Inegy pills 10 mg + 20 mg N28
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Active ingredients
Simvastatin + Ezetimibe
Release form
Pills
Composition
Ezetimibe 10 mg simvastatin 20 mg Auxiliary substances: lactose monohydrate, microcrystalline cellulose, hypromellose 2910 6 cps, croscarmellose sodium, citric acid monohydrate, butyl hydroxyanisol, propyl gallate, magnesium stearate.
Pharmacological effect
Pharmacodynamics Combined lipid-lowering drug that reduces the absorption of cholesterol and related plant sterols in the intestine, and also suppresses endogenous cholesterol synthesis. The drug contains ezetimibe and simvastatin, two lipid-lowering components that complement each other with their mechanism of action. Cholesterol enters the blood plasma as a result of intestinal absorption and endogenous synthesis. Inegy lowers elevated levels of total Xc, LDL, apolipoproteins B (Apo B), TG, and low density lipoproteins (non-HDL), and increases the level by double inhibition: absorption and cholesterol synthesis. Ezetimibe The mechanism of action of ezetimibe is different from other classes of hypolipidemic agents (for example, statins, bile acid sequestrants, fibrates). Ezetimibe, when it enters the small intestine, slows down the absorption of cholesterol, which leads to a decrease in cholesterol from the intestine to the liver. After 2 weeks of use, ezetimibe reduces cholesterol absorption in the intestine by 54% compared with placebo. A series of preclinical studies of ezetimibe confirms its selectivity in reducing cholesterol absorption. Ezetimibe slows down the absorption of 14C-cholesterol, and does not affect the absorption of TG, fatty acids, bile acids, progesterone, ethinyl estradiol, or fat-soluble vitamins A and D. derivative with high inhibitory activity against HMG-CoA reductase. This enzyme starts the initial and most significant stage of cholesterol biosynthesis - the conversion of HMG-CoA to mevalonate. Simvastatin reduces both elevated and normal levels of LDL. LDLs are formed from VLDL and are cleaved primarily by the use of a high affinity LDL receptor.A decrease in LDL after administration of simvastatin leads to a decrease in the content of VLDL and activation of LDL receptors, which leads to a decrease in the formation and enhancement of the catabolism of LDL. With simvastatin therapy, the level of ApoB also decreases. In addition, simvastatin moderately increases HDL levels and lowers plasma TG. As a result of these changes, the level of total cholesterol and LDL are reduced. Pharmacokinetics in special clinical situations. Children Pharmacokinetic data, absorption and metabolism of ezetimibe are the same in children / adolescents (10-18 years old) and adults. There is no data on the pharmacokinetics of the drug in children under 10 years of age. The clinical use of the drug in pediatric practice (in children and adolescents 9–17 years old) is limited to data on patients with homozygous familial hypercholesterolemia (GOSH) or homozygous sitosterolemia (hyper-apo-beta lipoproteinemia). Elderly patients In elderly patients (over 65 years old), total plasma ezetimibe concentration is approximately 2 times higher than in younger patients (18-45 years old). The level of LDL reduction and safety profiles in elderly and younger patients taking ezetimibe are about the same. Patients with hepatic insufficiency After a single dose of ezetimibe 10 mg, the average AUC for total ezetimibe was 1.7 higher in patients with mild hepatic insufficiency (5-6 points on the Child-Pugh scale) than in patients with preserved liver function. In a 14-day study of ezetimibe at a dose of 10 mg / day with the participation of patients with moderate hepatic insufficiency (7–9 points on the Child-Pugh scale), the average AUC for total ezetimibe increased 4 times on the 1st and 14th day compared with patients with preserved liver function. For patients with mild liver failure, dose adjustment is not required. Since the effects of increased concentrations of total ezetimibe are unknown, ezetimibe is not recommended for patients with moderate and severe (more than 9 points on the Child-Pugh scale) liver failure. Patients with renal failure Ezetimibe. After a single dose of 10 mg of ezetimibe, the average AUC in patients with severe renal insufficiency (average CC less than 30 ml / min / 1.73 m2) increased 1.5 times as compared with healthy patients. Simvastatin.In a study of patients with severe renal insufficiency (CC less than 30 ml / min), after administration of HMG-CoA reductase inhibitors, the total concentration of simvastatin metabolites was 2 times higher than in healthy volunteers. Gender The overall concentration of ezetimibe is slightly higher (20%) in women than in men. The level of LDL reduction and safety profiles are about the same for men and women taking ezetimibe.
Indications
Primary hypercholesterolemia: heterozygous (familial and non-familial) hypercholesterolemia or mixed hyperlipidemia (as a supplement to a diet to reduce total cholesterol, LDL, apolipoprotein B, TG, low density lipoprotein, to increase HDL). Homozygous familial hypercholesterolemia: to reduce elevated levels of total cholesterol and LDL (both as an additional treatment to other lipid-lowering therapy, for example, LDL-apheresis, and in its absence).
Contraindications
Hypersensitivity to the drug. liver disease in the active phase or a persistent increase in the activity of hepatic transaminases of unknown etiology. moderate and severe degree of liver failure (7 or more points on the Child-Pugh scale). pregnancy and lactation (breastfeeding). age up to 18 years. With caution: the drug should be used for severe renal failure (CC less than 30 ml / min), alcohol abuse, history of the liver, painful sensations in the muscles or changes in skeletal muscle tone of unknown etiology, gall bladder diseases with the simultaneous appointment of Inegy with fibrates.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breastfeeding).
Dosage and administration
Before initiating therapy with Inegy, patients should switch to a cholesterol-lowering diet and follow it throughout the entire course of treatment. The drug is administered orally 1 time / day, in the evening, regardless of the meal. The dose depends on the initial level of LDL, the purpose of treatment and the therapeutic effect and can vary from 10/10 mg (10 mg of ezetimibe + 10 mg of simvastatin) to 10/80 mg (10 mg of ezetimibe + 80 mg of simvastatin) per day. An initial dose of 10/20 mg (10 mg of ezetimibe + 20 mg of simvastatin) per day is usually recommended.In order to gradually reduce the level of LDL, a dose of 10/10 mg can be recommended (10 mg of ezetimibe + 10 mg of simvastatin). For a significant reduction in LDL (more than 55%), patients may be recommended an initial dose of 10/40 mg (10 mg of ezetimibe + 40 mg of simvastatin) per day. 2 weeks after the start of treatment, as well as throughout the course of treatment, lipid levels should be monitored and, if necessary, the dose of the drug should be adjusted. Primary hypercholesterolemia (heterozygous familial and non-familial hypercholesterolemia, mixed dyslipidemia) Inegy is recommended to be taken daily at a dose of 10/40 mg (10 mg of ezetimibe + 40 mg of simvastatin) or 10/80 mg (10 mg of ezetimibe + 80 mg of simvastatin) in the evening. Therapy should always be carried out against the backdrop of a cholesterol-lowering diet. To further reduce levels of TG and non-HDL and increase HDL in patients with mixed dyslipidemia, treatment with Inegy can be supplemented with fenofibrate. Injegi's homozygous familial hypercholesterolemia is recommended to be taken in a dose of 10/40 mg or 10/80 mg 1 time / day in the evening. The drug should be used in combination with another lipid-lowering therapy (for example, LDL-apheresis). In the absence of the possibility of additional treatment, Inegy can be prescribed as monotherapy. Elderly patients dose adjustment is not required. Patients with mild liver failure (5-6 points on the Child-Pugh scale) do not require dose adjustment. It is not recommended to prescribe the drug to patients with moderate (7–9 points on the Child-Pugh scale) or severe (more than 9 points on the Child-Pugh scale) liver failure. Patients with renal insufficiency of mild to moderate severity do not require dose adjustment. In case of severe renal failure (QC less than 30 ml / min), the drug in a dose of more than 10/10 mg / day should be used with caution. When used in combination with other drugs, Inegy should be taken at least 2 hours before or 4 hours after taking bile acid sequestrants. For patients receiving nicotinic acid in a dose of more than 1 g / day, cyclosporine or danazol, the maximum dose of Inegy is 10/10 mg / day. For patients receiving amiodarone or verapamil, the maximum dose of Inegy is 10/20 mg / day.
Side effects
The safety of the drug Inegy has been studied in clinical studies involving more than 3,800 patients and during post-marketing surveillance in different countries. In general, Inegy is well tolerated by patients. The side effects of taking Inegy are comparable to the side effects previously reported when taking ezetimibe and / or simvastatin. According to placebo-controlled studies and in the period of post-marketing follow-up in patients who took Inedzhi, the following characteristic side effects were noted with a frequency of less than 1/100 and less than 1/10, both with and without a well-established connection: From the digestive system : flatulence, abdominal pain, constipation, diarrhea, dyspepsia, vomiting, cholelithiasis, cholecystitis, jaundice, hepatitis. rarely (> 1/10 000, less than 1/1000) - nausea. very rarely (less than 1/1 000) - pancreatitis. in some cases - liver failure. According to controlled combined clinical studies, a clinically significant increase in serum transaminases (ALT and / or ACT 3 times or more) was observed in 1.7% of patients who received Inegy (these changes were asymptomatic, did not lead to cholestasis and passed on their own when discontinuing or continuation of treatment). From the hematopoietic system: thrombocytopenia, anemia. From the musculoskeletal system: myalgia, arthralgia. very rarely - myopathy / rhabdomyolysis. From the side of the central nervous system: dizziness, headache. Allergic reactions: rarely (> 1/10 000, less than 1/1000) - skin rash and urticaria. very rarely (less than 1/10 000) - anaphylactic reactions and angioedema. Other: fatigue, asthenia. In 0.2% of patients who received Inegy, there was a clinically significant increase in CPK (10 times or more VGN).
special instructions
The safety of the drug Inegy has been studied in clinical studies involving more than 3,800 patients and during post-marketing surveillance in different countries. In general, Inegy is well tolerated by patients. The side effects of taking Inegy are comparable to the side effects previously reported when taking ezetimibe and / or simvastatin. According to placebo-controlled studies and in the period of post-marketing follow-up in patients who took Inedzhi, the following characteristic side effects with a frequency of> 1/100 and less than 1/10 were noted, as associated with taking the drug,and without a clearly established connection: On the part of the digestive system: flatulence, abdominal pain, constipation, diarrhea, dyspepsia, vomiting, cholelithiasis, cholecystitis, jaundice, hepatitis. rarely (> 1/10 000, less than 1/1000) - nausea. very rarely (less than 1/1 000) - pancreatitis. in some cases - liver failure. According to controlled combined clinical studies, a clinically significant increase in serum transaminases (ALT and / or ACT 3 times or more) was observed in 1.7% of patients who received Inegy (these changes were asymptomatic, did not lead to cholestasis and passed on their own when discontinuing or continuation of treatment). From the hematopoietic system: thrombocytopenia, anemia. From the musculoskeletal system: myalgia, arthralgia. very rarely - myopathy / rhabdomyolysis. From the side of the central nervous system: dizziness, headache. Allergic reactions: rarely (> 1/10 000, less than 1/1000) - skin rash and urticaria. very rarely (less than 1/10 000) - anaphylactic reactions and angioedema. Other: fatigue, asthenia. In 0.2% of patients who received Inegy, there was a clinically significant increase in CPK (10 times or more VGN).