Rosuvastatin Tablets 10mg
MECHANISM OF ACTION:
Rosuvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol. Rosuvastatin produces its lipid-modifying effect in two ways; it increases the number of hepatic LDL receptors on the cell-surface, enhancing uptake and catabolism of LDL and it inhibits the hepatic synthesis of VLDL, thereby reducing the total number of VLDL and LDL particles. High density lipoprotein (HDL) is involved in transport of cholesterol from tissues back to the liver (reverse cholesterol transport).
Summary of clinical studies: FILROXY® reduces elevated LDL- cholesterol, total cholesterol, and triglycerides and increases HDL-cholesterol. A therapeutic response to FILROXY® is evident within one week of commencing therapy and 90% of maximum response in usually achieved in 2 weeks. The maximum response is usually achieved in four weeks and is maintained after that.
The mechanism of action of Rosuvastatin is similar to that of other statins. Its approximate elimination half life is 19 h and its time to peak plasma concentration is reached in 3–5 h following oral administration. Putative beneficial effects of Rosuvastatin therapy on chronic heart failure may be negated by increases in collagen turnover markers as well as a reduction in plasma coenzyme Q10 (CoQ10) levels in patients with chronic heart failure.
It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease.
Hyperlipidemia and Mixed Dyslipidemia
FILROXY(R) is indicated as adjunctive therapy to diet to reduce elevated Total-C, LDL-C, ApoB, non HDL-C, and triglycerides (TG) levels and to increase HDL-C in adult patients with primary hyperlipidemia or mixed dyslipidemia. Lipid altering agents should be used in addition to a diet restricted in saturated fat and cholesterol when response to diet and non pharmacological interventions alone has been inadequate.
Pediatric Patients 10 to 17 years of age with Heterozygous Familial Hypercholesterolemia (HeFH)
Adjunct to diet to reduce Total-C, LDL-C and ApoB levels in adolescent boys and girls, who are at least one year post menarche, 10-17 years of age with heterozygous familial hypercholesterolemia if after an adequate trial of diet therapy the following findings are present: LDL-C > 190 mg/dL or > 160 mg/dL and there is a positive family history of premature cardiovascular disease (CVD) or two or more other CVD risk factors.
FILROXY(R) is indicated as adjunctive therapy to diet for the treatment of adult patients with hypertriglyceridemia.
Primary Dysbetalipoproteinemia (Type III Hyperlipoproteinemia)
FILROXY(R) is indicated as an adjunct to diet for the treatment of patients with primary dysbetalipoproteinemia (Type III Hyperlipoproteinemia).
Homozygous Familial Hypercholesterolemia (HoFH)
FILROXY(R) is indicated as adjunctive therapy to other lipid lowering treatments (e.g., LDL apheresis) or alone if such treatments are unavailable to reduce LDL-C, Total-C, and ApoB in adult patients with homozygous familial hypercholesterolemia.
Slowing of the Progression of Atherosclerosis
FILROXY(R) is indicated as adjunctive therapy to diet to slow the progression of atherosclerosis in adult patients as part of a treatment strategy to lower Total-C and LDL-C to target levels.
Primary Prevention of Cardiovascular Disease
In individuals without clinically evident coronary heart disease but with an increased risk of cardiovascular disease based on age ≥ 50 years old in men and ≥ 60 years old in women, hsCRP ≥ 2 mg/L, and the presence of at least one additional cardiovascular disease risk factor such as hypertension, low HDL-C, smoking, or a family history of premature coronary heart disease, FILROXY(R) is indicated to:
- reduce the risk of stroke
- reduce the risk of myocardial infarction
- reduce the risk of arterial revascularization procedures
Limitations of Use
FILROXY(R) has not been studied in Fredrickson Type I and V dyslipidemias.
FILROXY® is contra-indicated in:
- Patients with hypersensitivity to any component of this product
- Patients with active liver disease or with unexplained persistent elevations of serum transaminases
- Patients receiving concomitant cyclosporine
- Patients with myopathy
- Children as safety and efficacy have not been demonstrated
Safety in pregnancy and lactation has not been established.
DOSAGE AND ADMINISTRATION
General Dosing Information
Before treatment initiation, the patient should be placed on a standard cholesterol-lowering diet that should continue during treatment.
FILROXY(R) can be administered as a single dose at any time of day, with or without food.
The dose range for FILROXY(R) is 5 to 40 mg orally once daily (Max: 40 mg/day). The usual starting dose is 10-20 mg.
When initiating FILROXY(R) therapy or switching from another HMG-CoA reductase inhibitor therapy, the appropriate FILROXY(R) starting dose should first be utilized, and only then titrated according to the patient’s response and individualized goal of therapy.
After initiation or upon titration of FILROXY(R), lipid levels should be analyzed within 2 to 4 weeks and the dosage adjusted accordingly.
The 40 mg dose of FILROXY(R) should be used only for those patients who have not achieved their LDL-C goal utilizing the 20 mg dose.
ADVERSE REACTIONS/SIDE EFFECTS:
Rosuvastatin is generally well tolerated. The most frequent adverse events thought to be related to rosuvastatin were myalgia, constipation, asthenia, abdominal pain, and nausea.
The adverse events with rosuvastatin are generally mild and transient. In controlled clinical trials less than 4% of rosuvastatin treated patients are withdrawn due to adverse events. The incidence of adverse drug reactions tends to increase with increasing dose.
Skeletal muscle effects: Rhabdomyolosis, which impairment of renal function, has been reported with Rosuvastatin.
Renal effects: Proteinuria
Known symptoms of overdosage and particular of its treatment: There is no specific treatment in the event of overdosage. In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Haemodialysis is unlikely to be of benefit.
WARNINGS AND PRECAUTIONS:
It is recommended that liver function tests be performed before and at 12 weeks following both the initiation of therapy and any elevation of dose, and periodically (e.g., semiannually) thereafter
PREGNANCY AND LACTATION:
The safety of FILROXY® during pregnancy and whilst breastfeeding has not been established.
Store in a cool, dry place at a temperature not exceeding 30°c.
PRESENTATION: 3 x 10 Tablets Alu Alu Pack