Simvageksal pills 40 mg 30 pcs
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Active ingredients
Simvastatin
Release form
Pills
Composition
1 tab. Simvastatin 40 mg. Excipients: starch, lactose monohydrate, microcrystalline cellulose, butylhydroxyanisol, ascorbic acid, citric acid monohydrate, magnesium stearate, hypromellose, talc, titanium dioxide, iron red oxide.
Pharmacological effect
The lipid-lowering drug obtained synthetically from the fermentation product Aspergillus terreus. Is inactive lactone, in the body undergoes cleavage to form a hydroxy acid derivative. The active metabolite inhibits HMG-CoA reductase - an enzyme that catalyzes the initial reaction of the formation of mevalonate from HMG-CoA. Since the transformation of HMG-CoA into mevalonat is an early stage of cholesterol synthesis, the use of simvastatin does not cause the accumulation of potentially toxic sterols in the body. HMG-CoA is easily metabolized to acetyl-HMG-CoA, which is involved in many processes of synthesis in the body. The drug causes a decrease in plasma levels of TG, LDL, VLDL and total cholesterol (CH) (in cases of heterozygous familial and non-familial forms of hypercholesterolemia, with mixed hyperlipidemia, when elevated cholesterol is a risk factor). Increases the content of HDL and reduces the ratio of LDL / HDL and total HCF / HDL. The beginning of the manifestation of the effect - after 2 weeks from the start of the reception, the maximum therapeutic effect is achieved after 4-6 weeks. The effect persists with continued treatment, with the termination of therapy, the cholesterol content gradually returns to its original level.
Pharmacokinetics
Absorption: Simvastatin absorption is high. After ingestion, Cmax in the blood plasma is reached in about 1.3-2.4 hours and decreases by about 90% in 12 hours. Distribution: Binding to plasma proteins is about 95%. Metabolism: Exposed to the “first pass” effect through the liver. Hydrolyzed to form the active derivative - beta-hydroxy acids; other active and inactive metabolites were also found. Withdrawal: T1 / 2 of the active metabolites is 1.9 h. Excreted mainly with feces (60%) as metabolites. About 10-15% is excreted by the kidneys in the form of inactive metabolites.
Indications
- primary hypercholesterolemia (type IIa and IIb according to Fredrickson's classification) with the ineffectiveness of dietary therapy with low cholesterol and other non-drug measures (exercise and weight loss) in patients with an increased risk of developing coronary atherosclerosis - combined hypercholesterolemia and hypertriglyceridemia, in case of non-fever, hyperglyceridemia, and in case of non-occurring arteriosclerosis and hypertriglyceridemia, who are not subject to death, who are not subject to death, and who are not exposed to nodal and arthrosclerosis and who are not subject to the risk of hypertension, and who are not subject to the risk of developing coronary atherosclerosis - combined hypercholesterolemia and hypertriglyceridemia will not be affected by the risk of developing coronary atherosclerosis. and physical activity - CHD: prevention of myocardial infarction (secondary prevention of myocardial infarction) in patients with elevated urinary hears cholesterol (> 5.5 mmol / l).
Contraindications
- liver failure, acute liver disease, persistent increase in liver transaminases of unknown etiology - porphyria - myopathy - simultaneous administration of ketoconazole, itraconazole, drugs for treating HIV infection - hypersensitivity to the components of the drug - hypersensitivity to other statin drugs (HMG inhibitors CoA reductase) in history. Precautions should be prescribed to patients with chronic alcoholism after organ transplantation, which are treated with immunosuppressants (due to an increased risk of rhabdomyolysis and renal failure) in conditions that may lead to the development of severe renal failure, such as arterial hypertension, acute infectious diseases severe, severe metabolic and endocrine disorders, water and electrolyte imbalance, surgical interventions (including dental) or trauma patients with reduced or elevated skeletal muscle tone of unclear etiology in epilepsy and adolescents under 18 years of age (safety and efficacy have not been established).
Use during pregnancy and lactation
Simvagexal should not be prescribed during pregnancy. There are several reports of the development of anomalies in newborns whose mothers took simvastatin. Due to the fact that HMG-CoA reductase inhibitors inhibit cholesterol synthesis, and cholesterin and other products of its synthesis play a significant role in the development of the fetus, including the synthesis of steroids and cell membranes, simvastatin can have an adverse effect on the fetus when prescribing it to pregnant women.Women of childbearing age who take simvastatin should avoid conception. If pregnancy is still in the process of taking the drug, it is necessary to stop taking Simvagexal, and the woman should be warned about the possible danger to the fetus. Data on the allocation of simvastatin with breast milk are not available. If necessary, the appointment of the drug Simvageksal women during breastfeeding should be aware that many drugs are excreted in breast milk, and there is a risk of severe reactions, so breastfeeding while taking the drug is not recommended.
Dosage and administration
Simvageksal should be taken orally 1 time / day in the evening, drinking plenty of water. When hypercholesterolemia, depending on the severity of the initial dose of the drug is 5-10 mg / day. The dose is determined on the basis of plasma cholesterol, which is determined at intervals of at least 4 weeks. The daily dose is usually 40 mg. With a lack of effectiveness and with the risk of the cardiovascular system, a dose increase of up to a maximum of 80 mg / day is allowed. In IHD, the initial dose is 20 mg / day. If necessary, gradually increase the dose every 4 weeks to 40 mg. If the content of LDL is less than 75 mg / dl (1.94 mmol / l), and the total cholesterol content is less than 140 mg / dl (3.6 mmol / l), the dose of the drug should be reduced. For patients with chronic renal failure (CK less than 30 ml / min) or taking simultaneously cyclosporine, fibrates or nicotinamide, the initial dose is 5 mg, and the maximum daily dose is 10 mg. On the background of immunosuppressive therapy, the recommended initial daily dose is 5 mg, the maximum daily dose is 5 mg. The duration of the drug is determined by the attending physician individually.
Side effects
On the part of the digestive system: possible abdominal pain, constipation, flatulence, nausea, diarrhea, dyspepsia, pancreatitis, vomiting, hepatitis, increased activity of hepatic transaminases, alkaline phosphatase and CK. On the part of the central nervous system and peripheral nervous system: asthenic syndrome, headache, dizziness, insomnia, paresthesia, peripheral neuropathy, blurred vision, impaired taste sensations are possible.On the part of the musculoskeletal system: possible myopathy, myalgia, muscle cramps, weakness; rarely - rhabdomyolysis. Allergic reactions: rarely - angioedema, rheumatic polymyalgia, vasculitis, thrombocytopenia, increased ESR, fever, arthritis, urticaria, skin hyperemia, eosinophilia. Dermatological reactions: skin rash, itching, alopecia, photosensitivity. Other: possible "hot flashes", shortness of breath, lupus-like syndrome, anemia, palpitations, acute renal failure (due to rhabdomyolysis), decreased potency.
Overdose
None of the known cases of overdose (maximum dose of 450 mg) revealed any specific symptoms. Treatment: should induce vomiting, take activated charcoal; Symptomatic therapy is indicated. It should monitor the function of the liver and kidney, the content of CK in the serum.
Interaction with other drugs
Cytotoxic agents, antifungals (ketoconazole, itraconazole), fibrates, high doses of nicotinic acid, immunosuppressants, erythromycin, clarithromy, protease inhibitors, while using Simvagexal, increase the risk of developing rhabdomyolysis. Simvageksal enhances the action of oral anticoagulants (for example, fenprokumon, warfarin) and increases the risk of bleeding, which requires the need to monitor blood clotting before treatment and at regular time intervals. Simvageksal raises level of digoxin in a blood plasma. Kolestiramin and Kolestipol reduce the bioavailability of simvastatin. The use of Simvagexal is possible 4 hours after taking these drugs, with an additive effect.
special instructions
At the beginning of therapy with simvastatin, a transient increase in liver transaminase activity is possible. Before starting therapy and further, liver function tests should be carried out regularly (monitor liver transaminase activity every 6 weeks for the first 3 months, then every 8 weeks for the remaining first year, and then once a year), as well as increasing the dose liver function test. If you increase the dose to 80 mg, you need to test every 3 months.With a persistent increase in transaminase activity (3 times compared with the initial level), taking the drug Simvagexal should be stopped. Simvagexal, like other inhibitors of HMG-CoA reductase, should not be used with an increased risk of developing rhabdomyolysis and renal failure (against the background of severe acute infection, hypotension, planned major surgery, trauma, severe metabolic disorders). Cancellation of hypolipidemic drugs during pregnancy has no significant effect on the results of long-term treatment of primary hypercholesterolemia. In patients with reduced thyroid function (hypothyroidism) or in the presence of certain kidney diseases (nephrotic syndrome), with an increase in cholesterol level, the therapy underlying the disease should first be carried out. Patients should inform the doctor about any unusual symptoms from the musculoskeletal system. For timely diagnosis of myopathy, it is recommended to regularly measure CPK values. Simvagexal is prescribed with caution to patients who abuse alcohol and / or have a history of liver disease. Before and during treatment, the patient should be on a cholesterol diet. The simultaneous intake of grapefruit juice can increase the severity of adverse reactions associated with the administration of Simvagexal, therefore, their simultaneous administration should be avoided. In patients with myalgia, myasthenia and / or a pronounced increase in the activity of CPK, treatment with the drug is stopped. Simvagexal is not indicated for the treatment of hypertriglyceridemia type I, IV and V. Simvagexal is effective both in the form of monotherapy and in combination with sequestrants of bile acids. In case of missing the current dose, the drug should be taken as soon as possible. If it is time to take the next dose, do not double the dose. Patients with renal insufficiency severe treatment is carried out under the control of renal function. The duration of the drug is determined by the attending physician individually.