Cardiostatin, tablets 20 mg, 30 pcs.
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Hypolipidemic agent, disrupts early stages of cholesterol synthesis in the liver (at the stage of levanic acid).
In the body it forms free beta-hydroxy acid, which competitively inhibits Z-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) and disrupts its conversion into mevalonate, resulting in reduced cholesterol synthesis and increased catabolism.
Reduces the blood content of very low density lipoproteins, low density lipoproteins and triglycerides, moderately increases high density lipoproteins.
Significantly reduces the amount of apoprotein B (part of low-density lipoproteins) and other circulating components of low-density lipoproteins.
The pronounced therapeutic effect is manifested within 2 weeks, and the maximum effect – after 4-6 weeks from the start of treatment.
Pharmacokinetics
In the gastrointestinal tract is absorbed slowly and not completely – about 30% of the taken dose, intake on an empty stomach reduces absorption by 30%.
Maximal concentration (7,8 ng/ml for lovastatin and 11,9 ng/ml for beta-hydroxyacid) in plasma is noted within 2-4 hours, then plasma level decreases rapidly, being 10% of maximal level in 24 hours.
Blood plasma protein binding is 95%. Clearance of lovastatin and its active metabolites in case of a single administration at night is achieved on 2-3 days of therapy and is 1.5 times higher than after single administration.
Passes through the blood-brain barrier and the placental barrier.
It is metabolized intensively during the “first passage” through the liver and is oxidized to beta-hydroxy acid, its 6-oxy derivative and other metabolites, some of which are pharmacologically active (block Z-hydroxy-3-methylglutaryl coenzyme A reductase).
CYP3A4, CYP3A5 and CYP3A7 isoenzymes are involved in metabolism of the drug.
Half-life – 3 hours. Excreted through the intestine – 83%, by the kidneys – 10%.
Indications
- Primary hypercholesterolemia (heterozygous familial and nonfamilial types IIa, IIb and mixed), combined hypercholesterolemia and hypertriglyceridemia (with ineffective diet therapy in patients with high risk of coronary atherosclerosis).
- Ischemic heart disease: prevention of myocardial infarction, reducing the risk of unstable angina, treatment of atherosclerosis.
Active ingredient
Lovastatin
How to take, the dosage
Oral, with meals, in hypercholesterolemia the initial dose is 10-20 mg once a day, in the evening, in atherosclerosis – 20-40 mg/day. If necessary the dose is increased every four weeks.
The maximum daily dose is 80 mg in 1 or 2 doses (during breakfast and dinner).
In case the plasma concentration of total cholesterol decreases to 140 mg/100ml (3.6 mmol/L) or low-density lipoproteins to 75 mg/100ml (1.94 mmol/L), the dose should be reduced.
In concomitant administration with drugs that suppress immunity, as well as in severe chronic renal failure (creatinine clearance less than 30 ml/min) the daily dose should not exceed 20 mg (the recommended dose is 10 mg/day).
Interaction
Immunosuppressants, fibrates (gemfibrozil), nicotinic acid (more than 1 g/day), cyclosporine, erythromycin, azole antifungals (itraconazole and others) increase the risk of rhabdomyolysis, myopathy, acute renal failure.
It increases the effect of indirect anticoagulants and risk of bleeding. Regular control of prothrombin time is necessary.
Colestiramine and colestipol decrease bioavailability (use of lovastatin is possible 2-4 hours after taking the mentioned drugs, herewith an additive effect is noted).
Cyclosporine increases plasma concentration of lovastatin metabolites. Consumption of grapefruit juice in large quantities increases the concentration of the drug in blood plasma, therefore simultaneous use is not recommended.
Special Instructions
Patients should be warned that in case of unexplained muscle pain, soreness and muscle weakness (especially in combination with fever), they should consult a doctor.
During treatment, patients should be on a standard low-cholesterol diet.
In the case of steady increase of liver transaminases and/or CPK in blood the drug is indicated cancellation.
Therapy should be interrupted for a long time or discontinued in the generally severe condition of the patient due to a disease.
In long-term therapy a biochemical control of liver function is indicated. Hepatic transaminase activity is determined before the treatment start and every 8 weeks during the first year of therapy, further – at least once every six months.
Patients with daily drug dose of 80 mg should be examined once every three months.
If the activity of “hepatic” transaminases increases, the study should be repeated and conducted more frequently thereafter.
If liver transaminases levels increase, especially when exceeding 3 times the upper limit of normal, the drug should be stopped.
If the current dose is missed, the drug should be taken as soon as possible. If it is time for the next dose, the dose should not be increased.
Contraindications
Hypersensitivity to the drug (to any of the drug components, including hereditary lactose intolerance), as well as to other HMG-CoA reductase inhibitors in the history, liver disease in the acute phase.
Increase of liver transaminases activity (of unknown etiology) more than 3 times, general severe state of a patient, pregnancy, lactation, age up to 18 years old (safety and efficacy of use are not established).
With caution
In case of liver diseases (in anamnesis), alcohol abuse, after organ transplantation, concomitant immunosuppressive therapy, chronic renal insufficiency (creatinine clearance less than 30 ml/min).),
urgent surgical manipulations (including dental), while concomitant use with gemfibrozil and other fibrates, nicotinic acid (more than 1 g/day) due to the risk of myopathy.
Side effects
Digestive system: heartburn, nausea, diarrhea or constipation, flatulence, abdominal pain, dry mouth, taste disorders, decreased appetite, cholestatic jaundice, liver function disorders, increased activity of liver transaminases, hepatitis, acute pancreatitis.
Central nervous system: dizziness, headache, general weakness, seizures, insomnia, paresthesias, mental disorders
Musculoskeletal system: Myalgia, myositis, myopathy, rhabdomyolysis (in patients receiving simultaneously cyclosporine, gemfibrozil or nicotinic acid (more than 1 g/day)), arthralgia.
Blood organs: hemolytic anemia, leukopenia, thrombocytopenia.
Senses: blurred vision, blurred lens, cataract, optic atrophy.
Laboratory parameters: increased activity of hepatic transaminases, increased creatine phosphokinase (CPK), alkaline phosphatase, bilirubin, eosinophilia, accelerated sedimentation, positive test for antinuclear antibodies.
Allergic reactions: urticaria, angioneurotic edema, toxic epidermal necrolysis (Lyell’s syndrome), skin itching, rash.
Other: decreased potency, acute renal failure (due to rhabdomyolysis), chest pain, palpitations.
Overdose
The company has no information about the symptoms of overdose.
Pregnancy use
It is contraindicated. Breastfeeding should be stopped during treatment.
Weight | 0.017 kg |
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Shelf life | 2 years |
Conditions of storage | In a dry, dark place at temperatures from 12 ° C to 15 ° C Keep out of reach of children. |
Manufacturer | Chemopharm LLC, Russia |
Medication form | pills |
Brand | Chemopharm LLC |
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