Statinox

Statinox

rosuvastatin

Manufacturer:

Mepro Pharma

Distributor:

Royal Distribution

Marketer:

ESTI Pharma
Full Prescribing Info
Contents
Rosuvastatin.
Description
Each film coated tablet contains: Rosuvastatin calcium equivalent to Rosuvastatin 5 or 10 mg.
Rosuvastatin is a synthetic lipid-lowering agent, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Rosuvastatin calcium is a white amorphous powder that is sparingly soluble in water and methanol, and slightly soluble in ethanol.
Action
Pharmacology: Pharmacodynamics: Mechanism of action: Rosuvastatin is a selective and 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 effects in two ways. First, it increases the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL. Second, rosuvastatin inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.
Rosuvastatin reduces total cholesterol (total-C), LDL-C, ApoB, and nonHDL-C (total cholesterol minus HDL-C) in patients with homozygous and heterozygous familial hypercholesterolemia (FH), nonfamilial forms of hypercholesterolemia, and mixed dyslipidemia.
Pharmacokinetics: Absorption: In clinical pharmacology studies in man, peak plasma concentrations of rosuvastatin were reached 3 to 5 hours following oral dosing.
The absolute bioavailability of rosuvastatin is approximately 20%.
The major metabolite is N-desmethyl rosuvastatin, which is formed principally by cytochrome P450 2C9. Overall, greater than 90% of active plasma HMG-CoA reductase inhibitory activity is accounted for by rosuvastatin.
Indications/Uses
As an adjunct to diet to reduce elevated total-C, LDL-C, ApoB, non HDL-C, and TG levels and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia.
As an adjunct to diet for the treatment of patients with elevated serum TG levels.
To reduce LDL-C, total-C, and ApoB in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis).
Dosage/Direction for Use
The patient should be on a Standard Cholesterol lowering diet before starting treatment with STATINOX and should continue this diet during the course of treatment.
STATINOX can be given as a single dose with or without food at any time of the day.
Dosage in Asian Patients: Initiation of treatment with STATINOX 5 mg once daily should be considered in Asian patients. The potential for increased systemic exposures relative to Caucasians is relevant when considering dose escalation in cases where Hypercholesterolemia is not adequately controlled at doses of 5, 10 or 20 mg once daily.
Dosage in Patients Taking Cyclosporin: Treatment should be limited to STATINOX 5 mg once daily in patients on Cyclosporine.
Concomitant Lipid Lowering Therapy: STATINOX should be limited to 10 mg once daily if used in combination with Gemfibrozil as the effects on LDL-C and total-C may be enhanced.
Dosage in Patients with Renal Insufficiency: Modification of dosage is not required in patients with Mild to Moderate Renal Insufficiency while in patients with severe impairment of Renal Function and not on hemodialysis, STATINOX should be started at 5 mg once daily and should not exceed 10 mg once daily.
Contraindications
Rosuvastatin is contraindicated in patients with a known hypersensitivity to any component of this product as well as in patients with active liver disease or with unexplained persistent elevations of serum transaminases. Rosuvastatin is contraindicated in women who are or may become pregnant.
Warnings
It is recommended that liver function tests be performed regularly to check aminotransferase levels during the treatment.
Myopathy/Rhabdomyolysis: Rare cases of rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with rosuvastatin. Uncomplicated myalgia has been reported in rosuvastatin-treated patients. The incidence of myopathy increased at doses above the recommended dosage range.
Information for Patients: Patients should be advised to report promptly unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever.
Adverse Reactions
Rosuvastatin is generally well tolerated. The most frequent adverse events have been mild and transient. Following adverse events were reported, regardless of causality assessment in 81% of 10,275 patients treated with rosuvastatin in clinical studies.
Body as a Whole: Abdominal pain, accidental injury, chest pain, infection, pain, pelvic pain, and neck pain.
Cardiovascular System: Hypertension, angina pectoris, vasodilatation, and palpitation.
Digestive System: Constipation, gastroenteritis, vomiting, flatulence, periodontal abscess, and gastritis.
Endocrine: Diabetes mellitus.
Hemic and Lymphatic System: Anemia and ecchymosis.
Metabolic and Nutritional Disorders: Peripheral oedema.
Musculoskeletal System: Arthritis, arthralgia, and pathological fracture.
Nervous System: Dizziness, insomnia, hypertonia, paresthesia, depression, anxiety, vertigo and neuralgia.
Respiratory System: Bronchitis, cough increased, dyspnea, pneumonia, and asthma.
Skin and Appendages: Rash and pruritus.
Drug Interactions
Rosuvastatin mean Cmax and AUC were increased 11-fold and 7-fold, respectively, compared with healthy volunteers when co-administered with Cyclosporine. Rosuvastatin therapy has not been associated with bleeding or with changes in INR in patients not taking anticoagulants. Rosuvastatin clearance is not dependent on metabolism by Cyp.4503A4.
Warfarin: Coadministration of warfarin (20 mg) with rosuvastatin (40 mg) did not change warfarin plasma concentrations but increased the International Normalized ratio (INR).
Gemfibrozil: Coadministration of gemfibrozil (600 mg twice daily for 7 days) with rosuvastatin (80 mg) resulted in a 90% and 120% increase for AUC and Cmax of rosuvastatin, respectively. This increase is considered to be clinically significant.
Oral Contraceptives: Coadministration of oral contraceptives (ethinyl estradiol and norgestrel) with rosuvastatin resulted in an increase in plasma concentrations of ethinyl estradiol and norgestrel by 26% and 34% respectively.
Storage
Store below 25°C in a dry place. Protect from light.
ATC Classification
C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Presentation/Packing
FC tab 5 mg x 10's. 10 mg x 10's.
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