Rosulip film-coated pills 10 mg N28
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Description
Rosulip pills - a drug to reduce the concentration of cholesterol in atherosclerosis and other cardiovascular diseases. Rosulin treatment does not give an immediate effect - its effect becomes noticeable by the end of the first week of use, and the maximum effect is achieved by the end of the first month of therapy.
Active ingredients
Rosuvastatin
Release form
Pills
Composition
Rosuvastatin zinc, ludipress (lactose monohydrate), povidone, crospovidone, magnesium stearate, Shell film: Opadry II white 85F 18422 (polyvinyl alcohol, titanium dioxide, macrogol 3350, talc).
Pharmacological effect
Selective and competitive inhibitor of HMG-CoA reductase - an enzyme that catalyzes the conversion of HMG-CoA to mevalonate, which is a precursor of cholesterol (Xc). Rosuvastatin increases the number of LDL receptors on the surface of liver cells, thereby enhancing the absorption and catabolism of LDL, and also suppresses the synthesis of VLDLP in the liver. As a result, the total number of particles of VLDL and LDL is reduced. It reduces the increased concentration of Xc-LDL, total Xc and triglycerides, and also increases the concentration of Xc-HDL. In addition, rosuvastatin reduces the concentration of apolipoprotein B (ApoB), Xc-non-LPVP, Xc-VLDL, triglycerides of VLDL (TG-VLDL) and increases the content of apolipoprotein AI (ApoA-I). Also, rosuvastatin reduces the ratio of Xc-LDL / Xc-HDL, total Xc / Xc-HDL, Xc-non-LPVP / Xc-HDL and ApoB / ApoA I. The therapeutic effect is manifested within one week after the start of treatment. For 2 weeks of therapy, the efficiency reaches 90% of the maximum possible. The maximum therapeutic effect is usually achieved by the 4th week of therapy and is maintained with regular intake.
Pharmacokinetics
Cmax of rosuvastatin in plasma is reached approximately 5 hours after ingestion. The absolute bioavailability of the drug is about 20%. Rosuvastatin undergoes limited metabolism (about 10%) in the liver. More than 90% of the pharmacological activity on inhibition of circulating HMG-CoA reductase is provided by rosuvastatin, the rest is provided by its metabolites. Approximately 90% of the dose of rosuvastatin is excreted unchanged through the intestines. Approximately 5% of the dose is excreted by the kidneys unchanged.T1 / 2 of the drug from blood plasma is approximately 19 hours and does not change with increasing dose of the drug. Rosuvastatin plasma clearance reaches an average of 50 l / h (coefficient of variation - 21.7%).
Indications
- Primary hypercholesterolemia (type On according to Fredriksen, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type Ib) as a supplement to the diet when diet and other non-drug therapies (such as exercise, weight loss) prove to be insufficient. hypercholesterolemia as an adjunct to diet and other treatment methods aimed at reducing the level of lipids in the blood (for example, LDL apheresis), as well as in cases where these methods are deficient internally effective. Hypertriglyceridemia (type IV according to Fredrikson) as a supplement to the diet. - To slow the progression of atherosclerosis as a supplement to the diet in patients, including those who have shown therapy to reduce the level of total Xc and LDL-C.
Contraindications
Hypersensitivity to rosuvastatin and other components of the drug, liver disease in the active phase, including a persistent increase in serum transaminase activity or an increase in serum transaminase activity by more than 3 times compared to VGN, severe renal impairment (Cl creatinine less than 30 ml / min ), myopathy, concomitant use of cyclosporine, susceptibility to the development of myotoxic complications, lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose ).
Use during pregnancy and lactation
Contraindicated
Dosage and administration
Inside, do not chew or crush the pill, swallow whole, washed down with water. Can be taken at any time of the day, regardless of the meal. Before treatment, the patient should be prescribed a standard diet with a low content of Xc for the entire period of therapy. The dose of the drug should be selected individually, depending on the indications and therapeutic response to treatment, taking into account the current recommendations on target lipid levels.
Side effects
Headache, dizziness, constipation, nausea, abdominal pain, myalgia, asthenic syndrome.
Overdose
Treatment: there is no specific antidote.It is recommended to carry out symptomatic therapy and activities aimed at maintaining the functions of vital organs and systems. Monitoring of liver function and serum CK level is necessary. The effectiveness of hemodialysis is unlikely.
Interaction with other drugs
With the simultaneous use of rosuvastatin and cyclosporine, AUC of rosuvastatin is on average 7 times higher than the value observed in healthy volunteers. The combined use leads to an increase in plasma concentration of rosuvastatin 11 times, while the plasma concentration of cyclosporin does not change. The combined use of rosuvastatin and gemfibrozil leads to a 2-fold increase in C max in plasma and AUC of rosuvastatin. Perhaps FDV. Gemfibrozil, other fibrates and nicotinic acid in lipid-lowering doses (more than 1 g / day) increased the risk of myopathy while being used with other HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy and when used as monotherapy. At the same time taking the drug with gemfibrozil, fibrates, nicotinic acid in lipid-lowering doses (more than 1 g / day), an initial dose of 5 mg is recommended for patients. Rosuvastatin therapy at a dose of 40 mg is contraindicated with the concomitant use of fibrates. Joint administration of protease inhibitors can lead to a significant increase in the exposure of rosuvastatin. A pharmacokinetic study on the simultaneous use of 20 mg of rosuvastatin with a combination preparation containing two protease inhibitors (400 mg of lopinavir / 100 mg of ritonavir) in healthy volunteers resulted in an approximately twofold and fivefold increase in AUC0-24 and Cmax of rosuvastatin, respectively. Therefore, simultaneous administration of rosuvastatin and protease inhibitors in the treatment of patients with HIV is not recommended. Simultaneous use of rosuvastatin and suspensions of antacids containing aluminum and magnesium hydroxide, reduces the plasma concentration of rosuvastatin by about 50%. This effect is less pronounced if the antacid suspension is applied 2 hours after taking rosuvastatin. The simultaneous use of rosuvastatin and erythromycin leads to a decrease in AUC of rosuvastatin by 20% and Cmax of rosuvastatin by 30%, probably as a result of increased motility of the intestine caused by taking erythromycin.
special instructions
After 2–4 weeks of therapy and / or with an increase in the dose of Rosulip, control of lipid metabolism indices is necessary, and dose adjustment is necessary if necessary.