Composition, structure and packing
Film-coated tablets, round, biconvex, beige.
Table 1.
simvastatin 10 mg.
"-" 20 mg.
"-" 40 mg.
Excipients: lactose monogidratnaya, MC; povidone, sodium croscarmellose, talc, ascorbic acid, citric acid; butilgidroksianizol, magnesium stearate.
Coverage: gipromelloza, titanium dioxide, macrogol, iron oxide yellow and iron oxide red
Pharmacological action
The drug has hypolipidemic, hypocholesterolemic. The body is hydrolyzed with the formation gidroksikislotnogo derivative - the main metabolite. Active metabolite inhibits HMG-CoA reductase, an enzyme that catalyzes the initial limiting speed, the stage of the biosynthesis of cholesterol. Lowers total cholesterol in plasma, LDL and VLDL.
Increases the content of HDL and reduces the ratio of LDL / HDL and total cholesterol / HDL, lowers plasma triglycerides. Active metabolite of simvastatin - a specific inhibitor of HMG-CoA reductase, an enzyme catalyzing the reaction of mevalonate from HMG-CoA. Since the conversion of HMG-CoA to mevalonate is an early stage of cholesterol biosynthesis, the use of simvastatin should not cause the accumulation in the body of potentially toxic sterols. HMG-CoA easily metabolized to acetyl-CoA, which is involved in many processes of biosynthesis in the body.
Pharmacokinetics
Absorption - high, has the effect of "first pass" through the liver. After oral administration, Cmax is achieved through 1,5-2,4 hours plasma protein binding - 90%. Metabolised in liver. Excreted in the bile. About 10% of output by the kidneys in an inactive form.
Statement
treatment of patients with hyperlipidemia, including primary hypercholesterolemia, heterozygous familial hypercholesterolemia or combined hyperlipidemia, when the therapeutic diet is inadequate;
treatment of patients with coronary heart disease for:
reduce the risk of death;
reduce the risk of coronary death, nonfatal myocardial infarction and transient ischemic states;
reduce the risk prior to the procedures for myocardial revascularization (coronary bypass and percutaneous transluminal coronary angioplasty);
reduce the progression of coronary atherosclerosis, including for reducing the development of new deposits and complete blockage of vessels;
treatment of patients with homozygous familial hypercholesterolemia.
Aktalipid used as an adjunct to primary therapy.
Dosage regimen
The drug is taken by mouth. Before starting treatment with Aktalipid patients should designate standard, poor cholesterol diet, which must be observed during treatment.
Hyperlipidemia. For weak or moderate hyperlipidemia treatment can begin with a dose of 5 mg (single administration in the evening). When expressed hyperlipidemia initial dose is 10 mg / day.
Increasing the dose can be no earlier than 4 weeks, gradually reaching a maximum of 80 mg / day, in a single dose in the evening. If the levels of LDL-cholesterol levels fall below 1,94 mmol / l (75 mg / dl) or total cholesterol levels - below 3.6 mmol / l (140 mg / dl), consult with your doctor about reducing the dose.
Homozygous familial hypercholesterolemia. The recommended daily dose - 40 mg in a single dose in the evening or 80 mg, divided into 3 - 20, 20 and 40 mg in the evening. Aktalipid should be used as a supplement to other, lipidoponizhayuschim drugs (LDL-afferez).
Coronary heart disease. The initial dose of -20 mg / day, once in the evening. If necessary, increase the dose every 4 weeks to 40 mg.
Combination therapy. Aktalipid effective as monotherapy and in combination. Patients receiving Aktalipid more years together with cyclosporine, fibrates or nicotinamide, should begin with a dose of 5 mg, the maximum daily dose is 10 mg 1 time per day.
Dose in renal impairment. In patients with severe renal impairment (Cl creatinine <30 ml / min) maximum daily dose is 10 mg. Aktalipid not apply in children
Side effect
The part of the digestive system:
abdominal pain, constipation, flatulence, nausea, diarrhea, dyspepsia, pancreatitis, vomiting, hepatitis, jaundice, increased activity of transaminases, alkaline phosphatase, gammaglutamintranspeptidazy.
Of the nervous system and sensory organs:
asthenia, dizziness, headache, peripheral neuropathy.
From the musculoskeletal system:
myalgia, myopathy, muscle cramps, paresthesia, rhabdomyolysis.
Allergic and immunological:
angioedema, lupus-like syndrome, polymyalgia rheumatica, vasculitis, thrombocytopenia, eosinophilia, ESR increase, arthritis, arthralgia, urticaria, photosensitivity, fever, flushing of the skin, flushing, malaise, shortness of breath.
Dermatological reactions: skin rash, itching, alopecia.
Other: anemia.
Contraindications
Hypersensitivity to the active or any of the excipients
hepatic failure,
increased activity of serum transaminases of unknown etiology,
pregnancy
period of breastfeeding,
simultaneous treatment mibefradilom (tetrazole type calcium antagonist)
Pregnancy and lactation
Do not use during pregnancy. If during pregnancy the treatment begins, then taking the drug abolished. Although data on the transition of the drug or its metabolites in breast milk no Aktalipid should not be used during breastfeeding.
Cautions
Effects on muscle. Aktalipid, like other inhibitors of HMG-CoA reductase may cause the appearance of myopathy, which manifests muscle pain or weakness associated with strong increase in creatine kinase (10 times above normal). Rhabdomyolysis with acute renal failure (as a result mioglobinurii) or without it described rarely.
Myopathy of drug interactions. The frequency and severity of myopathy is increased while receiving inhibitors of HMG-CoA reductase inhibitors with drugs that themselves cause myopathy, such as gemfibrozil and other fibrates or nicotinic acid in lipidoponizhayuschih doses (≥ 1 g / day).
Certain drugs, which at therapeutic doses are often significant depressing effect on cytochrome P450 3A4 saccharization can increase plasma levels of inhibitors of HMG-CoA reductase and increase the risk of myopathy. These drugs are cyclosporine, tetrazole calcium antagonist - mibefradil, intrakonazol and other azoles, erythromycin and antidepressant nefazodon. For each combination Aktalipida with other drugs should carefully evaluate the ratio of benefit / risk and monitor against the onset of patient symptoms such as headache, fatigue, soreness, especially during the first month of treatment and during dose changes. For patients receiving both Aktalipid with cyclosporine, fibrates or niacin, the dose Aktalipida not exceed 10 mg / day, as risk of myopathy increases with its increase. Aktalipid not apply simultaneously with mibefradilom.
Effects on liver
It is recommended to investigate liver function before starting treatment and then 2 times during the first year of treatment. Patients who take 80 mg / day, should be monitored 1 time in 3 months. Particular attention should be given to patients with elevated transaminases and more control over their condition. If the enzymes show a tendency to increase (up to 3 times higher than the upper limit of normal) or are resistant to change, treatment must stop. Patients who consume alcohol or have a history of liver disease, should carefully take the drug Aktalipid.
Active liver disease or increased transaminases of unknown etiology is a contraindication for treatment Aktalipidom.
The drug contains as an excipient lactose. Therefore, it is contraindicated in patients with lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome. The drug has no effect on the ability to drive a motor vehicle and work with mechanisms.
Drug Interactions
Combined admission Aktalipida and inhibitors of cytochrome P450 3A4 (cyclosporine, mibefradil, azolnye protivomikoticheskie means, including intrakonazol and ketoconazole, inhibitors of HIV protease, macrolides such as erythromycin and clarithromycin, an antidepressant nefazodon) should be started with caution. With greater caution applies combination with fibrates and niacin. It should avoid eating large quantities of grapefruit juice (more than 1 liter per day). Aktalipid potentiates the effect coumaric anticoagulants. Patients undertaking such therapy, the prothrombin time is necessary to determine prior to receiving Aktalipida and monitor frequently during therapy. This is necessary and when changing dosage Aktalipida.
Terms and Conditions of storage
Store at temperatures not above 25 ° C.
Shelf life 3 years.
Film-coated tablets, round, biconvex, beige.
Table 1.
simvastatin 10 mg.
"-" 20 mg.
"-" 40 mg.
Excipients: lactose monogidratnaya, MC; povidone, sodium croscarmellose, talc, ascorbic acid, citric acid; butilgidroksianizol, magnesium stearate.
Coverage: gipromelloza, titanium dioxide, macrogol, iron oxide yellow and iron oxide red
Pharmacological action
The drug has hypolipidemic, hypocholesterolemic. The body is hydrolyzed with the formation gidroksikislotnogo derivative - the main metabolite. Active metabolite inhibits HMG-CoA reductase, an enzyme that catalyzes the initial limiting speed, the stage of the biosynthesis of cholesterol. Lowers total cholesterol in plasma, LDL and VLDL.
Increases the content of HDL and reduces the ratio of LDL / HDL and total cholesterol / HDL, lowers plasma triglycerides. Active metabolite of simvastatin - a specific inhibitor of HMG-CoA reductase, an enzyme catalyzing the reaction of mevalonate from HMG-CoA. Since the conversion of HMG-CoA to mevalonate is an early stage of cholesterol biosynthesis, the use of simvastatin should not cause the accumulation in the body of potentially toxic sterols. HMG-CoA easily metabolized to acetyl-CoA, which is involved in many processes of biosynthesis in the body.
Pharmacokinetics
Absorption - high, has the effect of "first pass" through the liver. After oral administration, Cmax is achieved through 1,5-2,4 hours plasma protein binding - 90%. Metabolised in liver. Excreted in the bile. About 10% of output by the kidneys in an inactive form.
Statement
treatment of patients with hyperlipidemia, including primary hypercholesterolemia, heterozygous familial hypercholesterolemia or combined hyperlipidemia, when the therapeutic diet is inadequate;
treatment of patients with coronary heart disease for:
reduce the risk of death;
reduce the risk of coronary death, nonfatal myocardial infarction and transient ischemic states;
reduce the risk prior to the procedures for myocardial revascularization (coronary bypass and percutaneous transluminal coronary angioplasty);
reduce the progression of coronary atherosclerosis, including for reducing the development of new deposits and complete blockage of vessels;
treatment of patients with homozygous familial hypercholesterolemia.
Aktalipid used as an adjunct to primary therapy.
Dosage regimen
The drug is taken by mouth. Before starting treatment with Aktalipid patients should designate standard, poor cholesterol diet, which must be observed during treatment.
Hyperlipidemia. For weak or moderate hyperlipidemia treatment can begin with a dose of 5 mg (single administration in the evening). When expressed hyperlipidemia initial dose is 10 mg / day.
Increasing the dose can be no earlier than 4 weeks, gradually reaching a maximum of 80 mg / day, in a single dose in the evening. If the levels of LDL-cholesterol levels fall below 1,94 mmol / l (75 mg / dl) or total cholesterol levels - below 3.6 mmol / l (140 mg / dl), consult with your doctor about reducing the dose.
Homozygous familial hypercholesterolemia. The recommended daily dose - 40 mg in a single dose in the evening or 80 mg, divided into 3 - 20, 20 and 40 mg in the evening. Aktalipid should be used as a supplement to other, lipidoponizhayuschim drugs (LDL-afferez).
Coronary heart disease. The initial dose of -20 mg / day, once in the evening. If necessary, increase the dose every 4 weeks to 40 mg.
Combination therapy. Aktalipid effective as monotherapy and in combination. Patients receiving Aktalipid more years together with cyclosporine, fibrates or nicotinamide, should begin with a dose of 5 mg, the maximum daily dose is 10 mg 1 time per day.
Dose in renal impairment. In patients with severe renal impairment (Cl creatinine <30 ml / min) maximum daily dose is 10 mg. Aktalipid not apply in children
Side effect
The part of the digestive system:
abdominal pain, constipation, flatulence, nausea, diarrhea, dyspepsia, pancreatitis, vomiting, hepatitis, jaundice, increased activity of transaminases, alkaline phosphatase, gammaglutamintranspeptidazy.
Of the nervous system and sensory organs:
asthenia, dizziness, headache, peripheral neuropathy.
From the musculoskeletal system:
myalgia, myopathy, muscle cramps, paresthesia, rhabdomyolysis.
Allergic and immunological:
angioedema, lupus-like syndrome, polymyalgia rheumatica, vasculitis, thrombocytopenia, eosinophilia, ESR increase, arthritis, arthralgia, urticaria, photosensitivity, fever, flushing of the skin, flushing, malaise, shortness of breath.
Dermatological reactions: skin rash, itching, alopecia.
Other: anemia.
Contraindications
Hypersensitivity to the active or any of the excipients
hepatic failure,
increased activity of serum transaminases of unknown etiology,
pregnancy
period of breastfeeding,
simultaneous treatment mibefradilom (tetrazole type calcium antagonist)
Pregnancy and lactation
Do not use during pregnancy. If during pregnancy the treatment begins, then taking the drug abolished. Although data on the transition of the drug or its metabolites in breast milk no Aktalipid should not be used during breastfeeding.
Cautions
Effects on muscle. Aktalipid, like other inhibitors of HMG-CoA reductase may cause the appearance of myopathy, which manifests muscle pain or weakness associated with strong increase in creatine kinase (10 times above normal). Rhabdomyolysis with acute renal failure (as a result mioglobinurii) or without it described rarely.
Myopathy of drug interactions. The frequency and severity of myopathy is increased while receiving inhibitors of HMG-CoA reductase inhibitors with drugs that themselves cause myopathy, such as gemfibrozil and other fibrates or nicotinic acid in lipidoponizhayuschih doses (≥ 1 g / day).
Certain drugs, which at therapeutic doses are often significant depressing effect on cytochrome P450 3A4 saccharization can increase plasma levels of inhibitors of HMG-CoA reductase and increase the risk of myopathy. These drugs are cyclosporine, tetrazole calcium antagonist - mibefradil, intrakonazol and other azoles, erythromycin and antidepressant nefazodon. For each combination Aktalipida with other drugs should carefully evaluate the ratio of benefit / risk and monitor against the onset of patient symptoms such as headache, fatigue, soreness, especially during the first month of treatment and during dose changes. For patients receiving both Aktalipid with cyclosporine, fibrates or niacin, the dose Aktalipida not exceed 10 mg / day, as risk of myopathy increases with its increase. Aktalipid not apply simultaneously with mibefradilom.
Effects on liver
It is recommended to investigate liver function before starting treatment and then 2 times during the first year of treatment. Patients who take 80 mg / day, should be monitored 1 time in 3 months. Particular attention should be given to patients with elevated transaminases and more control over their condition. If the enzymes show a tendency to increase (up to 3 times higher than the upper limit of normal) or are resistant to change, treatment must stop. Patients who consume alcohol or have a history of liver disease, should carefully take the drug Aktalipid.
Active liver disease or increased transaminases of unknown etiology is a contraindication for treatment Aktalipidom.
The drug contains as an excipient lactose. Therefore, it is contraindicated in patients with lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome. The drug has no effect on the ability to drive a motor vehicle and work with mechanisms.
Drug Interactions
Combined admission Aktalipida and inhibitors of cytochrome P450 3A4 (cyclosporine, mibefradil, azolnye protivomikoticheskie means, including intrakonazol and ketoconazole, inhibitors of HIV protease, macrolides such as erythromycin and clarithromycin, an antidepressant nefazodon) should be started with caution. With greater caution applies combination with fibrates and niacin. It should avoid eating large quantities of grapefruit juice (more than 1 liter per day). Aktalipid potentiates the effect coumaric anticoagulants. Patients undertaking such therapy, the prothrombin time is necessary to determine prior to receiving Aktalipida and monitor frequently during therapy. This is necessary and when changing dosage Aktalipida.
Terms and Conditions of storage
Store at temperatures not above 25 ° C.
Shelf life 3 years.
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