parameters characterizing the lipid content and on achieving the goal of therapy.
As a result of titration of doses up to 40 mg per day (12 weeks of therapy), the content of LDL-C decreased by 53%. In 33% of patients, LDL-C was achieved (below 3 mmol / l), relevant guidelines of the guidelines of the European Society for the Study of Atherosclerosis. In patients with homozygous familial hypercholesterolemia who took rosuvastatin in doses of 20 and 40 mg, the average decrease in LDL-C was 22%. An additive effect is observed in combination with fenofibrate in relation to the content of TG and with nicotinic acid (more than 1 g per day) in relation to the content of HDL-C.
Research on the effect of rosuvastatin on reducing the number of complications caused by lipid disorders, such as coronary artery disease, has not yet been completed. In patients with a low risk of coronary heart disease (defined as a Framingham risk of less than 10% over a period of more than 10 years), with an average LDL-C content of 4.0 mmol / L (154, 5 mg / dl) rosuvastatin at a dose of 40 mg / day significantly slowed down the increase in the maximum value characterizing the thickening of the carotid artery wall in 12 segments, compared with placebo at a rate of -0.0145 mm / year (95% confidence interval: from – 0.0196 to 0.0093, with p
Indications
– Hypercholesterolemia and combined (mixed) dyslipidemic conditions to reduce high total cholesterol, low-density lipoprotein cholesterol, serum apo-lipoprotein B and triglycerides in blood serum as a supplement to diet therapy, when diet and other non-drug methods (such as exercise, weight loss) are insufficient.
– Family homozygous hypercholesterolemia as an adjunct to diet therapy and other lipid-lowering therapy (eg, LDL apheresis) or in cases where such therapy is not effective enough.
Contraindications
– Hypersensitivity to rosuvastatin or any of the components of the drug.
– Liver diseases in the active phase, including a persistent increase in the activity of liver transaminases, as well as any increase in the activity of transaminases in blood serum by more than 3 times compared with the upper limit of normal.
– Severe renal impairment (QC less than 30 ml / minute).
– Myopathy.
– Concomitant use of cyclosporine.
– In patients predisposed to the development of myotoxic complications.
– Pregnancy.
– Lactation.
– In women of childbearing age, not using reliable contraceptives.
– Age under 18 years of age (efficacy and safety not established).
– Patients with liver failure with a score of greater than 9 on the Childe-Pugh scale.
– Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Precautions:
– Risk of developing myopathy / rhabdomyolysis, including: – Renal failure.
– Hypothyroidism.
– A personal or family history of hereditary muscle disease and a previous history of muscle toxicity with other HMG-CoA reductase inhibitors or fibrates.
Use during pregnancy and lactation
Mertenil is contraindicated in pregnancy and lactation. Women of childbearing age should use reliable and adequate contraceptives.
Since cholesterol and cholesterol biosynthesis products are important for fetal development, the potential risk of inhibiting HMG-CoA reductase exceeds the benefits of its use in pregnancy. In case of pregnancy, the drug should be stopped immediately.
There are no data on the excretion of the drug with breast milk. If necessary, the appointment of the drug during lactation, breastfeeding must be stopped.
Composition
In 1 film-coated tablet, contains: rosuvastatin calcium 5.2 mg., which corresponds to the content of rosuvastatin 5 mg.
Excipients:
microcrystalline cellulose 12,
lactose monohydrate,
magnesium hydroxide,
crospovidone (type A),
magnesium stearate.
Composition of the film coat:
opadray II white (talc, macrogol-3350, titanium dioxide (E171), polyvinyl alcohol).
Dosage and administration of
Before starting treatment, the patient should follow a standard diet with low cholesterol products, which should be continued during the entire period of treatment. Doses of the drug should be selected individually in accordance with the purpose of the treatment and the patient’s therapeutic response to the therapy, taking into account current generally accepted recommendations for target lipid levels.
Inside, at any time of the day, regardless of food intake, do not chew or grind, swallow whole, washed down with water.
The recommended initial dose of the drug is 5 mg or 10 mg 1 time per day for patients who have not previously taken statins, and for patients transferred to receive this drug after treatment with other HMG-CoA reductase inhibitors. Choosing the initial dose of the drug, you should take into account the level of cholesterol in each individual patient, as well as the possible risk of developing cardiovascular complications and the potential risk of side effects. If necessary, after 4 weeks you can make a dose adjustment.
For patients older than 70 years, the recommended initial dose of the drug is 5 mg. Dose adjustment due to age is not required.
In patients with mild or moderate renal failure, dose adjustment is not required. The recommended initial dose of the drug is 5 mg for patients with moderate renal failure (CC less than 60 ml / minute). The appointment of Mertenil in any dose is contraindicated in patients with severe renal failure.
No increase in systemic concentration of rosuvastatin in patients with a Child-Pugh score of 7 or lower was not detected. However, an increase in systemic drug concentration was observed in patients with Child-Pugh scores of 8 and 9. In such patients, liver function should be monitored during therapy. There are no data on the administration of the drug by patients with a Child-Pugh score higher than 9. Patients with liver disease 8 active phase Mertenil is contraindicated.
In patients of the Asian race, an increase in the systemic concentration of rosuvastatin is possible. When prescribing doses of 10 and 20 mg, the recommended initial dose of the drug for patients of Asian origin is 5 mg.
When prescribing doses of 10 and 20 mg, the recommended initial dose of the drug for patients with a predisposition to myopathy is 5 mg. The use of the drug in a dose of 40 mg is contraindicated in such patients.
Side effects of
As with other HMG-CoA reductase inhibitors, the incidence of side effects is dose-dependent.
The incidence of rhabdomyolysis, severe side effects from the kidneys and liver increases in patients taking rosuvastatin at a dose of 40 mg.
From the urinary system: when taking rosuvastatin, proteinuria was observed, mainly of tubular origin. Changes in protein in the urine (from the absence or presence of trace amounts to the level of ++ and above) were found in less than 1% of patients taking rosuvastatin in doses of 10 mg and 20 mg, and in about 3% of patients taking the drug in a dose of 40 mg .
The minimum change in the amount of protein in the urine, expressed as a change from zero level or the presence of traces to level +, was observed when taking the drug at a dose of 20 mg. In most cases, proteinuria decreased and passed independently during treatment. An analysis of clinical trial data did not reveal a causal relationship between proteinuria and acute or progressive kidney disease. In a number of patients treated with rosuvastatin, hematuria was observed, but clinical trial data showed that the incidence of such cases is very low.
From the musculoskeletal system: the effect on skeletal muscle causing myalgia, myopathy (including myositis) and, in rare cases, rhabdomyolysis with or without the development of acute renal failure, was observed in patients taking any dose of rosuvastatin, especially a dose of more than 20 mg. An increase in the content of CPK depending on the dose taken was found in patients taking rosuvastatin, but in most cases these manifestations were minor, asymptomatic and temporary. If the content of CPK is 5 times higher than VGN, then treatment should be discontinued.
From the liver: as with other HMG-CoA reductase inhibitors, an increase in hepatic transaminase activity depending on the dose was detected in a small number of patients taking rosuvastatin. Moreover, in most cases, this increase was moderately pronounced, asymptomatic and transient.
On the part of laboratory indicators: an increase in the concentration of glucose, bilirubin, the activity of GGT, alkaline phosphatase, impaired thyroid function.
Post-marketing use of
From the digestive system: very rarely – jaundice, hepatitis rarely – increased activity of hepatic transaminases, unspecified frequency – diarrhea.
From the musculoskeletal system: very rarely – arthralgia.
From the nervous system: very rarely – polyneuropathy, memory loss.
From the respiratory system: unspecified frequency – cough, shortness of breath.
From the urinary system: very rarely – hematuria.
Dermatological reactions: unspecified frequency – Stevens-Johnson syndrome.
Other: unspecified frequency – peripheral edema.
The following side effects have been reported with some statins: depression, sleep disturbances, including insomnia and nightmares, sexual dysfunction. Isolated cases of interstitial lung disease have been reported, especially with prolonged use of drugs.
Overdose
Symptoms: increased side effects.
Treatment: There is no specific treatment for overdose. In case of overdose, symptomatic treatment and supportive measures are recommended. Liver function and the degree of CPF activity should be monitored. Hemodialysis in this case is probably ineffective.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 30 ° C.
Expiration
2 years.
Deystvuyuschee substances
Rosuvastatin
pharmacy terms for prescription
dosage form
dosage form
tablets
Gedeon Richter Vengriya
