1. Description:
Rosuva (Rosuvastatin calcium) is a synthetic lipid-lowering agent. Rosuvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase.
This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.
2. Composition:
Rosuva Tablets for oral administration contain: 5, 10, 20, or 40 mg of Rosuvastatin.
3. Indications and usage:
Rosuva is indicated:
§ as an adjunct to diet to reduce elevated total-C, LDL-C, ApoB, nonHDL-C, and TG levels and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (Fredrickson Type IIa and IIb).
§ as an adjunct to diet for the treatment of patients with elevated serum TG levels (Fredrickson Type IV);
§ to reduce LDL-C, total-C, and ApoB in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments or if such treatments are unavailable.
4. Contraindicatios:
Rosuva is contraindicated in patients with a known hypersensitivity to any component of this product.
Rosuva is contraindicated in patients with active liver disease or with unexplained persistent elevations of serum transaminases (see WARNINGS, Liver Enzymes).
Pregnancy and Lactation:
Rosuva may cause fetal harm when administered to a pregnant woman.
It is contraindicated in women who are or may become pregnant..
Also in nursing mothers, since it pass through milk breast to the newborn, so a decision of stopping the lactation should be taken from the doctor.
Rosuva should be administered to women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards.
5. Warnings:
Liver Enzymes:
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.
Liver enzyme changes generally occur in the first 3 months of treatment with rosuvastatin.
Patients who develop increased transaminase levels should be monitored until the abnormalities have resolved.
Rosuvastatin should be used with caution in patients who consume substantial quantities of alcohol and/or have a history of liver disease .
Myopathy/Rhabdomyolysis:
Rosuva should be prescribed with caution in patients with predisposing factors for Myopathy such as renal impairment advanced age, and hypothyroidism and are not be treated adequate.
Rosuva therapy should be discontinued if markedly elevated CK levels occur or Myopathy is diagnosed or suspected.
The risk of Myopathy during treatment with Rosuva may be increased with concurrent administration of other lipid –lowering therapies.
The risk of Myopathy during treatment with Rosuva may be increased in circumstances which increase Rosuvastatin drug levels.
Rosuva therapy should also be temporarily withheld in any patient with an acute, serious condition suggestive of Myopathy or predisposing to the development of renal failure secondary to Rhabdomyolysis.
Precautions:
General:
Before instituting therapy with Rosuvastatin, an attempt should be made to control hypercholesterolemia with appropriate diet and exercise, for weight reduction in obese patients, and treatment of underlying medical problems.
Administration of Rosuvastatin 20 mg to patients with severe renal impairment (CLcr<30 mL/min/1.73 m2) resulted in a 3-fold increase in plasma concentrations of rosuvastatin compared with healthy volunteers .
6. Information for Patients:
Patients should be advised to report promptly unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever.
When taking Rosuvastatin with aluminum and magnesium hydroxide combination antacid, the antacid should be taken at least 2 hours after Rosuvastatin administration .
A dose reduction should be considered for patients on Rosuvastatin 40 mg therapy with unexplained persistent proteinuria during routine urinalysis testing.
7. Drug-Drug Interactions:
Cyclosporine+ Rosuvastatin = No significant change in plasma concentrations of Cyclosporine, but Cmax and AUC of Rosuvastatin increased 11 and 7 foldspecial consideration in the dosing of Rosuvastatin to patients taking concomitant Cyclosporine .
Warfarin+ Rosuvastatin = Clinically significant rises in INR(>4, baseline 2-3),but No change in plasma concentrations of Warfarin.
Gemfibrozil+ Rosuvastatin = 90% and 120% increase for AUC and Cmax of Rosuvastatin respectively compared with health volunteers.
This increase is considered to be clinically significant.
Antacid+ Rosuvastatin =Decrease in plasma concentrations of Rosuvastatin
Oral contraceptives + Rosuvastatin = Increase in plasma concentrations of ethinyl estradiol and norgestrol.
8. Adverse reactions:
Rosuvastatin is generally well tolerated.
Adverse reactions have usually been mild and transient, due to adverse reaction of Rosuvastatin.
The most frequent adverse events thought to be related to Rosuvastatin were myalgia, constipation, asthenia, abdominal pain, and nausea.
9. Overdosage:
There is no specific treatment in the event of overdose. In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Hemodialysis does not significantly enhance clearance of rosuvastatin.
10. Dosage and administration:
The patient should be placed on a standard cholesterol-lowering diet before receiving Rosuva and should continue on this diet during treatment.
Rosuva can be administered as a single dose at any time of day, with or without food.
§ Hypercholesterolemia (Heterozygous Familial and Nonfamilial)and Mixed Dyslipidemia (Fredrickson Type lla and lib):
The dose range for Rosuva is 5 to 40 mg once daily.
Therapy with Rosuva should be individualized according to goal of therapy and response.
The usual recommended starting dose of Rosuva is 10 mg once daily.
Initiation of therapy with 5 mg once daily may be considered for patients requiring less aggressive LDL-C reductions or who have predisposing factors for myopathy.
For patients with marked hypercholesterolemia (LDL-C > 190mg/dL) and aggressive lipid targets, a 20-mg starting dose may be considered.
After initiation and/or upon titration of Rosuva, lipid levels should be analyzed within 2 to 4 weeks and dosage adjusted accordingly.
§ Homozygous Familial Hypercholesterolemia:
The recommended starting dose of Rosuva is 20 mg once daily in those patients.
The maximum recommended daily dose is 40 mg.
Rosuva should be used in these patients as an adjunct to other lipid-lowering treatments or if such treatments are unavailable.
Response to therapy should be estimated from pre-apheresis LDL-C levels.
§ Patients Taking Cyclosporine:
In patients taking cyclosporine, therapy should be limited to Rosuva 5 mg once daily .
§ Concomitant Lipid-Lowering Therapy
The effect of Rosuva on LDL-C and total-C may be enhanced when used in combination with a bile acid binding resin.
If Rosuva is used in combination with gemfibrozil, the dose of Rosuva should be limited to 10 mg once daily .
§ Dosage in Patients With Renal Insufficiency:
No modification of dosage is necessary for patients with mild to moderate renal insufficiency.
For patients with severe renal impairment (CLcr<30 mL/min/1.73 m2) not on hemodialysis, dosing of Rosuva should be started at 5 mg once daily and not to exceed 10 mg once daily.
11. Package:
Packs of 30 Tablets.