Cardiolipus pills 5mg, 30pcs

Composition

One film-coated tablet contains:

Active ingredient:

rosuvastatin calcium in terms of rosuvastatin 5,00 mg;

excipients:

microcrystalline cellulose,

pregelatinized starch,

colloidal silicon dioxide (aerosil),

magnesium stearate;

tablet shell:

opadray II pink (polyvinyl alcohol, titanium dioxide, macrogol (polyethylene glycol), talc, carmine red dye (E120)).

Pharmacological action

Cardiolip is a lipid-lowering drug, a selective competitive inhibitor of HMG-CoA reductase.

It is effective in adult patients with hypercholesterolemia, with or without hypertriglyceridemia (regardless of race, gender, or age), including those with diabetes mellitus and familial hypercholesterolemia.

The additive effect is observed in combination with fenofibrate (with respect to reducing the concentration of TG) and nicotinic acid in lipid-lowering doses (with respect to reducing the concentration of HDL-C).

Indications

-Primary Fredricksen hypercholesterolemia (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb) as a dietary supplement when diet and other non-drug treatments (exercise, weight loss) are insufficient.

– Familial homozygous hypercholesterolemia as an adjunct to diet and other lipid-lowering therapy (for example, LDL apheresis), or in cases where such therapy is not effective enough.

– Hypertriglyceridemia (type IV according to Fredriksen) as a dietary supplement.

– To slow the progression of atherosclerosis as an adjunct to diet in patients who are indicated for therapy to reduce the concentration of total cholesterol and LDL-C.

– Primary prevention of major cardiovascular complications (stroke, myocardial infarction, arterial revascularization) in adult patients without clinical signs of coronary heart disease, but with an increased risk of its development (the age of 50 years for men and over 60 years for women, the increased concentration of C-reactive protein (more than 2 mg/l) in the presence of at least one additional risk factors such as arterial hypertension, a low concentration of HDL-C, Smoking, family history of early CHD).

Contraindications

• Hypersensitivity to rosuvastatin or to any component of the drug;
• liver disease in the active phase, including a persistent increase in serum transaminases and any increase of transaminases in blood serum (more than 3 times compared with the upper limit of normal);
• severe renal dysfunction (creatinine clearance (CC) of less than 30 ml/min);
• myopathy;
• concomitant use of cyclosporine;
• in women: pregnancy, lactation, lack of adequate methods of contraception;
• patients predisposed to the development of myotoxicity complications;
• children up to age 18 years.

With caution:

Risk of developing myopathy/rhabdomyolysis – renal failure, hypothyroidism, personal or family history of inherited muscle diseases and previous history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates; alcohol dependence; age over 65 years; conditions with increased plasma concentrations of rosuvastatin; race (Asian race-Japanese and Chinese); concomitant use with fibrates; liver diseases in the presence of a drug that is not recommended for use with other HMG – CoA reductase inhibitors or fibrates. medical history; sepsis; hypotension; extensive surgery, trauma, severe metabolic, endocrine, or electrolyte disturbances, or uncontrolled seizures.

Patients with hepatic insufficiency: there are no data or experience of using the drug in patients with a score higher than 9 on the Child-Pugh scale.

Use during pregnancy and lactation: Rosuvastatin is contraindicated during pregnancy and lactation. Since cholesterol and substances synthesized from cholesterol are important for fetal development, the potential risk of HMG-CoA reductase inhibition exceeds the benefit of using the drug during pregnancy.

If pregnancy is diagnosed during therapy, the drug should be discontinued immediately.

Women of reproductive age should use adequate methods of contraception.

Side effects

From the central nervous system: often-headache, dizziness, asthenic syndrome; very rarely-polyneuropathy, memory loss.

From the digestive system: often-constipation, nausea, abdominal pain; rarely-pancreatitis; very rarely-jaundice, hepatitis; unspecified frequency-diarrhea.

From the respiratory system: unspecified frequency-cough, shortness of breath.

From the musculoskeletal system: often-myalgia; rarely-myopathy (including myositis), rhabdomyolysis with or without acute renal failure; very rarely – arthralgia.

From the urinary system: proteinuria (less than 1% of cases-for doses of 10 mg and 20 mg,3% of cases – for a dose of 40 mg); unspecified frequency-peripheral edema; very rarely-hematuria.

Endocrine system disorders: type 2 diabetes mellitus.

Allergic reactions: rarely-hypersensitivity reactions, including angioedema; infrequently-pruritus, rash, urticaria; unspecified frequency-Stevens-Johnson syndrome.

Laboratory parameters: transient dose-dependent increase in creatine phosphokinase (CPK) activity (with an increase in CPK activity by more than 5 times compared to the upper limit of normal, therapy should be temporarily suspended); reversible transient dose-dependent increase in the activity of “hepatic” transaminases; increased concentration of glucose, bilirubin, activity of gamma-glutamyltranspeptidase, alkaline phosphatase, changes in the level of thyroid hormones.

The following side effects have been reported with some HMG-CoA reductase inhibitors (statins): depression, sleep disorders, including insomnia and ‘nightmarish’ dreams, sexual dysfunction. Isolated cases of interstitial lung disease have been reported, especially with long-term drug use.

With simultaneous use of several daily doses, the pharmacokinetic parameters of rosuvastatin do not change. Treatment of overdose is symptomatic, monitoring of liver function and CPK activity is necessary; there is no specific antidote, and hemodialysis is ineffective.

Interaction

of Cyclosporine: with simultaneous use of Cardiolip and cyclosporine, the AUC of rosuvastatin is on average 7 times higher than that observed in healthy volunteers. Combined use with rosuvastatin leads to an 11-fold increase in Cmax in blood plasma. It does not affect the plasma concentration of cyclosporine.

Vitamin K antagonists: starting rosuvastatin therapy or increasing the dose of the drug in patients receiving concomitant vitamin K antagonists (for example, warfarin) may lead to an increase in prothrombin time (International Normalized Ratio – INR). Discontinuation of rosuvastatin or reduction of the dose of the drug may lead to a decrease in INR (monitoring of INR is recommended).

Gemfibrozil and other lipid-lowering agents: the combined use of rosuvastatin and gemfibrozil leads to a 2-fold increase in the Cmax and AUC of rosuvastatin. Based on specific interaction data, no pharmacokinetically significant interaction with fenofibrates is expected, and a pharmacodynamic interaction is possible.

Gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses of nicotinic acid (high doses or equivalent to 1 g per day) increase the risk of myopathy when used concomitantly with HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy and when used in monotherapy. When taking the drug simultaneously with gemfibrozil, fibrates, nicotinic acid in a dose of more than 1 g / day, patients are recommended an initial dose of 5 mg (1/2 tablets of 10 mg).

Ezetimibe: concomitant use of rosuvastatin and ezetimibe was not associated with changes in the AUC and Cmax of both drugs.

HIV protease inhibitors: Although the exact mechanism of interaction is unknown, co-use of HIV protease inhibitors can lead to a significant increase in rosuvastatin exposure. Therefore, simultaneous use of rosuvastatin and HIV protease inhibitors in the treatment of patients with human immunodeficiency virus (HIV) is not recommended.

Antacids: concomitant use of rosuvastatin and antacid suspensions containing aluminum and magnesium hydroxide leads to a decrease in the plasma concentration of rosuvastatin by approximately 50%. This effect is less pronounced if antacids are applied 2 hours after taking rosuvastatin. The clinical significance of this interaction has not been studied.

Erythromycin: concomitant use of rosuvastatin and erythromycin leads to a decrease in rosuvastatin AUC by 20% and Cmax by 30%. This interaction may occur as a result of increased intestinal motility caused by taking erythromycin.

Oral contraceptives / hormone replacement therapy: concomitant use of rosuvastatin and oral contraceptives increases the AUC of ethinyl estradiol and AUC of norgestrel by 26% and 34%, respectively. Such an increase in plasma concentration should be taken into account when selecting the dose of oral contraceptives. Pharmacokinetic data on the simultaneous use of rosuvastatin and hormone replacement therapy are not available, therefore, a similar effect cannot be excluded with the use of this combination.

Other medications: No clinically significant interaction of rosuvastatin with digoxin is expected.

Cytochrome P 450: In vivo and in vitro studies have shown that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P 450 isoenzymes. In addition, rosuvastatin is a non-core substrate for these isoenzymes. There was no clinically significant interaction between rosuvastatin and fluconazole and ketoconazole. Co-use of rosuvastatin and itraconazole increases the AUC of rosuvastatin by 28% (clinically insignificant). Thus, no interaction associated with metabolism by the cytochrome P450 system is expected.

How to take, course of use and dosage

The drug is taken orally. The tablet should not be chewed or crushed, swallowed whole, washed down with a sufficient amount of water, it can be taken at any time of the day, regardless of food intake. If you need to take the drug at a dose of 5 mg, you should divide the tablet with a dosage of 10 mg.

Before starting Cardiolip therapy, the patient should start following a standard hypocholesterolemic diet and continue to follow it during treatment. The dose of the drug should be selected individually, depending on the goals of therapy and the therapeutic response to treatment, taking into account current recommendations for target lipid levels.

The recommended starting dose for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, should be 5 mg (1/2 tablets of 10 mg) or 10 mg of the drug 1 time per day.

With simultaneous use of Cardiolip with gemfibrozil, fibrates, nicotinic acid in a dose of more than 1 g/day, the recommended initial dose of the drug is 5 mg (1/2 tablets of 10 mg).

When choosing the initial dose, the individual cholesterol level should be guided and the possible risk of cardiovascular complications should be taken into account, as well as the potential risk of side effects should be evaluated. If necessary, the dose can be increased to a larger one after 4 weeks.

Due to the possible development of side effects when taking a dose of 40 mg, compared with lower doses of the drug, an increase in the dose to 40 mg, after an additional dose above the recommended initial dose for 4 weeks of therapy, can only be carried out in patients with severe hypercholesterolemia and at high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia), Especially careful monitoring of patients receiving the drug at a dose of 40 mg is recommended.

It is not recommended to use a dose of 40 mg in patients who have not previously consulted a doctor. After 2-4 weeks of therapy and/or when increasing the dose of the drug, it is necessary to monitor the parameters of lipid metabolism (if necessary, dose adjustment is required).

Elderly patients: no dose adjustment is required.

No dose adjustment is required in patients with mild or moderate renal insufficiency. It is contraindicated to use all dosages of the drug in patients with severe renal insufficiency (creatinine clearance less than 30 ml / min). It is contraindicated to use the drug at a dose of 40 mg in patients with moderate renal impairment (creatinine clearance less than 60 ml / min). In patients with moderate renal impairment, an initial dose of 5 mg (1/2 tablet of 10 mg) is recommended.

Patients with hepatic insufficiency: rosuvastatin is contraindicated in patients with active liver disease. There is no experience of using the drug in patients with hepatic insufficiency above 9 on the Child-Pugh scale.

Special populations

When studying the pharmacokinetic parameters of rosuvastatin in patients belonging to different ethnic groups, an increase in the systemic concentration of rosuvastatin among Japanese and Chinese was noted. This fact should be taken into account when using Rosuvastatin in this group of patients. When using doses of 10 mg and 20 mg, the recommended starting dose for Asian patients is 5 mg (1/2 tablets of 10 mg). It is contraindicated to use the drug at a dose of 40 mg in patients of Asian race.

Patients predisposed to myopathy

It is contraindicated to use the drug at a dose of 40 mg in patients with factors indicating a predisposition to the development of myopathy. When using doses of 10 mg and 20 mg, the recommended initial dose for this group of patients is 5 mg (1/2 tablets of 10 mg).

When used with gemfibrozil, the dose of the drug should not exceed 10 mg / day.

Special instructions

Before starting therapy and throughout the entire treatment period, a standard lipid-lowering diet should be observed. During treatment, the lipid profile should be monitored every 2-4 weeks and the dose adjusted accordingly, if necessary.

Short-term proteinuria may occur when rosuvastatin is used at all doses, and especially at a dose exceeding 20 mg. In patients taking the drug at a dose of 40 mg, it is recommended to monitor the indicators of renal function.

Patients taking rosuvastatin at a dose exceeding 20 mg may experience myalgia, myopathy, and rarely rhabdomyolysis. Determination of CPK activity should not be performed after intense physical activity or in the presence of other possible causes of increased CPK, which may lead to misinterpretation of the results obtained. If the CPK increases 5 times above the upper limit of normal, a second measurement should be performed after 5-7 days. Do not start therapy if a repeated test confirms the initial increased activity of CPK by more than 5 times compared to the upper limit of normal.

In patients at risk of developing myopathy/rhabdomyolysis, the risk-benefit ratio of therapy should be considered and clinical monitoring should be carried out throughout the course of treatment.

The patient should be informed of the need for immediate notification to the doctor in cases of unexpected occurrence of muscle pain, muscle weakness or spasms, especially in combination with malaise and fever. CPK activity should be monitored in these patients. Therapy should be discontinued if CKD activity is more than 5 times higher than the upper limit of normal, or if muscle symptoms are severe and cause daily discomfort (even if CKD activity is 5 times lower than the upper limit of normal). If symptoms disappear and CKD activity returns to normal, repeated use of the drug or other HMG-CoA reductase inhibitors in smaller doses should be considered under close medical supervision. Routine monitoring of CPK in the absence of symptoms of rhabdomyolysis is not advisable.

An increased incidence of myositis and myopathy has been reported in patients treated with other HMG-CoA reductase inhibitors in combination with fibrinic acid derivatives, including gemfibrozil, cyclosporine, nicotinic acid in lipid-lowering doses, azole antifungal drugs, HIV protease inhibitors, and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when co-administered with certain HMG-CoA reductase inhibitors. Therefore, concomitant use of rosuvastatin and gemfibrozil is not recommended. The risk-benefit ratio of rosuvastatin and fibrates or nicotinic acid in lipid-lowering doses should be carefully weighed.

It is recommended to determine liver function indicators before the start of therapy and 3 months after the start of therapy. If the activity of “hepatic” transaminases in the blood serum is 3 times higher than the upper limit of normal, the dose of the drug should be reduced or discontinued.

If hypercholesterolemia is combined with hypothyroidism or nephrotic syndrome, treatment of the underlying diseases should be carried out before starting treatment with rosuvastatin.

There was an increase in the plasma concentration of rosuvastatin in Asian patients compared to Caucasian patients.

In patients with a blood glucose concentration of 5.6 to 6.9 mmol / L, rosuvastatin therapy was associated with an increased risk of developing type 2 diabetes mellitus.

Women of reproductive age should use adequate methods of contraception.

During the treatment period, dizziness and weakness may occur, so caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 2 years.

Active ingredient

Rosuvastatin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets