Cardiostatin - instructions for use, reviews, analogs and forms of release (20 mg and 40 mg tablets) drugs for the treatment of hypercholesterolemia, coronary atherosclerosis in adults, children and pregnancy. Composition and side effects

In this article, you can read the instructions for using the drug Cardiostatin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of cardiostatin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of cardiostatin in the presence of existing structural analogues.Use for the treatment of primary hypercholesterolemia, combined hypercholesterolemia and hypertriglyceridemia, coronary atherosclerosis in patients with IHD in adults, children, as well as during pregnancy and lactation. Composition of the drug and side effects when it is taken.

Cardiostatin - a hypolipidemic drug. Inhibitor of endogenous cholesterol synthesis. It breaks the early stages of cholesterol synthesis in the liver. In the body, lovastatin (the active substance of the drug Cardiostatin) forms a free beta hydroxy acid, which competitively inhibits 3-hydroxy-3-methylglutaryl coenzyme A-reductase (GMC-CoA reductase) and disrupts its conversion to mevalonate, resulting in reduced cholesterol synthesis and its catabolism increases.

Reduces the content of triglycerides, low density lipoproteins (LDL), very low density lipoproteins (VLDL) in blood plasma, moderately increases the high density lipoprotein (HDL) content. Significantly reduces the amount of apoprotein B, which is part of LDL, and other circulating components of LDL.

The expressed therapeutic effect of the drug is observed within 2 weeks of treatment, the maximum is achieved in 4-6 weeks from the start of treatment.

Cardiostatin is effective in primary hypercholesterolemia in patients with uncomplicated compensated type 1 and type 2 diabetes mellitus.

Composition

Lovastatin + excipients.

Pharmacokinetics

From the gastrointestinal tract (GIT) is absorbed slowly and not completely - about 30% of the dose taken, taking an empty stomach reduces absorption by 30%. The maximum concentration in the blood plasma is observed after 2-4 hours, then the level in the blood plasma rapidly decreases, making after 24 hours 10% of the maximum. Binding to blood plasma proteins - 95%. Penetrates through the blood-brain barrier (GEB) and the placental barrier.

It is subjected to intensive metabolism during the "first passage" through the liver, is oxidized to beta-hydroxy acid, its 6-hydroxy derivative and other metabolites, some of which are pharmacologically active (blocking 3-hydroxy-3-methylglutaryl coenzyme A-reductase). Output through the intestine - 83%, kidneys 10%.

Indications

• primary hypercholesterolemia (type 2a and 2b) with high LDL (not corrected by special diet and exercise);
• combined hypercholesterolemia and hypertriglyceridemia;
• coronary atherosclerosis in patients with IHD (in order to slow its progression).

Forms of release

Tablets of 20 mg and 40 mg.

Instructions for use and dosing regimen

The initial dose for hypercholesterolemia is 10-20 mg once a day, in the evening; when atherosclerosis - 20-40 mg per day. If necessary, increase the dose every 4 weeks. The maximum daily dose is 80 mg in 1 or 2 doses (during breakfast and dinner).

If the total cholesterol concentration in the plasma is reduced to 140 mg / dL (3.6 mmol / L) or LDL to 75 mg / dL (1.94 mmol / L), the dose of cardiostatin should be reduced. For patients who are simultaneously receiving immunosuppressants, fibrates, nicotinamide, daily dose should not exceed 20 mg.

Patients with chronic renal insufficiency of severe degree (creatinine clearance less than 30 ml / min) should not be prescribed at a dose exceeding 20 mg per day.

The drug is taken orally during a meal. If the next dose is missed, the drug should be taken as soon as possible. If it's time for the next appointment, do not increase the dose.

Side effect

• heartburn, nausea;
• diarrhea, constipation;
• flatulence (bloating), abdominal pain;
• dry mouth;
• a taste disorder;
• anorexia (eating disorder);
• gastralgia (pain in the stomach);
• Cholestatic (as a result of violation of outflow of bile) jaundice;
• hepatitis (inflammation of the liver);
• acute pancreatitis (inflammation of the pancreas);
• increased activity of hepatic transaminases, alkaline phosphatase, increased levels of bilirubin;
• dizziness, headache;
• general weakness;
• insomnia;
• convulsions;
• paresthesia (numbness, tingling, crawling);
• mental disorders;
• "fog" before the eyes;
• opacity of the lens, cataract;
• atrophy of the optic nerve;
• Myalgia (pain in the muscles);
• myositis (inflammation of a muscle group);
• Myopathy (dystrophic changes in muscle fibers);
• rhabdomyolysis (extreme degree of myopathy) with simultaneous application with cyclosporine, gemfibrozil or nicotinic acid;
• arthralgia (joint pain);
• increased activity of CK (creatine phosphokinase);
• eosinophilia, increased ESR (erythrocyte sedimentation rate), positive analysis for antinuclear antibodies;
• hives;
• angioedema;
• toxic epidermal necrolysis;
• skin rash, itching;
• decreased potency;
• acute renal failure due to rhabdomyolysis;
• pain in the chest, palpitations.

Contraindications

• liver disease in acute phase;
• increased activity of hepatic transaminases of unclear etiology;
• the general severe condition of the patient;
• pregnancy;
• lactation period (breastfeeding);
• children and adolescents under 18;
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

The drug Cardiostatin is contraindicated in pregnancy and lactation.

Use in children

The drug is contraindicated in children and adolescents under 18 years. Safety and effectiveness of the drug in patients under the age of 18 years are not established.

special instructions

Patients should be warned that if there is unexplained muscle pain, muscle weakness, especially accompanied by fever, the doctor should be informed immediately.

In the case of a persistent increase in the activity of transaminases and / or CPA, the drug should be discontinued.

If the patient's general serious condition is due to a disease, discontinue therapy for a long time or cancel the drug.

During the treatment, patients should follow a standard diet with low cholesterol.

With prolonged therapy, biochemical control of liver function is indicated. The activity of hepatic transaminases is determined before the start of therapy, every 8 weeks during the first year of therapy, then - at least 1 time in six months. Patients who have a daily dose of 80 mg should be examined once every 3 months. When the activity of transaminases increases, the study should be repeated and subsequently carried out more often. Therapy should be discontinued if the activity of aspartate aminotransferase (AST) and / or alanine aminotransferase (ALT) is 3 times higher than the upper limit of the norm (VGN).

With caution appoint a drug for liver disease (in the anamnesis), with chronic alcoholism, organ transplantation, concomitant immunosuppressive therapy, chronic renal failure, during urgent surgical procedures (including dental), while taking gemfibrozil and other fibrates, nicotinamide ( more than 1 g per day) because of the risk of developing myopathy.

Drug Interactions

Simultaneous reception of immunosuppressants, gemfibrozil, nicotinic acid, cyclosporine, erythromycin, antifungal drugs from the azole group increases the risk of myopathy with rhabdomyolysis and acute renal failure.

Simultaneous reception of cardiostatin increases the anticoagulant effect of indirect anticoagulants and the risk of bleeding. In the case of joint intake, regular monitoring of prothrombin time is necessary.

Kolestyramin and colestipol reduce the bioavailability of lovastatin (the use of cardiostatin is possible 4 hours after the administration of these drugs, with an additive effect noted).

Cyclosporine with simultaneous application increases the plasma level of lovastatin metabolites.

Analogues of the drug Cardiostatin

Structural analogs for the active substance:

• Apexstatin;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Medostatin;
• Rovacor;
• Holletar.

Analogues for the pharmacological group (statins):

• Akorta;
• Aktalipid;
• Anistat;
• Apexstatin;
• Atherostat;
• Atokord;
• Atomax;
• Ator;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Vazilip;
• Vero-Simvastatin;
• Zocor;
• Zorstat;
• The Cross;
• Leskol;
• Lipobay;
• Lipon;
• Lipopraim;
• Lipostat;
• Lipofford;
• Liprimar;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Medostatin;
• Mertenil;
• Novostat;
• Ovenkor;
• Pravastatin;
• Reddistatin;
• Ro-statin;
• Rovacor;
• Rosystark;
• Rosuvastatin;
• Rosewood;
• Rosulip;
• Rozufast;
• Roxer;
• Simvakol;
• Simvale;
• Simvastatin;
• Simvastol;
• Symvor;
• Simgal;
• Simlo;
• Sinquard;
• Suvardio;
• Tevastor;
• Torvacard;
• Torvalip;
• Tulip;
• Holvasim;
• Holletar.

Response of a therapist

I administer statins to many of my patients with high cholesterol levels, with atherosclerosis of the heart vessels in IHD. But I specifically try not to use the drug Cardiostatin. Why? In my practice, there were enough cases when patients developed severe side reactions in the treatment of cardiostatin, namely Quincke's edema, mental disorders, a significant increase in the blood level of bilirubin and liver enzymes. Therefore, I try to choose and prescribe to my patients the analogues of Cardiostatin, which have proved to be the best side in terms of development of side effects.

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