Vasilip 20mg coated film pills N28
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Active ingredients
Simvastatin
Release form
Pills
Composition
Simvastatin 20 mg adjuvants: lactose monohydrate, pregelatinized starch, butylhydroxyanisol, anhydrous citric acid, ascorbic acid, corn starch, microcrystalline cellulose, magnesium stearate.
Pharmacological effect
Lipid-lowering drug. The active substance of Vasilip is simvastatin, the main effect of which is the reduction of total cholesterol (total Xc) and low-density lipoprotein cholesterol (Xc-LDL) in plasma. It is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid (early stage of Xc synthesis). Simvastatin reduces the concentration of total Xc, Xc-LDL and triglycerides (TG). The content of Xc of very low density lipoproteins (Xc-VLDL) also decreases, while the content of Xc of high-density lipoproteins (Xc-HDL) increases moderately. Reduces the content of total Xc and LDL in cases of heterozygous familial and nonfamily forms of cholesterolemia, with mixed hyperlipidemia, when elevated levels of Xc are a risk factor. The drug reduces the level of total Xc and LDL-C in patients with coronary artery disease, reducing the risk of myocardial infarction and death for these patients. Simvastatin also significantly reduces the content of apolipoprotein B, moderately increases the concentration of HDL-C and LDL and reduces plasma concentrations of TH. As a result of these effects of simvastatin, the ratio of total Xc to total Xc-HDL and Xc-LDL to Xc-LPVN decreases. The anti-atherosclerotic effect of simvastatin is due to the effect of the drug on the walls of blood vessels and blood components. Simvastatin alters the metabolism of macrophages, inhibiting the activation of macrophages and the destruction of atherosclerotic plaques. The drug inhibits the synthesis of isoprenoids, which are growth factors in the proliferation of smooth muscle cells of the inner lining of blood vessels. Under the action of simvastatin, the endothelium-dependent expansion of blood vessels improves. The therapeutic effect occurs after 2 weeks, the maximum effect is observed after 4-6 weeks of treatment.
Pharmacokinetics
Absorption and distributionSimvastatin is presented in an inactive lactone form, which is relatively well absorbed (from 61% to 85%) from the gastrointestinal tract. Bioavailability - less than 5%. After ingestion, Cmax is reached after 1-2 hours and decreases by 90% after 12 hours. Simultaneous ingestion of food does not affect the absorbability of the drug. With long-term admission cumulation of the drug in the body does not occur. Plasma protein binding - 98%. MetabolismSimvastatin is a substrate of CYP3A4. Metabolized in the liver, exposed to the effect of the first passage through the liver (mainly hydrolyzed to its active form β-hydroxy acid). Excretion It is mainly excreted through the intestine (60%) as metabolites. About 13% is excreted by the kidneys in an inactive form. T1 / 2 is 1.9 h.
Indications
Hypercholesterolemia - primary hypercholesterolemia or mixed dyslipidemia (in addition to the diet and with the ineffectiveness of other non-drug interventions / exercise and weight loss); ). Prevention of cardiovascular diseases - reduction of cardiovascular mortality and morbidity in patients with clinical manifestations of atherosclerosis cally cardiovascular disease or diabetes, with normal or elevated cholesterol level, and as a further measure to correct other risk factors and cardioprotective therapy.
Contraindications
- liver disease in the active phase or persistent increase in liver transaminases of unknown etiology; - simultaneous administration of CYP3A4 isoenzyme inhibitors (for example, itraconazole, ketoconazole, HIV protease inhibitors, erythromycin, clarithromycin, telithromycin and nefazodone); ); - age up to 18 years (efficacy and safety of use have not been studied); - hypersensitivity to simvastatin and other components of the drug. With caution, you should prescribe the drug for abuse alcohol prior to treatment, a history of liver disease, severe electrolyte imbalance, severe endocrine and metabolic disorders, arterial hypotension, severe acute infections (sepsis), myopathy, uncontrolled epilepsy, extensive surgery, trauma, lactase deficiency, galactosemia or lactase syndrome, galactosemia or syndrome, galactosemia or lactase syndrome glucose galactose (becausethe drug contains lactose), concurrently with gemfibrosin, cyclosporine, nicotinic acid (more than 1 g / day), amiodarone, verapamil, diltiazem, fenofibrate, grapefruit juice.
Precautionary measures
Application for violations of liver functionWith caution, you should prescribe the drug for violations of the liver.It is not necessary to change the dose in case of renal dysfunction. The concentration of amplodipine in the blood plasma does not depend on the degree of reduction of renal function. Use in children It is contraindicated in children and adolescents under the age of 18. Application in elderly patients With caution in elderly patients.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy. An increase in the incidence of congenital malformations in children of women who took simvastatin or another HMG-CoA reductase inhibitor has not been proven. When pregnant women take simvastatin, they may decrease the levels of mevalonate in the fetus, which is the precursor of Xc biosynthesis. Cancellation of hypolipidemic drugs during pregnancy does not have a significant effect on the results of short-term risk associated with primary hypercholesterolemia. Simvastatin should not be used in pregnant women, women planning a pregnancy, or if a pregnancy is suspected. If a pregnancy occurs during the treatment, the drug should be canceled and the woman warned of possible danger to the fetus. During Vasilip treatment, women of reproductive age should use reliable contraceptives. It is not known whether the drug is excreted into breast milk, therefore therapy with Vasilip breastfeeding period is contraindicated.
Dosage and administration
Inside, once in the evening. The recommended dose of simvastatin varies from 5 mg to 80 mg 1 time per day in the evening. The most common initial dose of the drug is 10 mg. Changes (selection) of the dose should be carried out at intervals of at least 4 weeks. The maximum daily dose is 80 mg. The maximum daily dose is recommended only for patients with severe hypercholesterolemia or high risk of cardiovascular complications. The duration of the drug use is determined individually by the attending physician. Hypercholesterolemia The patient must follow a standard hypocholesterol diet throughout the entire period of treatment with Vasilip. The recommended initial dose for patients with hypercholesterolemia is 10 mg.In order to more pronounced decrease in the level of Xc-LDL (more than 45%), treatment can be started from 20-40 mg / day (once in the evening). In patients with homozygous hereditary hypercholesterolemia, the recommended daily dose of Vasilip is 40 mg in the evening or 80 mg in 3 doses (20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening); these patients should use Vasilip in combination with another lipid-lowering therapy (for example, LDL apheresis). Prevention of cardiovascular diseases In patients with a high risk of coronary heart disease, with or without hyperlipidemia, Vasilip is 20–40 mg / day. Therefore, the recommended initial dose in such patients is 20 mg / day. Changes (selection) of the dose should be carried out at intervals of 4 weeks, if necessary, the dose can be increased to 40 mg / day. If the content of LDL is less than 75 mg / dl (1.94 mmol / l), the total XC content is less than 140 mg / dl (3.6 mmol / l), the dose of the drug should be reduced. Concomitant therapy Vasilip is effective in monotherapy or in combination with bile acid sequestrants (for example , colestyramine and colestipol). In patients receiving treatment with cyclosporine, gemfibrozil, other fibrates or nicotinic acid (more than 1 g / day), the recommended initial dose of 5 mg, the maximum daily dose of Vasilip is 10 mg. A further dose increase in such situations is not recommended. In patients receiving amiodarone or verapamil at the same time, daily doses of Vasilip should not exceed 20 mg. In elderly patients and in patients with moderately severe renal insufficiency, the dosage of the drug is not required. In patients with severe renal failure (CC less than 30 ml / min), the recommended dose of Vasilip should not exceed 10 mg / day. If you need to increase the dose, it is necessary to carefully monitor such patients.
Side effects
Classification of the incidence of side effects (WHO): very often (> 1/10), often (from> 1/100 to <1/10), infrequently (from> 1/1000 to <1/100), rarely (from> 1/10 000 to <1/1000), very rarely (from <1/10 000), including separate messages. On the part of the digestive system: rarely - constipation, abdominal pain, flatulence, dyspepsia, nausea, vomiting, diarrhea, pancreatitis, hepatitis, jaundice, increased liver transaminases,SchF, KFK. From the central and peripheral nervous system and sensory organs: rarely - headache, paresthesia, dizziness, peripheral neuropathy, asthenia, insomnia, convulsions, blurred vision, impaired taste sensations. From the musculoskeletal system: rarely - myopathy , rhabdomyolysis, myalgia, muscle cramps. Allergic and immunopathological reactions: unfolded hypersensitivity syndrome (angioedema, lupus-like syndrome, rheumatic polymyalgia, dermatomyositis, vasculitis, tro bocytopenia, eosinophilia, increased ESR, arthritis, arthralgia, urticaria, photosensitization, fever, flushing of the skin of the face, shortness of breath and severe weakness). Dermatological reactions: rarely - skin rash, pruritus, alopecia. acute renal failure (due to rhabdomyolysis), reduced potency.
Overdose
There is evidence of several cases of overdose of simvastatin. The maximum accepted dose is 3.6 g. Treatment: in case of overdose, symptomatic treatment is carried out; It is necessary to carry out general activities: monitoring and maintaining vital functions, preventing further absorption of the drug (gastric lavage, taking activated carbon or laxatives). Monitoring liver function and CK is recommended. There is no specific antidote. When myopathy develops with rhabdomyolysis (a rare but severe side effect), you should immediately stop taking the drug, give the patient diuretic and sodium bicarbonate (intravenous infusion). Rhabdomyolysis can cause hyperkalemia, which can be eliminated by / in the administration of calcium chloride and calcium gluconate, by the infusion of glucose with insulin, by using potassium ion exchangers or, in severe cases, by hemodialysis.
Interaction with other drugs
Pharmacodynamic interactions Simultaneous use of simvastatin with fibrates, nicotinic acid (more than 1 g / day) increases the risk of myopathy, including rhabdomyolysis (when used with fenofibrate, there is no proven increase in the risk of myopathy compared to monotherapy with each drug separately). Simultaneous use with hemfibrozil may lead to an increase in serum simvastatin concentration. Pharmacokinetic interactions Cytochrome CYP3A4 inhibitors (itraconazole, ketoconazole, Erie tromycin, clarithromycin, telithromycin, HIV protease inhibitors and nefazodone),involved in the metabolic transformation of simvastatin in the liver, increase the risk of myopathy and rhabdomyolysis during therapy with simvastatin. Simultaneous use with these drugs is contraindicated. It is necessary to prescribe at the same time with less potent inhibitors of CYP3A4: cyclosporine, verapamil and diltiazem. The daily dose of simvastatin while taking it with cyclosporine should not exceed 10 mg. The daily dose of simvastatin on the background of simultaneous administration of amiodarone or verapamil should not exceed 20 mg, and 40 mg - on the background of simultaneous administration of diltiazem, unless the expected benefit clearly exceeds the potential risk of developing myopathy and rhabdomyolysis. Simvastatin at a dose of 20-40 mg / day volunteers and patients with hypercholesterolemia potentiates the effects of coumarin anticoagulants (for example, warfarin), in particular, an increase in prothrombin time, MHO. Therefore, in patients taking coumarin anticoagulants, prothrombin time and MHO must be determined before starting therapy with simvastatin, in the initial period of treatment, when changing the dose of simvastatin or discontinuation of the drug. When a stable indicator of prothrombin time and MHO is reached, further monitoring should be carried out at intervals recommended for patients receiving anticoagulant therapy. Simvastatin therapy does not cause changes in prothrombin time and risk of bleeding in patients not taking anticoagulants. Grapefruit juice inhibits CYP3A4 activity. The simultaneous intake of a large amount of grapefruit juice (more than 1 l per day) and simvastatin leads to a significant increase in plasma concentration of simvastatinic acid. Therefore, during therapy with simvastatin, grapefruit juice should be avoided.
special instructions
In patients with reduced thyroid function (hypothyroidism) or in the presence of certain kidney diseases (nephrotic syndrome), if the level of Xc is elevated, the underlying disease should be first treated. Patients with severe renal failure are treated with renal function. Treatment with simvastatin, as and other inhibitors of MMC-CoA reductase, can cause myopathy, sometimes leading to rhabdomyolysis with or without development of renal failure, due to myoglobinuria. The risk of myopathy increases with increasing doses of simvastatin and in patients with severe renal insufficiency.When treating with simvastatin, an increase in the serum CPK content is possible, which should be taken into account in the differential diagnosis of chest pain and after intense physical exertion. Before starting Vasilip therapy or increasing its dose, patients should be informed about the risk of myopathy and the need to immediately consult a doctor if unexplained pain, tension or weakness in the muscles, especially if this is accompanied by malaise or fever. The initial level of CPK before starting treatment should be determined in the following situations: - in elderly patients; - in kidney damage; - in decompensated hypothyroidism; - in aggravated family history of hereditary muscle diseases; - in the presence of toxic effects on the muscles of statins or fibrates; - in case of alcohol abuse. It is necessary to assess the possible risk and the expected benefit, and during therapy, clinical monitoring during therapy is recommended. If the initial level of CPK is significantly increased (more than 5 times relative to VGN), the measurement should be repeated after 5-7 days to confirm the results. With a significant initial increase in the level of CPK (more than 5 times relative to VGN), it is not recommended to prescribe the drug. Before and during the course of treatment, the patient must be on a hypocholesterol diet. . The criterion for the abolition of the drug is an increase in the content of CK in the serum of more than 5 times relative to VGN. If muscle symptoms are severe and cause discomfort, even with a CPK level of less than 5 times relative to VGN, you may need to stop treatment. If myopathy is suspected, the therapy should be discontinued, regardless of the cause of myopathy. If the symptoms disappear and the content of CPK returned to normal levels, it is possible to reappoint a statin or an alternative drug of the same class in the minimum clinically effective dose and under careful medical supervision. Vasilip therapy should be temporarily stopped several days before major surgical interventions. Patients with severe renal insufficiency are treated under the control of renal function. MeasuresReducing the risk of myopathy caused by drug interactions. The risk of myopathy and rhabdomyolysis increases significantly with the simultaneous use of simvastatin and powerful CYP3A4 inhibitors (for example, itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors, HIV, nephazodone), hemfibrozilol or nephazodone, hemfibrozilol or nephazodone, hemfibrozilol or nephazodone, hemfibrozilol or nephazodone, hemfibrozilol, tephithromycin, HIV protease inhibitors, nephazodone, hemfibrozilol, telithromycin, HIV proteases, nephazodone, hemfibrozil, or nephazodone inhibitors; The risk of myopathy and rhabdomyolysis also increases with the combined use of fibrates and high doses of nicotinic acid (more than 1 g / day) or with simultaneous therapy with amiodarone or verapamil with high doses of simvastatin. The risk also increases slightly with simultaneous administration of diltiazem and high doses of simvastatin (80 mg). Therefore, the use of simvastatin simultaneously with itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors and nefazodone is contraindicated. If it is impossible to refuse therapy with the listed CYP3A4 inhibitors, one should refrain from prescribing simvastatin. Simvastatin also needs to be carefully combined with some other, less potent inhibitors of CYP3A4: cyclosporine, verapamil and diltiazem. Simulastatin and grapefruit juice should be avoided at the same time. Patients taking cyclosporine, gemfibrozil or high doses of nicotinic acid (more than 1 g / day) The daily dose of simvastatin should not exceed 10 mg. Simultaneous prescription of simvastatin and gemfibrozil is possible only in cases where the expected benefit significantly exceeds the potential risk of tacos. th drug combination. The advantages of combined use of simvastatin 10 mg / day and other fibrates (except fenofibrate), nicotinic acid (more than 1 g / day) or cyclosporine should be carefully weighed, taking into account the potential risk of such combinations. There is a risk of myopathy when administered separately fenofibrate and simvastatin, therefore, caution is necessary when taking this combination at the same time. When taking simvastatin in doses exceeding 20 mg / day, it is necessary to avoid the simultaneous administration of amiodarone or verapamil, except in cases where the expected benefit outweighs the potential risk of myopathy. Effects on the liver Treatment with simvastatin can cause an increase in the activity of liver enzymes in blood serum. This increase is usually insignificant and clinically insignificant. After discontinuation of the drug, transaminase levels usually decrease slowly to baseline.However, before starting treatment and in the future, it is necessary to conduct a study of liver function (monitor the activity of hepatic transaminases every 6 weeks for the first 3 months, then every 8 weeks for the remaining first year, and then once every six months). If it is necessary to increase the dose to 80 mg, it is necessary to monitor liver function before increasing the dose, 3 months after the increase and then periodically (for example, 1 time in 6 months) during the first year of treatment. With a persistent increase in the activity of ACT and / or ALT in the serum by 3 times relative to VGN, treatment with simvastatin should be discontinued. With caution to appoint people who abuse alcohol and / or having a history of liver disease. Effect on ability to drive vehicles and control mechanisms About adverse effects of Vasilip on the ability to drive and work with mechanisms were not reported. Nevertheless, it should be noted that in the post-marketing use of simvastatin isolated cases of vertigo were noted.